pharm block 3

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pharm block 3
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  1. slope of decline in number of DA cells is sensitive to:
    encephalitis (spanish flu), arteriosclerosis (reducing blood flow), chemical exposures (CO, CN, methanol, Mg, MPTP, insecticides), brain trauma, autoimmune disease, exposure to antipsychotics, genetics?
  2. levodopa
    • enters brain via amino acid transporters and is converted into dopamine by LAAAD
    • two problems: too much dopamine in periphery and too little dopamine in CNS
    • to solve this, it is coadministered with carbidopa (inhibts LAAAD in the periphery
    • COMT inhibitors can be added to that pair
    • must take on an empty stomach
    • plasma half life is short 1-3 hours but the benefits outlast the half life
    • very effective especially for bradykinesia but only for a certain amount of time so wait to give until significant debilitation
    • side effects: wearing off, dyskinesias, hallucinations/confusion, GI, orthostatic hypotension
    • ADR: vit B6, MAOI (HTN), halothane (arrhythmias), typical antipsychotics 
    • contraindications: glaucoma, psychosis, cardiac arryhthmias, malignant melanoma
  3. carbidopa
    • inhibits LAAAD
    • does not cross BBB
    • coadministered with L-DOPA
    • decreases peripheral side effects
  4. pramipexole
    • D2 receptor agonist in striatum, given orally
    • better than L-DOPA because longer half life, isn't converted so more useful in late disease, selectivity of receptor is good for side effect control, can be titrated to therapeutic doses in a week or less
    • side effects: fatigue, narcolepsy, worse confusion but better dyskinesia
    • initial therapy for young patients (<60), on/off phenomenon
  5. ropinerole
    • D2 receptor agonist in striatum, given orally better than L-DOPA because longer half life, isn't converted so more useful in late disease, selectivity of receptor is good for side effect control, can be titrated to therapeutic doses in a week or less
    • side effects: fatigue, narcolepsy, worse confusion but better dyskinesia
    • initial therapy for young patients (<60), on/off phenomenon
  6. apomorphine
    • given as a subcutaneously as a rescue treatment for "off" episodes (severe hypokinesia) in PD
    • D4 receptor agonist
    • longer half life than L-DOPA
    • used more for young (<60 years) patients refractory to other treatments
    • side effects: nausea, fatigue, narcolepsy, worse confusion and better dyskinesia, can prolong QT syndrome
  7. selegiline
    • irreversible MAOB inhibitor (avoids inhibiting MAOA which is in liver and gut needed to metabolize tyramine)
    • potentiates endogenously produced dopamine and reduces oxidative stress of its breakdown
    • given when initially diagnosed with PD, has some anti-depressant effects
    • modest effect in slowing disease progression
    • can be given with L-DOPA to prolong its half life and decrease on/off effects
    • metabolized to amphetamine&methamphetamine-can lead to anxiety, insomnia (this is reduced when given as patch/orally disintegrating tablet)
    • ADR: drugs that elevate serotonin--leads to stupor, rigidity, agitation, hyperthermia
  8. rasagiline
    • irreversible MAOB inhibitor (avoids inhibiting MAOA which is in liver and gut needed to metabolize tyramine)
    • potentiates endogenously produced dopamine and reduces oxidative stress of its breakdown
    • given when initially diagnosed with PD, has some anti-depressant effects
    • modest effect in slowing disease progression
    • can be given with L-DOPA to prolong its half life and decrease on/off effects
    • ADR: drugs that elevate serotonin--leads to stupor, rigidity, agitation, hyperthermia
  9. entacapone
    • COMT inhibitor--increases L-DOPA access to brain and prolongs action of dopamine
    • short half life, only useful with co-administered L-DOPA because does not cross BBB
    • side effects: nausea, orthostatic hypotension, vivid dreams, confusion, hallucinations
  10. trihexyphenidyl
    • striatal muscarinic antagonist
    • 3rd line for PD, can be used early, in elderly, or with L-DOPA to decrease dose of L-DOPA
    • does not help bradykinesia
    • side effects: sedation, mental confusion, atropine like effects
  11. benztropine
    • striatal muscarinic antagonist
    • 3rd line for PD, can be used early, in elderly, or with L-DOPA to decrease dose of L-DOPA
    • does not help bradykinesia
    • side effects: sedation, mental confusion, atropine like effects
  12. amantadine
    • anti-viral that increases dopamine release (mildly anticholinergic, blocks NMDA receptors)
    • often given with L-DOPA (not useful if L-DOPA is ineffective) or anticholinergics
    • side effects: sleep disturbances, dizziness, lethargy, anticholinergic effects, peripheral edema
    • contraindicated with CHF (due to its sympathomimetic effects)
    • as an antiviral: prophylaxis against influenza A-reduces fever in 50% patients and ilness duration by 1-2 days if given in first 2 days
    • blocks viral uncoating by interfering with influenza A M2 protein
    • generally well tolerated but side effects are CNS (slured speech, anxiety, confusion, depression)
  13. donepezil, rivastigmine, galantamine
    AchEI  for dementia!
