- Composition
- Dosage form
- Basic physical and chemical properties:
- Pharmacological group
- Pharmacological properties
- Indications
- Contraindications
- Interaction with other drugs and other types of interactions
- Features of application
- Use during pregnancy or breastfeeding
- The ability to influence the reaction rate when driving vehicles or other mechanisms
- Directions for use and doses
- Children
- Overdose
- Adverse reactions
- Storage conditions
- Package
- Vacation category
Pharmacological properties of the drug Gastrocepin
Pirenzepine is a selective blocker of M1-cholinergic receptors of the parietal and main cells of the gastric mucosa, inhibits the production of hydrochloric acid and increases the pH of the stomach. In therapeutic doses it does not penetrate the BBB. Pharmacokinetics. Pirenzepine is not completely absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is determined 2–3 hours after administration. After oral administration, the average bioavailability is 10–20%. Concomitant use with food reduces the AUC value by 30%. Only 12% of pirenzepine is bound to plasma proteins. It penetrates poorly through the placental barrier and the blood-brain barrier, and is excreted into breast milk in minimal quantities. After oral administration, it is almost completely excreted in feces; when administered parenterally, it is excreted equally in urine and feces. Total plasma clearance is about 250 ml/min. Renal clearance is about half this value, which is approximately equivalent to the level of glomerular filtration. The drug is characterized by a long half-life (10–12 hours), which explains its long-lasting therapeutic effect. The pharmacokinetics of the drug does not change significantly in case of renal or hepatic failure. The apparent volume of distribution averages 14 L, which corresponds to the approximate volume of the extracellular space in humans.
Gastrozepin instructions for use
Composition active ingredient: pirenzepine;
1 tablet contains Pirenzepine dihydrochloride 25 mg
excipients: lactose monohydrate, corn starch; silicon dioxide colloidal magnesium stearate.
Dosage form
Pills.
Basic physical and chemical properties:
round, white tablets, flat on both sides, with beveled edges on one side of the tablet - a break line and the marking “61C” on both sides of the break line, on the other side of the tablet - the company symbol.
Pharmacological group
Drugs for the treatment of peptic ulcers and gastroesophageal reflux disease. ATX code A02B X03.
Pharmacological properties
Pharmacological.
Pirenzepine selectively blocks muscarinic receptors, reduces gastric acid production and increases gastric pH. In therapeutic doses, it does not penetrate the blood-brain barrier.
Pharmacokinetics.
Pirenzepine is not completely absorbed in the digestive tract. The average absolute bioavailability is only 10-20%.
When taking 50 mg of Pirenzepine half an hour before meals, peak plasma concentrations of approximately 30-35 ng/ml are achieved after 1-3 hours.
When taking Pirenzepine half an hour before meals or during meals, the area under the plasma concentration-time curve (AUC) is reduced by up to 30% compared to using the drug after an overnight fast.
Pirenzepine is weakly bound to plasma proteins (approximately 12%).
The volume of distribution averages 14 L, corresponding to the approximate human extracellular space.
Diffusion across the blood-brain barrier and placenta is minimal; It has been found that only minimal amounts of the drug pass into breast milk.
Pirenzepine is excreted almost entirely unchanged in the feces. The total clearance is approximately 250 ml/min. Renal clearance is approximately half this value, approximately equivalent to the glomerular filtration rate.
The half-life of Pirenzepine is from 10 to 12:00. The pharmacokinetics of pirenzepine are not significantly affected by hepatic impairment and mild or moderate renal impairment.
Indications
Ulcer of the stomach and duodenum.
Contraindications
Established hypersensitivity to any of the components of the drug.
Severe renal failure (creatinine clearance <20 ml/min).
Paralytic intestinal obstruction. Patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (see section "Peculiarities of use").
Interaction with other drugs and other types of interactions
Stimulation of gastric secretions induced by certain foods and medications (eg alcohol, caffeine) may be suppressed.
