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Glossary of Cholingergics, Anticholingergics and Ganglionic Drugs

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What receptors are at the end organs?
Muscarinic ... so no stimulation there by nicotine
What are muscarinic receptor subtypes?
M1, M2, M3
M1 receptor expressed where?
CNS, secretory glands in GI
for example: pirenzepine
M2 expression
myocardium i.e. AF-DX 116
M3 expression
everywhere else i.e. tiotropium
cholinergic agonists?
bethanecol, muscarine, pilocarpine, methacholine etc
Bethanecol does what?
Chol. agonist... trt urinary retention, abd. distension, gastric atony
Muscarine?
from Amanita muscarina mushrooms
Pilocarpine?
natural cholinergic agonist... topical miotic, glaucoma to decrease pressure
ACh action on arterioles?
acts on M3 receptors on vessels, to increase Calcium, activating NO, generating cGMP causing muscle relaxation and reduction in peripheral resistance.
Mushroom poisoning: inocybe species
high concentration, fast onset (salivation, lacrimation, headache, nausea, hypotension, shock)... trt with atropine
Mushroom poisoning: Amanita muscaria
low conc., fast onset... sx inocybe plus CNS ataxia , mania, hallucinations etc
Mushroom poisoning: Amanita phalloides
slow onset.. liver and renal damage, grave prognosis... only supportive trt
Some Anti-cholinergics Teritary amines
ipratropium, tiotropium (asthma propylaxis), Tiotropium is M1, M3 selective*** , glycopyrrolate (pre-anesthetic)
Some signs of atropine toxicity
Hot (no sweating), dry, red (peripheral vasodilation), blind (can't focus due to cycloplegia), Mad (stimulations)

trt with: AChE-I (increase local ACh)
Pirenzepine
M1 selective antagonist, used in peptic ulcer pts

pire= burning???
Scopolamine
sedation drug and antimotion drug
Nicotine actions?
In ganglia, both SNS and PANS activated... at high doses may close a blockade there.

Sensory stim: respir stim., nausea, vomiting, ADH secretion, depression of knee jerk.

Nm receptors on muscle < little activity
What's the oxidation product of nicotine
cotinine, negligible activity
therapies for nicotine dependance
nicotine replacement therapy by patches//// buproprion, an antidepressant that increases dopamine./// varenicline: nicotine receptor partial agonist at alpha 4 beta 2 form.
non-depolarizing ganglionic blockers
hexamethonium, trimethaphan: competitive blockade of nicotinic receptors at ganglion.

Mecamylamine: enters CNS and blocks central nicotine action. ...

No longer used clinically
problems with non-depolarizing ganglionic blockers
orthostatic hypotension, tachycardia, urinary hesitancy, constipation, cycloplegia, impotence!!!

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