Metoclopramide

When ATH:
A03FA01

Characteristic.

Metoclopramide hydrochloride is a white crystalline substance, without smell, soluble in water, ethanol. pKa — 0,6 and 9,3.

Pharmacological action.
Antiemetic, protivoikotnoe.

Application.

Nausea, vomiting, hiccups of various origins (in some cases it may be effective for vomiting, caused by radiation therapy or receiving cytostatics), functional digestive disorders, gastro-ézofagealʹnaâ reflûksnaâ disease, atonia and hypotonia of the stomach and duodenum (incl. Postoperative), biliary dyskinesia, flatulence, aggravation of gastric ulcer and duodenal ulcer (in the complex therapy), preparation for diagnostic gastrointestinal studies; syndrome Zill de la Turetta (generalized tics in children and vocalism).

Contraindications.

Hypersensitivity, bleeding from the gastrointestinal tract, pryvratnyka stenosis of stomach, Mechanical bowel obstruction, perforation of the wall of the stomach or intestines (incl. states, when the gain of undesirable gastrointestinal motor activity), glaucoma, pheochromocytoma (possible hypertensive crisis due to the release of catecholamines from the tumor), epilepsy (the severity and frequency of seizures may be increased), Parkinson's disease and other extrapyramidal disorders (may increase), prolaktinzavisimye tumor, early childhood up 2 years (increased risk of dyskinetic syndrome).

Restrictions apply.

Bronchial asthma (increased risk of bronchospasm), arterial hypertension (at / in a possible deterioration due to the release of catecholamines), liver and / or kidney failure, advanced age, Children up to age 14 years (for parenteral administration).

Pregnancy and breast-feeding.

In experiments on mice, rats and rabbits at / in, / m, n / a and orally administered at doses of metoclopramide, at 12-250 times the human dose, adverse effects on the fetus revealed no.

When pregnancy is permitted only when necessary (adequate and well-controlled studies in humans have not held).

Category actions result in FDA - B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)

Although complications in humans has not been registered, during the period of breast-feeding should be used with caution (It passes into breast milk).

Side effects.

The frequency of adverse events correlated with the dose and duration of dosing.

From the nervous system and sensory organs: restlessness (about 10%), drowsiness (about 10%, often at high doses), unusual tiredness or weakness (about 10%). Extrapyramidal disorders, incl. acute dystonic reactions (0,2% at doses of 30-40 mg / day), such as convulsive twitching of facial muscles, Trizm, opisthotonus, Muscle hypertonicity, spasmodic torticollis, spasm of the extraocular muscles (incl. okulohyrnыy crisis), rhythmic protrusion of tongue, bulbar type of speech; rarely, stridor and dyspnea, possibly due laringospazmom. Parkinsonian symptoms: bradikineziâ, tremor, Muscle rigidity is a manifestation of dopamine-blocking activity, the risk of children and adolescents increased by overdose 0,5 g / kg / day. Pozdnyaya dyskinesia, including involuntary movements of the tongue, bombast, uncontrolled chewing movements, uncontrolled movements of arms and legs (in elderly, in patients with chronic liver failure) (cm. and "Safety Precautions"). Insomnia, headache, dizziness, disorientation, depression (the symptoms were moderate to severe intensity and included suicidal ideation and suicide), anxiety, perplexity, noise in ears; rarely, hallucinations.

Cardio-vascular system and blood (hematopoiesis, hemostasis): hypotension / hypertension, tachycardia / bradycardia, fluid retention.

From the digestive tract: constipation / diarrhea, dry mouth; rarely is the hepatotoxicity (jaundice, violation of the liver functional parameters — if metoclopramide was used together with other hepatotoxic means).

Allergic reactions: hives.

Other: increased urination, urinary incontinence, in the long admission in high doses is gynecomastia, galactorrhea, menstrual disorders, asymptomatic weak hyperemia of the nasal mucosa, agranulocytosis.

It was reported on the development of methemoglobinemia in preterm and term infants born, in which / m administered metoclopramide doses of 1-2 mg / kg / day for 3 days or more.

Cooperation.

Antipsychotics (especially phenothiazines and derivatives butirofenona) increase the likelihood of extrapyramidal disorders. In an application reduces the effectiveness of levodopa. When taken with medicines, causing CNS oppression — increased sedative effect. When co-administered with cyclosporine metoclopramide caused a decrease in gastric emptying time may increase the bioavailability of cyclosporine (it may be necessary monitoring concentrations of cyclosporine). May reduce the absorption of digoxin from the stomach (it may be necessary a dose adjustment of digoxin). Can accelerate the absorption of mexiletine. It accelerates absorption of paracetamol, tetracycline. Concomitant use with alcohol may enhance the depressant effect of alcohol on the CNS or metoclopramide, and accelerate the removal of alcohol from the stomach, probably thereby improving the rate and extent of its absorption in the small intestine. The combined use of drugs, containing opioids, can block the effect of metoclopramide on motility of the gastrointestinal tract. The simultaneous use of metoclopramide may reduce the effect of cimetidine due to the reduction of its absorption.

Overdose.

Symptoms: hypersomnia, confusion, extrapyramidal disorder.

Treatment: discontinuation of the drug (symptoms disappear within 24 h after administration).

Dosing and Administration.

Inside, / m, I /. Adults: inside-5-10 mg 3 times a day before meals; v/m or/in- 10 mg; The maximum single dose - 20 mg, maximum daily - 60 mg (for all routes of administration). Children over 6 years are 2.5-5 mg 1-3 times a day, children under 6 years-0.5-0.1 mg/kg/day; The maximum single dose - 0,1 mg / kg. Patients with hepatic and / or renal insufficiency initial dose reduced 2 times, subsequent dose depends on the individual response of the patient.

Precautions.

Patients, having an increased sensitivity to procaine or procainamide, may be sensitive to metoclopramide.

Duration of therapy should not exceed 12 Sun.

There should be appointed after operations on the gastrointestinal tract (such as intestinal anastomosis or pyloroplasty), because muscle contractions hinder the healing of joints.

Metoclopramide can be administered to patients with a history of depression only in case, if the expected benefit outweighs the potential risk.

Extrapyramidal disorders may occur when using metoclopramide in therapeutic doses in patients of any age (cm. and "Side Effects"). But more often they occur when high doses. Extrapyramidal symptoms, voice, mainly, both acute dystonic reactions, manifested in the first 24-48 hours of treatment, more frequent in adolescents and adults younger than 30 years.

Parkinsonian symptoms were noted typically within the first 6 months after starting treatment, but could occur later and over a longer period of time. These symptoms disappear, usually, for 2-3 months after discontinuation of metoclopramide.

Tardive dyskinesia occurs more frequently in elderly patients, especially in women. The appearance of signs or symptoms of tardive dyskinesia is typically observed after continuous treatment for at least 1 years and may persist after discontinuation.

Against the backdrop of metoclopramide may distort laboratory indicators — such as the functional liver samples, prolactin and aldosterone levels in the serum.

During treatment, metoclopramide should not drink alcoholic beverages in order to avoid the risk of complications.

Consideration should be given the possibility of reducing the increase concentration and reaction time during treatment (better to give up driving and working with potentially dangerous equipment).

Cooperation