Pharmacology Exam 3

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Rx2013
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44039
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Pharmacology Exam 3
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2010-10-21 15:57:13
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Cholinergic Agonists
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Cholinergic Agonists
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  1. Acetylcholine site of action
    • cholinergic agonist
    • muscarinic receptors
    • nicotinic receptors
  2. Properties of Acetylcholine
    • rapidly hydrolized
    • for surgical use only to constrict iris
  3. Physiological effect of ACH at lower doses
    • muscarinic action
    • Blood pressure
  4. Physiological effect of acetylcholine at higher doses
    • ganglionic
    • primarily nicotinic
    • parasympathetic effects
  5. Respiratory effects of acetylcholine
    • bronchoconstricion
    • increased mucous
  6. GI effects of acetylcholine
    digestion and motility
  7. Methacholine
    • ACH-CH3
    • cholinergic agonist
    • muscarinic specific
    • little nicotinic effect
  8. uses of methacholine
    • diagnosis of asthma
    • use a B2 agonist to overcome the effect
  9. Bethanechol
    • cholinergic agonist
    • little nicotinic effect
    • highly resistant to AChE and Pseudocholinesterase
    • used for systemic effects
  10. Uses of Bethanechol
    • urinary retention
    • abdominal distention
    • gastric atony (no movement)
  11. Avoid used of bethanechol with
    • GI obstruction
    • leads to ischemia and tissue necrosis
  12. Adverse reactions that occur with muscarinic cholinergic agonists
    • salivation
    • nausea
    • GI cramping
    • warm, sweating
    • faintness
  13. Nicotine
    • cholinergic agonist
    • activates neuromuscular junction
    • leads to depolarization block (overstimulation)
    • activates chemoreceptors
    • stimulates respiration
  14. Carbachol
    • cholinergic agonist
    • little hydrolysis at AChE and PSChE
    • high nicotinic effect
    • some muscarinic effect (GI/Bladder)
  15. Use for carbachol
    • glaucoma
    • causes miosis
    • enhances aqueous humor outflow (muscarinic)
  16. muscarine
    • cholinergic agonist
    • mushrooms
    • hypotention
    • decreased HR
    • increased gland secretions
  17. Pilocarpine & Cevimeline
    • cholinergic agonist
    • tertiary amines that cross BBB
  18. Pilocarpine use
    • glaucoma treatment
    • xerostomia
  19. side effects of pilocarpine and cevimeline
    sweating
  20. cevelemine
    • cholinergic agonist
    • m1 and m3 selective
    • fewer side effects
    • less toxicity
  21. Reversible AChE inhibitors
    • cations
    • competitively bind to the anionic site of AChE
  22. Edrophonium
    • reversible AChE inhibitor
    • quaternary alcohol (cannot cross BBB)
    • differential diagnosis of myasthenia gravis
  23. Physostigmine
    • reversible AChE inhibitor
    • freely crosses BBB
    • glaucoma
    • myasthenia gravis
    • reverse mydriasis or NMJ blockade
  24. Neostigmine
    • reversible AChE inhibitor
    • quaternary amine (can't cross BBB)
    • nicotinic agonist (NMJ)
    • reversible AChE inhibitor
  25. Neostigmine uses
    • myasthenia gravis
    • glaucoma
    • NMJ blockade reversal (curariform toxicity)
    • GI and Urinary atony
    • Antimuscarinic drug overdose (Atropine)
  26. Donepezil & Rivastigmine
    • treat alzheimer's disease
    • reversable AchE inhibitors
  27. Direct acting cholinergic agonists
    • acetylcholine
    • Metacholine
    • Bethanechol
    • Muscarine
    • Pilocarpine
    • Cevimeline
    • Nicotine
    • Carbachol
  28. Reversible AChE inhibitors
    • Edrophonium
    • Physostigmine
    • Neostigmine
    • Donepezil
    • Rivastigmine
  29. Irreversible AChE inhibitors
    • Organophosphates
    • covalently bind to the esteratic side of AChE
    • insecticide
    • sarin gas
  30. Use of irreversible AChE inhibitors leads to:
    overstimulation of parasympathetics leading to paralysis of respiratory muscles
  31. Treatments for exposure to irreversible AChE inhibitors
    • vital sign maintenance
    • atropine
    • pralidoxime
    • bzd's
  32. Toxicology of AChE Inhibitors 1st symptoms
    • Muscarinic effects
    • miosis
    • tightness of chest
    • salivation/sweating
    • bradycardia
  33. Toxicology of AChE inhibitors 2nd effect
    • Nicotinic effects
    • skeletal muscle fasciculations
    • weakness
    • paralysis
  34. Toxicology of AChE inhibitors (3rd phase)
    • CNS
    • restless/anxiety
    • confusion
    • convulsion
  35. 4th toxicological effect of AChE inhibitors
    • respiratory arrest
    • paralysis of muscles
    • central depression of respiration
    • airway obstruction (increased secretions)
  36. Used for Glaucoma
    • pilocarpine
    • physostigmine
  37. used for paralytic ileus and bladder atony
    • bethanechol
    • neostigmine
  38. used for xerostomia
    • pilocarpine
    • cevimeline
  39. used for myasthenia gravis
    • edrophonium (diagnosis and dose check)
    • neostigmine
  40. antidote for atropine poisoning or TCA overdose
    physostigmine
  41. Used for alzheimer's/dementia
    • donepezil
    • rivastigmine
    • galantamine
  42. other uses for cholinergic agonsits
    • paroxysmal supraventricular tachycardia
    • edrophonium for specific arrhythmias
  43. Toxicity of direct actin muscarinic stimulants
    • N/V
    • Diarrhea
    • Urination/Salivation/Sweating
    • cutaneous vasodilation
    • bronchial constriction
  44. Acute toxicity of direct acting nicotinic stimulants
    • central stimulant
    • depolarization blockade => respiratory paralysis
    • HTN and arrhythmias
  45. Chronic toxicity of direct acting nicotinic stimulants
    • vascular disease risk
    • sudden coronary death
    • ulcer recurrences
    • varenicline (partial agonist)
  46. Major pharmacologic effects of muscarinic receptors
    • SLUDGE
    • Salivation
    • Lacrimation
    • Urination
    • Defication
    • GI motility
    • Emesis
  47. Myasthenia gravis
    • autoantibodies against alpha 1 subunit of the nicotinic receptor
    • results in weakness of commonly used voluntary muscles
  48. Makes Myasthenia gravis worse
    • activity
    • aminoglycosides
  49. Myasthenia gravis vs. cholinergic crisis
    • myasthenia needs more AChE inhibition
    • Crisis needs less AChE inhibition
    • edrophonium used to distinguish

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