Gastrocepin
Gastrocepin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Drug interactions
- 10. Analogs
- 11. Terms and conditions of storage
- 12. Terms of dispensing from pharmacies
- 13. Reviews
- 14. Price in pharmacies
Latin name: Gastrozepin
ATX code: A02BX03
Active ingredient: Pirenzepine (Pirenzepine)
Manufacturer: BOEHRINGER INGELHEIM INTERNATIONAL (Germany)
Description and photo update: 2019-12-08
Gastrocepin is a drug used in the treatment of gastric ulcer and duodenal ulcer.
Release form and composition
Gastrocepin is available in the following dosage forms:
- Tablets: round, flat, beige or white, with a beveled edge, on one side there is a risk and an embossed designation "61C" on both sides, the company logo is engraved on the other (10 pcs. In blisters, 2, 5, 10 blisters in a cardboard box);
- Solution for intramuscular and intravenous administration (2 ml in ampoules, 5 ampoules in blisters, 1 package in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: pirenzepine dihydrochloride (in the form of monohydrate) - 25 or 50 mg;
- Auxiliary components: lactose, corn starch, colloidal silicon dioxide (aerosil 200), magnesium stearate.
The composition of 1 ampoule (2 ml) contains the active substance: pirenzepine dihydrochloride - 10 mg.
Pharmacological properties
The drug reduces the acidity of gastric juice.
Pharmacodynamics
Pirenzepine - the active ingredient of Gastrocepin - has the ability to selectively block muscarinic receptors, reduce the secretion of gastric juice and increase the pH in the stomach. In recommended doses, the substance does not penetrate the blood-brain barrier.
Pharmacokinetics
Pirenzepine is not completely absorbed from the gastrointestinal tract. The approximate absolute oral bioavailability is only 10-20%. When Gastrocepin is taken at a dose of 50 mg 30 minutes before meals, the maximum concentration of pirenzepine in plasma, equal to 30–35 ng / ml, is observed 1–3 hours after taking the drug.
Taking the drug 30 minutes before a meal or simultaneously with it causes a decrease in the area under the concentration-time curve by 30% compared to the area recorded according to the results of taking after fasting at night. The volume of distribution of pirenzepine is approximately 14 liters, which, on average, coincides with the volume of the human extracellular space. The substance slightly binds to plasma proteins (no more than 12%).
Pirenzepine practically does not penetrate the placental and blood-brain barriers, and only a minimal amount of the drug is determined in breast milk. When taken orally, the drug is excreted mainly in the faeces, mainly unchanged. The total plasma clearance is approximately 250 ml / min. Renal clearance is approximately 125 ml / min, which is the same as glomerular filtration rate. The average half-life of pirenzepine from the body is 10-12 hours. Its pharmacokinetics are not significantly affected by renal (mild and moderate) or hepatic impairment.
Indications for use
- Peptic ulcer of the stomach and duodenum;
- Acute gastric ulcer and duodenal ulcer.
Contraindications
- Paralytic ileus;
- Hypersensitivity to drug components.
Patients with galactose intolerance (lactase deficiency, galactosemia or impaired absorption of glucose-galactose in the intestine) should not use Gastrocepin in tablet form, since the maximum recommended daily dose contains 833.64 mg of lactose.
The drug should be used with caution in patients with glaucoma, tachycardia and benign prostatic hyperplasia.
Instructions for the use of Gastrocepin: method and dosage
The tablets should be taken before meals (about half an hour) with a small amount of liquid. In cases where there are no other instructions from the doctor, the drug is taken in a daily dose of 50-150 mg, divided into several doses. The usual dosage regimen is 50 mg 2 times a day (in the morning and evening).
In some cases, in the first few days of therapy, it may be necessary to take an additional dose of Gastrocepin in the middle of the day. If the patient subjectively feels a rapid improvement in the condition, it is impossible to reduce the dose taken or the frequency of use of the drug without consulting the doctor.
The average duration of therapy is 1-1.5 months.
The solution for injection is administered intramuscularly or intravenously (slowly over 3 minutes or by drip) for 2-3 days, 10 mg at intervals of 12 hours. For the treatment and prevention of stress ulcers, the recommended dose is 10 mg 3 times a day (every 8 hours). In the treatment of Zollinger-Ellison syndrome, the dose can be doubled; in severe cases, it is possible to use 20 mg 3 times a day.
For intravenous infusion, the injection solution can be mixed with Ringer's solution, isotonic sodium chloride solution, 5% glucose or fructose solution under visual control (no precipitation, turbidity or color change of the solution). The prepared infusion solution should be used within 12 hours if stored at room temperature.
Side effects
During therapy, the development of such side effects as: accommodation disturbances, dry mouth, tachycardia, diarrhea, constipation, headache, urinary retention are possible.
There have also been reports of anaphylactic shock and allergic reactions.
Overdose
To date, there is no information on cases of acute overdose. However, with oral administration of significant doses of pirenzepine, the following anticholinergic effects may occur: athetosis, chorea, muscle twitching, mydriasis, dry mouth, dryness and flushing of the skin, urinary retention, intestinal obstruction, tachycardia, delirium.
Clinical experience in the treatment of Gastrocepin overdose is rather small. In case of poisoning with large doses of pirenzepine taken orally, therapy should be started with general measures (for example, gastric lavage and taking activated charcoal). Peritoneal dialysis, hemodialysis, re-administration of activated charcoal, and blood transfusion do not eliminate pirenzepine from the body. In cases of acute intoxication, accompanied by tachycardia, delirium, or fever, intravenous administration of physostigmine in a small dose is recommended. With the development of an acute attack of glaucoma, it is necessary to use drugs that have an m-cholinomimetic effect (for example, pilocarpine in the form of eye drops), and urgently seek medical advice.
special instructions
Lactating and pregnant women Gastrocepin should be taken only if the expected benefit from therapy to the mother outweighs the potential risk to the newborn or fetus.
Patients with glaucoma are advised to periodically measure intraocular pressure.
Due to impaired accommodation and vision, the ability to drive vehicles and machinery may be impaired.
Drug interactions
The simultaneous use of Gastrocepin with blockers of H2-histamine receptors may be accompanied by a more pronounced decrease in the secretion of hydrochloric acid in the stomach.
According to the instructions, Gastrocepin in combination with anti-inflammatory drugs does not reduce their effect, but improves their tolerance.
Analogs
Analogues of Gastrocepin are: Gaviscon, Gastal, Gastrozem, Gastro-Norm, Vikair, Venter, De-Nol, Pyrene, Rabiril.
Terms and conditions of storage
Store in a dry place out of reach of children at temperatures up to 25 ° C. The solution must not be frozen.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Gastrocepin
According to reviews, Gastrocepin quickly and effectively improves the condition of most patients. Symptoms accompanying gastrointestinal diseases disappear quickly enough. No clinically significant side effects have been reported.
Price for Gastrocepin in pharmacies
The price of Gastrocepin 25 mg tablets is about 430-520 rubles (the package includes 50 pcs.). The solution for intravenous and intramuscular administration is currently not available in pharmacies.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
