Pharm Midterm

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Pharm Midterm
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Pharmacology I Midterm 1
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  1. Acetylcholine
    • •Category: ANS- Parasympathomimetic
    • •MOA: Muscarinic  and nicotinic agonist
    • •Distinguishing characteristics:
    • –Rapidly hydrolyzed by esterases
    • –Acts on both muscarinic and nicotinic receptors
    • –Quaternary ammonium group invokes polarity
    • •Predictable characteristics:
    • –Short half life (seconds)
    • –Diffuse activity (parasympathomimetic, sympathomimetic and skeletal muscle)
    • –Limited distribution
    • •Predictable uses: Possible local ophthalmic use, but other products better.
  2. Bethanechol
    (URECHOLINE)
    • •Category: ANS- Parasympathomimetic
    • •MOA: Muscarinic agonist
    • •Distinguishing characteristics
    • –Not metabolized by esterase enzymes
    • –Quaternary ammonium compound
    • –Particular affinity for gut and bladder smooth muscle
    • –Oral route preferred
    • •Predictable characteristics
    • –No CNS effect
    • –T1/2 allows distribution to areas of low blood flow
    • •Predictable uses
    • –Gastroparesis (postoperative)
    • –Urinary retention
    • –Xerostomia
    • –Ocular diagnostics
    • •Predicable side effects
    • –Other parasympathomimetic effects especially following parenteral Rx
  3. Pilocarpine
    • •Category: ANS- Parasympathomimetic
    • •MOA: Muscarinic receptor agonist
    • •Distinguishing characteristics
    • –Plant origin- Pilocarpus jabarundi
    • –Tertiary ammonium compound
    • –Preferential activity on sweat glands
    • –Resistant to esterases
    • •Predictable characteristics
    • –Used as miotic and in treatment of glaucoma
    • –Will cause accommodation
    • –Used to treat xerostomia
    • –May cause CNS effects at high plasma levels
    • –Diaphoresis is common side effect
    • –Duration of action up to 8 hours
  4. Neostigmine
    • •Category: ANS- Parasympathomimetic
    • •MOA: Reversible cholinesterase inhibitor
    • •Distinctive characteristics:
    • –Quaternary ammonium compound (contrast to physostigmine)
    • –Contains ester group- slowly hydrolyzed (1-2 hr T1/2)
    • –Poorly absorbed following oral Rx
    • •Predictable activities
    • –Elevates Ach levels
    • –Causes both muscarinic and nicotinic stimulation
    • –Numerous peripheral side effects but not CNS
    • •Predictable uses
    • –Miosis and Rx glaucoma (local administration)
    • –Rx myasthenia gravis
    • –Antidote to some drugs (atropine)
    • –Atonic gut and bladder
  5. Malathione
    • •Category: ANS- Parasympathomimetic
    • •MOA: Irreversible cholinesterase inhibitor
    • •Distinguishing characteristics:
    • –Tertiary ammonium compound
    • –Binds covalently to esterase enzymes
    • –Not hydrolyzed by esterase enzymes
    • –Rapidly absorbed through multiple routes
    • •Predictable characteristics
    • –Causes SLUD and other ANS activities
    • –Causes CNS disturbances
    • –No therapeutic use
    • –Used as insecticide
    • –Similar agents used as chemical weapons
    • –Atropine is antidote plus supportive therapy
  6. Atropine
    • •Category: ANS- Parasympatholytic
    • •MOA: Muscarinic receptor antagonist
    • •Distinguishing characteristics:
    • –From plant source- Atropa belladona
    • –Tertiary ammonium compound
    • –Ester group required for activity
    • –Resistant to hydrolysis by esterases
    • –Metabolized in liver with T1/2 of about 4 hr.
