Domidon

General characteristics. Structure:

Active ingredient: domperidone;

1 tablet contains a domperidon of 10 mg;

excipients: lactoses monohydrate, starch corn, cellulose microcrystallic, starch prezhelatinizirovanny, povidone, magnesium stearate. Film cover: Sepifilm 752 Blanc.

Pharmacological properties:

Domperidon – a stimulator of motility of digestive tract. The mechanism of action is caused by blockade of dopamine (D2) receptors thanks to what the inhibiting influence of a dopamine on motor function of digestive tract is eliminated. Increases duration of peristaltic reductions of antral department of a stomach and duodenum, accelerates motility of a stomach, raises a tone of the lower sphincter of a gullet. Does not influence gastric secretion. Has the antiemetic effect caused by a combination of gastrokinetichesky effect and antagonism to dopamine receptors in the trigger zone of chemoceptors located out of a blood-brain barrier. Eliminates a hiccups and nausea.

It is quickly and completely soaked up in a digestive tract. Is exposed to intensive metabolism in a wall of intestines and liver therefore has low bioavailability – about 15%. Meal and decrease in acidity of a gastric juice slow down and reduce absorption of a domperidon. The maximum concentration in blood is reached in 60 min. Linkng with proteins of plasma – 91-93%. Badly gets through a blood-brain barrier. Comes to breast milk where its level makes about ¼ from concentration in a blood plasma. It Biotransformirutsya by a hydroxylation and N-dezalkirovaniya. The elimination half-life makes 7-9 hours, at the expressed renal failure increases. It is brought out of an organism through intestines (66%) and kidneys (33%), including in not changed type of 7-10% and 0,4-1% respectively.

Indications to use:

Adults. Nausea and vomiting, epigastric feeling of overflow, pain in an upper part of a stomach, heartburn with emission of contents of a stomach in a mouth or without emission.

Children. Nausea and vomiting.

Route of administration and doses:

Domidon is recommended to apply orally, to food. At reception after food absorption is a little slowed down.

To adults and children (12 years with the body weight of 35 kg and are more senior more) appoint 10-20 mg

(1-2 tablets) 3 times a day in 15-30 minutes prior to food and if it is necessary, before going to bed.

The maximum daily dose of drug – 80 mg.

Duration of primary treatment – 4 weeks. The doctor defines need of further use of drug.

At a renal failure it is necessary to reduce the frequency of administration of drug; at a liver failure the patient should not appoint drug (watch the section "Appropriate Security Measures at Use").

Features of use:

Use during pregnancy or feeding by a breast.

Domidon is not recommended to apply during pregnancy. Drug gets into breast milk therefore it is not recommended to use drug during feeding by a breast.

Ability to influence speed of response at control of motor transport or work with other mechanisms. It is necessary to refrain from management atotransporty and works with other mechanisms during treatment as drug.

Children. To children up to 12 years with body weight drug in this dosage form is not recommended to appoint less than 35 kg.

Drug is used for treatment of children 12 years with the body weight of 35 kg and are more senior more.

Side effects:

From immune system: very seldom – anaphylactic reactions, including an acute anaphylaxis, a Quincke's disease, a small tortoiseshell, allergic reactions.

From endocrine system: seldom – increase in level of prolactin.

Mental disorders: seldom – nervousness, it is very rare – agitation.

From a nervous system: often – dryness in a mouth, a headache; infrequently – sleeplessness, dizziness, thirst, slackness, irritability; seldom – extrapyramidal side effects; very seldom – drowsiness, spasms.

From cardiovascular system: seldom – swelled, a heart consciousness; disturbance of frequency and rhythm of cordial reductions: lengthening of an interval of QT, ventricular arrhythmias.

From digestive tract: seldom – gastrointestinal frustration, including abdominal pain, diarrhea, regurgitation, appetite change, nausea, heartburn, a lock; very seldom – short-term intestinal spasms.

From skin and hypodermic cellulose: seldom – an itch, rash.

From reproductive system and mammary glands: seldom – a galactorrhoea, a gynecomastia, an amenorrhea.

Frustration from an urinary system: seldom – a frequent urination, a dysuria.

Disturbance from a musculoskeletal system and connecting fabric: seldom – onychalgias, an adynamy.

Others: seldom – konyunktivit, stomatitis.

Change of laboratory indicators: increase in the ALT, nuclear Heating Plant level and cholesterol.

As the hypophysis is outside a blood-brain barrier, use of a domperidon can lead to increase in prolactin. Seldom the giperprolaktinemiya can result in neuroendocrinal side effects, such as a galactorrhoea, a gynecomastia and an amenorrhea.

