Med Chem Final Spring 2011

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Med Chem Final Spring 2011
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  1. Carisoprodol- Soma
    MOA: Congener of meprobamate- central sedative properties and spinal cord block of intraneuronal activity

    Occasional idosyncratic reaction including allergy

    Cenrally-acting agent
  2. Diazepam- Valium
    MOA: enhances spinal cord brain stem GABA-mediated presynaptic inhibition resulting in muscle relaxtion

    Centrally-acting agents
  3. Cyclobenzaprine HCl- Flexeril
    MOA: Acts centrally at the brain stem level on descending serotonergic pathways to reduced tonic motor activity, No peripheral effects on skeletal muscle fibers or neuromuscular junction.

    Ineffective in spasm due to CNS disease

    Similar structurally to TCAs
  4. Gabapentin - Neurontin
    MOA: Unknown- structurally related to GABA but NOT GABA agonist

    Recently used for management of postherpetic neuralgia (intense burning/tearing pain)

    No hepatic induction or inhibition

    Dosage is function of Crcl
  5. Lamotrigine - Lamictal
    MOA: unknown details but appears to modulate sodium channels

    Warnings: Serious rashes including Stevens-Johnson syndrome, not recommended during lactation, photosensitization possible
  6. Hydrocodone/APAP - Vicodin
    Less effective as analgesic and less respiratory depression than morphine

    Full agonist at the mu receptor

    Opiate agonists- Phenathrenes: Semi-Synthetic agents
  7. Propoxyphene-N/APAP- Darvon-N, Darvocet
    Discontinued November 19 2010 due to risk of caridac toxicity

    DO NOT use in patients that are suicidal or addiction prone, patients using other tranquilizer or antidepressant medication, do not use with alcohol- one of the major cuases of drug related deaths.
  8. Tramadol HCl- Ultram
    MOA: binds to mu receptors and prevents reuptake of norepinephrine and serotonin in the CNS

    Non-schedule agent with narcotic agonist (Opioid) activity

    Modify dose interval if Crcl is <30
  9. Sumatriptan - Imitrex
    5-HT1 Receptor Agonist

    Nasal spray is one spray per nostril (5mg) 20 mg dose has higher side effects, do not increase with MD consultation
  10. Metoclopramide - Reglan
    Antidopaminergic agents - Non-Phenothiazine agent

    If extrapyramidal symptoms occur administer 50 mg diaphenhydramine IM.

    Off-label use: stimulates production of lactation
  11. Ondansetrion HCl - Zofran
    Seretonin 5-HT3 receptor antagonist

    N/V: unlabled N/V due to APAP poisoning, tx of acute levodopa-induced vidual hallucinations, prostacyclin induced N/V, reduction in bulimic episodes in bulimia, social anziety disorders, spinal or epidural morphine-induced pruritus.
  12. Alprazolam - Xanax
    • Benzodiazepine
    • Intermediate acting

    Indications: anxiety, PMS, panic disorder with or without agoraphobia, depression
  13. Benzodiazepine
    Many drug interactions

    No well documented fatal overdosage due to oral use without multiple drug ingestions

    • Patient Information:
    • Take with food or water if stomach upset occurs
    • Do not discontinue use abruptly if long term use has occured
    • Do not take concurrently with antacids due to decreased rate of absorption
    • Avoid alcohol or other CNS depressants
    • May cause drowsiness-use caution
  14. Lorazepam - Ativan
    Benzodiazepine

    Intermediate acting

    Indications: anxiety, parenteral for preanesthetic use, status epilepticus, chemotherapy induced N/V, acute alcohol withdrawl, psychogenic cataonia, chronic insomnia
  15. Buspirone HCl - BuSpar
    MOA: unknown has affinity for seretonin 5-HT1A (partial agonist) and D2-dopamine receptors, but has NO anticonvulsant activity nor muscle relaxant properties.

    Indications: management of anxiety diorders, PMS

    Often takes 3-4 weeks to see results

    Oxidative liver metabolism with active metabolites
  16. Hydroxyzine - Atarax, Vistaril
    MOA: subcortical area CNS-depressant, a rapid acting true ataraxic (calmative)

    Indications: anxiety and tension, prior to dental procedures, acute emotional problems, alcoholism, allergic conditions with emotional overlap, anxiety caused by heart disease, pruritus, parenteral antiemetic and adjunct analgesia
  17. Amitriptyline - Elavil
    TCA's: Tertiary Amines

    Depression: tablets and injections

    Inhibit NE and 5-HT reuptake: 5-HT Selective

    Many side effects: seizures, sedation, hypotension, weight gain, sexual effects
  18. Nortiptyline - Pamelor, Aventyl
    TCA: Secondary amine

    Depressioin: not recommended for children

    Moderate NE and high serotonin uptake blocking activity and moderate anticholinergic effects

    Slight orthostatic hypotension
  19. Buproprion - Wellbutrin
    MOA: related to phenethylamines and mechanims is a reuptake inhibitor of NE and dopamine

    • Indications:
    • Depression and smoking Cessation

    Photosensitivity possible, associated with seizures and frequency increases with dosage, less sexual dysfunction, weight gain or sedation
  20. Venlafaxine - Effexor
    SNRI: Phenethylamine

    MOA: potent inhibiots of serotonin and NE reuptake

    Depression and GAD

    Photosensitivity possible, notify MD if a rash or hives or other allergic reactions occur.
  21. Fluoxetine - Prozac
    SSRI

    Obsessive-complusive disorder, depression, bulimia nervosa and other unlabeled use

    Half life 1-348 hours - takes 28 days to reach steady state
  22. Paroxetine HCl - Paxil
    SSRI

    Obessive compulsive disorder, depression, panic disorders, social anxiety disorders, and other unlabled uses

    Elderly or devilitated patients with severe renal or hepatic impairment-start as 10 mg/day but do NOt exceed 40 mg/day

    Use caution on withdrawl- may cause development of psychiatric problems such as severe behavioral symptoms
  23. Sertraline - Zoloft
    • SSRI
    • Obsessive compulsive disorder, depression, panic disorder, post traumatic stress disorder, and unlabeled uses.

    Half-life 26-104 hours - takes 7 days to reach steady state

    Hepatic metabolism
  24. Citalopram - Celexa
    • SSRI
    • S-enantiomer = Lexapro
    • Depression, panic disorders, social anxiety disorders, and other unlabeled uses

    Half-life 35 hours, takes 7 days to reach steady state

    Hepatic impairment- 20 mg/day. Use caution

    Claim to have favorable SE profile: no assocaiated weight gain, lower potential CYP450 drug interactions, insomnia, anxiety, agitation, nervousness and fatigue

    CI: concurrent use or within 14 days of discontinuation of MOAI; cisapride and fluvoxamine
  25. Escitalopram - Lexapro
    MOA: inhibition of CNS neuronal reuptake of serotonin (5-HT)- highly selective agent

    Enantiopure drug- Sentantiomer of Celexa- 100X more potent than the R-enantiomer

    10 mg recommended in hepatic impairment

    Metabolized by 3A4, 2C19, and modest inhibitory effect on 2D6
  26. Prochlorperazine - Compazine
    1st generation anti-psychotic

    Indications: psychotic disorders, anxiety, acute headache in the ER, commonly used antiemetic

    Moderate sedative effects, 7.5 times more potent than chlorpromazine
  27. Olanzapine - Zyprexa
    • 2nd generation anti-psychotic
    • Thienobenzodiazepine

    Indications: Schizophrenia, bipolar mania, dementia related Alzheimer's disease

    Dosing in debilitated patients: 5 mg to start with max of 20 mg/day

    Heavily sedating with less weight gain as a side effect
  28. Aripiprazole - Abilify
    2nd generation anti-psychotic agents

    MOA: partial agonist at D2 and 5-HT1A receptors and antagonistic activity at 5-HT2A receptors

    Orthostatic hypotension due to antagonistic activity at alpha 1 adrenergic receptors

    Primary metabolite is de-hydro-aripiprazole via 2D6 steady state reached in 14 days

    99% plasma protein bound- primarily albumin

    Can be taken with or without food
  29. Ziprasidoone - Geodan
    • 2nd generation anti-psychotic agent
    • Benzthiazole

    Indications: schizophrenia

    Initial dose 20 mg bid taken with food

    >80 mg not recommended due to dose dependent QT elongation

    No inhibition effect on CYP enzymes
  30. Pramiprexole - Mirapex
    Dopaminergic Agents

    MOA: direct agonist activity at the dopamine receptors in the striatum (D3 only)

    Indications: treatment of the signs and symptoms of idiopathic Parkinson's disease with or without levedopa/carbidopa

    Approved for restless leg syndrome
  31. Carbidopa - Lodosyn
    • Antiparkinsons agent
    • Indications: must be given concurrently with levodopa for parkinsons, carbon monoxide poisoning and maganese toxicity

    MOA: inhibits peripheral decarboxylase enzyme that is responsible for decarboxylation of levodopa to produce dopamine - inhibits the action of pyridoxine HCl (vitamin B6)

    Does not cross BBB

    High protein diets inhibit carbidopa absorption

    Do not administer to nursing mothers or use in children <18 years old

    Max daily dose of carbidopa should not exceed 200 mg per day

    Watch for blepharospam (eyelid spams) as a sign of excess dosage
  32. Carbidopa and Levodopa - Sinemet
    MOA: prodrug converted by central decarboxylase into dopamine in CNS following active transport across the BBB

    Peripheral blood dopamine is responsible for drug side effects: N/V, anorexia, dystonic movements, dry mouth, numbness, darkening of urine and sweat

    Use in extreme caution in: wide angle glaucoma, severe CV disease, or pts with suspected skin lesions or a hsitory of melanoma, do not use in lactating mothers or chidren <12 years, can interfere wtih urine tests for sugar or ketones

    CI: pts taking MAOI

    Watch for on-off phenomenon- try drug holiday, keep dosage as low as possible
  33. Donepexil HCl- Aricept
    MOA: Centrally acting reversible cholinesterase inhibitor

    Indications: mild to moderate Alzheimer's disease

    Dosage is adjusted based on serum transaminase leves
  34. Memantine HCl- Namenda
    MOA: Orally active N-methyl-D-aspartate (NMDA) uncompetitive open-channel antagonist--blocks the action of the neurotransmiter glutamate by binding to the NMDA receptor-operated cation channels.

    Indication: moderate to severe Alzheimer's disease- first drug for severe stage of disease

    Persistant activation of CNS NMDA receptors by glutamate

    Helps relieve symptoms only -- not curative-- low incidence of side effects

    Side effects observed-- dizziness, headache, constipation

    Anything acidifies urine will increase excretion.
  35. Zolpidem Tartrate - Ambien
    MOA: non-benzo modulation of the GABA-BZ receptor chloride channel macromoleculare complex

    No myorelaxant or anticonbulsant properties

    Indications: Short-term treatment of insomnia
  36. Temazepam- Restoril
    Benzodiazepine

    MOA: potentiates GABA neuronal inhibition by interacting with the GABA chloride ion channel receptor complex.

    Indication: Insomnia
  37. Phenobarbital
    • Barbiturate
    • MOA: Enhances GABA mediated chloride influx (GABA inhibition)

    Indications: Grand mal seizures in pediatric patients, status epilecticus

    Can cause CNS depression, drowsiness, and associated in decreased IQ in chronically treated children.

    Stimulates P450 enzymes
  38. Eszopiclone - Lunesta
    Non-barbiturate/Benzodiaxepine Hypnotic

    MOA: unknown, believed to result from GABA-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.

    Insomnia--difficulty falling asleep and staying asleep

    Looks safe for long term use - no loss of efficiancy
  39. Metaxalone - Skelaxin
    MOA: general CNS depression - no direct effect on muscle

    Indications: adjunct to rest, physical therapy and other measures for the relief of discomfort associated with acute, painful, musculoskeletal conditions.

    Use in caution with hepatic dsyfunction- conduct liver function tests

    Possible teratogen, inform patients to watch for signs of liver dysfunction
  40. Oxybutynin chloride - Ditropan XL
    MOA: inhibits muscarinic action of acetylcholine via direct anti-spasmotic effect on smooth muscle relaxing the bladder smooth muscle -primarily the R stereoisomer

    Indications: overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency

    Contraindicated in urinary retention, gastric retention or uncontrolled narrow-angle glaucoma
  41. Darifenacin - Enablex
    MOA: potently inhibits muscarinic action of acetylcholine via a direct antispasmotic effect on smooth muscle relaxing the bladder smooth muscle - very selective for the M3 muscurinic receptor over others

    Indictions: overaction bladder with symptoms of urge urinary incontinence urgency and frequency

    Contraindicated in urinary retntion, gastric retention or uncontrolled narrow angle glaucoma; No effect on QT elongation

    Most common side effects: dry mouth, constipation, blurred vison, heat prostration
  42. Solifenacin succinate- Vesicare
    MOA: inhibits muscarinic action of acetylcholine via a direct anti-spasmotic effect on smooth muscle relaxing the bladder smooth

    Indications: overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency

    Contraindicated in urinary retention, gastric retention or uncontrolled narrow angle glaucoma; appears to prolong QT interval as dosage is increased
  43. Tolterodine tartrate- Detrol
    MOA: competitive inhibitor of muscarinic action of acetylcholine on the bladder smooth muscle

    Indications: overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency

    Higly bound to alpha acid glycoprotein

    Dose dependent effect on QT elongation

    Contraindicated in urinary retention, fastric retention or uncontrolled narrow-angle glacoma
  44. Phenytoin Sodium- Dilantin
    MOA: produces a sustained depolarization by slowing the rate of voltage-activated Na channels-prevents hyperexitability

    Indications: tonic-clonic (grand mal), psychomotor, status epilepticus, cardiac arrhythmias

    Ineffective in absence seizures

    Use a single manufacturers product bioavailability issues

    Serum therapeutic level 5-20 micrograms/ml

    Chronic use toxicity includes gingival hyperplasia, hirsutism, and overdoseage is manifest by atazia, nystagmus, vertigo, blurred vision, confusion, lethargy, hallucination

    Many drug interactions inhibitio and induction

    Never IM
  45. Clonazepam - Klonopin
    • Benzodiazepines
    • Indications: petit mal, akinetic or myoclonic seizures alone or as an adjuct

    Therapeutic conc: 20-80 ng/ml

    Be aware of additive sedative effects
  46. Carbamazepine - Tegretol
    MOA: reduces polysynaptic responses and blocks post-tetanic potentials

    Indications: partial seizures, grand mal and mixed seizures, trigeminal neuralgia pain relief, psychiatric disorders, alcohol, cocaine, and benzo withdrawl

    Warning: aplastic anemia and agranulocytosis, blod dyscrasias and hypersensitivity reactions, stevenspjohnsons syndrome
  47. Oxcarbazepine - Trileptal
    MOA: reduction of the ketone to the hydroxy group is the pcol active compound which produces blockage of the voltage sensitive sodium channel

    Indications: monotherapy of adjunct use in adults and children 4-16 years of age suffering from partial seizures, atypical panic disorders

    Monitor for blood dyscrasias and hypersensitivity reactions, use ethanol cautiously due to additive sedation
  48. Pregabalin - Lyrica
    MOA: unknown mechanism except it binds to the alpha2-delta site (an auxiliary subunit of voltage-gate ca2 channels) in the CNS and appears to decrease the release of several neurotransmitters

    Structural analog of GABA but does NOT bind these receptors nor the benzo receptors

    Indications: neuropathic pain associated with postherpetic neuralgia, diabetic peripheral neuropathy, partial onset seizures in adults and the first drug approved for fibromyalgia
  49. Lamotrigine - Lamictal
    MOA: unknown details but appears to modulate sodium channels

    Indications: epilepsy as a sole therapy in adults and as adjucnt therapy in pediatric use (2 years and older)

    Warning: serious rashes including Stevens-Johnson syndrome

    Often confused with other medications due to similarity of names
  50. Valproic acid - Depakene, Depakote
    MOA: appears to increase levels of GABA

    Indications: Petit mal and mixed seizures with absence, grand mal, and myoclonic seizures; bipolar manic-deressive illness, migraine prophylaxis

