Metoclopramidum

General characteristics. Structure:

Active agent of Metoclopramidum of a hydrochloride monohydrate (in terms of Metoclopramidum a hydrochloride)-10 mg.
Excipients: dinatrium эдетат - 0,20 mg, sodium sulfite - 0,25 mg, sodium chloride - 18 mg, acetate sodium trihydrate - 1,08 mg, acetic acid - 0,00132 ml, water for injections - to 2,0 ml.

Description: transparent colourless liquid.

Pharmacological properties:

Pharmacodynamics. Antiemetic. 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 duodenopilorichesky and gastroesophageal 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 on hypomotor type. 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 the m-holinoblokatorami is eliminated). 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 after intravenous administration, 10-15 minutes - after intramuscular introduction and is shown by acceleration of evacuation of contents of a stomach (approximately of 0,5-6 o'clock depending on a way of introduction) 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, a hiccups of various genesis (it can be in certain cases effective at the vomiting caused by radiation therapy or reception of tsitostatik);
- atony and hypotonia of a stomach and intestines (in particular, postoperative);
- dyskinesia of biliary tract on hypomotor type;
- reflux esophagitis;
- meteorism;
- functional pyloric stenosis;
- 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;
- as the means facilitating duodenal sounding (for acceleration of gastric emptying and advance of food on a small bowel).

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 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 liver and/or renal failure 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.

Due to the content of sodium sulfite it is not necessary to appoint injection solution of Metoclopramidum the patient with bronchial asthma, with hypersensitivity to sulfites (see the section "Contraindications").

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.

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.

Features of influence of drug on ability to manage the vehicle or during the work as potentially dangerous mechanisms

It is recommended to be careful when driving or during the work with potentially dangerous mechanisms demanding the increased concentration of attention and speed of psychomotor reactions.

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 (including okulogirny crisis), a spastic wryneck, an opisthotonos, a muscle hyper tone; parkinsonism (the hyperkinesia, muscular rigidity - manifestation of dofaminblokiruyushchy action, 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, depression

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

From system of a hemopoiesis: a neutropenia, a leukopenia, a sulfhemoglobinemia at adults. From cardiovascular system: atrioventricular block.

From a metabolism: porphyria.

Allergic reactions: small tortoiseshell, bronchospasm, Quincke's disease.

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.

If at you any of the side effects specified in the instruction developed, as soon as possible see a doctor.
If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Strengthens effect of ethanol on the central nervous system, sedation of hypnagogues, increases efficiency of therapy by blockers of H2-histamine receptors.

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.

Cholinesterase inhibitors can weaken action of Metoclopramidum.

If you accept other drugs, it is necessary to consult with the doctor.

Contraindications:

Hypersensitivity to Metoclopramidum or any of drug components;
bleedings from digestive tract;
stomach pyloric stenosis;
mechanical intestinal impassability;
perforation of a wall of a stomach or intestines;
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;
bronchial asthma at patients with hypersensitivity to sulfites (see the section "Special Instructions");
pregnancy (the I trimester), the lactation period (see the section "Use at Pregnancy and during Breastfeeding");
early children's age (to children up to 2 years - use of Metoclopramidum in the form of any dosage forms is contraindicated, to children up to 6 years - contraindicated parenteral administration).

Do not appoint after digestive tract operations (such as pyloroplasty or anastomosis of intestines) as vigorous muscular contractions interfere with healing.

If you have a hypersensitivity to Metoclopramidum or other components of drug, before reception surely consult with the doctor.

With care

Bronchial asthma, arterial hypertension, Parkinson's disease, renal and/or liver failure, advanced age (65 years are more senior), children's age (the increased risk of development of a diskinetichesky syndrome).

If at you one of the listed diseases, before administration of drug surely consult with the doctor.

Use at pregnancy and during breastfeeding

Metoclopramidum is contraindicated to use in the I trimester of pregnancy.

Use in II and III trimesters of pregnancy is possible only according to vital indications.

In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

Symptoms: hypersomnia, disorientation and extrapyramidal frustration.

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

Storage conditions:

In the place protected from light at a temperature not above 25 °C. To store the place, unavailable to children. Period of validity: 5 years. Not to use on expiry date, specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 5 mg/ml.
On 2 ml in ampoules of colourless neutral glass type I with a color ring of a break or with a color point and a notch. One, two or three color rings and/or a two-dimensional barcode, and/or the alphanumeric coding or without additional color rings, a two-dimensional barcode, the alphanumeric coding in addition apply on ampoules. On 5 ampoules in a blister strip packaging. On 1 or 2 blister strip packagings together with the application instruction in a pack from a cardboard.