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32 Cards in this Set
- Front
- Back
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What do all of the direct acting muscarinic agonists have in their name? what are the 2 exceptions?
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cho
pilocarpine and cevimeline = exceptions |
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Name the direct acting muscarinic agonists?
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Acetylcholine
Methacholine Bethanechol Pilocarpine Carbachol Cevimeline Muscarine(not a drug) |
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What is the MOA for direct acting muscarinic agonists?
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bind to and anctivate muscarinic receptors
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Muscarinic agonists behave like the parasympathetic system or sympathetic?
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parasympathetic
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What is the effect of muscarinic agonists on HR?
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decrease
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Muscarinic agonists cause blood vessels to vaso_______, via _____.
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dilation via NO from M receptors on endothelial cells
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muscarinic agonists cause the ciliary muscle to______ and the iris sphincter to ______.
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contract--> near vision (PS reading a book)
contract--> miosis |
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to pee or not to pee when using muscarinic agonists?
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to pee (via M3 on detrusor)
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What would be the problem with using ACh as a drug?
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waay too non specific
rapidly hydrolyzed by AChE and pseudoAChE --> so the half life is very short - would get stim. of muscles and ganglia too |
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Bethanechol binds well to the ______ _________ and the GI tract. It does not bind well to the _______ or _______ _______.
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urinary bladder
heart or blood vessels |
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What is the benefit of bethanechol binding well to the bladder and GI tract and not the heart of blood vessels?
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good to eliminate cardiac side effects
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What are 2 theraputic uses for Bethanechol?
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post operative abdominal distension and urinary retention,
neurogenic atony of the urinary bladder |
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Would you use bethanechol to treat BPH?
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No because bethanechol is only used for NONobstructive urinary retention
BPH= obstructive due to pinching urethea from prostate |
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Name 3 theraputic uses for Pilocapine
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Miotic
Open angle glaucoma Closed angleglaucoma |
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What effects do muscarinic receptor activation have in the eye?
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contract ciliary m. (M)
contract iris sphincter (M3) |
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What is Sjogrens syndrome?
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autoimmune disease that causes destruction to moisture producing glands
(big complaint = dry mouth) |
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What drug is used to treat sjogrens syndrome?
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pilocarpine
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What drug is used to teat radiation induced dry mouth?
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pilocarpine
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What effect does muscarinic receptor activation have on glands? and do glands have M2 or M3 receptors?
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increase secretions via M3 receptors
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Why do you tx sjogrens syndrome and radiation of cancer in head and neck with pilocarpine?
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these(sjogrens & radiation of cancer) cause decreases salivary secretion and DRY MOUTH--> pilocarpine activates M receptors to help w/ salivation
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What is the newer drug that can also be used to tx sjogrens syndrome?
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Cevimeline
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Why is cevimeline better for the tx of sjogrens?
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works relatively selectively on salivary glands (good b/c you would get less side effects)
-also longer lasting effect |
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Carbachol is used to tx what disease of the eye that we keep ignoring?
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glaucoma
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Is muscarine a drug?
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NO
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Where can you find muscarine in the wild?
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mushrooms (inocybe and clitocybe)
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What are some of the symptoms you might see in a person who has mushroom poinsioning from Inocybe mushrooms?
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- side affects that mimic M agonists
- increase salivation - sweating - intestinal cramps/NVD |
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What is a potential adverse effect of muscarinic agonists having to do w/ the stomach?
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if patient has an ulcer these would aggrevate it by acting on the M receptors and secreting more gastric acid
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Adverse CV effects from muscarinic agonists?
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dilation via M3 receptors on endothelial cells ( NO)
bradycardia (M2--> slows heart) reflex tachycardia--> if blood pressure drops from dilating blood vessels heart will increase |
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What is the direct effect of muscarine on blood vessels and the heart?
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M3 on endothelial cells--> VD
m2 on heart --> decrease HR |
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Why would you get an increase in HR when taking a muscarinic agonist?
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M3 receptors on blood vessels will cause VD and a decrease in BP--> this could be sense by baroreceptors and be followed by an increase in HR that overrides the direct effect of drug on heart
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What are some adverse effects of muscarinic agonists on the lungs?
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difficulty breathing/asthma attack b/c M3 on bronchial smooth m. --> bronchoconstricion
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What is an adverse effect from muscarinic agonists on the eye?
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the iris sphincter will contract--> miosis & the ciliary m. will cause the lens to be round for near vision--> essentially stuck this way and can have spasm of accomodation (fixed for near vision)
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