Clenbuterol is a drug , selective β2- adrenostimulyator . Exciting β2- adrenoreceptors , has a powerful bronchodilator effect.
Clenbuterol | |
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Clenbuterol | |
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Chemical compound | |
IUPAC | (RS) -4-amino-3,5-dichloro-alpha - [[(1,1-dimethylethyl) amino) methyl] benzenemethanol (as mono hydrochloride ) |
Gross formula | C 12 H 18 Cl 2 N 2 O |
Molar mass | 277.19 |
CAS | |
Pubchem | |
Drugbank | |
Classification | |
ATH | |
Pharmacokinetics | |
Bioavailable | 89-98% orally |
Metabolism | ? |
The period is half out. | 36-39 hours |
Excretion | ? |
Dosage Forms | |
tablets, syrup | |
Other names | |
Clenbuterol, Dilaterol, Spiropent, Ventipulmin | |
Content
Pharmacological action
Selective β2-adrenostimulyator, has a bronchodilator and secretolytic action. It stimulates β2-adrenoreceptors , stimulates adenylate cyclase , increases concentration in cAMP cells, which, affecting the protein kinase system, deprives myosin of its ability to bind to actin and promotes relaxation of the bronchi . Slows down the release of mast cells from mast cells , contributing to bronchospasm and inflammation of the bronchi. Reduces swelling or stagnation in the bronchi, improves mucociliary clearance . In large doses, it causes tachycardia , tremor of the fingers. The beginning of the bronchodilator effect after inhalation - after 10 minutes, maximum - after 2-3 hours, duration of action - 12 hours.
Pharmacokinetics
Absorption is high. Therapeutically effective concentrations are created in plasma 15 minutes after a single dose and persist for 7-24 hours. It is mainly excreted by the kidneys. T1 / 2 - 3 h.
Indications
COPD , bronchial obstruction , bronchial asthma .
Contraindications
Hypersensitivity , thyrotoxicosis , tachyarrhythmia , GOKMP , myocardial infarction (acute period), pregnancy (I term), prenatal period.
Side Effects
Tachycardia , extrasystole , decrease or (more often) increase in blood pressure .
The nervous system
Tremor of the fingers, anxiety, headache .
On the part of the digestive system
Dry mouth, nausea .
Allergic reactions
Skin rash, urticaria .
Other
Hypokalemia .
Overdose
Symptoms
Light tremor of the limbs, tachycardia.
Treatment
Reduce the dose of the drug, symptomatic therapy.
Special instructions
Perhaps the development of resistance and syndrome "rebound" . It should stop taking the drug shortly before childbirth, since clenbuterol has a tocolytic effect. Do not allow the drug to get into the eyes, especially with glaucoma .
Interaction
Antagonism with β-blockers. Reduces the effect of hypoglycemic drugs. Increases the risk of developing disorders of intracardiac conduction, while the appointment with MAO inhibitors and theophylline . Increases the toxicity of cardiac glycosides and the risk of arrhythmias . In combination with sympathomimetic drugs, they mutually increase toxicity.
Use in sports
Clenbuterol has been banned in sports since 1992. It is determined by anti-doping control for a long time, as it accumulates in adipose tissue and is released during exercise or competition. Popular with bodybuilders at the level of amateurs who are not covered by anti-doping control. Clenbuterol is believed to have a fat burning effect.
One of the possible ways for Clenbuterol to enter the body of an athlete can be meat, as in some countries (China, Mexico) it is used to increase the weight of fattened animals.
In 2012, Chinese Olympians before the Olympics in London were transferred to a vegetarian diet. This was done because of the fear of getting into their bodies with the meat of a prohibited substance - clenbuterol. Violation of the ban was punished by exclusion from the national team.
On September 8, 2016, Jin Jingdao, a Chinese football club Shandong Luneng , was suspended from the match for 60 days by the Asian Football Confederation after a positive test for clenbuterol in the 2016 AFC Champions League match against Seoul . [one]
Notes
- ↑ Church, Michael Shandong Luneng's Jin Jingdao suspended for doping violation . ESPN FC .com (9 September 2016). The appeal date is September 10, 2016.
Links
- The article “Clenbuterol. What you didn’t know "// Iron World Magazine