    • •Predictable activities:
    • –CNS toxicity in especially in children even after ophthalmic Rx
    • –Inhibit SLUD and other parasympathetic activities
    • –Used in ophthalmology- mydriasis and cycloplegia
    • –Used as antidote- parasympathomimetics
    • –Used to treat diarrhea
    • –Once used to treat asthma, but now better drugs available
  7. Scopolamine
    • •Category: ANS- parasympatholytic
    • •MOA: Muscarinic receptor antagonist
    • •Distinguishing characteristics:
    • –From plant source- Hyocyamus niger
    • –Greater CNS distribution than atropine
    • –Other characteristics similar to atropine
    • •Predictable actions:
    • –Greater CNS side effects and abuse potential than atropine
    • –Used less frequently than atropine
    • –Used to treat motion sickness
  8. Ipratropium(Atrovent)
    • •Category: Parasympatholytic
    • •MOA: Muscarinic antagonist
    • •Distinguishing characteristics:
    • –Quaternary ammonium compound
    • –Minimal inhibition of mucociliary clearance
    • •Predictable actions:
    • –No CNS effects
    • –Bronchodilation
    • –Limited mucous accumulation
  9. Muscarine
    • •Category: ANS- Parasympathomimetic
    • •MOA: Muscarinic receptor agonist
    • •Distinguishing characteristics:
    • –Naturally occurring
    • –Quaternary ammonium compound
    • –Found in Amanita muscaria, but not major toxic entity in mycetism
    • •Predictable characteristics:
    • –SLUD
    • –No CNS activity
    • –Greater historical than therapeutic importance
  10. Epinephrine
    • •Category: ANS- Sympathomimetic
    • •MOA: Stimulate Alpha and Beta receptors (G protein which facilitate second messengers.)
    • •Distinguishing characteristics:
    • –Metabolized in gut, blood and multiple tissues
    • –More Beta and less Alpha activity than norepinephrine
    • •Predictable Characteristics & Uses
    • –Ineffective orally
    • –Very short half-life (minutes)
    • –Cardiac emergencies
    • –Brochospasm
    • –Adjunct to local anesthesia
    • •Predictable side effects
    • –Tachycardia & increased force of contraction
    • –Blood pressure disturbance (usually hypertension)
  11. Phenylephrine(NEOSYNEPHRINE)
    • •Category: ANS- Sympathomimetic
    • •MOA: Alpha 1 receptor agonist
    • •Distinguishing characteristics:
    • –Effective orally
    • –Limited access to CNS
    • •Uses:
    • –Nasal decongestant
    • –Mydriatic
    • •Side effects:
    • –Rebound congestion
    • –Increased peripheral resistance
    • –Reflex bradycardia
  12. Clonidine(Catapres)
    • •MOA: Alpha 2 receptor agonist
    • •Distinguishing characteristics
    • –Effective orally
    • –Crosses blood-brain barrier
    • –Prefers alpha receptors in brainstem
    • –Long half-life and duration of action
    • –Diminish discharge from medular vasomotor center
    • •Predictable uses: Antihypertensive
    • •Predictable side effects:
    • –Dry mouth
    • –Sedation
    • –Sexual dysfunction
  13. Isoproterenol(ISUPREL)
    • •Category: ANS- Sympathomimetic
    • •MOA: Beta receptor agonist (Both 1 & 2)
    • •Distinguishing characteristics
    • –Metabolized by COMT
    • –Short duration of action
    • –Both beta 1 and beta 2
    • •Predictable uses: Cardiac arrest
    • •Predictable actions:
    • –Tachycardia
    • –Bronchodilation
    • –Replaced often by more selective beta agonists (Why?)
