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Pharm Autonomic NS

Cholinergic Agonists

cholinergic agonists also known as parasympathomimetics or muscarinic agonists; promote or mimic the action of acetylcholine
3 categories in this class: 1. muscarinic agonists 2. cholinesterase inhibitors 3. ganglionic stimulants
MUSCARINIC AGONISTS: 1. acetylcholine[Miochol] 2. carbachol[Isopto Carbachol] 3. pilocarpine[Isopto Carpine] 4. bethanechol[Urecholine] 5. methacholine[Provocholine]
muscarinic receptors[acetylcholine] are located in: eye, heart, blood vessels, lung, GI tract, urinary bladder, sweat glands
MAs are used clinically to tx glaucoma and to improve GI and urinary bladder tone
ACh is destroyed rapidly by cholinesterase and Miochol has too short of a half-life so its use is restricted to pupil constriction for procedures
methacholine is only used for dx of bronchiol airway hyper-reactivity by specialists
carbachol and pilocarpine are used to tx glaucoma pilocarpine comes in an oral form that can also be used to tx xerostomia by increasing salivary gland secretion
bethanechol[Urecholine] increases the tone of the detrusor urinae muscle and produces contraction strong enough to initiate micturition and empty the bladder
bethanechol also stimulates gastric motility
bethanechol is not destroyed by cholinesterase as quickly as acetycholine so its effects are more prolonged
bethanechol is contraindicated in: PUD[can cause excessive secretion of gastric acid that could lead to perforation], intestinal obstruction[d/t increased peristalsis], urinary obstruction or weak bladder wall[d/t increase urinary tract pressure]
also contraindicated in: bronchospastic disease[stimulation of muscarinic receptors in lungs resulting in bronchoconstriction] preexisting hypotension, bradycardia, CVD hyperthyroidism
other adverse rxns increased tearing, miosis of pupils, facial flushing
Muscarinic poisoning can occur from overdosage and also from certain poisonous mushrooms. Sx are abdominal cramps, salivation, flushing, n/v. Antidote: Atropine subq
drug interactions include nicotine which could create a critical fall in BP
drugs that have antimuscarinic activity and decrease the effects of muscarinic agonists are: H1 blockers, pheonothiazines, quinidine, procainamide
clinical indications: neurogenic atony of the bladder with retention
Created by: heatherbrown2020