Domperidone
Domperidone: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Domperidone
ATX code: A03FA03
Active ingredient: domperidone (domperidone)
Producer: CJSC "ALSI Pharma", LLC "Ozon" (Russia)
Description and photo update: 2019-18-09
Prices in pharmacies: from 100 rubles.
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Domperidone is an antiemetic drug.
Release form and composition
Domperidone is produced in the form of film-coated tablets: almost white or white, biconvex, round; on a cross-section - an inner layer of white with a creamy shade or white (10 pcs. in blisters, 1-5 packs in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: domperidone - 10 mg;
- Auxiliary components: magnesium stearate - 0.45 mg; microcrystalline cellulose - 60 mg; pregelatinized starch - 19.46 mg; colloidal silicon dioxide (aerosil) - 0.09 mg; talc - 0.53 mg; titanium dioxide - 0.9 mg; polyvinyl alcohol - 1.44 mg; polyethylene glycol (macrogol) - 0.73 mg.
Pharmacological properties
Pharmacodynamics
Domperidone is a dopamine antagonist with antiemetic effects. However, the substance poorly penetrates the blood-brain barrier. In some cases, taking domperidone is accompanied by extrapyramidal side reactions, especially in adult patients. The drug enhances the release of prolactin from the pituitary gland. Presumably, its antiemetic properties are due to a combination of antagonism to dopamine receptors localized in the chemoreceptor trigger zone, and peripheral (gastrokinetic) action. Experiments on animals, as well as the results of studies in which it was found that domperidone is found in the brain in small quantities, confirm its central action on dopamine receptors.
When taken orally, the drug increases the duration of duodenal and antral contractions, accelerates the evacuation of stomach contents and increases the sphincter pressure of the lower esophagus in healthy individuals. Domperidone does not affect gastric secretion.
Pharmacokinetics
When taken orally on an empty stomach, domperidone is absorbed at a high rate. The maximum concentration of the drug in plasma is recorded within 30-60 minutes after administration. The low absolute bioavailability of oral domperidone (approximately 15%) is due to the high metabolic rate during the first pass effect through the liver and intestinal wall. Domperidone should be taken 15-30 minutes before meals. Reduced acidity in the stomach leads to disorders of drug absorption.
With the preliminary administration of sodium bicarbonate and cimetidine, the bioavailability of domperidone decreases (with oral administration). The intake of the drug into the body after a meal increases the time to reach maximum absorption, and the area under the pharmacokinetic curve (AUC) also slightly increases.
When taken orally, domperidone does not cumulate or induce its own metabolism. Its maximum plasma concentration was 21 ng / ml 1.5 hours after ingestion of the drug as part of a course of treatment that lasted 2 weeks and calculated for taking 30 mg of the drug per day, and practically did not differ from the concentration of domperidone in plasma after taking the first dose, which was 18 ng / ml.
The degree of binding of domperidone to plasma proteins is 91–93%. Studies of the effect of a radioactively labeled drug on the animal organism have shown that it is largely distributed in tissues, but in the brain it is determined at low concentrations. It also penetrated in small amounts through the placental barrier in pregnant rats.
Domperidone is rapidly and extensively metabolized by N-dealkylation and hydroxylation. When studying metabolism in vitro with the participation of diagnostic inhibitors, it was revealed that the isoenzyme CYP3A4 is the main form of cytochrome P 450, which is involved in the N-dealkylation of domperidone. At the same time, the isoenzymes CYP2E1, CYP1A2 and CYP3A4 are responsible for aromatic hydroxylation of the substance.
When administered orally, domperidone is excreted in urine (31% of the dose taken) and feces (66% of the dose taken). The amount of the drug that is excreted unchanged is insignificant (10% of free domperidone is excreted through the intestines and about 1% through the kidneys). The plasma half-life after a single oral administration is 7-9 hours in healthy volunteers, but increases in patients with renal insufficiency.
In patients with renal dysfunction (serum creatinine is 6 mg / 100 ml, that is, exceeds 0.6 mmol / l), the half-life of domperidone increases from 7.4 to 20.8 hours, but the drug content in the blood plasma is lower than that of healthy volunteers. A small amount of unchanged domperidone (about 1%) is excreted in the urine.
In patients with moderate liver dysfunctions (according to the Child - Pugh scale 7-9 points), AUC and maximum concentration of domperidone were 2.9 and 1.5 times higher than in healthy people participating in the study. The proportion of the unbound fraction increased by 25%, and the elimination half-life increased from 15 to 23 hours. In patients with mild hepatic insufficiency, a decrease in systemic exposure was observed compared to healthy patients. Pharmacokinetic parameters of the drug in patients with severe hepatic insufficiency have not been studied.
