Ch. 14 Review-Pharm

  1. muscarinic receptor locations:
    sweat glands, blood vessels, all organs of parasympathetic nervous system
  2. nicotinic N receptor locations:
    all ganglia of the autonomic nervous sx.
  3. Nicotinic M receptor location:
    neuromuscular junction
  4. effects of muscarinic receptor activation:
    decrease heart rate, increase gland secretion, smooth muscle contraction
  5. effects of nicotinic M receptor activation:
    promotes ganglionic transmission
  6. muscarinic receptor agonists:
    • bethanecol
    • choinesterase inhibitors: physostigmine, neostigmine
  7. muscarinic receptor antagonists:
  8. effects of nicotinic N receptor activation:
    promotes ganglionic transmission
  9. nicotinic N receptor agonists:
  10. nicotinic N receptor antagonists:
  11. receptor location for nicotinic M:
    neuromuscular junciton
  12. Nicotinic M effects of receptor activation:
    skeletal muscle contraction
  13. nicotinic M receptor agonists:
    nicotine (must be in much higher doses than nicotinic n receptors)
  14. nicotinic M receptor antagonists:
    d-Tubocurarine, succynilcholine
  15. muscarinic agonists are also known as:
    parasympathomimetic agents
  16. Bethanecol (urecholine) mechanism of action:
    direct acting muscarinic agonist, binds reversibly to muscarinic cholinergic receptors and causes activation
  17. pharmacologic effects of Bethanecol:
    • muscarinic effects:
    • bradychardia
    • increase secretions including sweat
    • GI motility
    • bladdy emptying
    • vascular dilation
    • pupil constriciton
  18. pharmacokinetics of bethanecol:
    • oral administration only
    • effects begin 30-60 min after admin.
    • crosses membranes poorly and therefore only a small portion of administered dose is absorbed
  19. therapeutic use of Bethanecol:
    • urinary retention
    • GI- investigational basis for gastroesohageal reflux
  20. bethanecol adverse effects:
    • cardiovascular: hypotension and bradychardia
    • GI: increase motility, diahrrea, excess salivation, increase gastric acid
    • lungs: exacerbation of asthma from bronchoconstriction
    • urinary tract: increases pressure in bladder and causes voiding
    • thyroid pts- causes dysrythmias
  21. Bethanecol preparations, dosages and administration:
    • available in tablets 5,10,25,50; for adults 10-50mg q 3-4x daily
    • given an hour before or 2 hours after a meal because it causes vomiting and nausea
  22. Cevimeline (Evovax):
    • for relief of xerostomia caused by Sjogren's syndrome
    • activates muscarinic receptors

    adverse: same as muscarinic activation- excess sweating, nausea, rhinitis, diarrhea

    contraindicated: uncontrolled asthma

    drug interaction: intensifies cardiac depression from beta blockers(both drugs decrease heart rate)

    preparations: 30mg capsules, dose=30mg x3 daily
  23. Pilocarpine (Salagen):
    is a muscarine agonist for topical therapy of glaucoma and oral therapy of dry mouth
  24. acetylcholine (Miochol-E):
    • primarily acts to produce rapid pupil constriciton,
    • lacks selectivity
    • extremely short half life
  25. muscarine:
    • not used clinically
    • has role in discoery of cholinergic receptor cybtypes
    • toxic and found in certain mushrooms
  26. sources for muscarinic poisoning:
    certain mushrooms, OD from direct-acting muscarinic agonists (bethanecol, pilocarpine) and cholinesterase inhibitors
  27. symptoms of muscarinic poisoning:
    profuse salivation, lacrimation, visual disturbances, bronchospasm, diarrhea, bradycardia, hypotension
  28. treatment of muscarinic poisoning:
    atropine becuase it is selective and blocks the receptors for muscarine and it reverses the signs of toxicity
  29. muscarinic antagonists (anticholinergic drugs):
    • atropine
    • OAB DRUGS:(overactive bladder)
    • -oxybutinin-Ditropan, Ditropan XL, Oxytrol
    • -darifenacin-Enablex
    • -solifenacin-Vesicare
    • -tolterodine-Detrol, Detrol LA
    • -trospium-Santura, Sanctura XR
    • scopolamine
    • ipatropium bromide
    • antisecretory anticholinergics
    • dicyclomine
    • pirenzepine
    • telenzepine
    • mydriatic cycloplegics
    • centrally acting cholinergics
  30. sources of antimuscarinic poisoning:
    • atropa belladonna
    • datura stramonium
    • antihistamines
    • phenothiazines
    • tricyclic antidepressants
  31. symptoms of antimuscarinic poisining:
    • direct result of muscarinic blockade:
    • dry mouth, blurred vision, photophobia, hyperthermia, CNS effects, skin that it hot,dry and flush
Card Set
Ch. 14 Review-Pharm
pharmacology test 2-ch 14