Motilak

General characteristics. Structure:

Active ingredient: 10 mg of a domperidon.

Excipients: potato starch, lactoses monohydrate, cellulose microcrystallic, silicon dioxide colloid, polyvinylpirrolidone, magnesium stearate, sodium carboxymethylstarch, metiloksipropiltsellyuloz, polysorbate 80, titanium dioxide, talc.

Antiemetic synthetic drug of the central action.

Pharmacological properties:

Pharmacodynamics. Domperidon increases duration of peristaltic reductions of antral department of a stomach and duodenum, accelerates gastric emptying in case of delay of this process, raises a tone of the lower esophageal sphincter, eliminates development of nausea and vomiting.

Domperidon badly gets through a blood-brain barrier therefore use of a domperidon seldom is followed by extrapyramidal side effects, especially at adults, but домперидон stimulates release of prolactin from a hypophysis. Its antiemetic action, perhaps, is caused by a combination of peripheral (gastrokinetichesky) action and antagonism to dopamine receptors in a trigger zone of chemoceptors. Domperidon has no effect on gastric secretion.

Pharmacokinetics. Absorption. After administration of drug inside домперидон it is quickly soaked up. Has low bioavailability (about 15%). The lowered acidity of gastric contents reduces absorption of a domperidon. The maximum concentration in plasma is reached in 1 h.

Distribution. Domperidon is widely distributed in various fabrics, in brain tissues its concentration is small. Linkng with proteins of plasma makes 91-93%.

Metabolism. Is exposed to intensive metabolism in a wall of intestines and liver.

Removal. It is removed through intestines (66%) and kidneys (33%), in an invariable look 10% and 1% of dose size are removed, respectively. The elimination half-life makes 7-9 h, at the expressed renal failure it is extended.

Indications to use:

a) a complex of the dispepsichesky symptoms connected with the slowed-down gastric emptying, a gastroesophagal reflux, an esophagitis:
 • feeling of overflow in epigastriums, feeling of abdominal distention, pain in an upper part of a stomach;
 • eructation, meteorism;
 • heartburn with throwing or without throwing of contents of a stomach in an oral cavity.

b) the nausea and vomiting of a functional, organic, infectious origin caused by radiotheraphy, medicinal therapy or disturbance of a diet and also against the background of dopamine agonists in case of their use at Parkinson's disease (such as L-dopa and Bromocriptinum).

At introduction by an animal in doses to 160 mg/kg/days of Motilak had no teratogenic effect. However, as the majority of medicines, Motilak it is necessary to appoint during the first trimester of pregnancy only if its use is justified by the expected therapeutic advantage. So far people do not have data on increase in risk of malformations. At women of concentration of a domperidon in breast milk is 4 times lower, than the corresponding concentration in plasma. It is unknown whether this level makes negative impact on newborns. Therefore if mother accepts Motilak, feeding by a breast is not recommended, except for cases when the expected advantage justifies potential risk.

Route of administration and doses:

1. Chronic dyspepsia
Adults: on 10 mg (1 tablet) 3 times a day, in 15-30 min. prior to food and in case of need, before going to bed. Children are more senior than 5 years: on 2,5 mg on 10 kg of body weight. 3 times a day to food and in case of need, before going to bed. If necessary the specified dosage can be doubled.

2. Acute and subacute states (first of all nausea and vomiting).
Adults: on 20 mg (2 tablets) 3-4 times a day to food and before going to bed. Children are more senior than 5 years: on 5 mg on 10 kg of body weight, 3-4 times a day before food and before going to bed.

Oral administration of Motilak to food is recommended. At administration of drug after food absorption is a little slowed down.

At a renal failure reduction of frequency of administration of drug is recommended.

Features of use:

At the combined use of Motilak with antiacid or anti-secretory drugs the last should be accepted after food, but not to food, i.e. they should not be accepted along with Motilak.

Considering metabolism of a domperidon in a liver, it is necessary to appoint it with care the patient with a liver failure.

At patients with a heavy renal failure (serumal creatinine> of 6 mg / 100 ml, i.e.> 0,6 mmol/l) the elimination half-life of a domperidon increases from 7,4 to 20,8 o'clock, but concentration of drug in plasma were lower, than at healthy volunteers. As very small percent of drug is removed by kidneys in not changed look, correction of a single dose at patients with a renal failure is hardly necessary. However at repeated appointment the frequency of introduction has to be reduced to 1-2 times a day, depending on weight of insufficiency, there can also be a need of dose declines. At long therapy patients have to be under regular observation.

Domperidon does not break speed of reaction.

Side effects:

Side effects are observed seldom, exceptional cases of passing enterospasms were celebrated. The extrapyramidal phenomena are observed at children and at a hyperpermeability of a blood-brain barrier. These phenomena are completely reversible and spontaneously disappear after the treatment termination. As the hypophysis is out of a blood-brain barrier, домперидон can induce increase in level of prolactin in plasma. In rare instances this giperprolaktinemiya can stimulate emergence of a galactorrhoea, gynecomastia and dysmenorrhea. Rare allergic reactions, such as rash and urticaria were noted.

Interaction with other medicines:

At simultaneous use anticholinergic drugs can neutralize action of a domperidon. At simultaneous use with Motilak antiacid and anti-secretory drugs reduce its bioavailability. On the basis of the researches in vitro it is possible to assume that at simultaneous use with Motilak of the medicines considerably inhibiting enzyme CYP3A4 cytochrome (antifungal drugs of group of azoles, antibiotics from group of macroleads, HIV protease inhibitors, antidepressant нефазодон) increase in level of a domperidon in plasma can be observed. Domperidon does not influence the level of paracetamol and digoxin in blood. It is not excluded that домперидон can influence absorption applied at the same time in drugs with the slowed-down release of active agent or covered with a kishechnorastvorimy cover.

Contraindications:

The established intolerance of drug, prolactin - the cosecreting tumor of a hypophysis (prolaktinom), children's age up to 5 years. It is not necessary to apply Motilak when stimulation of motive function of a stomach can be dangerous, i.e. at gastrointestinal bleeding, mechanical impassability or perforation.

Overdose:

Extrapyramidal frustration, the increased drowsiness, disorientation in space and time are registered. Purpose of enterosorbents is recommended (absorbent carbon), a timely gastric lavage, purpose of posindromny therapy.

Antihistaminic medicines help to stop extrapyramidal disturbances.

Storage conditions:

Store in the place protected from moisture and light at a temperature not above 30 °C. Store in the place, unavailable to children. Period of storage of 5 years.

Issue conditions:

Without recipe

Packaging:

Tablets on 10 mg, coated. On 10 tablets in planimetric yacheykoyovy packaging. On the 3rd blister strip packagings in a pack.