Montemak 10 30 x 10 mg film-coated tablets

The instruction for medical use of Montemak medicine 10 the Trade name Montemak 10 International unlicensed name Montelukast Dosage Form of the Tablet film coated, 10 mg Structure One tablet, film coated, contains active agent - sodium montelukast of 10.40 mg (it is equivalent montelukastu10 to mg), excipients: lactoses monohydrate (Pharmatose 200 M), cellulose microcrystalline (Avicel PH 101), sodium of a kroskarmelloz (Ac-di-sol), dinatrium edetat, magnesium stearate, cover of Instacoat Aqua Brown ICG-A10310, structure of a cover: a gipromelloza 2910, hydroxypropyl cellulose, the titan dioxide (E171), gland (III) oxide yellow (E172), gland (III) oxide red (E172) the Description of the Tablet, film coated beige color, square shape with the rounded-off corners, biconvex, with an engraving CL 26 on one party. Pharmacotherapeutic group Drugs for treatment of obstructive respiratory diseases. Other drugs drugs for treatment of obstructive respiratory diseases for system use. Leukotriene receptors antagonists. Montelukast the ATX R03DC03 Code the Pharmacological Pharmacokinetics Absorption Montelukast properties is quickly absorbed after oral administration. For tablets, film coated, on 10 mg, average maximum concentration (Cmax) in blood plasma was reached in 3 hours (Tmax) after drug use by adults on an empty stomach. The average bioavailability at oral administration is 64%. Intake of usual food did not affect bioavailability at oral administration and on Cmax. Safety and efficiency are confirmed in clinical trials at use of tablets, film coated, 10 mg, irrespective of meal. For chewable tablets of 5 mg Cmax it was reached in 2 hours after reception on an empty stomach at adults. The average bioavailability at oral administration was 73% and decreased to 63% at reception with standard food. Distribution Montelukast more than for 99% contacts proteins of blood plasma. The volume of distribution of montelukast in an equilibrium state averages 8-11 liters. Researches using radioactive and marked montelukast indicate the minimum distribution at penetration through a blood-brain barrier. Besides, concentration of radioactive and marked substance in 24 hours after reception of a dose were minimum in all other fabrics. Metabolism Montelukast is actively metabolized. At use of therapeutic doses, concentration of metabolites of montelukast are in blood plasma below a detection limit at an equilibrium state at adults and children. Metabolism of montelukast happens mainly by means of the system of P450 2C8 cytochrome. Small impact is had CYP 3A4 and 2C9 though when assigning an itrakonazol which is CYP inhibitor 3A4 montelukast pharmacokinetics at the healthy volunteers receiving montelukast of 10 mg of 1 times/days did not change. Clinical trials of microsomes of a liver of the person of in vitro showed that therapeutic concentration of montelukast in blood plasma do not inhibit P450 3A4, 2C9, 1A2, 2A6, 2C19 or 2D6 cytochromes. The role of metabolites in therapeutic effect of montelukast is minimum. Removal Plasma clearance of montelukast at healthy adults averages 45 ml/minute. After oral administration it is radioactive marked montelukast of 86% of radioactivity it is removed for 5 days with a stake and & lt, 0.2% is removed with urine. Considering bioavailability of montelukast after oral administration, it indicates that montelukast and its metabolites are removed, almost completely, with bile. Feature of pharmacokinetics various groups of patients have no need for dose adjustment at patients of advanced age or in an abnormal liver function from easy to moderate severity. Researches with participation of patients with renal failures were not conducted. As montelukast and its metabolites are removed with bile, it is not supposed that patients will have necessary a dose adjustment of montelukast with renal failures. Patients have no data on montelukast pharmacokinetics with a severe form of an abnormal liver function (& gt, 9 on a scale of Chayld-Pyyu). At use of high doses of montelukast (in 20 and 60 times exceeding the recommended dose for adults) decrease in concentration of theophylline in blood plasma was observed. This effect was not observed at use of drug in the recommended dose of 10 mg of 1 times/days. A pharmacodynamics Cysteic leukotrienes (LTC4, LTD4, LTE4) are inflammation eicosanoids which are emitted from various cells, including mast cells and eosinophils. These important pro-asthmatic mediators contact cysteic leukotriene receptors (CysLT). CysLT type-1 (CysLT1) receptors are in airways (including smooth muscle cells and macrophages of airways) and on other pro-inflammatory cells (including eosinophils and some myeloid stem cells). CysLTs are interconnected with a pathophysiology of asthma and allergic rhinitis. In asthma the effects of leukotrienes include a bronchospasm, secretion of a phlegm, permeability of vessels and mobilization of eosinophils. In allergic rhinitis of CysLTs under the influence of allergen are released from a mucous membrane of a nose both on early, and on late phases of reactions with symptoms of allergic rhinitis. Intranasal test with CysLTs showed increase in resilience of airways of a nose and symptoms of congestion of a nose. Montelukast is active connection which competitively ties CysLT1-receptors with sharp selectivity and chemical affinity. Clinical trials established that montelukast suppresses the bronchospasm caused by inhalation of LTD4 even when assigning in a dose of 5 mg and causes a bronkhodilatation within 2 hours after intake. Montelukast also has additive effect on effect β-agonists. Treatment by montelukast suppresses a bronchospasm both on early, and on late stages, reducing