Composition and release form
The drug is dispensed in the form of tablets and solution for injection.
The active ingredient is metoclopramide hydrochloride. Excipients:
- Saline.
- Acetic acid.
- Water for injections.
- Sodium sulfite.
- Edetate disodium.
Sold without a doctor's prescription. The cardboard package contains 1 bottle of clear liquid or 1-5 blisters of 10 tablets with attached instructions.
Shelf life 2 years. Optimal conditions are temperatures up to +25 C, in a dark place, away from children.
pharmachologic effect
Metoclopramide is a serotonin and dopamine receptor antagonist. It has a pronounced anti-hiccup, antiemetic and prokinetic effect. Stimulates intestinal motility in the upper section and regulates sphincter function.
The drug improves the tone of muscle contractions of the stomach, helps relax the duodenum and helps speed up the digestion process. It also has a positive effect on the functioning of the gallbladder, eliminating its disorder.
The antiemetic therapeutic effect is based on the suppression of dopamine receptors in the peripheral and central regions. Therefore, the medicine is effective in suppressing nausea and the gag reflex of various natures, namely due to anesthesia, chemotherapy, and taking certain groups of drugs when side effects occur.
The drug inhibits the effect of apomorphine, increasing the production of prolactin and increasing the content of aldosterone. Therefore, there is a temporary retention of fluid in the body.
When administered orally, the medicine is quickly absorbed into the bloodstream and reaches its maximum therapeutic effect after 1-2 hours. The overall bioavailability is 80%.
The half-life is 6 hours, in case of kidney disease it increases to 14 hours.
When the drug is administered by injection, the pharmacological effect is observed 1-3 minutes after intravenous administration and 15 minutes after intramuscular administration. Duration is 2 hours.
Instructions for use METOCLOPRAMIDUM
In patients with a history of depression, especially moderate or severe depression, accompanied by suicidal tendencies, a relapse of the disease may occur during treatment with metoclopramide. Before starting treatment, it is necessary to weigh the ratio of the potential benefits of treatment to the possible risks.
During the first 24-48 hours of treatment with metoclopramide, extrapyramidal symptoms may appear in the form of disturbances in muscle tone, dystonic movements, paroxysmal dystonia, and spasmodic torticollis. These symptoms most often occur in children and people under 30 years of age, and also after using metoclopramide to prevent vomiting caused by cancer chemotherapy.
During the first 6 months of treatment with metoclopramide, symptoms of parkinsonism may appear. These symptoms disappear within 2-3 months after discontinuation of the drug product.
Elderly patients, especially women, treated with metoclopramide may experience dyskinesias, often irreversible. These symptoms occur less frequently during short-term treatment using lower doses of the drug product.
In patients with impaired renal function, hypokalemia may occur during treatment with metoclopramide because the drug increases plasma aldosterone concentrations and decreases sodium excretion.
In patients with hypertension treated with MAO inhibitors, metoclopramide potentiates the effect of MAO inhibitors.
Metoclopramide causes a transient increase in plasma aldosterone levels. This can lead to fluid retention in the body, especially in patients with cirrhosis or congestive heart failure. If these symptoms are observed during the first weeks of treatment with metoclopramide, the drug should be discontinued.
In vitro studies have shown that about 1/3 of breast tumors depend on prolactin levels. Metoclopramide increases prolactin levels, so the drug should be used with great caution in patients with a history of breast neoplasm.
IV administration of diluted metoclopramide should continue for at least 15 minutes.
Influence on the ability to control transport or other mechanisms
Metoclopramide may cause CNS side effects such as:
- drowsiness and dizziness, which impair psychophysical performance. Therefore, it is necessary to inform the patient about the dangers associated with driving motor vehicles and servicing moving mechanisms.
Indications
Clinical conditions for which metoclopramide is indicated are:
- Nausea.
- Vomiting of various origins.
- Dysfunction of the digestive system.
- Atony and hypotension of the intestines and stomach.
- Postoperative gastrointestinal disorders.
- Increased gas formation.
- The period of exacerbation of ulcerative pathology of the gastrointestinal tract.
- Preparation for examination of the digestive system.
- Diseases of the biliary tract.
Mode of application
Depending on the form of the drug, Metoclopramide has some application features:
- Oral method - take half an hour before meals, do not chew the tablets, be sure to wash them down with water. The maximum duration of treatment for vomiting and nausea is up to 5 days. Intervals between doses of the drug should be at least 6 hours. The dosage of the drug is calculated individually, according to age, body weight and pronounced clinical picture. Do not exceed the amount of medication above 0.5 mg/kg. The optimal adult dosage is 10 mg 3 times a day.
- Injection method - the drug is prescribed for a course of 5 days. The solution is administered intravenously or intramuscularly over 3 minutes. Dosage for adults: 10 mg once or 30 mg 3 times a day.
In childhood, the use of Metoclopramide is possible from 2 years of age. If you weigh less than 60 kg, 0.1-0.15 mg/kg of the drug is indicated three times a day. Children over 15 years old weighing more than 60 kg are prescribed 10 mg 3 times a day.