  14. ALBUTEROL(VENTOLIN
    • •Category: ANS- Sympathomimetic
    • •MOA: Beta 2 receptor agonist
    • •Distinguishing characteristics
    • –Effective orally or by inhalation
    • –Limited cardiovascular effects
    • –Duration of action several hours
    • •Predictable uses: Bronchodilator
    • •Predictable side effects:
    • –Weak and occasional tachycardia
    • –Vasodilation
  15. Amphetamine
    • •Category: ANS Sympathomimetic
    • •MOA: Stimulate release of Norepinephrine and Dopamine
    • •Distinguishing Characteristics:
    • –Enters CNS
    • –Inhibits MAO
    • •Predicted actions:
    • –Alpha and Beta Stimulation by norepinephrine: Vasoconstriction, cardiac stimulation, increased blood pressure, mydriasis
    • –CNS stimulation: euphoria, insomnia, anxiety, loss of appetite, hyperthermia
    • –Used to treat: narcolepsy, obesity and ADD
    • –High abuse potential makes it scheduled substance
  16. Substances that increase norepinephrine release:
    • •Cocaine
    • •Tyramine
    • •Reserpine (although its overall effect is to deplete norepinephrine)
    • •Ephedrine
    • •Pseudoephedrin
    • •Methamphetamine
  17. Phenelzine(NARDIL)
    • •Category: ANS- Sympathomimetic
    • •MOA: Monoamine oxidase inhibitor
    • •Distinctive characteristics
    • –Readily absorbed
    • –Crosses blood-brain barrier
    • –Increases synaptic catecholamine levels
    • •Predictable use: Antidepressant
    • •Predictable side effects: Sympathomimetic actions
  18. Prazocin(Minipress)
    • •Category: ANS- Sympatholytic
    • •MOA: Alpha 1 receptor antagonist
    • •Distinctive characteristics:
    • –Effective orally
    • –Highly protein bound (5% free)
    • –Limited reflex tachycardia
    • •Predicted use: Hypertension
    • •Predicted side effects:
    • –Hypotension
    • –Syncope
  19. Propranolol(INDERAL)
    • •Category: ANS- Sympatholytic
    • •MOA: Beta 1 & 2 receptor antagonist
    • •Distinguishing characteristics:
    • –Very lipid soluble
    • –Significant 1st pass metabolism
    • –Highly variable plasma levels
    • –Multiple uses (not all very predictable)
    • •Uses
    • –Antihypertensive
    • –Antiangina
    • –Antiarrythmic
    • •Side effects
    • –Place asthma patients at risk
    • –Place diabetics at risk
  20. Metoprolol(LOPRESSOR)
    • •Category: ANS- Sympatholytic
    • •MOA: Beta 1 receptor antagonist
    • •Distinctive characteristics:
    • –Similar to propranolol
    • •Uses: Antihypertensive without risk to asthmatics and diabetics
  21. Reserpine
    • •Category: ANS- Sympatholytic
    • •MOA: Promotes release of Norepinephrine and reduces reuptake resulting in depletion of norepinephrine stores
    • •Distinctive characteristics:
    • –Derived from plant
    • –Transitory sympathomimetic followed by prolonged sympatholytic effect
    • –Antiquated for therapeutic use, extensive research use
    • •Predictable uses: Antihypertensive
    • •Predictable side effects: Prolonged paralysis of sympathetic nervous system
  22. Levodopa
    • Category: Anti-parkinson
    • Mechanism of Action: Replace dopamine, the neurotransmitter that is absent in Parkinson’s Disease
    • Distinguishing Characteristics:
    • Levodopa converted to dopamine in brain
    • Dopamine destroyed in gut and doesn’t cross BBB.
    • Dopamine is sympathomimetic
    • Predictable actions:
    • Sympathomimetic side effects
    • Often given with carbidopa (a drug that prevents conversion of dopa to dopamine in periphery) to reduce sympathomimetic side effects.
  23. Sertraline(Zoloft)
    • Category: Antidepressant
    • Mechanism of Action: Selective serotonin reuptake inhibition(SSRI)
    • Distinguishing Characteristics:
    • –Must “titrate” dose for optimum effect
    • Predictable Actions:
    • –Similar Action to other SSRIs:
    • •Escitalopram (Lexapro)
    • •Fluoxetine (Prozac)
    • –Side effects related to serotonin activity (central & peripheral)
    • •Insomnia
    • •Headache
    • •Nausea
    • •Dry mouth
  24. Venalfaxine(Effexor)
    • Category: Antidepressant