  14. memantine
    • NMDA receptor antagonist for dementia
    • associated with a reduced rate of clinical deterioration
  15. riluzole
    • for ALS
    • inhibits glutamate release, increases glutamate uptake, inhibits glutamate receptors
    • increases life span 2-3 months
  16. components of the anesthetic state
    • amnesia
    • unconsciousness
    • analgesia (inability to interpret, respond, remember pain)
    • immobility in response to  noxious stimuli
    • attenuation of autonomic responses to noxious stimuli
  17. MAC-minimal alveolar concentration
    • describes the potency of inhaled anesthetics--the concentration that will prevent movement as a response to pain in 50% of patients
    • can be continusouly monitored by end-tidal concentrations, provides a direct correlate to concentration at site of action in CNS, simple to measure the end-point
  18. sodium thiopental
    • activates GABAA receptor
    • used to induce anesthesia-takes 10-30 seconds and lasts for 10 minutes
    • barbituate
    • half life is 12 hours-produces a hang over
    • can be administerd rectally in peds patients
    • side effects: reduces cerebral O2 utilization and thus reduces cerebral blood flow (good for swelling of brain), produces vasodilation which produces severe BP lowering in patients unable to compensate for venodilation--hypovolemia, cardiomyopathy, respiratory depression (so put on ventilator)
    • dose should be reduced if other CNS depressants have been taken--alpha 2 agonists, opiates, benzodiazepines
  19. propofol
    • activates GABAA receptor
    • usually used to induce and maintain anesthesia for short procedures
    • takes 10-30 seconds to induce and lasts 10 minutes
    • anti-emetic
    • half life is 3 hours-good for outpatient surgery
    • side effects: pain on injection so given with lidocaine, excitation during induction, reduces cerebral O2 utilization, decreases BP more than thiopental (vasodilates, depresses contractility, blunts baroreceptor reflexes)
    • produces more respiratory depression than thiopental at equi-anesthetic doses
  20. etomidate
    • used to induce anesthesia in patients at risk for hypotension
    • side effects: pain and myoclonus so co-administered with lidocaine and premedicated with benzodiazepines/opiates, reduced cerebral O2 utilization, only produces small increase in HR, less respiratory depression than thiopental, ++vomiting and nausea than thiopental, increased post-surgical mortality due to suppression of adrenocortical stress response
  21. ketamine
    • NMDA receptor antagonist
    • produces dissociative anesthesia
    • profound analgesia, unresponsive to commands, amnesia, spontaneous respiration
    • side effects: nystagmus, salivation, spontaneous limb movements and increased muscle tone, increased intracranial pressure, hallucinations, illusions, increases BP
    • used for patients with bronchospasm, children having short, painful procedures
  22. midazolam
    • short acting benzodiazepine
    • used for conscious sedation, anxiolysis, amnesia for minor surgery
    • used as induction agent and adjunct during regional anesthesia (tooth extraction)
    • slower induction and longer duration than thiopental
    • side effects: respiratory depression/arrest especially when IV, should be cautious in patients with neuromuscular diease, PD, bipolar, dilates veins and so can cause severe BP drop in patients with hypovolemia and cardiomyopathy
  23. inhaled anesthetic properties
    • brain is well perfused, so anesthesia is reached when brain partial pressure is equal to MAC--shortly after MAC is reached in alveolae
    • occurs more quickly in agents that are less fat soluble
    • recovery from agents with low blood and tissue solubility is rapid and unrelated to length of anesthetic exposure!
    • recovery from agents with high blood and fat solubility is a function of duration of anesthetic administration
  24. isoflurane
    • inhaled anesthetic
    • moderate blood:gas partition coefficient
    • 99% excreted in lungs unchanged
    • can be for induction but mostly used for maintenance
    • co-administration with nitrous oxide allows a lower dose
    • side effects: respiratory irritant that causes coughing, decreases TV and increases respiratory rate, respiratory depressant, myocardial depression leading to decrease in BP, arrythmogenic because sensitizes the heart to catecholamines, increases intracranial pressure by dilating cerebral blood vessels
  25. desflurane
    • very volatile inhaled anesthetic
    • very low blood:gas partition coefficient
    • predominantly excreted unchanged
    • used for outpatient surgeries, produces direct skeletal muscle relaxation
    • side effects: causes coughing and bronchospasm in awake patients-respiratory irritant, decreases TV
    • and increases respiratory rate, respiratory depressant, myocardial depression leading to decrease in BP, arrythmogenic because sensitizes the heart to catecholamines, increases intracranial pressure by dilating cerebral blood vessels
  26. sevoflurane
    • very low blood:gas partition coefficient
    • 5% is metabolized to F- in the liver, can be degraded by absorbents in tubes if not careful
    • NOT A RESPIRATORY IRRITANT--inpatient and outpatient induction and maintenance
    • side effects: decreases TV and increases respiratory rate, less respiratory depression than others, myocardial
    • depression leading to decrease in BP, arrythmogenic because sensitizes the heart to catecholamines, increases intracranial pressure by dilating cerebral blood vessels
  27. nitrous oxide
    • very insoluble in blood-rapid induction and recovery
    • this rapid uptake will increase the concentration of other inhaled anesthetics so often co-administered
    • must be given 100% O2 when emerging because otherwise it will dilute the oxygen
    • 99% excretion in lungs
    • used to produce sedation and analgesia in dentistry-weak alone
    • contraindications: don't use in pneumothorax because can exhange nitrogen in any air space
    • negative inotrope but also sympatho-stimulant
  28. busiprone
    • 5-HT1A partial agonist, also binds D2
    • elimination half life 2-11 hours
    • less sedative effect than benzodiazepine
    • used to treat generalized anxiety syndrome-may take 1-2 weeks for effect
    • doesn't potentiate other sedatives/depressants, has no cross tolerance with benzodiazepines
  29. benzodiazepine receptor
    • increases frequency of GABAA induced chloride channel openings
    • only see effect if GABA is around
  30. barbituate receptor
    • on GABAA receptor complex
