CHOLINOMIMETIC (CHOLINERGIC) DRUGS

DIRECT-ACTING INDIRECT ACTING

MUSCARINIC NICOTINIC ORGANOPHOSPHATE

CHOLINE ESTER
Ex. Carbachol
• Ligand gated ion channel.
• Binds two ACh molecules elicits a
ALKALOID
Ex. Atropine
• binds to M1, M3, and M5 receptors
→ activates the inositol
• Related in structure and sequence to
trisphosphatem (IP3), diacylglycerol
(DAG) cascade→ DAG open smooth
muscle calcium channels→IP3
releases calcium from endoplasmic
and sarcoplasmic reticulum→increase
cellular cGMP
concentration,→increases potassium
flux across cardiac cell membranes
and decreases it in ganglion and
smooth muscle cells→attenuate the
activation of adenylyl cyclase and
modulate the increase in cAMP levels
induced by hormones such as
catecholamines→reduce the
physiologic response of the organ to
stimulatory hormones.
Ex. Nicotine
conformational change → allows the
entry of sodium ions →
depolarization of the effector cell →
mediate fast excitatory synaptic
transmission.
receptors of GABA, glycine, 5HT3,
glutamate.
S
Ex. Echothiophate
• IRREVERSIBLE ANTICHOLINESTERASE
• covalently binds via its phosphate group to
the serine-OH group at the active site of
acetylcholinesterase→ enzyme is
permanently inactivated.
• Inhibits acetylcholinesterase for a longer
duration
CARBAMATES
Ex. Neostigmine
• MEDIUM DURATION ANTICHOLINESTERASE
• Increase the concentration of endogenous
acetylcholine at cholinoreceptors by inhibiting
acetylcholinesterase.
• Undergoes two-step hydrolysis that allow
covalent bond formation→ reversible
carbamylation of acetylcholinesterase →
accumulation of acetylcholine.
• 30 mins-6 hrs
•
EDROPHONIUM
Ex. Tensilon

• SHORT ACTING ANTICHOLINESTERASE

• Bind reversibly to the anionic active site of
AChE→ ionic bond formed→preventing
hydrolysis of ACh
• 10 to 20 minutes

SUBMITTED BY: AGGABAO. IVY

D.