Cholinergic Drugs I Flashcards
choline acetyl transferase
catalyzes formation of Ach from acetyl-CoA and choline
acetylcholinesterase
major means of inactivation of Ach by degrading it into choline and acetyil-CoA; choline is transported back into axon terminal
muscarinic receptors
postganglionic parasympathetic neurons innervating heart, smooth muscle, and exocrine glands; also postganglionic sympathetic neurons innervating sweat glands
sympathetic activation of sweat glands (muscarinic)
increased secretion
parasympathetic activation of heart (muscarinic)
slow heart rate (bradycardia); reduced rate of spontaneous depolarization of SA node and increased refractory period of AV node
parasympathetic activation of blood vessels (muscarinic)
vasodilator; results from production of NO at muscarinic receptors of vascular endothelial cells
parasympathetic activation of GI tract (muscarinic)
increase tone and motility, secretory activity; relaxation of sphincters
parasympathetic activation of bladder (muscarinic)
contraction of detrusor and relaxation of sphincter
parasympathetic activation of eye (muscarinic receptor)
pupillary contraction and ciliary contraction for near vision
parasympathetic activation of bronchi (muscarinic receptor)
constriction
parasympathetic activation of exocrine glands (muscarinic receptor)
secretion of tears, saliva, mucus, stomach acid, digestive enzymes
choline esters
direct-acting muscarinic cholinergic agonists; Ach with chemical groups attached to protect from AchE
examples of choline esters
bethanechol, methacholine, carbachol
bethanechol uses
relief of postoperative GI distension, constipation, and urinary retention
topical carbachol use
wide-angle glaucoma and cataract surgery
cholinomimetic muscarinic alkaloids
direct-acting agonists; not same structure as acetylcholine
cholinomimetic muscarinic alkaloid examples
muscarine, pilocarpine, and cevimeline
cevimeline
used for Sjogren Syndrome
Sjogren Syndrome
immune systems attacks healthy cell in salivary glands and eyes causing decrease in tearing and saliva
topical pilocarpine
cataract surgery
cholinesterase inhibitors
indirect-acting agonists
cholinesterase inhibitors can be _
reversible (overcome with more AchE) or irreversible (dangerous, can not be overcome unless new enzyme made)
reversible cholinesterase inhibitors
physostigmine, neostigmine, edrophonium, pyridostigmine, donepezil, and carbamate insecticides
irreversible cholinesterase inhibitors
isoflurophate (DFP), organophosphate insecticides (parathion, diazinon, and malathion), and nerve gases (sarin, tabun, soman, novichok)
Alzheimer’s disease treatment
galantamine, donepezil, and rivastigmine
Myasthenia gravis treatment
pyridostigmine
reverse effects of neuromuscular blockers with _
neostigmine
atropinic poisonings treatment
physostigmine
signs of toxicity from organophosphorus compounds
wheezing (bronchoconstriction), sweating, miosis (pupil contraction), cramps, and bradycardia
treatment for organophosphorus toxicity
termination of exposure, artificial respiration, IV atropine (repeated every 5-10 minutes until sign of relief), and IV 2-PAM (slowly for reactivation of enzyme)