Elderly people should reduce the therapeutic dose, taking into account the deterioration of the liver and excretory system.
Patients with kidney pathologies should use the drug with caution. The dose is reduced by 75% or 50% depending on the condition.
If liver function is impaired, take 10 mg once, or reduce the dosage by half.
Instructions for use METOCLOPRAMIDUM tablets
In patients with a history of depression, especially moderate or severe depression, accompanied by suicidal tendencies, a relapse of the disease may occur during treatment with metoclopramide. Before starting treatment, it is necessary to weigh the ratio of the potential benefits of treatment to the possible risks.
In the first 24-48 hours of treatment with metoclopramide, extrapyramidal symptoms may appear in the form of disturbances in muscle tone, dystonic movements, paroxysmal dystonia, and spasmodic torticollis. These symptoms most often occur in children and people under 30 years of age, and also after using metoclopramide to prevent vomiting caused by cancer chemotherapy.
Within 6 months of treatment with metoclopramide, symptoms of parkinsonism may appear. These symptoms disappear 2-3 months after discontinuation of the drug product.
Elderly patients, especially women, treated with metoclopramide may experience dyskinesias, often irreversible. These symptoms are less common with short-term treatment using lower doses of the drug product.
In patients with impaired renal function, hypokalemia may occur during treatment with metoclopramide because the drug increases plasma aldosterone concentrations and decreases sodium excretion.
In patients with hypertension treated with MAO inhibitors, metoclopramide potentiates the effect of MAO inhibitors.
Metoclopramide causes a transient increase in plasma aldosterone levels. This can lead to fluid retention in the body, especially in patients with cirrhosis or congestive heart failure.
In vitro studies have shown that about 1/3 of breast tumors depend on prolactin levels. Metoclopramide increases prolactin levels, so the drug is contraindicated in patients with prolactin-dependent breast tumors.
The medicinal product contains lactose and should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or glucose-galactose malabsorption syndrome.
Impact on the ability to drive vehicles and operate machinery
Metoclopramide may cause undesirable CNS effects such as drowsiness and dizziness, which impair psychophysical performance. Therefore, it is necessary to inform the patient about the dangers associated with driving motor vehicles and servicing moving mechanisms.
Side effects
The antiemetic may cause the following side effects:
- Constipation, dry mouth, profuse diarrhea.
- Feelings of drowsiness, malaise, headache and dizziness during the initial period of therapy.
- Tension of the facial muscles.
- Symptoms of parkinsonism and dyskinesia with prolonged use.
- Hormonal imbalance.
- Allergic manifestations.
Metoclopramide
The frequency of adverse reactions is given according to the classification: very often (≥ 1/10); often (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (<1/10000); frequency unknown (frequency cannot be estimated from available data).
Blood and lymphatic system disorders:
frequency unknown - methemoglobinemia, probably associated with deficiency of the enzyme NADH-dependent cytochrome b5 reductase (especially in newborns), sulfhemoglobinemia (most often with the simultaneous use of high doses of sulfur-containing drugs).
Cardiac disorders:
infrequently - bradycardia; frequency unknown - cardiac arrest, which may be caused by bradycardia, atrioventricular block, sinus node block, prolongation of the QT interval on the electrocardiogram, ari.
Vascular disorders:
often - decreased blood pressure, frequency unknown - cardiogenic shock, acute increase in blood pressure in patients with pheochromocytoma.
Endocrine system disorders*
: infrequently - amenorrhea, hyperprolactinemia; rarely - galactorrhea; frequency unknown - gynecomastia.
* Endocrine disorders during long-term treatment are associated with hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia).
Gastrointestinal disorders:
often - diarrhea; rarely - dry mouth.
Immune system disorders:
uncommon - hypersensitivity reactions; frequency unknown - anaphylactic reactions (including anaphylactic shock).
Nervous system disorders:
very often - drowsiness; often - extrapyramidal disorders (especially in children and young patients and/or when recommended doses of the drug are exceeded, even after a single administration), parkinsonism, akathisia; infrequently - dystonia, dyskinesia, impaired consciousness; rarely - seizures, especially in patients with epilepsy; frequency unknown - tardive dyskinesia, sometimes persistent, during or after long-term treatment, especially in elderly patients, neuroleptic malignant syndrome.
Mental disorders:
often - depression; infrequently - hallucinations; rarely - confusion.
General disorders and disorders at the injection site:
often - asthenia.
Adverse reactions that are most common when using high doses of the drug:
— Extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonism syndrome, akathisia developed even after using a single dose of the drug, especially in children and young patients (see section “Special instructions”),
- Drowsiness, decreased level of consciousness, confusion, hallucinations.
Overdose
In case of non-compliance with the therapeutic dose, an overdose is possible. It manifests itself with a pronounced clinical picture in the form of nervous disorders. Hallucinations and unclear consciousness are noted.
Rarely - deterioration of the cardiovascular system with a decrease in blood pressure, the appearance of bradycardia, even cardiac arrest.
Signs of an overdose last a day after starting to take the drug.
Treatment based on symptoms, medication with monitoring of cardiac and respiratory function.
