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medicalmeds.eu Medicines Antiemetic — dopamine receptors a blocker central. Motilak

Motilak

Препарат Мотилак. ОАО "ВЕРОФАРМ" Россия


Producer: JSC VEROPHARM Russia

Code of automatic telephone exchange: A03FA03

Release form: Firm dosage forms. Tablets.

Indications to use: Esophagitis. Eructation. Meteorism. Heartburn. Nausea.


General characteristics. Structure:

Acting substance: 1 таб. домперидон 10 mg. Excipients: fructose (advantoza of FS 95), sugar (sucrose), dextrose, полипласдон EL-10 X (кросповидон), sodium carboxymethylstarch (примогель), magnesium stearate, peppermint oil.




Pharmacological properties:

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 intake, on an empty stomach — bystry (reception after food, reduced acidity of a gastric juice slow down and reduce absorption). The maximum concentration in a blood plasma (TCmax) — 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 a gematoentsefalich-sky barrier (GEB). It is metabolized in a liver and in an intestines wall (by a hydroxylation and N-dealkylation). It is removed through intestines of 66%, kidneys — 33%, in t.   h in not changed look — 10 and 1% respectively. The elimination half-life (T1/2) — 7–9 h, at the expressed chronic renal failure (CRF) — is extended.


Indications to use:

The complex of dispepsichesky symptoms which is often associated 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 gastric contents in an oral cavity. The nausea and vomiting of a functional, organic, infectious origin caused by radiotheraphy, medicinal therapy or disturbances 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 бромкриптин).


Route of administration and doses:

Tablets: it is necessary to rassasyvat 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 and  in case of need in addition before going to bed. At the expressed nausea and vomiting — on 20 mg 3–4 times a day and before going to bed. 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:

Pregnancy and lactation. Use of drug in the I trimester of pregnancy is possible only in cases when the expected advantage of therapy for mother surpasses potential risk for a fruit. So far   the person does not have data on increase in risk of malformations. At women concentration of a domperidon in breast milk is 4 times lower, than the corresponding concentration in plasma. It is unknown whether renders домперидон in this concentration negative influence on newborns. Therefore in the period of a lactation (breastfeeding) Motilak's use is not recommended, except for cases when the expected advantage of therapy for mother surpasses potential risk for the baby.

With care: Renal/liver failure, lactation period, pregnancy.


Side effects:

 From the alimentary system: passing enterospasms.

 From a nervous system: extrapyramidal frustration (at children and at persons with GEB hyperpermeability).

Allergic reactions: skin rash, small tortoiseshell.

Others: giperprolaktinemiya (galactorrhoea, gynecomastia).


Interaction with other medicines:

Cimetidinum, Natrii hydrocarbonas reduce bioavailability of a domperidon. The anticholinergic and antiacid medicines (M) neutralize action of a domperidon. Increase concentration of a domperidon in plasma: antifungal medicines of an azolovy row, antibiotics from group of macroleads, HIV protease inhibitors, нефазодон (antidepressant). Let's combine with reception of antipsychotic HP (neuroleptics), agonists of dofaminergichesky receptors (Bromocriptinum, L-dopa). The concomitant use with paracetamol and digoxin did not exert impact on concentration of these HP in blood.


Contraindications:

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


Overdose:

Symptoms: drowsiness, a disorientation, extrapyramidal frustration (especially at children). Treatment: reception of absorbent carbon, at extrapyramidal disturbances — anticholinergic HP, protivoparkinsonichesky or antihistaminic HP with anticholinergic properties.


Storage conditions:

Period of validity 2 years. Not to use after the period of validity specified on packaging. In dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C.


Issue conditions:

Without recipe


Packaging:

On 10 tablets in a blister strip packaging; on 1 or 3 blister strip packagings together with  the application instruction in a pack. On 30 tablets in bank of light-protective glass. Each can together with  the application instruction is placed in a pack.



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