Pirenzepine-Ratiopharm

Instructions for use

The manufacturer provides a description of the composition of the medication, describes the principle of its action on the digestive system, and indicates possible side effects. Additionally, the instructions provide a list of pathological conditions that are contraindications for taking the drug. Only a doctor can change the dosage and duration of the course based on data about the patient’s diseases.

pharmachologic effect

Its main properties:

• 
  After oral administration, pirenzepine is poorly absorbed from the gastrointestinal tract. Manifestation of peripheral anticholinergic action;

• Reduces basal and stimulated secretion of hydrochloric acid;
• Reduces peptic activity of gastric juice;
• Reduces the tone of smooth gastric muscles;
• Inhibits the release of bicarbonate from the epithelium into the lumen of the stomach in patients with erosive lesions of the antrum;
• Increases protection of the gastric mucosa;
• Increases blood flow in the submucosal layer of the stomach and intestines;
• Improves microcirculation.

The medication does not affect the activity of the central nervous system. The heart rate also remains unchanged.

The drug is difficult to remove from the gastrointestinal tract. “Pirenzepine” also has difficulty coping with the blood-brain barrier.

The half-life of the drug takes from 10 to 12 hours. Approximately 10% of the substance (in its original form) is excreted in the urine, most of it is excreted in the feces.

Indications for use

Doctors recommend using Pirenzepine if you have these diseases:

• Gastric ulcer (acute periods, chronic course);
• Duodenal ulcer (acute and chronic stage);
• Pylorospasm;
• Duodenitis;
• Esophagitis;
• Stress ulcers of the gastrointestinal tract;
• Zollinger-Ellison syndrome;
• Ulcerative bleeding;
• Erosive lesions of the gastrointestinal tract.

Mode of application

Tablets of 0.025 and 0.05 g - 50 pcs in a package. The full dosage per day is from 50 mg to 150 mg. The average dose should consist of 50 mg of medication. The drug is taken twice a day half an hour before the main meal.

The duration of treatment recommended by experts is from a month to 1.5 months. Interruptions in therapy are not allowed.

The drug in ampoules is administered both intramuscularly and intravenously. Injections are given twice a day. A single dosage is 2 ml. In case of severe gastric and duodenal ulcers, the patient is administered 10 mg of the drug every 8 or 12 hours.

Release form

There are 2 forms of drug release:

• Tablets 25 mg;
• Ampoules (2 ml) with 10 mg injection solution.

Compound

The basis of the drug is:

• pirenzepine;
• silicon dioxide;
• corn starch;
• lactose;
• magnesium stearate.

The drug reduces basal and stimulated secretion of hydrochloric acid. Reduces peptic activity of gastric juice.

Interaction with other drugs

Using Pirenzepine together with other drugs can cause the following effects:

• with anticholinergic drugs - increased anticholinergic effect, the appearance of paralytic intestinal obstruction;
• with opioid analgesics - a high probability of constipation or urinary retention;
• with Metoclopramide - reducing the impact of the latter on the motor activity of the gastrointestinal tract;
• with "Cimetidine" - an increase in the therapeutic effect of the latter;
• with NSAIDs – do not affect each other;
• with histamine receptor blockers - both enhance the antisecretory effect;
• with “Ketoconazole”, “Doxycycline” - decreased absorption and therapeutic effect;
• with antacids and adsorbents - the absorption of Pirenzepine is reduced.

Pirenzepine

Pirenzepine

(lat.
pirenzepine
) - antiulcer, gastroprotective agent, M1-cholinergic receptor blocker.
pirenzepine
in Russian scientific literature . Pirenzepine is the international nonproprietary name (INN) of the drug. According to the pharmacological index, pirenzepine belongs to the group “M-anticholinergics”, according to ATC - to the group “A02BX Other antiulcer drugs and drugs for the treatment of gastroesophageal reflux” and has the code A02BX03.

Comparison of pirenzipine with other anticholinergics

Anticholinergics are the earliest, but currently little popular group of antisecretory drugs.
For many years, atropine was the main drug in the treatment of acid-related diseases, but many side effects have led to the search for new drugs. The result of the research was pirenzepine, a selective antagonist of M1-cholinergic receptors, which does not affect the cholinergic receptors of smooth muscles and the heart, thereby reducing the incidence of side effects. Pirenzepine selectively inhibits the production of hydrochloric acid and pepsin in the stomach, improves blood flow in its mucous membrane, and stimulates mucus formation. If atropine and its related platyphylline are non-selective M-cholinergic drugs, i.e. they block both M1 and M2 cholinergic receptors, then pirenzepine is a selective antagonist of M1 cholinergic receptors. It selectively inhibits the secretion of acid and pepsin under the control of the vagus nerve, suppressing gastric secretion in humans caused by false feeding, distension of the gastric fundus and peptone, without affecting gastric emptying and cardiac activity.

