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Gastrotsepin solution for injections

Gastrotsepin solution for injections (Solutio Gastrozepin pro injectionibus)

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: transparent, colourless or yellowish liquid, practically without third-party parts;

structure: 1 ampoule includes 10 mg of a pirentsepin of a hydrochloride;

other components: polypropylene glycol, sodium chloride, sodium acetate trihydrate, acid ice acetic.

Form of production of medicine. Solution for injections.

Farmakoterapevtichesky group. Antiulcerous means. Code of automatic telephone exchange A02BX03.

Pharmacological properties. Pharmacodynamics. 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 in a digestive tract with concentration peak in plasma which arises within 2-3 hours after introduction. 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 (about 12%).

Diffusion through a blood-brain barrier and a placenta minimum, it is established that only the minimum quantities are present at milk of women who nurse.

At parenteral administration pirentsepin by an identical measure it is removed with urine and a stake. The general plasma 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 hepatic, nor easy or moderate renal insufficiency.

The imaginary volume of distribution of the central department averages 14 liters which answer approximate extracellular space of the person.

Indications for Gastrotsepin's use. Prevention and treatments of the ulcers caused by a stress; erosion or ulcers of upper parts of a digestive tract that bleed, Zollingera-Ellison's syndrome, for initial therapy of severe acute and chronic forms of stomach ulcers and a duodenum.

Way of use and dose. If it is not appointed differently, each 12 hours need to be entered intramusculary or intravenously one ampoule.

For prevention and treatment of stressful ulcers it is recommended to enter one ampoule, 3 times a day (each 8 hours).

This dose needs to be increased, at least, twice for patients with the diagnosis of a syndrome of Zollingera-Ellison, and in especially hard cases introductions of two ampoules, three times a day are recommended. At Zollingera-Ellison's syndrome parenteral administration precedes surgical intervention.

Parenteral therapy by Gastrotsepin has to continue before disappearance of symptoms, ordinary within 2-3 days, after that Gastrotsepin it is necessary to accept orally.

Note. Intravenous administration has to be carried out by a slow injection (more, than in 3 minutes) or it is desirable by infusion.

Intravenous infusion: Gastrotsepin's solution can integrate with isotonic saline solution, Ringer's solution, 5% solution of a levuloza, 5% glucose solution.

Side effect. At use of drug there can be such side effects as 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. Pregnancy, lactation period.

Overdose. Symptoms. To there were no messages about overdose cases for the person today. 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). A hemodialysis, hemoperfusion, a peritoneal dialysis and repeated dosages of absorbent carbon inefficient for removal of anticholinergic agents.

In case of serious intoxication (for example, a hyperthermia, hard cases to a delirium or tachycardia) can enter small doses of physostigmine intravenously.

In case of developing of acute glaucoma it is necessary to begin treatment with miotic drops and to handle immediately the help to 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 security measures the concerning uses of medicines, especially during the first trimester. It is established what pirentsepin can pass into breast milk. As a result of it in the child which is on breastfeeding the anticholinergic effect can be observed.

Gastrotsepin need to use with care patients with glaucoma, a prostatauxe.

Intravenous injections always have to be slow:

because of risk of development of thrombophlebitis owing to contents 39, 2% of propylene glycol;

the constant control of a blood pressure is necessary for patients with unstable blood circulation through high initial level.

Through chances of vision disorders and accommodation ability to steer the car or mechanisms can be broken.

Interaction with other medicines. To give simultaneous use of Gastrotsepin and blockers of H2 receptors to more expressed decrease in secretion of hydrochloric acid which has special value for treatment of patients with Zollingera-Ellison's syndrome.

At simultaneous use of antiinflammatory agents with Gastrotsepin the effect does not change. On the other hand, tolerance of these products touching a digestive tract improves.

Terms and storage conditions. To store at the room temperature (it is not above 25 °C), in the place unavailable to children. To protect from direct sunshine, heat and to a frost. A period of validity – 5 years.

"Gastrotsepin   Gelusil-Lak"