    Warning: hepatotoxicity, teratogenic, pancreatitis

    Will interfer with urine ketone tests, >5 years decreased bone density in young children
  51. Topiramate - Topomax
    MOA: a sulfamate monosaccharide that exerts sodium channel blocking action, increases activity GABA at its receptor and antagonizes the effect of glutamate

    Indications: adjunct therapy for patrial onset seizures in adults/kids and Lennox-Gastaut (LGS) syndrome in children

    Dosage should be titrated as a fucntion of Crcl

    Maintain fluid intake due to stone formation
  52. Levetiracetam - Keppra
    MOA: unknown

    Indications: adjunct in partial onset seizures in adults

    Dosage must be individualized based on renal function

    Possible teratogen
  53. Varenicline tartrate - Chantix
    MOA: high affinity and partial agonist for the alpha4 beta 2 nicotinic acetylcholine receptor subtypes--simultaneously prevents nicotine binding. Although the drug binds and stimulates receptor mediated activity it is at a significantly lower level than nicotine. By competing with nicotine it blocks the stimulation of the central nervous mesolimbic dopamine system- blocks the reward reinforcement system

    Indications: aid to smoking cessation treatment-appears to be the most effective drug available to treat tobacco dependence

    Side effects: N/V, flatulence, insomnia, headache, abnormal dreams

    Black box warning: exacerbations of pre-existing psychiatric illness-- agitation, hostility, depressed mood, suicidal ideation and behavior possible
  54. Methotrexate - Rhumatrex
    MOA: inhibition of dihydrofolate reductase and thymidylate synthase--cell cycle specific agent? that inhibits DNA production

    Do not take with food, avoid alcohol, salicylates and sun exposure, USE contraception, inform MD of any signs of neutropenia, bleeding, shortness of breath, yellow skin

    Produces bone marrow depression, hepatotoxicity and death, diarrhea, lung disease not reversible, very nasty drug, inform patient of risks involved
  55. Duloxetine HCl- Cymbalta
    • SNRI
    • MOA: antidepressant and pain inhibitory actions related to its potentiation of serotonergic and noradrenergic actibity in the CNS.
    • -potent inhibitor of neuronal serotonin and NE reuptake and less potent inhibitor of dopamine reuptake

    Indications: 1. MDD- a major mood disorder characterized by one or more episodes of major depression with or without full recovery between episodes. 2. Fibromyalgia

    Unlabeled uses: stress, and urinary incontinence, diabetic peripheral neuropathy

    Duloxetine has no significantly affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opiod, glutamate, and y-aminobutyric (GABA) receptors in vitro. Duloxetine does not inhibit monoamine oxidase
  56. Eletriptan HBr - Relpax
    • Serotonin 5HT1b/5HT1D receptor agonist
    • Highly specific for certain 5-HT receptor subtypes with no affinity for adrenergic alpha or beta receptors, dopaminergic receptors, muscurinic or opiod receptors

    Not indicated for prophylaxis

    Contraindicated in patients with ischemic heart disease
  57. Rizatriptan Benzoate - Maxalt
    • Serotonin 5HT1 Receptor Agonist
    • Not intended for prophylactic therapy

    Dosing must be no more often than every two hours
  58. Meloxicam - Mobic
    • NSAID
    • Sulfonamide
  59. Naproxen - Aleve
    • NSAID
    • Aryl-and Heteroaryl propionic acid derivatives
  60. Ibuprofen - Motrin, Advil
    • NSAID
    • Aryl-and heteroarylpropioinic acid derivatives
  61. Celecoxib - Celebrex
    • NSAIDS
    • At therapeutic concentrations inhibition of COX-1 does not occur:
    • Advantageous when one does not want to inhibit COX-1: GI problems are apparently less due to continued COX-1 prostaglandin protection of the GI mucosa

    Use linked to increased risk of MI event rate
  62. Clonidine - Duraclon
    • Central analgesic agents
    • Agents that produce analgesia not mediated by opiate receptors but via other neruonal mechanisms

    MOA: produces analgesia at both presynaptic and postjunctional alpha 2 adrenoceptors in the spinal cord that are responsible for pain transmission to the brain

    Orally used as an anti-hypertensice agent, most off label uses of any drug

    For analgesic activity it is given via the epidural route. Use in combination with opiates when opiates alone are ineffective

    Not recommend for ostetrical, post-partum or peri-operative pain management
  63. Buprenorphine HCl and Naloxone HCl sublingual tablets - Suboxone
    To treat heroin and other opiate addiction: First dosage form approved that can be prescribed in a doctor's office rather than at a treatment clinic
  64. Fentanyl
    Opiod agonist- synthetic phenylpiperidines

    Sublimaze injection: analgesic action of short duration during anesthesia and in post-operative pain relief

    Transmucosal Lozenges: Oralet- pre-operative anesthesia, Actiq sugar free lozenge on a stick- breakthrough cancer pain only

    Transdermal patches: Duragesic 25-100 mcg/hr delivery serious and life threatening hypoventilation possible

    Transmucosal tablet: Fentora-breakthrough cancer pain only

    Buccal Soluble film: Onsolis- breatkthrough cancer pain only
  65. Hydromorphone
    • Opiate Agonists - phenanthrenes: semi synthetic agents
    • Full agonist at the mu receptor

    Eqipontent as an analgesic (relief of moderate/sever pain) and less constipating effect, equipotent respiratory depression

    Refrigerate suppositories
  66. Oxycodone - Oxycontin controlled release, Roxicodone immediate release and oral solution, percodan with APAP
    • Opiate agonist - phenanthrenes: Semi synthetic agents
    • Full agonist at the mu receptor

    Equipotent as morphine as an analgesic and cause of respiratory depression and constipation
  67. Diclofenac - Volarern ER, cataflam IR.
    combo with misoprostol -Arthrotec
    • NSAID
    • aryl and heteroarylacetic acid derivatives
    • Patch and gel
  68. Acetylsalicylic acid- Aspirin ASA
    • Salicylate
    • MOA: all analogs are hydrolyzed to salicylic acid

    Salicylic acid lowers body temp via vasodilation

    1. ASA is a potent inhibitor of prostaglandin synthase by acetylating primarly COX-1. Cyclooxygenase is the first enzyme in the prostaglandin synthesis pathway

    2. ASA and only aspirin: irreversible inhibitor of platelet aggregation (7-10 days) by preventing COX mediated synthesis of thromboxane A2 a mediator of platelet aggregation and a potent vasoconstrictor

    3. ASA in large doses inhibits COX in arterial walls preventing synthesis of prostacyclin (PGI2) - a potent inhibitor of platelet aggregation this is why low doses are best in anti platelet applications


    Lethal dose is 10-30 grams in an adult and 4 grams in children

    Chewable tablets, gum tablets, enteric coated tablets, extended release tablets, delayed release tablets, suppositories included buffered produces
  69. Modafinil - Provigil
    • 100 and 200tablets
    • MOA: unknown, although it has wakeful-promoting effectst similar to sympathomimetic agents, however, its pharmacological profile does not resemble thes agents

    Indications: narcolepsy- recurring episodes of sleep during the day and disrupted nocturnal sleep- genetic predisposition

    Moderate CYP induction and 2c19 inhibitor
  70. Lesdexamfetamide dimesylate - Vyvanse
    • A prodrug! That provides for once a day dosing with less abuse potential
    • 30, 50, 70 mg capsule
    • Can't shoot this drug IV b/c serum protease doesn't clip the amphetamine part
  71. Racemic amphetamine sulfate
    Dextroamphetamine sulfate - Dexedrine
    Mixture of various salts - Adderall
    • Amphetamines - A CNS stimulant
    • MOA: prevent reuptake of neurotransmitters NE and dopamine into the pre-synaptic neuron and increase the realse of these monamines into the extra-neuronal space- indirect agonist

    CNS effects: increased arousal and wakefulness mood alteration- increased confidence, ability to concentrate, exhilaration, euphoria; increased motar activity, anorexia, insomnia

    CV efffects: similar to sympathomimetic amines, CI in any CV abnormality

    Indications: ADHD

    Problems: addiction and tolerance, toxic psychosis with underlying undiagnosed psychosis, hypertension, angina, hyperthyroidism can be aggravated
  72. Methylphenidate - Ritalin, Concerta
    MOA: mild CNS stimulant similar to amphetamines but with an unknown mechanism

    Indications: ADHD, narcolepsy; unlabeled uses- treatment of depression in elderly, cancer and post stroke patients, post-anesthesia related hiccups

    Patient info: take last dose prior to 6 pm to avoid insomnia, do not crush or chew SR products
  73. Atomoxetine HCl - Strattera
    MOA: selective inhibitor of pre-synaptic NE transporter

    Indications: Attention Deficit/Hyperactivity Disorder in children and adults

    1st new drug and non stimulant to treat this disorder in 3 decades

    Not a schedule II or controlled substance

    CYP2D6 followed by glucuronidation-slower metabolism

    Patient info: can be taken with or without food, dosage adjustment necessary in moderate/severe hepatic insufficiency; dry mouth, insomnia, nausea, dizziness
  74. Morphine- Avinza
    • Opiate agonist- phenanthrenes: Natural products
    • Full mu receptor agonist

    Regular and controlled release tablets and capsules, solutions, injection and rectal suppositories

    Indications: analgesic activity, and as an anesthetic agent preoperative
  75. Diphenoxylate/Atropine - Lomotil
    • Combined with atropine to prevent shooting
    • Indicated in diarrhea

    MOA: slows GI motility, no analgesic activity

    Preferred in children 2-12 years old with the dose determined based on weight
  76. Methadone HCl - Dolophine and Methadose
    Opiod Agonist: Synthetic diphenlheptanes

    Indications: relief of severe pain (any pharmacy) detoxification and maintenance of narcotic addiction- ie Heroin (only approved pharmacies as oral dose form only) milder withdrawl effects and longer actin

    Not useful preoperatively to reduce anxiety or for induction
  77. Nabumetone- Relafen
    • NSAID
    • Aryl and heteroarylacetic acid derivatives
    • Prodrug
  78. Indomethacin- Indocin
    • NSAID
    • aryl and heteroarylacetic acid derivatives

    MOA: inhibits COX that is responsible for prostaglandidn synthesis

    Indications: to promote closure of significant patent ductus arteriosus in infants in which 48 hours of usual medical supportive treatment fails
  79. Quetiapine Fumarate - Seroquel
    • Dibensothiazepine: 2nd generation antipshychotic
    • Indications: psychotic disorders
    • Multiple neurotransmitter receptor antagonist: 5-HT, Dopamine, Histamine, H1 and alpha 1 and 2

    No anticholinergic side effects!! no binding to muscarinic receptors

    Moderately sedating, less weight gain is a side effect, increased heart issues when compared wih other atypicals
  80. Benztropine mesylate - Cogentin
    Anticholinergic Agents - usually less effective than levodopa

    Indications: idiopathic, postencephalitic, arterosclerotic and drug/chemical induced (neuroletpics) parkonsonims

    CI: children <3 years old
  81. Adapalene - Differin gel
    MOA: binds to specific retinoic acid nuclear receptors but not cytosolic receptor proteins - modulates cellular differentiation, keratinization and inflammatory processes

    Potential for teratogenicity - topical application studies unknown

    Combo with benzoyl peroxide- Epiduo
  82. Lantanoprost - Xalatan
    Agents used to treat glaucoma- Prostagladin analog

    MOA: opthalmic solutions that reduce intra-ocular pressure by increasing trabecular meshwork and uveoscleral outflow of aqueous humor

    Indications: reduction of intraocular pressure in open-end glaucoma if other medications have failed

    These drugs can cause permanent change in eye color

    Do not administer while wearing contact lens

    Eventual systemic systemic distribution and hepatic metabolism
  83. Bimatoprost - Lumigan
    Agents used to treat glaucoma- Prostagladin analog

    • MOA: opthalmic solutions that reduce intra-ocular pressure by increasing
    • trabecular meshwork and uveoscleral outflow of aqueous humor

    Indications: reduction of intraocular pressure in open-end glaucoma if other medications have failed

    These drugs can cause permanent change in eye color

    Do not administer while wearing contact lens

    Eventual systemic systemic distribution and hepatic metabolism
  84. Travoprost - Travatan
    Travoprost - Travatan Z does NOT contain benzalkonium chloride
    Agents used to treat glaucoma- Prostagladin analog

    • MOA: opthalmic solutions that reduce intra-ocular pressure by increasing
    • trabecular meshwork and uveoscleral outflow of aqueous humor

    Indications: reduction of intraocular pressure in open-end glaucoma if other medications have failed

    These drugs can cause permanent change in eye color

    Do not administer while wearing contact lens

    Eventual systemic systemic distribution and hepatic metabolism
  85. Olopatadine HCl - Pataday
    MOA: relatively selective dual H1-receptor antagonist and a inhibitor of histamine and other mediator release from mast cells by acting as a mast cell stabilzer- dual mechanism

    Indications: prevention of itching associated with allergic conjuctivitis

    No alpha adrenergic, dopaminergic or muscurinic type 1/2 receptor effects

    Important patient info: remove contact lenses prior to use and leave them out for 10 minutes following use-- soft lenses can absorb the benzalkonium chloride preservative
  86. Topical cyclosporine - restais
    MOA: unknown but beleved related to immunomodulating and anti-inflammatory properties

    Normally used as an immunosuppressants in organ transplantation
  87. Baclofen - Lioresal
    Centrally acting agent

    MOA: hyperpolarization of afferent nerve terminals and by binding to GABA receptors

    Indications: oral-spasticity due to MS, spinal cord injuries and diseases, intrathecal- management of sever spasticity of spinal cord origin when unresponsive to oral dosing-- can be used with constant infusion pump (do single dose testing first) this rout allows 100X decrease in dosing

    Elimination as the parent drug by urinary excretion, abrupt discontinuation may cause hallucinations, may cause painful urination
  88. Desvenlafaxine - Pristiq
    • SNRI
    • Main metabolite of venlafaxine

    Metabolized by 3A4

    Discontinuation can be more severe thatn SSRI's increased diastolic BP and more dangerous in overdosage situations
  89. Hydrochlorthiazide - Esidreix, hydroDiuril, oretic, ezide, microzide, hydro-par
    • Thiazide and thiazide-like related diuretics
    • Diuretics that act at the Distal convoluted tubule
  90. Spironolactone - Aldactone
    • Diuretics that act on collecting tubule
    • Potassium sparing agents- diuresis with no concomitant K loss

    MOA: competitive inhibitor of aldosterone (induces the synthesis of transport proteins including the Na/K/ATP ase carrier system protein and luminal channel protein sythesis) preventing Na reabsorption and K echange for Na -- sparing K. Overal preventing na reabsorption of 2-3% of the filtered NA

    SE: hyperkalemia and acidosis in cases of poor renal function, gynecomastia, breast tenderness, menstrual disturbances, GI disturbances, skin rashes

    Drug interactions: anticoagulants (antagonize), ACE inhibitors, potassium preparations (hyperkalemia), salicylates (antagonixes the diuretic effect)
  91. Triamterene - Dyrenium
    • Diuretic that acts on collecting tubule
    • Potassium sparing agents- diuresis with no concomitant K loss

    MOA: plugs the sodium channels preventing electrogenic reabsorption of 2-3% of the filtered NA

    Indications: secodnary hyperaldosteronism, edema from CHF and cirrhosis of the liver, ascites, nephrotic syndrome, hypokalemia

    SE: hyperkalemia, formation of renal stones, N/V, leg cramps, dizziness

    Do NOT use alone for hypertension treatment or in patients with renal impairment

    • Drug interactions: amantadine (increases plasma levels and apperance of toxicity), ACE inhibitors, potassium preperations (hyperkalemia), cimetidine (increase triamterene bioavailability, decreases hydroxylation and renal clearance)
    • Indomethacin- concurrent use has lead to acute renal failure
  92. Digoxin - Lanoxin, Lanoxicaps
    Isolated from plants like foxgloves flowers and some other common household and yard plants

    MOA: inhibition of the Na/K/ATP-ase pump located on the sarcolemma membrane of cardiac muscle. Makes more Ca available to the actin and mysoin resulting in an increase in the force of contraction

    Works best for low output failure: diuresis, alleviates symptoms of right sided failure (venous congestion, edema) and left side failure (dyspna, orthopnea, cardiac asthma)

    Narrow therapeutic range

    Pay attention to the dosage dispensed. Do not change dosage forms without monitoring plasma levels.

