Metoclopramidum hydrochloride

General characteristics. Structure:

International and chemical names: metoclopramide; 4-amino-5-hlor-N-(2-diethylamino-ethyl) - a 2-metoksibenzamida a hydrochloride; main physical and chemical properties: transparent, colourless liquid; sostav:1 the ml contains 5 mg of Metoclopramidum of a hydrochloride; excipients: sodium sulfite anhydrous, dinatrium эдетат, sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. The specific blocker of dopamine (D2) and serotoninovy (5-HT3) receptors, oppresses chemoceptors of a trigger zone of a brainstem, 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 GIT innervation) exerts the regulating and coordinating impact on a tone and a physical activity of digestive organs.
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 his tone, eliminates dyskinesia of a gall bladder. The m-holinoblokiruyushchim, antihistaminic, antiserotoninovy and ganglioblokiruyushchy action does not possess; kidneys and a liver, on blood formation, secretion of a stomach and pancreas do not influence a tone of blood vessels of a brain, the ABP, breath function, and also. Stimulates prolactin secretion (like other blockers of dopamine receptors).
The beginning of action on a GIT is noted in 10-15 min. after intramuscular introduction and in 1-3 min. – after intravenous and is shown by acceleration of evacuation of contents of a stomach (approximately during 3 h) and antiemetic effect (12 h proceed).

Pharmacokinetics. At parenteral administration it is quickly and completely soaked up. In insignificant degree it is metabolized in a liver by linkng with sulfuric and glucuronic acids. The elimination half-life makes 2,5 – 6 h. About 85% of a dose are removed with urine in not changed look or in the form of metabolites during 72 h, other part – with a stake. At patients with renal failures the elimination half-life is increased.
Easily gets through hematoencephalic and placental barriers, it is allocated with breast milk.

Indications to use:

Vomiting and nausea of various genesis, disturbance of motility of digestive tract at not ulcer dyspepsia, a reflux esophagitis, a gastroduodenita, a round ulcer, a diabetic gastroparez, a postoperative atony of a stomach and intestines, a meteorism; apply to simplification of sounding or carrying out X-ray contrast researches of digestive tract.

Route of administration and doses:

Intravenously, intramusculary. The single dose makes 10 mg, 2 - 3 times a day. The maximum single dose – 20 mg; daily – 60 mg.
To newborns and children up to 6 years the single dose is established at the rate of 0,5 mg/kg of body weight a day, frequency rate of 1 - 3 time a day. To children 6 years are more senior appoint 5 mg 1-3 times a day.
Before X-ray inspection adult enter intravenously 10 – 20 mg in 5  15 min. prior to a research.
The patient with clinically expressed hepatonephric insufficiency appoint a dose twice smaller usual in the beginning, the subsequent dose depends on individual reaction of the patient to Metoclopramidum.

Features of use:

It is not effective at vomiting of vestibular genesis.
Drug is not appointed after GIT operations (for example, a pyloroplasty or an anastomosis of intestines) as vigorous muscular contractions interfere with healing of seams.
It is not necessary to apply in operating time to drivers of vehicles and people whose profession requires special attention and speed of psychomotor reactions. The majority of side effects arises during 36 h from an initiation of treatment and disappear during 24 h after cancellation.
With care: children's age up to 14 years, a renal and/or liver failure, bronchial asthma, arterial hypertension, a diabetes mellitus, long starvation, acidosis.
At use of drug in the period of a lactation it is necessary to consider that Metoclopramidum is allocated with breast milk therefore in need of prolonged use of drug it is necessary to resolve an issue of the feeding termination by a breast. During treatment not to take alcohol because of risk of development of possible complications.

Side effects:

From a GIT: in an initiation of treatment the lock, diarrhea are possible, it is rare – dryness in a mouth.
From TsNS: in an initiation of treatment the feeling of fatigue, drowsiness, dizziness, a headache, a depression, an akathisia are possible; seldom – emergence of extrapyramidal symptoms at children and teenagers (even after single use of drug): a spasm of facial muscles, hyperkinesias, a spastic wryneck (as a rule, passes right after drug phase-out);
parkinsonism phenomena are in some cases possible (the risk of development in children and teenagers increases at exceeding of a dose of 0,5 mg/kg/days), dyskinesia (at prolonged use, at patients of advanced age, at a renal failure). Allergic reactions:  skin rash is rare.

Interaction with other medicines:

Strengthens effect of ethanol on TsNS, efficiency of therapy _{H2-gistaminoblokatorami}.
Increases absorption of acetylsalicylic acid, paracetamol, diazepam, ethanol, a levodopa, tetracycline, ampicillin (strengthens absorption thanks to more bystry evacuation of contents of a stomach).
Reduces absorption of digoxin and Cimetidinum (disturbance of absorption in connection with acceleration of a vermicular movement of intestines).
At simultaneous use of drug and neuroleptics (especially fenotiazinovy number and derivatives of phenyl propyl ketone) the risk of development of extrapyramidal symptoms increases.

Contraindications:

Hypersensitivity, bleedings in a GIT, intestinal impassability, perforation of a GIT (including states when strengthening of a physical activity of a GIT is undesirable); a pheochromocytoma (hypertensive crisis, in connection with emission of catecholamines from a tumor is possible); epilepsy, glaucoma, extrapyramidal frustration; pregnancy (the I trimester), vomiting at patients with cancer of a mammary gland.

Overdose:

Symptoms: strengthening of manifestations of the described by-effects is possible.
Treatment: there is no specific antidote. Drug withdrawal, symptomatic therapy.

Storage conditions:

To store in protected from light, the place, unavailable to children, at a temperature from 15 °C to 25 °C.
Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule, on 5 ampoules in the cartridge, on 2 cartridges in a pack.