Atropine in patients with peptic ulcer causes a marked increase in the concentration of gastrin in the blood, while pirenzepine significantly reduces it during the gastric phase of digestion induced by distension of the gastric fundus or peptone.

M1 anticholinergics have generally low antisecretory activity, but may be indicated for moderately increased gastric secretion, especially in the case of vagotonia. An important feature of selective anticholinergics is that, unlike non-selective ones, they do not cause hypergastrinemia.

Indications for use of pirenzepine

• treatment and prevention of gastric and duodenal ulcers, chronic hyperacid reflux esophagitis
• erosive and ulcerative lesions of the digestive tract, including those caused by antirheumatic and anti-inflammatory drugs
• digestive tract stress ulcers
• Zollinger-Ellison syndrome
• bleeding from erosions and ulcerations in the upper digestive tract

Method of administration of pirenzepine and dose

Pirenzepine is taken orally or administered intravenously or intramuscularly.
When taken orally - 50 mg of pirenzepine in the morning and evening, half an hour before meals, with a small amount of water. Duration of treatment is from 4 to 8 weeks. For severe forms of gastric and duodenal ulcers, pirenzepine is administered intravenously or intramuscularly at 10 mg every 8–12 hours.

The maximum daily dose of pirenzepine when taken orally is 200 mg.

Use of pirenzepine during pregnancy and lactation

Pirenzepine is not recommended to be taken during pregnancy. During breastfeeding, pirenzepine is excreted in small quantities into breast milk.

Professional medical publications regarding the use of pirenzepine

• Loschakova O.Yu. Rationale and evaluation of the effectiveness of the combined use of pirenzepine and misoprostol in the treatment of gastropathy induced by NSAIDs. Abstract of dissertation. PhD, 14.00.05 - internal diseases. IzhSMA, Izhevsk, 2008.

• Rapoport S.I., Lakshin A.A., Rakitin B.V., Trifonov M.M. pH-metry of the esophagus and stomach in diseases of the upper digestive tract. / Ed. Academician of the Russian Academy of Medical Sciences F.I. Komarova. – M.: ID MEDPRACTIKA-M. – 2005. – 208 p. / Ch. 9.1. Drug correction of acid-dependent conditions.

Trade names of drugs with the active ingredient pirenzepine:
Gastrozem, Gastrozepin, Piren.

There are contraindications, side effects and application features; consultation with a specialist is necessary. Back to section

Side effects

Undesirable consequences of taking Pirenzepine can affect the following organ systems:

• Digestive system: dry mouth is bothersome, appetite increases, constipation occurs, or bowel movements become more frequent;
• Visual system: accommodation is impaired, mydriasis, the sensitivity of the visual organs to light increases;
• Excretory system: urinary retention, decreased sweating;
• Cardiovascular system: tachycardia;
• Immune system: allergic manifestations;
• Nervous system: headaches.

Overdose

Exceeding the dosage of the drug prescribed by a specialist or indicated in the instructions may cause deviations in the operation of some systems. The degree of intensity of side symptoms depends on the body’s sensitivity to the components of its composition and some individual characteristics of the patient’s health status.

Long-term overdoses lead to serious pathological processes, which require a visit to a specialist to eliminate them.

An overdose can provoke the following pathological conditions:

• tachycardia and other heart rhythm disorders;
• hallucinations, changes in consciousness and excessive weakness of the body;
• muscle weakness and convulsions of varying degrees of intensity;
• increased dryness of the mucous membranes in the mouth and sinuses (the symptom may be accompanied by discomfort in the eyes and sore throat);
• breathing problems (from difficulty breathing and shortness of breath to asthma-like attacks);
• increased body temperature;
• deterioration of vision (with regular overdose and hypersensitivity to the drug).

Contraindications

It is strictly forbidden for people with the following pathological conditions to take the drug:

• Individual hypersensitivity to individual components of the drug;
• Prostatic hyperplasia;
• Pyloric stenosis;
• Paralytic intestinal obstruction.

If these diseases are present, the medication is taken as prescribed and under the supervision of the attending physician:

• Glaucoma;
• Tachycardia;
• Kidney and liver failure (due to difficulty removing the drug);
• Intestinal atony (in elderly patients);
• Chronic lung diseases in children (plugs may form in the lumen of the bronchi due to the thicker consistency of the secretion);
• Chronic heart failure;
• Mitral stenosis;
• Atrial fibrillation;
• Arterial hypertension;
• Cardiac ischemia;
• Thyrotoxicosis;
• Acute bleeding.

During pregnancy

The product is not recommended for use by women in the 1st trimester of pregnancy.

In the second and third trimester, it can be used in pregnant women if the benefits of its use are higher than the likely risks for the unborn baby.

During the lactation period, Pirenzepine is also not recommended for use by young mothers , since it can pass into breast milk in small quantities. It is also necessary to take into account the fact that the medicine can worsen lactation.

