Metoclopramidum

General characteristics. Structure:

Active ingredient: 10 mg of Metoclopramidum of a hydrochloride in each tablet.

Excipients: lactose monohydrate, potato starch, povidone, calcium stearate.

Pharmacological properties:

Pharmacodynamics. The antiemetic, promotes reduction of nausea, a hiccups; stimulates a peristaltics of an upper part of digestive tract. Antiemetic action is caused by blockade of dopamine receptors and increase in a threshold of excitement of chemoceptors of a trigger zone. Believe that Metoclopramidum inhibits the relaxation of smooth muscles of a stomach caused by a dopamine, strengthening thus cholinergic reactions of smooth muscles of digestive tract.

Promotes acceleration of gastric emptying by prevention of relaxation of a body of a stomach and increase in phase activity of antral department of a stomach. At the same time there is a relaxation of upper parts of a small bowel that leads to improvement of coordination of a vermicular movement of a body and antral department of a stomach and upper parts of a small bowel. Reduces a contents reflux in a gullet due to increase in pressure of the lower sphincter of a gullet at rest and increases clearance of acid from a gullet thanks to increase in amplitude of its peristaltic reductions.

Metoclopramidum stimulates secretion of prolactin and causes tranzitorny increase in level of the circulating Aldosteronum that can be followed by a short-term delay of liquid.

Pharmacokinetics. Linkng with proteins of plasma makes about 30%. Gets through hematoencephalic and placental barriers, gets into maternal milk. After intake it is quickly soaked up, time of achievement of Cmax in a blood plasma of 30 - 120 min. Bioavailability makes 60 – 80%.

In insignificant degree it is metabolized by linkng with glucuronic and sulphuric acid. It is removed preferential by kidneys both in not changed look, and in the form of metabolites. T1/2 makes from 4 to 6 h. At renal failures of T1/2 can increase to 14 h.

Indications to use:

Vomiting, nausea, hiccups of various genesis (including at therapy by foxglove drugs, antibiotics, antitubercular drugs, at cytostatic and cytotoxic therapy); atony and hypotonia of a stomach and intestines (including postoperative); dyskinesia of biliary tract; reflux esophagitis; functional pyloric stenosis; stomach paresis at a diabetes mellitus; an aggravation of a peptic ulcer of a stomach and a 12-perstny gut (in complex therapy); for strengthening of a vermicular movement when carrying out X-ray contrast researches of digestive tract); as the medicine facilitating duodenal sounding (for acceleration of gastric emptying and advance of food on a small bowel).

At patients aged up to 20 years apply only according to the following indications:

- heavy unremovable vomiting of the known etiology.

- the vomiting connected with radiation therapy and reception of cytotoxic means;

- inspections of digestive tract;

- premedication before surgical procedures.

Route of administration and doses:

Metoclopramidum should be accepted in 30 min. prior to meal, tablets are swallowed without chewing, wash down with a small amount of water.

The dose is defined individually depending on clinical symptomatology and age of the patient. A usual dose for adults on 10 mg three times a day.

To persons at the age of 15-19 years: at body weight more than 60 kg on 10 mg three times a day; 30-59 kg on 5 mg three times a day.

At implementation of diagnostic procedures apply once in 5-10 min. prior to a research the adult 10-20 mg, to teenagers – on 10 mg.

Features of use:

During treatment by Metoclopramidum it is impossible to take alcohol and alcohol-containing medicines.

Use for patients with an abnormal liver function and kidneys. At patients with clinically significant degree of a renal failure or an abnormal liver function therapy has to be carried out in the reduced dosage.

Features of use in pediatric and geriatric practice. Children aged up to 15 years are not recommended to apply Metoclopramidum. As at children Metoclopramidum pharmacodynamics after peroral and intravenous administration is very changeable and accurate connection concentration effect is not established.

At teenagers and young people (15-19 years), and also elderly persons the risk of emergence of extrapyramidal reactions at treatment is increased by Metoclopramidum.