reaction to antigens. Treatment by montelukast considerably reduces quantity of eosinophils in airways (it is confirmed with the analysis of a phlegm) and in peripheral blood, improving control over a clinical course of bronchial asthma. Indications - addition to basic therapy of bronchial asthma for patients since 15 years with persistent asthma easy and moderate severity (at insufficient efficiency of inhalation corticosteroids and β-agonists of short action) - treatment of aspirinchuvstvitelny patients with bronchial asthma and prevention of the bronchospasm caused by physical activity - treatment of allergic rhinitises at patients with bronchial asthma. The route of administration and doses For patients with asthma or with asthma and the accompanying seasonal allergic rhinitis at the age of 15 years are also more senior, the dose makes 10 mg a day (1 tablet), in the evening. General recommendations. Therapeutic effect of the drug Montemak 10 with change of indicators of a course of bronchial asthma develops within 1 day. Patients should report that it is necessary to continue reception Montemak 10 even if will reach control of asthma and also during the periods of deterioration in a course of asthma. Montemak 10 it is not necessary to accept along with other drugs containing the same active ingredient – montelukast. There is no need for dose adjustment for patients with a renal failure or with abnormal liver functions from easy to moderate severity. There are no data on patients with a severe form of an abnormal liver function. A dosage for boys and girls identical. Treatment by Montemak 10 depending on other methods of treatment of asthma. At Montemak's use 10 as additional therapy to inhalation corticosteroids, it is not necessary to reduce sharply a dose or to cancel inhalation corticosteroids. Inhalation corticosteroids. Treatment by Montemak 10 can be performed as additional therapy at patients who have a use of inhalation corticosteroids and as necessary β-agonists of short action does not provide sufficient clinical control of asthma. Montemak 10 should not replace inhalation corticosteroids. For children aged from 6 up to 14 years chewable tablets on 5 mg are produced. Side effects Side effects are distributed on groups with the following frequency of their emergence: very often (≥1/10), it is frequent (≥1/100 & lt, 1/10), infrequently (≥1/1000 & lt, 1/100), is rare (≥1/10,000 & lt, 1/1,000), is very rare (& lt, 1/10,000) it is frequent (≥1/100 & lt, 1/10) - a headache - abdominal pain Post-marketing data Very often (≥1/10) - upper respiratory tract infections * is frequent (≥1/100 & lt, 1/10) - diarrhea **, nausea **, vomiting ** - rash ** - increase in level of transaminases (ALT and nuclear heating plant) - a pyrexia * Infrequently (≥1/1,000 & lt, 1/100) - reactions of hypersensitivity, including an anaphylaxis - pathological dreams, including dreadful dreams, insomnia, a sleep-walking, excitement, agitation, including aggression and hostility, the depression, psychomotor hyperreactivity, including irritability, a bespokoynost, a tremor *** - dizziness, drowsiness, a paresthesia/hypesthesia, spasms - nasal bleeding - dryness in a mouth, dyspepsia - bruises, urticaria, an itching - an arthralgia, myalgia, including muscular spasms - asthenia/fatigue, hypostasis - enuresis in children Seldom (≥1/10,000 & lt, 1/1,000) - tendency to bleeding - disturbance of concentration of attention, a dysmnesia - palpitation - a Quincke's disease Very seldom (& lt, 1/10,000) – eosinophilic infiltrates in a liver - hallucinations, a disorientation, suicide intentions and behavior (including attempts of a suicide) - Cherdzha-Stross's syndrome – hepatitis, including cholestatic, hepatocellular and damages of a liver of the mixed genesis - a multiformny erythema, a nodal erythema * These by-effects occurred very often as in the patients accepting montelukast and in group of the patients accepting placebo in clinical trials. ** These by-effects met often as at the patients accepting montelukast and in group of the patients accepting placebo in clinical trials. *** Met frequency seldom of the Contraindication - hypersensitivity to active ingredient or - pregnancy and a lactation - hereditary intolerance of a galactose, deficiency of enzyme of Lappa lactase, glucose galactose malabsorption Medicinal interactions Montelukast can be applied to any of excipients with other drugs which are usually used for prevention and long-term treatment of asthma. In researches of interactions with other drugs the recommended clinical dose of montelukast had no clinically significant effect on pharmacokinetics of the following medicines: theophylline, Prednisolonum, oral contraceptives (ethinylestradiol/norethindrone 35/1), terfenadin, digoxin and warfarin. The area under a concentration curve in blood plasma (AUC) of montelukast decreased approximately by 40% at patients who at the same time applied phenobarbital. As montelukast is metabolized by means of CYP 3A4, 2C8 and 2C9 it is necessary to appoint with care montelukast, especially to children, along with inductors CYP 3A4, 2C8 and 2C9 such as Phenytoinum, phenobarbital and rifampicin. The researches in vitro showed that montelukast is strong CYP inhibitor 2C8. However data of clinical trials of interactions with drugs in which use of montelukast and a rosiglitazon was studied (marker substrate, the representative of the drugs which are metabolized mainly by means of CYP 2C8) showed that montelukast does not inhibit CYP 2C8 of in Vivo. Therefore it is not expected that montelukast it will be expressed to influence metabolism of the drugs which are metabolized by means of this enzyme (for example, paklitakset, rosiglitazon and repaglinid). Laboratory