BMSII_Dr.Rorabaugh_Drugs

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BMSII_Dr.Rorabaugh_Drugs
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2012-01-16 15:09:44
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BMSII_Dr.Rorabaugh_Drugs
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  1. Acetylcholine(MIOCHOL-E)
    • Choline ester, N, M Agonist
    • Metabolism: Ach.esterase, Psudoesterase
    • Therapeutic use: production of miosis during ophthalmic surgery (MIOCHOL-E)
    • 5-10s 1/2 life, IM, SubQ for local effects
  2. Methacholine(PROVOCHOLINE)
    • Choline ester, Selective M Agonist, little activity on N receptor
    • Metabolism: more resistant to Ach.esterase
    • Therapeutic use: diagnosis of bronchial hypersensitivity
    • Systemic use is limited due to cardiovascular effects, Longer 1/2 life
  3. Carbachol(CARBOPTIC)
    • Choline ester, Selective N Agonist
    • Metabolism: completely resistant to Ach.esterase
    • Therapeutic use: wide angle glaucoma
    • Greater effects on S.M. of eye, GI, urinary bladder than cardiovascular S.M.
  4. Bethanechol(URECHOLINE)
    • Choline ester, Selective M Agonist (Spe. GI, urinary)
    • Metabolism: completely resistant to Ach.esterase and pseudoesterase
    • Therapeutic use: stimulates GI and urinary bladder
  5. Muscarine
    • Cholinomimetic alkaloids
    • Only M Agonist
    • No therapeutic application
    • from Amanita muscaria
  6. Nicotine
    • Only N Agonist
    • Therapeutic use: smoking cessation
    • Has been used as an insecticide
  7. Pilocarpine(SALAGEN, PILOCAR)
    • Selective M Agonist
    • Therapeutic use: xerostomia, ophthalmic solution for side angle glaucoma
    • Derived from the Pilocarpus
  8. Physostigmine(eserine)
    • Reversible Carbamate Ach esterase inhibitors
    • Therapeutic use: wide angle glaucoma, antidote for atrpine toxicity
    • Lipophilic, 0.5-2hr 1/2 life, ordeal poison
  9. Neostigmine
    • Reversible Carbamate Ach esterase inhibitors
    • Therapeutic use: Myasthenia gravis, stimulation of atonic S.M. of GI and urinary bladder, Reversal of neuromuschular blockade induced by curare, pancuronium, and skeletal muscle relaxant
    • Stimulates Nm receptors in skeletal muscle
    • No CNS effect (charged), 0.5-2hr 1/2 life
  10. Pyridostigmine, ambenonium, demacarium
    • Reversible Carbamate Ach esterase inhibitors
    • Therapeutic use: myasthenia gravis
    • Stimulates Nm receptors in skeletal muscle
    • No CNS effect, 3-8hrs
  11. Edrophonium
    • Reversible noncarbamate Ach esterase inhibitors
    • Therapeutic use: diagnosis of myasthenia gravis
    • Stimulates Nm receptors in skeletal muscle
    • Quick onset, short duration (5-15min)
  12. Galantamine, Tacrine
    • Reversible noncarbamate Ach esterase inhibitors
    • Therapeutic use: Alzheimer's disease
  13. diisopropylfluorophosphate(DFP)
    • Irreversible organophosphate Ach esterase inhibitors
    • Therapeutic use: glaucoma (ointment)
    • lipid soluble, low MW, volatile = inhalation and transdermal, last 4 weeks, retina detachment and cataracts possible
  14. ecothiophate
    • Irreversible organophosphate Ach esterase inhibitors
    • Therapeutic use: glaucoma
    • aqueous solution, no CNS, last 4 weeks
  15. parathion
    • Irreversible organophosphate Ach esterase inhibitors
    • converted to paraoxon-active metabolite
    • Use: insecticide (not used anymore)
  16. malathion(Chemathion, Mala-spray)
    • Irreversible organophosphate Ach esterase inhibitors
    • converted to malaoxon
    • Use: insecticide, for lice (safe due to plasma carboxylesterase in mammals)
  17. sarin, tabun, soman
    • Irreversible organophosphate Ach esterase inhibitors
    • Use: nerve gas
  18. Pralidoxime (2-PAM)
    • causes hydrolysis of the organophosphate from Ser of Ach esterase
    • Therapeutic use: reverses Irreversible organophosphate Ach esterase inhibitors
  19. Atropine
    • competitive muscarinic antagonist
    • Therapeutic use: to induce mydriasis, cylcloplegia, prevent respiratory secretions during surgery, Parkinson's disease, Decrease AV node block when vagal tone is hihg, antidote for Achesterase inhibitors, diarrhea (with Diphenoxylate)-Lomotil
  20. Scopalamine
    • competitive muscarinic antagonist
    • Therapeutic use: Prevents motion sickness
    • CNS effects
  21. Glycopyrrolate
    • competitive muscarinic antagonist
    • Therapeutic use: inhibit GI motility, Peptic ulcer, Reduce salivation and bronchial secretion during surgery
  22. Propantheline
    • competitive muscarinic antagonist
