CLENBUTEROL

Absorption

89-98% orally

Description

Clenbuterol is a long-acting, potent, and specific β2 stimulator that is used orally.

Chemical properties

White Crystalline Solid

Originator

Spiropent,Thomae,W. Germany,1977

The Uses of CLENBUTEROL

bronchodilator, beta2 adrenergic agonist

The Uses of CLENBUTEROL

Substituted phenylethanolamine with β2 sympathomimetic activity. Bronchodilator.

Background

A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.

Indications

Used as a bronchodilator in the treatment of asthma patients.

Definition

ChEBI: Clenbuterol is a primary arylamine that is 2,6-dichloroaniline in which the hydrogen at position 4 is substituted by a 2-(tert-butylamino)-1-hydroxyethyl group.

Manufacturing Process

127 g of 1-(4'-aminophenyl)-2-t-butylaminoethanol-(1) hydrochloride were dissolved in a mixture of 250 cc of glacial acetic acid and 50 cc of water, and chlorine added while stirring the solution and maintaining the temperature of the reaction mixture below 30°C by cooling with ice water. After all of the chlorine had been added, the reaction mixture was stirred for thirty minutes more, then diluted with 200 cc of water, and made alkaline with concentrated ammonia while cooling with ice, taking care that the temperature of the reaction mixture did not rise above 40°C. The alkaline mixture was extracted three times with 200 cc portions of chloroform, and the chloroform extract solutions were combined, dried with sodium sulfate and evaporated. The residue, the free base 1-(4'-amino-3',5'-dichlorophenyl)-2-tbutylaminoethanol-(1), was dissolved in absolute ethanol, gaseous hydrogen chloride was passed through the solution, and the precipitate formed thereby was collected. It was identified to be 1-(4'-amino-3',5'-dichlorophenyl)-2-tbutylaminoethanol-(1) hydrochloride, melting point 174.0°C to 175.5°C (decamp.).

Therapeutic Function

Anti-asthmatic

Pharmacokinetics

Clenbuterol is a substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma. Although approved for use in some countries, as of fall, 2006, clenbuterol is not an ingredient of any therapeutic drug approved by the U.S. Food and Drug Administration.

Side Effects

The risks of misusing a drug like clenbuterol include its lack of proven effectiveness and its hazardous side effects. Clenbuterol is well-known to cause symptoms such as rapid heart rate (tachycardia), palpitations, tremors, anxiety, lowered blood potassium (hypokalemia), and elevated blood sugar (hyperglycemia). Adverse effects happen more often with the large doses used for performance enhancement and weight loss. Because the drug has a long half-life in the body, toxic symptoms can last from 1 to 8 days.

Metabolism

Not Available