Metoclopramide, 5 mg/ml 2 ml 10 pcs

An antiemetic, promotes reduction of nausea, hiccups; stimulates peristalsis of the upper gastrointestinal tract. Antiemetic effect is caused by blockade of dopamine receptors and increase of excitation threshold of trigger zone chemoreceptors. It is believed that metoclopramide inhibits dopamine-induced relaxation of gastric smooth muscle, thus enhancing cholinergic responses of gastrointestinal smooth muscle. It promotes acceleration of gastric emptying by preventing relaxation of the gastric body and increasing phase activity of the gastric antrum. It relaxes the upper sections of the small intestine, which leads to improved coordination of peristalsis of the body and the antrum of the stomach and the upper sections of the small intestine. It decreases reflux of contents into the esophagus by increasing the pressure of the lower esophageal sphincter at rest and increases clearance of acid from the esophagus by increasing the amplitude of its peristaltic contractions.

Metoclopramide stimulates prolactin secretion and causes transient increase in circulating aldosterone that may be accompanied by transient fluid retention

Pharmacokinetics

Protein binding is approximately 30%. Passes through placental barrier and blood-brain barrier, penetrates into the mother’s milk. The effect begins to develop 10 to 15 minutes after intramuscular injection and 1 to 3 minutes after intravenous injection. T1/2 is 3-5 hours, in case of impaired renal function – up to 14 hours. Excretion of the drug occurs mainly through the kidneys (85% within 72 hours) unchanged and in the form of sulphate and glucuronide conjugates.

Indications

Vomiting, nausea, hiccups of various genesis (in some cases may be effective for vomiting caused by radiation or chemotherapy), atony and hypotonia of the stomach and intestines (in particular, postoperative); biliary dyskinesia; reflux esophagitis, flatulence, exacerbation of gastric and duodenal ulcer (in combination therapy).

Gastrointestinal X-ray contrast studies (to enhance peristalsis).

Active ingredient

Composition

Active ingredient:

Methoclopramide hydrochloride – 5 mg;

Auxiliary substances:

Sodium chloride,

sodium sulfite anhydrous,

dinatrium edetate,

propylene glycol,

hydrochloric acid,

water for injection.

How to take, the dosage

The solution for injections is given intravenously or intramuscularly for 1-2 minutes: adults in a dose of 10 mg 3 – 4 times a day (maximum single dose – 20 mg, maximum daily dose – 60 mg); children over 6 years old – 2.5 – 5 mg 1 – 3 times a day; for children under 6 years old a daily dose is 0.5 – 1 mg/kg, number of injections – 1-3 times. The highest daily dose for children is 0.5 mg/kg.

The average duration of therapy is 4-6 weeks, in some cases – up to 6 months.

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

– Intermittent intravenous infusion (for at least 15 minutes) in a dose of up to 2 mg/kg 30 minutes before cytostatics or irradiation, as well as 1.5; 3.5; 5.5 and 8.5 hours after application (maximum daily dose 10 mg/kg);

– Prolonged intravenous infusion at a dose of 1 (0.5) mg/kg body weight per hour, starting 2 hours before and ending at the time of cytostatic drug administration, then at a dose of 0.5 (0.25) mg/kg body weight per hour for 12 to 24 hours after cytostatic drug administration (maximum daily dose 10 mg/kg).

Each short (within 15 minutes) intravenous drip infusion is carried out after prior dilution of a single dose in 50 ml of infusion solution. The solution can be diluted with isotonic sodium chloride solution or glucose 5% solution. The drug must not be mixed with alkaline infusion solutions.

With decreased renal function the drug is administered:

– In creatinine clearance up to 10 ml/min – 10 mg once a day;

– In creatinine clearance from 11 to 60 ml/min – 15 mg/day divided into 2 injections (10 mg and 5 mg).

Interaction

The drug increases absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol; reduces absorption of digoxin and cimetidine.

The preparation is not prescribed simultaneously with neuroleptics (increased risk of extrapyramidal disorders).

Special Instructions

You should not drink alcohol or alcohol-containing drugs during treatment with the drug.

Contraindications

Hypersensitivity, gastrointestinal bleeding, gastric pylorus stenosis, mechanical intestinal obstruction, gastric or intestinal perforation, 3-4 days after gastric and/or intestinal surgery, pheochromocytoma, extrapyramidal disorders, epilepsy, prolactin-dependent tumors, pregnancy, children under 3 years of age, lactation period.

Due to the content of sodium sulfite, metoclopramide solution should not be administered to patients with bronchial asthma with hypersensitivity to sulfite.

Side effects

Digestive system disorders: at the beginning of treatment constipation, diarrhea are possible; rarely – dry mouth.
Central nervous system disorders: at the beginning of treatment fatigue, drowsiness, dizziness, headache, depression, akathisia are possible. Extrapyramidal symptoms may occur in children and young patients (even after single use of metoclopramide): facial spasm, hyperkinesis, spastic torticollis (usually disappear immediately after discontinuation of metoclopramide). Parkinsonism and dyskinesia phenomena are possible during long-term use, especially in elderly patients.
Blood system disorders: agranulocytosis is possible at the beginning of treatment.
Endocrine system: rare, with long-term use in high doses – galactorrhea, gynecomastia, menstrual disorders.

Allergic reactions: rare – skin rash.

Overdose

Symptoms:

Hypersomnia, high or low blood pressure, cardiovascular dysfunction with bradycardia, disorientation and extrapyramidal disorders.

The symptoms disappear after discontinuation of the drug within 24 h.

Treatment:

In severe poisoning, extrapyramidal disorders can be quickly resolved by slow intravenous administration of biperiden (doses for adults are 2.5 to 5 mg, for children 0.04 mg/kg body weight).

Similarities