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

Composition:Active substance: metoclopramide hydrochloride hydrate (in terms of anhydrous substance) - 5 g,
Excipients: sodium pyrosulfite (sodium sulphurous-
acid pyro) -0.075 g; sodium chloride - 8 g; disodium salt of ethylenediaminetetraacetic acid (Trilon B) 0.25 g; water for injection - up to 1000 ml.

Description:Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:Antiemetics - dopamine receptors 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-HTZ) receptors, inhibits chemoreceptors of the trigger zone of the brainstem,weakens the sensitivity of the visceral nerves that transmit the impulses from the pylorus to the vomiting center of the stomach and duodenum. 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 kidney and liver, on hematopoiesis, gastric and pancreatic 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 holinob locators). Stimulating the secretion of aldosterone, enhances the retention of sodium ions and elimination of ions.
The onset of action on the gastrointestinal tract is noted 1-3 minutes after intravenous administration, 10-15 minutes after intravenous administration and is manifested by the acceleration of evacuation of the stomach contents (approximately from 0.5 to 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 is 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 and blood-brain barrier and penetrates into the mother's milk.

Indications:Vomiting, nausea, hiccough of various genesis (in some cases can be effective in vomiting caused by radiation therapy or the use of cytotoxic drugs). Atony and hypotension of the stomach and intestines (in particular, postoperative); biliary dyskinesia; reflux esophagitis; flatulence; in the complex therapy of exacerbations of gastric ulcer and duodenal ulcer. It is used to enhance peristalsis during radiocontrast studies of the gastrointestinal tract.

Contraindications:Hypersensitivity, bleeding from the gastrointestinal tract, pyloric stenosis, mechanical intestinal obstruction, perforation of the stomach or intestines, pheochromocytoma, epilepsy, glaucoma, extrapyramidal disorders, Parkinson's disease, prolactin-dependent tumors, vomiting during treatment or overdose with antipsychotics and in breast cancer patients, pregnancy (I trimester), lactation period, early childhood (up to 2 years).

Carefully:Childhood age, renal / hepatic insufficiency, bronchial asthma, arterial hypertension, elderly age.

Pregnancy and lactation:The drug can be used in pregnancy only if the intended benefit to the mother exceeds the potential risk to the fetus.
Metoclopramide is excreted in breast milk, so the use of the drug during breastfeeding is contraindicated.

Dosing and Administration:Intravenous or intramuscular. Adults in a dose of 10-20 mg 1 -3 times a day (maximum daily dose - 60 mg); children older than 6 years of 5 mg 1-3 times a day; for children aged 2 to 6 years, the daily dose is 0.5-1 mg / kg body weight, the frequency of administration is 1-3 times.
For the prevention and treatment of nausea and vomiting due to the use of cytostatics or radiation therapy, the drug is administered intravenously at a dose of 2 mg / kg body weight 30 minutes before the use of cytostatics or radiation; if necessary, repeat the introduction after 2-3 hours.
Before the X-ray study, adults are administered intravenously 10-20 mg for 5-15 minutes before the study.
Patients with clinically expressed hepatic renal failure are prescribed a dose twice as low as usual, the subsequent dose depends on the individual reaction of the patient to metoclopramide.

Side effects:From the nervous system: extrapyramidal 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.
From the digestive system: constipation or diarrhea, rarely dry mouth.
Allergic reactions: hives.
From the endocrine system: rarely (with prolonged admission in high doses) - gynecomastia, galactorrhea, menstrual cycle.
Other: at the beginning of treatment, agranulocytosis is possible, rarely (when used in high doses) - hyperemia of the nasal mucosa.

Overdose:Symptoms: hypersomnia, disorientation and extrapyramidal disorders. As a rule, the symptomatology disappears after stopping the drug within 24 hours. If necessary, treatment with holinoblokatorami and antiparkinsonian means.

Interaction:Strengthens the action of ethanol on the central nervous system, the sedative effect of hypnotics, increases the effectiveness of therapy H₂-gastamin 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.

Special instructions: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.
During the use of the drug should be avoided potentially dangerous activities that require increased concentration of attention, rapid mental and motor reaction (driving vehicles, etc.).
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.
During the treatment with the drug, alcohol is not recommended.

Effect on the ability to drive transp. cf. and fur:During the use of the drug should be avoided potentially dangerous activities that require increased concentration of attention, rapid mental and motor reaction (driving vehicles, etc.).

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

Packaging:2 ml in neutral glass ampoules. 10 ampoules are placed in a box of cardboard. 5 ampoules per contour cell pack.For 1, 2 contour packs are laid in a pack of cardboard.
At 5, 10 ampoules are placed in a pack of cardboard with septa or gratings, or a separator made of cardboard or sack paper.
In each pack or box, insert the instructions for use and a knife for opening ampoules or an ampoule ceramic knife. When using ampoules with incisions, dots or rings, the ampoule opener is not inserted.

Storage conditions:In a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C.

Shelf life:5 years. Do not use after the expiry date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001657

Date of registration:30.11.2011 / 31.08.2015

Expiration Date:Unlimited

The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp2016-09-01

Illustrated instructions

Instructions

Metoclopramide (Metoclopramide)