Very seldom at adults the extrapyramidal phenomena were observed. These side reactions disappear completely after drug phase-out.

Other side effects connected with a nervous system – spasms, agitation and drowsiness were observed very seldom.

Interaction with other medicines:

Anticholinergic drugs can neutralize effect of drug Domidon. Bioavailability of drug at intake decreases after the previous reception of Cimetidinum or Natrii hydrocarbonas. It is not necessary to accept antiacid and anti-secretory drugs along with drug Domidon as they reduce its bioavailability after intake. The main way of metabolic transformations of a domperidon occurs with the participation of an isoenzyme of CYP 3A4 of system of P450 cytochrome therefore at the simultaneous use of a domperidon and medicines considerably inhibiting this isoenzyme increase in level of a domperidon in plasma is possible. Examples of inhibitors of an isoenzyme of CYP 3A4 are the following medicines: antifungal drugs of an azolovy row (fluconazole, интраконазол, кетоконазол, вориконазол), antibiotics of group of macroleads (кларитромицин, erythromycin), HIV protease inhibitors (ампренавир, атазанавир, фозампренавир, индинавир, нелфинавир, ритонавир, саквинавир), antagonists of calcium (diltiazem, verapamil), Amiodaronum, aprepitant, нефазодон, телитромицин.

At simultaneous use of drug with m cholinolytics and narcotic analgetics influence of a domperidon on a motor evakuatornuyu activity of a stomach and intestines decreases.

Simultaneous use with ketokonazoly, erythromycin or other potential CYP3A04 inhibitors can lead to increase in an interval of QT.

At simultaneous use of a domperidon in a dose of 10 mg 4 times a day and a ketokonazol in a dose of 200 mg twice a day were observed lengthening of an interval of QT on 10-20 ms. At monotherapy domperidony both in similar dosing, and at reception of a daily dose of 160 mg (that is twice higher than the most admissible daily dose), clinically significant changes of an interval of QT were not observed.

Digoxin or paracetamol at a concomitant use of a domperidon does not influence the level of these drugs in blood.

Domidon can be combined with neuroleptics which action he does not strengthen also; agonists of dopaminergic receptors (Bromocriptinum, L-finish singing), which undesirable peripheral effects, such as digestion disturbances, nausea, vomiting, it suppresses, without neutralizing their main properties.

Contraindications:

Hypersensitivity to a domperidon or to any of drug components.
Cases when stimulation of motor function of digestive tract can be dangerous (for example, gastrointestinal bleedings, mechanical intestinal impassability, perforation of a stomach or intestines).
The patient about prolactin - the cosecreting tumor of a hypophysis (prolaktinom).
Concomitant use of peroral forms of a ketokonazol, erythromycin or other strong CYP 3A4 inhibitors, medicines which extend QT interval, such as флуконазол, вориконазол, кларитромицин, Amiodaronum, телитромицин (see the section "Interaction with Other Medicines and Other Types of Interactions").

Appropriate security measures at use.

 

Domidon it is not necessary to accept along with antiacid or anti-secretory drugs.

Drug contains lactose therefore patients should not appoint it with rare hereditary forms of intolerance of a galactose, deficit of lactase or a syndrome of glyukozo-galaktozny malabsorption.

In view of a high metabolic rate of a domperidon in a liver, it is not necessary to appoint drug sick with a liver failure.

At patients with a heavy renal failure (plasma creatinine> of 6 mg / 100 ml, i.e.> 0,6 mmol/l) the elimination half-life of a domperidon increased from 7,4 to 20,8 o'clock, but concentration of drug in plasma was lower, than at healthy volunteers. As the insignificant percent of drug is removed by kidneys in not changed look, the single dose can be not adjusted. But at prolonged use of a domperidon it is necessary to reduce the frequency of administration of drug to 1–2 times a day depending on weight of disturbances of functions of kidneys. Also there can be a need of a dose decline. At long therapy these patients have to be under regular observation of the doctor.

Domperidon patients should apply with care with risk factor of prolongation of an interval of QT, including a hyperpotassemia, a heavy gipermagniyemiya, organic heart diseases, a concomitant use of medicines which extend QT interval.

Overdose:

Symptoms: drowsiness, disorientation, extrapyramidal frustration.

Treatment: drug withdrawal, reception of absorbent carbon. For elimination of extrapyramidal symptomatology use holinoblokiruyushchy drugs, means for treatment of parkinsonism or antihistaminic drugs with anticholinergic action.

Storage conditions:

Period of validity. 3 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister. On 1 or 3 blisters enclosed in a pack.