Cholinomimetics Flashcards
What class is Bethanechol in?
Direct acting carbonic acid ester
Name the drugs that act through the mechanism of direct-acting muscarinic cholinomimetic
Bethanechol
Muscarine
Pilocarpine
Cevimeline
Which cholinomimetics are in the class od direct acting non-ester alkaloid?
Muscarine
Pilocarpine
Cevimeline
Nicotine
What is the mechanism of action for nicotine?
Direct-acting nicotinic cholinomimetic
Which cholinomimetic is used for post-operative and neurogenic ileum; urinary retention?
Bethanechol
Which cholinomimetic is used for Glaucoma?
Pilocarpine–ACh activates sphincter and ciliary muscles of eye
Which cholinomimetic is used to treat dry mouth, such as in Sjogren’s, or with post-radiation therapy?
Cevimeline
Which cholinomimetic is used for smoking cessation?
Nicotine
What are the side effects seen with all the cholinomimetics, besides nicotine? (Bethanechol, Muscarine, Pilocarpine, Cevimeline)
SLUDGE
Name the 2 indirect acting carbamate cholinomimetics…
Neostigmine
Physostigmine
What is the mechanism of action for neostigmine, an indirect acting carbamate?
AChE inhibitor (short acting)
What is the mechanism of action for physostigmine, an indirect acting carbamate?
AChE inhibitor (short acting)
Name the two indirect acting non-ester cholinomimetics…
Donepezil
Edrophonium
What class is Echothiphate, a cholinomimetic, in?
Indirect acting organophosphate
What is the mechanism of action for Donepezil and Edrophonium?
AChE inhibitors
What is the mechanism of action for Echothiphate?
AChE inhibitor (long acting)
Which cholinomimetic regenerates phosphorylated AChE and is a strong nucleophile?
Pralidoxime
Name the 2 very potent indirect acting organophosphate cholinomimetics…
Sarin
Parathion
What is the mechanism of action of Sarin and Parathion?
AChE inhibitors
Name the 7 AChE inhibitors…
Neostigmine Physostigmine Donepezil Edrophonium Echothiophate Sarin Parathion
AChE inhibitor used for post-operative and neurogenic ileum; urinary retention; myasthenia graves; reversal of neuromuscular blockage…
Neostigmine
What are the two AChE inhibitors used to treat Glaucoma by allowing ACh to activate papillary sphincter and ciliary muscles of the eye?
Physostigmine
Echothiophate
Cholinomimetic used to treat Alzheimer’s?
Donepezil
Cholinomimetic AChE inhibitor used to treat Myasthenia gravis?
Edrophonium
Cholinomimetic used for poisoning by nerve gas and insecticide?
Pralidoxime
Used as a volatile nerve gas?
Sarin
Used as an insecticide?
Parathion
What are the side effects of all the AChE inhibitors?
SLUDGE + general increase in cholinergic neurotransmission; paralysis
What two AChE inhibitors have death as one of their side effects?
Sarin
Parathion
What two AChE inhibitors have a short half life (lasting 0.5-2 hrs)
Neostigmine
Physostigmine
What AChE inhibitor has a VERY short half life (lasting 5-15 min)
Edrophonium
Which AChE inhibitor has a LONG half life (lasting > 100 hrs)?
Echothiophate
How is poisoning by sarin or parathion (AChE inhibitors) treated?
Treat with pralidoxime (regenerates phosphorylated AChE) and atropine