    Desired serum range: 0.5-2.2 ng per ml
  93. Amiodarone HCl- Cordarone, Paceroine
    Class III anti-arrhythmic agent

    MOA: block of cardiac potassium channels to prolong the repolarization phase

    Clearly demonstrated to decarease arrhythmia mortality in post-MI and heart failure patients

    t 1/2 = 45 days, possible accumulation

    Adverse effects: photosensitivity, blue-gray skin discoloration, hypo/hyperthyroidism, nightmares, corneal deposits, hepatotoxicity, pulmonary fibrosis;

    Monitor: liver, pulmonary and thyroid function, ophthalmic exams, chest roentgenograms

    DI: can cause increased levels of digoxin, flecainide, cyclosporine, phenytoin, quinidien, procainamide
  94. Sotalol HCl- Betapace
    Class III & II Anti-arrhythmic agents: Ethanolamine class

    MOA: beta blocker and K channel blocker

    Indications: suppression of ventricular arrhythmias

    AE: bradycardia, hypotension, exaverbation of heart failure, tordades de pointes

    Racemic mixture at hydroxy sterocenter-- the pure d enantiomer has been shown to increase mortality by 65%
  95. Verapamil
    • Phenylalkylamines
    • Inhibition of CA influx is the basis of anti-arrhythmic activity

    Does not bind in resting state but only after the channels is opened. Water soluble that diffuses into the open channel
  96. Diltiazem HCl- Cardizem, Cartia, tiamate, tiazac, dilacor
    • Benzothiazepine
    • Inhibition of CA influx is the basis of anti-arrhythmic activity

    Does not bind in resting state but only after the channels is opened. Water soluble that diffuses into the open channel

    Incompatible for mixing with furosemide solutions

    Use in extreme caution in patients with CHF

    DI: histamine H2 antagonists (cimetidine), may increase bioavailability by 50%, Serum digoxin levels may be increased

    Notify MD if the following occur: irregular heart beat, shortness of breath, edema of hands or feet, pronounce dizziness, constipation, nausea, hypotension
  97. Amlodipine - Norvasc
    • Ca channel blocker
    • 1-4 dihydropyridines
    • Effective in open or closed state by diffusion through the lipid bilayer to reach its binding site

    Avoid abrupt withdrawl of all calcium blocking drugs must be gradual and under medical supervision

    Use caution in patients with hepatic dysfucntion since all these agents are extensively metabolxied by the liver

    Pass through mothers milk

    Food interactions: grapefruit juice

    Do not chew sustained release formulations
  98. Isosorbide dinitrate - Isordil, Sorbitrate
    Isosorbide mononitrate - Monoket, Imdur, Isotrate
    Nitrate vasodilator products

    Problems with use: tolerance, withdrawl must be gradual, avoid alcohol duet to severe hypotension, do not change brands, dont use with camp phoshodiaesterases
  99. Hydralazine HCl
    Direct peripheral vasodilator

    MOA: alters intracellular CA movements in vascular smooth muscle

    Problem: rebound renin/ATII response- fluid retention

    Aggravation of angina-lupus like reaction is pssible >200 mg/day
  100. Nitroglycerin
    • Nitrate vasodilator product
    • Topical ointment, IV, Sublingual, translingual, transmucosal, transdermal
  101. Propanolol- Inderal
    • Non- selectibe Beta blocker
    • Propanolamine class
    • 1st drug marketed

    Indications: cardiac arrhythmias, MI, hypertrophic subaortic stenosis, pheochromocytoma, hypertension, migraine prophylaxis, angina, essential tremor, stage freight, PSTD
  102. Atenolol - Tenormin
    Selective beta 1 receptor beta blocker

    Indications: hypertension, MI, angina

    Dosage needs reduction in renal failure as a function of crcl
  103. Furosemide - Lasix
    Diuretics that act at the thick ascending loop of henle

    MOA: inhibits the Na/K/Cl carrier system primarily in the Loop of Henle, some trace of activity in the proximal and distal tubules

    SE: hypokalemia, excessive fluid and electrolyte loss (reduced GFR and loss of efficacy), increase in resorption of agents normally excreted by the proximal tubule (can increase lithium toxicity, hyperurcemia), possible hypersensitivity due to sulfa, ototoxicity (additive with aminoglycosides), hyperglycemia, nausea, vomiting , myalgia
  104. Metoprolol- Lopressor, Toprol XL
    • Selective beta 1 blocker
    • Indications: hypertension, MI, angina pectoris, CHF

    Toprol XL given presurgical to prevent heart complications appears to increase the danger of stroke or death
  105. Nevivolol - Bystolic
    New selective beta 1 blocker and the durg modulates nitric oxide system

    MOA: new two fold mechanism. Produces vasodilation decreasing total peripheral resistance by modulation of nitric oxide release

    Indications: approved for hypertension

    Metabolism 2D6
  106. Labetalol HCl- Normodyne, Trandate
    Non-selective alpha and beta blocker

    Indications: hypertension, clonidine withdrawl induced hypertension, phechromocytoma

    IV use not compatable with basic solution (5% bicarbonate, furosemide, or other alkaline products)
  107. Carvedilol- Coreg
    Nonselective alpha and beta blocking agent

    Indications: essential hypertension, angina, idiopathic cardiomyopathy & CHF including severe heath failure.

    Not recommended in hepatic impairment, watch glycemic control

    Several polymorphism identified but most important is the Arg-Gly at amino acid position 389 which has been associated with CVD
  108. Doxazosin- Cardura
    Selective alpha 1 adrenergic antagonist- peripheral acting

    Marked first dose effect postural hypotension- take first dose at bedtime

    Indications: hypertension, benign prostatic hypertrophy, treatment of CHF in conjunction with beta blockers and dig
  109. Nifedipine - Procardia, Adalat
    1-4 dihydropyridines Ca channel blocker

    Indications: chronic stable angina, vasospastic angina, hypertension (SR only)
  110. Tamsulosin - Flomax
    Indications: Benign prostatic hypertrophy

    38-fold greater affinity for alpha1a receptors which have a high density in prostatic smooth muscle--prevents contraction by antagonizing the receptors

    Take with food to prevent orthostatis, 99% protein bound to alpha1 acid glycoprotein,
  111. Enalapril maleate- Vasotec
    ACEI: di varbocyl containing agents

    Indications: hypertension, heart failure and asymptomatic LVD

    Ethyl ester prodrug, no food effect on absorption
  112. Lisinopril - Prinivil, Zestril
    ACEI

    Indications: hypertension, heart failure, acute MI

    100% urinary excretion (why so popular), impared renal function prolongs effect, reduce dosage as a function of glomerular filtration rate, no food effect on absorption
  113. Benzapril HCl- Lotensin
    ACEI - dicarbocyl containing agents

    Indications: hypertension

    Ethyl ester prodrug, slight reduced food effect on absorption, dosage adjustment as fucntion of crcl
  114. Quinapril HCl- Accupril
    • ACEI
    • Indications: hypertension, heart failure

    Ethyl ester prodrug, reduce dosage as a function crcl
  115. Ramipril- Altace
    • ACEI
    • Indications: hypertension, heart failure, post MI

    Ethyl ester prodrug, slight reduced food effect on absorption, reduce dosage as a function of crcl
  116. Losartan Potassium - Cozaar
    • ARB
    • Contraindicated in pregnancy due to fetal damage and death

    Less cough side effect than with ACEI drugs- no bradykinin buildup

    Indications: hypertension, sustantial first pass effect by 2C9, 3A4, active metabolites, anti-platelet effect

    Appears to cause zn depletion and complexes with cu
  117. Candesartan cilexetil -Atacand
    • ARB
    • Contraindicated in pregnancy due to fetal damage and death

    Less cough side effect than with ACEI drugs- no bradykinin buildup

    Indications: hypertension

    Double ester prodrug, no dosage adjustment needed in mild hepatic impairment, renal impairment can increase plasma conc
  118. Valsartan - Diovan
    • ARB
    • Indications: hypertension
    • Very minor hepatic metabolism, major food effect on absorption, severe renal disease and hepatic impairment use caution in dosing, can casue a 20% increase in serum K
  119. Telmisartan- Micardis
    • ARB
    • Indications: hypertension
    • Use extreme caution in hepatic impairment- dose can not be reduced below 40 mg and be useful
  120. Olmesartan medoxomil- Benicar
    • ARB
    • Indications: hypertension
    • 20 mg/day starting dose

    Following ester hydrolysis during intestinal absorption no further metabolic events occur

    Anti-hypertensive effect onset occurs within one week and largely manifested after 2 weeks
  121. Aliskiren - Tekturna
    Direct non-peptide renin inhibitor

    MOA: inhibits renin, the first and rate limiting step in the production of angiotensin I and II aldosterone

    Indications: mild to moderate hypertension alone or in combo with other agents

    No increase in bradykinin levels

    Do not use during pregnancy tetratogenic

    t 1/2 life approx 45 hours
  122. Lovastatin - Mevacor
    HMG- CoA reductase inhibitor

    A prodrug activated by liver hydrolysis of the lactone ring

    Indications: familila and non-familial hypercholesterolemia including type IIa and IIb disease, artherosclerosis--CHD

    Extensive 1st pass effect by 3A4, renal disease can lead to increased plasma levels, take with meals
  123. Simvastatin - Zocor
    • Compactin class: HMG-CoA reductase inhibitor
    • Prodrug activated by liver hydrolysis of the lactone ring

    Indications: familial, and non-familial hypercholesterolemia including type IIa and IIb disease, artherosclerosis--CHD

    Extensive 3A4 can be taken without regard to meals
  124. Pravastatin - Pravachol
    HMG- CoA reductase inhibitor compactin class

    Indications: familial and non-familial hypercholesterolemia including type IIa and IIb hyperproteinemias, artherosclerosis, previous MI, or other coronary events

    Extensive first pass effect via sulfunation, hepatic disease can lead to huge increases in plasma concentrations, food will result in decreased absorption
  125. Atorvastatin calcium - Lipitor
    HMG- CoA reductase inhibitor non-compactin

    Indications: familial and non familial hypercholesterolemia including type IIa and type IIb hyperproteinemias, Type III dysbetalipoproteinemia, Type IV elevated serum triglycerides

    Extensive 1st pass 3A4 (active metabolites), renal disease does not increase plasma levels, hepatic diease can lead to huge increases in plasma conc, can be taken without regard to meals

    Atorvastatin phototoxi
  126. Rosuvastatin calcium - Crestor
    HMG-CoA reducase inhibitor non compactin class

    Indications: familial and non familial hypercholesterolemia including type IIa and IIb disease

    Very minor 1st pass by 2C9 resulting in N-demethylation, no effect on 3A4

    50% decrease in absorption if taken concurrently with antacides--2 hour rule applies, sulfonamide
  127. Gemfibrozil - Lopid
    • Anti-hyperlipidemic agents
    • Fibric acid derivative

    MOA: inhibits peripheral lipolysis, decreases hepatic extraction of free fatty acids, decreases VLDL synthesis and its carrier molecule synthesis

    Indications: Type IV and V hyperlipidemia in patients at risk fro pancreatitis with tirglycerides of 1000-2000 mg/dl, patients at risk of CHD in which all other approaches have failed
  128. Bisoprolol fumarate - Zebeta
    Selective beta 1 blocker

    Indications: hypertension

    Dosage adjustment may be necessary in renal or hepatic failure
  129. Terazosin HCl - Hytrin
    Selective alpha 1 adrenergic antagonist - peripheral acting

    Indications: hypertension, benign prostatic hypertrophy

    Minimal 1st pass effect

    Marked 1st does effect-postural hypotension- take 1st dose at bedtiem
  130. Fenofibrate - Tricor
    Fibric acid dervative

    MOA: unknown but appears to inhibit triclyceride and VDLD synthesis

    • ndications: Type IV and V hyperlipidemia in patients at risk fro
    • pancreatitis with tirglycerides of 1000-2000 mg/dl, patients at risk of
    • CHD in which all other approaches have failed
  131. Colesevelam HCl- Welchol
    • Bile acid sequestrant
    • MOA: form insoluable compelx with fatty acids and bile acid sterols which are excreted from the gall bladder. Complex passes out with the stool

    Anion-exchange resins - do not use at the same time as anionic drugs, can reduce folate absorption

    Often as combinatin therapy with HMG-CoA reductase inhibitors or with nicacin, take before meals, do not take in dry form, do not chew tablet dose forms

    Indications: elevated LDL Type IIa hyperlipidemia in combination therapy with other agents, adjunct in treatment of type II diabetes
  132. Ezetimibe - Zetia
    • Anti-hyperlipidemia agent
    • Lipase inhibitor

    MOA: selective inhibits intestinal absorption of cholesterol and other phytosterols at teh brush border area of the intestinal membrane

    Indications: hyperlipidemia can be used in combination with the statin agents or fenofibrate

    Inhibits the lipase enzymes by acylation of the enzyme active site nucleophile
  133. Dipyridamole - Persantine combo with ASA- Aggrenox
    MOA: platelet aggregation inhibitor bia phosphodiesterase inhibition leading to increased cAMP, prevents adenosine reuptake into red blood cells, inhibition of thromboxane A2 synthesis (activator of platelet aggregation)

    Indications: adjunctive to coumarin anticoagulants in the preventionof post-operative thromboembolic complication of cardiac valve replacement, prevention of MI and stroke-in combo with ASA
  134. Clopidogrel - Plavix
    • MOA:
    • 1. inhibits ADP binding to platelet receptor
    • 2. inhibits induction of the adhesion receptor glycoproteing IIb/IIIa adhesion of platelets
    • 3. Effective for the entire life of the platelet
    • 4. Does not inhibit cAMP phosphodiesterase

    • Indications:
    • 1. reduction of artherosclerotic events associated with MI, stroke or other peripheral artery disease, stent deployment-- DES stents more likely to experience late-stent thrombosis than BMS post discontinuation
    • 2. Acute coronary syndrome

    Inform dentist ---bleeding time is much longer

    Metabolized intestinal esterase and hepatic metabolism

    Need 2C19 so interact with PPIs that inhibit 2C19
  135. Enoxaparin Sodium - Lovenox
    Low molecular weight Glycosaminoglycans: LMW heparin

    Less plasma protein binding, increased bioavailability and duration, less thrombin activity with potent factor Xa inhibition

    Indications: post-surgical prophylaxis for DVT with or without PE, abdominal surgery, unstable angina, non-Q wave MI, other unlabeled uses related to surgery and trama

    • Advantages:
    • 1. self administered in outpatient setting
    • 2. improved control of bioavailability
    • 2. more selective for factorXa
    • 4. less potential of thrombocytopenia
  136. Warfarin Sodium - Coumadin
    Vitamin K reductase inhibitor

    Indications: prophylaxis and treatment of venous thrombosis, pulmonary embolism, and atrial fibrillation

    Dosage must be individualized

    Watch for signs of bleeding - Petechiae

    Displacement is major cause of drug interactions

    Do not switch brands

    • 2C9 metabolizes S enantiomer-5x more potent
    • 3A4 metabolizes R enantiomer

    • 3 types of drug-drug interactions:
    • 1. pharmacokinetic
    • 2. pharmacodynamic
    • 3. new drug interaction mechanicsm identified

    Watch drinking with cranberry juice, and taking with ginseng
  137. Sildenafil citrate - Viagra
    MOA: selective inhibitors of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase 5 enhances effects of NO by preventing the degradation of cGMP--leads to smooth muscle relaxation and inflow of blood to the corpus cavernosum

    SE: high plasma levels will cause abnormal color vision (blue/green); sudden hearing loss which may include tinnitus, vertigo an ddizziness

    3A4 and 2C9

    CI: any patient taking organic nitrate -- dangerous hypotension, known QT elongation

    Use caution: in patients with pre-existing CV disease, anti-hypertensices, 4 hour or longer erection seek immediate medical attention
  138. Vardenafil HCl- Levitra
    • MOA: selective inhibitors of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase 5 enhances effects of NO by preventing the degradation of cGMP--leads to smooth muscle relaxation and inflow of
    • blood to the corpus cavernosum

