GUANABENZ

Absorption

Approximately 75% absorbed from gastrointestinal tract

Toxicity

Excessive contraction of the pupils, irritability, low blood pressure, sleepiness, slow heartbeat, sluggishness

Description

Guanabenz is an α2-adrenergic agonist that exhibits pronounced hypotensive action, and that is associated with a reduction of overall peripheral vascular resistance, decline in frequency of cardiac contractions, and reduced cardiac output.

Originator

Wytensin,Wyeth,US,1982

The Uses of GUANABENZ

alpha agonists

The Uses of GUANABENZ

It is used both independently and in combination with oral diuretics for treating various degrees of hypertension.

Indications

For management of High blood pressure

Background

An alpha-2 selective adrenergic agonist used as an antihypertensive agent. [PubChem]

Definition

ChEBI: Guanabenz is a dichlorobenzene.

Manufacturing Process

A mixture of 14.0 g of 2,6-dichlorobenzaldehyde, 10.8 g of aminoguanidine bicarbonate and 100 ml of pyridine was refluxed for 3 hours. The reaction mixture was poured into water and the crystalline precipitate filtered off; MP 225°C to 227°C.

Therapeutic Function

Antihypertensive

Pharmacokinetics

Guanabenz, a centrally acting α-2 adrenergic agonist, is indicated for treatment of hypertension.

Synthesis

Guanabenz, [(2,6-dichlorobenzyliden) amino] guanidine (22.3.1), is synthesized in one step by reacting 2,6-dichlorobenzaldehyde with amino guanidine.

Metabolism

Hepatic

Purification Methods

Crystallise the guanidine from MeCN and store it in a CO2–free atmosphere. The monoHCl [23256-5-0] has m 178o(dec) [solubility w% at 25o is 1.1(H2O), 5(EtOH), 0.1(EtOAc), 0.06(CHCl3)]. It is an antihypertensive drug. [Holmes et al. Drugs 26 212 1983.]