• If you have any symptoms of the disease, you should immediately consult a doctor. You can view a list of gastroenterology clinics on our website
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Use of the drug Pirenzepine

Orally, 50–150 mg per day is prescribed (usually at a dose of 50 mg) with a small amount of liquid in the morning and evening 30 minutes before meals. In rare cases, during the first 2–3 days of treatment, it may be necessary to take an additional dose during the day. Continuous oral therapy should be carried out (even in the case of rapid subjective improvement) for at least 4–6 weeks without dose reduction. 0.5% solution is usually administered intramuscularly or intravenously, 2 ml at an interval of 12 hours. For the prevention and treatment of “stress” ulcers of the upper gastrointestinal tract, it is recommended to administer 2 ml of solution 3 times a day at an interval of 8 h. For Zollinger-Ellison syndrome, the dose can be increased 2 times (4 ml of 0.5% solution 3 times a day). Parenteral administration for Zollinger-Ellison syndrome usually precedes surgery. Parenterally administered until clinical improvement (usually within 2-3 days), after which pirenzepine is prescribed orally. IV is administered as a slow bolus (over at least 3 minutes) or, preferably, as an IV drip. For intravenous infusion, pirenzepine can be diluted in isotonic sodium chloride solution, Ringer's solution, 5% levulose solution or 5% glucose solution.

special instructions

Impact on the ability to drive vehicles and operate machinery

Caution is advised. Pirenzepine can provoke increased sensitivity of the body to the drug and a slowdown in the speed of some mental reactions.

Pregnancy and lactation

It is not recommended to take Pirenzepine during pregnancy. Pirenzepine is not prescribed in the first trimester of pregnancy. At later stages, the decision to prescribe the drug should be made by the doctor (the potential benefit to the woman must outweigh the risk to the fetus). The ability of the drug to pass into breast milk causes a ban on its use during lactation.

Use in childhood

In pediatric practice, Pirenzepine is used only in case of emergency. The drug should not be taken by children with chronic diseases of the respiratory and nervous systems, as well as the brain. If a child has symptoms of body weakness, the medication should not be prescribed. The decision to use Pirenzepine in pediatric practice should be made by a pediatrician.

If kidney function is impaired

Pathologies associated with impaired renal function increase the risk of side effects (the drug is used with caution).

In case of liver dysfunction

The drug is used with caution in cases of serious pathological processes in the liver (liver failure).

Conditions for dispensing from pharmacies

Pirenzepine can be purchased at pharmacies only with a prescription.

Storage conditions and periods

The storage location should be at room temperature and protected from moisture. The shelf life is 5 years.

All gastroenterology clinics and medical centers in your city. Tests and ultrasound. Consultation with a gastroenterologist. Diseases of the digestive system. Find out more: - In Kiev (Hertz, Ilaya, Euromed) - In St. Petersburg (SM-Clinic, Longevity, Allergomed, Doctor +, BaltZdrav, Professor) - In Moscow (SM-Clinic, Medlux, Onmed) - In Kharkov ( TsMEI, Olympic, Victoria, Fortis, Ecomed) - In Minsk (Belgirudo, Art-Med-Company, Sinlab, Mikosha, GrandMedica, MedClinic) - in Odessa (Medea, On Clinic, Into Sano, Venus) - In Razyan (Trust + , Polyclinic-Pesochnya, Evrikas +) - in Nizhny Novgorod (Only Clinic, Alpha Center, EuroClinic, SOLO, Altea) - gastroenterological clinics of Tyumen (Doctor A+, Clinic "Vera", Avicenna, Medis, Sibirina, Your Doctor)

Reviews

You can read patient reviews about the drug "Pirenzepine" at the end of this article.

According to the majority of patients who have personally tried to use Pirenzepine, the drug effectively eliminates heartburn and helps cope with pain in acute peptic ulcers of the stomach and duodenum, and gastritis.

Patients used the drug both in the acute period of the disease and as a prophylactic agent to consolidate the therapeutic effect. However, you should not abuse the drug, because it also has its side properties.

So, some of the most common side effects are: dry mouth , temporary digestive problems, headache. The average duration of the course of taking the drug is at least 30 calendar days.

Pharmacological properties of the drug Pirenzepine

A specific inhibitor of gastric secretion, a selective blocker of M1-cholinergic receptors of parietal and main cells of the gastric mucosa. Inhibits the production of hydrochloric (hydrochloric) acid and pepsin without disturbing the physiological functions of the digestive tract. It has pronounced hydrophilic properties, and therefore does not penetrate the BBB in clinically significant quantities and, unlike most tricyclic compounds, does not have a central effect. It is characterized by a long half-life (10–12 hours), which explains its long-lasting therapeutic effect; It is characterized by rapid development of effect in hyperacid conditions (a few hours from the start of treatment) and good tolerability.