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

Composition:One ampoule contains: active substance - metoclopramide hydrochloride in terms of 100% substance - 10.0 mg; Excipients: sodium chloride - 16.0 mg, sodium sulfite anhydrous 0.5 mg, disodium edetate (disodium ethylenediamine tetraacetic acid) 0.8 mg, propylene glycol 200.0 mg, 0.1 M hydrochloric acid solution to pH 4,5, water for injection - up to 2,0 ml.

Description:Transparent colorless liquid.

Pharmacotherapeutic group:Antiemetics - dopamine receptor blocker central

ATX: & nbsp

A.03.F.A Motility stimulators GIT

A.03.F.A.01 Metoclopramide

Pharmacodynamics: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 function of the upper parts of the digestive tract, mainly the stomach and duodenum, without affecting gastric and pancreatic secretion. Besides, metoclopramide 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 tract. Normalizes the separation of bile, reduces the spasm of the sphincter of Oddi. Without changing its tone, it eliminates dyskinesia of the gallbladder. Stimulates the secretion of prolactin and aldosterone. It enhances the retention of sodium ions and the excretion of potassium ions.

Pharmacokinetics:

The onset of action on the gastrointestinal tract is noted 1-3 minutes after intravenous administration and 10-15 minutes after intramuscular injection.

It is metabolized in the liver. Removal of the drug occurs mainly through the kidneys for 24-72 hours (85% of the dose), 30% unchanged. Easily penetrates through placental and blood-brain barrier, excreted in 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 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;

- tardive 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 deficiencynico-tinamidadenindinucleotide (NADH) of cytochrome-b5 in the anamnesis;

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, 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 the anamnesis), renal insufficiency of moderate and severe severity (QC 15-60 ml / min), hepatic failure of severe severity, pregnancy (I -11 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), 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:

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 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 (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%.

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, acute arterial pressure in patients with pheochromocytoma, amenorrhea, hyperprolactinaemia, galactorrhea, gynecomastia, polyuria, incontinence, heart failure, atrioventricular blockade, blockade of the sinus node, prolongation of the QT interval on the electrocardiogram, pirouette arrhythmia, , sexual dysfunction, priapism, anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash), drowsiness, asthenia, extrapyramidal usheniya, parkinsonism akataziya, dystonia, disturbance of consciousness, convulsions, tardive dyskinesia, neuroleptic malignant syndrome, depression, hallucinations, confusion.

Overdose:

Symptoms: hypersomnia, increase or decrease in blood pressure, dysfunction of the cardiovascular system with bradycardia, disorientation and extrapyramidal disorders, drowsiness, confusion, hallucinations, irritability, dizziness, cardiac and respiratory arrest, abdominal pain.

Symptomatology disappears after discontinuation of the drug within 24 hours.

Treatment: when severe poisoning extrapyramidal disorders can be quickly eliminated by slow intravenous administration of biperidene (doses for adults are 2.5-5 mg, for children 0.04 mg / kg body weight). 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 histamine 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 deficiency of dopamine, 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 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 should refrain from drinking alcohol.

In adolescents and patients with severe impairment of kidney function, there is an increased risk of side effects.

Against the background of the use of metoclopramide, there are possible distortions of these laboratory parameters of liver function and determination of the concentration of aldosterone and prolactin in plasma.

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 per ampoule of glass.

For 10 ampoules, together with a knife or scarifier for opening ampoules and instructions for medical use, put in a box of cardboard.

10 ampoules in a blister pack. For 1 blister pack together with a knife or scarifier for opening ampoules and instructions for medical use are placed in a pack of cardboard.

For 10 ampoules, together with a knife or scarifier for opening ampoules and instructions for medical use, put in a pack with a cardboard insert to fix the ampoules from the cardboard.

In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003722

Date of registration:12.07.2016

Expiration Date:12.07.2021

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp09.05.2018

Illustrated instructions

Instructions

Metoclopramide (Metoclopramide)