The drug emetrol for vomiting includes the active ingredient domperidone. The action of the drug depends on its constituent components. In this case we will consider domperidone.
Clinico-pharmacological group: antiemetic drug of central action, which blocks dopamine receptors.
Pharmacotherapeutic group: Antiemetic drug – central dopamine receptor antagonist.
Anti-emetic drug. It has antiemetic effect, soothes hiccups and eliminates nausea in some cases. The action is caused by blockade of central dopamine receptors. Due to this, inhibitory effect of dopamine on motor function of gastrointestinal tract is eliminated and evacuatory and motility activity of the stomach is increased.
Absorption after oral intake, on an empty stomach is fast (intake after meal, decreased acidity of gastric juice slows down and reduces absorption). Cmax is reached in 1 hour. Bioavailability is 15% (effect of “first passage” through the liver). Binding to plasma proteins is 90%. It penetrates into various tissues, passes poorly through the BBB. Metabolized in liver and intestinal wall (by hydroxylation and N-dealkylation). It is excreted through the intestine at 66%, by the kidneys at 33%, including unchanged at 10% and 1% respectively. T1/2 is 7-9 hours, in severe CPN it is prolonged.
Indications for the use of emetrol
Nausea, vomiting, hiccups of various genesis (during toxemia, radiation therapy, dietary disorders, taking some drugs /morphine/, endoscopic and X-ray contrast tests, in the post-operative 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.
For oral administration. Dosage is adjusted individually depending on the patient’s age and clinical situation.
CNS disorders: rare – increased excitability and / or extrapyramidal disorders, headache.
Digestive system: spasms of the smooth muscles of the gastrointestinal tract, dry mouth and thirst.
Allergic reactions: itching, rash, urticaria.
Other: increase in plasma prolactin levels, galactorrhea, gynecomastia.
Contraindications to use
Gastrointestinal bleeding, mechanical intestinal obstruction, gastric or intestinal perforation, prolactinoma, pregnancy, lactation (breast-feeding), hypersensitivity to domperidone, children under 12 years of age and body weight less than 35 kg (for tablets).
Administration during pregnancy and lactation
Domperidone is contraindicated for use during pregnancy and lactation.
Application in case of liver dysfunction.
Caution should be used in patients with hepatic impairment.
Application in impaired renal function.
Caution should be exercised when using in patients with impaired renal function. It is necessary to decrease the use frequency in case of renal insufficiency.
Administration in children.
Contraindicated in children under 1 year of age (under 5 years of age and in children with body weight less than 20 kg – for tablets).
Caution should be exercised if liver and kidney function is impaired.
Preparations containing domperiodone should be taken in children in dosage forms intended for the appropriate age.
In concomitant use with antacids, antisecretory drugs (including cimetidine, sodium hydrocarbonate), the bioavailability of domperidone decreases. When concomitant use with anticholinergic drugs, the effect of domperidone is inhibited. As domperidone is metabolized mainly with participation of CYP3A4 isoenzyme, it is believed that during concomitant use of domperidone and inhibitors of this isoenzyme (including azole antifungal drugs, antibiotics of macrolide group, HIV protease inhibitors, nefazodone), increase in plasma level of domperidone is possible.