Pharm L16 Ach & AchE.txt

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kepling
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103704
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Pharm L16 Ach & AchE.txt
Updated:
2011-10-11 16:42:50
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Pharm L16 Ach AchE
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Pharm L16 Ach & AchE
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  1. Where are VAMPS (vSNARES) located?
    Presynaptic cleft on the vesicle containing Ach, ATP, etc..
  2. Where are SNAPs (t-SNAREs) located?
    Presynaptic cleft membrane itself
  3. What drug blocks SNAP & VAMP binding?
    Botulinum toxin
  4. What are the two cholinergic agonist receptors?
    • Muscarinic
    • Nicotinic
  5. What are the two cholinergic agonists and are they direct or indirect (specific or non-specific)?
    • Agonists: direct, rxn even w/o presence of nerve
    • Cholinesterase inhibitors: indirect, increase Ach, no rxn w/ no nerve present
  6. What happens to Nicotinic receptors during chronic stimulation?
    Desensitization
  7. What goes in and out of Nicotinic receptors?
    • In = Sodium
    • Out = potassium
  8. What are the 7 Direct acting cholinergic agonists?
    • (M & N)
    • Acetylcholine
    • Methacholine
    • Carbachol
    • (M only)
    • Bethanechol
    • Pilocarpine
    • Cevimeline
    • (N partial agonist)
    • Varenicline
  9. Three choline esters of Cholinergic agonists? importance?
    • Methacholine
    • Carbachol
    • Bethanechol
    • importance: AchE resistant
  10. What is the main Alkaloid of cholinergic agonists?
    Pilocarpine
  11. Why do arteries vasodilate in the presence of Acetylcholine although not innervated?
    There are M3 receptors on endothelial cells of BV that release NO
  12. 4 Function of M2 receptors in heart?
    • Bradycardia via A-V node conduction
    • Increase K current
    • Decrease cAMP
    • presynaptic = decrease NE release
  13. Pilocarpine: Group, sub-group, function, side effects
    • Group: Muscarinic Cholinergic agonists
    • Sub-group: Alkaloids (easily absorbed)
    • function: general M functions
    • Side effects: Excessive sweating, diarrhea, salivation
  14. Ach: Group, subgroup, side-effect
    • Group: M & N agonist
    • Subgroup: none
    • function: increase NO release (M3) = slow HR, decrease BP
    • side effect: bradycardia
  15. T/F Muscarinic agonists have a huge effect on the heart?
    F, M2 does not play a huge role
  16. Methacholine: Group, subgroup, function, side-effects
    • Group: M & N agonist
    • Sub group: Esters
    • Function: Bronchoconstric for asthmatic testing
    • side effect: choking if too much
  17. Bethanechol: Group, subgroup, function, side effects
    • Group: M agonist
    • Subgroup: esters
    • function: *PRINCIPAL GI/URINATION DRUG*
    • -GI tract
    • - Urinary Bladder/sphincters
    • side effect: sweating, etc...
  18. Carbachol: Group, subgroup, function, side effect
    • Group: M & N agonist
    • Subgroup: esters
    • Function: decrease intraocular pressure, constriction of pupil (rarely used)
  19. Most common drug to treat Xerostomia (dry skin)? Why?
    • Cevimeline
    • ** Less sweating than what Pilocarpine causes and longer lasting
  20. What is the physiological and competitive antagonist of the muscarinic system?
    • Physiologic: Epinephrine
    • Competitive: Atropine
  21. 4 contraindications to using Muscarinic agonists?
    • Ulcer
    • Coronary insufficiency
    • Asthma
    • Hyperthyroidism (more sensitive to Catecholamines)
  22. What type of desensitization do N receptors pass through?
    Rapid
  23. How does Nicotine work in the brain?
    Releases dopamine and increases alertness, attention and pleasure
  24. T/F nicotinic receptors in ganglion activate Sympathetics?
    • F, activate both PNS and SNS
    • SNS: hypertension, tachycardia
    • PNS: bradycardia, nausea, vomiting, diarrhea, urination
  25. Effects of Nicotinic stimulation?
    • **All receptors activated
    • ** muscle twitch followed by depolarizing block
    • hypertension followed by hypotension, convulsions, coma, respiratory arrest, paralysis
  26. Effect of Varenicline and how it works?
    • Help people stop smoking
    • * partial agonist on nicotine receptors and blocks effects of nicotine if smoking
  27. 3 main functions of Atropine?
