Motilium Express tab to the races. 10 mg 30 pcs

Description

Composition
Active substance:
10 mg domperidone.
Excipients:
Gelatin 5.513 mg Mannitol 4.136 mg Aspartame 0.750 mg, 0.300 mg mint essence, Poloxamer 188 1.125 mg.
Description:
White or almost white round tablets for sucking.
Product form:
10 tablets for sucking in a blister made of PVC-PVDC-PE / aluminum.
3 blisters with instruction for medical use in a cardboard package.
Contraindications
– increased sensitivity to domperidone or any of the components;
– prolactin-secreting pituitary tumor (prolactinoma);
– simultaneous reception oral forms of ketoconazole, erythromycin or other potent inhibitors of isoenzyme CYP3A4, causing elongation interval QTc, such as clarithromycin, itraconazole, fluconazole, posaconazole, ritonavir, saquinavir, amiodarone, telithromycin, telaprevir and voriconazole (see sections “Specific guidance”. “Interaction of c other drugs”);
– gastrointestinal bleeding, perforation, or mechanical obstruction (ie, when the stimulation of gastric motility can be dangerous..);
– human liver moderate and severe;
– phenylketonuria;
– body weight less than 35 kg;
– Children under 12 years of age with a body weight
Patients with impaired liver function and kidney
Since a very small percentage of the drug is excreted unchanged by the kidneys, the single dose adjustment in patients with renal impairment is not required. However, on repeated administration Motilium® EXPRESS frequency of application should be reduced to one or two times a day, depending on the severity of renal function (see. The section “Method of administration and dose”). During prolonged therapy, patients should be regularly monitored.
C care – renal dysfunction;
– violation of rhythm and conduction of the heart, including the lengthening of the interval QT, electrolyte disturbances, congestive heart failure.
Dosage
10 mg
Indications
a) Complex of dyspeptic symptoms, often associated with delayed gastric emptying, gastroesophageal reflux, esophagitis:
– a feeling of fullness in the epigastrium, sense of abdominal distention, pain in the upper abdomen;
– belching, flatulence;
– nausea, vomiting;
– heartburn, belching.
b) Nausea and vomiting of functional, organic, infectious origin, as well as caused by radiotherapy, drug therapy, or violation of the diet.
A specific indication is nausea and vomiting caused by dopamine agonists in the case of Parkinson’s disease (such as levodopa and bromocriptine).
Interaction with other drugs
Anticholinergic drugs may neutralize the effect of Motilium EXPRESS drug.
Oral bioavailability Motilium EXPRESS decreases after prior reception of cimetidine or sodium hydrogencarbonate. Do not take antacids and antisecretory drugs in conjunction with domperidone, as they reduce its bioavailability after oral administration (see. section “Special Instructions”).
A major role in the metabolism of domperidone plays isoenzyme CYP3A4. The results of in vitro studies and clinical experience indicate that the simultaneous use of drugs, which significantly inhibit this isoenzyme may cause an increase in plasma concentrations of domperidone.
Among the strong CYP3A4 isoenzyme inhibitors include:
• azole antifungals such as fluconazole *, itraconazole, ketoconazole * and voriconazole *;
• Antibiotics, macrolides such as clarithromycin * and erythromycin *;
• HIV protease inhibitors, e.g., amprenavir, atazanavir, fosamprenavir, indinavir, nelfinavir, ritonavir and saquinavir;
• calcium antagonists such as diltiazem and verapamil;
• Amiodarone *;
• aprepitant;
• Nefazodone;
• telithromycin *.
(Formulations asterisk further lengthen the interval QTc (see. The section “Contra ‘)).
Several studies have pharmacokinetic and pharmacodynamic interactions of domperidone with oral ketoconazole or oral erythromycin in healthy volunteers have shown that these drugs significantly inhibited the primary metabolism of domperidone exercised isoenzyme CYP3A4.
