The instruction for medical use of Doprokin Torgovoye medicine a name Doprokin Mezhdunarodnoye the unlicensed name Domperidon Lekarstvennaya a form of the Tablet, 10 mg Structure 1 tablet contains active agent – domperidon 10 mg, excipients: starch of corn 40 mg, cellulose microcrystalline (Avicel PH 101) of 65.5 mg, silicon dioxide colloidal anhydrous (Aerosil 200) of 0.5 mg, K25 6 povidone of mg, sodium lauryl sulfate of 1 mg, magnesium stearate of 1 mg, talc of 1 mg. Description White round biconvex tablets. Pharmacotherapeutic group Drugs for treatment of functional disorders of digestive tract. Stimulators of motility of digestive tract. Domperidon. The ATX A03FA03 code the Pharmacological Pharmacokinetics Domperidon properties is quickly absorbed at oral administration on an empty stomach. The maximum concentration it in plasma is reached approximately within 1 hour. Low absolute biological availability of an oral way of introduction of a domperidon (about 15%) is caused by extensive primary metabolism in a wall of intestines and liver. Though at healthy people the biological availability of a domperidon increases at reception after a meal, patients with complaints from digestive tract should accept domperidon in 15-30 minutes prior to food. The Gipoatsidnost of gastric juice reduces absorption of a domperidon. Oral biological availability decreases after the previous intake of Cimetidinum or sodium bicarbonate. At reception of a domperidon after a meal the achievement of the maximum absorption requires more time, and AUC increases a little. At oral administration domperidon does not accumulate and own exchange, the maximum concentration in plasma in 90 minutes after introduction, equal 21 ng/ml, after two-week oral administration does not induce 30 mg a day, was almost same, as after reception of the first dose (18 ng/ml). Domperidon for 91-93% contacts proteins of plasma. Concentration of a domperidon in breast milk of the feeding women are 4 times lower, than the corresponding concentration in plasma. Domperidon is metabolized in a liver by hydroxylation and N-dealkylation. Removal with urine and a stake makes 31% and 66% of an oral dose respectively. Discharge of a domperidon in not changed look makes small percent (10% with a stake and about 1% with urine). Plasma elimination half-life after reception of a single dose makes 7-9 hours at healthy people, but is extended at patients with a heavy renal failure. Doprokin’s pharmacodynamics – antiemetic drug, a stimulator of motility of digestive tract for oral administration. Domperidon – the antagonist of dopamine possessing similar to Metoclopramidum and some neuroleptics, antiemetic properties. However, unlike these medicines, domperidon badly gets through a blood-brain barrier. Use of a domperidon seldom is followed by extrapyramidal side effects, especially at adults, but domperidon stimulates prolactin discharge 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. At use inside domperidon increases duration of antral and duodenal reductions, accelerates gastric emptying – an exit of liquid and semisolid fractions at healthy people and firm fractions at patients at whom this process was slowed down, and increases pressure of a sphincter of a lower part of a gullet at healthy people. Domperidon has no effect on gastric secretion. Indications – relief of symptoms of nausea and vomiting. The route of administration and doses to Adult children at the age of 12 years are also more senior: on 1 tablet 3 times a day. It is recommended to take the pill Doprokin to food, in case of their reception after a meal the absorption of a domperidon can slow down. If administration of drug is missed, the passed dose should be excluded, having renewed the appointed reception mode. The passed dose of drug should not be doubled to compensate the missed reception. Duration of treatment should not exceed one week. Side effects on condition of observance of recommendations about a dosage and duration of treatment domperidon it is usually transferred well, and the undesirable phenomena arise infrequently. From the immune system: allergic reactions, including an anaphylaxis, an acute anaphylaxis, a Quincke’s disease, a small tortoiseshell, hypersensitivity. From an endocrine system: increase in level of prolactin. Mental disorders: nervousness, irritability, agitation, depression, uneasiness, decrease or lack of a libido. From nervous system: dryness in a mouth, insomnia, dizziness, thirst, spasms, slackness, a headache, drowsiness, an akathisia, extrapyramidal disorders. From a cardiovascular system: hypostasis, heart consciousness, disturbance of frequency and rhythm of warm reductions, lengthening of an interval QT, serious ventricular arrhythmias, sudden