Metoclopramidum

General characteristics. Structure:

Active ingredient: 10 mg of Metoclopramidum of a hydrochloride of hydrate.

Excipients: sodium pyrosulphite, sodium chloride, disodium salt of ethylene diamine tetraacetic acid (Trilonum of B), water for injections.

Pharmacological properties:

Pharmacodynamics. The specific blocker of dopamine (D2) and serotoninovy (5-NTZ) receptors, oppresses chemoceptors of a trigger zone of a trunk of a brain, weakens sensitivity of the visceral nerves transferring impulses from a pylorus and a duodenum to the emetic center. Through a hypothalamus and a parasympathetic nervous system (a digestive tract innervation) exerts the regulating and coordinating impact on a tone and a physical activity of an upper part of digestive tract (including a tone of the lower sphincter of a gullet).

Raises a tone of a stomach and intestines, accelerates gastric emptying, reduces hyperacid стаз, interferes with a peloric and ezofagealny reflux, stimulates an intestines peristaltics. Normalizes department of bile, reduces a spasm of a sphincter of Oddi. Without changing its tone, eliminates dyskinesia of a gall bladder. Kidneys and a liver, on blood formation, secretion of a stomach and pancreas do not influence a tone of blood vessels of a brain, arterial pressure, breath function, and also. Stimulates prolactin secretion. Increases sensitivity of fabrics to acetylcholine (action does not depend on a vagal innervation, but is eliminated with holinoblokator). Stimulating secretion of Aldosteronum, strengthens a delay of ions of sodium and removal of potassium ions.

The beginning of action on digestive tract is noted in 1 - 3 minutes later in/in introductions, 10-15 minutes - after introduction in oil and is shown by acceleration of evacuation of contents of a stomach (approximately of 0,5-6 o'clock depending on a way of maintaining) and antiemetic effect (12 hours proceed).

Pharmacokinetics. Communication with proteins of plasma - about 30%. Is exposed to metabolism in a liver. The elimination half-life makes 4-6 hours, at a renal failure - till 14 o'clock. Removal of drug happens generally through kidneys within 24-72 hours in not changed look and in the form of conjugates. Passes through placental and hematoencephalic barriers and gets into maternal milk.

Indications to use:

Vomiting, nausea, hiccups of various genesis (it can be in certain cases effective at the vomiting caused by radiation therapy or reception of tsitostatik). An atony and hypotonia of a stomach and intestines (in particular, postoperative), dyskinesia of biliary tract, a reflux esophagitis, a meteorism, as a part of complex therapy of aggravations of a peptic ulcer of a stomach and a duodenum. It is applied to strengthening of a vermicular movement when carrying out X-ray contrast researches of digestive tract.

Route of administration and doses:

Intravenously or intramusculary. The adult in a dose of 10-20 mg of 1 - 3 time a day (the maximum daily dose - 60 mg), to children 6 years on 5 mg 1-3 times a day are more senior; for children aged from 2 to 6 years the daily dose makes 0,5-1 mg/kg of body weight, frequency rate of introduction of 1 - 3 time.

For prevention and treatment of nausea and the vomiting caused by reception of tsitostatik or radiation therapy, the drug is administered intravenously in a dose of 2 mg/kg of body weight in 30 minutes prior to use of tsitostatik or radiation, if necessary introduction is repeated in 2-3 hours.

Before X-ray inspection adult enter intravenously 10-20 mg in 5-15 min. prior to the research.

The patient with clinically expressed hepatonephric insufficiency appoint a dose twice smaller usual, the subsequent dose depends on individual reaction of the patient to Metoclopramidum.

Features of use:

It is not effective at vomiting of vestibular genesis. Against the background of use of Metoclopramidum distortions of these laboratory indicators of function of a liver and definition of concentration of Aldosteronum and prolactin in plasma are possible.

During use of drug it is necessary to avoid potentially dangerous types of activity demanding the increased concentration of attention, bystry mental and motor reaction (driving of vehicles, etc.).

The majority of side effects arises within 36 hours from an initiation of treatment and passes within 24 hours after cancellation.

Treatment has to be whenever possible short-term. During treatment by drug alcohol intake is not recommended.

Side effects:

From a nervous system: extrapyramidal frustration - a spasm of facial muscles, a lockjaw, a rhythmic protrusion of language, bulbar type of the speech, a spasm of extraocular muscles (W. h okulogirny crisis), a spastic wryneck, an opisthotonos, a muscle hyper tone, parkinsonism (a hyperkinesia, muscular rigidity - manifestation dopamine - the blocking action, the risk of development in children and teenagers increases at exceeding of a dose of 0,5 mg/kg/days), dyskineses (at elderly, at a chronic renal failure); drowsiness, fatigue, uneasiness, confusion, headache, sonitus.

From the alimentary system: a lock or diarrhea, it is rare - dryness in a mouth.

Allergic reactions: small tortoiseshell.

From endocrine system: seldom (at long reception in high doses) - a gynecomastia, a galactorrhoea, disturbance of a menstrual cycle.

Others: in an initiation of treatment the agranulocytosis is possible, it is rare (at use in high doses) - a hyperemia of a mucous membrane of a nose.

Interaction with other medicines:

Strengthens effect of ethanol on TsNS, sedation of hypnagogues, increases efficiency of therapy H2-gistaminoblokatorami.

Increases absorption of diazepam, tetracycline, ampicillin, paracetamol, acetylsalicylic acid, a levodopa, ethanol, slows down absorption of digoxin and Cimetidinum.

At simultaneous use with neuroleptics the risk of development of extrapyramidal symptoms increases. Antikholinesterazny means can weaken action of Metoclopramidum.

Contraindications:

Hypersensitivity, bleedings from digestive tract, a pyloric stenosis, mechanical intestinal impassability, perforation of a stomach or intestines, a pheochromocytoma, epilepsy, glaucoma, extrapyramidal disturbances, Parkinson's disease, prolaktinozavisimy tumors, vomiting against the background of treatment or overdose by neuroleptics and at patients with cancer of a mammary gland, pregnancy (1 trimester), the lactation period, early children's age (up to 2 years).

With care - children's age, a renal/liver failure, bronchial asthma, arterial hypertension, advanced age

Overdose:

Symptoms: hypersomnia, disorientation and extrapyramidal frustration.

Treatment. As a rule, the symptomatology disappears after the termination of administration of drug within 24 hours. If necessary treatment is carried out by holinoblokator and protivoparkinsonichesky means.

Storage conditions:

In the protected from light, dry place at a temperature not above 25 °C. In the place, unavailable to children, the Period of validity 4 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for vnugrivenny and intramuscular introduction of 5 mg/ml. On 2 ml in ampoules of neutral glass. On 10 ampoules stack in a box from a cardboard. On 5 ampoules in a blister strip packaging. On 2 planimetric packagings stack in a pack from a cardboard. On 10 ampoules will prevent in a pack from a cardboard with partitions or lattices, or a separator from a cardboard or paper bag. Put the application instruction and a knife for opening of ampoules in each pack or a box or a knife ampoule ceramic. When using ampoules with notches, points or rings the knife ampoule is not put.