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Domperidone is a dopamine antagonist with antiemetic properties. Domperidone poorly penetrates through the HEB. Domperidone use is rarely accompanied by extrapyramidal side effects, especially in adults, but domperidone stimulates prolactin release from the pituitary gland. Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) action and antagonism to dopamine receptors in the chemoreceptor trigger zone, which is outside the GEB.
Animal studies and low concentrations of the drug detected in the brain indicate a predominantly peripheral effect of domperidone on dopamine receptors.
When administered orally, domperidone increases the duration of antral and duodenal contractions, accelerates gastric emptying and increases lower esophageal sphincter pressure. Domperidone has no effect on gastric secretion.
After oral administration on an empty stomach, domperidone is rapidly absorbed. Cmax in blood plasma is reached within about 30-60 min. Low absolute bioavailability of domperidone when administered orally (approximately 15%) is associated with intense presystemic metabolism in the intestinal wall and liver.
Domperidone should be taken 15-30 min before a meal. Decreased acidity in the stomach leads to impaired absorption of domperidone.
Bioavailability when taken orally is reduced if cimetidine and sodium bicarbonate are taken beforehand.
When taking the drug after meals, it takes longer to reach Cmax and the AUC is slightly increased.
When administered orally, domperidone does not accumulate and does not induce its own metabolism. After oral domperidone administration for 2 weeks at the dose of 30 mg/day, Cmax in plasma after 90 min was 21 ng/ml and was almost the same as after the first dose (18 ng/ml).
Binding to plasma proteins was 91-93%.
Studies of the distribution of the drug with the radioactive label in animals showed its wide distribution in tissues, but low concentrations in the brain. Small amounts of the drug penetrate the placental barrier in rats.
Domperidone undergoes rapid and intensive metabolism by hydroxylation and N-dealkylation. In vitro metabolism studies with diagnostic inhibitors have shown that CYP3A4 isoenzyme is the major form of cytochrome P450 involved in N-dealkylation of domperidone, while CYP3A4, CYP1A2 and CYP2E1 isoenzymes are involved in aromatic hydroxylation of domperidone.
Renal and intestinal excretion is 31% and 66% of the dose when administered orally, respectively. The proportion of the drug excreted unchanged is small (10% is excreted through the intestine and approximately 1% through the kidneys). Plasma T1/2 after a single oral administration is 7-9 h in healthy volunteers, but is increased in patients with severe renal impairment.
Pharmacokinetics in special clinical cases
In patients with severe renal impairment (serum creatinine >6 mg/100 ml, i.e. >0.6 mmol/L) the T1/2 of domperidone is increased from 7.4 to 20.8 h, but plasma concentrations of the drug are lower than in patients with normal renal function. A small amount of unchanged drug (about 1%) is excreted by the kidneys.
In patients with liver dysfunction of moderate severity (Child-Pugh score 7-9) AUC and Cmax of domperidone were 2.9 and 1.5 times higher than in healthy volunteers, respectively. The unbound fraction increased by 25%, and the T1/2 increased from 15 to 23 h. In patients with mild hepatic impairment, slightly decreased systemic drug levels were observed compared with those in healthy volunteers based on Cmax and AUC, with no changes in protein binding or T1/2. Patients with severe hepatic impairment have not been studied.
Contraindications to use
- Hypersensitivity to domperidone or any other component of the drug;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- concomitant use of oral forms of ketoconazole, erythromycin or other potent CYP3A4 isoenzyme inhibitors that cause QT interval prolongation (such as clarithromycin, itraconazole, fluconazole, posaconazole, ritonavir, saquinavir, amiodarone, telithromycin, telaprevir and voriconazole), except for apomorphine;
- Significant electrolyte abnormalities or cardiac disease, such as chronic heart failure;
- Gastrointestinal bleeding, mechanical intestinal obstruction, or perforation of the stomach or intestines;
- Moderate to severe hepatic impairment;
- body weight less than 35 kg;
- Children under 12 years of age with body weight less than 35 kg;
- Breast-feeding period.
With caution: childhood, renal dysfunction.
Administration during pregnancy and lactation
Motilium is contraindicated for use during pregnancy and lactation.
Administration in liver dysfunction
The drug is contraindicated in case of liver dysfunction of moderate or severe degree. No dosage adjustment is required in mild hepatic impairment.
Administration in impaired renal function
This drug should be used with caution in patients with impaired renal function.
Administration in children
The drug is contraindicated in children under 12 years of age and body weight less than 35 kg.
Mostly Motilium suspension should be used in pediatric practice.
Administration in elderly patients
Domperidone use may be associated with an increased risk of serious ventricular arrhythmias or sudden death. The risk may be more probable in patients over 60 years old.
Indications of Motilium
For the relief of symptoms of nausea and vomiting.
The drug is taken orally. It is recommended to take Motilium® tablets 15-30 min before meal, in case of taking the drug after meal, absorption of domperidone may be delayed.
Adults and adolescents over 12 years of age and children with body weight ≥35 kg - 1 tablet. (10 mg) 3 times / day, the maximum daily dose is 3 tablets. (30 mg).
For children under 12 years of age and with body weight of 35 kg or more - 1 tablet (10 mg) 3 times daily. (10 mg) 3 times a day, the maximum daily dose is 3 tablets (30 mg). (30 mg).
In pediatric practice, Motilium suspension should be mainly used.
Continuous use of Motilium without physician's consultation should not exceed 7 days. If necessary, the doctor may prolong the course of treatment.
Patients with renal insufficiency. As the T1/2 of domperidone in severe renal failure (at serum creatinine level >6 mg/100 ml, i.e. >0.6 mmol/l) increases, the frequency of Motilium®, film-coated tablets administration should be decreased to 1 or 2 times per day, depending on the severity of the failure. Regular examination of patients with severe renal failure is necessary (see section "Pharmacological action").
Patients with hepatic failure. Motilium use is contraindicated in patients with mild to severe hepatic insufficiency. No dose adjustment is required in patients with mild hepatic impairment.