    • Mechanism of Action: Non-selective neurotransmitter reuptake inhibition
    • Distinguishing Characteristics:
    • –Increase levels of serotonin, norepinephrine and dopamine in central and peripheral synapses
    • Predictable actions:
    • –Side effects related to all of the neurotransmitters
    • •Hypertension or hypotension
    • •Tachycardia
    • •Insomnia
    • –Similar Drugs:
    • •Trazadone (Desyrel)
    • •Bupropion (Wellbutrin)
  25. Monoamine inhibitors:
    • –Increase amount of norepinephrine, dopamine and serotonin in synapse by decreasing metabolism
    • –Includes: Tranylcypromine (Parnate)
    • –Reacts with other sympathetic drugs
  26. Phenytoin
    • Category: Antiseizure
    • MOA: Inhibit Na channels
    • Unique Characteristics:
    • –Hydantoin derivative (Formerly known as diphenylhydantoin)
    • –Poor water solubility causes variable bioavailability
    • –Metabolized by cytochrome p450 system (induces CYP3A4 isoenzyme)
    • –Side effects:
    • •Interferes with folate metabolism
    • •Causes gingival hyperplasia
    • •May cause hirsutism
    • –Indications
    • •Partial seizures
    • •Generalized tonic-clonic seizures
    • Predicted Actions
    • –Accelerates metabolism of valproate, digoxin, steroids, vitamin K
    • –Monitor plasma levels especially when changing formulations
    • –Folate-related side effects and teratologies
  27. Gabapentin
    • Category: Antiseizure
    • MOA: Increases release of GABA
    • Unique Characteristics:
    • –Short half-life
    • –Few side effects
    • –Indications: Adjunct to other antiseizure drugs
    • Predictable Actions:
    • –Rx several times daily
    • –Rx broad spectrum of seizures
  28. Two types of analgesics:
    • –Narcotic (Morphine, hydrocodone, oxycodone, Pentazocine, Meperidine, propoxyphen)
    • –Non-narcotic (Acetaminophen, aspirin, ibuprophen)
  29. some combinations of analgesics
    • –Hydrocodone + acetaminophen = Vicodin
    • –Acetaminophen + codeine = Tylenol with codeineOxycodone + aspirin = Percodan
  30. Analgesic mechanisms of action
    • –Narcotics stimulate opiate receptor in thalamus
    • –Non-narcotic block enzymes responsible for producing prostaglandins and other chemical transmitters
  31. Hydrocodone
    • Category: Analgesic
    • Mechanism of Action: Opiate receptor agonist (especially in thalamus, brainstem, gut, eye)
    • Distinguishing Characteristics:
    • –Scheduled substance (2-3)
    • –Tolerance upon repeated use
    • Predictable Actions:
    • –Pain less objectionable
    • –Depresses respiratory center, overdose causes apnea
    • –Physical and psychological dependance
    • Similar drugs include oxycodone, morphine
  32. Tramadol
    • Category: Analgesic
    • Mechanism of Action: Opiate receptor agonist in thalamus also inhibits reuptake of serotonin and norepinephrine
    • Distinguishing characteristics:
    • –May lower seizure threshold
  33. Alprazolam(Xanax)
    • Category: Anxiolytic, Sedative Hypnotic, Anti-epileptic, Muscle Relaxant
    • Mechanism of Action: GABA receptor agonist (Gama-aminobutyric Acid is inhibitory neurotransmitter)
    • Distinguishing Characteristics:
    • –Benzodiazapine
    • Similar drugs include: Lorazepam, Clonazepam, Diazepam (Differ in onset and duration of action)
  34. Benzodiazapines
    • •Diazepam (Valium) – Anxiety
    • •Flurazepam (Dalmane) – Insomnia
    • •Clonazepam (Klonopin) – Anxiety
    • •Chlordiazepoxide ( Librium) – Anxiety
    • •Lorazepam (Ativan)  - Sedation
    • •Oxazepam ( Serax) – Anxiety in hepatic pts.
  35. PLF of Procaine (Novocaine)
    • •Category: Local Anesthetic
    • •MOA: Sodium Channel Inhibition
    • •Distinguishing Characteristics:
    • –Ester-linked
    • –First synthetic local anesthetic
    • –Diminished contemporary use
    • •Predictable Qualities:
    • –Quickly metabolized
    • –Metabolized to PABA
    • –High incidence of hypersensitivity
  36. PLF of Lidocaine(Xylocaine)
    • •Category: Local Anesthetic
    • •MOA: Sodium Channel Inhibition
    • •Distinguishing Characteristics:
    • –Amide-linked local anesthetic.
