Clenbuterol

Pharmachologic effect:

adrenomimetic, bronchodilator.

Pharmacodynamics:

Clenbuterol is a drug with a rapid bronchodilator effect. Its action is due to the specific stimulation of β2-adrenergic receptors of smooth muscles. When bound to them, the enzyme adenylate cyclase is activated, which leads to an increase in the intracellular concentration of cyclic adenosine monophosphate and activation of protein kinase A, and deprives myosin of the ability to combine with actin, resulting in relaxation of the bronchi. Clenbuterol stimulates the cells of the bronchial mucosa and enhances expectoration. At prescribed therapeutic doses, clenbuterol does not affect heart rate or blood pressure.

Pharmacokinetics:

Clenbuterol is relatively rapidly absorbed from the gastrointestinal tract. Communication with plasma proteins is 89-98%. The biological T1/2 is 3.5 hours. Clenbuterol is excreted mainly through the kidneys in the form of sulfo-conjugated derivatives.

Indications:

Bronchial asthma, chronic obstructive bronchitis, pulmonary emphysema and other lung diseases with broncho-obstructive syndrome.

Contraindications:

thyrotoxicosis;
hypertrophic obstructive cardiomyopathy;
angle-closure glaucoma;
pheochromocytoma;
tachyarrhythmia;
myocardial infarction (acute period);
pregnancy (I and III trimester);
lactation period;
children's age up to 6 years;
hypersensitivity to the active substance or to any of the excipients.

Use with caution:

Use with caution immediately after a myocardial infarction, with liver and kidney failure, heart rhythm disturbances, myocarditis, mitral valve defects, hypokalemia, unstable or uncompensated diabetes.

Pregnancy and breast-feeding:

Clenbuterol is contraindicated in the I trimester of pregnancy and just before birth.

Side effects:

Cardio-vascular system and blood: tachycardia, arrythmia, reduction or (more often) increase in blood pressure. Nervous system and sensory organs: the tremor of fingers, anxiety, headache. Digestive tract: dry mouth, nausea. Allergic reactions: skin rash, urticaria. Other: hypokalemia.

Interaction:

Beta-blockers inhibit the action of Clenbuterol, and when they are taken simultaneously, there is a risk of developing bronchospasm.
The use of the drug simultaneously with hypoglycemic agents reduces their effect.
Clenbuterol enhances the action and side effects of beta-agonists, theophylline and anticholinergics.
With the simultaneous use of clenbuterol and halogenated hydrocarbons for anesthesia (with manipulations and interventions), there is an increased risk of arrhythmia.
Clenbuterol can be used simultaneously with diuretics and cardiac glycosides, but with periodic monitoring of serum electrolytes.
With simultaneous use with MAO inhibitors (tricyclic antidepressants), cardiac arrhythmias are possible.

Dosing and Administration:

Adults and children over 12 years - 10-20 mcg 2-3 times a day, maintenance dose - 10 mcg 2 times a day.
Young children - in small doses, depending on the age, 2 times a day.
The duration of the course of treatment with Clenbuterol is 2-3 days, until the acute symptoms of the disease are relieved.
The duration of maintenance therapy should not exceed 7 days. The decision on treatment for a period exceeding seven days is made by the attending physician.

Overdose:

Symptoms: tremor of the extremities, restlessness, tachycardia. Treatment: dose reduction, symptomatic therapy

Special instructions:
The drug contains the so-called parabens as excipients: methyl parahydroxybenzoate and propyl parahydroxybenzoate, which can cause urticaria and contact dermatitis (delayed-type allergic reactions). Rarely, immediate allergic reactions (bronchospasm) may occur.
The drug contains glycerol as an auxiliary substance, which at high doses can cause headache, stomach irritation and diarrhea.
The drug contains 0.63 vol.% of ethyl alcohol. Each dose contains 0.005 g of alcohol per 1 ml. It is dangerous for people with liver disease, alcoholism, epilepsy, brain damage or disease, as well as for pregnant women and children. May enhance the effect of other medicines.
The drug is not suitable for patients with congenital fructose intolerance due to the presence of sorbitol in it.
In the first days of treatment, clenbuterol can cause slight tremors and restlessness, which requires increased caution when driving a car and working with machinery.

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