Lecture -3

Pharmacology of adrenergic neuron blockers

Dr. Jibachha Sah

M.V.Sc (Veterinary pharmacology)
College of Veterinary Science, NPI
Bhojard, Chitwan
Definition: Adrenergic neuron blockers

Adrenergic neuron blocking agents are transported into adrenergic neurons by the carrier
mechanism utilized by noradrenaline and related amines.

In other word, a drug that blocks sympathetic nerve impulses but does not inhibit the
responses of adrenergic receptors to epinephrine and other adrenergic amines.

Adrenergic neuron blockers drug

● Reserpine- Antihypertensive

● Guanethidine- Antihypertensive

●Guanadrel - Antihypertensive

● Bretylium- Anti-arrhythmic
 Classification of Adrenergic Neuron Blockers

Adrenergic neuron blockers may be classified into drugs which

prevent release of noradrenaline, drugs that inhibit storage of
noradrenaline or drugs that interfere with synthesis of noradrenaline.

Drugs which prevent release of noradrenaline

•Guanethidine
•Guanadrel
•Bethanidine
•Debrisoquine
•Bretylium
Drugs that inhibit storage of noradrenaline
Reserpine

Drugs that interfere with synthesis of noradrenaline:

Metyrosine
 (i) Reserpine

Reserpine is a naturally occurring drug that has been used for centuries in India. It
is extracted from the root of Rauwolfia serpentina or Rauwolfia vomitoria plants
found there and in Africa.

Horses
Reserpine is used as a long-acting tranquilizer in horses. It is used to sedate
excitable or difficult horses that are on enforced rest. It sometimes is used illicitly to
sedate show horses, sale horses, or in other circumstances where a "quieter" horse
might be desired.

Mechanism of action

Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of
catecholamines and serotonin from central and peripheral axon terminals. It has been used as
an antihypertensive and an antipsychotic as well as a research tool, but its
adverse effects limit its clinical use.
(ii) GUANATHEDINE/BRETYLIUM

● It inhibits nerve impulse coupled N.A release from vesicles(bretylium).

● Displaces N.A from storage vesicles
●Engages and blocks the N.A reuptake at axonal membrane(REUPTAKE -1)
Reserpine Side Effects

Different horses vary greatly in their sensitivity to this drug.

Common side-effects include, colic, gastrointestinal upset and mild diarrhea that
may last for days, and sweating over the back and hind legs. Signs of sedation
include depression, droopy eyes, and a dropped penis.
Reserpine increases gastric secretion in humans and increases the risk of ulcers.

Drug Interactions

Reserpine may interact with drugs used for general anesthesia.

Methamphetamine is an antidote to reserpine.