|Metoclopramide 10 mg|
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Anti-emetic agent. Specific blocker of dopamine (D2) and serotonin (5-NTZ) receptors, inhibits chemoreceptors of brain stem trigger zone, impairs sensitivity of visceral nerves which transmit impulses from stomach and duodenum gatekeeper to vomiting center. Through hypothalamus and parasympathetic nervous system (innervation of gastrointestinal tract) it has regulatory and coordinating effect on tone and motor activity of upper GI tract (including tone of lower esophageal sphincter). Increases the tone of the stomach and intestines, accelerates gastric emptying, reduces hyperacidic stasis, prevents duodenopyloric and gastroesophageal reflux, stimulates intestinal peristalsis. Normalizes bile secretion, reduces spasm of sphincter of Oddi. Without changing its tone, it eliminates hypomotor type gall bladder dyskinesia. It does not affect blood vessel tone of the brain, blood pressure, respiratory function, as well as kidney and liver, hematopoiesis, secretion of the stomach and pancreas. Stimulates secretion of prolactin. Increases tissue sensitivity to acetylcholine (action does not depend on vagal innervation, but is eliminated by m-cholinoblockers). By stimulating aldosterone secretion, it increases sodium ion retention and potassium ion excretion.
Onset of action on gastrointestinal tract is noted 1-3 minutes after intravenous administration, 10-15 minutes after intramuscular administration and is manifested by accelerated evacuation of gastric contents (about 0.5-6 hours depending on route of administration) and antiemetic effect (lasts 12 hours).
Binding to plasma proteins is about 30%. It is metabolized in liver. Period of half-life is 4-6 hours, in case of impaired renal function - up to 14 hours.
Excretion of the drug mainly occurs through the kidneys during 24-72 hours in unchanged form and as conjugates. The drug passes through the placental and blood-brain barrier and penetrates into the mother's milk.
Contraindications to use
- bleeding from the gastrointestinal tract;
- gastric pylorus stenosis;
- mechanical intestinal obstruction;
- perforation of the gastric or intestinal wall;
- extrapyramidal disorders;
- Parkinson's disease;
- Prolactin-dependent tumors;
- vomiting against the background of treatment or overdose of neuroleptics and in patients with breast cancer;
- bronchial asthma in patients with hypersensitivity to sulfites (see section "Cautions");
- Pregnancy (1st trimester), lactation;
- early childhood (children under 2 years of age - contraindicated for the use of metoclopramide in any dosage form, children under 6 years of age - contraindicated for parenteral administration);
- Hypersensitivity to metoclopramide or any of the drug components.
Do not prescribe after gastrointestinal surgery (such as pyloroplasty or bowel anastomosis) because vigorous muscle contractions impede healing.
If you are hypersensitive to metoclopramide or other components of the drug, consult your physician before taking it.
Caution: bronchial asthma, arterial hypertension, Parkinson's disease, renal and/or hepatic insufficiency, older age (over 65 years), childhood (increased risk of dyskinetic syndrome).
Use during pregnancy and lactation
Metoclopramide is contraindicated for use in the first trimester of pregnancy. It is possible to use in II and III trimesters of pregnancy only under vital indications.
If it is necessary to apply the drug during lactation, it is necessary to decide on stopping breast-feeding.
Administration in liver function abnormalities
Caution: liver failure. Patients with clinically significant hepatic insufficiency should be prescribed a dose half as large as usual; the further dose depends on individual reaction of a patient to metoclopramide.
Administration in renal dysfunction
Caution: renal failure. Patients with clinically significant renal insufficiency prescribe a dose half as much as usual; further dose depends on individual patient's reaction to metoclopramide.
Administration in children
Contraindicated in early childhood (in children under 2 years of age - use of metoclopramide in any dosage form is contraindicated; in children under 6 years of age - parenteral administration is contraindicated).
Administration in children causes an increased risk of dyskinetic syndrome.
Administration in elderly patients
Caution: advanced age (over 65 years).
Indications of the drug Metoclopramide
- Vomiting, nausea, hiccups of various genesis (in some cases, it may be effective for vomiting caused by radiation therapy or cytostatics);
- Atony and hypotonia of the stomach and intestines (in particular, postoperative);
- biliary dyskinesia of the biliary tract by hypomotor type;
- reflux esophagitis;
- Functional stenosis of the pylorus;
- in the complex treatment of acute exacerbations of gastric ulcer and duodenal ulcer;
- used to enhance peristalsis during X-ray contrast studies of the gastrointestinal tract;
- as a means to facilitate duodenal probing (to accelerate gastric emptying and food movement through the small intestine).
Intravenously or intramuscularly.
In adults, 10-20 mg 1-3 times a day (maximum daily dose is 60 mg). For children over 6 years old - 5 mg 1-3 times per day.
For prevention and treatment of nausea and vomiting caused by cytostatics and radiotherapy, the drug is administered intravenously in a dose of 2 mg/kg of body weight 30 min before cytostatics or radiotherapy, repeated for 2-3 hours if necessary.
Before radiological examination in adults, 10-20 mg intravenously administered 5-15 min before the examination.
Patients with clinically significant hepatic and/or renal insufficiency are prescribed a dose half the usual one; the subsequent dose depends on the patient's individual response to metoclopramide.