Domperidone-Teva 10 mg 30 pcs.

1 tablet contains:

Active substance:

 domperidone 10 mg; 

Excipients: 

microcrystalline cellulose - 60.00 mg,

pregelatinized starch - 19.46 mg,

silicon dioxide colloidal (aerosil) - 0.09 mg,

magnesium stearate - 0.45 mg,

polyvinyl alcohol - 1.44 mg,

macrogol (polyethylene glycol) - 0.73 mg,

talc - 0.53 mg

titanium dioxide - 0.90 mg.

Domperidone is a dopamine receptor blocker with an antiemetic effect.

The action is due to a combination of peripheral (gastrokinetic) action and inhibition of dopamine receptors in the trigger zone of brain chemoreceptors located outside the blood-brain barrier in the areapostrema region.

When taken internally, domperidone increases the reduced pressure in the esophagus, improves antroduodenal motility and accelerates the emptying of the stomach without affecting gastric secretion.

Domperidone increases prolactin secretion in the pituitary gland.

Pharmacokinetics

When taken on an empty stomach, domperidone is rapidly absorbed, its Cmax in plasma is reached within 30-60 minutes. Low absolute bioavailability after ingestion (about 15%) is due to the effect of the "first passage" through the liver. Although in healthy volunteers, the bioavailability of domperidone increases after ingestion, patients with complaints of the gastrointestinal tract should take domperidone 15-30 minutes before meals. With a decrease in the acidity of gastric juice, a violation of the absorption of domperidone is observed. Preliminary administration of cimetidine and sodium bicarbonate reduces the bioavailability of domperidone. When taken orally after a meal, it takes a slightly longer time to achieve maximum absorption.

When administered, domperidone does not cumulate and does not induce its own metabolism. Domperidone binds to plasma proteins by 91-93%. Domperidone is distributed in various tissues of the body, 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 blood plasma.

Domperidone metabolism occurs in the liver and in the intestinal wall by hydroxylation and N-dealkylation with the participation of CYP3A4, CYP1A2 and CYP2E1 isoenzymes.

Domperidone is excreted by the intestines (66%) and the kidneys (33%), including unchanged (10% and 1%, respectively). T1 / 2 is 7-9 hours.

Pharmacokinetics in special clinical cases

In patients with a serum creatinine concentration of more than 0.6 mmol / L, T1 / 2 is from 7.4 to 20.8 hours, while the concentration of domperidone in the blood plasma is reduced.

Dyspeptic symptoms, such as:

• Nausea, vomiting.
• Feeling of overflow in the epigastric region.
• Discomfort in the upper abdomen.
• Regurgitation of gastric contents.

Domperidone-Teva is contraindicated in pregnancy, breast-feeding, and children under the age of 1 year.

• Hypersensitivity to domperidone or any other component of the drug.
• Prolactin-secreting pituitary tumor (prolactinoma).
• Gastrointestinal bleeding.
• Gastrointestinal perforation.
• Mechanical obstruction of the intestine.
• Hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
• The period of breastfeeding.
• Children weighing less than 35 kg.

Carefully:

• Pregnancy.
• Liver failure.
• Renal failure.

From the digestive system: gastrointestinal disorders (transient intestinal cramps).

From the side of the nervous system: extrapyramidal disorders (in children and in persons with increased BBB permeability, in adults - isolated cases); these phenomena are completely reversible and disappear after stopping the drug.

Allergic reactions: skin rash, urticaria.

Other: hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea).

Cimetidine, sodium bicarbonate reduce the bioavailability of domperidone.

M-anticholinergics and antacid drugs neutralize the effects of domperidone.

Inhibitors of the CYP3A4 isoenzyme increase plasma concentrations of domperidone: antifungal drugs of the azole series, macrolide antibiotics, HIV protease inhibitors, nefazodone (antidepressant). When taken together with ketoconazole, an approximately three-fold increase in the maximum concentration of domperidone is achieved.

Concomitant use with paracetamol and digoxin did not affect the concentration of these drugs in the blood.

Compatible with antipsychotic drugs (antipsychotics) and with dopaminergic receptor agonists (bromocriptine, levodopa).

Inside before eating, drinking 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 is 4 weeks. Further administration of the drug is possible after consultation with a doctor.

Patients with renal insufficiency are recommended to reduce the frequency of taking the drug to 1-2 times a day.

Symptoms: drowsiness, disorientation, extrapyramidal disorders (especially in children).

Treatment: taking activated carbon, with extrapyramidal disorders -
m-anticholinergics, anti-Parkinsonian drugs or antihistamines with anticholinergic properties.

Cimetidine, sodium bicarbonate reduce the bioavailability of domperidone.

M-anticholinergics and antacid drugs neutralize the effects of domperidone.

Inhibitors of the CYP3A4 isoenzyme increase plasma concentrations of domperidone: antifungal drugs of the azole series, macrolide antibiotics, HIV protease inhibitors, nefazodone (antidepressant). When taken together with ketoconazole, an approximately three-fold increase in the maximum concentration of domperidone is achieved.

Concomitant use with paracetamol and digoxin did not affect the concentration of these drugs in the blood.

Compatible with antipsychotic drugs (antipsychotics) and with dopaminergic receptor agonists (bromocriptine, levodopa).

Domperidon-Teva. Film-coated tablets.