7. Cholinomimetics Flashcards
Direct acting
Choline esters
Alkaloids
SYNTHETIC COMPOUNDS (Muscarinic)
SYNTHETIC COMPOUNDS (Nicotinic)
INDIRECT ACTING
Cholinesterase inhibitors
Alcohols
Carbamates
Organophosphates
Choline esters
acetylcholine (ACh)
Methacholine
Carbachol
Bethanechol
Alkaloids
Muscarine
Pilocarpine
Nicotine
Arecoline
SYNTHETIC COMPOUNDS (Muscarinic)
Cevimeline
SYNTHETIC COMPOUNDS (Nicotinic)
Varenicline
Suxamethonium / Succinylcholine
Alcohols
Reversible, competitive
Edrophonium
Donepezil
Galantamine
Tacrine
Carbamates
Non-competitive
Physostigmine Rivastigmine Neostigmine Pyridostigmine Ambenonium Demecarium
Organophosphates
Echothiophate
War gases (nerve agents)
Insecticides
acetylcholine (ACh)
N / M receptor
Miosis
rapidly inactivated
Methacholine
M receptor Challenge test (asthma)
Carbachol
N / M receptor
Ophthalmology
resistance to hydrolysis
high potency -> rarely used
Bethanechol
M receptor
bladder atony / mega colon
resistance to hydrolysis
Muscarine
Quaternary amine
Pilocarpine
M receptor
Sjogren’s / glaucoma
Tertiary amine
stable to hydrolysis
Nicotine
N receptor
tertiary amine
smoking cessation / poison
Cevimeline
M receptor
Sjogren’s
Varenicline
N (Neuronal) receptor
smoking cessation
May cause depression
Suxamethonium / Succinylcholine
NM
depolarizing muscle relaxant
Quaternary amine
Edrophonium
quaternary
Short duration
diagnosis of MG (tensilon test)
(excess drug -> Cholinergic crisis)
Donepezil
Lipid soluble
Alzheimer’s disease
long acting (58-90 hr)
Galantamine
Lipid soluble
Alzheimer’s disease
DOA 5-7 hr
Physostigmine
Tertiary
DOA 0.5-2 hr
Bladder atony / antidote against anticholinergic
convulsions
Rivastigmine
Lipid soluble
DOA 9 hr
Alzheimer’s disease or dementia
Neostigmine
Quaternary
Bladder + GI stimulator / MG
DOA 0.5-2 hr
Pyridostigmine
Quaternary
Chronic treatment of MG
DOA 3-6 hr
Echothiophate
Glaucoma
Pralidoxime
used against organophospate
nucleophile agent
splits P-O bond before aging
Types of Cholinomimetics
Direct & indirect acting
War gases
Tabun
Soman
Insecticides
Parathion
Malathion