Pharmacology of CHOLINERGIC SYSTEM

Dr.U.P.Rathnakar
MD.DIH.PGDHM

www.scribd.com/Urval R

Cholinergic Drugs
[Cholinomimitics]

[Cholinergic Agonists]

[Anticholinesterases]

Cholinergic Agonists [Agonists]

Choline esters Acetylcholine Methacholine Carbachol Bethanechol
Alkaloids Pilocarpine Muscarine Arecoline

Properties of Choline Esters

Uses

1. Ach-too short acting & non selective

2. Methacholine-PSVT-Obsolete

Bethanochol
Therapeutic Uses:
To reverse Non obstructive urinary retention as in

post-operative atony of bladder and neurogenic bladder. To treat GIT atony without obstruction as in paralytic ileus.
Cevimeline-(EVOXAC) is a newer muscarinic agonist

available orally for use in treatment of xerostomia

Pilocarpine:
[Pilocarpine is too toxic for systemic use]

Actions: [Initial]---[Persistent]---

Mainly muscarinic Fall of BP [Peripheral] Rise in BP[Ganglionic]

This action exception to pilocarpine

Therapeutic uses:
Opthalmic use:

( Eye drops) Open angle glaucoma. To counteract mydriasis. In iridocyclitis to break adhesions between iris and lens.

Muscarine:
Muscarine occurs in poisonous mushrooms:

Early mushroom poisoning

Inocybe

Symptoms of muscarine actions Reversed by Atropine

Late mushroom poisoning

Amanita phalloides Majority of fatal mushroom poisonings worldwide

Symptoms of mucosal damage[GIT, Liver,

Kidney-inhibition of RNA synthesis] Supportive tt[No sp tt]

Hallucinogenic type

Pilocybe Mexicana

Block muscarinic receptors in brain-

Hallucination Atropine is contra indicated!

Anticholinesterases [Indirectly acting cholinergics]

Reversible anticholinesterases Carbamates Acridine Tacrine. Physostigmine Neostigmine Pyridostigmine Edrophonium Ambenonium Demecarium Rivastigmine, Donepezil, Galantamine. Irreversible anticholinesterases

Irreversible anticholinesterases
Organophosphates: Carbamates: Carbaryl* Propoxur*
Echothiophate

Parathion*
Malathion* Diazinon* Tabun# Sarin# Soman#
a

*Insecticides # Nerve gaseschemical warfare