Drugs Flashcards
Methacholine
muscarinic agonist
beta methyl group slows hydrolysis
beta methyl group-selective for muscarinic
alpha methyl group-selective for nicotinic
tx: paraxysmal atrial tachycardia
dx: agent for asthma
Carbachol
direct agonist
carbamate makes it less of a substrate for AChE
competitive inhibitor of AChE
Uses:dx of asthma, miosis, topically for glaucoma, urinary retention, postsurgical optical hypertension
Bethanechol
muscarinic agonist
increased stability to hydrolysis
uses: alzeheimer’s disease, tx postoperative postpartum urinary retention
Pilocarpine
direct muscarinic agonist
treat glaucoma
natural alkoid
Muscarine
natural alkoid
Arecoline
natural alkoid
Verinicline
partial agonist at nicotine receptors
Carbamic acid esters of penols
fit active site of AChE
AChE becomes carbomoylated rather than acetylated
inhibit slow K3
hydrolysis requires minutes instead of msec
Physostigmine
tertiary amine-penetrate CNS
competitive inhibitor of AChE
induce miosis in open-angle glaucoma
Neostigmine
quaternary ammonium-no CNS activity
activity not a function of pH
uses: postoperative paralytic ileus and myasthenia gravis, reversal of neuromuscular blockade
Pyridostigmine
No CNS activity
longer duration of action when compared to neostigmine, thus better for myasthenia gravis
Edrophonium
quaternary ammonium-no CNS activity
competitive inhibitor of AChE
does not carbamylate the enzyme
reverse nondepolarizing blockers
Tacrine
tx alzheimer’s disease
CNS cholinesterase inhibitor
nonselective for AChE or butyrylcholinesterase
Donepezil
tx of alzheimer’s disease
greater affinity for AChE in the brain than periphery
Rivastigme
Centrally selective
pseudo-irreversible AChEI (slow dissociation of the carbamylated enzyme)
