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95
Drugs Acting on Autonomic Nervous System (ANS)
Chemical name: (RS)-N-{3-Acetyl-4-[2-hydroxy-3-(propan-2-ylamino)-propoxy]-phenyl}-
butanamide.
Uses: It is used to treat angina (chest pain), and hypertension.
Formulation: Injectable.
Brand names: Sectral and Prent.
Esmolol
Structure:
O
O O
OH
NH
Chemical name: Methyl (RS)-3-{4-[2-Hydroxy-3-(propan-2-ylamino)-propoxy]-phenyl}-
propanoate.
Uses: It is used to control heart rate and hypertension.
Formulations: Infusion and Injectable.
Brand names: Miniblok and Brevibloc.
Labetolol
Structure:
O
NH
2
H
N
OH
OH
Chemical name: (RS)-2-Hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)-amino]-ethyl}-
benzamide.
Uses: It is effective in the management of hypertensive emergencies. In postoperative
hypertension and pheochromocytoma associated hypertension.
Formulations: Tablet and Injectable.
Brand names: Labesol and Labeta.
96
A Textbook of Pharmaceutical
Chemistry
Carvedilol
Structure:
HN
O
O
HO O
NH
Chemical name: (±)-[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl][2-methoxyphenoxy)-
ethyl]-amine.
Uses: In the treatment of hypertension (high blood pressure) and heart failure after the attack.
Formulations: Tablet and Injectable.
Brand names: Carvil, Carloc, and Coreg.
8.3 PARASYMPATHOMIMETICS
Parasympathomimetic agents are also called cholinomimetic or cholinergic drugs that
stimulate the parasympathetic nervous system. These chemicals are called cholinomimetic drugs
because they mimic the actions of acetylcholine.
These drugs act either directly by stimulating the nicotinic or muscarinic receptors (thus
mimicking acetylcholine) or indirectly by inhibiting the cholinesterase enzyme.
Acetylcholine is the neurotransmitter used by the parasympathetic system. The primary
transmitter of nerve impulses within the parasympathetic nervous system that contracts smooth
muscles dilates blood vessels, increases body secretions, and slows down the heart rate.
Acetylcholine itself produces extremely short-lived effects because it is destroyed rapidly in the
blood by an enzyme called cholinesterase.
Muscarinic Receptors
Muscarine is a naturally occurring plant alkaloid, obtained from the poisonous mushroom,
Amanita muscaria. Its actions on the smooth muscle, cardiac muscles, exocrine gland are very
much alike that exhibited by acetylcholine. Hence, it was proposed that acetylcholine exhibits
some of its action via muscarinic receptors while remaining actions are propagated through the
nicotinic receptors.
97
Drugs Acting on Autonomic Nervous System (ANS)
Nicotinic Receptors
Nicotine, the principal addictive ingredient in the tobacco used in cigarettes and cigars,
exerts its actions at a subset of cholinergic receptors known as nicotinic receptors. They are
divided into those that act mainly on skeletal muscle and those that act on ganglia cells.
Parasympathomimetic agents are classified as follows.
(a) Cholinergic Agonists
(i) Choline esters
Acetylcholine
Methacholine
Carbachol
Bethanechol
(ii) Alkaloids
Muscarine
Pilocarpine
Arecoline
(b) Anticholinesterases (Choline Esterase Inhibitors)
(i) Reversible
Physostigmine
Neostigmine
Pyridostigmine
Rivastigmine
Donepezil
(ii) Irreversible (Organophosphates)
Malathion
Sarin
Parathion
Echothiophate
98
A Textbook of Pharmaceutical
Chemistry
(c) Acridine
Tacrine
Acetylcholine
Acetylcholine was the first neurotransmitter discovered by scientists as well as the most
abundant neurotransmitter in the body. A neurotransmitter is a chemical that is released by a
neuron or nerve cell that sends a signal to another neuron across a synapse. Chemically it is a
choline ester of acetic acid.
Acetylcholine plays an important role in muscle movement, sensation of pain, learning, and
memory formation.
Structure:
O N
+
O
Chemical name: 2-Acetoxy-N,N,N-trimethylethanaminium.
Uses: It is used as a neurotransmitter and neuromodulator, to cause constriction of the pupil
in cataract surgery.
Formulation: Injectable, Eye drops.
Bethanechol
Structure:
N
+
OH
2
N
O
Chemical name: 2-(Carbamoyloxy)-N,N,N-trimethylpropan-1-aminium.
Uses: It is useful in the treatment of urinary retention resulting from the general anesthetic
and diabetic neuropathy of the bladder. It is a drug of choice in the treatment of cerebral palsy
(permanent movement disorders that appear in early childhood. Symptoms include poor
coordination, stiff muscles, weak muscles, and tremors).
Formulations: Tablet, Injectable.
Brand names: Urecholine, Bethacol and Urotonin.
99
Drugs Acting on Autonomic Nervous System (ANS)
Methacholine
Structure:
N
+
O
O
Chemical name: 2-(Acetyloxy)-N,N,N-trimethylpropan-1-aminium.
Uses: It is primarily used to diagnose bronchial hyper-reactivity (Bronchial challenge test).
Formulations: Inhaler, Injectable.
Brand name: Provocholine.
Carbachol
Structure:
N
+
O
O
H
2
N
Cl
-
Chemical name: 2-[(Aminocarbonyl)-oxy]-N,N,N,-trimethylethanaminium chloride.
Uses: It is useful in the treatment of glaucoma and during ophthalmic surgery.
