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

Excipients: cellulose microcrystalline 60.00 mg, pregelatinized starch 19.46 mg, silicon dioxide colloid (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 0.90 mg.

Description:

Round tablets of biconvex form, covered with a film coat of white or almost white color. On the cross-section - the inner layer of white or white with a creamy shade of color.

Pharmacotherapeutic group:antiemetics - dopamine receptor blocker central

ATX: & nbsp

A.03.F.A.03 Domperidone

Pharmacodynamics:

Domperidone is a dopamine receptor antagonist, similar to metoclopramide and some neuroleptics with antiemetic properties. But unlike these drugs, domperidone poorly penetrates the blood-brain barrier (BBB). It blocks the peripheral and to a lesser extent the central (in the trigger zone of the emetic center) dopamine receptors, eliminates the inhibitory effect of dopamine on the motor function of the gastrointestinal tract (GIT), and increases the evacuation and motor activity of the stomach.Has antiemetic effect, soothes hiccups and eliminates nausea. Has no effect on gastric secretion. Increases the concentration of prolactin in the blood serum.

Pharmacokinetics:

Absorption after ingestion on an empty stomach is rapid (intake after meals, decreased acidity of gastric juice slow down and decrease absorption). Time to reach the maximum concentration - 1 hour Bioavailability - 15% (the effect of "first passage" through the liver). The connection with plasma proteins is 90%. Penetrates into various tissues, it does not pass well through GEB. Domperidone Do not cumulate or induce your own metabolism. Metabolized in the liver and in the intestinal wall (by hydroxylation and Ndealkylation involving cytochrome P450). Output through the intestine 66%, kidneys - 33%, incl. in unchanged form - 10 and 1% respectively. The half-life (T_1/2) - 7-9 hours; with severe chronic renal failure - lengthens.

Indications:

Vomiting and nausea of different genesis (including on the background of functional and organic diseases, infections, toxemia, radiation therapy, diet disorders, drug genesis - taking morphine, apomorphine, levodopa and bromocriptine, endoscopic and radiocontrast studies of the gastrointestinal tract) hiccough, atony of the digestive tract (incl.postoperative); the need to accelerate peristalsis in radiocontrast studies of the gastrointestinal tract.

Dyspeptic disturbances against delayed gastric emptying, gastroesophageal reflux and esophagitis: a feeling of overfilling in the epigastrium, a sensation of bloating, flatulence, gastralgia, heartburn, belching with or without casting gastric contents into the oral cavity.

Contraindications:

Hypersensitivity, bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestine, prolactinoma, lactation period, children's age (up to 5 years and children weighing up to 20 kg).

Carefully:

In pregnancy, severe renal and / or hepatic insufficiency.

Pregnancy and lactation:

Data on the use of domperidone during pregnancy is not enough. To date, there is no evidence of an increased risk of developmental malformations in humans. However, appoint domperidone in pregnancy should only be if its use is justified by the expected therapeutic benefit for the mother and the minimum risk to the fetus.

In women, the concentration of domperidone in breast milk is 10 to 50% of the corresponding plasma concentration and does not exceed 10 ng / ml.The total amount of domperidone excreted into breast milk is less than 7 μg per day when the maximum permissible doses of domperidone are administered. It is not known whether this concentration has a negative effect on infants. In this regard, when using domperidona during lactation should stop breastfeeding.

Dosing and Administration:

Inside, 15-20 minutes before meals.

Adults and children over 5 years of age with chronic dyspeptic phenomena - 10 mg 3-4 times a day, including before bedtime if necessary.

At the expressed nausea and vomiting - on 20 mg 3-4 times a day, last reception before a dream. The maximum daily dose is 80 mg.

For patients with renal insufficiency dose correction is necessary, the frequency of reception should not exceed 1-2 times during the day.

Side effects:

From the digestive system: gastrointestinal disorders (transient intestinal spasms).

From the nervous system: extrapyramidal disorders (in children and in persons with increased permeability of the BBB, in adults - single cases); these phenomena are completely reversible and disappear after discontinuation of the drug.

Allergic reactions: skin rash, hives.

Other: hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea).

Overdose:

Symptoms: drowsiness, disorientation, extrapyramidal disorders (especially in children).

Treatment: reception of activated carbon, with extrapyramidal disorders - m-holinoblokatory, antiparkinsonian drugs or antihistamines with anticholinergic properties.

Interaction:

Cimetidine, sodium hydrogen carbonate reduce the bioavailability of domperidone. M-cholinoblockers and antacid drugs neutralize the action of domperidone.

Increase the concentration of domperidone in plasma inhibitors of isoenzyme CYP3A4: antifungal azole agents, antibiotics from the macrolide group, HIV protease inhibitors, nefazodone (antidepressant).

When co-administered with ketoconazole, approximately a threefold increase in the maximum concentration of domperidone is achieved.

Simultaneous administration with paracetamol and digoxin had no effect on the concentration of these drugs in the blood.

Compatible with antipsychotic drugs (neuroleptics) and dopaminergic receptor agonists (bromocriptine, levodopa).

Special instructions:

When combined with the use of domperidone antatsidnymi drugs or drugs that reduce the secretion of gastric juice, the latter should be taken after eating, and not before eating, i.e. they should not be taken concomitantly with domperidone.

Effect on the ability to drive transp. cf. and fur:

Domperidone does not affect the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 10 mg.

Packaging:

For 10 tablets in a contour mesh box made of PVC film and aluminum foil printed lacquered.

1, 2, 3, 4 or 5 contour squares with instruction in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006942/10

Date of registration:21.07.2010

The owner of the registration certificate:ALSI Pharma, ZAO ALSI Pharma, ZAO Russia

Manufacturer: & nbsp

ALSI Pharma, ZAO Russia

Representation: & nbspALSI Pharma CJSC ALSI Pharma CJSC Russia

Information update date: & nbsp18.01.2016

Illustrated instructions

Instructions

Domperidone (Domperidone)