Metoklopramid-Darnitsa

General characteristics. Structure:

Active ingredient: metoclopramide; 1 tablet contains hydrochloride Metoclopramidum in terms of Metoclopramidum a hydrochloride anhydrous – 10 mg;

excipients: potato starch, lactoses monohydrate, cellulose microcrystallic, povidone, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Metoklopramid-Darnitsa – the specific blocker of dopamine (D2) and serotoninovy (5-HT3) receptors, oppresses chemoceptors of a trigger zone of a brainstem, weakens sensitivity of the visceral nerves transferring impulses to the emetic center. Through a hypothalamus and a parasympathetic nervous system exerts the regulating and coordinating impact on a tone and a physical activity of an upper part of digestive tract. Raises a tone of a stomach and intestines, accelerates gastric emptying, reduces гастростаз, interferes with a peloric and ezofagalny reflux, stimulates an intestines peristaltics. Has the expressed antiemetic effect at vomiting of various genesis (except vomiting of psychogenic and vestibular genesis). Normalizes department of bile, reduces a spasm of a sphincter of Oddi, without changing his tone, eliminates dyskinesia of a gall bladder. Does not render M-holinoblokiruyushchego, antihistaminic, antiserotoninovy and ganglioblokiruyushchy action, kidneys and a liver, on blood formation, secretion of a stomach and pancreas do not influence a tone of blood vessels of a brain, arterial pressure, breath function, and also. Stimulates prolactin secretion (like other blockers of dopamine receptors). Increases sensitivity of fabrics to acetylcholine.

Pharmacokinetics. After intake it is quickly and completely soaked up. The maximum concentration in a blood plasma is reached in 30–120 min. Bioavailability – about 50%. 13–30% of Metoclopramidum contact proteins of a blood plasma. Distribution volume – 3,5 l/kg. The therapeutic effect after intake and intravenous administration is identical. It is metabolized in a liver. An elimination half-life – 4–6 hour, at a chronic renal failure it increases to the 14th hour. With urine within 24–72 hour about 85% of the entered dose, about 30% in not changed look are excreted. Passes through hematoencephalic and placental barriers, it is allocated in breast milk.

 

Pharmaceutical characteristics.

main physical and chemical properties: tablets of color, white or white with a yellowish shade, a ploskotsilindrichesky form with a facet.

Indications to use:

Disturbances motor эвакуаторной functions of a stomach at gastritises, a round ulcer, diabetic paresis of a stomach, its postoperative atony, including after a stomach resection; gastoroezofagalny reflux; the vomiting and nausea caused by an anesthesia, radiation therapy, emetogenny chemotherapy, diseases of a liver and kidneys, a craniocereberal injury, migraine, foxglove drugs, antibiotics, morphine; functional dyspepsia, dyspepsia at cirrhosis, a cholecystopathy, chronic pancreatitis, uraemia; a hiccups and an eructation irrespective of a type of a basic disease; when conducting diagnostic testings (gastroscopy, duodenal sounding, radiodiagnosis of diseases of a stomach and duodenum).

Route of administration and doses:

Apply inside to adults and teenagers 14 years are more senior. Appoint on 1 tablet 3–4 times a day in 30 min. prior to food (the single dose makes 10 mg, a daily dose – 30–40 mg.

At a renal failure the dose of drug is selected depending on weight of a renal failure.

Clearance of creatinine – a dose of Metoklopramida-Darnitsa:

to 10 ml/min. – 10 mg once a day;

from 11 to 60 ml/min. – 15 mg a day: 10 mg in the first reception and 5 mg – in the second (Metoclopramidum drugs with a possibility of such dosage are used).

One course of treatment is enough to be conducted within 4–6 weeks. In some cases treatment can be continued up to 6 months.

Features of use:

Use during pregnancy or feeding by a breast. Metoclopramidum is contraindicated in І a pregnancy trimester. In ІІ and ІІІ trimesters it is possible to use drug only according to vital indications. During treatment it is necessary to stop feeding by a breast.

Children. Metoklopramid-Darnitsa do not appoint to children aged up to 14 years because of impossibility of an exact dosage.

With care apply at patients with a renal, liver failure, at arterial hypertension. Against the background of use of Metoklopramida-Darnitsa false results of functional hepatic tests and definition of concentration of Aldosteronum and prolactin in a blood plasma are possible.

During treatment it is not recommended to take alcohol.

Ability to influence the speed of reactions at control of motor transport or other mechanisms. During treatment it is necessary to refrain from control of motor transport and performance of the work requiring special attention and speed of psychomotor reactions.

Side effects:

The majority of side effects arises during the 36th hour from an initiation of treatment and disappear during the 24th hour after cancellation of Metoklopramida-Darnitsa.

Extrapyramidal frustration, parkinsonism (a hyperkinesia, muscular rigidity – manifestation dopamine - the blocking action) at children and teenagers increases at exceeding of a daily dose of 0,5 mg/kg of body weight. A spasm of facial muscles, a lockjaw, a rhythmic protrusion of language, bulbar type of the speech, a spasm of extraocular muscles (including okulogirny crises), unnatural provisions of the head and shoulders, an opisthotonos, a muscle hyper tone. Drowsiness, fatigue, concern, confusion, a headache, a sonitus, dyspepsia, dryness in a mouth, a small tortoiseshell, a gynecomastia, a galactorrhoea.

At prolonged treatment of Metoklopramidom-Darnitsa at patients of advanced age Parkinsonism develops.

Interaction with other medicines:

At use of Metoclopramidum and neuroleptics (especially fenotiazinovy number and derivatives of phenyl propyl ketone) the risk of emergence of extrapyramidal symptoms increases. Metoklopramid-Darnitsa strengthens absorption of acetylsalicylic acid, paracetamol, ethanol, a levodopa, tetracycline, ampicillin; reduces digoxin absorption. At use with Cimetidinum decrease in efficiency of the last because of disturbance of its absorption is possible.

Contraindications:

Hypersensitivity to Metoclopramidum. Gastrointestinal bleedings, intestinal impassability, perforation of a digestive tract; a pheochromocytoma, epilepsy, glaucoma, extrapyramidal frustration, Parkinson's disease, prolaktino-dependent tumors, vomiting against the background of treatment or overdose by neuroleptics, vomiting at patients with cancer of a mammary gland. First trimester of pregnancy, feeding period breast.

Overdose:

Overdose symptoms: drowsiness, motive concern, spasms, extrapyramidal and motor frustration, dysfunction of cardiovascular system with bradycardia.

Treatment: Drug withdrawal. Apply caffeine, anticholinergic protivoparkinsotichesky means or benzodiazepine to drug treatment of overdose. Watch the vital functions before complete cessation of symptoms of poisoning.

Storage conditions:

Period of validity. 4 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, on 5 blister strip packagings in a pack.