CLENBUTEROL TABLETS INSTRUCTIONS
Clenbuterol Sofarma - instructions for use
INSTRUCTION on
medical use of the drug
Registration number
Trade name:
Clenbuterol Sofarma.
International non-proprietary name:
Clenbuterol
Dosage form:
Tablets
Composition per 1 tablet:
Active substance: 0.02 mg clenbuterol hydrochloride
Excipients: lactose monohydrate - 70.00 mg, wheat starch - 31.48
mg, microcrystalline cellulose - 48.50 mg, colloidal silicon dioxide - 2.00 mg,
magnesium stearate - 2.00 mg, povidone (povidone K25) - 6.0 mg.
Description:
Round flat tablets
with a chamfer and a dividing groove on one side, white or almost white in
color.
Pharmacotherapeutic group:
Bronchodilator - beta -2-adrenomimetic selective agent
ATX code
[R03CC13]
Pharmacological properties
Pharmacological action
Selective
beta-2-adrenergic stimulant, has bronchodilator and secretolytic action.
Excites p2 - adrenoreceptors, stimulates adenylate cyclase, increases the
content of cyclic adenosine monophosphate (cAMP) in cells. The latter has an
effect on the protein kinase system, as a result of which myosin is deprived of
the ability to connect to actin and bronchodilation occurs. Inhibits the
release of mediators from mast cells that cause bronchospasm and bronchial
inflammation.
Prevents bronchospasm
caused by histamine, serotonin, and acetylcholine. Reduces edema or congestion
in the bronchi, improves mucociliary clearance. Secretolytic effect of the drug
is associated with a decrease in the viscosity of sputum and facilitates its
excretion. Causes dilation of cerebral vessels and skeletal muscles. It has a
tocolytic effect. Side effects are associated with its ability, albeit weakly,
to excite p1 - adrenoreceptors of the heart, resulting in a positive in- and
chronotropic effect.
It has a slight anabolic
effect, can increase body temperature.
The maximum effect of
the drug is observed in 2-3 hours and lasts up to 6-8 hours.
Pharmacokinetics
It is rapidly and
completely absorbed in the gastrointestinal tract. Metabolized to a small
extent in the liver, resulting in the formation of 8 metabolites that have no
pharmacological activity. Excretion from plasma takes place in two phases. The
half-life of the first phase is 1 hour, the second - 34 hours. Most of the body
is excreted unchanged through the kidneys, with 87% of the dose excreted within
168 hours.
Indications for use:
Chronic obstructive
pulmonary disease, bronchoobstructive syndrome, bronchial asthma.
Contraindications:
Hypersensitivity to
clenbuterol or to the excipients of the drug, thyrotoxicosis, tachyarrhythmia;
hypertrophic obstructive cardiomyopathy; myocardial infarction (acute phase),
severe ischemic heart disease, lactase insufficiency, lactose intolerance, glucose-galactose
malabsorption, children under 6 years of age, pregnancy (I and III trimester).
With caution:
hyperthyroidism,
myocardial infarction in the anamnesis, ischemic heart disease, arterial
hypertension, prostatic hypertrophy, diabetes mellitus, II trimester of
pregnancy.
Pregnancy and lactation period
It is necessary to
avoid administration of the drug in the first 3 months of pregnancy due to
possible adverse effect on fetal development. Its administration is not
recommended in the last months of pregnancy and during labor due to the
presence of tocolytic action of the drug and possible suppression of uterine
tone. There have been no special clinical studies of the drug penetration into
breast milk, therefore its administration to nursing women is not recommended.
Method of administration and dosage
Inside.
Adults: 0.02 mg (one
tablet) 2 times a day (morning and evening). Maintenance dose of 0.01 mg (1/2
tablet) 2 times a day. In more severe conditions in the first days prescribe
0.04 mg (two tablets) 2 times a day (morning and evening). After improvement of
the patient's condition, the dose of the drug should be reduced.
Children: from 6 to
12 years - 0.01 mg (1/2 tablet) 2 times a day (morning and evening). Children
over 12 years of age - 0.01 mg (1/2 tablet) 2-3 times a day or 0.02 mg (1
tablet) 2 times a day (morning and evening).
Side effects
Central nervous
system - fear, psychiatric disorders, hyperkinesis, sleep disturbance,
headache, facial redness, sweating, trembling and restlessness, dizziness,
Parkinson's disease patients may experience increased tremor and muscle
rigidity.
Cardiovascular system
- palpitations, tachycardia, decreased or (more often) increased blood
pressure.
Urinary system -
urinary retention associated with spasm of renal vessels and bladder sphincter.
Metabolism -
hyperglycemia may occur in patients with diabetes mellitus as a result of
stimulation of glycogenolysis. Appearance of this side effect requires
reduction of the drug dose without discontinuation of treatment.
Digestive system -
dry mouth, nausea.
Possible allergic reactions:
skin rash, urticaria.
Others - hypokalemia.
Overdose
Manifested by an
increase in adverse reactions: arrhythmia, tachycardia, increased blood
pressure, cardialgia, tremor of the extremities. There is a risk of hypokalemia
after overdose, so it is necessary to monitor the serum concentration of
potassium.
Treatment: gastric
lavage, intake of activated charcoal, use of water-saline solutions,
symptomatic (including selective beta-adrenoblockers with caution).
Interaction with other medicinal products
Beta-adrenoblockers
due to antagonism with clenbuterol may reduce or eliminate its bronchodilator
effect.
Reduces the effect of
hypoglycemic drugs.
Concomitant use with
cardiac glycosides, monoamine oxidase inhibitors and theophylline increases the
risk of cardiac rhythm disturbances.
Reduces the effectiveness
of hypotensive drugs.
The effect of the
drug is potentiated by tricyclic antidepressants, beta-adrenomimetics and
anticholinergic agents. In combination with sympathomimetic drugs mutually
increases toxicity.
Halothane and other
halogenated hydrocarbon agents for anesthesia, as well as cyclopropane, can
potentiate proarrhythmogenic effect of p2 - adrenomimetics, including
clenbuterol.
Special instructions
When treating
patients with diabetes mellitus, it is necessary to periodically monitor blood
glucose levels. The use of the drug may lead to an increase in body weight due
to the presence of anabolic effect, and when administered to athletes, the drug
may cause a positive result during doping control.
During treatment with
the drug it is possible to develop resistance and "ricochet"
syndrome.
The drug contains
wheat starch. Wheat starch may contain gluten, but only in insignificant
amounts, and therefore it is considered safe for people with celiac disease.
Due to the
possibility of tremor, dizziness and weakness, during treatment with the drug
it is necessary to refrain from performing potentially dangerous activities
requiring special attention and quick reactions (driving a car and other
vehicles, work with moving mechanisms).
Form of release:
Tablets 0.02 mg.
10 tablets in a
blister of PVC film/aluminum foil.
5 blisters together
with instructions for use in a carton pack.
Storage conditions
In a dry place,
protected from light, at a temperature not exceeding 25 ° C.
Keep out of reach of
children!
Shelf life
3 years. Do not use
after expiration date.
Conditions of release
By prescription.
Name and address of the manufacturer
Bulgaria, 1220 Sofia,
Ilienskoye shosse Str. No. 16