The antiemetic Emetrol (domperidone)
Emetrol (domperidone) has an antiemetic effect, calms hiccups and eliminates nausea in some cases. The action is due to blockade of central dopamine receptors. Due to this, emetrol eliminates inhibitory effect of dopamine on motor function of the gastrointestinal tract and increases evacuatory and motility activity of the stomach.
Absorption after oral intake, on an empty stomach is fast (intake after meals, 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 h, prolonged in severe CKD.
Nausea, vomiting, hiccups of different genesis (toxemia, radiation therapy, dietary disorders, taking some drugs /morphine/, endoscopic and X-ray contrast 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.
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.
Caution should be exercised when using in patients with liver and kidney function disorders. Drugs containing domperiodone should be taken in children in dosage forms intended for the appropriate age. Domperidone is contraindicated in pregnancy and during lactation. It is contraindicated in children under 1 year of age. Taking into account the side effects on the nervous system, patients should be careful when driving motor transport or working with other mechanisms.
CNS disorders: rarely – 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 level, galactorrhea, gynecomastia.