cholinergic agonist (direct-acting cholinomimetic) Flashcards
bethanechol moa
selective muscarinic agonist (M1, M2, M3) in peripheral tissues
bethanechol clinical app
postoperative ileus, neurogenic ileus, urinary retention
bethanechol admin
oral, im
bethanechol duration of action
~30 min
bethanechol PK
poor lipid solubility & does NOT enter CNS
bethanechol toxicity/interactions
parasympathetic effects
bronchospasm in asthma
pilocarpine moa
partial muscarinic agonist (M1, M2, M#) in peripheral tissues
pilocarpine clinical app
glaucoma
sjogren’s (inc salivation)
pilocarpine admin
oral lozenge
topical (eyedrops)
pilocarpine duration of action
0.5-2h
pilocarpine PK
good lipid solubility
pilocarpine toxicity/interactions
parasymp effects
bronchospasm in asthma
vasoconstriction (ganglionic effect)
ACh moa
nicotinic
muscarinic agonist
receptor: nicotinic & muscarinic
L: muscle cell membrane
Ach clinical app
during eye surgery - contraction of the sphincter muscles of the iris –> miosis
contraction of the ciliary muscle –> accommodation spasm
ACh admin
topical (opthalmic/intraocular)
ACh duration of action
~20 min, up to 6h
ACh PK
rapidly hydrolyzed by cholineresterase
ACh toxicity/interactions
bradycardia, flushing, hypotension
diaphoresis
cloudy vision, corneal decompensation, corneal edema
dyspnea
Muscarine moa
binds to postganglionic cholinergic neurons in the ANS
does not cross BBB (Not in CNS)
Muscarine admin
oral (consumption of mushroom)
Muscarine duration of action
2-6 hours
Muscarine toxicity/interactions
SLUDGE/DUMBBELLS
Nicotine moa
selective nicotinic agonist
activates autonomic postganglionic neurons
skeletal muscle endplate (PNS + CNS)
Nicotine clinical app
smoking cessation
insecticides
Nicotine admin
oral (gum)
transdermal
inhalation
Nicotine duration of action
1-6 hours
Nicotine PK
high lipid solubility
Nicotine toxicity/interactions
Acute: increase GI activity, hypertension
OD: seizures, paralysis, coma, death
Long term: GI & CV risk factors
Chantix moa
partial agonist at one specific nicotinic receptor
Chantix clinical app
smoking cessation
Chantix admin
oral
Chantix duration of action
12-24 h
Chantix toxicity/interactions
hypertension
sweating
GI activity
Chantix PK
high lipid solubility
Succinylcholine moa
selective for neuromuscular end plate
Succinylcholine clinical app
muscle relaxation (clinically mimics effects of cholinergic antagonist; paralysis)
Succinylcholine admin
IV
Succinylcholine duration of action
5-10 min
Succinylcholine PK
highly polar
Succinylcholine toxicity/interactions
prolonged action in people w abnormal levels of butyrylcholinesterase