cardiac death. From digestive tract: gastrointestinal disorders, including abdominal pain, regurgitation, change of appetite, nausea, heartburn, a constipation, short-term intestinal spasms, diarrhea. From skin and hypodermic fabrics: itching, rashes. From a reproductive system and mammary glands: a galactorrhoea, a gynecomastia, an amenorrhea, increase in mammary glands, sensitivity of mammary glands, pain in mammary glands, disturbance of a lactation, an irregular menstrual cycle. From the musculoskeletal system and connective tissue: onychalgia, asthenia. From an urinary system: ischuria, dysuria, frequent urination. Other: conjunctivitis, stomatitis. Changes of laboratory indicators: increase in the ALT, nuclear Heating Plant level and cholesterol. As the hypophysis is out of a blood-brain barrier, domperidon can cause increase in level of prolactin. Such giperprolaktinemiya can result in neuroendocrinal side effects, such as galactorrhoea, gynecomastia and amenorrhea. Extrapyramidal by-effects meet only at adults. These side reactions disappear spontaneously and completely soon after the treatment termination. Contraindications – hypersensitivity to a domperidon or any of excipients – gastrointestinal bleeding, mechanical impassability or perforation at which stimulation of motility of a stomach can be dangerous – prolactin – the cosecreting tumors of a hypophysis (prolaktinom) – heavy and moderate degree of a liver failure – patients with disturbances of conductivity now or in the anamnesis, in particular lengthening of an interval of QT on the ECG – patients with the significant disturbances of electrolytic balance or serious heart diseases (for example, stagnant heart failure) – combined use with the medicines extending QT interval – combined use with medicines which are strong CYP3A4 inhibitors (irrespective of their effect to extend QT) – pregnancy and the period of a lactation – children’s age up to 12 years Medicinal interactions It is necessary to avoid use of a domperidon together with ketokonazoly, erythromycin or other powerful CYP3A4 inhibitors as it can lead to lengthening of an interval of QT. Anticholinergic drugs can neutralize action of a domperidon. Oral biological availability of a domperidon decreases after the previous intake of Cimetidinum or sodium bicarbonate. It is not necessary to take the antiacid and anti-secretory drugs along with domperidony as they reduce its biological availability after intake. The main way of metabolic transformations of a domperidon – through CYP3A4. The concomitant use of a domperidon with the medicines considerably inhibiting this enzyme can cause increase in level of a domperidon in blood plasma – antifungal drugs of an azolovy row (flukonazol, itrakonazol, ketokonazol, vorikonazol), antibiotics from group of macroleads (klaritromitsin, erythromycin), HIV protease inhibitors (amprenavir, atazanavir, fosamprenavir, nelfinavir, ritonavir, sakhinavir), nefazodon, antagonists of calcium (diltiazem, verapamil), Amiodaronum, an aprepitant, telitromitsin. Ketokonazol inhibits CYP3A4 – dependent primary metabolism of a domperidon therefore approximately triple increase in the maximum concentration of a domperidon and AUC in a plateau phase is reached. At combined use of a domperidon in a dose of 10 mg 4 times a day and a ketokonazol in a dose of 200 mg 2 times a day are observed lengthening of an interval of QT on 10-20 ms, at monotherapy domperidony clinically significant changes of an interval of QT were not noted. The accompanying use of the following medicines is contraindicated in view of emergence of risk of prolongation of an interval of QT: • antiarrhytmic drugs of the class IA (for example, Disopyramidum, hydroquinidine, quinidine), • antiarrhytmic drugs of class III (for example, Amiodaronum, dofetilida, dronedaron, ibutilid, sotalol), • neuroleptics (for example, haloperidol, Pimozidum, sertindol), • antidepressants (for example, to tsitalopra, estsitalopra), • antibiotics (for example, erythromycin, levofloxacin, moxifloxacin, Spheromycinum), • antifungal means (for example, pentamidine), • antimalarial means (in particular galofantrin, lyumefantriny), • drugs for treatment of diseases of digestive tract (for example, tsizaprid, dolasetron, prukaloprid), • antihistaminic (for example, mekvitazin, mizolastin), • antineoplastic drugs (for example, toremifen, vandetanib, Vincaminum), • drugs of various groups (for example, bepridit, difemanit, methadone). Use of a domperidon for patients against the background of intake of paracetamol or the picked-up therapy with digoxin did not influence the level of these drugs in blood. Domperidon can be combined also with neuroleptics which action he does not strengthen, agonists of dofaminergichesky