341 - Cholinergic Agonist Drugs

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estee08
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107898
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341 - Cholinergic Agonist Drugs
Updated:
2011-10-10 21:29:08
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pharmacy
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PHAR 341 Cholinergic Agonist Drugs
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  1. Acetylcholine (ACh)
    • Non-Selective Direct-Acting Cholinergic Agonist (drugs that activate both nicotinic and muscarininc receptors)
    • Administered iv, short duration of action
    • Most the effects are muscarinic (it activates muscarinic receptors at low dose and sympathetic ganglion nicotinic receptors at high dose or a muscarinic blocker is co-administered)
    • Muscarinic Effects: All the effects of increased parasympthathetic tone, hypotension (leads to reflex tachychardia via baroreceptor reflex), does not cross blood-brain barrier, inotropy (decreased force of heart contraction), sweating (because ACh effects sympathetic muscarinic sweat glands)
  2. Carbachol
    • Non-Selective Direct-Acting Cholinergic Agonist (drugs that activate both nicotinic and muscarininc receptors)
    • Longer action than ACh
    • Little use therapeutically
    • Glaucoma Treatment
  3. Bethanechol
    • Muscarinic Receptor Selective Direct Acting Cholinergic Agonist
    • It's resistant to cholinesterases so it has a longer action than ACh
    • Oral dose that effects GI and urinary tracts
    • Urinary Retention: treats this by increasing urge to urinate
    • Gastroesophageal Reflux: treats this by increasing the speed of gastric emptying
  4. Pilocarpine
    • Muscarinic Receptor Selective Direct Acting Cholinergic Agonist
    • Longer action than ACh
    • Open Angle Glaucoma
    • Xerostomia: a condition of having dry mouth, this drug will increase salivation
  5. Muscarinic Receptor Subtypes
    • Muscarinic receptors are G-protein Linked
    • M1: stimulatory - increases parasympathetic tone, increases saliva production, increases stomach acid release
    • M2: inhibitory - decreases heart rate, decreases force of contraction, opposes sympathetically-mediated relaxation in the GI and Bladder smooth muscle
    • M3: stimulatory - contraction of GI and Bladder wall muscles, relaxation of bladder sphincter, bronchoconstriction, contraction of the pupil (miosis), increased salivation
    • M4 (inhibitory) and M5 (stimulatory): minor
  6. Cevimeline
    • Activates M1 and M3 receptors which are prevalent in salivary glands
    • Sjorgen's Syndrome: autoimmune disorder of mucous membranes which causes dryness of the mouth, skin, nasal, and vaginal passages. This drug increases salivation but causes a lot of nausea (because this drug stimulates the gut - M1 and M3 effects)
  7. Nicotine
    • Nicotinic Receptor Agonist (activates alot of neuronal and a little NMJ nictonic receptors)
    • Activates both sympathetic and parasympathetic ganglion
    • Effects: CNS stimulation, CNS mediated nausea, CNS temor and convulsions, hypertension, tachycardia, bronchoconstriction, diarrhea, initial salivary and bronchial secretion (followed by inhibition), PNS stimulation followed by desensitization of autonomic ganglia and skeletal muscle (so prolonged use of nicotine makes you feel relaxed)
    • Cessation of smoking
  8. Epibatidine
    • Nicotinic Receptor Agonist
    • High affinity for neuronal and NMJ nicotinic receptors
    • Potent analgesic
    • Isolated from poison dart frog
    • Too toxic to be used therapeutically
  9. Edrophonium
    • Indirect-Acting Cholinergic Agonist (Acetylcholinesterase inhibitor)
    • Reverse paralysis of non-depolarizing neuromuscular blockers
    • Myasthenia gravis diagnostic agent
    • Toxicity Effects: Increased parasympathetic tone effects, increased sweating, initial muscle spasms leading to muscle weakness, DUMBELS
  10. Neostigmine
    • Indirect-Acting Cholinergic Agonist (Acetylcholinesterase inhibitor)
    • Postoperative ileus (intestine stops contracting)
    • Postoperative urinary retention
    • Toxicity Effects: Increased parasympathetic tone effects, increased sweating, initial muscle spasms leading to muscle weakness, DUMBELS
  11. Pyridostigmine
    • Indirect-Acting Cholinergic Agonist (Acetylcholinesterase inhibitor)
    • Myasthenia Gravis
    • Toxicity Effects: Increased parasympathetic tone effects, increased sweating, initial muscle spasms leading to muscle weakness, DUMBELS
  12. Parathion, Diazinon, Malathion
    Former insectides
  13. DUMBELSSS
    • Effects of a high dose of an acetylcholinesterase inhibitor (increases ACh effect)
    • All are parasympathetic effects (unless noted)
    • Diarrhea
    • Urination
    • Miosis
    • Muscle weakness (NMJ effect)
    • Bronchospasm
    • Excitation
    • Lacrimation
    • Seizures
    • Sweating (sympathetic)
    • Salivation (para and symp)
  14. Pralidoxime
    • Quickly reactivates acetylcholinesterase (leads to decreased ACh)
    • Only works acutely
    • Given orally with an onest within 1 hour

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