Metoclopramide-acres

Active material: Metoclopramide
When ATH: A03FA01
CCF: Antiemetic drugs of the central action, blocking dopamine receptors
When CSF: 11.06.02
Manufacturer: Chemical-pharmaceutical plant AKRIKHIN OJSC (Russia)

Pharmaceutical form, composition and packaging

Pills white or white with a yellowish tint, Valium, chamfered; tolerance of marbling.

Excipients: lactose, potato starch, colloidal silicon dioxide, magnesium stearate.

10 PC. – packings Valium planimetric (5) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Antiemetic, reduces nausea, hiccups; stimulates peristalsis of the digestive tract. Antiemetic effect due to blockade of dopamine D₂-receptors and increase the threshold chemoreceptor trigger zone, It is a blocker of serotonin receptors. It is believed, that metoclopramide inhibits the relaxation of smooth muscles of the stomach, caused by dopamine, thus enhancing cholinergic reaction gastrointestinal tract smooth muscle. It helps accelerate gastric emptying by preventing the relaxation of the body and increase the activity of the stomach antrum and upper small intestine. Decreases reflux contents into the esophagus by increasing the pressure of the esophagus sphincter at rest and improves the acids of esophageal clearance by increasing the amplitude of its peristaltic.

Metoclopramide stimulates the secretion of prolactin and causes a transient increase in circulating levels of aldosterone, which may be accompanied by short-term fluid retention.

Pharmacokinetics

After ingestion is rapidly absorbed from the gastrointestinal tract. Plasma protein binding is about 30%. Biotransformed in the liver. Write mainly kidneys in an unmodified form, as well as metabolites. T_1/2 It is between 4 to 6 no.

Testimony

Vomiting, nausea, hiccups of various origins. Atonia and hypotonia of the stomach and intestines (incl. Postoperative); biliary dyskinesia; reflux esophagitis; flatulence; in the complex treatment of acute gastric ulcer and duodenal ulcer; acceleration of peristalsis during gastrointestinal radiocontrast studies.

Dosage regimen

Adults inside – by 5-10 mg 3-4 times / day. Vomiting, severe nausea administered metoclopramide / m or / dose 10 mg. Intranasal – by 10-20 mg in each nostril 2-3 times / day.

The maximum dose: single ingestion – 20 mg; daily – 60 mg (for all routes of administration).

The average single dose for children over 6 s is 5 mg 1-3 times / day orally or parenterally. For children under the age of 6 years of daily dose for parenteral administration is 0.5-1 mg / kg, frequency of administration – 1-3 times / day.

Side effect

From the digestive system: at the beginning of treatment may be constipated, diarrhea; rarely – dry mouth.

CNS: at the beginning of treatment may be feeling tired, drowsiness, dizziness, headache, depression, akathisia. Perhaps the emergence of extrapyramidal symptoms in children and young adults (even after a single application of metoclopramide): spasm of the facial muscles, hyperkinesis, spasmodic torticollis (usually, held immediately after the discontinuation of metoclopramide). With prolonged use, more frequently in elderly patients, possible effects of Parkinson's disease, dyskinesias.

From the hematopoietic system: early treatment possible agranulocytosis.

On the part of the endocrine system: rarely, long-term use in high doses – galactorrhea, gynecomastia, menstrual irregularities.

Allergic reactions: rarely – skin rash.

Contraindications

Bleeding from the gastrointestinal tract, Mechanical bowel obstruction, perforation of the stomach or intestines, pheochromocytoma, extrapyramidal disorders, epilepsy, prolaktinozavisimыe opuholi, glaucoma, pregnancy, lactation, concurrent use of anticholinergic drugs, Hypersensitivity to metoclopramide.

Pregnancy and lactation

Contraindicated during pregnancy.

When used in lactation (breast-feeding) should be considered, metoclopramide that passes into breast milk.

IN experimental studies not established adverse effects on the fetus of metoclopramide.

Cautions

To use caution in patients with asthma, hypertension, impaired liver and / or kidney, Parkinson's disease.

With extreme caution should be used in children, especially young children, because they have much higher risk of dyskinetic syndrome. Metoclopramide in some cases it may be effective for vomiting, caused by taking cytostatics.

When applied in elderly patients should be borne in mind, that long-term use of metoclopramide in high doses or medium most common side effects are extrapyramidal disorder, especially parkinsonism and tardive dyskinesia.

Against the background of metoclopramide may be distorted data in laboratory parameters of liver function and determine the concentration of aldosterone and prolactin in the blood plasma.

Effects on ability to drive vehicles and management mechanisms

During treatment should avoid potentially hazardous activities, requiring attention, fast psychomotor reactions.

Drug Interactions

In an application with anticholinergics possible mutual weakening effects.

While the use of neuroleptics (especially phenothiazine series and derivatives of butyrophenone) increased risk of extrapyramidal reactions.

In an application enhanced absorption of acetylsalicylic acid, Paracetamol, ethanol.

Metoclopramide in / introduction increases the absorption rate of diazepam and increases its maximum concentration in plasma.

In an application with a slowly dissolving dosage form may be reduced digoxin concentration of digoxin in the blood serum 1/3. While the use of digoxin in a liquid dosage form or in the form of a rapidly dissolving dosage forms of interaction were observed.

In an application with accelerated absorption of zopiclone zopiclone; with cabergoline – may decrease the effectiveness of cabergoline; ketoprofen – reduced bioavailability of ketoprofen.

Due antagonism of dopamine receptors may reduce metoclopramide antiparkinsonian action of L-dopa, thus may increase the bioavailability of levodopa due to its accelerated gastric emptying under the influence of MCP. The results are ambiguous interaction.

At simultaneous application with Valium accelerated absorption of mexiletine; with mefloquine – mefloquine absorption rate increases and its concentration in blood plasma, thus it is possible to reduce the side effects.

While the use of morphine faster absorption when administered morphine and enhanced its sedative effect.

In an application with nitrofurantoin reduced absorption of nitrofurantoin.

When using metoclopramide immediately prior to administration of propofol or thiopental may be required to reduce their induction doses.

Patients, receiving metoclopramide, amplify and prolong the effects of suxamethonium chloride.

In an application with tolterodinom decreases the effectiveness of metoclopramide; with fluvoxamine – described the case of extrapyramidal disorders; fluoxetine – there is a risk of extrapyramidal disorders; Cyclosporin – increases absorption of cyclosporin and increase its concentration in the blood plasma.