Metoclopramide - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Metoclopramide is a specific blocker of dopamine (D2) and serotonin (5-HT3) receptors of the central nervous system,has a pronounced antiemetic effect (except for vomiting of psychogenic and vestibular origin), regulates tone and motor activity of the upper parts of the digestive tract, mainly the stomach and duodenum, without affecting gastric and pancreatic secretion. In addition, it increases the tone of the lower sphincter of the esophagus and reduces gastroesophageal reflux. The prokinetic effect of metoclopramide decreases in the distal direction of the digestive canal. The drug normalizes the secretion of bile, reducing spasm of the sphincter of Oddi, reduces dyskinesia of the gallbladder. Stimulates the secretion of prolactin. Increases tissue sensitivity to acetylcholine. Stimulates the secretion of aldosterone. It enhances the retention of sodium ions and the excretion of potassium ions.

Pharmacokinetics:The connection with plasma proteins is about 30%. It is metabolized in the liver. Half-life (T_1/2 ) - 4-6 hours, with renal dysfunction - up to 14 hours. Removal of the drug occurs mainly through the kidneys for 24-72 hours in unchanged form and in the form of conjugates. Passes through the placental barrier and the blood-brain barrier penetrates into breast milk.

Indications:

Adults. Prevention of postoperative nausea and vomiting. Symptomatic treatment of nausea and vomiting, including acute migraine. Prevention of nausea and vomiting caused by radiation therapy and chemotherapy. To enhance peristalsis in radiocontrast studies of the gastrointestinal tract.

Children. The second line of treatment for postoperative nausea and vomiting. The second line of prevention of delayed nausea and vomiting caused by chemotherapy.

Contraindications:Hypersensitivity to metoclopramide and components of the drug; gastrointestinal hemorrhage, mechanical intestinal obstruction, perforation of the wall of the stomach and intestines, conditions in which stimulation of the peristalsis of the gastrointestinal tract represents a risk; confirmed or suspected pheochromocytoma in connection with the risk of developing severe arterial hypertension; tardive dyskinesia, which developed after treatment with neuroleptics or metoclopramide in history; epilepsy (increased frequency and severity of seizures); Parkinson's disease; simultaneous application with levodopa and agonists of dopamine receptors; methemoglobinemia due to metoclopramide ordeficiency of nicotinamide adenine dinucleotide (NADH) cytochrome b5 in history; prolactinoma or prolactin-dependent tumor; children under 1 year; the period of breastfeeding.

Carefully:When used in elderly patients, cardiac conduction disorder (including prolongation of QT interval), disturbance of water-electrolyte balance, bradycardia, with the use of other drugs that extend the QT interval, arterial hypertension, concomitant neurological diseases, when taking drugs affecting the central nervous system, depression (in history), renal failure of moderate and severe severity (creatinine clearance 15-60 ml / min), hepatic failure of severe severity, pregnancy.

Pregnancy and lactation:Metoclopramide can be used during pregnancy (I and II trimesters) only if the potential benefit to the mother exceeds the potential risk to the fetus. In connection with the pharmacological features (like other neuroleptics), the use of metoclopramide at the end of pregnancy can not exclude the possibility of developing extrapyramidal symptoms in a newborn. Metoclopramide Do not use at the end of pregnancy (during the third trimester). Metoclopramide in small amounts excreted in breast milk. It is impossible to exclude the possibility of developing adverse reactions in the child. The use of metoclopramide during breastfeeding is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Intravenous (intravenously), intramuscularly (in / m).

In / in the drug should be administered bolus slowly (at least 3 minutes). To avoid an overdose, a minimum interval of 6 hours between administration of the drug should be observed.

Adults. Prevention of postoperative nausea and vomiting.

The recommended single dose is 10 mg.

Symptomatic treatment of nausea and vomiting, including acute migraine. Prevention of nausea and vomiting caused by radiation therapy and chemotherapy. The recommended single dose of 10 mg should be administered up to three times a day.

To enhance peristalsis in radiocontrast studies of the gastrointestinal tract.

Recommended IV bolus slow administration of 10-20 mg for 10 minutes before the start of the study.

The maximum daily dose is 30 mg or 0.5 mg / kg. The period of administration of the drug in the form of injections should be as short as possible, followed by a transition to a dosage form for oral administration.

Children age from 1 year to 18 years.

It is recommended IV bolus slow administration at a dose of 0.1-0.15 mg / kg up to 3 times a day. The maximum daily dose of 0.5 mg / kg / day. The maximum duration of metoclopramide for the prevention of postoperative nausea and vomiting is 2 days. To prevent nausea and vomiting caused by chemotherapy - 5 days. Elderly patients may need to reduce the dose due to a decrease in kidney and liver function.

In patients with terminal stage of renal failure (creatinine clearance less than 15 ml / min), the daily dose should be reduced by 75%. In patients with moderate or severe renal insufficiency (creatinine clearance 15-60 ml / min), the dose should be reduced by 50%. In patients with hepatic insufficiency of severe severity, the dose should be reduced by 50%.