    • SE: high plasma levels will cause
    • abnormal color vision (blue/green); sudden hearing loss which may include tinnitus, vertigo an ddizziness
    • 3A4 and 2C9

    CI: any patient taking organic nitrate -- dangerous hypotension, known QT elongation

    • Use caution: in patients with pre-existing CV disease, anti-hypertensices, 4
    • hour or longer erection seek immediate medical attention
  139. Tadalafil - Cialis
    MOA: Selective inhibitor (>10,000X) of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase 5 (PDE5)

    Metabolized by 3A4 to catechol metabolite

    SE: high plasma levels will cause abnormal color vision (blue/green), sudden hearing loss which may include tinnitus, vertigo and dizziness

    CI: any pt taking an organic nitrate--48 hours before admin possible, dangerous hypotension, known QT elongation

    Use caution: 4 hour or longer erection seek immediate medical attention
  140. Glipizide - Glucotrol
    • 2nd generation Sulfonylureas
    • No active metabolites
    • MOA:
    • 1. Stimulate insulin release from pancreatic beta islet cells by binding to and blocking an ATP-ase sensitive K channel
    • 2. This causes depolarization and an increase in intracellular Ca which leads to the release of the hormone
    • 3. May also decrease the hepatic clearance of insulin

    • Adverse effects:
    • 1. Hypoglycemia-most common in the elderly taking agents that have long half-lives--this may appear as an acute neurologic emergency stroke--check blood glucose
    • 2. DI caused by inhibition/induction of CYP systems
    • 3. 10-15% patients will experience a disulfram-like reaction with ehtanol especially with chlorpropamide

    Dosage must be individualized

    CI: patients with IDDM, pregnancy, lactation or hepatic and renal failure
  141. Glyburide - DiaBeta, Micronase, Glynase PresTab
    • 2nd Generation Sulfonylureas
    • Weakly active metabolites
    • MOA:
    • 1. Stimulate insulin release from pancreatic beta islet cells by binding to and blocking an ATP-ase sensitive K channel
    • 2. This causes depolarization and an increase in intracellular Ca which leads to the release of the hormone
    • 3. May also decrease the hepatic clearance of insulin

    • Adverse effects:
    • 1. Hypoglycemia-most common in the elderly taking agents that have long
    • half-lives--this may appear as an acute neurologic emergency
    • stroke--check blood glucose
    • 2. DI caused by inhibition/induction of CYP systems
    • 3. 10-15% patients will experience a disulfram-like reaction with ehtanol especially with chlorpropamide

    Dosage must be individualized

    CI: patients with IDDM, pregnancy, lactation or hepatic and renal failure
  142. Glimepiride - Amaryl
    • 3rd Generation Sulfonylureas
    • Active metabolites
    • MOA:
    • 1. Stimulate insulin release from pancreatic beta islet cells by binding to and blocking an ATP-ase sensitive K channel
    • 2. This causes depolarization and an increase in intracellular Ca which leads to the release of the hormone
    • 3. May also decrease the hepatic clearance of insulin

    • Additional mechanisms of action:
    • 1. Appears to cause translocation of GLUT-4 glucose transporter to the cell surface from the cytoplasm- insulin like activity
    • 2. May bind to a different protein than the usual sulfonylurea receptor on the beta islet cell

    • Adverse effects:
    • 1. Hypoglycemia-most common in the elderly taking agents that have long
    • half-lives--this may appear as an acute neurologic emergency
    • stroke--check blood glucose
    • 2. DI caused by inhibition/induction of CYP systems
    • 3. 10-15% patients will experience a disulfram-like reaction with ehtanol especially with chlorpropamide

    Dosage must be individualized

    CI: patients with IDDM, pregnancy, lactation or hepatic and renal failure
  143. Rosiglitazone maleate - Avandia
    Thiazolidinediones

    MOA: Increase the activity of teh nuclear receptor PPAR-gamma that regulate genes responsible for the control of glucose and insulin metabolism in adipose, liver and skeletal muscle tissues-increase tissue sensitivity

    Indications: Type 2 diabetes alone or in combo with a sulfonylurea or insulin

    These drugs work only work in presence of insulin

    Watch for possibility of hepatic failure- monitor transaminase levels before and after starting therapy

    Can be taken with or without food

    Metabolized by 2C8 lesser extend by 2C9
  144. Pioglitazone - Actos
    Thiazolidinediones

    • MOA: Increase the activity of teh nuclear receptor PPAR-gamma that
    • regulate genes responsible for the control of glucose and insulin
    • metabolism in adipose, liver and skeletal muscle tissues-increase tissue
    • sensitivity

    Indications: Type 2 diabetes alone or in combo with a sulfonylurea or insulin

    These drugs work only work in presence of insulin

    Watch for possibility of hepatic failure- monitor transaminase levels before and after starting therapy

    Can be taken with or without food

    Metabolized by 3A4. Decreases the efficacy of OC's- suggest alternate method of BC, monitor ALT for hepatotoxicity
  145. Metformin HCl - Glucophage
    MOA: Decrease hepatic gluconeogenesis and intestinal glucose absorption, increases peripheral tissue insulin sensitivity, does NOT cause insulin release in the pancreas

    Indications: Type 2 diabetes with diet and exercise or in combination with a sulfonylurea

    Can cause decrease B12 and folate absorption,

    CI: In hepatic and renal failure or a history of lactic acidosis, Stop taking if MI occurs or septicemia

    No protein binding, no metabolism with rapid renal excretion
  146. Insulin glargine - Lantus
    Recombinant/chemically modified insulins

    Forms microprecipitates in Sub-Q tissue prolonging duration from 18-26 hours
  147. Insulin lispro - Humalog
    • Recombinant/chemically modified insulins
    • Rapid acting 3-5 hours duration, take 15 minutes before meals or immediately after eating
  148. Insulin aspart - Novolog
    • Recombinant/chemically modified insulins continued
    • Rapid acting 3-5 hour duration, take 5-10 minutes before meals
  149. Exenatide - Byetta
    Recombinant/chemically modified/synthetic polypeptides

    Incretin mimetic or glucagon-like peptide-1 (GLP-1) receptor agonist that binds the GLP-1 receptor on beta islet cells causing insulin synthesis and excretion
  150. Levothyroxine Sodium - Levo-T, Levothyroid, Levoxyl, Synthroid, Eltroxin
    • Thyroid Hormone
    • T4
    • DI: amiodarone, warfarin, dicoumarol, iopanoic acid, sulfonamides and heparin (interfer with T4 binding to plasma transport protein)

    In the diabetic patient: If you start thyroid replacement therapy you must also monitor blood glucose levels closely and increase insulin and hypoglycemic medications
  151. Liothyronine Sodium -Cytomel
    • hyroid Hormone
    • T3

    • DI: amiodarone, warfarin, dicoumarol, iopanoic
    • acid, sulfonamides and heparin (interfer with T4 binding to plasma transport protein)

    In the diabetic patient: If you start thyroid replacement therapy you must also monitor blood glucose levels closely and increase insulin and hypoglycemic medications
  152. Famotidine - Pepcid
    H2 antagonists

    Indications: duodenal ulcer, benign gastric ulcer, erosive GERD, pathological hypersecretory conditions, GI bleeding , (heart burn, acid indigestion, sour stomach -OTC)

    Does not inhibit cyp 450 enzymes
  153. Omeprazole - Prilosec
    • Proton Pump Inhibitor
    • MOA: at acidic pH within the parietal cells these prodrugs undergo an intramolecular rearrangement generating a sulfenamide that covalently reacts with thiol functional groups forming a disulfide on the extracellular luminal domain of the pump protein

    These are permanent inhibitors of the pump system until protein/membrane turnover occurs which takes 3-5 days

    Indication: delayed release capsules for duodenal ulcer associated with/without H. Pylori, erosive esophagitis, GERD, hypersecretory conditions, posterior laryngitis

    Hepatic disease can increase bioavailability
  154. Rabeprazole Na - Achiphex
    • Proton pump inhibitor
    • MOA: at acidic pH within the parietal cells these prodrugs undergo an intramolecular rearrangement generating a sulfenamide that covalently
    • reacts with thiol functional groups forming a disulfide on the extracellular luminal domain of the pump protein

    These are permanent inhibitors of the pump system until protein/membrane turnover occurs which takes 3-5 days

    Indications: delayed release tablets for duodenal ulcers, GERD, maintenance of healing of GERD, hypersecretory conditions and for H. pylori eradication

    CYP450 metabolized- no dosage adjustment in patients with mild to moderate dysfunction use caution in severe impairment

    Take before eating
  155. Pantoprazole Na - Protonix
    • Proton Pump Inhibitors
    • MOA: at acidic pH within the parietal cells these prodrugs undergo an intramolecular rearrangement generating a sulfenamide that covalently
    • reacts with thiol functional groups forming a disulfide on the extracellular luminal domain of the pump protein

    These are permanent inhibitors of the pump system until protein/membrane turnover occurs which takes 3-5 days

    Indications: Short term treatment of GERD

    Can be taken with or without food

    Accumulation in hepatic dysfunction is possible-use caution if concurrent C19 and 3A4 inhibitors are used

    Enteric coated--low stomach pH will destroy the compound, can be taken with antacids or food
  156. Ranitidine HCl - Zantac
    • H2 antagonist
    • Indications: duodenal ulcer, benign gastric ulcer, erosive GERD, pathological hypersecretory conditions

    Does not inhibit CYP 450 enzymes

    Stagger doses of antacids and H2 blockers to maximize bioavailability
  157. Esomeprazole Magnesium - Nexium
    • Proton Pump Inhibitor
    • S enantiomer of omeprazole

    Indications: Erosive esophagitis, GERD, triple therapy for duodenal ulcer associated with H. Pylori

    Capsules can also be opened and taken in a smiliar manner as lansoprazole in patients that have difficulty swallowing capsules: suspension for use down feeding tubes
  158. Lansoprazole - Prevacid
    • Proton Pump Inbitior
    • MOA: at acidic pH within the parietal cells these prodrugs undergo an intramolecular rearrangement generating a sulfenamide that covalently
    • reacts with thiol functional groups forming a disulfide on the extracellular luminal domain of the pump protein

    These are permanent inhibitors of the pump system until protein/membrane turnover occurs which takes 3-5 days

    Indications: delayed release capsules for duodenal ulcer associated with/without H. pylori, erosive esophagitis, GERD, hypersecretory conditions, dual and triple therapy, approved for children age 1-11 for GERD

    For patients who have difficulty swallowing the capsules can be opeaned and sprinkled on applesauce, cottage cheese or yogurt or fruit juices if swallowed immediate upon mixing; Take before eating
  159. Sitagliptin phosphate - Januvia
    Sitagliptin phosphate + metformin = Janumet
    • DPP-IV inhibitor of incretin
    • MOA: Dipeptidyl protease IV inhibitor--prolongs the biological levels of the natural incretins GLP-1 and GIP--thereby increasing insulin release and decreasing release of glucagon

    Modify dosage in moderate to end-stage renal failure as a function Crcl excreted via OCT tubular secretion as unchanged drug

    Indications: monotherapy for type 2 diabetes (Do Not use for type I)

    Potential adverse side effects: other peptides as cleaved by DPP-IV such as neuropeptides, cytokines, chemokines--what is the consequence of inhibiting their metabolims
  160. Lubiprostone - Amitiza
    MOA: A locally acting selective Cl- channel activator of ClC2 that produces a Cl-rich intestinal fluid without alteration of Na and K serum levels. This fluid production increases GI motility clearing the intestinal of stool

    Indication: idiopathic chronic consitpation in adults (24 mcg bid with food)

    Low systemic activity or absorption past the GI epithelia membrane. Not cyp metabolized but processed by carbonyl reductase in the stomach and jejunum

    CI: pts with history of mechanical bowel obstruction
  161. Albuterol - Proventil, volmax, ventolin tablets including extended release, syrup aerosol, solution and capsules for inhalation
    Short acting agent, beta 1 activity <beta 2 activity, PO onset 30 minutes with duration 4-8 hours, inhalation onset 5 minutes with duration of 3-6 hours, third most poten beta 2 agent--most widely used agent bia a nebulizer in ER
  162. Levoalbuterol - Xopenex
    Short acting agent, a solution for inhalation. Reported to have much less beta1 activity thatn racemic mixture
  163. Salmeterol
    Serevent inhalation powder - Advair Discus- combo with a corticosteriod fluticasone
    Beta 1 activity < beta 2 activity, inhalation onset 20 minutes with duration of 12 hours, greatest beta 2 potency available (2X isoproterenol)
  164. Iparatropium Bromide - Atrovent
    • Anti-cholinergic brochodilators
    • Solution for inhalation, aerosol, nasal spray

    MOA: Synthetic quaternary anticholinergic parasympatholytic ammonium compound chemically related to atropine which antagonize the effects of acetylcholine to decrease the intracellular concentrations of cGMP

    CI: Food allergy to soy bean or peanut products

    • Patient info:
    • 1. avoid contact of solutions with the eyes since temporary blurred vision, precipitation or worsening of narrow-angle glaucoma or eye pain will result
    • 2. If mixed with albuterol for nebulizer use the solution must be used within 1 hour
    • 3. Nasal spray pumps require priming of up to 7 actuations
  165. Montelukast Sodium - Singulair
    • Leukotriene Receptor Antagonist
    • MOA: selective and competitive CysLT1 receptor antagonist of leukotriene C3 D4 and E4 which are components of slow-reacting substance of anaphylaxis (SRSA) preventing bronchoconstriction

    Indications: prophylaxis and chronic treatment of asthma in adults and children one year of age and older, 4 mg oral granules for children 0.5-5 years old for perennial allergic rhinitis

    Metabolized by 2C9 and 3A4

    Tablets and chewable tablets, oral granules-once daily in the evening and with or without food
  166. Fluticasone - Flovent
    • Respiratory corticosteriod inhalation products
    • MOA: adrenal corticosteriods with basic glucocorticoid activity and actions--exact mechanism in the lung tissue is unknown--local lung delivery can reduced the systemic glucocorticoid activity

    Indications: tx including maintenance and prophylaxis of chronic asthma pts including those that require systemic corticosteriods of those that could benefit from systemic dose reduction/elimination

    After withdrawl of systemic agents it takes several months for hypothalamic-pituitary-adrenal function to return to normal. Adrenal insufficiency will manifest itself during trauma, surgery or infection--use extreme caution--be on the lookout for severe asthmatic attack

    Patient Information: rinse mouth out with water following use without swallowing to avoid oral candidiasis, do not abruptly stop use or use to treat acute attack, immediately contact MD if exposed to chicken pox or measles or if sore mouth or throat occurs
  167. Mometasone furoate - Asmanex twisthaler
    • Respiratory corticosteriod inhalation products
    • MOA: adrenal corticosteriods with basic glucocorticoid activity and
    • actions--exact mechanism in the lung tissue is unknown--local lung
    • delivery can reduced the systemic glucocorticoid activity

    • Indications: tx including maintenance and prophylaxis of chronic asthma
    • pts including those that require systemic corticosteriods of those that
    • could benefit from systemic dose reduction/elimination

    • After withdrawl of systemic agents it takes several months for
    • hypothalamic-pituitary-adrenal function to return to normal. Adrenal
    • insufficiency will manifest itself during trauma, surgery or
    • infection--use extreme caution--be on the lookout for severe asthmatic
    • attack

    • Patient Information: rinse mouth out with water following use without
    • swallowing to avoid oral candidiasis, do not abruptly stop use or use to
    • treat acute attack, immediately contact MD if exposed to chicken pox or
    • measles or if sore mouth or throat occurs
  168. Triamcinoone Acetonide - Nasacort
    • Respiratory Corticosteriod Intranasal product
    • MOA: Adrenal corticosteriods with basic glucocorticoid activity and actions--exact mechanism in the nasal tissue is unknown (decreased inflammatory mediators)

    Warning: Use caution in pts in systemic alternate-day corticosteroid treatment since HPA suppression likelihood may increase--local delivery can reduce the systemic glucocorticoid activity, some weak mineralcotoricoid activity

