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Gastrotsepin
Last reviewed: 01.06.2018
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Gastrotsepin - one of the effective drugs used in gastroenterology for the treatment of various diseases of the gastrointestinal tract, including those prone to bleeding. In most cases, it is prescribed as a first-line drug, which prevents the transition of the disease to a more severe stage.
Indications of the gastrotsepina
The drug is intended for the therapy of patients with gastrointestinal pathologies, in which the main condition for effective treatment is the protection of the mucous membrane of the digestive organs from the irritating effect of the acidic medium.
The main indications for the use of the drug are gastric ulcer and / or duodenal ulcer (treatment of acute and chronic pathology), as well as gastroesophageal flux disease.
In addition, the drug can be used to treat gastritis with normal and increased secretory function of the stomach, duodenitis, esophagitis, pilorospasm, erosive processes on the gastric mucosa prone to bleeding.
Release form
The drug "Gastrotsepin" can be found on the drugstore shelves in the form of tablets and a solution for injections. The main active substance in both cases is pigenzepine dihydrochloride (benzodiazepine derivative, which is a blocker of M 1 -cholinoreceptors).
Tablets containing 25 or 50 mg of pirenzepine dihydrochloride have a circular shape and a beige hue typical of tablets. On one plane of the tablet there is a risk for the fracture, on both sides of which the engraving "61C" is seen. Another plane of the tablet is decorated with an engraved logo of the manufacturer.
Auxiliary components of the drug in the form of tablets are lactose, corn starch, magnesium stearate and silicon dioxide.
Tablets are packaged in blisters of 10 pieces. The carton pack of the preparation can contain 2, 5 or 10 blisters (20.50 or 100 tablets). This information is reflected on the outside of the package.
The injectable colorless solution is packaged in cardboard packages of 5 ampoules. Each ampoule contains 2 ml of a solution in which we find more than 10 mg of pyrenesin and additional components in the composition of chloride and sodium acetate, propylene glycol, trihydrate, acetic acid, water for injection.
Pharmacodynamics
Gastrotsepin belongs to the category of dose-dependent anticholinergic drugs. The action of pirenzepine in prescribed doses is associated with blockade of M 1 -cholinoreceptors (muscarinic receptors) of the gastrointestinal tract, as a result of which the production of gastric juice decreases and its acidity decreases due to selective inhibition of the production of pepsin and hydrochloric acid. High doses of the drug may affect the muscarinic receptors of other organs. Pirenzepine is not able to pass through the blood-brain and placental barriers, if it is taken in doses that do not exceed the maximum effective.
Has the properties of a gastroprotector. Slightly reduces the motility of the stomach.
[6], [7], [8], [9], [10], [11], [12], [13], [14], [15], [16], [17], [18], [19]
Pharmacokinetics
When oral intake is absorbed from the intestine only partially, mainly acting locally on the receptors of the mucosa of the gastrointestinal tract. The maximum concentration of the drug in the blood is observed after half an hour with an injection, and after 2-3 hours with oral administration. Bioavailability is about 20%.
It is excreted in urine and feces in its original form. The half-life of the drug is within 10-11 hours.
[20], [21], [22], [23], [24], [25], [26], [27], [28], [29], [30], [31], [32], [33]
Use of the gastrotsepina during pregnancy
In connection with the insufficient study of the effect of the drug on the fetus, the use of "gastrotsepin" during pregnancy is considered undesirable.
A small amount of pirenzepine can enter the breast milk. In connection with this, it is advisable to stop breastfeeding during therapy with the drug.
Contraindications
The drug is not prescribed to patients who have been intolerant of at least one of the components of the drug. It is forbidden to use the drug to treat patients with intestinal obstruction.
Peroral forms of the drug are not used for galactosemia, lactase deficiency or impaired absorption of lactose in the intestine.
Caution during drug therapy should be observed for patients who are diagnosed with glaucoma or benign prostatic hyperplasia, as well as those with an increased heart rate (tachycardia).