Treatment by Metoclopramidum should be avoided more than 12 weeks in all cases, except when assume that the therapeutic effect outweighs risk of development of late dyskinesia.

Use at pregnancy and feeding by a breast. Metoclopramidum is contraindicated at pregnancy. Metoclopramidum gets into breast milk therefore at its reception it is necessary to separate the child from a breast.

In pilot studies it is not established adverse action of Metoclopramidum on a fruit.

Influence on ability to control of motor transport and mechanisms. During treatment it is necessary to be careful at control of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: in an initiation of treatment the lock, diarrhea are possible; seldom - dryness in a mouth.

From the central nervous system: in an initiation of treatment the feeling of fatigue, drowsiness, dizziness, a headache, a depression, an akathisia are possible.

At treatment by Metoclopramidum extrapyramidal symptoms in the form of disturbances of a muscle tone, involuntary movements of extremities, spasms of mimic face muscles and a wryneck can appear. Emergence of such symptoms can arise when using in therapeutic doses at any age group, but most often at children and youth, and also after use of Metoclopramidum in higher doses used for prevention of vomiting owing to antineoplastic chemotherapy. Dystonic reactions usually take place within 24 – 48 hours after the termination of reception of Metoclopramidum.

Late dyskinesia. After reception of Metoclopramidum at patients of old age, especially at women, dyskineses (biting of lips, inflation of cheeks, the bystry or worm-shaped movements of language, the uncontrollable chewing movements, the uncontrollable movements of hands and legs), often irreversible can be shown. Such symptoms are shown, as a rule, after prolonged continuous treatment by Metoclopramidum, is more rare during short-term treatment by smaller doses of drug. Therapy by Metoclopramidum has to be stopped at patients at whom signs or symptoms of late dyskinesia develop. There is no known way of treatment of late dyskinesia. At some patients symptoms can be resolved or decrease after the treatment termination by Metoclopramidum.

From system of a hemopoiesis: in an initiation of treatment the agranulocytosis is possible.

From endocrine system: seldom, at prolonged use in high doses - a galactorrhoea, a gynecomastia, disturbances of a menstrual cycle.

Allergic reactions: seldom - skin rash.

Interaction with other medicines:

Cholinesterase inhibitors can weaken action.

Medicine strengthens absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, a levodopa, ethanol, bioavailability of Bromocriptinum and cyclosporine (control of its concentration in blood is necessary); reduces absorption of digoxin and Cimetidinum.

Appointment of Metoclopramidum with neuroleptics is not allowed (the risk of emergence of extrapyramidal disturbances increases).

Metoclopramidum reduces effects of blockers of H2 - histamine receptors.

Metoclopramidum increases risk of side effects at a combination with gepatotoksichny means.

Contraindications:

Hypersensitivity, gastrointestinal bleeding, pyloric stenosis, mechanical intestinal impassability, perforation of a stomach or intestines, the first 3-4 days after stomach and/or intestines operations, a pheochromocytoma, extrapyramidal disturbances, epilepsy, prolaktinozavisimy tumors, pregnancy, children's age up to 15 years, the lactation period, hypersensitivity to Metoclopramidum.

With care to apply at bronchial asthma, arterial hypertension, Parkinson's disease, a liver and/or renal failure, at advanced age.

Overdose:

Symptoms: a hypersomnia, increase or lowering of arterial pressure, disturbance of functions of cardiovascular system with bradycardia, a disorientation and extrapyramidal frustration.

Symptoms remain 24 h after reception.

Treatment: at a serious poisoning extrapyramidal frustration can be eliminated quickly with purpose of Cyclodolum (doses for adults make 2-4 mg, for children of 0,04 mg/kg of body weight).

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

10 or 25 tablets in a blister strip packaging; in packaging No. 10 x 1, No. 10 × 5, No. 25 x 1, No. 25 x 2.