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Cholinergic drugs
Parasympathomimetics
� They can produce some or all the effects that Ach can produce.
Classification
1) Directly acting (agonists at cholinergic receptors)
1. Choline esters: Ach, Methacholine, Carbachol, Bethanecol
2. Cholinomimetic alkaloids: Muscarine, Pilocarpine.
2) Indirectly acting (Anticholinesterases)
1. Reversible : Neostigmine, Physostigmine
2. Floxin Drops Irreversible: organic phosphate compounds
Acetylcholine (Ach)
A quaternary ammonium compound that cannot penetrate membranes.
Therapeutically of NO importance because it is NON Buy Floxin specific (M and N)
and its rapid inactivation by the cholinesterases.
The choline moiety contains quaternary ammonium group that gives Ach a
permanent positive charge (NOT absorbed orally).
Pharmacological actions of Acetylcholine
Muscarinic effects
I- Cardiovascular system:
- >P HR (negative chronotropy) <& \U cardiac output: Mimic the effect
of vagal stimulation. This is mediated by direct stimulation of cardiac
M2 receptors in the SA node and AV node. Otic Floxin This will lead to increase
K+ permeability and reduces cAMP Floxin Otic levels.
- Vasodilatation Production of nitric oxide (endothelium-derived relaxing
factor) from arginine -> stimulate guanylate cyclase -> 1^cGMP ->
�]/Ca 2 *-> Vascular smooth muscle relaxation hyperpolarization.
- Atropine blocks these muscarinic receptors and prevents
acetylcholine from producing vasodilation
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