Metoclopramidum

General characteristics. Structure:

Active ingredient: 10 mg of Metoclopramidum of a hydrochloride in 2 ml of solution.

Excipients: sodium chloride, sodium sulfite anhydrous, dinatrium эдетат, propylene glycol, Acidum hydrochloricum, water for injections.

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 makes about 30%. Passes through a placental barrier and a blood-brain barrier, gets into maternal milk. The effect begins to develop in 10-15 minutes after intramuscular introduction and in 1-3 min. after intravenous administration. T1/2 is 3-5 h, at a renal failure - to 14 h. Removal of drug happens generally through kidneys (85% during 72 h) in not changed look and in the form of sulphatic and glyukuronidny conjugates.

Indications to use:

Vomiting, nausea, hiccups of various genesis (it can be in certain cases effective at the vomiting caused beam or chemotherapy), an atony and hypotonia of a stomach and intestines (in particular, postoperative); dyskinesia of biliary tract; a reflux esophagitis, a meteorism, an aggravation of a peptic ulcer of a stomach and a 12-perstny gut (as a part of complex therapy).

X-ray contrast researches GITs (for strengthening of a vermicular movement).

Route of administration and doses:

Solution for injections is entered intravenously or intramusculary within 1-2 minutes: the adult in a dose of 10 mg 3 – 4 times a day (the maximum single dose – 20 mg, the maximum daily dose - 60 mg); to children 6 years - on 2,5 - 5 mg of 1 - 3 time a day are more senior; for children under 6 years the daily dose makes 0,5 - 1 mg/kg, frequency rate of introduction - 1-3 times. The highest daily dose for children – 0,5 mg/kg.

The average duration of a course of treatment – 4-6 weeks, in some cases – up to 6 months.

For prevention and treatment of nausea and the vomiting caused by reception of tsitostatik or radiation therapy, the drug is administered:

- discontinuous intravenous infusion (within not less than 15 minutes) in a dose to 2 mg/kg in 30 min. prior to use of tsitostatik or radiation, and also later 1,5; 3,5; 5,5 and 8,5 hours after use (the maximum daily dose of 10 mg/kg);

- long intravenous infusion in a dose of 1 (0,5) mg/kg of body weight an hour, beginning in 2 hours prior to use of cytostatic means and finishing at the time of use of cytostatic means, then in a dose of 0,5 (0,25) mg/kg of body weight an hour within 12 - 24 hours after use of cytostatic means (the maximum daily dose of 10 mg/kg).

Everyone short (within 15 min.) intravenous drop injection is carried out after preliminary cultivation of a single dose to 50 ml of infusion solution. Solution can be dissolved with isotonic solution of sodium chloride or solution of glucose of 5%. Drug cannot be mixed with alkaline infusion solutions.

At the lowered function of kidneys drug is appointed:

- at clearance of creatinine to 10 ml/min. - 10 mg once a day;

- at clearance of creatinine from 11 to 60 ml/min. – 15 mg/days divided into 2 introductions (10 mg and 5 mg).

Features of use:

During treatment by drug it is impossible to take alcohol and alcohol-containing drugs.

Use at pregnancy and feeding by a breast. It is contraindicated to use at pregnancy.

At use in the period of a lactation (breastfeeding) it is necessary to consider that Metoclopramidum gets into breast milk.

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

Influence on ability to driving of motor transport and to control of mechanisms. During treatment it is necessary to be careful during the driving 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. Emergence of extrapyramidal symptoms at children and persons of young age is possible (even after single use of Metoclopramidum): a spasm of facial muscles, hyperkinesias, a spastic wryneck (as a rule, pass right after the termination of reception of Metoclopramidum). At prolonged use, is more often at patients of advanced age, the phenomena of parkinsonism, dyskinesia are possible.

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.

Drug strengthens absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, a levodopa, ethanol; reduces absorption of digoxin and Cimetidinum.

Drug is not appointed along with neuroleptics (the risk of emergence of extrapyramidal disturbances increases).

Contraindications:

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

Due to the content of sodium sulfite it is not necessary to appoint solution of Metoclopramidum the patient with bronchial asthma with hypersensitivity to sulfite.

With care to apply at bronchial asthma, arterial hypertension, Parkinson's disease, a liver and/or renal failure, at advanced age, early children's age (the increased risk of emergence of a diskinetichesky syndrome).

Overdose:

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

The symptomatology disappears after the termination of administration of drug during 24 h.

Treatment: at a serious poisoning extrapyramidal frustration can be eliminated quickly with slow intravenous administration of Biperidinum (doses for adults make 2,5 – 5 mg, for children of 0,04 mg/kg of body weight).

Storage conditions:

In the place protected from light, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

In ampoules on 2 ml, in packaging No. 10, No. 10 x 1.