receptors (Bromocriptinum, L-finish singing) which undesirable peripheral effects, such as digestion disturbances, nausea, vomiting, he suppresses, without neutralizing their main properties. It is not recommended to accept at the same time with moderate CYP3A4 inhibitors, for example, diltiazem, verapamil and some macroleads. It is required to be careful at simultaneous use of medicines at the inducing development of bradycardia and a hypopotassemia and also with macroleads the azithromycin and roksitromitsi-numbers extending QT interval (klaritromitsin it is contraindicated for use as strong CYP3A4 inhibitor). Special instructions it is not necessary to take the Antiacid or anti-secretory drugs along with the drug Doproksen as they reduce oral bioavailability of a domperidon. At combined use domperidon it is necessary to accept before food, antiacid or anti-secretory drugs – after a meal. It is not necessary to exceed the recommended dose or to independently prolong the therapy course recommended by the doctor. Patients at whom nausea and vomiting proceed more than 48 hours need to see a doctor. Patients at whom discomfort symptoms after a meal do not pass and which should accept constantly domperidon within more than 2 weeks should see a doctor. Doproksen patients should apply with care with risk factors of prolongation of an interval of QT, including a hypopotassemia, a heavy hypomagnesiemia, organic heart diseases, a concomitant use of the medicines extending QT interval and to patients with slight abnormal liver functions and/or kidneys. It is necessary to consider the following information on risk of development of complications of the cardiovascular diseases caused by the medicines containing domperidon: • some epidemiological researches were shown that domperidon can be associated with the increased risk of serious ventricular arrhythmias or a sudden cardiac death, • the risk of serious ventricular arrhythmias or a sudden cardiac death can be higher at patients at the age of 60 years or at oral administration of doses of drug more than 30 mg a day, • domperidon should appoint adults and children in the lowest effective dose. Domperidon is not recommended to use for the purpose of motion desease relief of symptoms. If you established intolerance of some sugars, consult with the doctor before taking this drug as drug contains lactose. Pregnancy and the period of a lactation Data on post-marketing use of a domperidon to pregnant women are limited. Therefore Doproksen during pregnancy it is necessary to appoint only when, according to the doctor, the expected positive effect for mother exceeds potential risk for a fruit. In researches it was shown what domperidon gets into breast milk. It is unknown whether it harms the baby therefore mothers accepting Doproksen should refrain from feeding by a breast. Features of influence of medicine on ability to run the vehicle or potentially dangerous by mechanisms Considering possible side effect from nervous system, patients need to be attentive at control of motor transport or work with other mechanisms. Overdose Symptoms: agitation, disturbance of consciousness, a spasm, a disorientation, drowsiness and extrapyramidal reactions can be symptoms of overdose. Treatment. There is no specific antidote of a domperidon, but in case of considerable overdose the gastric lavage within one hour and use of activated carbon and also careful observation of the patient and maintenance therapy is recommended. Anticholinergic drugs, drugs for treatment of Parkinson’s disease can be effective for control of extrapyramidal reactions. The form of release and packing On 10 tablets place in blister strip packagings from a film of polyvinylchloride and aluminum foil. On the 2nd planimetric packing together with the instruction for medical use in the state and Russian languages place in a cardboard pack. To Store storage conditions at a temperature not above 25 °C. To store out of children’s reach! 3 years not to apply a period of storage after an expiration date. Prescription status Without prescription SEDIKO Pharmaceutical Co. Producer, the First industrial zone, Six ov Oktober City, Egypt. “SEDICO Pharmaceutical Co.”, First Industrial Zone, 6th October City, Egypt. Owner of the registration certificate of UORLD MEDITSIN LIMITED, LONDON/GREAT BRITAIN. (“WORLD MEDICINE LIMITED”, LONDON/GREAT BRITAIN). The address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products of RIN Pharm LLP, RK, Almaty, Turksibsky district, Suyunbaya Ave., 222b the Address of the organization responsible for post-registration observation of safety of medicine, TROKA-S PHARMA LLP acting through Toleuisheva Sandugash, Almaty, Suyunbaya Ave., 222b
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