    Localized infections from Candida albicans is rare but if any infection occurs anti-infective therapy must be used

    Patient information: May dry and irritate the nasal mucosa, sneezing may occur, if problems persist after 3 weeks contact the MD, do not exceed recommended dosage, contact MD if exposed to chicken pox or measles
  169. Budesonide - Rhinocort
    • Respiratory Corticosteriod Intranasal product
    • MOA: Adrenal corticosteriods with basic glucocorticoid activity and
    • actions--exact mechanism in the nasal tissue is unknown (decreased
    • inflammatory mediators)

    • Warning: Use caution in pts in systemic alternate-day corticosteroid
    • treatment since HPA suppression likelihood may increase--local delivery
    • can reduce the systemic glucocorticoid activity, some weak
    • mineralcotoricoid activity

    Localized infections from Candida albicans is rare but if any infection occurs anti-infective therapy must be used

    • Patient information: May dry and irritate the nasal mucosa, sneezing may
    • occur, if problems persist after 3 weeks contact the MD, do not exceed
    • recommended dosage, contact MD if exposed to chicken pox or measles
  170. Mometasone furoate - Nasonex
    • Respiratory Corticosteriod Intranasal product
    • MOA: Adrenal corticosteriods with basic glucocorticoid activity and
    • actions--exact mechanism in the nasal tissue is unknown (decreased
    • inflammatory mediators)

    • Warning: Use caution in pts in systemic alternate-day corticosteroid
    • treatment since HPA suppression likelihood may increase--local delivery
    • can reduce the systemic glucocorticoid activity, some weak
    • mineralcotoricoid activity

    Localized infections from Candida albicans is rare but if any infection occurs anti-infective therapy must be used

    • Patient information: May dry and irritate the nasal mucosa, sneezing may
    • occur, if problems persist after 3 weeks contact the MD, do not exceed
    • recommended dosage, contact MD if exposed to chicken pox or measles
  171. Budesonide & Formoterol - Symbicort
    • Sympathomimetic Bronchodilators
    • MOA: relative selectivity of a particular agent for alpha, beta 1 & 2 adrenergic effects determines it usefulness clinically--and predicts an agents SE that will be observed

    200X higher affinity for beta 2 receptors over beta 1 (SS) is 1000X less potent as a beta 2 agonist than (RR) cpd

    Also inhibitor of mast cell mediators such as histamine and leukotrienes
  172. Tiotropium Br - Spiriva
    • An inhalation powder using the HandiHaler device
    • Long-acting agent to be used once daily

    • MOA: Synthetic quaternary anticholinergic parasympatholytic ammonium
    • compound chemically related to atropine which antagonize the effects of
    • acetylcholine to decrease the intracellular concentrations of cGMPCI: Food allergy to soy bean or peanut productsPatient info: 1.
    • avoid contact of solutions with the eyes since temporary blurred
    • vision, precipitation or worsening of narrow-angle glaucoma or eye pain
    • will result2. If mixed with albuterol for nebulizer use the solution must be used within 1 hour3. Nasal spray pumps require priming of up to 7 actuations
  173. Fexofenadine HCl- Allegra
    2nd generation Antihistamines- Piperidine peripheral selective

    Indications: seasonal allergic rhinitis (6 years of age or older) and chronic idiopathic urticaria
  174. Benzonatate capsules - Tessalon
    MOA: structurally related to tetracaine--anesthetizes stretch receptors in the respiratory areas dampening their activity reducing cough reflex at its source

    Swallow capsules whole--do not chew or break
  175. Estradiol- Estrace, Climara, Vivelle, FemPatch, Alora, EvaMist
    Estrogen replacement
  176. Levocertirizine - Xyzal
    • 2nd generation antihistamine
    • 1 enantiomer drug
    • Approved also for use in children 6-11 years of age - one half of a 5 mg tablet
  177. Congugated Estrogens - Premarin
    • Additional indication of osteoporosis treatment
    • Isolated from pregnant horse urine-sugar conjugates

    FDA placed saftey monitoring list for possible angioedema
  178. Raloxifene - Evista
    Selective Estrogen Receptor Modulator (SERM)

    MOA: Estrogen receptor antagonist lacking estrogen activity in breast and uterine tissue, reduces bone resorption and turnover, increased bone mineral density

    Indication: Osteoporosis tx

    Extensive 1st pass metabolism

    CI: women planning to become pregnant or pregnant, blood clot disorders

    Use caution: discontinue use 72 hours prior to surgery or immobilization due to clotting potential, hepatic failure, not effective in treating hot flash disorders
  179. Medroxyprogetsterone Acetate
    • Progestin
    • Specific indication: secondary amenorrhea, abnormal uterine bleeding due to hormonal imbalance, injectable contraceptive

    Depo-Provera- Injectable--off label use-chemical castration of male sex offenders
  180. Nuvaring
    Vaginal ring containing etonogestrel and ethynyl estradial
  181. Ortho Evra
    First transdermal skin patch approved for birht control

    Contains ethinyl estradiol (Estrogen) and norelgestromin (Progestin)
  182. Ortho Tri-cyclen LO
    A low dose but yeat effective agent when taken correctly containing norgestimate and ethinyl estradiol
  183. Yasmin & Yaz
    Drospirenone (progestin) and ethinyl estradiol (estrogen activity)

    Drospirenone is an analog of spironolactone--can cause increased K levels--measure during the 1st treatment period--watch for interactions wit other drugs that increase K

    Claims less SE such as HA, N/V, breast tenderness, emotional lability

    Decreases production of testosterone in ovaries and skin --a benefit in preventing mood symptoms

    CI: renal, hepatic, or adrenal insufficency

    Additionally Yaz is used for premenstrual dysphoric disorder for women that choose OC as a method of contraception
  184. Dutasteride- Avodart
    MOA: Inhibits steroid 5 alpha reductase preventing testosterone conversion to 5 alpha dihydrotestosterone

    Indications: Benign prostatic hyperplasia
  185. Finasteride - Propecia or Proscar
    MOA: inhibits steriod 5 alpha reducatase preventing testosterone conversion to 5 alpha dihydrotestosterone

    Indications: benign prostatic hyperplasia, androgenic alopecia
  186. Alendronate - Fosamax
    • Bisphosonate
    • MOA: appears the bisposphoante is incorporated into the bone matrix and is imbibed by oseoclasts. this incapacitiates the osteoclas preventing resorption of the bone

    All of these drugs are poorly absorbed in the intestine therefore take them at least 90 minutes before or after meals and only with water

    Use caution in renal impairment, avoid Al or Mg containing antacids, may cause Nasuea and diarrhea
  187. Risedronate sodium - Actonel
    • Bisphosonate
    • MOA: appears the bisposphoante is incorporated into the bone matrix and
    • is imbibed by oseoclasts. this incapacitiates the osteoclas preventing
    • resorption of the bone

    • All of these drugs are poorly absorbed in the intestine therefore take
    • them at least 90 minutes before or after meals and only with water

    Use caution in renal impairment, avoid Al or Mg containing antacids, may cause Nasuea and diarrhea

    Now available with CaCO3- Day 1 you take 35 mg of drug and days 2-7 one tablet of 1250 mg CaCO3
  188. Ibandronate sodium - Boniva
    • New generation of bisphosphonate
    • Indicated postmenopausal osteoporosis

    Renal clearance is lineraly related to Crcl

    New dosage form 150 mg tab taken once a month
  189. Methylprednisolone - Medrol
    Triamcinolone
    Prednisone
    Hydrocortisone
    Dexamethasone
    Adrenocorticoal Steriods
  190. Cohchicine
    MOA: decreases granulocyte phagocytosis and prevents leukocyte migration and lactate production, decreases inflammatory response to deposited crystals--an antimitotic agent- prebents spindle formation. Does not decrease plasma uric acid levels

    Indications: Unique anti-inflammatory agent that is largely effective only in gout-can be used to relieve pain of an acute atttack or prophylactically; also some unlabeled uses-MS , cirrhosis and others

    Natural product isolated from the flowering plant seeds and corn of colchicum autumale, a member of the lilly family

    Always use with urcosuric agent

    Perform periodic blood counts to look for leukopenia, not an analgesic nor an uricosuric agent, dc use at 1st sign of N/V, diarrhea or stomach pain; causes malabsorption of vit b12
  191. Allopurinol - Zyloprim
    MOA: inhibits xanthine oxidase which is responsible for the synthesis of urate from xanthine and hypoxanthine

    Indications: Management of gout, management of patients with malignancies, calcium oxalate calculi

    • Metabolism:
    • 1. allopurinol is rapidly oxidized to the metabolite alloxanthine--this has a longer half life and accumulates contributing significantly to the overall therapeutic effects and side effects as dosage increases
    • 2. inhibits liver microsomal enzymes cyp

    Therapy should be started at low doses and tirated upward to prevent precipitation of a gouty attack, water consumption should be >2 liters/day useful agent in renal impairment when urcosuric agents do not work well
  192. Cyancobalamin
    • Vitamin B12
    • Primarly produced in microorganism
    • Meats, eggs, seafood, dairy, and fermented products
    • Water soluble
    • Absorption is dependent on intrinsic factor
    • A glycoprotein secreted by parietal cells of the gastric mucosa
    • Deficiency leads to anema
  193. Folic Acid
    • Vitamin B9
    • Humans can not synthesize folic acid and get it from diet or microbial gut bacteria synthesis

    Deficiency result of malabsorption or alcoholism

    Need for folic acid increases during pregnancy
  194. Valacyclovir HCl - Valtrex: Prodrug form of acyclovir
    Acyclovir- Zovirax
    Anti-herpes agents- Synthetic nucleoside class of agent

    MOA: following phosphorylation via first thymidine kinase, the triphosphate inhibits DNA polymerase and replication by being incorporated into DNA

    Indications: HSV1 &2, shingles, epstein-barr, CMV, and chicken poz

    Class B pregnancy--routinely used during pregnancy to suppress outbreaks and to aid in vaginal delivery to lower risk of offspring infection
  195. Oseltamivir phosphate - Tamiflu
    Anti-infulenza- Neuraminidase inhibitor

    MOA: ethyl eser prodrug that appears to inhibit influenza neuraminidase enzyme system thereby altering particle aggregation and release

    Dosage reduction necessary in renal Ccr <30

    75 mg capsules for adults--take without regard to food, suspension for kids plus 30 and 45 mg capsules
  196. Penicillin V-Beepen VK, Peen-VeeK, Veetids
    • Penicillin beta lactam antibiotic
    • Indications: susceptible organisms causing Streptococcal, Pneumonoccal, Staphylococcal infections, rheumatic fever or chorea, Lyme's disease and mild to moderate anerobic infections.

    Use extreme caution in Staph infections: resistance, Do Not use in cases of severe infection initially

    Oral use only , May be taken with meals but blood levels higher if taken on empty stomach

    Not penicillinase resistant, Not acid stable

    Dosage adjustments are required in severe renal failure

    Store reconstituted oral solutions in the regrigerator

    Dosage typically 125-500 mg up to 4 times per day for 10-20 days
  197. Amoxicillin - Amoxil, Trimox, Wymox
    • Penicillin beta lactam antibiotics
    • Aminopenicillins
    • Indications: Spectrum of activity essentially identical to ampicillin except more active against Shigella spp., Chlamydia trachomatis in pregnancy

    More complete absorption than ampicillin, 3X per day dosing, less diarrhea than ampicillin

    Oral use only, Not penicillinase resistant, actid stable, May be taken with meals

    Pediatric use: administer with milk, juice, or cold drink
  198. Amoxicillin/Clavulanate Potassium -Augmentin
    • Penicillin beta lactam antibiotics
    • Aminopenicillin
    • Indications: Susceptible strains of organisms in lower respiratory infections, Otitis media and sinusitis, skin and skin structure infections, UTI

    Oral use only, take with food if GI upset occurs

    Penicillinase resistant due to clavulanate presence

    Suspension and chewable tablets contain aspartame and should not be used by phenylketourics
  199. Cephalexin - Keflex, Biocef, Keftab
    First generation Cephalosporin Antibiotics: generally all agents are inactivated by beta lactamases

    Indications: Respiratory tract infections, Otitis Media, skin and skin structure infections, bone infections, GU infections

    Oral use only

    Cross allerginicity with penicillins

    • DI:
    • Alcohol use may produced a disulfiram like reaction
    • Aminoglycoside nephrotoxicity can be increased
    • Anticoagulant effects can be potentiated
    • Antacids can decrease plasma concentrations of oral agents
    • Loop diuretics nephrotoxicity can be increased

    Monitor renal function since all are renally excreted with the exception of cefoperazone
  200. Cefdinir - Omnicef
    3rd generation cephalosporin antibiotic

    Indications: Community acquired pna, acute exaccerbation of chronic bronchitits, acute maxillary sinusitis, pharnygitis, tonsillitis, skin and skin structure infections, acute otitis media

    Oral use only, reduce in renal failure
  201. Ciprofloxacin - Cipro
    Fluoroquinolines

    DOC for inhalation anthrax

    MOA: bactericidal agents that inhibit the enzyme DNA-gyrase (topoisomerase II) that is involved in introducing negative supercoils into circular duplex DNA. These coils relieve torsional stress in unwinding helical DNA therby permitting transcription and replication

    Indications: Acute sinusitis, lower respiratory tract infections, nosocomial pna (IV only), skin and skin structure infections, bone and joint infections, UTI, chronic bacterial prostatitis, empirical therapy, for febrile neutropenia patients, complicated intra-abdominal infections, infectious diarrhea--agent of choice, thypoid fever, susceptible sexually transmitted diseases (oral)

    Admix incompatibility with aminophylline, amozacillin, clindaymycin, floxacillin, heparin, maziocillin (alkaline solutions)

    Photoactive drugs, may cause dizziness or lightheadedness, do not use magnesium or aluminum containing antacids, iron or zinc containing products or multiple vitamins 4 hours before or 2 hours after taking the medication. Do not take with milk or dairy products
  202. Cefuroxime - Ceftin, Kefurox, Zinacef
    2nd generation cephalosporin antibiotics

    • Indications: Oral: respiratory tract infection, UTI, early Lyme disease, uncomplicated gonorrhea, skin and skin structure infections,
    • Parenteral: as above plus septicemia, meningitis, bone and joint infections, mixed infections

    Reduce dosage in renal impairment based on Crcl, may be taken with food, do not mix in the same IV as animoglycosides, or use sodium bicarbonate injection as diluent, do not chew tablets due to very bad taste, swallow whole
  203. Moxiflocacin HCl- Avelox
    • Fluoroquinolines
    • Indications: acute bacterial sinusitis, acute bacterial exacerbation of chronic bronchitis, community acquired pna

    Oral use only

    Can severely prolong the QT portion of an electrocardiogram in some patients, avoid use in patients with hypokalemia or ones taking Class Ia or III anti-arryhthmia drugs

    Not recommend for patient with moderate or severe hepatic failure
  204. Levofloxacin - Levaquin
    • Fluoroquinolines
    • Indications: acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, community acquired pna, skin and skin structure infections, UTI, acute pylelonephritis

    Oral or IV use only

    Dosage adjustment a fucntion of Crcl
  205. Doxycycline - Vibramycin, Periostat, Monodox, Doxy, Bio-tabs, Doryx, Doxychel Hycate
    Tetracycline

    • MOA: bind 30s bacterial ribosomal subunit which prevents the binding of aminoacyl tRNA to the mRNA-ribosomal complex--leads to inhibition of bacterial protein synthesis
    • Also binds to mammalian 30s but with much lower affinity, bacterial cells seem to concentrate tetracyclines--active (requires mg, and ATP) and passive transport

    Indications: sensative organisms in URI, UTI inclduding acute gonococcal infections (single visit 300 mg immediately and 300 mg after 1 hour), syphilis, chlamydia infections, prevention of traveler's diarrhea at 100 mg/day

    Oral and IV use only, DO NOT use SC or IM

    May be taking with food or milk

    Highest lipid solubility of the TCN's
  206. Minocycline- Dynacin, Vectrin, Minocin
    • Tetracycline
    • MOA: bind 30s bacterial ribosomal subunit which prevents the binding of aminoacyl tRNA to the mRNA-ribosomal complex--leads to inhibition of
    • bacterial protein synthesis
    • Also binds to mammalian 30s but with much
    • lower affinity, bacterial cells seem to concentrate
    • tetracyclines--active (requires mg, and ATP) and passive transport