The simultaneous use of the drug Gastrocepin and H2 receptor blockers leads to a more pronounced decrease in the secretion of gastric acid.
With simultaneous use of Pirenzepine with anti-inflammatory drugs, the sensitivity of the digestive tract to these drugs improves and the anti-inflammatory effect does not change.
Features of application
Pirenzepine should be used with caution in patients with:
- closed-angle glaucoma;
- prostatic hypertrophy and urinary retention
- tachycardia.
The use of gastrocepin may mask the symptoms of stomach cancer and thereby delay the correct diagnosis. Therefore, before starting treatment for a stomach ulcer, it is necessary to conduct appropriate examinations to identify malignant diseases.
Patients with duodenal or gastric ulcers should be tested for Helicobacter pylori (HP) infection. If the presence of HP infection is confirmed, eradication therapy should be carried out, since successful implementation of this therapy usually also leads to healing of the ulcer.
Gastrocepin tablets contain 833.64 mg of lactose in the maximum recommended daily dose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug (see section “Contraindications”).
In patients with severe renal impairment (creatine clearance <30 ml/min), attention should be paid to the development of adverse reactions and the dose should be reduced if necessary.
If anticholinergic adverse reactions, such as visual disturbances or urinary retention, occur, gastrocepin treatment should be discontinued.
Use during pregnancy or breastfeeding
Information on the use of Pirenzepine in pregnant women is limited.
It has been established that pirenzepine passes into breast milk in very small quantities. As a result, anticholinergic effects may be observed in the breastfed baby.
The use of the drug should be avoided during pregnancy and breastfeeding.
No studies have been conducted on the effect on fertility.
The ability to influence the reaction rate when driving vehicles or other mechanisms
Studies on the ability to influence reaction speed when driving vehicles or working with other mechanisms have not been conducted.
During treatment with gastrocepin, side effects may occur, such as impaired accommodation, so this drug is recommended to be used with caution when driving vehicles or other mechanisms.
If patients experience accommodation disturbances, they should avoid driving or operating machinery.
Directions for use and doses
Unless otherwise prescribed, use 50 to 150 mg per day in divided doses. It is usually recommended to take 50 mg 2 times a day in the morning and evening (2 tablets in the morning and 2 tablets in the evening). Sometimes during the first 2-3 days of treatment it may be necessary to take an additional dose during the day. The tablets should be taken approximately 30 minutes before meals with a small amount of liquid. In case of rapid subjective improvement in the patient's condition, the course of treatment prescribed by the doctor should not be reduced or interrupted.
The duration of use of the drug should be from 4 to 6 weeks.
Children
Currently, there is no evidence of the safety and effectiveness of the use of Pirenzepine dihydrochloride in children.
Overdose
Symptoms When using large doses of Pirenzepine, anticholinergic effects may develop: increased body temperature, dryness and redness of the skin, dry mouth, dilated pupils, delirium, tachycardia, intestinal obstruction, urinary retention, reflex myoclonic movements, choreoathetosis. Therapy.
Hemodialysis, hemoperfusion, peritoneal dialysis, and repeated doses of activated charcoal are not effective in removing anticholinergic agents.
In case of severe intoxication (for example, hyperthermia, severe cases of delirium or tachycardia), physostigmine can be used intravenously in small doses.
In case of acute glaucoma, you must immediately seek help from a specialist and begin treatment with miotic drops.
Adverse reactions
According to the frequency of manifestations of adverse reactions, they are classified as follows: very often (≥ 1/10); often (≥ 1/100 to <1/10); uncommon (≥ 1/1000 to <1/100); rare (≥ 1/10,000 to <1/1000); very rare (≤1/10,000) unknown (cannot be determined from available data).
