A parasympathomimetic drug, sometimes called a cholinomimetic drug, is a substance that stimulates the parasympathetic nervous system (PSNS). These chemicals are also called cholinergic drugs because acetylcholine (ACh) is the neurotransmitter used by the PSNS. Chemicals in this family can act either directly by stimulating the nicotinic or muscarinic receptors (thus mimicking acetylcholine), or indirectly by inhibiting cholinesterase, promoting acetylcholine release, or other mechanisms.
Contents
- Structure activity relationships for parasympathomimetic drugs
- Direct acting
- Indirect acting
- References
Some chemical weapons such as sarin or VX, non-lethal riot control agents such as tear gas, and insecticides such as diazinon fall into this category.
Structure activity relationships for parasympathomimetic drugs
For a cholinergic agent, the following criteria describe the structure activity relationship:
- Ing's Rule of 5: there should be no more than five atoms between the nitrogen and the terminal hydrogen for muscarinic (or cholinergic) activity;
- the molecule must possess a nitrogen atom capable of bearing a positive charge, preferably a quaternary ammonium salt;
- for maximum potency, the size of the alkyl groups substituted on the nitrogen should not exceed the size of a methyl group;
- the molecule should have an oxygen atom, preferably an ester-like oxygen capable of participating in a hydrogen bond;
- there should be a two-carbon unit between the oxygen atom and the nitrogen atom.
Direct-acting
These act by stimulating the nicotinic or muscarinic receptors.
Indirect-acting
Indirect acting parasympathomimetic drugs may be either reversible cholinesterase inhibitors, irreversible cholinesterase inhibitors or drugs that promote ACh release or anti-adrenergics. The latter inhibits the antagonistic system, the sympathetic nervous system.
See also: alpha blocker and beta blocker