GASTROCEPIN

Active material: Pirenzepine
When ATH: A02BX03
CCF: M Blocker₁-holinoretseptorov with impact on receptors in the stomach
When CSF: 11.01.02
Manufacturer: BOEHRINGER INGELHEIM ESPANA S.A.. (Spain)

Pharmaceutical form, composition and packaging

Solution for in / and the / m clear, colourless or slightly yellowish, with a faint odor of acetic acid.

Excipients: sodium chloride, sodium acetate trihydrate, glacial acetic acid, propylene glycol, water d / and.

2 ml – colorless glass vials (5) – Plastic trays (1) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES.

Pharmacological action

M Blocker₁-cholinergic, synthetic tertiary amine. Has a predominantly peripheral antiholinergicescoe effect. Decreases basal and stimulirovannuyu secretion of hydrochloric acid. Reduces peptic activity gastric juice. Slightly reduces tone smooth muscles stomach.

Secretion of pepsin, insulin-driven, reduced by 49%, gistaminom – on 34%, gastrinom – on 24%. Oppressing secretion of bicarbonate from the epithelium of the stomach cavity in patients with jerozivnym defeat antralnogo and enhances protection of gastric mucosa; increases blood flow in the podslizistom layer of the stomach and intestines, improves microcirculation.

Has no effect on the central nervous system, practically does not change the HEART RATE.

In therapeutic doses, other antiholinergicakie effects pirenzepina are expressed weakly.

Pharmacokinetics

After intake of pirenzepine is poorly absorbed from the digestive tract. Bioavailability is 20-30%, together with the admission of food – 10-20%. Plasma protein binding – 10-12%. Poor penetrate the BBB. A very small amount of pirenzepina metabolizmu.

T_1/2 is 10-12 no. About 10% excreted unchanged in the urine, the rest of the – with feces.

Testimony

Treatment and prevention of ulcers stomach and duodenal ulcers (as an adjuvant); chronic gastritis with increased gastric secretion, erosive esophagitis, reflux esophagitis, Zollinger-Ellison; erosive and ulcerative lesions of the gastrointestinal tract, antirheumatic therapy arising on and anti-inflammatory agents.

Dosage regimen

Adults inside in the first 2-3 day – by 50 mg 3 times / day for 30 minutes before eating, then 50 mg 2 times / day. A course of treatment – 4-6 weeks.

If necessary, – give/m or/in the 5-10 mg 2-3 times / day. Possible combined use of Parenteral and inside.

The maximum dose: ingestion – 200 mg / day.

Side effect

From the digestive system: dry mouth, constipation, frequent stools, increased appetite.

On the part of the organ of vision: ccomodation; rarely – eye sensitivity to light.

Other: decreased sweating.

Contraindications

Prostate hyperplasia; pseudoileus, stenosis pryvratnyka; I trimester of pregnancy; hypersensitivity to pirenzepinu.

Pregnancy and lactation

Contraindicated for use in the I trimester of pregnancy. Not recommended for use in groups II and III trimestrah pregnancy.

If you must use during lactation should be considered, that pirenzepine in small amounts out of breast milk.

Cautions

(C) to apply caution in patients with cardiovascular disease, where an increase in HEART RATE may be undesirable: atrial fibrillation, tachycardia, congestive heart failure, CHD, mytralnыy stenosis, arterial hypertension, acute bleeding; thyrotoxicosis (Perhaps increased tachycardia); elevated temperature (may still rise due to oppression activity of sweat glands); When reflux-ezofagite, hiatal hernia, coupled with reflux esophagitis (decrease motility esophagus and stomach and lower esophageal sphincter relaxation may help slow gastric emptying and gastroesophageal reflux through strengthening the sphincter with compromised function); in diseases of the digestive tract, accompanied by obstruction – Esophageal ahalazija, stenosis pryvratnyka (possible reduced motility and tonus, resulting in obstruction and delay stomach contents), atony ulcers in patients older or debilitated patients (Perhaps the obstruction), pseudoileus; with increasing intraocular pressure – closure (mydriatic effect, leading to an increase in intraocular pressure, can cause acute attack) and open-angle glaucoma (midriaticheskij effect can cause some increase of intraocular pressure; may require correction therapy); When nonspecific ulcerative colitis (high doses can depress peristalsis, increasing the likelihood of paralytic ileus, Besides, possible manifestation or worsening of such serious complications, as toxic megacolon); dryness in the mouth (prolonged use can cause a further increase in the symptoms of xerostomia); hepatic failure (a decrease in the metabolism) and renal insufficiency (the risk of side effects as a result of the decline in breeding); in chronic lung diseases, particularly in young children and handicapped patients (reduce bronchial secretions can lead to thickening of secretions and education traffic jams in the bronchi); myasthenia (the condition may deteriorate due to inhibition of the action of acetylcholine); Prostate hypertrophy without obstruction of the urinary tract, delayed urine or predisposition thereto or diseases, accompanied by obstruction of the urinary tract (incl. bladder neck due to hypertrophy of the prostate gland); During gestosis (may increase hypertension); brain damage in children, children's cerebral palsy, Down's syndrome (reaction to antiholinergicakie funds intensifies).

When giperacidnom with continuous type of secretion of appropriate combine pirenzepine with blokatorami gistaminovykh n₂-receptors.

Avoid using antacids within 2-3 h after administration pirenzepina.

Against the background of the prolonged use of pirenzepina is recommended that regular measurement vnutriglaznogo pressure.

Drug Interactions

Together with the use of anticholinergic means perhaps increased anticholinergic effects.

Together with the use of opioid analgesics increases the risk of severe constipation or urinary retention.

If you are applying may reduce the action of metoclopramide on the motor activity of the DIGESTIVE TRACT.

At the same time the application increases the clinical efficacy of cimetidine.