Side effects:Nausea, diarrhea, constipation, methemoglobinemia, sulfgemoglobinemia, leukopenia, neutropenia,agranulocytosis, bradycardia, cardiac arrest, atrioventricular blockade, blockade of the sinus node, QT interval prolongation on the electrocardiogram, pirouette arrhythmia, lowering of arterial pressure, cardiogenic shock, acute blood pressure rise in patients with pheochromocytoma, amenorrhea, hyperprolactinaemia, galactorrhea, gynecomastia, polyuria, urinary incontinence, sexual dysfunction, priapism, anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash), drowsiness, and taenia, extrapyramidal disorders, Parkinsonism, akataziya, dystonia, disturbance of consciousness, convulsions, tardive dyskinesia, neuroleptic malignant syndrome, depression, hallucinations, confusion.

Overdose:

Symptoms: hypersomnia, disorientation, extrapyramidal disorders, drowsiness, confusion, hallucinations, irritability, dizziness, bradycardia, changes in blood pressure, cardiac and respiratory arrest, abdominal pain.

As a rule, the symptomatology disappears after stopping the drug within 24 hours.

Treatment: symptomatic, m-holinoblokatory, antiparkinsonian means. There is no specific antidote.

Interaction:Contraindicated simultaneous use of metoclopramide with levodopa or dopamine receptor agonists in connection with the existing mutual antagonism. Alcohol increases the sedative effect of metoclopramide. In connection with the prokinetic effect of metoclopramide, absorption of certain drugs may be impaired. M-holinoblokatory and derivatives of morphine have a mutual antagonism with metoclopramide in relation to the effect on peristalsis of the gastrointestinal tract. Drugs that depress the central nervous system (morphine derivatives, tranquilizers, H blockers₁-gistaminovyh receptors, antidepressants with sedative effect, barbiturates, clonidine and other drugs of these groups) may enhance the sedation effect of metoclopramide. Metoclopramide intensifies the action of neuroleptics in relation to extrapyramidal symptoms. With the concomitant use of metoclopramide and tetrabenazine, there is a possibility of a dopamine deficiency, which can be accompanied by muscle spasm,difficulties in speech and swallowing, anxiety, tremor, involuntary movements of muscles, including facial muscles. The use of metoclopramide with serotonergic drugs, for example, with selective serotonin reuptake inhibitors, increases the risk of developing serotonin syndrome (serotonin intoxication). Metoclopramide reduces the bioavailability of digoxin, increases the bioavailability of cyclosporine. The exposure of metoclopramide increases with simultaneous use with potent inhibitors of the CYP2D6 isoenzyme, for example, fluoxetine and paroxetine. With the simultaneous use of metoclopramide with atovahona significantly reduced the concentration of atovahona in blood plasma (about 50%). Metoclopramide increases the concentration of bromocriptine in the blood plasma, enhances the absorption of tetracycline, mexiletine and lithium, reduces the absorption of cimetidine.

Special instructions:

During the treatment with the drug is not recommended the use of ethanol.

In connection with the content of sodium sulfite in the preparation of metoclopramide should not be prescribed to patients with bronchial asthma with increased sensitivity to sulfites.Against the background of the use of metoclopramide, laboratory parameters of liver function and concentration of aldosterone and prolactin in plasma may be distorted. Treatment should be as short as possible.

Effect on the ability to drive transp. cf. and fur:During the treatment period it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for intravenous and intramuscular injection 5 mg / ml.

Packaging:

2 ml per ampoule of colorless neutral glass type I with a colored break ring or with a colored dot and a notch or without a kink ring, a colored dot and a notch. One, two or three color rings and / or a two-dimensional barcode, and / or alphanumeric coding, or without additional color rings, a two-dimensional bar code, or alphanumeric coding, can additionally be applied to the ampoules.

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film or without foil and without film.Or 5 ampoules are placed in a prefabricated form (tray) made of cardboard with cells for laying ampoules.

One or two contour squares or cardboard trays, together with the instruction for use and the ampoule ampoule or ampoule scarifier or ampoule ampoule and ampoule scarifier, are placed in a cardboard package.

20, 50 or 100 contour squares or cardboard trays with the appropriate number of instructions for use, and with an appropriate number of ampoule or ampoule ampoule scalers, or ampoule ampoules and ampoule scarifiers, are placed in boxes of corrugated cardboard with septa or grids (for inpatient).

One or two contour squares or cardboard trays, together with an instruction for use and a scarifier or knife, ampoule, or without a scarifier and a knife ampullum, are placed in a cardboard package (bundle).

20, 50 or 100 contour squares or cardboard trays with the appropriate number of instructions for use, and with an appropriate number of scarifiers or knives, ampoules, or without scarifiers and knives, the ampoules are placed in boxes of corrugated cardboard with partitions orgrids (for hospitals).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002769

Date of registration:17.12.2014 / 09.09.2015

Expiration Date:17.12.2019

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp09.05.2018

Illustrated instructions

Instructions

Metoclopramide (Metoclopramide)