Classification by organ system | frequency |
From the immune system | |
anaphylactic reactions | unknown |
hypersensitivity | unknown |
From the nervous system | |
headache | often |
confusion | Very rarely |
From the organs of vision | |
disturbance of accommodation | often |
cardiac disorders | |
tachycardia | unknown |
From the digestive system | |
dry mouth | Often |
constipation | often |
diarrhea | often |
From the skin and subcutaneous tissue | |
rashes | often |
From the urinary system | |
urinary retention | infrequently |
Use of the drug Gastrocepin
tablets are prescribed orally at a dose of 50–150 mg/day in several doses. As a rule, 50 mg 2 times a day is recommended. Very rarely in the first 2-3 days of treatment there is a need to take an additional dose during the day. Take morning and evening 30 minutes before meals with a small amount of liquid. Continuous oral therapy must be carried out (even with rapid subjective improvement) for at least 4-6 weeks without reducing the dose of the drug. The injection solution is usually administered intramuscularly or intravenously, 2 ml (contents of 1 ampoule) at intervals of 12 hours. For the prevention and treatment of stress ulcers of the upper gastrointestinal tract, it is recommended to administer 2 ml of the solution 3 times a day at intervals 8 hours. For Zollinger-Ellison syndrome, the dose of the drug can be increased by 2 times; in especially severe cases, it is recommended to administer the contents of two ampoules (4 ml of solution 3 times a day). Parenteral administration of the drug for Zollinger-Ellison syndrome usually precedes surgery. Parenteral therapy with Gastrocepin should be carried out until clinical improvement (usually within 2-3 days), after which they switch to taking the oral form of the drug. Note. IV administration of the drug is carried out as a slow bolus (at least 3 minutes) or, preferably, by infusion (iv drip). For intravenous infusion, Gastrocepin injection solution can be diluted in isotonic sodium chloride solution, Ringer's solution, 5% levulose solution or 5% glucose solution.
Special instructions for the use of the drug Gastrocepin
The drug should be prescribed with caution for glaucoma and prostatic hypertrophy. During pregnancy and breastfeeding. Preclinical studies did not reveal any side effects of the drug, but the safety of its use during pregnancy has not been established. During this period, it is necessary to adhere to the usual precautions regarding the use of medications, especially in the first trimester of pregnancy. The active substance Gastrocepin passes into breast milk and as a result, an anticholinergic effect can be detected in a breastfed baby. IV injections should always be administered slowly due to the risk of thrombophlebitis due to the 39.2% propylene glycol content; patients with unstable blood circulation due to high initial blood pressure levels require constant monitoring. Impaired accommodation during treatment with the drug may reduce the ability to drive vehicles and operate potentially dangerous mechanisms.
Overdose of the drug Gastrocepin, symptoms and treatment
Symptoms: To date, there have been no reports of human overdose. However, when the drug is administered in high doses, anticholinergic effects are possible - dryness and hyperemia of the skin, a feeling of dryness of the oral mucosa, mydriasis, delirium, tachycardia, intestinal obstruction, urinary retention, reflex myoclonic movements, choreoathetosis. Treatment: despite the fact that experience in the treatment of pirenzepine overdose is very limited, in case of intoxication, general measures should be taken aimed at eliminating the unabsorbed substance in the digestive tract (gastric lavage, activated charcoal). Hemodialysis, hemoperfusion, and peritoneal dialysis are ineffective. In case of significant overdose, manifested by serious intoxication (hyperthermia, severe delirium and tachycardia), intravenous administration of physostigmine in low doses is indicated. If an attack of glaucoma develops, it is necessary to prescribe miotic drugs and consult a specialist.
Gastrocepin 25 mg tablets 50 pcs - Instructions
Compound
The main active substance is pirenzepine dihydrochloride.
Other ingredients: lactose, corn starch, magnesium stearate and silicon dioxide.
Release form
The drug is in the form of tablets placed in packages of 50 pieces each.
pharmachologic effect
Gastrocepin belongs to the category of dose-dependent anticholinergics. Pirenzepine acts in certain doses according to the instructions by blocking M1-cholinergic receptors (muscarinic receptors) in the gastrointestinal tract, thereby reducing the production of gastric juice, and its acidity is reduced by selectively suppressing the production of hydrochloric acid and pepsin. High doses of the drug may affect muscarinic receptors in other organs. Pirenzepine cannot cross the blood-brain barrier and the placenta when taken in doses not exceeding the maximum effective dose.