    • –Topical and parenteral preparations
    • –Used as antiarrythmic
    • •Predictable Qualities:
    • –Most commonly used local anesthetic
    • –Low incidence of hypersensitivity
    • –Wide variance of applications
  37. PLF of Benzocaine
    • •Category: Local Anesthetic
    • •MOA: Sodium Channel Inhibition
    • •Distinguishing Characteristics:
    • –Ester-linked
    • –Low solubility
    • –Used topically
    • •Predictable Qualities
    • –Sunburn Ointments
    • –Over the counter
  38. PLF of Cocaine
    • •Category: Local Anesthetic and Sympathomimetic
    • •MOA: Sodium Channel Inhibition
    • •Distinguishing Characteristics:
    • –Ester-linked
    • –Sympathomimetic
    • –Inhibits norepinephrine uptake
    • –CNS stimulation (euphoria)
    • •Predictable qualities
    • –High abuse potential
    • –Vasoconstrictor
    • –Used in topical anesthesia of upper respiratory tract (mucosal vascular constriction)
  39. Levothyroxine
    • Category: Thyroid Drug
    • MOA: Bind to nuclear receptors that cause gene transcription and protein synthesis
    • Unique Characteristics:
    • –T4
    • –Converted to T3 (some in periphery, remainder in cell)
    • –Half-life 7 days
    • –80% bioavailability
    • –Metabolized in cytochrome P450 system
    • –Highly protein bound (99%+)
    • Predictable Actions
    • –Slow onset of action (Week or more)
    • –Daily administration
    • –Drug interactions due to metabolism and protein binding
    • –Drug of choice for replacement and suppression therapy
  40. Liothyronine
    • Category: Thyroid Drug
    • MOA: Bind to nuclear receptors that cause gene transcription and protein synthesis
    • Unique Characteristics:
    • –T3
    • –95% bioavailable
    • –Several times more potent than T4
    • –Similar protein binding and metabolism to T4
    • Predicted Actions:
    • –Less physiologic than T4
    • –Disturb thyroid function tests
  41. Iodide Salts
    • Category: Antithyroid
    • MOA: Inhibit release of thyroid hormones
    • Unique Characteristics:
    • –Include potassium iodide
    • –Rapid onset of therapeutic effect (2-7 days)
    • –Often accompanied by propylthiouracil therapy
    • –Metalic taste, hypersensitivity
    • Predicted actions:
    • –Treatment of thyroid storm with beta blockers
  42. Propylthiouracil
    • Category: Antithyroid Drug
    • MOA: Inhibit several steps in thyroid hormone synthesis (peroxidase steps and coupling)
    • Unique Characteristics:
    • –Accumulate and stored in thyroid
    • –Therapeutic effects must await exhaustion of stored hormones
    • –Cross placenta
    • Predictable Characteristics:
    • –Pregnancey Category D
    • –Long onset of therapeutic effect
  43. Radioactive Iodine
    • Category: Antithyroid
    • MOA: Diagnostic and chemical ablation
    • Unique Characteristics:
    • –Iodine isotope 131
    • –Rapidly absorbed
    • –Concentrated and stored in gland
    • –Emits beta rays with half-life of 5 days
    • –Painless and few side effects
    • –Cross placenta
    • Predicted Activity
    • –Destroy thyroid tissue
    • –Contraindicated in pregnancy
  44. Insulin
    • Category: Antidiabetic
    • MOA: Binds to insulin receptors    activates tyrosine kinase     phosphorylates proteins    alter metabolic enzymes. MOVES GLUCOSE INTO CELL FROM PLASMA
    • Unique Characteristics:
    • –Protein
    • –Short half-life (3-5 min)
    • –Multiple forms differ in solubility and release from site of injection.
    • Predictable actions:
    • –Causes decreased plasma glucose
    • –Treat type 1 diabetes and occasional type 2 diabetes
    • –Ineffective orally (Rx subcutaneously, usually)
    • –Repeated injections
    • –Will cause hypoglycemia when in excess
  45. Glucagon
    • Category: Pancreatic Hormone
    • MOA: Bind to receptors in liver cause increased cAMP and glycogenolysis and gluconeogenesis
    • Unique Characteristics:
    • Polypeptide (29 amino acids)
    • Half-life 3 to 6 min.
    • Predictable Actions:
    • –Raise blood glucose at expense of stored hepatic glycogen.
