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32 Cards in this Set

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