Domperidon

General characteristics. Structure:

Active ingredient: 10 mg of a domperidon.

Excipients: cellulose microcrystallic, starch prezhelatinizirovanny, silicon dioxide colloid (aerosil), magnesium stearate, polyvinyl alcohol, macrogoal (polyethyleneglycol), talc, titanium dioxide.

The drug having antiemetic action, improving motility of digestive tract. At the same time secretion of a stomach remains invariable; drug practically does not get into a brain and the central nervous system. Thanks to the fact that the stomach begins to be reduced normally after use of drug weight in a stomach, painful and unpleasant feelings in it leaves. There pass such unpleasant feelings as abdominal distention, an eructation, a meteorism.

Pharmacological properties:

Pharmacodynamics. Domperidon is the antagonist of dopamine receptors having similar to Metoclopramidum and some neuroleptics antiemetic properties. But, unlike these medicines, домперидон badly gets through a blood-brain barrier (GEB). Blocks more peripheral and to a lesser extent central (in a trigger zone of the emetic center) dopamine receptors, the inhibiting influence of dopamine on motor function of the digestive tract (DT) eliminates and increases evakuatorny and physical activity of a stomach. Has antiemetic effect, calms a hiccups and eliminates nausea. Has no effect on gastric secretion. Increases concentration of prolactin in blood serum.

Pharmacokinetics. Absorption after intake on an empty stomach - bystry (reception after food, reduced acidity of a gastric juice slow down and reduce absorption). Time of achievement of the maximum concentration – 1 h. Bioavailability - 15% (effect of "the first passing" through a liver). Communication with proteins of plasma - 90%. Gets into various fabrics, badly passes through GEB. Domperidon does not kumulirut and does not induce own metabolism. It is metabolized in a liver and in an intestines wall (by a hydroxylation and N-dealkylation with P450 cytochrome participation). It is removed through intestines of 66%, kidneys  – 33%, including in not changed look – 10 and 1% respectively. An elimination half-life (T1/2)  – 7-9 h; at the expressed chronic renal failure - it is extended.

Indications to use:

Vomiting and nausea of various genesis (including against the background of functional and organic diseases, infections, at a toxaemia, radiation therapy, disturbances of a diet, medicinal genesis - reception of morphine, Apomorphinum, levodopa and Bromocriptinum; when carrying out endoscopic and X-ray contrast researches GITs), a hiccups, a GIT atony (including postoperative); need of acceleration of a vermicular movement when carrying out X-ray contrast researches GITs.

Dispepsichesky disturbances against the background of the slowed-down gastric emptying, a gastroesophageal reflux and an esophagitis: feeling of overflow in epigastriums, feeling of abdominal distention, a meteorism, a gastralgia, heartburn, an eructation with throwing or without throwing of gastric contents in an oral cavity.

Route of administration and doses:

Inside, in 15-20 min. prior to food. To adults and children 5 years at the chronic dispepsichesky phenomena are more senior - on 10 mg 3-4 times a day including before going to bed in case of need.

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

Dose adjustment is necessary for patients with a renal failure, frequency rate of reception should not exceed 1-2 times during the day.

Features of use:

Data on use of a domperidon during pregnancy are not enough. So far people do not have data on increase in risk of malformations. However it is necessary to appoint домперидон at pregnancy only if its use is justified by the expected therapeutic advantage for mother and the minimum risk for a fruit.

At women concentration of a domperidon in breast milk makes from 10 to 50% of the corresponding concentration in plasma and does not exceed 10 ng/ml. Total quantity of the domperidon excreted in breast milk – less than 7 mkg a day at use of the most admissible doses of a domperidon. It is unknown whether this concentration makes negative impact on babies. In this regard at use of a domperidon in the period of a lactation it is necessary to stop breastfeeding.

At the combined reception of a domperidon with the antiacid drugs or means reducing secretion of a gastric juice the last should be accepted after food, but not to food, i.e. they should not be accepted along with domperidony.

Impact on ability to drive the car and to work with the equipment. Domperidon does not influence ability to manage vehicles and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: gastrointestinal frustration (passing enterospasms).

From a nervous system: extrapyramidal frustration (children and at persons with GEB hyperpermeability, at adults have isolated cases); these phenomena are completely reversible and disappear after the termination of administration of drug.

Allergic reactions: skin rash, small tortoiseshell.

Others: giperprolaktinemiya (galactorrhoea, gynecomastia, amenorrhea).

Interaction with other medicines:

Cimetidinum, Natrii hydrocarbonas reduce bioavailability of a domperidon.

M-holinoblokatory and antiacid medicines neutralize action of a domperidon.

Increase concentration of a domperidon in plasma CYP3A4 isoenzyme inhibitors: antifungal medicines of an azolovy row, antibiotics from group of macroleads, HIV protease inhibitors, нефазодон (antidepressant). At joint reception with ketokonazoly approximately triple increase in the maximum concentration of a domperidon is reached.

The concomitant use with paracetamol and digoxin did not exert impact on concentration of these medicines in blood.

Let's combine with antipsychotic medicines (neuroleptics) and with agonists of dofaminergichesky receptors (Bromocriptinum, a levodopa).

Contraindications:

Hypersensitivity, bleedings from a GIT, mechanical intestinal impassability, perforation of a stomach or intestines, a prolaktinom, the lactation period, children's age (up to 5 years and to children with body weight to 20 kg).

With care. At the pregnancy expressed to a renal and/or liver failure.

Overdose:

Symptoms: drowsiness, a disorientation, extrapyramidal frustration (especially at children).

Treatment: reception of absorbent carbon, at extrapyramidal disturbances – m-holinoblokatory, protivoparkinsonichesky medicines or antihistaminic drugs with anticholinergic properties.

Storage conditions:

In the dry, protected from light place, at a temperature not over 25 ºС. To store in places, unavailable to children. Period of validity 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated 10 mg.

On 10 tablets in a blister strip packaging from the film of PVC and printing aluminum foil varnished.

1, 2, 3, 4 or 5 blister strip packagings with the instruction in a pack from a cardboard.