    Indications: sensitive organisms in URI, UTI including syphilis, Chlamydia infections, sexually transmitted diseases in patients in which penicillins are contraindicated, meningoccal carriers, mycobacterium infections

    May be taken with food or milk

    Parenteral solutions are stable at room temp for 12 hours then discard
  207. Azithromycin - Zithromax
    Macrolide agents

    MOA: Binds selectively to a specific site on the 50s bacterial ribosomal subunit therapy preventing the translocation step of protein synthesis--it does not bind to mamamilan ribosomes

    Indications: COPD bacterial infections, community acquired pna, genital ulcer disease, PID, suceptible sexually transmitted diseases including gonococcal and chlamydial infectiosn, URI, skin and skin structure infections,

    New indication: one does tx for pediatric otitis media

    IV and oral use only, do not administer as a bolus or IM

    • Food decreases absorption by 50%
    • Does not inhibit CYP
  208. Clarithromycin - Biaxin
    Macrolide agent

    MOA: Binds selectively to a specific site on the 50s bacterial ribosomal subunit therapy preventing the translocation step of protein synthesis--it does not bind to mamamilan ribosomes

    Indications: Upper and lower respiratory infections, mycobacterial infections, heliocobacter pylori double or triple therapy, greater potency agains a number of organisms when compared to base

    Oral use only, may be given with or without food, no dosage adjustment in hepatic failure but with Crcl of <30 dosage adjustment necessary, 3A4 inhibitor

    Markedly improved acid stability and oral bioavailability, reduced GI side effects
  209. Metronidazole - Flagyl, Protostat, Metro IV
    Use in CDAD

    Avoid unnecesary use--carcinogenic

    MOA: appears once metabolized binds DNA and prevents replication

    Indications: anaerobic infections, intra-abdominal infections, skin and skin structure infections, gynecological infections, septicemia, CNS infections, lower respiratory tract infections, endocarditis, prophylaxis for colorectal surgery, hepatic coma, Crohn's disease, pseudomembraneous colitis, Helobacter Pylori

    CDC recommended for bacterial vaginosis (single gram dose), giardiasis

    Reduce dosage based on hepatic function, renally excrete metabolites, avoid alcohol, may cause metallic taste
  210. Trimethoprim - Proloprim, Trimpex
    Combo product with sulfamethoxazole- Bactrim, Cotrim, Septra, Sulfatrim
    Folate Reductase Inhibitor

    • MOA: Some affinity for human folate reductase which causes some of the side effects in humans
    • Microbes can not use dietary folic acid

    • Sulfonamides MOA: competitive inhibitors of PABA--thes drugs are bacteriostatic
    • By preventing folate coenzyme synthesis no deoxy thymidine for DNA synthesis is produced

    These drugs with high pKa values are prone to crystalluria and resulting kidney damage

    • Indications: UTI--perform susceptibility testing--may initiate therapy before results are obtained
    • Use in caution in renal/hepatic failure

    Phenytoin action is increased due to inhibition of hepatic metabolism
  211. Nitrofurantoin - Furadantin
    Nitrofuran: may be carcinogenic or mutagenic

    MOA: may inhibit acetylcoenzyme A thereby intefering with bacterial carbohydrate metabolism, may inhibit cell wall synthesis

    Indications: UTI in susceptible strains of E. coli, enterococoi, staphylococus aureus, klebsiella and enterobacter sp

    Rapidly metabolized in the body-nitro reduction-carcinogenic-interaction with DNA, ineffective if Crcl is <40 may cause brown disocloration of the urine
  212. Mupirocin - Bactroban
    • Anti- infectives and antiseptics
    • MOA: inhibits the bacterial enzymes isoleucyl transfer RNA synthase

    Indications: Impetigo caused by Staph and Strep Organisms
  213. Fluconazole - Diflucan
    Systemic antifungal azole agent

    MOA: some details are known-appears to inhibit funal cyp450 enzymes that are responsible for fungal sterol biosynthesis in particular lanosterol 14 alpha demethylase (azole or tazole group chelates iron in active site)

    This is an enzyme in the pathway responsible for synthesis of ergosterol-the primary fungal sterol in cell membranes

    Indications: oropharyngeal, esophygeal or vaginal candidiases, cryptococcal meningitis, prophylactic use in chemo or radiation therapy

    Potent inhibitor of 3A4 therefore many drug interactions
  214. Nystatin A1 - Mycostatin, Nilstat
    Systemic Polyene

    MOA: appear to bind cell wall sterols leading to disruption of the membrane and loss of cellular constituents especially K

    Indications: Non-esophageal membrane GI candidiasis

    • GI absorption is insignificant--pass out of the stool
    • Oral tablets, mycostatin-also a vaginal product for candidiasis
  215. Ketoconazole - Nizoral
    Systemic antifugal azole agent

    • MOA: some details are known-appears to inhibit funal cyp450 enzymes that
    • are responsible for fungal sterol biosynthesis in particular lanosterol 14 alpha demethylase (azole or tazole group chelates iron in active
    • site)

    Indications: Systemic fungal infections, severe recalictrate cutaneous dermatophyte infections

    Do not use fore fungal meningitis--poorly penetrates the CSF, topical use product also

    Off label use: cushing disease and advanced prostate cancer--suppresses adrenal steroidogenesis

    Potent inhibitor of 3A4, do not take with antacids delay 2 hours

    Hepatotoxicity possible--monitor hepatic enzymes before and after starting tx
  216. Hydroxychloroquine - Plaquenil
    Anti-Malarials 7-chloro-4-aminoquinolines

    • MOA: lots of mechanisms have been ruled out or still under investigation
    • 1. Drug binding to ferriprotoporphyrin IX which by itself results in the lysis of erythrocytes and malaria protozoan cells-the drug complex is not a potent lysis agent
    • 2. The drug (pka 8-9) gets trapped in the protozoan lysosome where the pH is normally pH 4.8-5.2. By raising the lysosome pH, the hemoglobin-digesting enzymes are inactivated--the parasite is deprived of amino acids

    Indications: prophylaxis or treatment of acute attacks of malaria, lupus erythematosus, rheumatoid arthritis

    Accumulate in liver, spleen, the heart, kidnesy and brain
  217. Anastrozole - Arimidex
    Aromatase Inhibitors

    MOA: inhibitors of the enzyme aromatase that is responsible for the covnersion of adrennaly produced androstenedione to estradiol--no effect on aldosterone synthesis

    Reversible competitive inhibitor

    Use caution in hepatic and renal impairment

    1A2m 2C8/9, and 3A4 inhibitor at high dosages
  218. Imiquimod - Aldara
    MOA: immune response modulator that increases activity of CD3, CD4, CD8 and other immune cells, interferon alpha, infiltration of lymphocytes, macrophages

    Indications: actinic keratosis, superficial basal cell carcinoma, external gential warts
  219. Potassium Chloride - Klor Con
    Potassium replacement
  220. Ezetimibe and Simvastatin - Vytorin
    HMG- CoA reductase inhibitor and 2-azetidinone (ezetibibe)

    • MOA:
    • Ezetimibe: inhibits absorption of cholesterol at the brush border of the small intesting
    • Simvastatin: HMG-CoA reductase inhibitor

    Indications: homozygous familial hypercholesterolemia, hyperlipidemias,

    Dosage adjustment in chinese pts on niacin doses > 1 g/day
  221. Niacin-Niaspan
    • Vitamin B3
    • Indicated for hyperlipidemia to lower triglycerides and cholesterol (1-8 grams a day) ----NOT niacinamide

    Seriou deficiency leads to a disease called pellagra (chronic alcoholism is major cause in US)
  222. Losartan and HCTZ - Hyzaar
    ARB and Thiazide Diuretic

    Indication: hypertension, stroke risk reduction in pts with HTN and left ventricular hypertrophy

    Sulfonamide derived drug
  223. Irbesartan - Avapro
    ARB

    MOA: angiotension receptor antagonist.

    Indications: hypertension alone or in combo with other antihypertensives, diabetic nephropathy in pts with type 2 diabetes, htn

    Unlabeled uses: slow the rate of aortic root dilation in pediatric patients with Marfan's syndrome
  224. Ipratropium and Albuterol - Combivent
    Anticholinergic Agent and Beta 2 agonist

    Indications: COPD in those pts who are currently on a regular bronchodilator who continue to have bronchospasms and require a 2nd bronchodilator
  225. Ethinyl Estradiol and Norethindrone - Loestrin 24Fe
    Contraceptive

    Indications: prevent pregnancy, tx of acne, moder to sever vasomotor sx associated with menopause, prevetion of osteoporosis

    Unlabeled uses: tx of hypermenorrhea, pain associated with endometriosis, dysmenorrhea, dysfunctional uterine bleeding
  226. Irbesartan and HCTZ - Avalide
    ARB and thiazide diuretic

    Indications: combo therapy for the management of htn
  227. Lidocaine - Lidoderm
    Topical Analgesic

    MOA: blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with reultant blockade of conduction

    Indications: relief of allodynia (painful hypersensitivity) and chronic pain in postherpetic neuralgia
  228. Thyroid desiccated- Armour
    Thyroid product

    MOA: exact mechanism is unknown, T4 is converted from T3

    Indications: replacement or supplemental therapy in hypothyroidism
  229. Moxifloxacin - Vigamox
    Opthalmic quinolone antibiotic

    MOA: DNA gyrase inhibitor and inhibits topoisomerase IV.

    Indications: Treatment of bacterial conjunctivitis caused by susceptible organisms
  230. Influenza Virus Vaccine (inactivated) - Fluvirin, Fluzone
    MOA: promotes immunity to seasonal influenza virus by inducing specfic antibody production.

    Indications: Provide active immunity to influenza virus

    May experience N/V. diarrhea, flu- like sx and redness & tenderness at injection site
  231. Hydrocodone and Chlorpheniramine - Tussionex
    Hydrocodone (analgesic, antitussive) and Chlorpheniramine (1st generation histamine h1 antagonist)

    MOA: Suppresses cough in medullary center and competes with histamine for h1-receptor sites
  232. Amlodipine and Benzapril - Lotrel
    ACEI and dihydropyridine Ca channel

    MOA: Inhibits transmembrane influx of ca ions into vascular smooth muscle and cardiac muscle producing relaxation of coronary vasodilation and suppresses RAAS
  233. Estrogens (conjugated/equine) and medroxyprogesterone - Prempro
    Estrogen and Progestin combo

    Indications: women with an intact uterus: tx of moderate to sever vasomoter sx associated with menopause, tx of moderate to severe vulvuar and vaginal atrophy due to menopause, postmenopausal osteoporosis
  234. Dexmethylphenidate - Focalin XR
    CNS stimulant

    MOA: the more active d-threo-enantiomer or racemic methylphenidate. CNS stimulant blocks the reuptake of NE and dopamine and increases their release ino the extraneuronal space

    Indications: ADHD

    Response may take time, may experience decreased appetite or weight loss, restlessness, impaired judgment, HA, dry mouth or dizziness. Report unresolved rapid heartbeat, chest pain, difficutly breathing, excessive agitation, nervousness, insomnia, tremors, dizziness, or skin rash
  235. Ethyinyl Estradiol and Desogetrel - Kariva, Apri
    Contraceptive

    Indications: prevention of pregnancy

    Unlabeld uses: tx of hypermenorrhea, pain associated with endometriosis, dysmenorrhea, dysfunctional uterine bleeding
  236. Amlodipine and Valsartan - Exforge
    ARB and Dihydropyridine Ca channel blocker

    • MOA: Inhibits transmembrane influx of ca ions into vascular smooth
    • muscle and cardiac muscle producing relaxation of coronary vasodilation
    • and suppresses RAAS

    Indications: htn
  237. Amlodipine and Atorvastatin
    HMG-CoA and Dihydropyridine Ca blocker

    Indications: for use when tx with both is appropriate

    • Amlodipine: htn, chronic stable angina
    • Atorvasatatin: dyslipidemias or primary prevention of cardivascular disease
  238. Olopatadine - Patanol
    Opthalmic 2nd generation H1 histamine antagonist

    MOA: selective histamine H1-antagonist, inhibits release of histamine from mast cells. inhibits histamine induced effects on conjuctival epithelial cells

    Indications: tx of the signs and sx of allergic conjuncitvitis

    For eyes only, do not let tip touch eye, do not wear contacts if eyes are red, can cause cold-like symptoms and HA
  239. Ciprofloxacin and Dexamethasone - Ciprodex
    Antibiotic and corticosteriod

    MOA: cipro is quinolone antibiotic, dexamethasone is a corticosteriod used to decrease inflammatin accompanying bacterial infections

    Indications: tx of otitis media in pediatric patients with typanostomy tubes or acute otitis externa in children and adults
  240. Brimonidone - Alphagan P
    Alpha 2 agonist ophthalmic agent (antiglaucoma)

    MOA: selective antagonism for alpha 2 receptors causes reduction of aqueous humor formation and increased uveoscleral outflow

    Indications: lowering of intraocular pressure in pts with open angle glaucoma or ocular htn
  241. Fenofibric acid - Trilipix
    Antilipemic Agent

    MOA: downregulates apoprotein c-III and upregulates the synthesis of apolipoprotein A-I, fattty acidt transport protein, and lipoprotein lipase resulting in an increase in VLDL catabolism, fatty acid oxidation, and elimination of triglyceride rich particles

    Indications: adjunct to dietary therapy for tx of severly elevated serum triglyceride levels, to increase HDL, reduce LDL, and total cholesterol
  242. Progesterone - Prometrium
    MOA: natural steriod hormone that induces secretory changes in the endometrium, promotes mammary gland development, relaxes uterine smooth muscle, blocks follicular maturation and ovulation, and maintains pregnancy. When uses as part of an ART program in the luteal phase, progesterone supports embryo implantation.

    Indications: prevention of endometrial hyperplasia in nonhysterectomized postmenopausal women who are receiving estrogen, secondary amenorrhea, abnormal uterine bleeding, part of assisted reproductive technology for infertile women
  243. Insulin Detemir - Levemir
    Intermediate to long acting insulin

    MOA: intermediate to long acting insulin analog

    Indications: tx of type 1 diabetes and type 2 to improve glycemic control
  244. Budesonide - Pulmicort Respules
    Corticosteriod

    MOA: Controls the rate of protein synthesis, depresses the migration of leukocytes, fibroblasts; reverses capillary permeability and lysosomal staabilization at the cellular level to prevent or contol inflammation. Has potent glucocorticoid activity and weak mineralcorticoid activity

    Indications: asthma, active crohns disease (oral)
  245. Azelastine - Astelin
    2nd generation Histamine H1 antagonist

    MOA: Histamine H1 receptor competitor

    Indications: tx of seasonal allergic rhinitis and nasal pruritis, vasomotor rhinitis, eye itching
  246. Testosterone - AndroGel
    Androgen

    MOA: principal endogenous androgen responsible for promoting the growth and development of the male sex organs and maintaining secondary sex characteristics in androgen deficient males
  247. Fluticasone - Veramyst
    Corticosteriod
  248. Estradiol - Vagifem
    Estrogen Derivative

    MOA: in studies for vulvar and vaginal atrophy in postmenopausal women, local estrogens have been shown to reduce vagina pH levels and mature the vaginal and urethral mucosa after 12 weeks of therapy, therby impoving vaginal dryness and mucosal atrophy

    Indications: tx of moderate to severe vulvar and vaginal atrophy associated with menopause
  249. Pioglitazone and Metformin - Actosplus Met
    Biguanide and thiazolidinedione- antidiabetic agent

    • MOA:
    • Pioglitazone is a thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity.
    • Metformin decreases hepatic glucose production, decreasing intestinal absorption of glucose, and improves insulin sensitivity (increases peripheral glucose uptake and utilization).

