Composition, form of production and packaging
? The tablets covered with a film shell of white or almost white color, round, biconcave, with engraving "Do 10" on one side; on the cross-section - the core of white color.
domperidone maleate 12.73 mg,
which corresponds to the content of domperidone 10 mg
Excipients: lactose monohydrate 50 mg, corn starch 10 mg, sodium lauryl sulfate 200 Ојg, povidone K30 3 mg, microcrystalline cellulose 23.32 mg, silicon dioxide colloid 250 Ојg, magnesium stearate 500 Ојg.
Sheath composition: hypromellose 2.8 mg, propylene glycol 300 Ојg, talc 700 Ојg, titanium dioxide (E171) 1.2 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
Domperidone is a blocker of dopamine receptors, which has an antiemetic effect. Antiemetic effect is due to a combination of peripheral (gastrokinetic) action and inhibition of dopamine receptors in the trigger zone of chemoreceptors of the brain located outside the blood-brain barrier in the area ofapostrema. When ingesting domperidone increases the reduced pressure in the esophagus, improves anthroduodenal motility and accelerates the emptying of the stomach, without exerting an effect on gastric secretion. Domperidone increases the secretion of prolactin in the pituitary gland.
When administered on an empty stomach, domperidone is rapidly absorbed, its C max in plasma is reached within 30-60 minutes. Low absolute bioavailability after oral administration (about 15%) is due to the effect of "first passage" through the liver. Although in healthy volunteers the bioavailability of domperidone increases with admission after meals, patients with gastrointestinal complaints should take domperidone 15-30 minutes before meals. With a decrease in the acidity of gastric juice, there is a violation of absorption of domperidone. Preliminary intake of cimetidine and sodium bicarbonate reduces the bioavailability of domperidone. When taken orally after a meal, it takes a little longer to achieve maximum absorption.
When ingesting domperidone does not cumulate or induce its own metabolism. Domperidone binds to blood plasma proteins by 91-93%. Domperidone is distributed in various tissues of the body, it is found in breast milk, but does not penetrate the blood-brain barrier. The concentration of domperidone in breast milk is 10-50% of the concentration in the blood plasma.
Metabolism domperidona occurs in the liver and in the intestinal wall by hydroxylation and N-dealkylation with the participation of isoenzymes CYP3A4, CYP1A2 and CYP2E1.
Domperidone is excreted by the intestine (66%) and kidneys (33%), incl. in unchanged form (10% and 1% respectively). T 1/2 is 7-9 hours.
Pharmacokinetics in special groups of patients. In patients with a serum creatinine concentration greater than 0.6 mmol / l, T 1/2 is between 7.4 and 20.8 hours, with a decrease in domperidone concentration in the blood plasma.
Dyspeptic symptoms, such as nausea, vomiting, a feeling of overflow in the epigastric region, discomfort in the upper abdomen and regurgitation of gastric contents.
Inside before eating with plenty of water.
Adults and children weighing more than 35 kg 1-2 tablets 3-4 times a day. The maximum dose is 80 mg per day. Duration of admission - 4 weeks. Further administration of the drug is possible after consultation with a doctor.
Patients with renal failure are recommended to reduce the frequency of taking the drug to 1-2 times a day.
The incidence of adverse reactions is classified according to WHO recommendations: rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including isolated cases.
From the immune system: very rarely - anaphylaxis, including anaphylactic shock, urticaria and angioedema.
On the part of the endocrine system: rarely - increasing the concentration of prolactin.
From the nervous system: very rarely - extrapyramidal disorders.
From the digestive system: rarely - gastrointestinal disorders; very rarely - intestinal spasm, diarrhea.
From the skin and subcutaneous tissues: very rarely - itching, rash.
From the side of the reproductive system and mammary glands: rarely - galactorrhea, gynecomastia, amenorrhea.
- hypersensitivity to domperidone or any other component of the drug;
- Prolactin secretory tumor of the pituitary gland (prolactinoma);
- gastrointestinal hemorrhage;
- perforation of the gastrointestinal tract;
- mechanical intestinal obstruction;
- hereditary lactose intolerance, lactose deficiency or glucose-galactose malabsorption;
- the period of breastfeeding;
- Children weighing less than 35 kg.
Carefully. Pregnancy, hepatic insufficiency, renal failure.
PREGNANCY AND LACTATION
The use of domperidone during pregnancy is allowed only if the expected benefit to the mother exceeds the possible risk to the fetus. For the duration of Domperidone, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: kidney failure. Since only a very small amount of domperidone is excreted by the kidneys unchanged, it is hardly necessary to correct a single dose in patients with renal insufficiency. At repeated appointment the frequency of dosing should be reduced to 1-2 times a day, depending on the severity of the insufficiency;a dose reduction may also be required. With prolonged therapy, such patients should be under regular supervision.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: liver failure.
APPLICATION FOR CHILDREN
Contraindicated in children weighing less than 35 kg.
The drug Domperidone-Teva contains lactose, so it should not be prescribed to patients with lactose intolerance, galactosemia or impaired absorption of glucose or galactose.
Since only a very small amount of domperidone is excreted by the kidneys unchanged, it is hardly necessary to correct a single dose in patients with renal insufficiency. At repeated appointment the frequency of dosing should be reduced to 1-2 times a day, depending on the severity of the insufficiency; a dose reduction may also be required. With prolonged therapy, such patients should be under regular supervision. Taking the drug after a meal slows its absorption.
Influence on the ability to manage transport and work with machinery: not affected.
Symptoms of overdose include drowsiness, disorientation, and extrapyramidal disorders, especially in children.
Treatment: There is no specific antidote. In case of an overdose, gastric lavage and the use of activated charcoal may be effective. Careful observation and maintenance therapy is recommended.
To stop extrapyramidal disorders, m-cholinoblockers and drugs used to treat parkinsonism may be effective.
M-cholinoblockers can neutralize the action of domperidone.
Do not take antacid and antisecretory drugs at the same time as domperidone, as they reduce its bioavailability after ingestion.
Simultaneous administration of potent inhibitors of the isoenzyme CYP3A4 can cause an increase in the concentration of domperidone in the plasma. Ketoconazole inhibits the CYP3A4-dependent primary metabolism of domperidone, resulting in an approximately triple increase in Cmax domperidone and AUC in the plateau phase.
Inhibitors of the isoenzyme CYP3A4 are also the following drugs:
- antifungal agents in the azole series;
- antibiotics from the macrolide group;
- HIV protease inhibitors;
With the combined use of domperidone at a dose of 10 mg 4 times a day and ketoconazole at a dose of 200 mg twice daily, the Q-T interval is extended by 10-20 ms.With monotherapy with domperidone both at similar doses and with the intake of a daily dose of 160 mg, 2 times exceeding the maximum allowable, there were no clinically significant changes in the QT interval.
Domperidone can affect the absorption of concomitantly used oral preparations, in particular sustained-release preparations, or enteric-coated preparations. However, the use of domperidone in patients with paracetamol or selected treatment with digoxin did not affect the concentration of these drugs in the blood. Domperidone can also be combined with:
- Neuroleptics, the effect of which it does not increase;
- agonists of dopamine receptors (bromocriptine, levodopa), whose undesirable peripheral effects, such as digestive disorders, nausea, vomiting, it suppresses without neutralizing their basic properties.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
At a temperature of no higher than 25 В° C. Keep out of the reach of children.
Shelf life. 4 years. Do not use after the expiration date printed on the package.