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23 Cards in this Set
- Front
- Back
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Muscarinic Agonists
-Subtypes? (2) |
-Synthetic choline esters
-Naturally occurring |
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Choline Esters
-Stucture? -Resistent to? -Selective for? |
-Structurally similar to Ach
-Resistent to ChEs -Selective for Muscarinic subtype |
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2 common Choline Esters
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-Bethanechol
-Carbachol |
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Cardiovascular Effects of Ach (muscarininc agonist)
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-Little effect due to limited innervation
--Exception in atrium of heart |
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Cardiovascular Effects of Muscarininc Agonists
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-In heart:
--Negative inotopic --Negative chronotropic --Negative dromotropic |
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Muscarinic Effects on Vasculature
-Effects which receptor? -Effects (2)? |
-Activation of M3 receptors in endothelium
-Decreased PR -Vasodilation (thru NO) --cGMP and a decrease in phosphorlyated myosin light chain |
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Muscarinic Agonists
Side effects on cardio(2) |
-Bradycardia
-AV Block |
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Muscarinic Agonists
-GI Effects (2) |
-Increased Intestinal Motility
-Increase GI secretions |
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Muscarinic Agonists
GI side effects (3) |
-Nausea
-Cramps -Diarrhea |
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Muscarinic Agonists
GI effects-Clinical Use (1) |
-Increase GI motility (post-surgical)
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Muscarinic Receptors
Effect on Urinary Tract (1) |
-Promote micturition
--Relax trigone --Relax external sphincter --Contract detrusor |
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Muscarinic Receptors
Clinical Use for Urinary Tract (1) -Drug used |
-Useful in urinary retention
-Bethanechol |
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Bethanechol
-MOA? -Uses (2) |
-Selectivity for muscarinic receptors in urinary system
-Enhance intestinal activity -Promote urination |
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Advantage in using Bethanechol compared to carbachol or methacholine?
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Reduced cardiovascular SEs
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Muscarinic Effects
-Eye (3) |
-Contract sphincter muscle to produce miosis (pupillary constriction)
-Contract ciliary muscle to produce accommodation of the lens for near vision -Ciliary contraction opens spaces of trabecular network to enhance aqueous humor outflow through Canal of Schlemm --Reduces intraocular pressure |
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Muscarinic Agonists
Effects on the Lung (2) |
-Stimulates secretions
-Contracts bronchial smooth muscle |
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Muscarinic Agonists
Effects on Glands (1) |
-Stimulates secretion of:
--Tear ducts (lacrimal) --Salivary --Nasopharyngeal --Sweat |
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Uses of Muscarinic Agonists
2 -How are they administered? |
-Stimulate intestine and bladder
--Given orally -Open angle glaucoma --Topical application |
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First choice for muscarinic agonist in urinary system effects?
-Do NOT use in what cases (1)? |
-Bethanechol
-Do NOT use in cases of intestinal obstruction |
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MOA of muscarinic agonists in open angle glaucoma?
-Drug used? |
-Enhance aqueous humor outflow
-Carbachol |
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Muscarinic Agonist
Side effects when used for glaucoma? (2) |
-Impaired night vision (pupillary constriction)
-Spasms of accommodation for distant vision |
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Contra-indications for Muscarinic Agonists (3)
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-Asthmatic patients
--bronchoconstriction -Coronary Insufficiency --Decreased contractility --Decreased excitability -Peptic Ulcer --Stimulates HCl secretion |
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Pilocarpine
-MOA? -Uses (1) |
-Naturally occurring Muscarinic Agonist
-Similar to synthetic agents with similar SEs and no receptor selectivity -Used for open angle glaucoma -FIRST CHOICE of cholinomemetics for this use |
