Clenbuterol is a medication used to treat asthma and COPD in some countries, but it is not FDA-approved for human use in the United States. It is widely misused for possible anabolic and fat-burning effects, which have only been shown in animals. Clenbuterol causes toxicity at low doses. Symptoms include tremors, high heart rate, low blood potassium, seizures, and cardiac arrest.
Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Clenbuterol is an Anti-Asthmatic agent belonging to the Long-Acting Beta 2 Adrenergic Receptor Agonist Pharmacological class.
Clenbuterol is approved for the treatment of Bronchospasm, Emphysema, and Bronchial Asthma.
Clenbuterol doses of 20, 30,40mcg were administered to healthy volunteers and the plasma level achieved was found to be 0.1,0.2,0.35ng/ml within 2.5h. This lasted for four hours after the administration. The estimated half-life of Clenbuterol was found to be 35h. Following twice-a-day administration of Clenbuterol in male volunteers. The plasma levels were found to achieve a plateau within 4 days of initial administration. The plasma concentrations of the unchanged form of Clenbuterol were found to be 0.2-0.3ng/ml and 0.5-0.6ng/ml at doses of 20mg and 40mg. The amount of drug bound to the plasma protein was found to be 89-98% at 80mg doses of a single administration. The excretion rate of Clenbuterol after single administration is about 20% measured at 72hours. The unmetabolized drug in plasma and urine was estimated by an enzyme immunoassay test.
The common side effects associated with Clenbuterol are Headache, palpitations, nausea, nervousness, anxiety, dry mouth, etc.
Clenbuterol belonging to the pharmacological class of Short-Acting Beta 2 Adrenergic Receptor Agonists, acts as an Anti-asthmatic/Bronchodilator therapeutic agent. Clenbuterol acts via a series of pathways causing increasing cAMP, thereby deactivating myosin light chain kinase and activating myosin light chain phosphate leading to smooth muscle relaxation in the bronchioles. Clenbuterol hence leads to Bronchodilation of the smooth muscles and reverses bronchospasm.
Clenbuterol can be used in the treatment of bronchospasm in patients with bronchial asthma, and emphysema.
Clenbuterol can help to relax bronchial smooth muscle leading to Bronchodilation and improving the patient's respiration.
Although not approved, there have been certain Off-label uses documented for clenbuterol. These include:
- Performance enhancement in athletes
- Weight loss regimen
The common side effects of Clenbuterol include the following:
- Tachycardia
- Subaortic stenosis
- High blood pressure
- Nervousness
- Thyrotoxicosis
The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of the molecule Clenbuterol.
- A maximum dose of 120ug has been found to cause gastric irritation, headache, dizziness, tremors, and muscle cramps.
- People who self-administer Clenbuterol have experienced nausea, vomiting, tachycardia, myocardial infarction, and palpitations
- Pharmacodynamics:
Clenbuterol acts as a beta 2 adrenergic receptor agonist at low doses.
- Pharmacokinetics:
When therapeutic doses of 20, 30,40mcg were administered to healthy volunteers the plasma level achieved was found to be 0.1,0.2,0.35ng/ml within 2.5h.This lasted for four hours after the administration. The estimated half-life of Clenbuterol was found to be 35h. Following twice-a-day administration of Clenbuterol in male volunteers. The plasma levels were found to achieve a plateau in 4 days of initial administration. The plasma concentrations of the unchanged form of Clenbuterol were found to be 0.2-0.3ng/ml and 0.5-0.6ng/ml at doses of 20mg and 40mg. The amount of drug bound to the plasma protein was found to be 89-98% at 80mg doses of a single administration. The excretion rate of Clenbuterol after single administration is about 20% measured at 72hours. The unmetabolized drug in plasma and urine was estimated by an enzyme immunoassay test.
- Zhu Y, Culmsee C, Roth-Eichhorn S, Krieglstein J: Beta(2)-adrenoceptor stimulation enhances latent transforming growth factor-beta binding protein-1 and transforming growth factor-beta1 expression in rat hippocampus after transient forebrain ischemia. Neuroscience. 2001;107(4):593-602.
- Ryall JG, Gregorevic P, Plant DR, Sillence MN, Lynch GS: Beta 2-agonist fenoterol has greater effects on contractile function of rat skeletal muscles than clenbuterol. Am J Physiol Regul Integr Comp Physiol. 2002 Dec;283(6): R1386-94. Epub 2002 Sep 5.
- Choo JJ, Horan MA, Little RA, Rothwell NJ: Anabolic effects of clenbuterol on skeletal muscle are mediated by beta 2-adrenoceptor activation. Am J Physiol. 1992 Jul;263(1 Pt 1): E50-6.
- Sillence MN, Matthews ML, Spiers WG, Pegg GG, Lindsay DB: Effects of clenbuterol, ICI118551, and sotalol on the growth of cardiac and skeletal muscle and on beta 2-adrenoceptor density in female rats. Naunyn Schmiedebergs Arch Pharmacol. 1991 Oct;344(4):449-53.
- Mazzanti G, Di Sotto A, Daniele C, Battinelli L, Brambilla G, Fiori M, Loizzo S, Loizzo A: A pharmacodynamic study on clenbuterol-induced toxicity: beta1- and beta2-adrenoceptors involvement in guinea-pig tachycardia in an in vitro model. Food Chem Toxicol. 2007 Sep;45(9):1694-9. Epub 2007 Mar 12.
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
- Coleman RA, Johnson M, Nials AT, Vardey CJ: Exosites: their current status, and their relevance to the duration of action of long-acting beta 2-adrenoceptor agonists. Trends Pharmacol Sci. 1996 Sep;17(9):324-30.
- go.drugsbank.com
- pubchem.com