    • Block muscarinic receptors
    • Anticonvulsants
    • Assist respiration
    • ** all help nicotinic toxicity **
  28. 4 major side effects of Varenicline?
    • Constipation
    • Flatulence
    • Sleep problems
    • psychosis (bad dreams)
  29. Name the five common Cholinesterase inhibitors (NECPOe)?
    • Neostigmine
    • Edrophonium
    • Carbamates
    • Physostigmine
    • Organophosphates: echothiopate
  30. Neostigmine: group, function, side effects
    • group: Ache inhibitors, reversible
    • function: fast hydrolysis, MG treatment
    • side effects: No CNS entrance
  31. Edrophonium: group, function, side effects
    • group: Ache inhibitors, reversible
    • function: short acting 5-20 min, injection only, diagnose MG
    • side effect: No CNS effect
  32. Carbamate: group, function, side effect
    • group: Ache inhibitors
    • function: slow hydrolysis, 30 min-6hr
    • side effect: 2-PAM not effective
  33. Physostigmine: group, function, side effect
    • group: Ache inhibitor
    • function:
    • - directly to eye for glaucoma treatment = no miosis
    • - Atropine overdose
    • side effect: tertiary, CNS entry
  34. Organophosphate qualities?
    • long lasting by phosphorylation of AchE
    • 2-PAM is an inhibitor if used before long lasting irreversible effects occur
  35. Pralidoxime (2-PAM) function and qualities?
    • group: Ache inducer
    • function: inhibit effects of organophosphates
    • side effects: No CNS effects, too much = Ache inactivation
  36. T/F AchE inhibitors are able to change BP?
    F, they have no effect on BP
  37. What disease is commonly treated with AchE inhibitors?
    Myasthenia gravis
  38. Best AchE drug to treat MG?
    Neostigmine
  39. How does Edrophonium diagnose MG?
    When given, it will cause muscles to strengthen for 5 minutes and then will dissipate
  40. How does dosage of Edrophonium change strength?
    • Too much = weakness from desensitization
    • Too little = increased strength
  41. Drug used for glaucoma and atropine overdose?
    Physostigmine
  42. Echothiophate use and qualities?
    • Use
    • organophosphate AchE inhibitor
    • decrease intraocular pressure
    • treat narrow-angle glaucoma until surgery
    • Qualities
    • quaternary, no CNS
  43. DFP use and qualities?
    • Use
    • organophosphate AchE inhibitor
    • Qualities
    • lipid soluble
    • easily absorbed into CNS
    • highly toxic
  44. Soman, Sarin, Tabun use and qualities?
    • Use
    • Nerve gas
    • organophosphate AchE inhibitor
    • Qualities
    • more potent and faster than DFP
  45. Parathion & Malathion use and qualities?
    • Use
    • pesticide, organophosphate AchE inhibitor
    • Qualities
    • lipid soluble
    • Malathion - safer b/c of less bird and mammal effect
    • Parathion - taken off market b/c poisonous
  46. Name the two direct agonists and the two AchE inhibitors used to treat glaucoma?
    • Direct: Pilocarpine, Carbachol
    • AchE inhibitors: Physostigmine, Echothiophate
  47. What drugs are used to reverse NMJ blockade after surgery?
    cholinesterase inhibitors or Ach agonists
  48. Toxicity of AchE inhibitors?
    • SLUDGE: salivation, lacrimation, urination, defectation, GI distress, emesis (all PSN effects)
    • Miosis, sweating, bronchoconstriction
    • Heart: bradycardia & hypotension
    • CNS: confusion, slurring, convulsions, coma
    • NMJ: stimulation then paralysis after time
  49. What three drugs are used in combination to treat organophosphate AchE inhibitor poisoning?
    • Atropine: blocks Ach effects and antagonizes M receptors
    • 2-PAM: reactivates AchE (give quickly)
    • Diazepam: if convulsions have started

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