    Indications: Management of type 2 diabetes mellitus (noninsulin dependent, NIDDM)
  250. Polyethylene Glycol-Electrolyte Solution and Bisacodyl - Halflytely Bowel Prep
    Laxative, bowel evacuant

    • MOA: Bisacodyl acts on the colonic mucosa to increase peristalsis throughout
    • the large intestine.
    • Polyethylene glycol-electrolyte solution induces
    • catharsis through strong electrolyte and osmotic effects.

    Indications: Bowel cleansing prior to colonoscopy
  251. Mesalamine - Asacol
    5-Aminosalicylic Acid Derivative

    • MOA: Mesalamine (5-aminosalicylic acid) is the active component of
    • sulfasalazine; the specific mechanism of action of mesalamine is
    • unknown; however, it is thought that it modulates local chemical mediators of the inflammatory response, especially leukotrienes, and is
    • also postulated to be a free radical scavenger or an inhibitor of tumor necrosis factor (TNF); action appears topical rather than systemic

    Indications: ulcertive colitis
  252. Epinephrine - Epipen
    Alpha/Beta Agonist

    MOA: Stimulates alpha-, beta1-, and beta2-adrenergic receptors resulting in relaxation of smooth muscle of the bronchial tree, cardiac stimulation (increasing myocardial oxygen consumption), and dilation of skeletal muscle vasculature; small doses can cause vasodilation via beta2-vascular receptors; large doses may produce constriction of skeletal and vascular smooth muscle

    • Indications: reatment of bronchospasms, bronchial asthma, viral croup, anaphylactic
    • reactions, cardiac arrest; added to local anesthetics to decrease
    • systemic absorption of intraspinal and local anesthetics and increase duration of action; decrease superficial hemorrhage
  253. Desloratadine - Clarinex
    2nd generation Histamine H1 antagonist

    MOA: Desloratadine, a major metabolite of loratadine, is a long-acting tricyclic antihistamine with selective peripheral histamine H1 receptor antagonistic activity and additional anti-inflammatory properties.

    • Indications: Relief of nasal and non-nasal symptoms of seasonal allergic rhinitis
    • (SAR) and perennial allergic rhinitis (PAR); treatment of chronic idiopathic urticaria (CIU)
  254. Gatifloxacin - Zymar
    Quinolone opthalmic antibiotic

    MOA: Gatifloxacin is a DNA gyrase inhibitor, and also inhibits topoisomerase IV. DNA gyrase (topoisomerase II) is an essential bacterial enzyme that maintains the superhelical structure of DNA. DNA gyrase is required for DNA replication and transcription, DNA repair, recombination, and transposition; inhibition is bactericidal.

    Indications: Treatment of bacterial conjunctivitis
  255. Alfuzosin - Urozatral
    Alpha 1 blocker

    MOA: An antagonist of alpha1-adrenoreceptors in the lower urinary tract. Smooth muscle tone is mediated by the sympathetic nervous stimulation of alpha1-adrenoreceptors,which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade of these adrenoreceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and a reduction in BPH symptoms.

    Indications: Treatment of the functional symptoms of benign prostatic hyperplasia (BPH)
  256. Clindamycin and Benzoyl Peroxide -BenzaClin
    Topical Acne product

    • MOA: Clindamycin and benzoyl peroxide have activity against Propionibacterium acnes in vitro.
    • This organism has been associated with acne vulgaris. Benzoyl peroxide releases free-radical oxygen which oxidizes bacterial proteins in the sebaceous follicles decreasing the number of anaerobic bacteria and decreasing irritating-type free fatty acids. Clindamycin reversibly binds to 50S ribosomal subunits preventing peptide bond formation thus inhibiting bacterial protein synthesis; bacteriostatic or bactericidal depending on drug concentration, infection site, and organism.

    Indications: Topical treatment of acne vulgaris
  257. Beclomethasone (Oral Inhalation) -Qvar
    Corticosteriod

    • MOA: Controls the rate of protein synthesis; depresses the migration of polymorphonuclear leukocytes, fibroblasts; reverses capillary
    • permeability and lysosomal stabilization at the cellular level to prevent or control inflammation

    Indication: Oral inhalation: Maintenance and prophylactic treatment of asthma; includes those who require corticosteroids and those who may benefit from a dose reduction/elimination of systemically-administered corticosteroids. Not for relief of acute bronchospasm.
  258. Amlodipine and Olmesartan - Azor
    ARB and Dihydropyridine Ca Blocker

    Indications: Treatment of hypertension, including initial treatment in patients who will require multiple antihypertensives for adequate control
  259. Polyethylene Glycol-Electrolyte Solution -Moviprep
    Osmotic laxative

    MOA: Induces catharsis by strong electrolyte and osmotic effects

    Indications: Bowel cleansing prior to GI examination
  260. Letrozole - Femara
    Aromatase Inhibitor

    MOA: Nonsteroidal competitive inhibitor of the aromatase enzyme system which binds to the heme group of aromatase, a cytochrome P450 enzyme which catalyzes conversion of androgens to estrogens (specifically, androstenedione to estrone and testosterone to estradiol). This leads to inhibition of the enzyme and a significant reduction in plasma estrogen(estrone, estradiol and estrone sulfate) levels. Does not affect synthesis of adrenal or thyroid hormones, aldosterone, or androgens.

    • Indications: For use in postmenopausal women in the adjuvant treatment of hormone receptor positive early breast cancer, extended adjuvant treatment of early breast cancer after 5 years of tamoxifen, advanced breast cancer with disease progression following antiestrogen therapy, hormone receptor positive or hormone receptor unknown, locally-advanced, or first-line (or second-line) treatment of advanced or metastatic breast
    • cancer
  261. Nitroglycerin - Nitrostat
    Vasodilator

    MOA: Nitroglycerin forms free radical nitric oxide. In smooth muscle, nitric oxide activates guanylate cyclase which increases guanosine 3’5’ monophosphate (cGMP) leading to dephosphorylation of myosin light chains and smooth muscle relaxation. Produces a vasodilator effect on the peripheral veins and arteries with more prominent effects on the veins. Primarily reduces cardiac oxygen demand by decreasing preload (left ventricular end-diastolic pressure); may modestly reduce afterload; dilates coronaryarteries and improves collateral flow to ischemic regions

    Indications: Short-term management of pulmonary hypertension (I.V.); esophageal spastic disorders
  262. Tacrolimus (Systemic) - Prograf
    Calcineurin inhibitor, immunosuppressant

    • MOA: Suppresses cellular immunity (inhibits T-lymphocyte activation), by binding to an intracellular protein, FKBP-12 and complexes with
    • calcineurin dependent proteins to inhibit calcineurin phosphatase activity

    Indication: Prevention of organ rejection in heart, kidney, or liver transplant recipients
  263. Emtricitabine and Tenofovir - Truvada
    Antiretroviral Agent, Reverse Transcriptase Inhibitor (Nucleoside); Antiretroviral Agent, Reverse Transcriptase Inhibitor (Nucleotide)

    • MOA:
    • Nucleoside and nucleotide reverse transcriptase inhibitor combination;
    • emtricitabine is a cytosine analogue while tenofovir disoproxil fumarate
    • (TDF) is an analog of adenosine 5'-monophosphate. Each drug interferes
    • with HIV viral RNA dependent DNA polymerase resulting in inhibition of
    • viral replication.

    • Indication:
    • Treatment of HIV infection in combination with other antiretroviral agents
  264. Brimonidine and Timolol- Combigan
    Alpha2 Agonist, Ophthalmic; Beta Blocker, Nonselective; Ophthalmic Agent, Antiglaucoma

    • MOA:
    • Brimonidine: Selective agonism for alpha2-receptors; causes reduction of aqueous humor formation and increased uveoscleral outflowTimolol: Blocks both beta1- and beta2-adrenergic
    • receptors, reduces intraocular pressure by reducing aqueous humor
    • production or possibly outflow; reduces blood pressure by blocking
    • adrenergic receptors and decreasing sympathetic outflow, produces a
    • negative chronotropic and inotropic activity by blocking beta1-adrenergic receptors

    • Indications:
    • Reduction of intraocular pressure (IOP) in patients with glaucoma or ocular hypertension
  265. Omeprazole and Sodium Bicarbonate - Zegerid
    Proton Pump Inhibitor; Substituted Benzimidazole

    • MOA:
    • Suppresses gastric basal and stimulated acid secretion by inhibiting the parietal cell H+/K+ ATP pump

    • Indications:
    • Short-term (4-8 weeks)
    • treatment of active duodenal ulcer or active benign gastric ulcer;
    • treatment of heartburn and other symptoms associated with
    • gastroesophageal reflux disease (GERD); short-term (4-8 weeks) treatment
    • of endoscopically-diagnosed erosive esophagitis; maintenance healing of
    • erosive esophagitis; reduction of risk of upper gastrointestinal
    • bleeding in critically-ill patientsOTC labeling: Short-term (2 weeks) treatment of frequent (2 days/week), uncomplicated heartburn
  266. Clonidine - Catapres TTS
    Alpha2-Adrenergic Agonist

    • MOA:
    • Stimulates alpha2-adrenoceptors in the brain stem, thus
    • activating an inhibitory neuron, resulting in reduced sympathetic
    • outflow from the CNS, producing a decrease in peripheral resistance,
    • renal vascular resistance, heart rate, and blood pressure; epidural
    • clonidine may produce pain relief at spinal presynaptic and
    • postjunctional alpha2-adrenoceptors by preventing pain signal
    • transmission; pain relief occurs only for the body regions innervated
    • by the spinal segments where analgesic concentrations of clonidine
    • exist. For the treatment of ADHD, the mechanism of action is unknown; it
    • has been proposed that postsynaptic alpha2-agonist stimulation
    • regulates subcortical activity in the prefrontal cortex, the area of the
    • brain responsible for emotions, attentions, and behaviors and causes
    • reduced hyperactivity, impulsiveness, and distractibility.

    • Indications:
    • Transdermal patch: Management of hypertension (monotherapy or as adjunctive therapy)
  267. Loteprednol - Lotemax
    Corticosteroid, Ophthalmic

    • MOA:
    • Corticosteroids
    • inhibit the inflammatory response including edema, capillary dilation,
    • leukocyte migration, and scar formation. Loteprednol is highly lipid
    • soluble and penetrates cells readily to induce the production of
    • lipocortins. These proteins modulate the activity of prostaglandins and
    • leukotrienes.

    • Indications:
    • Temporary relief of signs and symptoms of seasonal allergic conjunctivitis
  268. Repaglinide - Prandin
    Antidiabetic Agent, Meglitinide Derivative

    • MOA:
    • Nonsulfonylurea hypoglycemic agent which blocks ATP-dependent potassium
    • channels, depolarizing the membrane and facilitating calcium entry
    • through calcium channels. Increased intracellular calcium stimulates
    • insulin release from the pancreatic beta cells. Repaglinide-induced
    • insulin release is glucose-dependent.

    • Indications:
    • Management of type 2 diabetes mellitus (noninsulin dependent, NIDDM) as
    • an adjunct to diet and exercise; may be used in combination with
    • metformin or thiazolidinediones
  269. Ritonavir - Norvir
    Antiretroviral Agent, Protease Inhibitor

    • MOA:
    • Binds to the site of HIV-1 protease activity and inhibits cleavage of
    • viral Gag-Pol polyprotein precursors into individual functional proteins
    • required for infectious HIV. This results in the formation of immature,
    • noninfectious viral particles.

    • Indications:
    • Treatment
    • of HIV infection; should always be used as part of a multidrug regimen
    • (at least three antiretroviral agents); may be used as a pharmacokinetic
    • "booster" for other protease inhibitors
  270. Scopolamine (Systemic)
    Anticholinergic Agent

    • MOA:
    • Blocks the action of acetylcholine at parasympathetic sites in smooth
    • muscle, secretory glands and the CNS; increases cardiac output, dries
    • secretions, antagonizes histamine and serotonin

    • Indications:
    • Transdermal: Prevention of nausea/vomiting associated with motion sickness and recovery from anesthesia and surgery
  271. Dexlansoprazole - Kapidex
    Proton Pump Inhibitor; Substituted Benzimidazole

    • MOA:
    • Proton pump inhibitor; decreases acid secretion in gastric parietal
    • cells through inhibition of (H+, K+)-ATPase enzyme system, blocking the
    • final step in gastric acid production

    • Indications:
    • Short-term (4 weeks) treatment of heartburn associated with nonerosive
    • GERD; short-term (up to 8 weeks) treatment of all grades of erosive
    • esophagitis; to maintain healing of erosive esophagitis for up to 6
    • months
  272. Trazadone- Oleptro
    Antidepressant, Serotonin Reuptake Inhibitor/Antagonist

    • MOA:
    • Inhibits reuptake of serotonin, causes adrenoreceptor subsensitivity,
    • and induces significant changes in 5-HT presynaptic receptor
    • adrenoreceptors. Trazodone also significantly blocks histamine (H1) and alpha1-adrenergic receptors.

    • Indications:
    • Treatment of major depressive disorder
  273. Promethazine - Phenadoz®; Phenergan®; Promethegan™
    Antiemetic; Histamine H1 Antagonist; Histamine H1 Antagonist, First Generation; Phenothiazine Derivative

    • MOA:
    • Phenothiazine derivative; blocks postsynaptic mesolimbic dopaminergic
    • receptors in the brain; exhibits a strong alpha-adrenergic blocking
    • effect and depresses the release of hypothalamic and hypophyseal
    • hormones; competes with histamine for the H1-receptor;
    • muscarinic-blocking effect may be responsible for antiemetic activity;
    • reduces stimuli to the brainstem reticular system

    • Indication:
    • Symptomatic treatment of various allergic conditions; antiemetic; motion
    • sickness; sedative; adjunct to postoperative analgesia and anesthesia
  274. Respiridone - RisperDAL®; RisperDAL® Consta®; RisperDAL® M-Tab®
    Antimanic Agent; Antipsychotic Agent, Atypical

    • MOA:
    • Risperidone is a benzisoxazole atypical antipsychotic with mixed serotonin-dopamine antagonist activity that binds to 5-HT2-receptors in the CNS and in the periphery with a very high affinity; binds to dopamine-D2 receptors with less affinity. The binding affinity to the dopamine-D2 receptor is 20 times lower than the 5-HT2
    • affinity. The addition of serotonin antagonism to dopamine antagonism
    • (classic neuroleptic mechanism) is thought to improve negative symptoms
    • of psychoses and reduce the incidence of extrapyramidal side effects.
    • Alpha1, alpha2 adrenergic, and histaminergic
    • receptors are also antagonized with high affinity. Risperidone has low
    • to moderate affinity for 5-HT1C, 5-HT1D, and 5-HT1A receptors, weak affinity for D1 and no affinity for muscarinics or beta1 and beta2 receptors

    • Indication:
    • Treatment of schizophrenia; treatment of acute mania or mixed episodes
    • associated with bipolar I disorder (as monotherapy in children or
    • adults, or in combination with lithium or valproate in adults);
    • treatment of irritability/aggression associated with autistic disorder
  275. Clindamycin - Cleocin HCl®; Cleocin Pediatric®; Cleocin Phosphate®
    Antibiotic, Lincosamide

    • MOA:
    • Reversibly
    • binds to 50S ribosomal subunits preventing peptide bond formation thus
    • inhibiting bacterial protein synthesis; bacteriostatic or bactericidal
    • depending on drug concentration, infection site, and organism

    • Indications:
    • Treatment of susceptible bacterial infections, mainly those caused by
    • anaerobes, streptococci, pneumococci, and staphylococci; pelvic
    • inflammatory disease (I.V.)
  276. Ethinyl Estradiol and Norgestimate -Tri-sprintec
    Contraceptive; Estrogen and Progestin Combination

    • MOA:
    • Combination hormonal contraceptives inhibit ovulation via a negative
    • feedback mechanism on the hypothalamus, which alters the normal pattern
    • of gonadotropin secretion of a follicle-stimulating hormone (FSH) and
    • luteinizing hormone by the anterior pituitary. The follicular phase FSH
    • and midcycle surge of gonadotropins are inhibited. In addition,
    • combination hormonal contraceptives produce alterations in the genital
    • tract, including changes in the cervical mucus, rendering it unfavorable
    • for sperm penetration even if ovulation occurs. Changes in the
    • endometrium may also occur, producing an unfavorable environment for
    • nidation. Combination hormonal contraceptive drugs may alter the tubal
    • transport of the ova through the fallopian tubes. Progestational agents
    • may also alter sperm fertility.