When simultaneous administration of 10 mg of domperidone 4 times a day, and 200 mg of ketoconazole 2 times a day interval QTc prolongation observed on average 9.8 ms over the entire period of observation, at certain moments changes ranged from 1.2 to 17.5 msec. When simultaneous administration of 10 mg of domperidone 4 times a day, and 500 mg of erythromycin 3 times daily observed lengthening QTc interval on average 9.9 ms over the entire period of observation, at certain moments of change varied between 1.6 and 14.3 ms. In each of these studies Cmax and AUC of domperidone were increased about three times (see. The section “Contra ‘).
At the present time it is not known what kind of contribution to the change in the QTc interval is made higher plasma concentrations of domperidone.
In these studies, monotherapy with domperidone (10 mg four times a day) resulted in a lengthening of QTc interval 1.6 msec (ketoconazole study) and
2.5 ms (research erythromycin), whereas ketoconazole monotherapy (200 mg twice daily) and erythromycin monotherapy (500 mg tid) resulted in a lengthening of the QTc interval 3.8 and 4.9 ms, respectively, during the observation period.
In another study using multiple doses in healthy volunteers found no significant elongation of QTc interval during stationary monotherapy domperidone (40 mg four times a day, the total daily dose is 160 mg, which is significantly greater than the recommended maximum daily dose). In this case, domperidone plasma concentrations were similar to those in studies of interaction with other drugs domperidone.
Theoretically, since Motilium® EXPRESS has gastrokinetic action, it could affect the absorption of both an oral preparations, particularly preparations with sustained release of active substances, or preparations, enteric-coated. However, the use of domperidone in patients while taking paracetamol or digoxin did not affect the levels of these drugs in the blood.
Motilium Express can be taken together with:
• neuroleptics, the action of which it does not increase;
• with dopaminergic receptor agonists (bromocriptine, levodopa) because it inhibits their unwanted peripheral effects such as digestive disorders, nausea and vomiting, without affecting their central effects.
Overdose
symptoms
Cases of overdose have been observed mainly in infants and older children. Overdose symptoms may include irritability, change of consciousness, convulsions, disorientation, somnolence and extrapyramidal reactions.
Treatment
Domperidone specific antidote does not exist. In case of overdose recommended gastric lavage for one hour after drug administration and the use of activated carbon. It is recommended to closely monitor the condition of the patient and supportive therapy. Anticholinergic drugs and drugs used for the treatment of Parkinsonism, may be effective for the relief of any extrapyramidal reactions.
pharmachologic effect
Pharmacological group:
Antiemetic agent, central dopamine receptor blocker.
Pharmacodynamics:
Domperidone – dopamine antagonist that has antiemetic properties. Domperidone does not penetrate the blood-brain barrier. Use of domperidone rarely accompanied by extrapyramidal side effects especially in adults, but domperidone stimulates prolactin release from the pituitary. Its antiemetic effect may be due to a combination of peripheral (gastrokinetic) action and antagonism of dopamine receptors in the chemoreceptor trigger zone, which is outside the blood-brain barrier. Studies in animals and low concentrations of drug detected in the brain, suggest domperidone predominantly peripheral action on dopamine receptors.
Applications inside domperidone increases the duration of antral and duodenal contractions, accelerates gastric emptying and increases the pressure of the lower esophageal sphincter. Domperidone has no effect on gastric secretion.
Pharmacokinetics:
When receiving domperidone fasting rapidly absorbed after oral administration, peak plasma concentrations are reached within 30 – 60 minutes. Low absolute bioavailability of domperidone when administered (approximately 15%) is associated with the intensive first-pass metabolism in the gut wall and liver.
Domperidone should be taken for 15 – 30 minutes before meals. Reducing the acidity in the stomach leads to poor absorption of domperidone. Oral bioavailability is reduced by preliminary admission of cimetidine and sodium bicarbonate. When taken after a meal the drug to achieve maximum absorption takes more time, and the area under the curve (AUC) increases slightly.
