Domperidone - instructions for use, dose, side effects, contraindications

Has antiemetic effect, soothes hiccups and in some cases eliminates nausea.The effect is due to blockade of central dopamine receptors. This eliminates the inhibitory effect of dopamine on the motor function of the gastrointestinal tract and increases the evacuation and motor activity of the stomach.

Pharmacokinetics:

Absorption after ingestion, fasting - fast (intake after meals and reduced acidity of gastric juice slow down and reduce absorption). C_maxachieved after 1 hour. Bioavailability is 15% (the effect of "first passage" through the liver). Binding to plasma proteins - 90%. Penetrates into various tissues, it does not pass well through the blood-brain barrier. Metabolised in the liver and in the intestinal wall (by hydroxylation and N-dealkylation). Output through the intestine 66%, kidneys - 33%, including unchanged - 10% and 1%, respectively. Half-life - 7-9 hours, with severe chronic renal failure - lengthens.

Indications:

Dyspeptic disorders on the background of delayed gastric emptying, gastroesophageal reflux disease: sensation of overfilling in the epigastrium, a sensation of bloating, pain in the upper abdomen, belching, flatulence, heartburn with or without casting the contents of the stomach into the mouth.Nausea and vomiting of various genesis (including against the background of functional and organic diseases, infections, toxemia, radiation therapy, diet disorders, drug origin, including dopamine agonists - levodopa, bromocriptine, endoscopic and radiocontrast studies of the gastrointestinal tract); hiccough, atony of the digestive tract (including postoperative); the need to accelerate peristalsis in radiocontrast studies of the gastrointestinal tract.

ICD-10

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K81.0 Acute cholecystitis

XI.K20-K31.K21.0 Gastroesophageal reflux with esophagitis

XI.K20-K31.K20 Esophagitis

XVIII.R00-R09.R06.6 Hiccups

XVIII.R10-R19.R14 Meteorism and related conditions

XVIII.R10-R19.R12 Heartburn

XVIII.R10-R19.R11 Nausea and vomiting

XVIII.R50-R69.R52 Pain, not elsewhere classified

XXI.Z80-Z99.Z98.8 Other specified post-surgical conditions

XI.K80-K87.K82.8 Other specified diseases of the gallbladder

XI.K20-K31.K30 Dyspepsia

Contraindications:

Hypersensitivity, gastrointestinal bleeding, mechanical intestinal obstruction, perforation of the stomach or intestine (stimulation of peristalsis can aggravate these conditions), hyperprolactinaemia, prolactinoma, hepatic insufficiency of moderate and severe severity, pregnancy,the period of breastfeeding, children under 12 years of age or body weight less than 35 kg, simultaneous use of drugs that increase the QT interval and inhibitors of the isoenzyme CYP34A.

Carefully:

With caution should be used for violations of the liver and kidneys. With renal failure, the frequency of application should be reduced.

Pregnancy and lactation:

The category of FDA recommendations is not defined. Adequate and well-controlled studies on humans have not been conducted, animal studies have not shown adverse effects on the fetus. Use only if the intended benefit to the mother exceeds the potential risk to the fetus.

Penetrates into breast milk, stop breastfeeding if necessary treatment with domperidone.

Dosing and Administration:

Vomiting and nausea of various genesis (including against the background of functional (40-80 mg per day) and organic diseases, infections, anesthesia (20 mg), toxemia, chemotherapy in cancer patients (60 mg per day), radiation therapy, disorders of diet, taking morphine, apomorphine, levodopa and bromocriptine (60 mg per day), endoscopic and radiopaque methods of GIT research).

Atony of the gastrointestinal tract, including postoperative, diabetic - 40-80 mg per day.

Hiccups, functional dyspepsia - 40-80 mg per day.

Dyspepsia against delayed emptying of the stomach, gastroesophageal reflux and esophagitis: a feeling of overflow in the epigastrium, a sensation of bloating, flatulence, gastralgia, heartburn, belching with or without casting gastric contents into the mouth. Inside 15-20 minutes before meals, 10 mg 3-4 times a day. With severe nausea and vomiting - 20 mg 3-4 times a day and before bedtime. If necessary, the dose can be doubled.

Acceleration of peristalsis during radiocontrast studies of the gastrointestinal tract - 20 mg, 50 mg, intravenously - 8 mg per day.

For patients with renal insufficiency, the frequency of administration should be no more than 1-2 times a day.

Side effects:

From the side of the central nervous system: rarely - increased excitability and / or extrapyramidal disorders, convulsions, drowsiness, headache.

From the digestive system: spasms of smooth muscles of the gastrointestinal tract, dry mouth, thirst, intestinal colic, constipation.

Allergic reactions: itching, rashes, hives, very rarely - anaphylactic shock, angioedema, conjunctivitis.

Other: increased plasma prolactin levels, galactorrhea, gynecomastia, changes in liver function tests.

From the cardiovascular system: very rarely ventricular tachycardia as pirouette, sudden coronary death.

Overdose:

Drowsiness, disorientation, extrapyramidal disorders, hypotension.

Treatment is symptomatic. When extrapyramidal disorders - antiparkinsonian or antihistamines with anticholinergic properties.

Interaction:

Domperidone may interfere with the absorption of sustained-release preparations or coated with enteric-coated membranes.

When used simultaneously with antacids, antisecretory drugs (including cimetidine, sodium bicarbonate), the bioavailability of domperidone decreases.

With simultaneous use with anticholinergic drugs, the action of domperidone is inhibited.

Because the domperidone is metabolized mainly with the participation of the CYP3A4 isoenzyme, it is believed that with the simultaneous use of domperidone and inhibitors of this isoenzyme (including antifungal agents of the azole group, macrolide antibiotics, HIV protease inhibitors, nefazodone), an increase in the level of domperidone in blood plasma is possible.

Special instructions:

Care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions due to the risk of adverse reactions that may affect these abilities.

Instructions

Domperidone (Domperidonum)