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Cholinomimetics
pharmacology
11
Pharmacology
Professional
02/21/2012

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Cards

Term
Acetylcholine
Definition
Direct Acting Muscarinic Agonist

Problem with using it as drug b/c it has short 1/2 life due to ACHe in plasma that breaks it down so it won't bind as much to receptor and it's way too non-specific b/c it binds at N and M receptors
Term
Bethanechol
Definition
Direct Acting Muscarinic Agonist

-more selective for urinary bladder and GI tract than BV and heart

therapeutic uses:
-post operative abdominal distension and urinary retention
-neurogenic atony of the urinary bladder with retention

NONOBSTRUCTIVE
Term
Pilocarpine
Definition
Direct Acting Muscarinic Agonist

Therapeutic uses:
-Sjogren's syndrome (autoimmune disease that effects moisture producing glands (decreases salivary secretion)
-radiation induced dry mouth
Term
Cevimeline
Definition
Direct Acting Muscarinic Agonist

-newer drug for sjogren's syndrome
-works relatively selectively on salivary glands
-longer lasting salivation effect (4-6 hr) and fewer side effects than pilocarpine
Term
Muscarine
Definition
Direct Acting Muscarinic Agonist

-not a drug
-present in Inocybe and clitocybe mushrooms
-mushroom poisioning
Term
what's the MOA for direct acting muscarinic agonists?
Definition
Bind to and activate muscarinic receptors
Term
What are the effects of activating muscarinic receptors on the heart, BV, ciliary m., iris sphincter, GI tract, bladder?
Definition
decrease HR, vasodilation (via NO), contraction/near vision, miosis, increase activity of gut, micturition
Term
Would you use Bethanechol to treat BPH?
Definition
No

-not getting rid of the obstruction, just squeezing bladder so still can't urinate
Term
what effect does muscarinic receptor activation have on glands?
Definition
M3; coupled to Gq; increases Ca+2 and increases secretion
Term
what symptoms might you expect to see in a person who has mushroom poisioning from Inocybe mushrooms?
Definition
salivation, sweating, intestinal cramps/NVD (nausea, vomiting, diarrhea)
Term
What are the adverse effects of direct acting muscarinic agonists?
Definition
stomach: increased gastric acid secretion-->aggravate ulcer
BV: dilation
Heart: bradycardia or reflex tachycardia
HYPOTENSION (decreased PVR b/c VD)

*baroreceptors can override the direct decrease in HR due to M receptor activation by the drug

lungs: increase secretion and bronchoconstriction so difficulty breathing/asthma attack

eye: spasm of accomodation; miosis
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