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

Pharmacodynamics:Antiemetic, is a specific blocker of dopamine (D₂) and serotonin receptors. Eliminates nausea and hiccups.Reduces the motor activity of the esophagus, increases the tone of the lower sphincter of the esophagus, accelerates the emptying of the stomach, and accelerates the movement of food through the small intestine, without causing diarrhea. Stimulates the secretion of prolactin. The onset of action on the gastrointestinal tract occurs after 1-3 min. after intravenous administration and after 10-15 minutes. after intramuscular injection and is manifested by accelerating the evacuation of stomach contents and antiemetic effect.

Pharmacokinetics:The maximum concentration (C_max) in the blood is observed 1-2 hours after taking the drug. Half-life time (T_1/2) - 3-5 hours, with a violation of kidney function - up to 14 hours Excretion occurs mainly through the kidneys for 24 hours in unchanged form and as conjugates. Passes through the placental barrier and the blood-brain barrier, penetrates into the mother's 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:

-Increased sensitivity to metoclopramide and components of the drug;

- gastrointestinal bleeding, 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;

- Late dyskinesia, which developed after treatment with neuroleptics or metoclopramide in history;

- Epilepsy (increased frequency and severity of seizures);

- Parkinson's disease;

- simultaneous use with levodopa and agonists dopamine receptors;

- Methemoglobinemia due to metoclopramide or nicotinamide adenine dinucleotide (NADH) deficiency of cytochrome b5 in history;

- prolactinoma or prolactin-dependent tumor:

- Children's age up to 1 year;

- pregnancy III trimester;

- the period of breastfeeding.

Carefully:When used in elderly patients, impaired cardiac conduction (including prolongation of the QT interval),disturbance of the water-electrolyte balance, bradycardia, with the use of other drugs that extend the QT interval, arterial hypertension, concomitant neurological diseases, with medications affecting the central nervous system, depression (history), renal failure of moderate and severe severity (KK15- 60 ml / min), hepatic failure of severe severity, pregnancy (I-II trimesters).

Pregnancy and lactation:Metoclopramide can be used during pregnancy (I-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), when metoclopramide is used at the end of pregnancy, it is impossible to exclude the possibility of developing extrapiramid 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:

Intravenously (intravenously) and 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 is administered up to three times a day. To enhance peristalsis when carrying out radiogenic contrast 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, with a subsequent 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 / ml 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 (QC less than 15 ml / min), the daily dose should be reduced by 75%.

In patients with moderate or severe renal insufficiency (KK 15-60 ml / min), the dose should be reduced by 50%.

Patients with hepatic impairment of severe severity should be reduced by 50%.

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

Overdose: Symptoms: hypersomnia, disorientation, extrapyramidal disorders, drowsiness, confusion, hallucinations, irritability, dizziness, cardiac and respiratory arrest, abdominal pain. Symptomatology disappears after discontinuation of the drug within 24 hours. 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, H1-histamine receptor blockers, antidepressants with sedative effect, barbiturates, clonidine and other drugs of these groups) can enhance the sedative effect under the influence of metoclopramide. Metoclopramide enhances the action of neuroleptics in relation to the extrapyramidal symptoms. With the concomitant use of metoclopramide and tetrabeine-nasin, there is a possibility of a dopamine deficiency, which can be accompanied by muscle spasm, difficulty in speaking 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. Exposure of metoclopramide increases with simultaneous use with potent inhibitors of CYP2D6 isoenzymes, for example, fluoxetine and paroxetine.With concomitant use of metoclopramide with atovaquine, the concentration of atovahona in plasma is significantly reduced (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 ethyl alcohol. The drug is not effective in vomiting vestibular genesis.

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 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 of the drug into neutral glass ampoules.

For 10 ampoules, together with instructions for medical use and a scarifier, the ampullum is placed in a cardboard bundle with cardboard partitions, or 5 or 10 ampoules are placed in a contour cell box made of a polyvinyl chloride film.

When using ampoules with a notch or a fracture ring, the scarifier is not inserted.On 1 or 2 contour acheikova packing together with the instruction on application place in a pack from a cardboard.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000282

Date of registration:17.02.2011 / 05.12.2016

Expiration Date:Unlimited

The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia

Manufacturer: & nbsp

ESKOM NPK, OAO Russia

Information update date: & nbsp09.05.2018

Illustrated instructions

Instructions

Metoclopramide-ESCOM (Metoclopramide-Eskom)