    • Therapeutic use: prevent spasms of GI smooth muscle, peptic ulcer
  23. Prienzepine
    • competitive muscarinic antagonist
    • Therapeutic use: inhibits gastric acid secretion
    • Selective for M1 and M4
  24. Ipratropium
    • competitive muscarinic antagonist
    • Therapeutic use: chronic obstructive pulmonary disease (aerosol), rhinorrhea associated with common cold
  25. Oxybutynin
    • competitive muscarinic antagonist
    • Therapeutic use: relieve bladder spasms following urologic surgery(prostatectomy), incontinence with neurologic diseases
  26. Tolterodine(Detrol)
    • competitive muscarinic antagonist
    • Therapeutic use:incontinence
    • Selective for M3
  27. Opthamology(mydriasis, cycloplegia) M receptor antagonists
    • Atropine: 7-10 days
    • Scopalamine: 3-7 days
    • Homatropine: 1-3 days
    • Tropicamide: 0.25 days
  28. M receptors
    • M1: neurons, some glands, CNS
    • M2: myocardium, smooth muscle, CNS
    • M3: smooth muscle, glands, endothelium, CNS
    • M4: smooth muscle, glands, CNS
    • M5: CNS
    • GPCR
  29. Direct-Acting Sympathomimetic Drugs
    a1
    • Epi, NorEpi
    • Phenylephrine
    • Methoxamine
    • Mephentermine
    • Metaraminol
    • Midodrine
  30. Direct-Acting Sympathomimetic Drugs
    a2
    • Epi, NorEpi
    • Peripheral: Oxymetazoline, Tetrahydrozoline, Naphazoline
    • CNS: a-Methyldopa, Clonidine, Guanabenz
    • apraclonidine
    • Guanfacine
    • bromidine
  31. Direct-Acting Sympathomimetic Drugs
    b1
    • Epi, NorEpi, Isoproterenol
    • Dobutamine
    • Dopamine
  32. Direct-Acting Sympathomimetic Drugs
    b2
    • Epi, Isoproterenol
    • Terbutaline
    • Albuterol
    • Levalbuterol
    • Bitolterol
    • Ritodrine
    • Salmetertol
    • formoterol
  33. Amphetamine/methamphetamine
    • Orally active
    • CNS effects
    • MOA: induce the relase of NorEpi
    • Increase BP, decrease CO by baro
    • Meth has greater CNS effects over Am
    • Uses: suppress appetite(Dexedrine), narcolepsy, ADHD, cocaine-dependece, reverse fatigue, increase altertness
  34. Methylphenidate (Ritalin)
    • orally active, sig. for abuse
    • Uses: ADHD, narcolepsy
  35. Tyramine
    • Metabolite of tyrosine in fermented foods, not a therapeutic drug
    • Caution with MAO inhibitors
    • MOA: induces the release of NorEpi
    • Foods: Cheese, Meat, Fruit(figs, raisins), Fermented beverages (beer, wine), soy sauce, yogurt
  36. Tricyclic antidepressants
    • desipramine, imipramine, amitriptyline, clomipramine, nortriptyline, cocaine
    • MOA: prevent reuptake of NorEpi, also inhibits reuptake of serotonin and dopamine
  37. Cocaine
    MOA: prevent reuptake of NorEpi, also inhibits reuptake of serotonin and dopamine, blocks VG Na channels (anesthetic for opthamology)
  38. Monoamine oxidase inhibitors
    • Phenelzine, Tranylcypromine, Isocarboxazid, Pargyline, Selegeline
    • Selegeline is MAO B selective
    • MOA: Inhibit MAO irreversibly
    • Danger of fatal hypertensive crisis: Tyramine, Methylphenidate, Amphetamine, Meth, Tri. antidepressants
  39. Ephedrine
    • Agonist at a and b
    • Enhances release of NorEpi
    • orally effective, Increase CO, BP=stroke!
    • Uses: Asthma (decrease likelyhood of acute asthma attack), Nasal congestion, Enhance athletic performance, Weight loss
  40. Pseudoephedrine (Sudafed)
    • Weak agonist at a, no activity at b
    • Enhances release of NorEpi
    • Uses: Nasal congestion
  41. Phenylpropanolamine
    • Agonist at a but little activity at b
    • Enhances release of NorEpi
    • Uses: Nasal congestion and weight loss
    • Discontinued due to hemorrhagic stroke
  42. Cariovascular
    • Cardiac Arrest: Epi, dobutamine
    • Cardiogenic Shock: dopamine, dobutamine
    • Cariac arrhythmias: AV node block=isoproterenol, paroxysmal atrial tachycardia=phenylephrine, methoxamine
    • Hypotension: phenylephrine, methoxamine, norepinephrine
    • Essential Hypertension: clonidine, guanabenz, a-methyldopa
  43. Respiratory (asthma, COPD)
    • Short acting: albuterol, rebutaline, metaproterenol, epinephrine (<1hr)
    • Long acting: salmeterol (12hr)
  44. Nasal Congestion
    pseudoephedrine, ephedrine, phenylephrine, oxymetazoline, naphazoline
  45. Uterus
    Delay premature labor: ritodine, terbutaline
  46. Ophthalmic
    • Induce mydriasis: phenylephrine
    • Wide angle glaucoma
    • Ocular congestion: phenylephrine, tetrahydrozoline
  47. Anaphylactic shock
    • Epi(b2)
    • Severe allergic reactions
  48. Increase duration of action of local anesthetics
    Epi

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