researches showed that montelukast is substrate for CYP 2C8, and to a lesser extent for 2C9 and 3A4. Data of researches on studying medicinal interactions with participation of montelukast and a gemfibrozil (inhibitor as CYP 2C8, and 2C9) showed that gemfibrozit raises a system sensitization of montelukast by 4.4 times. Correction of a dose for montelukast is not required at its simultaneous use with gemfibrozily or other potential CYP inhibitors 2C8, but doctors should mean a possibility of increase in side reactions. Clinically important medicinal interactions with other known CYP inhibitors 2C8 (for example, with Trimethoprimum) are not supposed. Besides, simultaneous use of montelukast only with itrakonazoly which is strong CYP3A4 inhibitor does not lead to significant increase in a system sensitization of montelukast. Patients have to know special instructions that montelukast for oral administration is never used for treatment of bad attacks of asthma and also that they have to have always at themselves the corresponding drug of the emergency help. At a bad attack it is necessary to use inhalation β-agonists of short action. Patients have to consult as soon as possible with the doctor if they need bigger amount of β-agonist of short action, than usually. Montelukast should not replace inhalation or oral corticosteroids sharply. There are no data confirming that the dose of oral corticosteroids can be reduced at simultaneous use of montelukast. The patients receiving treatment by antiasthmatic drugs, including the drug Montemak 10 can have a system eosinophilia, sometimes with clinical manifestations of a vasculitis characteristic of Cherdzha-Stross's syndrome (state at which treatment is often carried out by system corticosteroids). Sometimes these cases are connected with cancellation or a dose decline of oral corticosteroids the Communication between treatment by antagonists of receptors of leukotriene and emergence of a syndrome of Cherdzha-Stross cannot be excluded or confirmed. Nevertheless, in case of such symptoms as an eosinophilia, vascular rash, deterioration in pulmonary symptoms, cardiological complications and/or neuropathy, additional inspection and revision of tactics of treatment is necessary. At patients about aspirin - sensitive asthma treatment by montelukast does not affect need of use of aspirin or other non-steroidal anti-inflammatory drugs. Patients with such rare congenital diseases as intolerance of a galactose, deficiency of Lappa lactase or malabsorption of glucose galactose, should not use this drug. Psychological disorders of Disturbance from mentality were noted at the adults, teenagers and children accepting Montemak 10. Disturbances from mentality include such side effects as: excitement, agressive behavior, hostility, uneasiness, a depression, a disorientation, disturbance of concentration of attention, pathological dreams, a hallucination, insomnia, irritability, memory disturbances, concern, a sleep-walking, suicide thoughts and attempts (including a suicide) and a tremor. Data from post-marketing reports are comparable to the clinical data obtained during medicamentous therapy. Patients and health workers should know about possibility of the similar phenomena. Patients are recommended to notify the attending physician at emergence of these side effects. It is necessary to estimate a ratio advantage risk for continuation of therapy with Montemak 10 at emergence of these by-effects. Pregnancy and period of a lactation Pregnancy: limited information, from the available database concerning pregnancies, does not indicate cause and effect interrelation between Montemak's use 10 and emergence of malformation (such as defects of extremities) about which it was seldom reported during the global post-marketing experience of use. Lactation period: it is unknown whether montelukast gets into breast milk. The feature of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms is not expected that montelukast will affect ability of the patient to run motor transport or mechanisms. However it was in rare instances reported about drowsiness or dizziness in this connection it is necessary to be careful at control of motor transport or potentially dangerous mechanisms. Overdose In most cases before
an irovka of side reactions did not arise. Symptoms: abdominal pain, drowsiness, thirst, headache, vomiting and psychomotor hyperactivity. Treatment: drug withdrawal, symptomatic therapy. It is unknown whether montelukast at peritoneal dialysis is removed or at a hemodialysis. A form of release and packing On 10 tablets in blister strip packaging from aluminum foil (Alu/Alu). On the 3rd blister strip packagings together with the instruction for medical use in the state and Russian languages put in a pack from cardboard. To Store storage conditions in the dry, protected from light place, at a temperature not above 25 °C to Store out of children's reach! 2 years not to use a period of storage after an expiration date. Prescription status According to the prescription the Name and the country of the Macleods Pharmaceuticals Limited 304, Atlanta Arcade, Marol Church Road, Andheri (East), Mumbai manufacturing organization – 400,059, India. The holder of the registration certificate of Macleods Pharmaceuticals Limited, India the Name and the country of the organization of the packer of Macleods Pharmaceuticals Limited, India the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of the products and responsible for post-registration observation of safety of medicine in the territory of the Republic of Kazakhstan Branch KOO Macleods Pharmaceuticals Limited, Republic of Kazakhstan Almaty, Tulebayev St. 38/61, 5
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