international and chemical name: pirentsepin: 5, 11-digidro-11-[(4metil-1-piperazinil) acetyls] - 6H-pirido [2, 3-b] = [1, 4] benzodiazepine - 6 - it is dihydrochloride monohydrate;
Main physical and chemical properties: flat, round, white tablets with a dividing notch, almost inodorous. On one party of a tablet, two identical texts "61C" on both a side from risks, on other party - a logo are forced out;
structure: 1 tablet of Gastrotsepin contains 25 mg of a pirenzepin of dihydrochloride;
other components: lactose, starch corn, aerosil 200, magnesium stearate.
Form of production of medicine. Tablets.
Farmakoterapevtichesky group. Means for treatment of a round ulcer and a gastroezofagalny reflux. Automatic telephone exchange of A02B X03.
Pharmacological properties. Pirentsepin selektivno blocks muskarinovy receptors, reduces products of a gastric juice and raises rn in a stomach. In therapeutic doses it does not pass through a blood-brain barrier.
Pharmacokinetics. Pirentsepin is not completely soaked up from a digestive tract with concentration peak in plasma which is reached within 2-3 hours after reception. Therefore after peroral introduction the size of average absolute bioavailability makes only 10 - 20%.
If pirentsepin to accept with food, the area under a curve "concentration in plasma – time" (AUC) decreases by 30%.
Pirentsepin only poorly contacts plasma proteins (pribl. 12%).
Diffusion through a blood-brain barrier and a placenta is minimum, is established that only the minimum quantities are present at milk of women who nurse.
After peroral introduction pirentsepin it is almost completely removed with a stake. The general plasmatic clearance makes about 250 ml/min. The renal clearance makes about a half of this size that is approximately equivalent the level of glomerular filtering.
Pirentsepin is brought from an organism with an average elimination half-life from 10 to 12 hours. Mostly do not influence pharmacokinetics of a pirentsepin either a hepatic, nor slight or moderate renal failure.
Indications for use. Acute and chronic forms of stomach ulcers and duodenum; gastritises and duodenitis.
Way of use and dose. If another is not appointed, from 50 to 150 mg a day separate doses. As a rule, about 50 mg twice a day are recommended. Occasionally during the first 2 or 3 days of treatment can be necessary reception of an additional dose among day.
Pill has to be taken approximately in ½ hours before food with a small amount of liquid.
Even in case of fast subjective improvement of a state the patient should not reduce or interrupt treatments, is appointed the doctor.
Duration of peroral use of Gastrotsepin has to make from 4 to 6 weeks.
Side effect. At use of drug can be observed: dryness in a mouth, accommodation disturbance, tachycardia, diarrhea, a lock, an ischuria, a headache. There were messages about reactions of hypersensitivity and cases of an anaphylaxis.
Contraindications. Gastrotsepin should not be applied in cases of the established hypersensitivity to any of drug components.
Symptoms. So far information about overdose cases for the person did not arrive. However at introduction of large doses of a pirentsepin such anticholinergic effects can develop: moisture, dry, reddened skin; dryness in a mouth; expansion of pupils, delirious syndrome, tachycardia, intestinal impassability, ischuria, reflex myoclonic movements, choreoathetosis.
Therapy. In spite of the fact that experience of treatment of overdose pirentsepiny is very limited, in case of intoxication of treatment has to begin with the general actions (for example, absorbent carbon, a gastric lavage). The hemodialysis, hemoperfusion, a peritoneal dialysis and repeated dosages of absorbent carbon is not effective for removal of anticholinergic agents.
In case of the expressed intoxication (for example, a hyperthermia, hard cases to a delirium or tachycardia) can intravenously it is entered small doses of physostigmine.
In case of developing of acute glaucoma it is necessary to begin treatment with miotic drops and to ask immediately for the help the specialist.
Features of use.
Pregnancy and lactation. At preclinical trials the adverse effect is not revealed, but safety during pregnancy it is not established so far. For this period it is necessary to adhere to ordinary cautions the concerning uses of medicines, especially during the first trimester. It is established what pirentsepin gets to breast milk. As a result of it in the child which is on chest feeding the anticholinergic effect can be observed.
Gastrotsepin it is necessary to use with care at patients with glaucoma, a prostatauxe.
Through chances of vision disorders and accommodation the patient should abstain from driving by the car or mechanisms.
Interaction with other medicines. Simultaneous use of Gastrotsepin and blockers of H2 receptors brings to considerable braking of secretion of gastric acid which has special value for patients with Zollingera-Ellison's syndrome.
At simultaneous use of antiinflammatory agents with Gastrotsepin the effect does not change. On the other hand, portability of these funds from side of a digestive tract improves.
Conditions and periods of storage. To keep drug at the room temperature (it is not above 30 °C) in the place unavailable to children. A period of validity - 60 months.