Indications for use
- Vomiting and nausea of various origins (including with organic and functional diseases, infections, toxemia, diet disorders, radiation therapy, during X-ray contrast and endoscopic studies of the gastrointestinal tract, as well as associated with the intake of certain medications - apomorphine, morphine, bromocriptine and levodopa);
- Hiccups;
- The need to accelerate peristalsis when conducting X-ray contrast studies of the gastrointestinal tract;
- Atony of the gastrointestinal tract (including postoperative);
- Dyspeptic symptoms with delayed gastric emptying, gastroesophageal reflux and esophagitis: heartburn, a feeling of fullness in the epigastric region, a feeling of bloating, gastralgia, flatulence, belching with or without throwing gastric contents into the oral cavity.
Contraindications
- Mechanical intestinal obstruction;
- Bleeding from the gastrointestinal tract;
- Bowel or stomach perforation;
- Prolactinoma;
- Lactation period;
- Age up to 5 years and body weight less than 20 kg;
- Hypersensitivity to drug components.
Domperidone can be prescribed to pregnant women only if the intended benefits to the health of the mother are higher than the potential risk to the fetus.
The drug should be used with caution in severe hepatic and / or renal failure.
Instructions for the use of Domperidone: method and dosage
Domperidone is taken orally before meals (15-20 minutes).
For chronic dyspeptic symptoms, children from 5 years of age and adults are usually prescribed 10 mg 3-4 times a day (if necessary, and before bedtime).
With vomiting and severe nausea, Domperidone is taken 20 mg 3-4 times a day (the last dose is before bedtime).
The maximum dose is 80 mg per day.
Patients with renal insufficiency should adjust the dose and frequency of administration (no more than 1-2 times a day).
Side effects
During therapy, it is possible to develop disorders on the part of some body systems, manifested with different frequencies:
- Nervous system: extrapyramidal disorders (completely reversible and go away on their own after you stop taking Domperidone);
- Digestive system: gastrointestinal disorders (transient bowel spasms);
- Allergic reactions: urticaria, skin rash;
- Others: hyperprolactinemia (gynecomastia, galactorrhea, amenorrhea).
Overdose
Most often, overdose symptoms occur in children. These include extrapyramidal disorders, agitation, drowsiness, altered consciousness, disorientation in space, and seizures. In this case, symptomatic therapy is prescribed. There is no specific antidote. It is also recommended to wash the stomach, take activated charcoal, and with the development of extrapyramidal reactions - the use of antiparkinsonian and anticholinergic drugs. Since an overdose may prolong the QT interval, it is necessary to carry out regular ECG monitoring.
special instructions
According to the instructions, Domperidone with antacid drugs or drugs that reduce gastric secretion should not be taken together at the same time. When taking Domperidone before meals, the listed medicines should be taken after meals.
Influence on the ability to drive vehicles and complex mechanisms
When taking Domperidone, care should be taken when driving vehicles and performing potentially hazardous work that requires increased concentration and immediate psychomotor reactions, due to the high risk of adverse reactions that can affect the above abilities.
Application during pregnancy and lactation
Information on the use of Domperidone during pregnancy is considered insufficient, therefore its appointment to this category of patients is contraindicated.
In women, the content of the active substance of the drug in breast milk is 10-50% of the corresponding concentration in plasma and does not exceed 10 ng / ml. In breastfed babies whose mothers take Domperidone, adverse reactions from the cardiovascular system sometimes occur. Therefore, when prescribing the drug during lactation, it is necessary to refuse breastfeeding.
Drug interactions
With the simultaneous use of certain drugs, undesirable effects may occur:
- Antacid drugs and M-anticholinergics: neutralizing the action of domperidone;
- Sodium bicarbonate, cimetidine: decreased bioavailability of domperidone;
- Ketoconazole, CYP3A4 isoenzyme inhibitors (azole antifungal drugs, macrolide antibiotics, HIV protease inhibitors, nefazodone (antidepressant)): increased plasma domperidone concentration.
Domperidone is compatible with dopamine receptor agonists (levodopa, bromocriptine) and antipsychotic drugs (neuroleptics).
Analogs
Domperidone analogs are: Domperidon-Teva, Domperidon Hexal, Damelium, Domstal, Domet, Motilak, Motilium, Motorinorm, Motijekt, Motonium, Passage.
Terms and conditions of storage
Store in a dark, dry place out of reach of children at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Domperidone
Usually, patients leave good reviews about Domperidone, noting that it effectively relieves spasms and eliminates stomach pains, and also helps with nausea and vomiting. Reports of adverse reactions are rare, and they are mainly observed in the first days after starting treatment.
The price of Domperidone in pharmacies
The approximate price of Domperidone in pharmacies is 53–98 rubles (the package contains 30 tablets).
Domperidone: prices in online pharmacies
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Drug name Price Pharmacy |
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Domperidone 10 mg film-coated tablets 30 pcs. RUB 100 Buy |
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Domperidone tablets p.p. 10mg 30 pcs. 148 RUB Buy |
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Domperidone 10 mg film-coated tablets 30 pcs. 197 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
