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

An antiemetic, a specific blocker of dopamine (D2) and serotonin (5-HT3) receptors, depresses the chemoreceptors of the trigger zone of the brainstem, weakens the sensitivity of the visceral nerves that transmit impulses from the pylorus to the vomiting center. Through the hypothalamus and the parasympathetic nervous system (innervation of the gastrointestinal tract) has a regulating and coordinating effect on the tone and motor activity of the upper gastrointestinal tract (including the tone of the lower sphincter of the esophagus). Increases the tone of the stomach and intestines, accelerates the emptying of the stomach, reduces the hyperacid stasis, prevents pyloric and esophageal reflux, stimulates intestinal peristalsis. Normalizes the separation of bile, reduces the spasm of the sphincter of Oddi. Without changing its tone, it eliminates dyskinesia of the gallbladder. Does not affect the tone of the blood vessels of the brain, blood pressure, respiratory function, as well as nochek and liver, on hematopoiesis, gastric and pancreas secretion. Stimulates the secretion of prolactin.

Increases the sensitivity of tissues to acetylcholine, (the action does not depend on vagal innervation, but is eliminated by holinoblokatorami).Stimulating the secretion of aldosterone, enhances the retention of sodium ions and the excretion of potassium ions. The onset of action on the gastrointestinal tract is noted 1-3 minutes after intravenous administration, 10-15 minutes after intramuscular injection and is manifested by accelerating the evacuation of the stomach contents (approximately from 0.5-6 hours depending on the route of administration) and antiemetic effect ( lasts 12 hours).

Pharmacokinetics:The connection with plasma proteins is about 30%. It is metabolized in the liver. The half-life period (T1 / 2) is 3-5 hours, with renal dysfunction up to 14 hours. Removal of the drug 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 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 or intestine, 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 taking metoclopramide or a deficiency of nicotinamide adenine dinucleotide (NADH) cytochrome b5 in the anamnesis; prolactinoma or prolactin-dependent tumor; children under 1 year; 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,when taking other drugs that extend the QT interval, arterial hypertension, concomitant neurological diseases, when taking drugs that affect the central nervous system, depression (in the 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-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 of 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:

From the nervous system: extramedramidal disorders - spasm of facial musculature, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of extraocular muscles (including oculogic crisis), spastic torticollis, opisthotonus, muscular hypertonus; Parkinsonism (hyperkinesis, muscle rigidity is a manifestation of dopamine-blocking action, the risk of development in children and adolescents increases when the dose is exceeded 0.5 mg / kg / day); dyskinesia (in the elderly, with chronic renal failure); drowsiness, fatigue, anxiety, confusion, headache, tinnitus, asthenia, acacia, dystonia, impaired consciousness, convulsions, tardive dyskinesia, neuroleptic malignant syndrome, depression, hallucinations, confusion.

From the digestive system: constipation or diarrhea, dry mouth, nausea.

From the hematopoiesis: meghemoglobinemia, sulfgemoglobinemia, leukopenia, neutropenia, at the beginning of treatment, agranulocytosis is possible.

From the cardiovascular system: 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 increase in arterial pressure in patients with pheochromocytoma.

Allergic reactions: anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash).

From the endocrine system: with long-term admission in high doses - gynecomastia, galactorrhea, menstrual disorder, amenorrhea, hyperprolactinemia.

From the genitourinary system: polyuria, incontinence, sexual dysfunction, priapism.

Other: rarely (when used in high doses) - hyperemia of the nasal mucosa.

Overdose:Symptoms: hypersomnia, disorientation and extrapyramidal disorders, drowsiness, confusion, hallucinations, irritability,dizziness, bradycardia, changes in blood pressure, cardiac and respiratory arrest, abdominal pain. Symptomatology disappears after discontinuation of the drug within 24 hours. If necessary, treatment with holinoblokatorami and progivoparkinsonicheskimi means. There is no specific antidote.

Interaction:

Strengthens the action of ethanol on the central nervous system, the sedative effect of hypnotics, increases the effectiveness of therapy with H2-histamin blockers. Increases the absorption of diazepam, tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol; slows the absorption of digoxin and cimetidine.

With simultaneous use with neuroleptics, the risk of developing extrapyramidal symptoms increases.

The action of metoclopramide may weaken the anticholinesterase drugs. Contraindicated simultaneous use of metoclopramide with levodopa or dopamine receptor agonists in connection with the existing mutual antagonism. In connection with the inokinetic effect of metoclopramide, the 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. With the concomitant use of metoclopramide and tegrabenazine, 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 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.

It is not effective for vomiting of vestibular genesis.

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.

Most side effects occur within 36 hours of the start of treatment and take place within 24 hours after cancellation. Treatment should be as short as possible.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions.

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

Packaging:By 2 ml in ampoules of neutral colorless glass with a dot to indicate the location of the fracture. Each label is labeled or labeled with a quick-fixing paint. 10 ampoules per contour cell pack of PVC. One contour pack with instructions for use in a cardboard box.

Storage conditions:Store in a 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 the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000066

Date of registration:06.12.2010 / 21.03.2016

Expiration Date:Unlimited

The owner of the registration certificate:CES. Ouy Pharmaceutical Co. Ltd.CES. Ouy Pharmaceutical Co. Ltd. China

Manufacturer: & nbsp

CSPC OUYI PHARMACEUTICAL, Co.Ltd. China

Information update date: & nbsp09.05.2018

Illustrated instructions

Instructions

Metoclopramide-Vial (Metoclopramide-Vial)