Metoklopramid-Darnitsa

General characteristics. Structure:

Active ingredient: metoclopramide; 1 ml of solution contains Metoclopramidum a hydrochloride in terms of 100% anhydrous substance – 5 mg;

excipients: sodium chloride, dinatrium эдетат, sodium sulfite anhydrous, propylene glycol, 1 M Acidum hydrochloricum solution, water for injections.

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. Time of achievement of the maximum concentration in blood (TCmax) after intramuscular introduction makes 10 – 15 min. An elimination half-life (T1/2) – 3–5 h, at a renal failure – to 14 h. Removal of drug happens generally kidneys during 24 h in not changed look and in the form of conjugates. Passes through hematoencephalic and placental barriers, it is allocated in breast milk.

Pharmaceutical characteristics.

main physical and chemical properties: transparent, colourless liquid.

Incompatibility. Injection Metoklopramid-Darnitsa solution cannot be mixed with alkaline infusion solutions and other medicines.

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 intramusculary or intravenously (in the form of a slow injection, short-term or long infusion). As solvent use 0,9% solution of sodium of chloride, 5% glucose solution.

For intravenous jet administration the single dose of drug is parted in 10 ml of solvent, enter not less, than within 3 minutes.

For introduction in the form of short-term infusion the single dose of drug is parted in 50 ml of infusion solution, entered within 15 minutes.

To adults and teenagers 14 years are more senior appoint 2 ml 3–4 times a day (the single dose makes 10 mg, a sutochn a dose – 30–40 mg).

For children from 3 to 14 years the recommended single dose makes 0,1 mg/kg of body weight, the highest daily dose – 0,5 mg/kg of body weight.

Duration of a course of treatment is defined individually, depending on indications and the course of a disease. Generally one course is enough to be conducted within 4 – 6 weeks. Whenever possible it is necessary to pass to use of Metoklopramida-Darnitsa in tablets.

At a renal failure the dose of drug is selected according to 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 introduction and 5 mg – in the second.

At the nausea and vomiting caused by cytostatic means, drug is appointed:

– by short-term infusion (within 15 minutes) in a dose of 2 mg/kg of body weight for half an hour before introduction of cytostatic means, and also through 1,5; 3,5; 5,5; and 8,5 hours after use of cytostatic means;

– by long infusion at a dose of 0,5-1 mg/kg/h, beginning in 2 hours prior to use of cytostatic means, then in a dose of 0,25-0,5 mg/kg/h for 24 hours after use of cytostatic means.

Metoklopramid-Darnitsa apply during the entire period of treatment by cytostatic means.

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. Drug is used at children aged from 3 up to 14 years only according to vital indications.

Solution for injections of Metoklopramid-Darnitsa contains sodium sulfite which with hypersensitivity to sulfites can cause the hypersensitivity reaction which is shown nausea, a diarrhea, short wind, a bad attack of asthma, disturbance of consciousness or shock in patients with bronchial asthma.

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 36 h from an initiation of treatment and disappear during 24 h after cancellation of Metoklopramida-Darnitsa.

Extrapyramidal frustration, parkinsonism (a hyperkinesia, muscular rigidity – manifestation dopamine - the blocking action) at children and teenagers increase 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. Children's age up to 3 years.

Overdose:

Overdose symptoms: drowsiness, a motive unrest, 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 total disappearance 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 2 ml of solution in ampoules, on 5 or 10 ampoules in cardboard packaging.