Domrid (domperidone maleatee) coated tablets 10 mg. №30

Description

Domrid Storage
active substance: domperidone maleate;

1 tablet contains domperidone maleate equivalent to domperidone 10 mg;

Domrid Excipients: microcrystalline cellulose, croscarmellose sodium, colloidal anhydrous silica, magnesium stearate, Opadry II 31 G 58920 white *.

* Opadry II 31 G 58920 white: hypromellose, lactose monohydrate, titanium dioxide (E 171), polyethylene glycol, talc.

Domrid Dosage form
Coated tablets.

Main physical and chemical properties: round biconvex tablets, white coated.

Pharmacotherapeutic group
Stimulators of peristalsis. ATX code A03F A03.

Pharmacological properties

Pharmacodynamics.

Domperidone is a dopamine antagonist with antiemetic properties. Domperidone slightly crosses the blood-brain barrier. Domperidone is very rarely accompanied by extrapyramidal side effects, especially in adults, but

domperidone stimulates the secretion of prolactin from the pituitary gland. Its antidote may be due to a combination of peripheral (gastrokinetic) action and antagonism of dopamine receptors in the trigger zone of chemoreceptors, located outside the blood-brain barrier in the posterior region (area postrema). Animal studies

as well as low brain concentrations indicate a predominantly peripheral effect of domperidone on dopamine receptors.

Studies in humans have shown that oral domperidone increases the pressure in the lower esophagus, improves antroduodenal motility and accelerates gastric emptying. Domperidone does not affect gastric secretion.

Pharmacokinetics.

Absorption.

Domperidone is rapidly absorbed by oral administration on an empty stomach, with maximum plasma concentrations (Cmax) reached after approximately 60 minutes. The low absolute bioavailability of oral domperidone (approximately 15%) is due to extensive first-pass metabolism in the intestinal wall and liver. Although the bioavailability of domperidone increases in healthy people when taken after a meal, patients with gastrointestinal complaints should take domperidone 15-30 minutes before a meal.

Reduced gastric acidity reduces the absorption of domperidone. When the drug is taken orally after a meal, the maximum absorption is somewhat slowed down, and the area under the pharmacokinetic curve “concentration – time” (AUC) is slightly increased.

Distribution.

When taken orally, domperidone does not accumulate and does not induce its own metabolism; the maximum level in blood plasma after 90 minutes (21 ng / ml) after two weeks of oral administration of 30 mg per day was almost the same as after the first dose (18 ng / ml). Domperidone is 91-93% bound to plasma proteins. Studies of the distribution of domperidone in animals using a radiolabeled drug have shown significant tissue distribution but low concentrations in the brain. In animals, small amounts of the drug penetrate the placenta.

Metabolism.

Domperidone is rapidly and extensively metabolized in the liver by hydroxylation and N-dealkylation.

Breeding.

Excretion in urine and faeces is 31% and 66% of the oral dose, respectively. Excretion of the drug in unchanged form is a small percentage (10% – in the feces and about 1% – in the urine). The plasma half-life after a single dose is 7-9 hours in healthy volunteers, but prolonged in patients with severe renal insufficiency.

Indication
To relieve symptoms of nausea and vomiting.

Contraindication
Domrid® is contraindicated:

patients with established hypersensitivity to the drug or to excipients;
patients with prolactin-secretory pituitary tumor (prolactinoma);
patients with severe or moderate hepatic and / or renal impairment (see section “Special warnings and precautions for use”);
patients with known prolongation of cardiac conduction intervals, in particular QTc, patients with significant electrolyte imbalance or with background heart disease, such as congestive heart failure (see section “Features”);
patients with hepatic insufficiency;
if stimulation of motor function of the stomach can be dangerous, such as gastrointestinal bleeding, mechanical obstruction or perforation;
contraindicated concomitant use of ketoconazole, erythromycin or other potent CYP3A4 inhibitors;
Concomitant use of drugs that prolong the QT interval, such as fluconazole, erythromycin, itraconazole, oral ketoconazole, posaconazole, ritonavir, saquinavir, telaprevir, voriconazole, clarithromycin, amiodarone, telithromycin and telithromycin is contraindicated. (excluding apomorphine, see sections “Interaction with other medicinal products and other forms of interaction” and “Peculiarities of use”).