When ingestion of domperidone does not accumulate or induce its own metabolism; peak plasma level of 21 ng / ml 90 minutes after 2 weeks of oral administration of the drug at a dose of 30 mg per day was almost the same as the level of 18 ng / ml after administration of the first dose. Domperidone binds to the plasma protein at 91 – 93%. drug distribution studies with radiolabeled in animals have shown its wide tissue distribution, but low concentrations in the brain. Small amounts of drug cross the placenta in rats.
Domperidone undergoes rapid and extensively metabolized by hydroxylation and N-dealkylation. in vitro metabolism study with diagnostic inhibitors revealed that CYP3A4 isozyme is the major form of cytochrome P450 involved in the N-dealkylation of domperidone, whereas isozymes CYP3A4, CYP1A2 and CYP2E1 involved in the hydroxylation of aromatic domperidone.
Excretion of urine and feces was 31% and 66% of the dose when administered, respectively. Percentage of drug excreted unchanged in is small (10% – faeces and approximately 1% – in the urine). The plasma half-life after a single oral administration of 7 – 9 hours in healthy volunteers, but is increased in patients with severe renal insufficiency.
In such patients (serum creatinine> 6 mg / 100 ml, ie. E.> 0.6 mmol / L) increased the half-life of domperidone from 7.4 to 20.8 hours, but the concentration of drug in plasma is lower than that of patients with normal renal function. A small amount of the unchanged drug (about 1%) excreted by the kidneys.
In patients with impaired liver function moderate severity (score 7 – 9 points on a scale Child-Pugh), the AUC and Cmax of domperidone were 2.9 and 1.5 times higher than in healthy volunteers, respectively. Percentage of unbound fraction was increased by 25% and the half-life was increased from 15 to 23 hours. In patients with mild hepatic impairment observed several reduce systemic levels of the drug compared to those of healthy volunteers based on Cmax and AUC, without being bound to proteins or change in half-life. Patients with severe hepatic impairment have not been studied.
Pregnancy and breast-feeding
Pregnancy
Data on the use of domperidone during pregnancy is not enough. To date there is no evidence of an increased risk of malformations in humans. However, Motilium® EXPRESS should be used during pregnancy only if its use is justified by the expected therapeutic benefit.
Use during lactation
Number of domperidone, which can enter the body of the child with breast milk is small.
Maximum relative dose for infants (%) estimated at about 0.1% of the dosage adopted mother based on body weight. It is not known whether this level has a negative effect on the newborn. In this connection, when applying Motilium® EXPRESS during lactation is advisable to discontinue breastfeeding.
Conditions of supply of pharmacies
On prescription
side effects
According to clinical studies
Adverse reactions observed at> 1% of patients treated with Motilium EXPRESS, depression, anxiety, reduced or absent libido, headache, drowsiness, akathisia, dry mouth, diarrhea, rash, itching, breast enlargement / gynecomastia, pain and sensitivity in the breast, galactorrhea, menstrual disorders and amenorrhea, impaired lactation, asthenia.
Adverse reactions observed in
The following adverse effects were classified as follows: very often (> 10%), frequent (> 1%, 0.1% and 0.01%, but
According spontaneous adverse event messages
Violations by the immune system.
Very rare: anaphylactic reactions, including anaphylactic shock.
Mental disorders.
Very rarely: irritability (predominantly in infants and children), nervousness.
Disorders of the nervous system.
Very rare: dizziness, extrapyramidal disorders and convulsions (mainly in infants and children).
Violations by the cardiovascular system.
Very rare: lengthening of the interval QT, ventricular arrhythmia *, sudden cardiac death *.
Violations of the skin and subcutaneous tissue.
Very rare: urticaria, angioneurotic edema.
Violations of the kidneys and urinary tract.
Very rare: urinary retention.
Laboratory and instrumental data.
Very rare: laboratory abnormalities of liver function, increased blood prolactin levels.
Adverse reactions identified in the post-registration clinical studies
Violations by the immune system.
