CHOLINERGIC DRUGS

PARASYMPATHOMIMETICS

Prepared by – Jadhav R. S.
 SYLLABU
S
⮚Pilocarpine
⮚Neostigmine*
⮚Physostigmine
*
⮚Pyridostigmine
⮚Pralidoxime
 QUESTION

1. Define Cholinergic drugs. Write the uses of

Pilocarpine and Physostigmine.

2. Define ‘Parasympathomimetics’. Give properties

and uses of Pilocarpine.

3. Define and classify cholinergic drugs. Write

the uses of Acetylcholine

 DEFINITION
⮚agents that
⮚ mimic the action of acetylcholine or
⮚produce the effect of parasympathetic
nerve stimulation

The agents that mimic the action of

acetylcholine or produce the effect of
parasympathetic nerve stimulation are
called as cholinergic agents or
parasympathomimetic
agents.
 CLASSIFICATION
1) DIRECT ACTING CHOLINERGIC
AGONISTS :
i) Esters of choline:
- Acetylcholine
ii) Alkaloids:
- Pilocarpine
2)INDIRECT ACTING CHOLINERGIC
AGONISTS
Cholinergic inhibitors or anti
cholinesterases:
 CLASSIFICATION
1. Choline esters:
Acetylcholine, Methacholine, Carbachol
2. Cholinomimetic alkaloids:
Muscarine, Pilocarpine, Arecholine
3. Cholinesterase inhibitors (Indirectly
acting)
A) Reversible Inhibitors-
Physostigmine, Neostigmine, Pyridostigmine
B) Irreversible Inhibitors-
Organophosphates (Parathion, Malathion),
 PILOCARPINE
Properties:
1. It is white crystalline powder.
2. It has odorless.
3. It is having faintly bitter taste.
4. It is very soluble in water.
5. It is hygroscopic.
6. It affected by light.
(3S,4R)-3-Ethyl-4-[(1-methyl-1H-imidazol-5-
yl)methyl]dihydrofuran-2(3H)-one
Storage:
It should be stored in well closed light resistant container
at a cool place away from direct sunlight.
 PILOCARPINE
USES:
1. It is used as cholinergic agonist.
2. It is used to treat
a) As miotic (counteract mydriasis)
b) To reduce intra ocular pressure in
glaucoma.
c) For diagnosis of tonic pupil.
d) For accommodation of near vision of eye.
e) To counteract anti cholinergic side effects(
dryness of mouth, constipation and
impaired vision).
 PILOCARPINE
Official preparation:
# Pilocarpine I.P, B.P, U.S.P
# Pilocarpine hydrochloride eye
drops I.P, B.P

Brand Names:
Opthocarpine, Pilocar
 NEOSTIGMINE

3-(dimethyl carbamoyloxy) N, N, N-
Trimethyl anilinium bromide
NEOSTIGMINE

N, N, N- Trimethyl
anilinium
bromide

Dimethyl carbamoyloxy
 NEOSTIGMINE
Properties:
1. It is white crystalline powder.
2. It has odorless.
3. It is having bitter taste.
4. It is very soluble in water.
5. It affected by light and oxygen.

Storage:
It should be stored in well closed air tight light resistant
containers at cool place away from direct sunlight.
USES: NEOSTIGMINE
1. It is used as indirect acting parasympathomimetic agent.
2. It reduces the heart rate and lowers the blood pressure by
peripheral vasodilatation.
3. It is used to promote expulsion of intestinal flatus before
retinopathy.
4. It is used in the treatment of
a) Myasthenia gravis
b) Paralytic ileus.
c) Post operative urinary retention

Official preparation:
# Neostigmine I.P, B.P, U.S.P
# Neostigmine Injection I.P, B.P,
# Neostigmine Tablet I.P, B.P,
Prostigmine
Brand Names:
 PHYSOSTIGMIN
E

1,2,3,3a,8,8a hexahydro-1, 3a, 8-trimethyl,

5-(methyl carbamoxyloxy) pyrrolo (2, 3,-
b)
PHYSOSTIGMIN
E
pyrrolo (2, 3,-b) indole

methyl

methyl carbamoxyl
 PHYSOSTIGMIN
Properties: E
1. It is colorless crystals.
2. It has odorless.
3. It is having bitter taste.
4. It is sparingly soluble in water.
5. It affected by air & light.

Storage:
It is stored in well closed air tight light resistant containers
at cool place away from direct sunlight.
USES:
PHYSOSTIGMIN
E
1. It is used as indirect acting parasympathomimetic
agent.
2. It is used as miotic
3. It is used in treatment of
a. glaucoma.
b. Anti cholinergic drug poisoning
c. Tricyclic anti depressant drug poisoning.
d. Reversal of post operative over sedation
e. Psychotropic and neurological disease.
Official preparation:
# Physostigmine I.P, B.P, U.S.P
# Physostigmine eye drops I.P, B.P
# Physostigmine injection I.P, B.P
Brand Names:
Eserine,
 PYRIDOSTIGMINE
Properties:
1. It is white crystalline powder.
2. It is having bitter taste.
3. It is having characteristic odor.
4. It is very soluble in water.
5. It is affected by light.

Storage:
It is stored in well closed air tight container at a cool lace
away from direct sunlight.
 PYRIDOSTIGMINE
Uses:
1. It is used as indirect acting
parasympathomimetic
agent.
2. It reduces the heart rate and lowers the
blood pressure by peripheral vasodilatation.
3. It is used to promote expulsion of
intestinal flatus before retinopathy.
Official preparation:
# Pyridostigmine I.P, B.P, U.S.P
# Pyridostigmine injection I.P, B.P
# Pyridostigmine tablet I.P, B.P
Brand Names:
 PRALIDOXIM
E
Properties:
1. It is white to pale yellow crystalline
powder.
2. It is having bitter taste.
3. It is odorless.
4. It is freely soluble in water.
5. It is affected by light.
Storage:
It is stored in well closed air tight container at a
cool lace away from direct sunlight.
 PRALIDOXIM
Uses: E
1. It is used by combination with atropine for
treatment of organophosphorus poisoning.
Official preparation:
# Pralidoxime I.P,
# Pralidoxime Injection

Brand Names:
Actifed, Decdan, Oflomac-DX, Zoxan-
D, Daksone, Zoxan-D, Pyricort,
Pyrimon, Dexasone.