Shared Flashcard Set

Details

Direct Cholonergic Pharm.
Ach, Bethanecol, Methacholine, carbachol...
6
Medical
Professional
01/08/2013

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Cards

Term
Acetylcholine
Definition
endogenous transmitter has no therapeutic values
• not specific (nicotinic and muscarinic receptors are activated)
• readily hydrolyzed by AChE (esterases) [~ 5-20 s effect after large IV bolus]
• would activate non-discriminately parasympathetic and sympathetic
Term
Bethanecol
Definition
relatively selective for muscarinic receptors involved in GI and bladder control
• specific (Parasympathomimetic), with less activity at Nicotine receptor
• not readily hydrolyzed by AChE
• promotes GI / bladder motility in atony or in neurogenic bladder or paralytic ileus
• does not cross BBB
• side effects: sweating, urinary urgency, diarrhea, decreased BP and HR, nausea, abdominal pain, bronchoconstriction and spasms (asthma patients: be careful), increased salivation (sialogogue) and lacrimation
Term
Methacholine
Definition
• Bit more specific for muscarinic receptors
• less hydrolyzed by AChE
• Used as methacholine challenge test (MCT; bronchoprovocation test for asthma) in patients with normal spirometric readings but complain of chest tightness and difficulty breathing
Term
Carbachol
Definition
relatively selective for nicotinic receptors, but still has significant activity at muscarinic receptors
• Not hydrolyzed by AChE
• promotes miosis of iris (constrict sphincter); prior to occular surgery (miostat )
• Topical application (glaucoma
Term
Pilocarpine
Definition
used to treat in glaucoma (emergency) and xerostomia
• specific (muscarinic receptor agonist)-comes from a shrub (Pilocarpus jaborandi)
• not hydrolyzed by AChE
• causes miosis of iris (constrict sphincter); decreases intra-ocular pressure, and causes blurred vision (constrict ciliary muscle “forcing” near-vision)
• crosses BBB
Term
Cevimeline
Definition
useful in treatment of xerostomia as in the case of Sjogren’s disease; antineoplastic agents; neck radiation; aging.
• specific muscarinic receptor agonist at M1 and M3
• cheaper than pilocarpine (3tid instead of 4)
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