Бускопан®

General characteristics. Structure:

Active ingredient: 20 mg of hyoscine of butylbromide.

Excipients: sodium chloride, water for injections.

The drug for treatment of functional disorders of digestive tract having spasmolytic effect on smooth muscles of internals.

Pharmacological properties:

Pharmacodynamics. Бускопан® – blocker M-holinoretseptorov, has spasmolytic effect on smooth muscles of internals (gastrointestinal, bilious and urinogenital paths). Being quarternary ammonium connection, hyoscine butylbromide does not get through a blood-brain barrier therefore anticholinergic influence on the central nervous system is absent.

Pharmacokinetics. Absorption and distribution. After intravenous administration of hyoscine butylbromide is quickly distributed in fabrics (t1/2a = 4 min., t1/2b = 29 min. Distribution volume – 128 l (there correspond about 1,7 l/kg). Because of high similarity to muskarinovy and nicotinic receptors, hyoscine butylbromide is distributed, generally in muscle cells of belly and pelvic area, also as in intramural gangliya of an abdominal cavity.

Communication with proteins of plasma makes weak, about 4,4%. Hyoscine butylbromide does not get through a blood-brain barrier, however clinical trials in the field were not conducted.

Metabolism and removal. It is removed by hydrolytic splitting of radio bonds. An elimination half-life – about 5 hours. The general clearance – 1,2 l/min. After intravenous administration about 42 to 61 also from 28,3 to 37% through a GIT are removed through kidneys (50% in an invariable look). The metabolites removed through kidneys badly contact muskarinovy receptors, not a vliyayana effect of hyoscine of butylbromide.

Indications to use:

- spastic conditions of a gastrointestinal, bilious and urinogenital path, including renal and bilious colic;

- for elimination of a spasm before holding diagnostic and therapeutic procedures (endoscopic, X-ray inspections, etc.)

Route of administration and doses:

If the doctor it is not appointed differently, it is recommended to use the following dosages. Adults and teenagers are more senior than 12 years: on 1-2 ampoules (20-40 mg) by slow intravenous, intramuscular or hypodermic administration several times a day. Maximum daily dose of 100 mg.

Babies and children up to 12 years. At serious cases: 0,3-0,6 mg/kg of body weight, by slow intravenous, intramuscular or hypodermic administration a little разв day. Maximum daily dose of 1,5 mg/kg of body weight.

Drug should not be accepted on a constant daily basis or during a long span without clarification of the reasons of an abdominal pain.

Features of use:

If severe pain in a stomach remains or worsens, or morbidity of a stomach (proceeds with such symptoms as fever, nausea, vomiting, changes of a vermicular movement, when pressing), a lowering of arterial pressure, a loss of consciousness or blood in a chair, it is necessary to take the appropriate diagnostic measures for a research of an etiology of symptoms.

Anticholinergic BUSKOPANA® properties can cause increase in intraocular pressure in patients with not treated closed-angle glaucoma. At emergence of pain, reddening of eyes with disturbance of clearness of sight, after introduction БУСКОПАНА®, it is necessary to address the specialist immediately.

Also after parenteral administration БУСКОПАНА® isolated cases of an anaphylaxis, including cases of an acute anaphylaxis were observed. In this regard, the patients receiving БУСКОПАН® parenterally have to be under strict control of the doctor.

Fertility, pregnancy and period of a lactation. There are no sufficient data of use of drug of pregnancy in time. However it is necessary to appoint with care drug during pregnancy, especially in the first trimester and the lactation period. In need of use of drug it is necessary to estimate potential advantage of therapy for mother and possible risk for a fruit.

Researches on impact of drug on fertility of the person were not conducted.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. Researches about influence on ability to drive the car and potentially dangerous mechanisms were not conducted. However patients have to be informed on possible risk of emergence of side effects, such as: disturbance of visual accommodation or dizziness at administration of drug БУСКОПАН®. At emergence of disturbance of visual accommodation or dizziness, patients are recommended to avoid the driving of the car and occupations with other potentially dangerous types of activity demanding increase in attention and speed of psychomotor reactions until sight is not normalized.

Side effects:

Many of the side effects described below can be connected with anticholinergic BUSKOPANA® properties. Anticholinergic BUSKOPANA® properties generally moderate also pass independently.

- accommodation disturbances, mydriasis, increase in intraocular pressure;

- tachycardia;

- increase in arterial pressure, dizziness, rush of blood;

- dryness in a mouth;

- dyshydrosis;

- the ischuria which is usually not expressed and is allowed independently is possible;

- an acute anaphylaxis, including a lethal outcome, anaphylactoid reactions, диспноэ, skin reactions (for example, urticaria, rash, reddenings and an itch) and other manifestations of hypersensitivity.

Interaction with other medicines:

БУСКОПАН® can strengthen anticholinergic action three - and tetracyclic antidepressants, antihistaminic and antipsychotic drugs, quinidine, an amantadin, Disopyramidum and other cholinolytics (for example, a tiotropiya, an ipratropiya, atropinopodobny connections).

Co-administration БУСКОПАНА® and antagonists of a dopamine, for example, of Metoclopramidum, leads to weakening of effect of both drugs on digestive tract.

БУСКОПАН® can strengthen the tachycardia caused beta адреномиметическими by means.

Contraindications:

- hypersensitivity to hyoscine to butylbromide or any other component of drug;

- closed-angle glaucoma;

- a prostate hypertrophy with an ischuria;

- mechanical stenoses in digestive tract;

- tachycardia;

- myasthenia;

- megacolon.

Contraindicated intramuscular introduction БУСКОПАНА® to the patients accepting anticoagulants because of probability of formation of intramuscular hematomas. In this case, БУСКОПАНА® it is necessary to enter subcutaneously or intravenously.

Overdose:

So far cases of overdose БУСКОПАНОМ® are not described therefore the following symptoms can be connected with its anticholinergic effect.

Symptoms: dryness in a mouth, erubescence, tachycardia, oppression of motility of a GIT, passing vision disorders, an ischuria.

Treatment: symptoms of overdose БУСКОПАНОМ® are stopped by parasimptomametika. Urgent consultation of the ophthalmologist is necessary for patients with glaucoma. Symptomatic means for maintenance of function cardiovascular and respiratory systems. At paralysis of respiratory muscles the intubation, artificial ventilation of the lungs is shown. In case of an ischuria catheterize a bladder.

Storage conditions:

To store at a temperature not above 25 °C. Not to freeze! To store in the place, safe, unavailable to children! Period of validity of 5 years.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in ampoules from colourless glass with two rings of green and white color ampoule break rings are higher. On ampoules paste the self-adhesive label. On 5 ampoules in a blister strip packaging from a film polyvinyl chloride. Planimetric packaging together with the instruction on a medical use in the state and Russian languages is put in a box from a cardboard.