cholinergics Flashcards
direct agonists
act on nicotonic/muscarinic receptors
ACh
nicotinic
muscarinic
rapidly hydrolyzed
use: miosis induction
Methacholine
muscarinic
slowly hydrolyzed
use: inhalation test for bronchial hyperactivity
Bethanechol
muscarinic
hydrolysis resistant
use: urinary retention
SE: palpitations
Carbachol
nicotinic
muscarinic
hydrolysis resistant
use: topical opthalmic surgery, glaucoma
pilocarpine
muscarinic
hydrolysis resistant
use:
dry mouth
glaucoma
SE: palpitations
vecimeline
muscarinic
hydrolysis resistant
use:
dry mouth
Sjogren’s syndrome
nicotine
nicotinic
low dose: stimulate
high dose: inhibit
SE: increase HR, BP, GI tone, tremors, seizures
toxic!
AChE inhibitors
form irreveresible bond w/Ser
use: myasthenia gravis glaucoma Alzheimer's reverse NMJ blockers antimuscarinic drug toxicity
SE:
DUMBBELLS
NMJ blockade (paralysis)
alcohols: edrophonium
short-acting AChE inhibitor
competitive inhibitor (reversible)
use: Dx myasthenia gravis
doesn’t cross BBB
carbamates
intermediate-acting AChE inhibitor
slowly reversible
donepezil
carbamate
use: Alzheimer’s
SE: GI problems
rivastigmine
carbamate
use: Alzheimer’s
SE: GI problems
galantamine
carbamate
use: Alzheimer’s
SE: GI problems
neostigmine
carbamate
use: reverse NM block in surgery
pyridostigmine
carbamate
use: myasthenia gravis
ambenonium
carbamate
use: myasthenia gravis
guanidine
carbamate
use: Lambert-Eaton syndrome
organophosphates
long-acting AChE inhibitor
irreversible
aging: lose alkyl group
antidote: 2PAM before aging
echothiophate
organophosphate
use: glaucoma
malathion
organophosphate
soman
organophosphate
nerve gas
sarin
organophosphate
nerve gas
dizinon
organophosphate
insectiside
pralidoxime (2PAM)
organophosphate antidote
give before aging occurs
atropine
organophosphate antidote
muscarinic antagonist
blocks muscarinic effects of ACh
given to troops prophylactically
muscarinic antagonist
DUMBBELLS
use: preanesthetic - dry secretions asthma/COPD - bronchodilate motion sickness GI hypermotility antipsychotic SE
risk:
glaucoma - can’t see
prostatic hypertrophy - can’t pee
memory problems
scopolamine
muscarinic antagonist
use:
motion sickness
pre-op sedation
SE:
drowsiness
amnesia
psychosis
ipratropium
muscarinic antagonist
poor CNS penetration
use:
COPD
asthma