Formulations: Tablet, Ophthalmic, Inhalation and Injectable.
Brand names: Carbastat, Carboptic, IsoptoCarbachol and Miostat.
Pilocarpine
Structure:
O
O
N
N
Chemical name: (3S,4R)-3-thyl-4-[(1-methyl-1H-imidazole-5-yl)-methyl]-dihydrofuran-
2(3H)-one.
Uses: It is used to treat increased pressure inside the eye and Xerostomia (dry mouth). It is
particularly used in Sjögren’s syndrome (a long-term autoimmune disease in which the moisture-
producing glands of the body are affected).
100
A Textbook of Pharmaceutical
Chemistry
Pilocarpine is a selective muscarinic-receptor agonist that is used in the eye drops to
constrict the pupil and to decrease the intraocular pressure that is raised in glaucoma.
Formulations: Eye drops, Injectable.
Brand names: IsoptoCarpine, Salagen, Pilocar and Carpine.
Neostigmine
Structure:
N
+
O
O
N
Chemical name: 3-{[(Dimethylamino)-carbonyl]oxy}-N,N,N-trimethylbenzenaminium.
Uses: It is used to improve muscle tone in people with myasthenia gravis (Long-term
neuromuscular disease that leads to varying degrees of skeletal muscle weakness) and also to
reverse the effects of non-depolarizing muscle relaxants.
Formulations: Tablet, Ophthalmic and Injectable.
Brand names: Prostigmin, Vagostigmin and Myostigmin.
Pyridostigmine
Structure:
N
+
ON
O
Chemical name: 3-[(Dimethylcarbamoyl)-oxy]-1-methylpyridinum.
Uses: Pyridostigmine is used to treat muscle weakness in people with myasthenia gravis or
forms of the congenital myasthenic syndrome.
Formulations: Tablet and Injectable.
Brand names: Mestinon, Distinon and Myestin.
101
Drugs Acting on Autonomic Nervous System (ANS)
Edrophonium
Structure:
N
+
HO
Chemical name: N-Ethyl-3-hydroxy-N,N-dimethylbenzenaminium.
Uses: Edrophonium test is used to differentiate myasthenia gravis from the cholinergic crisis.
It is used in the treatment of Lambert-Eaton myasthenic syndrome (a rare autoimmune disorder
that is characterized by muscle weakness of the limbs).
Formulations: Tablet and Injectable.
Brand names: Tensilon and Enlon.
Tacrine
Structure:
N
NH
2
Chemical name: 1,2,3,4-Tetrahydroacridin-9-amine
Uses: It is the prototypical cholinesterase inhibitor for the treatment of Alzheimer’s disease.
Formulations: Tablet and Injectable.
Brand name: Cognex.
102
A Textbook of Pharmaceutical
Chemistry
Ambinonium
Structure:
O
O
HN
H
N
N
+
Cl
N
+
Cl
Chemical name: 2,2’-[(1,2-Dioxoethane-1,2-diyl)-diimino]bis[N-(2-chlorobenzyl)-N,N-
diethylethanaminium.
Uses: It is used in the management of myasthenia gravis.
Formulations: Tablet and Injectable.
Brand name: Mytelase.
Pralidoxime Chloride (2-Pyridine Aldoxime Methyl Chloride)
Structure:
N
+
N
O
H
Chemical name: 2-[(Hydroxyimino)-methyl]-1-methylpyridin-1-ium.
Uses: It is used to combat poisoning (antidote) caused by organophosphates or
acetylcholinesterase inhibitors (nerve agents) in conjunction with atropine and diazepam.
Formulation: Tablet.
Brand name: 2-PAM.
103
Drugs Acting on Autonomic Nervous System (ANS)
Isoflurophate
Structure:
F
P
O
O
O
Chemical name: bis-(propan-2-yl)-fluorophosphonate.
Uses: As a miotic in the treatment of glaucoma.
Formulation: Ophthalmic
Brand name: DFP
Echothiophate
Structure:
N
+
S P
O
O
O
I
-
Chemical name: 2-(Diethoxyphosphorylsulfanyl)-ethyl-N,N,N-trimethylazanium iodide.
Uses: It is used as an ocular antihypertensive in the treatment of chronic glaucoma.
Formulation: Ophthalmic (Eye drop).
Brand name: Phospholine.
Parathion
Structure:
P
O
O
O
S
N
+
O
-
O
104
A Textbook of Pharmaceutical
Chemistry
Chemical name: O,O-Diethyl-O-(4-nitrophenyl)-phosphorothioate.
Uses: As a pesticide, insecticide.
Formulation: Liquid
Brand names: AC 3422, Alkron and Alleron.
Malathion
Structure:
O
O
O
O
S
PO
O
S
Chemical name: Diethyl-2-[(dimethoxyphosphorothioyl)-sulfanyl]-butanedioate.
Uses: In low doses (0.5% preparations) used to treat head and body lice.
For the mosquito control or insecticide.
Formulation: Liquid.
Brand name: Carbophos.
8.4 PARASYMPATHOLYTICS (CHOLINERGIC BLOCKING
AGENTS)
Parasympatholytic agents reduce the activity of the parasympathetic nervous system. (The
parasympathetic nervous system is often colloquially described as the “Feed and Breed” or “Rest
and Digest” portion of the autonomic nervous system). They are also called anticholinergic agents
because they reverse or block the action of acetylcholine.
Parasympatholytic agents are classified as follows:
(a) Natural Alkaloids
Atropine
Hyoscine
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