Domperidon - Teva

General characteristics. Structure:

1 tablet contains active agent домперидон (a domperidona a maleate) 10,0 (12,73) mg;
excipients: lactoses monohydrate of 50,00 mg, starch of corn 10,00 mg, sodium lauryl sulfate of 0,20 mg, novidon-K30 3,00 mg, cellulose of microcrystallic 23,32 mg, silicon dioxide of colloid 0,25 mg, magnesium stearate of 0,50 mg, cover (gipromelloza of 2,80 mg, пропилснгликоль 0,30 mg, talc of 0,70 mg, titanium mg HI 71 1,20 dioxide).

Description
 White or almost white round biconvex tablets, film coated, with an engraving of "Do 10" on one party. On cross section - a kernel of white color.

Pharmacological properties:

Pharmacodynamics. Domperidon - the blocker of dopamine receptors possessing antiemetic action. Antiemetic action is caused by a combination of peripheral (gastrokinetichesky) action and inhibition of receptors of dopamine in a trigger zone of the chemoceptors of a brain located out of a blood-brain barrier in the field of area postrema. At intake домперидон increases reduced pressure in a gullet, improves antroduodenal motility and accelerates gastric emptying, without having effect on gastric secretion. Domperidon increases secretion of prolactin in a hypophysis.

Pharmacokinetics. At intake on an empty stomach домперидон it is quickly absorbed, its maximum concentration in plasma are reached within 30-60 min. Low absolute biological availability after intake (about 15%) is caused by effect of "the first passing" through a liver. Though at healthy volunteers bioavailability of a domperidon increases at reception after food, patients with complaints from digestive tract should accept домперидон in 15-30 min. prior to food. At decrease in acidity of a gastric juice disturbance of absorption of a domperidon is observed. Preliminary reception of a tsimegidin and Natrii hydrocarbonas reduces bioavailability of a domperidon. At intake after food achievement of the maximum absorption requires a little bigger time.
At intake домперидон does not kumulirut and does not induce own exchange. Domperidon for 91-93% contacts proteins of a blood plasma. Domperidon is distributed in various body tissues, it is found in breast milk, but does not get through a blood-brain barrier. Concentration of a domperidon in breast milk makes 10-50% of concentration in a blood plasma.
Metabolism of a domperidon happens in a liver and in an intestines wall by a hydroxylation and N-dealkylation to participation of isoenzymes of CYP3A4, CYP1A2 and CYP2E1.
Domperidon is brought by intestines (66%) and kidneys (33%), including in not changed look (10% and 1% respectively). The elimination half-life makes 7-9 h.
Pharmacokinetics at special groups of patients
 At patients with concentration of serumal creatinine more than 0,6 mmol/l the elimination half-life makes from 7,4 to 20,8 h, at the same time concentration of a domperidon in a blood plasma is reduced.

Indications to use:

Dispepsichesky symptoms, such as nausea, vomiting, feeling of overflow in эпигастралыюй areas, discomfort in upper parts of a stomach and a regurgigation of gastric contents.

Route of administration and doses:

Inside before meal, washing down with enough water.
Adults and children with body weight more than 35 kg
1-2 tablets 3-4 times a day. The maximum dose makes 80 mg a day. Reception duration - 4 weeks. Further administration of drug is possible after consultation at the doctor.
Reduction of frequency of administration of drug to 1-2 times a day is recommended to patients with a renal failure.

Features of use:

Drug Domperidon - Teva contains lactose therefore patients should not appoint it with a lactose intolerance, a galactosemia or disturbance of absorption of glucose or a galactose.
As only very small amount of a domperidon is removed by kidneys in not changed look, correction of a single dose at patients with a renal failure is hardly necessary. At repeated appointment the frequency of dosing has to be reduced to 1-2 times a day depending on weight of insufficiency; also the dose decline can be required. At long therapy such patients have to be under regular observation. Administration of drug after food slows down its absorption.
Influence of a pas ability to management of transport and work with the equipment: does not influence.

Side effects:

Frequency of development of side reactions is classified according to WHO recommendations: seldom - not less than 0,01%, but less than 0,1%; very seldom - less than 0,01%, including isolated cases.
From immune system: very seldom - an anaphylaxis, including an acute anaphylaxis, a small tortoiseshell and a Quincke's disease.
From endocrine system: seldom - increase in concentration of prolactin.
From a nervous system: very seldom - extrapyramidal disturbances.
From the alimentary system: seldom - gastrointestinal frustration; very seldom - an enterospasm, diarrhea.
From skin and hypodermic fabrics: very seldom - an itch, rash.
From reproductive system and mammary glands: seldom - a galactorrhoea, a gynecomastia, an amenorrhea.

Interaction with other medicines:

M-holinoblokatory can neutralize action of a domperidon.
It is not necessary to accept antiacid and anti-secretory drugs along with domperidony as they reduce its biological availability after intake.
The concomitant use of powerful inhibitors of an isoenzyme of CYP3A4 can cause increase in concentration of a domperidon in plasma. Ketokonazol inhibits CYP3A4 - dependent primary metabolism of a domperidon therefore approximately triple increase in the maximum concentration of a domperidon and the area under a curve "concentration time" in a plateau phase is reached.
Inhibitors of an isoenzyme CYP3A4 are also following medicines:
• antifungal drugs of an azolovy row;
• antibiotics from group of macroleads;
• HIV protease inhibitors;
• нефазодон.
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 Q-T on 10-20 ms. At monotherapy domperidony both in similar doses, and at reception of the daily dose of 160 mg twice exceeding the most admissible clinically significant changes of an interval of Q-T were not noted.
Domperidon can influence absorption of at the same time used peroral drugs, in particular drugs with the slowed-down release of active agent, or the drugs covered with a kishechnorastvorimy cover. However use of a domperidon for patients against the background of reception of paracetamol or the picked-up therapy with digoxin did not influence concentration of these drugs in blood. Domperidon can be also combined with: • neuroleptics which action it does not strengthen;
• agonists of dopamine receptors (bromokrigpiny, a levodopa) which undesirable peripheral effects, such as digestion disturbances, nausea, vomiting, it suppresses, without neutralizing their main properties.

Contraindications:

• Hypersensitivity to a domperidon or any other component of drug.
• Prolaktinsekregiruyushchy tumor of a hypophysis (prolaktinom).
• Gastrointestinal bleeding.
• Perforation of digestive tract.
• Mechanical obstruction of intestines.
• Hereditary lactose intolerance, deficit of lactose or glyukozo-galaktozny malabsorption.
• Breastfeeding period.
• Children with body weight less than 35 kg.
With care Pregnancy, liver failure, renal failure.

Use during pregnancy and during breastfeeding
 Use of a domperidon during pregnancy is allowed only if the expected advantage for mother exceeds possible risk for a fruit. For the period of use of a domperidon breastfeeding should be suspended.

Overdose:

Symptoms of overdose include drowsiness, a disorientation and extrapyramidal frustration, especially at children.
Treatment
 There is no specific antidote. In case of overdose there can be effective a gastric lavage and use of absorbent carbon. Careful observation and a maintenance therapy is recommended.
For stopping of extrapyramidal disturbances also the drugs used for treatment of parkinsonism can appear effective m-holinoblokatory.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 4 years. Not to use after the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

Tablets, film coated, 10 mg.
On 10 tablets in blisters from PVC / aluminum foil; 1 or 3 blisters together with the application instruction in a cardboard pack.