Gastrotsepin® (Gastrozepin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePyrenzepinePyrenzepine
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  • Gastrotsepin®
    pills inwards 
    Boehringer Ingelheim International GmbH     Germany
    • Dosage form: & nbsppills
    Composition:

    1 tablet contains active substance pirenzepine dihydrochloride monohydrate (based on the anhydrous substance of pyrenzepine dihydrochloride): 25 mg.

    Excipients: lactose 138.94 mg; corn starch 72.00 mg; silicon dioxide colloid (Aerosil 200) 10.00 mg; magnesium stearate 3.00 mg.

    Description:

    Round, flat on both sides, white or beige tablets with bevelled edge. On one side of the risk pill, on both sides of the risk is engraved "61C", on the other side of the tablet is engraved the sign of the firm.

    Pharmacotherapeutic group:M-holinoblokator
    ATX: & nbsp

    A.02.B.X.03   Pyrenzepine

    Pharmacodynamics:

    Pirenzepine selectively blocks muscarinic receptors, reduces the formation of gastric juice and increases pH in the stomach. In therapeutic doses, the drug does not penetrate the blood-brain barrier.

    Pharmacokinetics:

    Pyrenzepine is not completely absorbed from the gastrointestinal tract. The average absolute bioavailability with oral administration is only 10-20%. When taking 50 mg of pyrenesin at 3 minutes before meals, the maximum concentration in the plasma with a value of 30-35 ng / ml is noted 1-3 hours after taking the drug.

    Taking pirenzepine for 30 minutes or simultaneously with food leads to a decrease in the area under the concentration-time curve by 30%, compared to the area observed by the results of the reception after nighttime fasting. The volume of distribution of the main substance is about 14 liters, which roughly corresponds to the volume of the extracellular space of man. Pyrenzepine only to a small extent binds to plasma proteins (about 12%).

    Pirenzepine almost does not penetrate the blood-brain and placental barriers, and only a minimal amount of the drug is found in the milk of a nursing woman. For oral administration pirenzepine is excreted mainly with feces, mainly in unchanged form. The total plasma clearance is about 250 ml / min. Kidney clearance is approximately half this value, which corresponds to the level of glomerular filtration. Pyrenzepine is excreted from the body with an average half-life of 10-12 hours. The pharmacokinetics of pirenzepine are not significantly affected by either hepatic or renal (from mild to moderate) failure.

    Indications:

    Acute ulcer of the stomach and duodenum; peptic ulcer of the stomach and duodenum.

    Contraindications:
    • Hypersensitivity to any of the components of the drug, paralytic ileus in the patient.
    • Pregnancy, lactation.
    • The maximum recommended daily dose contains 833.64 mg of lactose. Patients with an existing intolerance to galactose (galactoseemia, lactase deficiency, or impaired absorption of glucose-galactose in the intestine) should not use this drug.
    • Children under 18 years of age (no studies on efficacy and safety for this group of patients).
    Carefully:

    Gastrotsepin should be used with caution in patients with glaucoma, benign prostatic hyperplasia, tachycardia.

    Pregnancy and lactation:

    Information on the results of the use of pirenzepine by pregnant women is not enough. There is evidence that pirenzepine is excreted in breast milk in small concentrations. As a result, in infants at the breastfeeding stage, anticholinergic effects can be observed. There were no studies of the effect of the drug on human fertility.

    Dosing and Administration:

    Tablets should be taken about half an hour before meals, washed down with a small amount of liquid.

    If the doctor is not prescribed otherwise, you should take the drug 50-150 mg / day, divided into several receptions.

    Usual dosing regimen: 50 mg twice daily, morning and evening. Sometimes in the first 2-3 days of treatment, an additional dose of the drug may be needed in the middle of the day.

    Despite the rapid subjective improvement of the condition, the patient should not reduce the dose of the drug or refuse to take the drug, if it is not recommended by the doctor.

    Treatment should be continued for 4-6 weeks.

    Side effects:

    From the immune system: anaphylactic reactions, hypersensitivity.

    From the nervous system: headache.

    From the side of the organ of vision: violation of accommodation.

    From the cardiovascular system: tachycardia.

    From the digestive system: dry mouth, constipation, diarrhea.

    From the skin and subcutaneous tissues: rash.

    From the urinary system: retention of urine.

    Overdose:

    Symptoms

    When ingested large doses of pyrenzepine may develop the following anticholinergic effects: dryness andhyperemia of the skin; dry mouth; mydriasis; delirium; tachycardia; paralytic ileus; retention of urine; myoclonic jerking of the muscles; involuntary chorionic-athetotic movements.

    Treatment

    Hemodialysis, hemoperfusion, peritoneal dialysis and re-administration of activated charcoal do not contribute to the removal of pirenzepine from the body.

    In cases of severe intoxication (with fever, delirium or severe tachycardia), physostigmine can be administered in a small dose intravenously.

    In case of development of an acute attack of glaucoma, drugs that exert a mholinomimetic effect (pilocarpine in the form of eye drops) and immediately consult a specialist for advice.

    Interaction:

    Simultaneous administration of gastrotsepin and H2-histamine receptor blockers is accompanied by a more pronounced decrease in the secretion of hydrochloric acid in the stomach.

    Gastrotsepin, used in combination with anti-inflammatory drugs, does not reduce their anti-inflammatory effect and improves their tolerability.

    Special instructions:

    Patients with glaucoma are advised to periodically measure intraocular pressure.

    Effect on the ability to drive transp. cf.and fur:

    Special clinical studies of the effect of the drug on the ability to control the car and mechanisms were not carried out. However, when driving and working with machinery, one should take into account the possibility of a violation of accommodation. In such cases, you should refuse to drive or work with machinery.

    Form release / dosage:

    Tablets 25 mg.

    Packaging:

    For 10 tablets in a blister of PVC / aluminum foil. For 2, 5 or 10 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    Store in a dry place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years. Do not use after the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014527 / 01
    Date of registration:16.10.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:Boehringer Ingelheim International GmbHBoehringer Ingelheim International GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspBERINGER INGELCHAIM INTERNATIONAL GmbH BERINGER INGELCHAIM INTERNATIONAL GmbH Germany
    Information update date: & nbsp16.03.2017
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