1) Cholinomimetics Flashcards
What is the class for Bethanechol (Urecholine)
Direct acting carbamic acid ester
What is the mechanism for Bethanechol (Urecholine)
Direct-acting muscarinic cholinomimetic
What are the therapeutics for Bethanechol (Urecholine)
Post-operative and neurogenic ileus; urinary retention (bowel and bladder smooth muscle ACh-innervated)
What are the important side effects for Bethanechol (Urecholine)
SLUDGE
What is the class for Muscarine
Direct acting non-ester alkaloid
What is the mechanism for Muscarine
Direct-acting muscarinic cholinomimetic
What are the important side effects for Muscarine
SLUDGE
What is the class for Pilocarpine (Salagen)
Direct acting non-ester alkaloid
What is the mechanism for Pilocarpine (Salagen)
Direct-acting muscarinic cholinomimetic
What are the therapeutics for Pilocarpine (Salagen)
Glaucoma (ACh activates sphincter and ciliary muscles of eye)
What are the important side effects for Pilocarpine (Salagen)
SLUDGE
What is the class for Cevimeline (Evoxac)
Direct acting non-ester alkaloid
What is the mechanism for Cevimeline (Evoxac)
Direct-acting muscarinic cholinomimetic
What are the therapeutics for Cevimeline (Evoxac)
Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation)
What are the important side effects for Cevimeline (Evoxac)
SLUDGE
What is the class for Nicotine (NRT)
Direct acting non-ester alkaloid
What is the mechanism for Nicotine (NRT)
Direct-acting nicotinic cholinomimetic
What are the therapeutics for Nicotine (NRT)
Smoking cessation (reduces cravings)
What is the class for Neostigmine (Prostigmin)
Indirect acting carbamate
What is the mechanism for Neostigmine (Prostigmin)
AChE inhibitor (short acting)
What are the therapeutics for Neostigmine (Prostigmin)
Post-operative and neurogenic ileus; urinary retention; myasthenia gravis; reversal of neuromuscular blockade
What are the important side effects for Neostigmine (Prostigmin)
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What are the miscellaneous for Neostigmine (Prostigmin)
Lasts 0.5-2 hours
What is the class for Physostigmine (Eserine)
Indirect acting carbamate
What is the mechanism for Physostigmine (Eserine)
AChE inhibitor (short acting)
What are the therapeutics for Physostigmine (Eserine)
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
What are the important side effects for Physostigmine (Eserine)
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What are the miscellaneous for Physostigmine (Eserine)
Lasts 0.5-2 hours
What is the class for Donepezil (Aricept)
Indirect acting non-ester
What is the mechanism for Donepezil (Aricept)
AChE inhibitor
What are the therapeutics for Donepezil (Aricept)
Alzheimer’s (amplifies endogenous ACh in brain)
What are the important side effects for Donepezil (Aricept)
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What is the class for Edrophonium (Enlon)
Indirect acting non-ester
What is the mechanism for Edrophonium (Enlon)
AChE inhibitor (v. short acting)
What are the therapeutics for Edrophonium (Enlon)
Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus
What are the important side effects for Edrophonium (Enlon)
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What are the miscellaneous for Edrophonium (Enlon)
Lasts 5-15 minutes
What is the class for Echothiophate (Phospholine)
Indirect acting organophosphate
What is the mechanism for Echothiophate (Phospholine)
AChE inhibitor (long acting)
What are the therapeutics for Echothiophate (Phospholine)
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
What are the important side effects for Echothiophate (Phospholine)
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What are the miscellaneous for Echothiophate (Phospholine)
Lasts >100 hours
What is the class for Pralidoxime (Protopam)
Strong nucleophile
What is the mechanism for Pralidoxime (Protopam)
Regenerates phosphorylated AChE
What are the therapeutics for Pralidoxime (Protopam)
Poisoning by nerve gas, insecticide
What is the class for Sarin
Very potent indirect acting organophosphate
What is the mechanism for Sarin
AChE inhibitor
What are the therapeutics for Sarin
Volatile nerve gas
What are the important side effects for Sarin
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What are the other side effects for Sarin
Death
What are the miscellaneous for Sarin
Treat with pralidoxime and atropine before aging