    • increases the duration of channel opening
    • can be opened in the absence of GABA which makes it a dangerous CNS stimulant (increased suicide potential, respiratory depressant)
  31. flumazenil
    antagonist at the benzodiazepine receptor which causes anxiety
  32. flurazepam
    • benzodiazepine
    • rapid onset, long duration
  33. triazolam
    • benzodiazepine
    • rapid onset, short duration
  34. lorazepam
    • benzodiazepine
    • does not from an active metabolite
    • as IV treats status epilecticus
  35. diazepam
    • most rapidly absorbed benzodiazepine because has high lipophilicity
    • muscle relaxer (reduces spasticity for spasms of all reasons)
    • as IV, causes consious sedation and anesthesia, treats status epilecticus
    • also used in alcohol withdrawal to prevent seizures, delirium, and arrythmias--gradual reduction of dose
  36. benzodiazepines
    • lipophilicity determines rate of redistribution from CNS
    • effects: decrease anxiety, cause sedation, hypnosis (go to sleep quicker, reduce awakenings), anterograde amnesia when given IV, anticonvulsant (increase seizure threshold)
    • produce additive CNS depression with most other depressents e.g. alcohol
    • drugs like cimetidine affect hepatic metabolism and therefore these drugs
    • used for generalized anxiety disorder, sleep disorders (increase stage 1&2 sleep), seizure treatment, IV sedation and anesthesia
    • tolerance develops, have bad withdrawl so must gradually reduce dose and use longer acting ones
    • adverse effects when used for insomnia: ataxia, rebound insomnia, daytime sedation, idiosyncratic stimulation-more common in children
  37. alprazolam
    • benzodiazepine
    • used for panic disorder (attacks)
    • quick onset of action
  38. chlordiazepoxide
    benzodiazepine used mostly for alcohol withdrawl to prevent seizures, delirium, and arrythmias
  39. clonazepam
    • benzodiazepine used for adjunct control of acute manic episodes
    • used for absence seizures and some types of myoclonic seizures
    • no EPS
  40. zolpidem
    • binds to benzodiazepine receptor- omega-1 BDZ
    • less disruption of sleep-more stage 3,4 preservation
    • doesn't have muscle relaxant or anxiolytic effects
    • used for insomnia
    • antagonized by flumazenil
    • ambien
  41. zaleplon
    • binds to benzodiazepine receptor- omega-1 BDZ
    • less disruption of sleep-more stage 3,4 preservation
    • doesn't have muscle relaxant or anxiolytic effects
    • used for insomnia
    • antagonized by flumazenil
    • sonata
  42. eszopiclone
    • binds GABA receptor near benzodiazepine spot
    • hypnotic
    • lunesta
  43. ramelteon
    • melatonin MT1, MT2 receptor agonist
    • insomnia where it is difficult to fall asleep
    • helps with jet lag
  44. barbituates
    • highly lipophilic, eliminated mainly by kidney
    • causes sedation, hypnotic action, anesthesia, respiratory depression, high dose can causes decrease in MAP, exacerbation of porphyrias, tolerance, physical dependence (can lead to life threatening seizures in withdrawal),
    • additive with other CNS depressants
  45. pentobarbital
    • barbituate used as hypnotic
    • facilitates withdrawal from short acting drugs
  46. chloral hydrate
    • pungent taste hypnotic
    • less effect on stages of sleep than benzodiazepines and barbituates
    • used for elderly people
  47. baclofen
    • GABA mimetic working at GABAB receptors
    • skeletal muscle relaxant
    • hyperpolarizes so causes presynaptic inhibition and blocks glutamate
    • works as well as diazepam but has much less sedative effect
  48. tizanidine
    • alpha 2 agonist related to clonidine
    • skeletal muscle relaxant
    • may enhance presynaptic and postsynaptic inhibition
    • efficacy is similar to diazepam and baclofen
    • side effects: drowsiness, hypotension, dry mouth, fatigue (asthenia)
  49. alcohol dehydrogenase
    • converts ethanol to acetaldehyde--rate limiting
    • uses NAD+
    • saturated by first couple of sips of a drink
    • primarily in the liver but also in GI tract
    • zero order elimination
  50. microsomal ethanol oxidizing system
    • includes CYP2E1
    • high Km--little contribution at concentrations below 100mg/dL
    • useds NADP+ to convert ethanol to acetaldehyde
    • induced in alcoholics
    • means that other drugs that use this P450 will be metabolized more quickly in an alcoholic
  51. acetaldehyde dehydrogenase
    • converts acetaldehyde to acetate
    • genetic polymorphisms--Asian flush bc don't have much of this enzyme
    • inhibited by disulfiram
  52. disulfiram
    • aversion therapy for alcoholism
    • inhibits acetaldehyde dehydrogenase
    • makes you feel uncomfortable if you drink
    • not very effective, is it ethical?
  53. naltrexone
    • reduces urge to drink
    • competitive opioid receptor antagonist-people need to want treatment because this can be surmounted
    • best with psychosocial therapy
  54. acamprosate
    • decreases drinking frequency and reduces relapse
    • GABAA mimetic and atagonist for NMDA receptor
    • well tolerated-side effect is diarrhea
    • normalizes dysregulated neurotransmission
  55. caffeine
    • blocks adenosine receptors (GPCR)
    • this leads to depolarization and glutamate release (because adenosine produces IPSP's and inhibits glutamate release)
    • also inhibits phosphodiesterase at higher doses--increase in cAMP which is good for asthma
    • induces release of Ca from ER
    • effects: increased alertness, decreased fatigue/drowsiness, (+)inotropic and chronotropic actions, dilates coronary and systemic blood vessels but constricts cerebral BV, diuretic, increases gastric secretion, modest bronchodilator, can cause nervousness, restlessness, tremors
    • at high doses can stimulate medullary respiratory, vasomotor, and vagal centers--tachycardia
    • used for staying awake and treating headache
    • tolerance does develop and physical dependence develops at 2 cups/day (withdrawal is sleepiness, headaches, nausea
  56. cocaine
    • sympathomimetic stimulanat
    • weak base so B predominates at high pH--very soluble
    • hydrochloride form and free base (crack-smoked or IV)
    • well absorbed through most mucous membranes
    • IV and smoking act quicker
    • short half-50 minutes, look for metabolites in urine
    • inhibits reuptake of NE, dopamine, and serotonin AND increases tyrosine and tryptophan hydroxylase--increases synthesis of NE and dopamine
    • rewarding effects due to action on dopamine synapses in ventral striatum
    • local anesthetic, vasoconstrictor
    • effects: vasoconstriction, tachycardia, increases alertness, euphoria
    • toxicity: tolerance and physical dependence, withdrawal is mild physically but strong psychologically, overdose can lead to seizures/CV effects, worse effects on the fetus(low birth weights, learning&emotional problems, attachment disorder)
    • therapeutic use:local anesthesia in nose surgery- ester so metabolized by plasma esterases, rare, but can cause allergic rxn
  57. amphetamine
    • CNS stimulant
    • duration of action 4-6 hours
    • releases NE, dopamine, serotonin AND blocks their reuptake
    • partial agonist of alpha adrenergic receptors
    • at high doses MAOI
    • effects: wakefulness, increase quantity of work, elevates mood, increases motor/speech, respiratory stimulation, decreases appetite
    • side effects: insomnia, abdominal pain, weight loss, suppresion of growth, fever
    • toxicity: sympathomimetic efects, restlessness, psychosis, neurodegeneration
    • used for narcolepsy, ADHD
    • ritalin
  58. methamphetamine
    • CNS stimulant
    • duration of action 4-6 hours
    • releases NE, dopamine, serotonin AND blocks their reuptake
    • partial agonist of alpha adrenergic receptors
    • at high doses MAOI
    • effects: wakefulness, increase quantity of work, elevates mood, increases motor/speech, respiratory stimulation, decreases appetite
    • side effects: insomnia, abdominal pain, weight loss, suppresion of growth, fever
    • toxicity: sympathomimetic efects, restlessness, psychosis, neurodegeneration
    • better CNS bioavailability than amphetamine and higher abuse potential (meth addiction is worse than cocaine)
  59. methylphenidate
    • CNS stimulant
    • duration of action 4-6 hours
    • releases NE, dopamine, serotonin AND blocks their reuptake
    • partial agonist of alpha adrenergic receptors
    • at high doses MAOI
    • effects: wakefulness, increase quantity of work, elevates mood, increases motor/speech, respiratory stimulation, decreases appetite
    • side effects: insomnia, abdominal pain, weight loss, suppresion of growth, fever
    • toxicity: sympathomimetic efects, restlessness, psychosis, neurodegeneration
    • used for ADHD
  60. nicotine
    • nAch agonist
    • NMJ receptors quickly desensitize
    • in CNS many regions have receptors including nucleus accumbens, results in membrane depolarization
    • increases alertness, activates dopamine signaling in nucleus accumbens (reward center), muscle relaxant, can cause nausea at CTZ
    • MOST ADDICTIVE PROCESS
    • gets to brain in 7 sec, each puff is its own reinforcement signal, true tachyphylaxis
    • withdrawal--irritability, anxiety, depression, difficulty in concentrating, weight gain
  61. bupropion
    • anti-depressant used for nicotine dependence
    • blocks NE and dopamine reuptake
    • adverse effects: dry mouth, insomnia
    • moderately effective, reduces craving and nicotine withdrawal symptoms
    • also used for SAD
    • does not cause weight gain or sexual dysfxn
  62. varenicline
    • partial agonist of CNS nicotinic receptors
    • activates enough to reduce craving and withdrawal but blocks nicotine if person does smoke
    • adverse effects: nausea, insomnia, headache, constipation
    • new warning for increasing thoughts of suicide;depression
  63. phenytoin
    • used for generalized tonic-clonic and partial seizures
    • block repetitive a.p. by blocking the inactivating gate of Na channel from closing--prolong refractory period
    • use dependent so has no effect when channel is not being used
    • pharmacokinetics are dose-dependent-switches from first to zero order outside of therapeutic range
    • may interact with drugs metabolized by P450s and drugs that are protein bound
    • toxicity: CNS effects are dose dependent (nausea, anorexia, apathy, sedation, ataxia, nystagmus, diplopia), gingival hyperplasia, hirsutism, teratogenic-fetal hydantoin syndrome, hypersensitive rash
  64. carbamazepine
    • used as anti-seizure for all except absence
    • blocks Na channels to increase refractory period
    • related to benzodiazepine but has no effect on GABA
    • unpredictable absorption, hepatic enzyme induction, dose related hepatotoxicity
    • used as drug of choice for partial seizures, trigeminal neuralgia, and bipolar disorder
    • toxicity (dose related)- diplopia, ataxia, GI upset, drowsiness, rare blood dyscrasias (most common in elderly)
  65. oxcarbazepine
    • carbamazepine analog for all types of seizures but absence
    • causes fewer CNS side effects and less enzyme induction
  66. phenobarbital
    • used for tonic-clonic and partial seizures-mostly in infants because causes a lot of sedation
    • acts on GABAA receptors
    • supresses firing from the foci and inhibiting spread
    • well absorbed, long half life
    • toxicity: drowsiness, sedation, confusion, exacerbation of acute intermittent porphyria
    • ADR: valproic acid, CNS depressants
  67. ethosuximide
    • choice drug for absence seizures
    • reduces low threshold T-type Ca currents in thalamic neurons
    • not protein bound-Vd=total body water
    • metabolism is inhibited by valproic acid
    • side effects: gastric distress, lethargy and fatigue
    • one of the safest anti-seizure drugs
  68. valproic acid
    • anti-seizure drug for all types (can also treat mania)
    • blocks Na channels and therefore repetitive firing, may reduce T-type Ca currents, increass GABA concentration
    • bound to plasma protein-competes with phenytoin
    • inhibits the metabolism of phenobarbital, phenytoin, carbamazepine, ethosuzimide
    • can treat myoclonic seizures which are difficult to treat, and combinations of seizures
    • side effects: GI upset, weight gain, and hair loss are dose related; others are hepatotoxicity, spina bifida
  69. felbamate
    • used for partial seizures refractory to other drugs
    • may antagonize at gly site of NMDA (needed for activation), potentiates GABA
    • side effects: aplastic anemia, hepatic failure
  70. gabapentin
    • adjunct therapy for partial seizures
    • GABA analog but not GABA agonist
    • excreted unchanged
    • low occurrence of side effects
    • also used for ALS and neuropathic pain
  71. pregabalin
    • adjunctive therapy for partial seizures
    • more potent than gabapentin
    • may interact with subunit of voltage-gated Ca channels to reduce NT release
    • used mostly for neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, and fibromyalgia
    • low abuse potential
  72. lamotrigine
    • used for partial and tonic-clonic seizures-monotherapy
    • blocks repetitive a.p.
    • does not interfere with pharmacokinetics of other drugs
    • used for bipolar disorder
    • side effect: serious rash-Stevens-Johnson syndrome
  73. topiramate
    • blocks spread of seizures by blocking AMPA glu receptors, enhancing GABA effects; may block Na channels
    • mainly used as adjunct for partial seizures
    • side effects: prevention of migraines, weight loss
  74. tiagabine
    • adjunctive treatment of partial seizures
    • inhibits the GABA transporter so blocks reuptake
    • side effects: dizziness, tremor, somnolence
  75. levetiracetam
    • adjunctive treatment of partial seizures, myoclonic seizures
    • side effects: somnolence, asthenia, dizziness
    • has few drug interactions
  76. zonisamide
    • used for adjunctive partial seizures of adults
    • stops the spread of seizures and suppresses their focus
    • inhibits T-type Ca channels and Na channels
    • CNS effects: ataxia, anorexia, nervousness, fatigue, speech impairment
  77. vigabatrin
    • adjunctive treatment of refractory complex partial seizures and infantile spasms
    • irreversible blocker of GABA metabolism
    • has potential permanent effects on vision
  78. lidocaine
    • amide local anesthetic-metabolized by liver
    • intermediate duration of action
    • produces faster, more intense, longer lasting, more extensive anasthesia than procaine
    • wide range of clinical uses
  79. local anesthetics
    • act on every type of nerve fiber
    • must be weak bases
    • travel to the inside of cells as B and then go into Na channel as BH+ to reversibly block it
    • increases threshold potential, slows rate of depolarization, reduces height of a.p., slows axonal conduction
    • use-dependent
    • *injured tissues can be acidic so might need more drug to create an effect since less drug is in B form at acidic pH
    • many are co-administered with vasoconstrictors-keeps drug there and prevents systemic side effects (epi is most common-works at alpha receptors)
    • S-enantiomers are usually less toxic
    • toxicity: if absorbed systemically causes CNS stim and then depression---death due to respiratory depression; CVS depression/arrhythmias happen after CNS effects
  80. order of local anesthetic block
    • pain
    • cold
    • warmth
    • touch
    • deep pressure
    • motor
  81. procaine
    • short acting ester local anesthetic
    • used for infiltration anesthesia
    • low potency, slow onset, short duration of action
  82. tetracaine
    • long acting ester local anesthetic
    • more potenr and longer duration than procaine
    • used in spinal, topical, opthalamic anesthesia
  83. benzocaine
    • ester local anasthetic that is slowly absorbed---not toxic topically--great for wounds and ulcers
    • lasts for a long time
  84. bupivacaine
    • long acting amide local anasthetic
    • causes prolonged anesthesia
    • provides more sensory than motor block-prolonged analgesia
    • more cardiotoxic than lidocaine--severe ventricular arrthymias, myocardial depression after large doses
    • S-enatiomer-lesss cardiotoxic
  85. ropivacaine
    • long acting amide local anesthetic
    • S-enantiomer
    • less cardiotoxic than bupivacaine and more motor sparing
    • for epidural and regoinal anesthesia
  86. SSRI
    • less toxicity than TCA and MAOI
    • side effects: nausea/vomiting, insomnia, nervousness, sexual dysfxn
    • if taken with MAOI, can get serotonin syndrome
    • discontinuation syndrome-most common with short acting ones- dizziness, light-headedness, vertigo, anxiety, fatigue, headache, tremor, visual disturbances
    • must taper or switch to a long acting like fluoxetine
    • used for major depressive disorder, OCD, panic disorder, soical phobia, PTSD, PMS, generalized anxiety disorder
  87. fluoxetine
    • SSRI
    • long half life and has active metabolite with long half life
    • used for depression, PMS
    • prozac
  88. sertraline
    • SSRI
    • short half life---can lead to withdrawal syndrome
    • zoloft
  89. citalopram
    SSRI aslo used for anxiety
  90. escitalopram
    S-enantiomer of  citalopram (SSRI)
  91. venlafaxine
    • SNRI
    • used for severe depression and anxiety
  92. duloxetine
    • SNRI
    • 12-18 hour half life
    • use with caution in patients with liver disease
    • also used for neuropathic pain, fibromyalgia, back pain, osteoarthritis
  93. milnacipran
    SNRI used for fibromyalgia
  94. mirtazapine
    • blocks alpha2 receptors in brain
    • atypical anti-depressant
    • increases appetite (might prescribe to an AIDS patient with wasting syndrome
  95. imipramine
    • tricyclic anti-depressant
    • used for enuresis (bed wetting)
  96. tricyclic anti-depressants
    • rapidly absorbed-high concentrations in brain and heart
    • long half life 8-100 hours
    • decreases REM and increases stage 4
    • prominent anticholinergic effects, sedation, orthostatic hypotension
    • cardiac abnormalities: (due to anticholinergic effects and increased NE), palpitations, tachycardia, arrhythmias, longer QRS interval and inverted T waves
    • overdoses: hyperpyrexia, BP extremes, seizures, coma, cardiac conduction defects
    • many drug interactions
  97. amitriptyline
    tricyclic anti-depressant used for chronic pain
  98. clomipramine
    tricyclic anti-depressant used for OCD
  99. phenelzine
    • irreversible MAO inhibitor
    • non-selective
    • blocks oxidative deamination of NE, dopamine, serotonin
    • anti-depressant activity probably due to inhibition of MAO
    • corrects sleep disorder, can lead to hypmania, may produce stim in normals, can produce orthostatic hypotension
    • used for depression (3rd line) and narcolepsy
    • watch out for tyramine!
  100. chlorpromazine
    • typical anti-psychotic
    • low-medium potency
    • sedative
    • pronounced anticholinergic actions!
  101. clozapine
    • atypical anti-psychotic
    • blocks D4 and 5HT-2
    • muscarinic antagonist (most potent of atypicals)
    • improves refractory (+) symptoms
    • improves (-) symptoms
    • lowers seizures threshold more than other anti-psychotics
    • can cause fatal agranulocytosis
    • fewer EPS, causes weight gain
  102. extra pyramidal actions- results of dopamine blockade
    • more common with typical anti-psychotics
    • dystonias-spasm of tongue, face, neck muscles (more common in young people
    • parkinsonism
    • akathisia-compulsive, restless movement, anxiety, agitation
    • tardive dyskinesia-only after months to years of treatment--oral facial dyskinesias, choreoathetoid movements
  103. anti-psychotic side effects
    • sedation
    • extrapyramidal actions
    • anticholinergic effects
    • orthostatic hypotension
    • weight gain
    • neuroleptic malignant syndrome-fever, mutism, EPS, possible death
    • decreased seizure threshold
  104. thioridazine
    • typical anti-psychotic
    • low potency
    • sedative
    • less EPS due to anticholinergic effects
    • cardiac side effects
  105. fluphenazine
    • typical anti-psychotic
    • high potency (50x as potent as chlorpromazine)
    • less sedative and anticholinergic effects
    • more EPS
  106. thiothixene
    • typical anti-psychotic
    • action like thioridazine, fluphenazine, and chlorpromazine
  107. haloperidol
    • typical anti-psychotic
    • used for Tourette's Syndrome, acute manic episode
    • low anticholinergic effects
  108. pimozide
    • typical anti-psychotic
    • used for Tourette's Syndrome only when haloperidol doesn't work because it has many side effects
  109. olanzapine
    • atypical anti-psychotic
    • D1, D2, 5HT-2 antagonist
    • few EPS
    • no agranulocytosis
    • weight gain and diabetes risk
    • also used for bipolar disorder
  110. risperidone
    • atypical anti-psychotic
    • dopamine and serotonin antagonist
    • low incidence of EPS
    • less seizure and antimuscarinic effects than clozapine
  111. quetiapine
    • atypical anti-psychotic
    • blocks D2 and 5HT-2
    • shorter half life than others
    • also used as augmentation in depression
  112. ziprasidone
    • atypical anti-psychotic
    • 5HT-2 and D2 antagonist
    • might also have 5HT-1 agonist activity
    • NO weight gain
  113. aripiprazole
    • atypical anti-psychotic
    • D2 partial agonist and 5HT-2 antagonist
    • adjunctive depression therapy
  114. lithium
    • treatment for mania
    • no behavioral effects on normals
    • blocks phosphatase needed to convert IP2 -> IP1 so decreases 2nd messengers
    • narrow therapeutic window
    • interactions with ACE inhibitors, AngII blockers and thiazide diuretics (increased Na excretion causes significant increases in Li levels)
    • side effects: fatigue, tremor, GI symptoms, goiter, teratogenic, slurred speech and ataxia,
    • toxicity: impaired consciousness, rigidity and hyperactive deep reflexes, coma
    • used for manic episodes and to prevent recurrences of bipolar depression and mania, aggressive behavior, cluster headaches
  115. morphine
    • mu agonist
    • strong analgesic
    • high first pass metabolism
    • duration of 4-5 hours
  116. heroin
    • mu agonist
    • activated by metabolism
    • more lipophilic than morphine so fast acting---high abuse potential
  117. codeine
    • mu agonist
    • activated by metabolism
    • for mild-moderate pain--will never get efficacy of morphine
    • often used synergistically with aspirin/acetaminophen
    • cough suppresion
  118. oxycodone
    • mu agonist
    • for moderate to severe pain
    • available as sustained release oral preparation--major abuse potential
  119. methadone
    • mu agonist
    • good oral bioavailability
    • longer duration of action than morphine but just as potent
    • used in the treatment of opiod abuse
  120. meperidine
    • mu agonist
    • shorter duration of action than morhpine
    • produces toxic metabolite---> seizures
    • interacts with MAOIs
    • used in conscious sedation with diazepam/midazolam
  121. dextromethorphan
    • opiod for cough suppression
    • robotussin
  122. fentanyl
    • mu agonist
    • 100x as potent as morphine
    • short acting 1-1.5 hours
    • used for breakthrough pain
    • most commonly abused by medical personel
  123. hydromorphone
    • mu agonist
    • 2-3x as potent as morphine
    • abused a lot
  124. hydrocodone
    • mu agonist
    • more poteent than morphine, not as efficacious
    • in cough syrup
    • vicodin
  125. nalbuphine
    • mu antagonist and kappa agonist
    • similar efficacy and potency to morphine
    • little euphoria so much lower abuse potential
    • can precipitate withdrawal in opiod dependent patients
    • only IV
  126. buprenorphine
    • parital mu agonist
    • 25-50x as potent as morphine
    • used to treat moderate to severe pain
    • used in comvo to treat opiod dependence with naloxone
  127. naloxone
    • mu antagonist
    • high first pass metabolism
    • short duration-1-2 hours
    • used to treat opiod overdoses
    • doesn't affect normals (ER patient who comes in and overdosed on something)
  128. tramadol
    • weak mu agoinst, weak NMDA antagonist
    • blocks NE and 5HT uptake
    • mild to moderate pain
    • oral use including a sustatined release prep
  129. suboxone
    • buprenorphine and naloxone together
    • used to treat opiod dependence
    • naloxone is only active if pill is crushed and snorted/injected/smoked
  130. opiod effects
    • all are equally efficacious in alleviating pain (except codeine)
    • analgesia
    • cough supression
    • antidiarrheal and constipation (decreases sensitivity to CO2
    • euphoria
    • sedation
    • respiratory depression
    • nausea
    • endocrine effects
    • miosis
    • decrease myocardial O2 demand
  131. marijuana
    most commonly abused drug in the USA
  132. cannabis
    plant smoked as marijuana
  133. Δ9-Tetrahydrocannabinol
    • active ingredient in marijuana
    • rapidly metabolized to active metabolite
    • metabolites in urine seen up to 7 days
    • 3-5 x more potent when smoked than when ingested
    • duration of action 1-6 hours; half life is 20-50 hours
    • CB1 (high density in cerebellum, hippocampus, and basal ganglia) and CB2 receptors (peripheral tissues like immune system)--both are Gi
    • effects: euphoria, memory impairment, CV effects like tachycardia, exascerbation of angina, bronchodilator but also a lung irritant, lowers testosterone, FSH, LSH, causes abnormal menses
    • only approved uses are for controlling nausea and AIDS wasting syndrome
  134. phencyclidine
    • PCP
    • blocks NMDA receptors
    • also anti-muscarinic
    • half life is 12-24 hours
    • sympathomimetic- tachycardia, HTN, potentiation of catecholamines
    • tolerance develops but no physical dependence
    • small doses-drunken state with numb extremities, large doses produce convulsions
    • overdose--anxiety, hallucinations, dysphoria, convulsions, delirium, hypertensive crisis
  135. Lysergic acid diethylamide
    • onset is 15-20 minutes, lasts 12 hours
    • cross tolerance with most hallucinogens
    • act at 5-HT2 receptors
    • very potent
    • sympathomimetic-tachycardia, increased BP, psychomotor stimulation
    • sensory--usually altered visual perception, lability of modd, imparied judgement
    • rapid tolerance but no physical dependence
    • adverse reactions: hallucinations, anxiety, panic, depersonalization--put them in a quiet place with BDZ
  136. methylenedioxymethamphetamine
    • ecstasy
    • induces feelings of "well-being and connection"
    • onset is 20-40 minutes, duration is 3-4 hours
    • psychomotor stimulation, restlessness, bruxism, anorexia, sweating, tremor, hangover
    • neurotoxicity- 5HT damage
  137. gamma-hydroxybutyrate
    • precursor and metabolite of GABA
    • effects last 3 hours, depressant--state of relaxation and tranquility
    • overdose-drowsiness, dizziness, nausea, vomiting, ataxia---even higher- loss of bladder control, temporary amnesia, clonus, seizures
  138. toluene
    • in airplane glue
    • toxicity: BM depression, aplastic anemia
  139. salvia divinorum
    • active ingredient-salvinorin A
    • k-opiod agonist
    • short duration of action 20-45 minutes
    • dream like experience, dissociation at high doses- fear, panic, perspiration
  140. oseltamivir
    • antiviral-prodrug, which enhances oral bioavailability
    • competitive inhibitor of influenza neuraminidase, thus interferes with viral release and viral penetration
    • treatment of influenza A and B and prophylaxis
    • must be given within 48 hours of onset of symptoms
    • oral administration
    • side effects: nausea/vomiting/diarrhea, bronchitis
  141. trifluridine
    • antiviral
    • thymidine analog-interferes with DNA synthesis
    • systemically toxic--use is for herpes in the eye (HSV1,2)
    • toxicity is burning, stinging, hypersensitivity
  142. acyclovir
    • antiviral
    • competitive inhibitor of dGTP---acts as a DNA chain terminator because nucleoside analog
    • phosphorylated form is produced 40-100x faster in infected cells by herpes thymidine kinase
    • also inhibits herpes DNA pol more than host DNA pol
    • as IV used for systemic herpes including encephalitis, severe initial genital herpes
    • orally used for primary genital herpes, primary herpetic gingivostomatosis (cold sores)
    • can be given to children with chickenpox
    • generally well tolerated but side effects can include rash, itching, nausea, vomiting, headache, fatigue
  143. famciclovir
    • antiviral, prodrug which is converted to penciclovir, which gets phosphorylated and inhibits viral DNA pol
    • great oral bioavailability
    • used for acute herpes zoster, treatment and suppression of recurrent genital herpes, treatment of recurent cold sores
    • generally well tolerated but side effects could be rash, itching, nausea, vomiting, headache, fatigue
  144. penciclovir
    • antiviral
    • inhibits DNA pol
    • used for recurrent herpes of lip and face
    • administered topically
  145. ganciclovir
    • antiviral
    • inhibits DNA pol--uses CMV protein kinase to get phosphorylated
    • used for treatment of CMV retinitis in AIDS patients, CMV prophylaxis for transplant recipients
    • toxicity: BM suppression, leukopenia, thrombocytopenia, anemia, abnormal liver function, even lower BM suppression if coadministerd with AZT
  146. foscarnet
    • antiviral
    • inhibits CMV DNA polymerase by binding to its pyrophosphate-binding site (keeps tri-P out)
    • does not require converstion to tri-P form to be active
    • used in AIDS patients with CMV retinitis, acyclovir-resistant herpes simplex
    • toxicity: renal damage, electrolyte imbalance which leads to seizures
  147. lamivudine
    • antiviral
    • nucleoside analog inhibitor of reverse transcriptase domain of polymerase
    • used for hep B, 85% orally bioavailable
    • also used for HIV synergistically with AZT--hard to be resistant to both drugs
    • very well tolerated but could have nausea, diarrhea
  148. tenofovir
    • antiviral, prodrug
    • adenosine monophosphate analog phosphorylated by cell enzymes to active nucleotide
    • inhibits reverse transcriptase domain
    • used for hep B and in combination therapy for HIV patients
    • toxicity is GI upset, otherwise well tolerated
  149. ribavirin
    • antiviral
    • nucleoside analog which interferes with viral mRNA synthesis
    • mono-P form inhibits inosine-5'P dehydrogenase and thus GTP synthesis
    • tri-P form inhibits GTP-dependent capping of viral mRNA
    • used: aerosol in infants and young children with documented severe lower RSV infections, hepatitis C in combo with interferon alpha
    • toxicity: aerosol--can clog respiratory equipment, pumonary function deterioration, rash
    • IV/oral use: anemia, BM suppression
  150. interferon, specifically alpha
    • host produced proteins that have been exploited
    • used for veneral warts--condyloma acuminata, hepatitis B and C (must be IV)
    • toxicity: flu-like symptoms, leukopenia, BM suppression, neurotoxicity, myalgia
    • with PEG and ribavirin--better for hepatitis C
  151. boceprevir
    • reversible inhibitor of hepatitis C NS3 protease thus blocing formation of infectious virus particles
    • used for hepatitis C genotype 1 in combo with PEG-interferon +ribavarin
    • toxicity: anemia, neutropenia, contraindicated with drugs that are CYP3A substrates or inducers because it is also metabolized by CYP3A
  152. zidovudine
    • AZT, NRTI
    • thymidine nucleoside analog which blocks reverse transcriptase---DNA chain terminator
    • used for treatment of HIV
    • toxicity: BM suppression, neutropenia, anemia, drugs that inhibit glucuronyl transferase (aspirin, acetaminophen, indomethacin, probenacid) because it converts it to an inactive metabolite instead of going through P450 system to toxic amine, myopathy with prolonged use
  153. emtricitabine
    • antiviral
    • fluorinated analog of 3TC that inhibits reverse transcriptase by competing for dCTP--chain termination
    • used in combo therapy for HIV +
  154. abacavir
    • NRTI-very potent dGTP analog
    • used in combo for HIV+
    • toxicity: hypersensitivity reactions (associated with HLA-B*5701)
  155. side effects of NRTIs
    • lactic acidosis
    • hepatic steatosis
    • (could be due to hurting mitochondrial DNA polymerase gamma)
  156. efavirenz
    • NNRTI
    • noncompetitive inhibitor which causes a conformational change, does not require phosphorylation for activity
    • used in multi therapy for HIV
    • toxicity: rash, CNS/psychiatric symptoms, nightmares (go away after a month)
  157. lopinavir
    • aspartic protease inhibitor-prevents viral protease from cleaving gag-pol polypeptide into separate functional proteins
    • competitive inhibitor
    • used in combination with RT inhibitors
    • significantly decreases viral load
    • toxicities: diabetes, increases in TG and cholesterol, lipodystrophy, potent CYP3A inhibitor, diarrhea
  158. ritonavir
    • aspartic protease inhibitor
    • used to increase levels of other PI-blocks their metabolism so they acheive higher blood levels and fewer doses
    • too toxic to be primary PI
    • avoid other drugs metabolized by CYP3A
    • toxicities: diabetes, increase in TG and cholesterol, lipodystrophy
  159. enfuvirtide
    • fusion inhibitor for HIV 1
    • used for detectable viral replication despite other therapy
    • inhibits fusion of viral and cellular membranes by binding to gp41 subunit of HIV glycoprotein--blocks conformational changes needed for membrane fusion
    • subcutaneous injection twice a day
    • toxicity: painful and disfiguring results at injection site, diarrhea, nausea, fatigue
  160. maraviroc
    • treatment of CCR5 tropic HIV1
    • CCR5 (chemokine co-receptor antagonist)
    • blocks the entry of HIV into the cell
    • used early
    • toxicity: hepatotoxicity, CV events
  161. raltegravir
    • integrase inhibitor
    • used for treatment of HIV1 resistant to other drugs as part of multi drug therapy
    • inhibits HIV-1 integrase preventing integration of HIV1 DNA into genome
    • generally well tolerated
  162. regular insulin
    • clear solution
    • self aggregating
    • human sequence
    • only one for IV use
  163. NPH insulin
    • cloudy suspension
    • longer course than regular
  164. lispro insulin
    shorter onset of action and quicker deactivation than regular insulin
  165. insulin aspart
    shorter onset of action and quicker deactivation than regular insulin
  166. insulin glargine
    • long acting insulin analog--for basal insulin
    • cannot be combined with others in needle because soluble at different pH
    • lantus
  167. insulin detemir
    • hydrophobic
    • self associating and binds albumin--so long acting
  168. glipizide
    • stimulates insulin release by acting at K transporter
    • side effects: drug interactions, hypoglycemia with renal failure or not eating
  169. glyburide
    • stimulates insulin release by acting at K transporter
    • side effects: drug interactions, hypoglycemia with renal failure or not eating
  170. glimepiride
    • stimulates insulin release by acting at K transporter
    • side effects: drug interactions, hypoglycemia with renal failure or not eating
  171. metformin
    • insulin sensitizing drug-reduces resistance
    • decreases hepatic gluconeogenesis
    • side effects: abdominal discomfort, diarrhea, fatal lactic acidosis
    • contraindications:renal insufficiency, elderly, CHF, acute illnesses, liver dysfxn
    • better CV risk, cancer risk
  172. rosiglitazone
    • make peripheral tissues such as far and muscle more sensitive to insulin by activating PPAR
    • side effects: liver toxicity, weight gain, fluid retention, contraindicated in advanced heart failure
  173. pioglitazone
    • make peripheral tissues such as far and muscle more sensitive to insulin by activating PPAR
    • side effects: liver toxicity, weight gain, fluid retention, contraindicated in advanced heart failure
    • FDA advisory for increased bladder cancer risk
  174. acarbose
    • glucosidase inhibitor--inhibits enteric enzymes that break down complex carbohydrates
    • reduces post-prandial hyperglycemia
    • side effects: bloating, abdominal discomfort, diarrhea, flatulence
  175. exenatide
    • GLP-1 analog which augments insulin secretion, increaes beta cell mass, inhibits glucagon secretion and promotes weight loss
    • side effects: nausea, emesis, diarrhea, headaches
  176. sitagliptin
    • DPP4 inhibitor (DPP4 degrades GLP1)
    • prolongs action of GLP1 in portal circulation

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