Clenbuterol instructions
OFFICIAL INSTRUCTIONS ON THE USE OF CLENBUTEROL SOPHARMA
(translated from Russian)
MINISTRY OF
HEALTH AND
SOCIAL
DEVELOPMENT
OF THE RUSSIAN FEDERATION
INSTRUCTION
on the use of
the drug
for medical use
CLENBUTEROL SOPHARMA
Brand Name: Clenbuterol Sofarma.
International
Nonproprietary 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 dividing risk on one side, white or
almost white.
Pharmacotherapeutic
group:
Bronchodilating agent - selective beta-2-adrenergic
agonist
ATX Code
[R03CC13]
Pharmacological
properties
Pharmachologic effect.
Selective beta-2-adrenostimulator, has a
bronchodilator and secretolytic effect. It excites β2-adrenergic receptors,
stimulates adenylate cyclase, and increases the content of cyclic adenosine
monophosphate (cAMP) in the cells. The latter has an effect on the protein
kinase system, as a result of which myosin loses its ability to bind to actin
and bronchodilation occurs. It inhibits the release of mediators from mast
cells, which cause bronchospasm and inflammation of the bronchi.
Prevents bronchospasm caused by histamine, serotonin
and acetylcholine. Reduces edema or congestion in the bronchi, improves
mucociliary clearance. The secretolytic effect of the drug is associated with a
decrease in the viscosity of sputum and facilitate its release. Causes the
expansion of blood vessels in the brain and skeletal muscles. It has a
tocolytic effect. Side effects are associated with its ability, albeit weakly,
to cause excitation of β1 - adrenoreceptors of the heart, as a result of which
a positive inotropic and chronotropic effect is manifested.
It has a slight anabolic effect, can increase body
temperature.
The maximum effect of the drug is observed after 2-3
hours and lasts up to 6-8 hours.
Pharmacokinetics
Quickly and completely absorbed in the
gastrointestinal tract. It is metabolized to a small extent in the liver, as a
result of which 8 metabolites are formed that do not have pharmacological
activity. Isolation from plasma passes in two phases. The half-life of the first
phase is 1 hour, the second 34 hours. For the most part, it is excreted
unchanged through the kidneys, with 87% of the dose taken excreted within 168
hours.
Indications
for use:
Chronic obstructive pulmonary disease, bronchial
obstructive syndrome, bronchial asthma.
Contraindications:
Hypersensitivity to clenbuterol or to excipients of
the drug, thyrotoxicosis, tachyarrhythmia; hypertrophic obstructive
cardiomyopathy; myocardial infarction (acute phase), severe coronary heart
disease, lactase deficiency, lactose intolerance, glucose-galactose
malabsorption, children under 6 years of age, pregnancy (I and III trimester).
With caution:
hyperthyroidism, a history of myocardial infarction, coronary heart disease,
arterial hypertension, prostate hypertrophy, diabetes mellitus, II trimester of
pregnancy.
Pregnancy and
lactation
It is necessary to avoid prescribing the drug in the
first 3 months of pregnancy due to a possible adverse effect on the development
of the fetus. Its prescription is not recommended in the last months of
pregnancy and during childbirth due to the presence of tocolytic effect of the
drug and the possible suppression of uterine tone. Special clinical studies of
the penetration of the drug into breast milk have not been conducted, and
therefore its administration to lactating women is not recommended.
Dosage and
administration
Inside.
Adults: 0.02 mg (one tablet) 2 times a day (morning
and evening). Supporting dose is 0.01 mg (1/2 tablet) 2 times a day. In more
severe conditions, in the first days, 0.04 mg (two tablets) is prescribed 2
times a day (morning and evening). After improving the patient's condition, the
dose of the drug must be reduced.
Children: from 6 to 12 years old - 0.01 mg (1/2
tablet) 2 times a day (morning and evening). For children over 12 years old -
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
On the part of the central nervous system - a sense of
fear, mental disorders, hyperkinesis, sleep disturbance, headache, redness of the
face, sweating, trembling and restlessness, dizziness, patients with
Parkinson's disease may experience increased tremors and muscle rigidity.
On the part of the cardiovascular system -
palpitations, tachycardia, decreased or (more often) increased blood pressure.
On the part of the urinary system - urinary retention
associated with spasm of the renal vessels and sphincter of the bladder.
On the part of metabolism, hyperglycemia may appear as
a result of stimulation of glycogenolysis in patients with diabetes mellitus.
The appearance of this side effect requires a decrease in the dose of the drug
without stopping treatment.
On the part of the digestive system - dry mouth,
nausea.
Allergic reactions are possible: skin rash, urticaria.
Others - hypokalemia.
Overdose
It is manifested by an increase in adverse reactions:
arrhythmia, tachycardia, increased blood pressure, cardialgia, tremor of the
extremities. There is a risk of hypokalemia after an overdose, therefore, it is
necessary to monitor the serum concentration of potassium.
Treatment: gastric lavage, intake of activated
charcoal, the use of water-salt solutions, symptomatic (including with caution
with selective beta-blockers).
Interaction
with other drugs
Beta-blockers due to antagonism with clenbuterol can
reduce or eliminate its bronchodilating effect.
Reduces the effect of hypoglycemic drugs.
With simultaneous use with cardiac glycosides,
monoamine oxidase inhibitors and theophylline, the risk of developing heart
rhythm disorders increases.
Reduces the effectiveness of antihypertensive drugs.
The effect of the drug is potentiated by tricyclic
antidepressants, beta - adrenergic agonists and anticholinergics.
In combination with sympathomimetic drugs, toxicity
mutually increases.
Halotane and other halogenated hydrocarbon
anesthetics, as well as cyclopropane, can potentiate the proarrhythmogenic
effect of β2 -adrenomimetics, including clenbuterol.
Special
instructions
When treating patients with diabetes mellitus, it is
necessary to periodically monitor the level of glucose in the blood. The use of
the drug can lead to an increase in body weight due to the presence of an
anabolic effect, and when prescribed to athletes, the drug can cause a positive
result during the doping control.
During treatment with the drug, the development of
resistance and rebound syndrome is possible.
The composition of the preparation contains wheat
starch. Wheat starch may contain gluten, but only in small quantities, and
therefore is considered safe for people with celiac disease.
Due to the possibility of tremor, dizziness and
weakness, during the period of treatment with the drug, it is necessary to
refrain from performing potentially dangerous activities that require special
attention and quick reactions (driving a car and other vehicles, working with
moving mechanisms).
Release form:
Tablets 0.02 mg.
10 tablets per blister of PVC film / aluminum foil.
5 blisters each along with instructions for use in a
cardboard pack.
Storage
conditions
In a dry, dark place at a temperature of no higher
than 25 ° C.
Keep out of the reach of children!
Shelf life
3 years. Do not use after expiration date.
Terms of
sale
On prescription.
Name and
address of manufacturer
AO SOFARMA
Bulgaria, 1220 Sofia, st. Ilienskoe highway №16