Frequency unknown: anaphylactic reactions including anaphylactic shock.
Mental disorders.
Uncommon: irritability (predominantly in infants and children), nervousness.
Disorders of the nervous system.
Common: dizziness.
Rare: convulsions (especially in infants and children).
Frequency unknown: extrapyramidal disorder (especially in infants and children).
Violations by the cardiovascular system.
Frequency unknown: lengthening of the interval QT, ventricular arrhythmia *, sudden cardiac death *.
Violations of the skin and subcutaneous tissue.
Frequency unknown: angioedema.
Violations of the kidneys and urinary tract.
Uncommon: urinary retention.
Laboratory and instrumental data.
Uncommon: laboratory abnormalities of liver function.
Rare: increase in blood prolactin levels.
* In some epidemiological studies have shown that the use of domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden death. The risk of these events is more likely in patients older than 60 years and in patients taking the drug at a daily dose of 30 mg. It recommended the use of domperidone in the lowest effective dose in adults and children.
special instructions
In a joint application of the drug Motilium® EXPRESS with antacids or antisecretory drugs should be taken after the last meal and not before meals, t. E. They should not be taken simultaneously with the preparation Motilium® EXPRESS.
Motilium® EXPRESS, lozenges contain aspartame and should not be used in patients with hyperphenylalaninemia.
Use in children
Motilium® EXPRESS in rare cases can cause neurological side effects (see. The section “Side effects”). In this connection it should strictly adhere to the recommended dose (see. The section “Method of administration and dose”). Neurological adverse effects may be caused by an overdose of the drug in adolescents, but it is necessary to take into account other possible causes such effects.
Use in diseases of the cardiovascular system.
Some epidemiological studies have shown that the use of domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden cardiac death (see. Section “Side effects”). The risk may be more likely in patients older than 60 years and in patients taking the drug at daily doses greater than 30 mg. Patients older than 60 years should take the drug Motilium® EXPRESS with caution.
Use of domperidone and other drugs that lead to a lengthening of the interval QTc, is not recommended for patients with existing conduction disturbances, in particular, elongation interval QTc, and in patients with severe disorders of electrolyte balance (hypokalemia, hyperkalemia, hypomagnesaemia) or bradycardia, or in patients with concomitant heart diseases such as congestive heart failure. As it is known, on a background of electrolyte balance and bradycardia and increased risk of arrhythmia.
If signs or symptoms that may be associated with cardiac arrhythmia therapy Motilium® EXPRESS should stop and consult a doctor.
Application of kidney diseases.
Since a very small percentage of the drug is excreted unchanged by the kidneys, the single dose adjustment in patients with renal impairment is not required. However, on repeated administration Motilium® EXPRESS frequency of application should be reduced to one or two times a day, depending on the severity of renal function (see. The section “Method of administration and dose”). During prolonged therapy, patients should be regularly monitored.
Potential drug interactions
The main metabolic pathway of domperidone performed by isoenzyme CYP3A4. In vitro данные и результаты исследований у человека показывают, что сопутствующее применение лекарственных средств, значительно ингибирующих этот фермент, может сопровождаться увеличением концентраций домперидона в плазме.
Сочетанное применение домперидона с сильнодействующими ингибиторами изофермента CYP3A4, которые, по полученным данным, вызывают удлинение интервала QT противопоказано (см. раздел «Противопоказания»).
Необходимо соблюдать осторожность при совместном применении домперидона с сильнодействующими ингибиторами изофермента CYP3A4, которые не вызывают удлинение интервала QT, такими, как индинавир, и необходим тщательный мониторинг пациентов на предмет возникновения признаков или симптомов нежелательных реакций (см. раздел «Взаимодействие с другими лекарственными средствами»).
Необходимо соблюдать осторожность при сочетанном применении домперидона с лекарственными средствами, которые, по полученным данным, вызывают удлинение интервала QT, и необходим тщательный мониторинг пациентов на предмет возникновения признаков или симптомов сердечно-сосудистых нежелательных реакций.