    • –Rx parenterally
    • –Emergency treatment of severe hypoglycemia
    • –Increased cAMP levels in heart may treat beta agonist toxicity
  46. Estrogens
    • Category: Estrogen
    • MOA: Bind to estrogen receptors in nuclei of target cells to regulate protein synthesis.
    • Unique Characteristics:
    • –Absorption varies widely with salt and formulation.
    • –Transdermal, oral, parenteral forms
    • –Highly protein bound, compete with thyroid and other drugs.
    • –Linked to breast cancer
    • Predicted actions:
    • –Hormone replacement therapy (postmenopausal)
    • –Oral contraception
  47. Progesterone
    • Category: Progestin
    • MOA: Bind to progesterone receptors in nuclei of target cells to regulate gene transcription in diverse cells.
    • Unique Characteristics:
    • –Rapidly absorbed following oral administration.
    • –Metabolized in liver on first pass.
    • Predictable Actions:
    • –Hormone Replacement Therapy (menopause)
    • –Contraception
  48. Clomiphene
    • Category: Antiestrogen
    • MOA: Partial antagonist at estrogen receptor.
    • Unique Characteristics:
    • –Blocks estrogen receptors in anterior pituitary
    • –Hot flashes similar to post-menopausal
    • Predictable Effects:
    • –Diminishes negative feedback inhibition
    • –Allows increase in LH and FSH
    • –Promotes ovulation
    • –Incidence of multiple pregnancy is 10%
    • –Used a fertility medication
  49. Mifepristone
    • Category: Antiprogesterone
    • MOA: Competetive antagonist of progesterone.
    • Unique Characteristics:
    • –Also known as RU 486 or “morning after pill”
    • –Prevents progesterone from maintaining endometrium for implantation
    • –Also binds to glucocorticoid receptor
    • Predicted actions:
    • –Emerging value as antineoplastic agent
  50. Oral Contraceptives
    • Category: Oral Contraceptive
    • MOA:
    • •Selective inhibition of pituitary function resulting in anovulation
    • •Change in cervical mucus
    • •Change in endometrium
    • •Uterine and fallopian tube motility
    • Unique Characteristics:
    • •Return to normal menstrual patterns following years of contraception
    • •Breast enlargement and diminished lactation
    • •Increase cortisol and cortisol binding proteins
    • •Increase thyroxin and thyroxin binding proteins
    • •Modifications in blood clotting
    • •Increased plasma triglycerides
    • •Increased risk of hypertension and myocardial infarct
    • Predictable actions:
    • •Contraception
    • •Treatment of Endometriosis
    • •Dysmenorrhea
  51. Progestin Oral Contraceptives
    • Category: Oral Contraceptives
    • MOA:
    • •Suppress ovulation
    • •Diminish endometrial implantibility
    • Unique Characteristics:
    • •Often accompanied by spotting and bleeding
    • •Available in depot forms for implantation
    • •Side effects include headache, dizziness, weight gain
    • Predictable Actions:
    • •Useful in patients for whom estrogen is undesirable
    • •Avoid side effects of estrogen including hepatic disease, hypertension and thromboembolism
    • •Less effective that combination contraceptives
  52. Prednisone
    • Category: Glucocorticoid
    • MOA: Modify gene transcription
    • Unique Characteristics:
    • •Short to medium acting
    • •Strong anti-inflammatory effect
    • •Orally effective
    • •Modest salt retention activity
    • Predictable characteristics
    • •Protein, lipid and carbohydrate metabolism
    • •Secondary followed by primary adrenal insufficiency with prolonged use
    • •Side effects customary of all glucocorticoids
  53. Calcium
    • Category: Mineral
    • MOA: Numerous effects in muscle, bone, cell membranes
    • Unique Characteristics:
    • •Incomplete absorption (30%) even in presence of Vitamin D
    • •Calcium carbonate absorption requires stomach acid, Calcium citrate absorption does not
    • Predictable Actions:
    • •Calcium citrate perferred in elderly
    • •Treat hypocalcemia
    • •Treat and prevent osteoporosis
    • •Constipation common side effect (Rx with fruits)
    • •Interacts with some drugs
  54. PLF of Alendronate (Fosamax)
    • Category: Bone resorption inhibitors
    • MOA: Prevent bone resorption by inhibiting osteoclasts.
    • –Prevent attachment of osteoclast precursor cells to bone
    • –Decrease metabolic activity of osteoclasts
    • Unique characteristics:
    • –Less than 5% absorbed from G.I. tract (less with food)
    • –Must take 30 minutes before eating in morning
    • –Half of absorbed drug deposited in bone
    • –Adsorb to hydroxyapatite and remains in bone
    • –Irritating to esophagus (erosions prevented by remaining UPRIGHT)
    • Predictable characteristics:
    • –Very long half-life (1 to 10 years)
    • –Rx osteoporosis, Paget’s disease, hypercalcemia
  55. Calcitonin
    • Category: Bone resorption inhibitor
    • MOA: Binds to receptors on osteoclasts inhibiting osteoclast activity
    • Unique Characteristics:
    • –Peptide secreted by parafollicular cells of thyroid
    • –Administered parenterally or via nasal inhalation
    • –Salmon calcitonin used and most potent
    • Predictable actions:
    • –Rx Osteoporosis, Paget’s disease, hypercalcemia
  56. Glyburide
    • Category: Oral Antidiabetic
    • MOA: Increase secretion of insulin and decrease secretion of glucagon
    • Unique characteristics:
    • –Sulfonylurea
    • –Effective orally
    • –Frequent drug interactions: thiazide diuretics, ACE inhibitors, ethanol (disulfiram-like effect)
    • –Metabolized in liver
    • –24 hour half-life
    • –Skin rashes (3% of patients)
    • –Occasional cholestasis
    • –Tachyphylaxis
    • Predicted actions:
    • –Treat type 2 diabetes
    • –Daily doses typically adequate
    • –May cause hypoglycemia
  57. Rosigliazone
    • Category: Oral Antidiabetic
    • MOA: Decrease insulin resistance by regulating genes involved in glucose and lipid metabolism.
    • Unique Characteristics:
    • –Often used in conjunction with other oral antidiabetic agents
    • –May cause fluid retention (edema)
    • –Used in prediabetics to prevent diabetes
    • Predicted Actions:
    • –Treat type 2 diabetes
    • –Slow onset (gene regulation)
    • –Weight gain is common
  58. Acarbose
    • Category: Oral Antidiabetic
    • MOA: Inhibit breakdown of polysaccharides in gut by inhibiting alpha-glucosidases.
    • Unique Characteristics:
    • –Target sucrase, maltase, glycoamylase, dextranase.
    • –Defer digestion and absorption of sugars to distal small intestine
    • Predicted actions:
    • –Lower post-meal glycemic levels
    • –Insulin sparing
    • –Flatulence, diarrhea and abdominal pain
  59. Testosterone
    • Category: Androgen
    • MOA: Bind to androgen receptor in nuclei to regulate protein synthesis.
    • Unique Characteristics:
    • –Converted to dihydrotestosterone by alpha reductase.
    • –Metabolized in liver to measurable metabolites.
    • –Some metabolized to estrogen.
    • –Rapidly absorbed from G.I. tract
    • –Used to treat endometriosis (especially Danazol)
    • –Used in treatment of osteoporosis
    • Predictable Actions:
    • –Increased muscle mass
    • –Contraindicated in pregnant women or women who may become pregnant
  60. Finasteride
    • Category: Antiandrogen
    • MOA: Inhibit 5-alpha reductase to prevent conversion of testosterone to dihydroxytestosterone.
    • Unique Characteristics: nothing remarkable
    • Predictable Actions:
    • –Diminish prostate size in BPH
    • –Treat hirsutism in women
  61. Actions of Vitamin D, Parathyroid hormone and Calcitonin
    • Vitamin D (increases serum Ca)
    • •Stimulates Ca absorption from G.I. tract
    • •Stimulates bone resorption
    • •Inhibit Ca excretion by kidney
    • Parathyroid hormone or PTH (increases serum Ca)
    • •Stimulates resorption of Ca by renal tubules
    • •Decreases resorption of phosphate by renal tubules
    • •Stimulate hydroxylation of vitamin D in kidney (active form)
    • •Increases bone resorption by osteoclasts
    • Calcitonin (decreases serum Ca)
    • •Inhibits resorption of Ca from bone
    •  

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