Domrid of a tablet

General characteristics. Structure:

Active ingredient: domperidone maleate; 1 tablet contains a domperidon of a maleate is equivalent to a domperidon of 10 mg.

Auxiliary veshchestva:mikrokristallichesky cellulose, croscarmellose sodium, silicon dioxide colloid anhydrous, magnesium stearate, a covering of Opadry II 31 G 58920 white which contains lactose, monohydrate; titanium dioxide (E171).

Pharmacological properties:

Domperidon is the antagonist of dopamine which has antiemetic properties. Practically does not get through a blood-brain barrier therefore use of a domperidon seldom is followed by extrapyramidal side effects, especially at adults, but домперидон stimulates release of prolactin from a hypophysis. Antiemetic action is caused by connection of peripheral (gastrokinetichesky) action and antagonism to dopamine receptors in a trigger zone of chemoceptors which is out of a blood-brain barrier.
At intake домперидон increases duration of antral and duodenal reductions, accelerates a passage on a stomach – an exit of liquid and semisolid fractions at healthy people and firm fractions at patients at whom this process was slowed down, and increases pressure of a sphincter of a lower part of a gullet at healthy people. Domperidon does not influence gastric secretion.

Domperidon is quickly absorbed at oral administration on an empty stomach with achievement of the maximum levels in a blood plasma in 30–60 min. Bioavailability of a domperidon at intake low (about 15%) due to intensive metabolism in a wall of intestines and in a liver.
Though at healthy people biological availability of a domperidon increases at reception after food, patients with disorders of digestive tract need to accept домперидон in 15–30 min. prior to food, at patients with reduced acidity of a stomach absorption of a domperidon decreases.

Biological availability at oral administration of drug decreases after the previous reception of Cimetidinum or sodium of bicarbonate.
Domperidon is metabolized in a liver by a hydroxylation and N-dealkylation. At researches of metabolism of the drug in vitro using diagnostic inhibitors it was revealed that the isoenzyme of CYP3A4 is the main isoenzyme of system of P450 cytochrome which takes part in process of N-dealkylation of a domperidon whereas isoenzymes of CYP3A4, CYP1A2 and CYP2E1 take part in process of an aromatic hydroxylation of a domperidon.
Linkng with proteins of a blood plasma makes 91–93%. It is removed with urine (31%) and a stake (66%). In an invariable look only the insignificant amount of drug is removed (10% – with a stake and about 1% – with urine). The semi-maintaining period after one-time reception makes 7–9 hours of a blood plasma, but can increase at a heavy renal failure.

Indications to use:

Complex of dispepsichesky symptoms which often is associated with the slowed-down stomach excrement, a gastrofood reflux, an esophagitis: feeling of overflow of a stomach, feeling of gastric flatulence, pain in an upper part of a stomach;
eructation, meteorism; nausea, vomiting; heartburn with an eructation to contents of a stomach or without it.
Nausea and vomiting of a functional, organic origin, owing to meal, and also caused by radiation or medicinal therapy. The specific indication is the nausea and vomiting caused by dopamine agonists in case of use at Parkinson's disease (a levodopa, бромкриптин).

Route of administration and doses:

 It is recommended to accept Domrid® orally to food. At administration of drug after food absorption is a little slowed down. At chronic dyspepsia:
- to adults and children 12 years are more senior it is recommended to accept Domrid® on 1 tablet (10 mg) 3 times a day in 15–30 min. prior to food and in case of need – before going to bed. If necessary the specified dose can be doubled. The maximum daily dose – 2,4 mg on 1 kg of body weight, but is no more than 80 mg. At an acute and subacute state (nausea and vomiting):
- to adults and children 12 years are more senior it is recommended to accept Domrid® on 2 tablets (20 mg) 3–4 times a day in 15–30 min. prior to food and in case of need – before going to bed, but it is no more than 80 mg in days.