Side effects of the gastrotsepina
During treatment with the drug, patients often complain of dryness of the oral mucosa. Quite often they have changes in the stool (more often constipation, less often diarrhea), various skin rashes, migraine-like pains, and accommodation disorders. There is much less evidence of urinary retention in the body. Severe allergic reactions (Quincke's edema and anaphylactic shock) can develop only on the background of intolerance of individual components of the drug.
The appearance of such undesirable effects as urinary retention, visual impairment, tachycardia and an increase in body temperature require withdrawal of the drug and contacting a doctor for advice.
In connection with the possibility of developing such a side effect as a violation of accommodation during drug therapy, it is better to be careful to perform work related to the need for concentration and to drive.
Dosing and administration
According to the official instruction for the drug "Gastrotsepin", taking the tablets should be done half an hour before meals. The tablet does not need to be chewed, but it is recommended to drink plenty of liquid (preferably water).
The usual daily dose of the drug is 50 mg (2 tablets with a dosage of 25 mg). Tablets in this case are taken 2 times a day (in the morning and in the evening).
Sometimes in the first days of therapy, doctors prescribe an extra dose of medicine at lunchtime.
In some cases, the dosage may be increased to 150 mg. And then the daily dose can be divided into 3 or more receptions.
The course of treatment can last from 1 to 1.5 months. During this time, the patient should regularly take the drug, even if the disease seems to have receded. Premature failure to take the drug is fraught with an early return of unpleasant and dangerous symptoms.
The drug solution is used for intramuscular and intravenous injections or infusions. Enter the solution into the vein slowly, to avoid pressure spikes and heart rate and prevent the development of thrombophlebitis.
A single dose is usually 10 mg (1 ampoule). You need to enter it 2 times a day. The interval between the administrations is 12 hours.
Stress ulcer therapy is performed by administering a single dose of the drug 3 times a day (a 30 mg dose). In severe cases of stomach ulcers and Zollinger-Ellison syndrome, it is recommended to inject a double dose of the drug once (single dose 20 mg, daily dose 60 mg).
Intravenous drip introduction of the drug is made after the drug from ampoules is mixed with saline solution, Ringer's solution or 5% glucose solution. Use the prepared composition for 12 hours.
Overdose
In cases of therapy according to the instruction for the use and appointment of a doctor, there were no cases of overdose.
Exceeding the allowable dose is fraught with the development of some undesirable effects. The patient may be troubled by hot flashes, dry skin and mucous membranes of the mouth, problems with vision. Taking the drug in large doses can provoke redness of the skin, fever and heart rate, urine retention and intestinal obstruction, choreoathetosis, mydriasis. There may also be a twitching of the facial muscles, drowsiness or, conversely, anxiety and anxiety, delusional conditions.
With the oral administration of the drug, first aid is given in the form of washing the stomach and taking activated charcoal. However, completely withdraw the drug from the body with its help will not succeed. Blood transfusion or its purification by hemodialysis or peritoneal dialysis will also be of little effect.
In case of severe intoxication, which is characterized by an increase in body temperature, tachycardia and delirium, a small amount of parasympathomimetic agent can be injected intravenously (the drug "Physostigmine" is recommended).
When glaucoma shows the local application of the drug "Pilocarpin". In acute attacks of the disease, m-cholinomimetics are indicated with the obligatory subsequent referral to a specialist doctor.
[37], [38], [39], [40], [41], [42], [43], [44], [45], [46], [47], [48], [49]
Interactions with other drugs
It is not recommended to take the drug "Gastrotsepin" in parallel with blockers of H2-histamine receptors. The drugs are able to enhance each other's action (synergy), resulting in a significant decrease in the production of gastric juice and its acidity, which is fraught with digestive disorders.
"Gastrotsepin" is also able to reduce the negative irritant effect on the gastrointestinal mucosa of anti-inflammatory drugs, improving their tolerability.
Shelf life
Under the appropriate storage conditions, the shelf life of the drug will be 5 years, after which "Gastrotsepin" is not recommended.
[52]
Attention!
To simplify the perception of information, this instruction for use of the drug "Gastrotsepin" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.