Domperidon

General characteristics. Structure:

Active ingredient: 10 mg of a domperidon.

The drug rendering the pro-kinetic, antiemetic, normalizing functions of bodies of a GIT action.

Pharmacological properties:

Pharmacodynamics. Blocks dopamine D2 receptors. Pro-kinetic properties are connected with blockade of peripheral dopamine receptors and elimination of the inhibiting influence of dopamine on the GITs functions. Increases duration of peristaltic reductions of antral department of a stomach and duodenum, improves work of a stomach, accelerating its emptying in case of delay of this process, raises a tone of the lower esophageal sphincter. Antiemetic action is caused by a combination of peripheral (gastrokinetichesky) action and blockade of chemoceptors of a trigger zone of the emetic center. Domperidon prevents development or reduces expressiveness of nausea and vomiting. Increases prolactin level in blood serum.

Pharmacokinetics. After intake it is quickly soaked up from a GIT (meal or the lowered acidity of a gastric juice slow down and reduce absorption). Cmax  in blood is reached in 0,5–1 h. Bioavailability — 15% (there is an effect of "the first passing" through a liver). Linkng with proteins of plasma makes 91–93%. Badly gets through GEB. In a small amount it is found in breast milk. Is exposed to intensive metabolism in a wall of intestines and liver (by a hydroxylation and N-dealkylation) with formation of a gidroksidomperidon and 2,3-дигидро-2-оксо-1-H-бензимидазол-1-пропионовой acids respectively. T1/2  after reception of a single dose makes the 7th p. T1/2 is extended at a chronic renal failure. It is removed by kidneys (31%) and through intestines (66%), including in not changed type of 1 and 10%, respectively. At patients with an abnormal liver function drug cumulation is possible.

Indications to use:

Dispeptic disturbances against the background of the slowed-down gastric emptying, a gastroesophageal reflux disease: feeling of overflow in epigastriums, feeling of abdominal distention, pain in an upper part of a stomach, an eructation, a meteorism, heartburn with throwing or without throwing of contents of a stomach in an oral cavity. Nausea and vomiting of various genesis (including against the background of functional and organic diseases, infections, at a toxaemia, radiation therapy, disturbances of a diet, medicinal genesis, including at reception of agonists of dopamine — levodopas, Bromocriptinum, when carrying out endoscopic and X-ray contrast researches GITs); hiccups, GIT atony (including postoperative); need of acceleration of a vermicular movement when carrying out X-ray contrast researches GITs.

Route of administration and doses:

Inside, in 15–30 min. prior to food. The adult — on 10 mg 3–4 times a day, if necessary a dose raise to 60 mg/days. The dose for children is calculated depending on body weight.

Features of use:

It is not necessary to appoint for prevention of postoperative vomiting.

Use at pregnancy and feeding by a breast. It is possible if the expected effect of therapy exceeds potential risk for a fruit and the child (researches at pregnant women are not conducted, low concentration of a domperidon are found in breast milk of women).

Side effects:

From bodies of a GIT: a spasm of smooth muscles of a GIT, dryness in a mouth, stomatitis, thirst, heartburn, appetite change, lock/diarrhea.

From a nervous system and sense bodys: extrapyramidal frustration (at children and patients with GEB hyperpermeability), a headache, an adynamy, irritability, nervousness, drowsiness, spasms of legs, a lethargy, conjunctivitis (an itch, redness, pain, puffiness of eyes).

Allergic reactions: skin rash, itch, small tortoiseshell, hypostasis (persons, hands, shins or foot).

Others: increase in level of prolactin in a blood plasma, a galactorrhoea, a gynecomastia, disturbance of a menstrual cycle, a mastalgiya, change of frequency of an urination, a dysuria (burning, difficulty and morbidity at an urination), heartbeat.

Interaction with other medicines:

Antiacid and anti-secretory drugs reduce bioavailability, anticholinergics weaken action of a domperidon.

P450 cytochrome CYP3A4 isoenzyme inhibitors (antifungal drugs of group of azoles, antibiotics of group of macroleads, HIV protease inhibitors) can block metabolism of a domperidon and increase its level in plasma (combined use demands discretion).

With care to apply along with MAO inhibitors.

Influence on absorption of at the same time used drugs with the slowed-down release of active ingredient is not excluded.

Domperidon does not influence the level of paracetamol and digoxin in blood.

Contraindications:

Hypersensitivity, gastrointestinal bleedings, mechanical intestinal impassability, perforation of a stomach or intestines (stimulation of a vermicular movement can aggravate these states), giperprolaktinemiya, prolaktinoma; children's age up to 5 years and children with a body weight up to 20 kg — for tablets.

Restrictions to use. Renal and/or liver failure, pregnancy, feeding by a breast.

Overdose:

Symptoms: drowsiness, arrhythmia, a disorientation, extrapyramidal frustration (especially at children), decrease in the ABP.

Treatment: use of absorbent carbon, at emergence of extrapyramidal reactions — anticholinergics or antihistaminic drugs with anticholinergic activity, the drugs used for treatment of parkinsonism. There is no specific antidote.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 10 mg, 20 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.