Cholinergic agonists and antagonists Flashcards
choline esters
Direct-acting cholinergic agonists
- acetylcholine
- methacholine
- carbachol
- bethanechol
cholinomimetic alkaloids
Direct-acting cholinergic agonists
- muscarine
- pilocarpine
- nicotine
- lobeline
clinical uses of direct acting cholinergic agonists
Diseases of eye: glaucoma, accommodative esotropia
GI/GU disorders: postoperative ileus, congenital megacolon, urinary retention, esophageal reflux, xerostomia, Sjogren syndrome
acetylcholine indication
Intraocular use during surgery, causes miosis
bethanechol indications
Selective mAChR, primarily affects urinary and GI tracts
Used to treat urinary retention and heartburn
AE: UTIs if sphincter fails to relax
carbachol indications
Treatment for glaucoma, used to produce miosis during surgery or opthalmic exam
cevimeline indication
Treatment for xerostomia in Sjogren syndrome
methacholine
Selective and potent mAChR agonist for treatment of bronchiole airway hyperreactivity
pilocarpine
Pure mAChR agonist, treatment for xerostomia in Sjogren syndrome, miosis during opthalmic procedures, and glaucoma
varenicline
Partial nAChR agonist, high affinity and selectivity for a4b2 nAChRs (Nn)
Used for smoking cessation
AE: suicidal ideation
direct-acting muscarinic cholinergic agonist contraindications
Asthma, hyperthyroidism, coronary insufficiency, acid peptic disease
AChE inhibitor toxicity
SLUDGE, NMJ effects (muscle fasciculations followed by paralysis)
Treatment: atropine (muscarinic antagonist), pralidoxime (cholinesterase regernerator)
antimuscarinic for motion sickness
Scopolamine
antimuscarinics for respiratory disorders
Ipratropium
Tiotropium
antimuscarinics for GI disorders
Atropine
Dicycloamine
Glycopyrrolate
Hyoscyamine