But-x-sha solution for infection. 20mg/ml amp. 2 ml No. 5

Structure and form of release

Structure

Active ingredient: drotaverine;

1 ml of solution;

excipients: ethanol of 96%, sodium metabisulphite (E 223), water for injections.

a release Form

Solution for injections.

Pharmacological properties

Pharmacodynamics.

Drotaverinum - an isoquinoline derivative which has spasmolytic effect on smooth muscles by oppression of effect of enzyme of phosphodiesterase IV (FDE IV) that leads to increase in concentration of tsAMF and, thanks to an inactivation of an easy chain of a kinase of myosin (MLCK), to relaxation of unstriated muscles.

In vitro Drotaverinum suppresses effect of FDE IV enzyme and does not influence action of isoenzymes of phosphodiesterase III (FDE III) and phosphodiesterase V (FDE V). FDE ІV has great functional value for decrease in sokratitelny activity of unstriated muscles therefore selective inhibitors of this enzyme can be useful to treatment of the diseases which are followed by hyper mobility and also various diseases at which there are digestive tract spasms.

In cells of unstriated muscles of a myocardium and vessels of tsAMF it is hydrolyzed mainly by FDE III isoenzyme therefore Drotaverinum is effective antispasmodic which has no considerable side effects from a cardiovascular system and strong therapeutic action on this system.

at spasms of smooth muscles of both nervous, and muscular origin. Drotaverinum affects smooth muscles of gastrointestinal, biliary, urinogenital and vascular systems irrespective of type of their autonomous innervation.

It strengthens blood circulation in fabrics thanks to the ability to expand vessels.

actions of a papaverine, absorption faster and full, it contacts serum proteins less. Advantage of Drotaverinum is also that, unlike a papaverine, after its parenteral administration such side effect as breath stimulation is not observed.

Pharmacokinetics.

after parenteral administration. It substantially (95–98%) contacts proteins of blood plasma of the person, especially albumine, gamma and beta globulins. After primary metabolism of 65% of the entered dose comes to a blood-groove in not changed look.

It is metabolized in a liver. The half-cycle of biological existence makes 8–10 hours.

In 72 hours from an organism, about 50% are removed with urine and about 30% — with a stake. Generally Drotaverinum is removed in the form of metabolites, in not changed form in urine it is not found.

Indication

Spasms of smooth muscles connected with diseases of a biliary path: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

Spasms of smooth muscles at diseases of an uric path: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus.

As auxiliary treatment (if use of medicine in the form of tablets is impossible):

• at spasms of smooth muscles of digestive tract: peptic ulcer of a stomach and duodenum, gastritis, kardio and/or pylorospasm, enteritis, colitis;
• at gynecologic diseases: dysmenorrheas.

Contraindication

Increased individual sensitivity to active ingredient or to any component of medicine (especially to sodium to metabisulphite); hypersensitivity to sodium to disulphite; heavy liver, renal or heart failure (syndrome of small warm emission).

Route of administration and doses

Usual average daily dose for adults makes 40–240 mg (for 1–3 separate introductions) intramusculary.

In sharp gripes at adult patients with concrements in uric or bilious ways - 40–80 mg intravenously.

Feature of application

Due to the risk of emergence of collapse at intravenous administration of medicine of the patient has to be in lying situation!

with care at arterial hypotension.

Drug contains metabisulphite which can cause reactions of allergic type, including symptoms of an acute anaphylaxis and a bronchospasm in sensitive patients, especially in those who have asthma or an allergy in the anamnesis. In case of hypersensitivity to sodium metabisulphite it is necessary to avoid parenteral administration of medicine.

Use during pregnancy or feeding by a breast

Pregnancy. as showed results of retrospective clinical trials, oral administration of medicine did not entail in one case of teratogenecity and embriotoxity. however pregnant women need to appoint medicine with care. not to apply Drotaverinum during childbirth.

Feeding by a breast. Due to the lack of these corresponding researches on animals during feeding by a breast introduction of medicine is not recommended.

Fertility. There are no data on influence on fertility of the person.

to Drivers

needs to warn patients that after parenteral, especially intravenous administration of medicine it is recommended to refrain from the driving and performance of work requiring special attention.

Children

to children did not conduct Clinical trials of use of medicine.

Overdose

Symptoms: the overdose by Drotaverinum was associated with violations of a warm rhythm and conductivity, including with a total block of legs of a ventriculonector and cardiac arrest which can be lethal.

At overdose the patient has to be under careful observation of the doctor and receive symptomatic treatment which includes induction of vomiting and/or gastric lavage.

Side reactions

Side effect which was observed during clinical trials and, perhaps, was caused by Drotaverinum, distributed on the systems of bodies.

from the immune system.

Allergic reactions, including a Quincke's disease, a small tortoiseshell, rash, the naggers, fever, a fever, fervescence, weakness, especially at patients with hypersensitivity to metabisulphite.

It was reported also about cases of an acute anaphylaxis with lethal and non-lethal consequences at application of an injection form.

Drug contains metabisulphite which can cause reactions of allergic type, including symptoms of an acute anaphylaxis and a bronchospasm in sensitive patients, especially those who have asthma or an allergy in the anamnesis.

from a cardiovascular system.

Cardiopalmus, arterial hypotension.

from nervous system.

Headache, dizziness, insomnia.

from digestive tract.

Nausea, lock, vomiting.

General violations and reactions in the injection site.

Local reactions in the injection site of an injection.

Interaction

phosphodiesterase Inhibitors (Drotaverinum, a papaverine) reduce antiparkinsonichesky effect of a levodopa. it is necessary to use with care medicament along with a levodopa as the antiparkinsonichesky effect of the last decreases, and the rigidity and a tremor amplify.

to Store

out of children's reach in original packing at a temperature not above 25 °C. An expiration date - 3 years.