Features of use:

At simultaneous use of antiacid or anti-secretory drugs they need to be accepted after food, but not to food, i.e. they should not be accepted along with the drug Domrid®.
With care it is necessary to appoint Domrid® the patient with a liver failure, considering high extent of metabolism of a domperidon in a liver. At long therapy patients have to be under regular observation.
At patients with a heavy renal failure (serumal creatinine> of 6 mg / 100 ml, i.e.> 0,6 mmol/l) the elimination half-life of a domperidon increases. Nevertheless, as very small percent of drug is removed by kidneys in not changed look, there is hardly a need for correction of a single dose for patients with a renal failure. However at repeated appointment it is necessary to reduce the frequency of reception to 1 or 2 times a day, depending on weight of a renal failure, there can also be necessary a dose decline. At long therapy patients have to undergo regular inspections or the doctor has to watch the patient carefully.

Use during pregnancy or feeding by a breast.
Домрид® it is necessary to appoint during pregnancy only if its use by reasonably expected therapeutic effect and excludes risk.
During feeding by a breast use of Domrid® is possible if the expected advantage for mother exceeds potential risk for the child.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
Домрид® in therapeutic doses does not influence intellectual activity, ability to drive the car and to work with other mechanisms.

Children. Drug is contraindicated to children age up to 12 years.

Appropriate security measures at use.
It is not necessary to exceed the recommended dose or to independently extend the therapy course recommended by the doctor. In case of any unusual reactions throughout use of drug it is necessary to consult in addition with the doctor.

Side effects:

Side effect meets in isolated cases; special cases of enterospasms were observed. The extrapyramidal phenomena are seldom observed at children and extremely seldom at adults treatments, in itself right after the termination, disappear.
Домрид® can induce increase in level of prolactin in plasma. This giperprolaktinemiya can stimulate such neuroendocrinal phenomena as a galactorrhoea and a gynecomastia and an amenorrhea in isolated cases.
At an underdeveloped blood-brain barrier (for example, at children) or its disturbances it is impossible to exclude possibility of neurologic side effects completely.
Allergic reactions were extremely seldom observed: skin rash, skin itch.

Interaction with other medicines:

Anticholinergic drugs can neutralize anti-dispeptic action of Domrid®.
It is not necessary to accept antiacid and anti-secretory drugs along with Domrid® as they reduce its bioavailability. The main way of metabolic transformations of a domperidon oposredstvutsya by P450 cytochrome.
At simultaneous use of a domperidon with P450 cytochrome inhibitors (antifungal drugs of an azolovy row, antibiotics of group of macroleads, HIV protease inhibitors, нефазодон) increase in level of a domperidon in plasma is possible.
In researches of interaction of a domperidon and ketokonazol it is shown that at combined use of a domperidon in a dose of 10 mg 4 times a day and a ketokonazol in a dose of 200 mg 2 times a day are observed lengthening of an interval of QT on 10–20 ms. At monotherapy domperidony both in similar doses, and at reception of a daily dose of 160 mg (that exaggerates the most admissible daily dose twice) clinically significant changes of an interval of QT were not noted.
Digoxin or paracetamol at a concomitant use of a domperidon does not influence the level of these drugs in blood.
Домрид® it is possible to combine with neuroleptics which action it strengthens; agonists of dopaminergic receptors (Bromocriptinum, a levodopa) which undesirable peripheral effects, such as digestion disturbance, nausea, vomiting it oppresses without neutralization of the main properties.

Contraindications:

Hypersensitivity to drug and its components.
Gastrointestinal bleeding, mechanical impassability or perforation of intestines at which stimulation of motive function of a stomach can be dangerous.
The prolactin-cosecreting tumor of a hypophysis (prolaktinom).
Concomitant use of peroral forms of a ketokonazol.
Children's age up to 12 years.

Overdose:

Symptoms: drowsiness, a disorientation and extrapyramidal reactions, especially at children.
Treatment: use of absorbent carbon and observation of the doctor. Anticholinergics, drugs which are used for treatment of parkinsonism or antihistaminic drugs can be effective at emergence of extrapyramidal reactions.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister; on 1 or 3 blisters in cardboard packaging.