SUBMITTED BY: AGGABAO, IVY D.
MED-2
ASSIGNMENT #2
ANTICHOLINERGIC DRUGS
ANTIMUSCARINIC
M1-SELECTIVE
Ex. Pirenzepine
MOA: Binds to the M1 muscarinic
acetylcholine receptor→ inhibition
of adenylate cyclase→ breakdown
of phosphoinositides→ modulation
of potassium channels through the
action of G proteins→ reduce
gastric acid secretion.
NON-SELECTIVE
Ex. Atropine
MOA: Acts centrally and peripherally to
bind competitively to muscarinic
receptors→ prevents actions such as
the release of inositol trisphosphate
(IP3) and the inhibition of adenylyl
cyclase caused by muscarinic agonists→
prevent acetylcholine from
binding→reduce activity of the GI tract.
tract.
9/17/20
CHOLINORECEPTOR BLOCKERS AND
CHOLINESTERASE REGENERATORS
CHOLINESTERASE REGENERATORS
ANTINICOTINIC OXIMES
Ex. Pralidoxime
GANGLION BLOCKERS
MOA: Reactivates the enzyme
Ex. Mecamylamine cholinesterase by cleaving the
phosphate-ester bond formed between
the organophosphate and
MOA: competitively block nicotinic
acetylcholinesterase→relieve skeletal
cholinoreceptors on postganglionic
muscle end plate block.
neurons in both sympathetic and
parasympathetic ganglia in the
autonomic nervous system.
NEUROMUSCULAR
BLOCKERS
DEPOLARIZING NON-DEPOLARIZING
Ex. Succinylcholine Ex. Rocuronium
MOA: MOA:
Phase 1 (depolarizing) Act predominantly at the nicotinic
React w/ nicotinic receptor to receptor site by competing with
open channel→ depolarization of acetylcholine→enter pore of ion
motor end plate→ spread to adjacent channel →produce more intense
membrane→ contractions of muscle motor blockade →weaken
neuromuscular transmission
motor unit.
→diminish ability of
Phase 2 (desensitizing)
acetylcholinesterase inhibitors to
Prolonged exposure→ initial end
antagonize the effect of
plate depolarization decreases → nondepolarizing muscle relaxants.
membrane becomes repolarized.