    • Indications:
    • Prevention of pregnancy; treatment of acne
  277. Phentermine - Adipex-P
    Anorexiant; Sympathomimetic

    • MOA:
    • Phentermine is a sympathomimetic amine with pharmacologic properties
    • similar to the amphetamines. The mechanism of action in reducing
    • appetite appears to be secondary to CNS effects, including stimulation
    • of the hypothalamus to release norepinephrine.

    • Indications:
    • Short-term (few weeks) adjunct therapy in obese patients with an initial body mass index (BMI) ≥30 kg/m2 or ≥27 kg/m2
    • in the presence of other risk factors (eg, diabetes, hyperlipidemia,
    • hypertension); therapy should be used in conjunction with a
    • comprehensive weight management program.
  278. Mirtzapine - Remeron
    Antidepressant, Alpha-2 Antagonist

    • MOA:
    • Mirtazapine is a tetracyclic antidepressant that works by its central presynaptic alpha2-adrenergic
    • antagonist effects, which results in increased release of
    • norepinephrine and serotonin. It is also a potent antagonist of 5-HT2 and 5-HT3 serotonin receptors and H1 histamine receptors and a moderate peripheral alpha1-adrenergic and muscarinic antagonist; it does not inhibit the reuptake of norepinephrine or serotonin.

    • Indications:
    • Treatment of depression
  279. Guaifenesin - Cheratussin AC
    Expectorant

    • MOA:
    • Thought to act as an expectorant by irritating the gastric mucosa and
    • stimulating respiratory tract secretions, thereby increasing respiratory
    • fluid volumes and decreasing mucous viscosity

    • Indications:
    • Help loosen phlegm and thin bronchial secretions to make coughs more productive
  280. Meclizine - Atrivert, Bonine
    Antiemetic; Histamine H1 Antagonist; Histamine H1 Antagonist, First Generation; Piperazine Derivative

    • MOA:
    • Has central anticholinergic action by blocking chemoreceptor trigger
    • zone; decreases excitability of the middle ear labyrinth and blocks
    • conduction in the middle ear vestibular-cerebellar pathways

    • Indications:
    • Prevention and treatment of symptoms of motion sickness; management of vertigo with diseases affecting the vestibular system
  281. Polyethylene glycol - Dulcolax Balance® [OTC]; MiraLAX® [OTC]
    Laxative, Osmotic

    • MOA:
    • An osmotic agent, polyethylene glycol 3350 causes water retention in the stool; increases stool frequency.

    • Indications:
    • Treatment of occasional constipation in adults
  282. Betamethasone and Clotrimazole -Lotrisone®
    Antifungal Agent, Topical; Corticosteroid, Topical

    • MOA:
    • Betamethasone
    • dipropionate is a corticosteroid which controls the rate of protein
    • synthesis; depresses the migration of polymorphonuclear leukocytes,
    • fibroblasts; reverses capillary permeability and lysosomal stabilization
    • at the cellular level to prevent or control inflammation. Clotrimazole
    • is an antifungal agent that binds to phospholipids in the fungal cell
    • membrane altering cell wall permeability resulting in loss of essential
    • intracellular elements.

    • Indication:
    • Topical treatment of various dermal fungal infections (including tinea pedis, cruris, and corpora in patients ≥17 years of age)
  283. Butalbital, Acetaminophen, and Caffeine - Alagesic LQ; Alagesic [DSC]; Anolor 300; Dolgic® Plus; Esgic-Plus™; Esgic®; Fioricet®; Margesic; Orbivan™; Repan®; Zebutal®
    Barbiturate

    • MOA:
    • Butalbital
    • is a short- to intermediate-acting barbiturate. Barbiturates depress
    • the sensory cortex, decrease motor activity, alter cerebellar function,
    • and produce drowsiness, sedation, hypnosis, and dose-dependent
    • respiratory depression. Acetaminophen
    • inhibits the synthesis of prostaglandins in the central nervous system
    • and peripherally blocks pain impulse generation; produces antipyresis
    • from inhibition of hypothalamic heat-regulating center Caffeine
    • increases levels of 3'5' cyclic AMP by inhibiting phosphodiesterase;
    • CNS stimulant which increases medullary respiratory center sensitivity
    • to carbon dioxide, stimulates central inspiratory drive, and improves
    • skeletal muscle contraction (diaphragmatic contractility)

    • Indications:
    • Relief of the symptomatic complex of tension or muscle contraction headache
  284. Ferrous Sulfate - Feosol® [OTC]; Fer-In-Sol® [OTC]; Fer-iron [OTC]; MyKidz Iron 10™ [OTC]; Slow FE® [OTC]
    Iron Salt

    • MOA:
    • Replaces iron, found in hemoglobin, myoglobin, and other enzymes; allows the transportation of oxygen via hemoglobin

    • Indications:
    • Prevention and treatment of iron-deficiency anemias
  285. Omega-3-Acid Ethyl Esters - Lovaza
    Antilipemic Agent

    • MOA:
    • Mechanism has not been completely defined. Possible mechanisms include
    • inhibition of acyl CoA:1,2 diacylglycerol acyltransferase, increased
    • hepatic beta-oxidation, a reduction in the hepatic synthesis of
    • triglycerides, or an increase in plasma lipoprotein lipase activity.

    • Indications:
    • Lovaza®: Adjunct to diet therapy in the treatment of hypertriglyceridemia (≥500 mg/dL)
  286. Tizanidine HCl - Zanaflex Capsules®; Zanaflex®
    Alpha2-Adrenergic Agonist

    • MOA:
    • An alpha2-adrenergic agonist agent which decreases excitatory
    • input to alpha motor neurons; an imidazole derivative
    • chemically-related to clonidine, which acts as a centrally acting muscle
    • relaxant with alpha2-adrenergic agonist properties; acts on the level of the spinal cord

    • Indications:
    • Skeletal muscle relaxant used for treatment of muscle spasticity

    Tension headaches, low back pain, and trigeminal neuralgia
  287. Methocarbamol - Robaxin®; Robaxin®-750
    Skeletal Muscle Relaxant

    • MOA:
    • Causes skeletal muscle relaxation by general CNS depression

    • Indications:
    • Adjunctive treatment of muscle spasm associated with acute painful musculoskeletal conditions (eg, tetanus)
  288. Clobetasol - Adjunctive treatment of muscle spasm associated with acute painful musculoskeletal conditions (eg, tetanus)
    Corticosteroid, Topical

    • MOA:
    • Stimulates the synthesis of enzymes needed to decrease inflammation, suppress mitotic activity, and cause vasoconstriction

    • Indications:
    • Short-term relief of inflammation of moderate-to-severe
    • corticosteroid-responsive dermatoses (very high potency topical
    • corticosteroid)
  289. Chlorhexidine gluconate - Avagard™
    [OTC]; Bactoshield® CHG [OTC]; Betasept® [OTC]; ChloraPrep® Frepp®
    [OTC]; ChloraPrep® Sepp® [OTC]; ChloraPrep® [OTC]; Chlorascrub™ Maxi
    [OTC]; Chlorascrub™ [OTC]; Dyna-Hex® [OTC]; Hibiclens® [OTC]; Hibistat®
    [OTC]; Operand® Chlorhexidine Gluconate [OTC]; Peridex®; PerioChip®; PerioGard® [OTC]
    Antibiotic, Oral Rinse; Antibiotic, Topical

    • MOA:
    • The
    • bactericidal effect of chlorhexidine is a result of the binding of this
    • cationic molecule to negatively charged bacterial cell walls and
    • extramicrobial complexes. At low concentrations, this causes an
    • alteration of bacterial cell osmotic equilibrium and leakage of
    • potassium and phosphorous resulting in a bacteriostatic effect. At high
    • concentrations of chlorhexidine, the cytoplasmic contents of the
    • bacterial cell precipitate and result in cell death.

    • Indications:
    • Skin cleanser for line
    • placement, skin wounds, preoperative skin preparation; germicidal hand
    • rinse; antibacterial dental rinse. Chlorhexidine is active against
    • gram-positive and gram-negative organisms, facultative anaerobes,
    • aerobes, and yeast. Orphan drug: Peridex®: Oral mucositis with cytoreductive therapy when used for patients undergoing bone marrow transplant
  290. Ropinirole HCl- Requip®; Requip® XL™
    Anti-Parkinson's Agent, Dopamine Agonist

    • MOA:
    • Ropinirole has a high relative in vitro specificity and full intrinsic activity at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4 receptor subtypes; relevance of D3 receptor binding in Parkinson's disease is unknown. Ropinirole has moderate in vitro affinity for opioid receptors. Ropinirole and its metabolites have negligible in vitro affinity for dopamine D1, 5-HT1, 5-HT2, benzodiazepine, GABA, muscarinic, alpha1-, alpha2-,
    • and beta-adrenoreceptors. Although precise mechanism of action of
    • ropinirole is unknown, it is believed to be due to stimulation of
    • postsynaptic dopamine D2-type receptors within the caudate
    • putamen in the brain. Ropinirole caused decreases in systolic and
    • diastolic blood pressure at doses >0.25 mg. The mechanism of
    • ropinirole-induced postural hypotension is believed to be due to D2-mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.

    • Indications:
    • Treatment of idiopathic Parkinson's disease; in patients with early
    • Parkinson's disease who were not receiving concomitant levodopa therapy
    • as well as in patients with advanced disease on concomitant levodopa;
    • treatment of moderate-to-severe primary Restless Legs Syndrome (RLS)
  291. Dicyclomine HCl - Bentyl®
    Anticholinergic Agent

    • MOA:
    • Blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands and the CNS

    • Indications:
    • Treatment of functional bowel/irritable bowel syndrome
  292. Phenazopyridine HCl - AZO Standard® Maximum Strength [OTC]; AZO Standard® [OTC]; Azo-Gesic™
    [OTC]; Baridium [OTC]; Pyridium®; ReAzo [OTC]; UTI Relief® [OTC]
    Analgesic, Urinary

    • MOA:
    • An azo dye which exerts local anesthetic or analgesic action on urinary tract mucosa through an unknown mechanism

    • Indications:
    • Symptomatic
    • relief of urinary burning, itching, frequency, and urgency in
    • association with urinary tract infection or following urologic
    • procedures
  293. Ethinyl Estradiol and Levonorgestrel - Aviane
    Contraceptive; Estrogen and Progestin Combination

    • MOA:
    • Combination hormonal contraceptives inhibit ovulation via a negative
    • feedback mechanism on the hypothalamus, which alters the normal pattern
    • of gonadotropin secretion of a follicle-stimulating hormone (FSH) and
    • luteinizing hormone by the anterior pituitary. The follicular phase FSH
    • and midcycle surge of gonadotropins are inhibited. In addition,
    • combination hormonal contraceptives produce alterations in the genital
    • tract, including changes in the cervical mucus, rendering it unfavorable
    • for sperm penetration even if ovulation occurs. Changes in the
    • endometrium may also occur, producing an unfavorable environment for
    • nidation. Combination hormonal contraceptive drugs may alter the tubal
    • transport of the ova through the fallopian tubes. Progestational agents
    • may also alter sperm fertility.

    • Indications:
    • Prevention of pregnancy; postcoital contraception
  294. Lecetiracetam - Keppra
    Anticonvulsant,

    • MOA:
    • The precise mechanism by which levetiracetam exerts its antiepileptic
    • effect is unknown. However, several studies have suggested the mechanism
    • may involve one or more of the following central pharmacologic effects:
    • inhibition of voltage-dependent N-type calcium channels; facilitation
    • of GABA-ergic inhibitory transmission through displacement of negative
    • modulators; reduction of delayed rectifier potassium current; and/or
    • binding to synaptic proteins which modulate neurotransmitter release.

    • Indications:
    • Adjunctive therapy in the treatment of partial onset, myoclonic, and/or primary generalized tonic-clonic seizures
  295. Felodipine - Plendil®; Renedil®
    Calcium Channel Blocker; Calcium Channel Blocker, Dihydropyridine

    • MOA:
    • Inhibits
    • calcium ions from entering the “slow channels” or select
    • voltage-sensitive areas of vascular smooth muscle and myocardium during
    • depolarization, producing a relaxation of coronary vascular smooth
    • muscle and coronary vasodilation; increases myocardial oxygen delivery
    • in patients with vasospastic angina

    • Indications:
    • Treatment of hypertension
  296. Fluocinonide - Vanos™
    Corticosteroid, Topical´╗┐

    • MOA:
    • Fluorinated
    • topical corticosteroid considered to be of high potency. The mechanism
    • of action for all topical corticosteroids is not well defined, however,
    • is felt to be a combination of three important properties:
    • anti-inflammatory activity, immunosuppressive properties, and
    • antiproliferative actions.

    • Indications:
    • Anti-inflammatory,
    • antipruritic; treatment of plaque-type psoriasis (up to 10% of body
    • surface area) [high-potency topical corticosteroid]
  297. Etodolac
    Nonsteroidal Anti-inflammatory Drug (NSAID), Oral

    • MOA:
    • Reversibly inhibits
    • cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, which results in decreased
    • formation of prostaglandin precursors; has antipyretic, analgesic, and
    • anti-inflammatory propertiesOther
    • proposed mechanisms not fully elucidated (and possibly contributing to
    • the anti-inflammatory effect to varying degrees), include inhibiting
    • chemotaxis, altering lymphocyte activity, inhibiting neutrophil
    • aggregation/activation, and decreasing proinflammatory cytokine levels.

    • Indications:
    • Acute and long-term use in the management of signs and symptoms of
    • osteoarthritis; rheumatoid arthritis and juvenile idiopathic arthritis
    • (JIA); management of acute pain
  298. Lithium Carbonate - Lithobid®
    Antimanic Agent

    • MOA:
    • Alters
    • cation transport across cell membrane in nerve and muscle cells and
    • influences reuptake of serotonin and/or norepinephrine; second messenger
    • systems involving the phosphatidylinositol cycle are inhibited;
    • postsynaptic D2 receptor supersensitivity is inhibited

    • Indications:
    • Potential augmenting agent for antidepressants; aggression, post-traumatic stress disorder, conduct disorder in children
  299. Fosinopril -
    ACEI

    • MOA:
    • Competitive
    • inhibitor of angiotensin-converting enzyme (ACE); prevents conversion
    • of angiotensin I to angiotensin II, a potent vasoconstrictor; results in
    • lower levels of angiotensin II which causes an increase in plasma renin
    • activity and a reduction in aldosterone secretion; a CNS mechanism may
    • also be involved in hypotensive effect as angiotensin II increases
    • adrenergic outflow from CNS; vasoactive kallikreins may be decreased in
    • conversion to active hormones by ACE inhibitors, thus reducing blood
    • pressure

    • Indications:
    • Treatment of hypertension, either alone or in combination with other antihypertensive agents; treatment of heart failure (HF)
  300. Doxepin - Silenor®
    Antidepressant, Tricyclic (Tertiary Amine)

    • MOA:
    • Increases the synaptic concentration of serotonin and norepinephrine in
    • the central nervous system by inhibition of their reuptake by the
    • presynaptic neuronal membrane; antagonizes the histamine (H1) receptor for sleep maintenance

    • Indications:
    • Depression; treatment of insomnia (with difficulty of sleep maintenance)
  301. Diltiazem - Cartia XT
    Antiarrhythmic Agent, Class IV; Calcium Channel Blocker; Calcium Channel Blocker, Nondihydropyridine

    • MOA:
    • Nondihydropyridine calcium channel blocker which inhibits calcium ion
    • from entering the “slow channels” or select voltage-sensitive areas of
    • vascular smooth muscle and myocardium during depolarization, producing a
    • relaxation of coronary vascular smooth muscle and coronary
    • vasodilation; increases myocardial oxygen delivery in patients with
    • vasospastic angina

    • Indications:
    • Oral: Essential hypertension; chronic stable angina or angina from coronary artery spasm Injection:
    • Control of rapid ventricular rate in patients with atrial fibrillation
    • or atrial flutter; conversion of paroxysmal supraventricular tachycardia
    • (PSVT)

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