Бускопан®

General characteristics. Structure:

Active ingredient: 10 mg of hyoscine of butylbromide.

Excipients: calcium hydrogen phosphate anhydrous (calcium hydrophosphate), the starch which corn is dried up, starch soluble { the potato starch hydrolyzed), silicon dioxide colloid, tartaric acid, stearic acid. Cover: povidone (polyvinylpirrolidone), sucrose, talc, gum Arabian (acacias gum), titanium dioxide, macrogoal 6000 (polyethyleneglycol), wax of karnaubskiya, wax white (white beeswax).

The drug having local spasmolytic effect on smooth muscles of internals.

Pharmacological properties:

Pharmacodynamics. Has local spasmolytic effect on smooth muscles of internals (digestive tract, biliary tract, urinary tract), reduces secretion of digestive glands. Local spasmolytic action is explained by ganglioblokiruyushchy and antimuskarinovy activity of the drug Being to quarternary ammonium derivatives, hyoscine butylbromide does not get through a blood-brain barrier therefore anticholinergic influence on TsNS is absent.

Pharmacokinetics. Being quarternary ammonium derivatives and having high polarity, hyoscine butylbromide is slightly soaked up in digestive tract. After use inside absorption of drug makes 8%. Average absolute bioavailability makes less than 1%. After single use of hyoscine of butylbromide inside in doses of 20-400 mg average peak concentration in plasma were reached approximately in 2 hours and made from 0,11 to 2,04 ng/ml. Hyoscine butylbromide owing to high affinity to muskarinovy and nicotinic receptors is distributed mainly in muscle cells of abdominal organs and a small pelvis, and also in intramural gangliya of abdominal organs. Communication with proteins of plasma (albumine) — low also makes about 4,4%. It is established that drug (in concentration of 1 mmol) in vitro interacts with sincaline transport (1,4 nmol) in epithelial cells of a human placenta.

The terminal elimination half-life of drug after single use inside in doses of 100-400 mg fluctuated from 6,2 to 10,6 hours. Metabolism is carried out generally by hydrolysis of radio communication. After intake excretion of drug happens to a stake and urine. After drug use inside: renal elimination makes from 2 to 5%, elimination through intestines - 90%. Renal excretion of metabolites of hyoscine of butylbromide makes less than 0,1% of dose size. After administration of drug inside in doses of 100-400 mg average sizes of clearance make from 881 to 1420 l/min., whereas the corresponding volumes of distribution for the same range of doses vary from 6,13 to 11,3 x 105 l that can speak low system bioavailability.

The metabolites which are excreted with urine poorly contact muskarinovy receptors therefore they are not active and do not possess pharmacological to properties

Indications to use:

Renal colic, bilious colic, spastic dyskinesia of biliary tract and gall bladder, cholecystitis, intestinal colic, пилороспаэм, a peptic ulcer of a stomach and duodenum in an aggravation phase (as a part of complex therapy }, альгодисменорея.

Route of administration and doses:

If the doctor it is not appointed differently, it is recommended to use the following dosages: adults and children are more senior than 6 years: on 1 - 2 tablets of 3-5 times a day, washing down with water. Drug should not be used daily more than 3 days without consultation of the doctor.

Features of use:

Influences on ability to control of motor transport and to use of mechanisms. Researches about influence of drug on ability to driving of motor transport and to control of mechanisms were not conducted.

Fertility, pregnancy and lactation. Data on use of drug at pregnancy and about penetration of drug and its metabolites into breast milk are limited. Researches about influence of drug on fertility were not conducted. As a precautionary measure use of drug during pregnancy and in the period of a lactation is not recommended.

Side effects:

Many of the listed undesirable effects can be connected with anticholinergic properties of drug. Anticholinergic side effects are usually expressed poorly and pass independently.

From immune system: acute anaphylaxis, anaphylactic reactions, asthma, skin reactions (for example, urticaria, rash, erythema, itch) and other manifestations of hypersensitivity.

From cardiovascular system: tachycardia.

From the alimentary system: dryness in a mouth.

From skin and hypodermic fabrics: disgidrotichesky eczema.

From an urinary system: ischuria.

Interaction with other medicines:

Buskopan can strengthen anticholinergic effect of tricyclic and tetracyclic antidepressants, antihistaminic, antipsychotic drugs, quinidine, an amantadin and Disopyramidum and anticholinergic drugs (for example, a bromide tiotropiya, an ipratropiya of bromide, atropinopodobny connections).

Simultaneous use of a buskopan and antagonists of dopamine, for example, of Metoclopramidum, leads to weakening of effect of both drugs on digestive tract.

Buskopan can strengthen the tachycardia caused by beta and adrenergic means.

Contraindications:

- Hypersensitivity to hyoscine to butylbromide or any other component of drug. Myasthenia гравис, megacolon.
- Children up to 6 years.
- Pregnancy, lactation period.

The tablet of a buskopan contains 41,2 mg of sucrose. Most recommended daily dose (10 tablets) contains 411,8 mg of sucrose. Patients with rare inherited disorders (intolerance of fructose), such as malabsorption of glucose galactose or insufficiency of invertase-isomaltase, should not accept drug.

With care. It is necessary to appoint with care drug in the following clinical situations: suspicion on intestinal impassability (including a pyloric stenosis); obstruction of urinary tract (including benign hyperplasia of a prostate), tachyarrhythmias (including ciliary tachyarrhythmia), closed-angle glaucoma.

When the abdominal pain of an unknown origin proceeds or amplifies or when such symptoms as fever, nausea, vomiting are at the same time noted, change of a consistence a calla and frequencies of defecations, sensitivity of a stomach, a lowering of arterial pressure, a faint or blood in Calais, it is necessary to address for medical consultation immediately.

Overdose:

So far cases of overdose of BUSKOPANOM are not described therefore the following symptoms and recommendations have theoretical character.

Symptoms. Anticholinergic symptoms are possible: an ischuria, dryness in a mouth, erubescence, tachycardia, oppression of motility of digestive tract, and also passing vision disorders.

Treatment. It is necessary to carry out a gastric lavage with absorbent carbon and then from 15% magnesium sulfate. Symptoms of overdose of BUSKOPANOM are stopped by cholinomimetics. To patients with glaucoma appoint Pilocarpinum in the form of eye drops. If necessary cholinomimetics enter systemically, for example, неостигмин 0,5 - 2,5 mg intramusculary or intravenously. Cardiovascular complications treat according to usual therapeutic rules. At paralysis of respiratory muscles the intubation, artificial ventilation of the lungs is shown. In case of an ischuria catheterize a bladder. The maintenance therapy is carried out.

Storage conditions:

At a temperature not over 25 to °s.khranit and the place, safe, unavailable to children! Period of validity of 5 years. Not to use after expiry date.

Issue conditions:

Without recipe

Packaging:

Tablets, coated 10 mg. On 10 or 20 tablets in a blister strip packaging (blister) from PVH/A1 foil, 1 ip 2 blisters with the application instruction in a cardboard pack