Has gastroprotector properties. Slightly reduces stomach motility.
Pharmacokinetics
When oral food is only partially absorbed from the intestine, it mainly acts locally on receptors in the mucous membrane of the gastrointestinal tract. The maximum concentration of the drug in the blood is observed half an hour after administration and 2-3 hours after ingestion. Bioavailability is approximately 20%.
It is excreted in urine and feces in its original form. The half-life of the drug is 10-11 hours.
Indications for use
The drug is intended for the treatment of patients with pathologies of the gastrointestinal tract, in whom the main condition for effective treatment is the protection of the mucous membrane of the digestive organs from the irritating effects of an acidic environment.
The main indications for use are peptic ulcers of the stomach and/or duodenum (treatment of acute and chronic pathologies), as well as gastroesophageal diseases.
In addition, the medication can be used to treat normal and gastritis, increased secretion of the stomach, duodenum, esophagitis, pylorospasm, inflammation of processes in the gastric mucosa with a tendency to bleeding.
Contraindications
The drug is not prescribed to people who cannot tolerate at least one of the components of the drug. It is prohibited to use the medicine in the treatment of patients with intestinal obstruction.
Oral forms of the drug are not used for galactose, lactase deficiency or impaired absorption of lactose in the intestine.
Side effects
During treatment, patients often complain of dryness of the oral mucosa. They often experience changes in stool (usually constipation, less often diarrhea), various skin rashes, migraine-like pain and housing disturbances. There is much less evidence of urinary retention in the body. Severe allergic reactions (Quincke's edema and anaphylactic shock) can develop only against the background of intolerance to individual components of the drug.
Side effects, such as urinary retention, visual disturbances, tachycardia and increased body temperature, require discontinuation of the drug and consultation with a doctor.
Compatibility with other medications
It is not recommended to take Gastrocepin in parallel with histamine H2 receptors. Medicines can enhance mutual action (synergism), which causes a significant decrease in the production of gastric juice and its acidity, which is fraught with digestive disorders.
The drug is also able to reduce the negative effect of anti-inflammatory drugs on the gastrointestinal mucosa, improving their tolerability.
Application and dosage
Tablets should be taken half an hour before meals.
The usual daily dose is 50 mg. In this case, tablets are taken 2 times a day (25 mg in the morning and 25 mg in the evening).
Sometimes in the first days of therapy, doctors prescribe additional medications at lunchtime.
In some cases, the dose may be increased to 150 mg. And then the daily dose can be divided into 3 or more doses.
The course of treatment can last from 1 to 1.5 months. During this time, the patient should take the medicine regularly, even if the illness has passed. Premature refusal to take the drug is fraught with a rapid return of unpleasant and dangerous symptoms.
Overdose
Exceeding the permissible dose is fraught with the development of some undesirable effects. The patient may be bothered by hot flashes, dry skin and oral mucosa, and vision problems. Taking the drug in high doses can cause redness of the skin, increased temperature and heart rate, urinary retention and intestinal obstruction, choreoathetosis and mydriasis. There may also be cramps of the facial muscles, drowsiness or vice versa, anxious and restless states, and delirious states.
When taking the drug orally, first aid is provided in the form of gastric lavage and activated charcoal.
special instructions
The medication should be used with caution in patients diagnosed with glaucoma or benign enlargement of the prostate gland, as well as in patients with an increased heart rate (tachycardia).
Use during pregnancy and breastfeeding
Use is not recommended.
Impact on the ability to drive vehicles and operate machinery
Due to the possible occurrence of such side effects as disturbance of accommodation during treatment, it is better to exercise caution when carrying out work that requires concentration and driving.
Terms of sale
As prescribed by a doctor.
Storage conditions
In a dry, cool place, with limited access for children.