Примеры таких лекарственных средств:
• антиаритмические средства класса IA (например, дизопирамид, хинидин);
• антиаритмические средства класса III (например, амиодарон, дофетилид, дронедарон, ибутилид, соталол);
• определенные антипсихотики (например, галоперидол, пимозид, сертиндол);
• определенные антидепрессанты (например, циталопрам, эсциталопрам);
• определенные антибиотики (например, левофлоксацин, моксифлоксацин);
• определенные противогрибковые средства (например, пентамидин);
• определенные противомалярийные средства (например, галофантрин);
• определенные желудочно-кишечные лекарственные средства (например, доласетрон);
• определенные противоопухолевые лекарственные средства (например, торемифен, вандетаниб);
• некоторые другие лекарственные средства (например, бепридил, метадон).
If the drug became useless or expired shelf life – do not throw it in the waste water and the street! Place the drug in the bag and place in the trash. These measures will help protect the environment!
Влияние на способность вождения транспорта
Необходимо соблюдать осторожность при управлении транспортными средствами и занятиями другими потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций в связи с риском развития побочных реакций, которые могут влиять на указанные способности.
Storage conditions
Stored in a dry place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Store in original container.
Dosing and Administration
Inside.
Рекомендуется принимать таблетки Мотилиум ЭКСПРЕСС за 15 – 30 минут до еды, в случае приема препарата после еды абсорбция домперидона может замедляться.
Взрослые и дети старше 12 лет с массой тела 35 кг и более
По 1 таблетке (10 мг) 3 раза в сутки, максимальная суточная доза составляет 3 таблетки (30 мг).
Дети до 12 лет и с массой тела 35 кг и более
По 1 таблетке (10 мг) 3 раза в сутки, максимальная суточная доза составляет 3 таблетки (30 мг).
В детской практике в основном следует использовать суспензию МОТИЛИУМ®.
Обычно для терапии острой тошноты и рвоты максимальная продолжительность непрерывного приема препарата не должна превышать одну неделю. Если тошнота и рвота продолжаются дольше одной недели, пациенту следует повторно проконсультироваться со своим врачом. По другим показаниям продолжительность терапии составляет 4 недели. Если симптомы не исчезают в течение 4 недель, необходимо провести повторное обследование пациента и оценить необходимость в продолжении терапии.
Use in patients with renal insufficiency
Поскольку период полувыведения домперидона при тяжелой почечной недостаточности (при уровне креатинина в сыворотке > 6 мг/100 мл, т. е., > 0,6 ммоль/л) увеличивается, частоту приема Мотилиум® ЭКСПРЕСС, таблетки, для рассасывания, следует снизить до 1 или 2 раз в сутки, в зависимости от тяжести недостаточности. Необходимо проводить регулярное обследование пациентов с тяжелой почечной недостаточностью (см. раздел «Фармакологические свойства»).
Use in patients with hepatic insufficiency
Применение МОТИЛИУМ® ЭКСПРЕСС противопоказано у пациентов со среднетяжелой (7 – 9 по классификации Чайлд-Пью) или тяжелой (> 9 по классификации Чайлд-Пью) печеночной недостаточностью (см. раздел «Противопоказания»). У пациентов с легкой (5 – 6 по классификации Чайлд-Пью) печеночной недостаточностью коррекции дозы препарата не требуется (см. раздел «Фармакологические свойства»).
Поскольку таблетки для рассасывания довольно хрупки, во избежание повреждения их не следует продавливать сквозь фольгу.
Для того чтобы достать таблетку из блистера необходимо следующее:
– возьмите фольгу за край и полностью снимите ее с ячейки, в которой находится таблетка;
– осторожно надавите снизу;
– извлеките таблетку из упаковки.
Положите таблетку на язык. В течение нескольких секунд она распадется на поверхности языка, ее можно будет проглотить со слюной, не запивая водой.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist