Pharmacological group: antiemetics. Dopamine receptor central antagonist.
ATX: A03FA03.
ICD-10: R06.6, R11, R12, R14, R52, Z98.8, K21.0, K30, K31.8, K59.8.
CAS: 57808-66-9
PubChem: 3151
Motilium®
Release form
Film-coated tablets of white or almost white color, round, biconvex; on the cross-section of the tablet, two layers are visible – an almost white core and a film shell.
Excipients: MCC – 60 mg; pregelatinized starch – 19.46 mg; colloidal silicon dioxide (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 – 0.9 mg
Pharmacological effects
Antiemetic. Has antiemetic effect, soothes hiccups and eliminates nausea in some cases. The action is due to the blockade of central dopamine receptors. Due to this, the inhibitory effect of dopamine on the motor function of the gastrointestinal tract is eliminated and the evacuation and motor activity of the stomach increases.
Pharmacokinetics
Domperidone is rapidly absorbed when taken orally on an empty stomach, with maximum plasma concentrations occurring within about 30-60 minutes. The low absolute bioavailability of the oral route of administration of domperidone (approximately 15%) is due to extensive primary metabolism in the intestinal wall and liver.
Although in healthy people the bioavailability of domperidone increases when taken after meals, patients with gastrointestinal complaints should take domperidone 15-30 minutes before meals. The hypoacidity of gastric juice reduces the absorption of domperidone.
When taking the drug after meals, it takes longer to achieve maximum absorption, and the area under the concentration-time curve (AUC) slightly increases.
When taken orally, domperidone does not cumulate and does not induce its own metabolism; maximum plasma concentration 90 minutes after administration, equal to 21
ng/ml after two weeks of oral administration of 30 mg per day was almost the same as after taking the first dose (18 ng/ml). Domperidoi is 91-93% bound to plasma proteins.
The drug is metabolized in the liver by hydroxylation and N-dealkylation. In studies of the metabolism of the drug in vitro using diagnostic inhibitors, it was found that CYP3A4 is the main isoenzyme of the cytochrome 450 system involved in the N-dealkylation of domperidone, while CYP3A4, CYP1A2 and CYP2E1 are involved in the aromatic hydroxylation of domperidone. Excretion in urine and feces is 31 and 66% of the oral dose, respectively. The excretion of the drug in unchanged form is a small percentage (10% – with feces and approximately 1% – with urine). The plasma half-life after taking a single dose is 7-9 hours in healthy volunteers, but lengthened in patients with severe renal failure.
In such patients (serum creatinine> 6 mg/100 ml, i.e.> 0.6 mmol/L), the half-life of domperidone increases from 7.4 to 20.8 hours, but plasma concentrations of the drug are lower than in healthy volunteers.
Indications
Nausea, vomiting, hiccups of various origins (with toxemia, radiation therapy, diet disorders, taking certain medications (morphine), endoscopic and radiopaque studies, in the postoperative period). Postoperative hypotension and atony of the stomach and intestines, biliary dyskinesia, flatulence, reflux esophagitis, cholecystitis, cholangitis, various types of dyspepsia. Nausea and vomiting caused by taking dopaminomimetics.
Dosage
Inside, 15-20 minutes before meals. Adults and children over 12 years old with chronic dyspeptic symptoms – 1 table. (10 mg) 3 times a day, incl. and before bed if necessary.
With severe nausea and vomiting – 1 table. (With 10 mg) 3 times a day, the last dose before bedtime.
The maximum daily dose is 30 mg.
For patients with renal insufficiency, dose adjustment is necessary, the frequency of administration should not exceed 1-2 times during the day.
Overdose
Overdose symptoms are most common in infants and children. Signs of overdose are agitation, altered consciousness, seizures, disorientation, drowsiness, and extrapyramidal reactions.
Overdose treatment: There is no specific antidote for domperidone. In case of overdose, gastric lavage and the use of activated charcoal are recommended. It is recommended to closely monitor the patient’s condition and carry out supportive therapy. Anticholinergics, drugs used to treat parkinsonism, or antihistamines may be effective for extrapyramidal reactions.
Side effects
From the side of the central nervous system: rarely – increased excitability and/or extrapyramidal disorders, headache.
From the digestive system: spasms of smooth muscles of the digestive tract, dry mouth, thirst.
Allergic reactions: itching, rash, urticaria.
Others: increased plasma prolactin levels, galactorrhea, gynecomastia.
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Contraindications
Gastrointestinal bleeding, mechanical intestinal obstruction, perforation of the stomach or intestines, prolactinoma, pregnancy, lactation (breastfeeding), hypersensitivity to domperidone; children under 12 years of age and body weight less than 35 kg (for tablets).
Restricting the use of Domperidone (Generic Motilium) due to cardiac side effects
Domperidone is mainly used to treat nausea and vomiting.
Domperidone may in rare cases cause cardiac arrhythmias that can be life-threatening, a known hazard that can occur in rare cases.
It is known that the risk of developing these rhythm disturbances increases in people aged 60 years and older; at a dosage exceeding 30 mg. per day; and when combined with certain complementary medications and when additional risk factors are present.
The new restrictions are listed below:
- It is necessary to prescribe this treatment for the shortest possible time. It is generally recommended not to take this drug for more than seven days;
- The dosage of the drug should be as low as possible to ensure its effectiveness. The dosage of this drug in tablets will be limited to 10mg. no more than three times a day;
- The maximum dosage of the drug is 30 mg. per day for adults and for children weighing over 35 kg;
- The use of this drug will only be limited to the treatment of nausea and vomiting (until recently, domperidone was registered as a drug for the treatment of additional digestive problems such as bloating, abdominal discomfort
- and heartburn, but these indications were canceled due to lack of sufficient evidence of the effectiveness of this drug in the treatment of these conditions);
- It is forbidden to prescribe this drug to patients at risk of developing these heart rhythm disturbances, and it is necessary to pay attention to the interaction of drugs that increase the risk of developing life-threatening
- heart rhythm disturbances (indicated in the insert);
- It is forbidden to prescribe this drug to patients suffering from electrolyte disturbances (for example, from a decrease in the level of potassium in the blood, or from a decrease in the level of magnesium in the blood).
Interactions
Anticholinergic drugs can neutralize the effect of domperidone. The oral bioavailability of domperidone decreases after previous administration of cimetidine or sodium bicarbonate. You should not take antacids and antisecretory drugs simultaneously with domperidone, as they reduce its bioavailability after oral administration (see section “Special instructions”).
The main role in the metabolism of domperidone is played by the isoenzyme CYP3A4. The results of in vitro studies and clinical experience show that the simultaneous use of drugs that significantly inhibit this isoenzyme can cause an increase in plasma concentrations of domperidone. Potent inhibitors of CYP3A4 include:
• Azole antifungals such as fluconazole, itraconazole, ketoconazole, and voriconazole;
• Macrolide antibiotics such as clarithromycin and erythromycin;
• HIV protease inhibitors such as amprenavir, atazanavir, fosamprenavir, indinavir, nelfinavir, ritonavir, and saquinavir;
• Calcium antagonists such as diltiazem and verapamil;
• Amiodarone;
• Aprepitant;
• Nefazodone;
• Telithromycin.