Single pill chewable 5mg N28
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Active ingredients
Montelukast
Release form
Pills
Composition
1 tab. montelukast sodium 5.2 mg, which corresponds to the content of montelukast 5 mg. Excipients: mannitol - 201.
Pharmacological effect
Montelukast has a high affinity and selectivity for binding to cysteinyl leukotriene receptors. The use of montelukast inhibits the early and late phases of bronchospasm. Montelukast reduces bronchospasm even in very low doses (5 mg). Bronchodilation continues for 2 hours after taking the drug inside. The effect of bronchodilation caused by beta-adrenergic aggravates the effect caused by montelukast. Montelukast reduces the number of eosinophils in the peripheral blood and in the airways (in the sputum) of children and adults and improves control over the clinical course of bronchial asthma. In adult patients, Montelukast significantly improves the morning forced expiratory volume (FEV1) in 1 second. Montelukast enhances the clinical effects of inhaled GCS. Montelukast reduces the severity of daytime (including coughing, wheezing, difficulty breathing and restriction of activity) and nocturnal symptoms of bronchial asthma. Montelukast reduces the need for beta adrenomimetics and corticosteroids, used when necessary (in case of deterioration). Patients receiving montelukast have a longer remission than patients who have not taken it. The therapeutic effect is observed after taking the first dose. In children aged 2 years with mild asthma and episodic exacerbations, montelukast significantly reduces the frequency of episodes of exacerbations of bronchial asthma and improves respiratory function. The bronchospasm arising against an exercise stress weakens. In patients with asthma sensitive to acetylsalicylic acid and taking concomitant therapy with inhaled and / or oral glucocorticosteroids, treatment with montelukast leads to a significant improvement in the control of symptoms of bronchial asthma.
Pharmacokinetics
Absorption: Cmax in the blood plasma was achieved in children aged 2 to 5 years 2 hours after ingestion on an empty stomach at a dose of 4 mg. The average Cmax was 66% higher, while the average Cmin was lower than in adults after taking 10 mg.In adult patients, when taken on an empty stomach at a dose of 5 mg Cmax is achieved 2 hours after administration. On average, bioavailability is 73%; it is reduced to 63% when taking the drug after a normal meal. Distribution: Montelukast is more than 99% bound to plasma proteins. Vd montelukast in equilibrium is an average of 8-11 liters. Bad penetrates through the BBB. Metabolism: Montelukast undergoes active metabolism in the liver. In equilibrium after administration at therapeutic doses, plasma concentrations of montelukast in children and adults are not determined. Cytochrome 3A4, 2A6, and 2C9 isoenzymes are involved in montelukast metabolism, but at therapeutic concentrations, montelukast does not inhibit the cytochrome 3A4, 2C9, isoenzymes, 1A2, 2A6, 2C19, and 2D6. The metabolites of montelukast have negligible pharmacological activity. Withdrawal: Montelukast plasma clearance in healthy adults averages 45 ml / min. After ingestion of labeled Montelukast, 86% of the drug was excreted through the intestines for 5 days and less than 0.2% by the kidneys. This suggests that the drug and its metabolites are excreted mainly with bile. T1 / 2 of montelukast in young patients ranges from 2.7 to 5.5 hours. The pharmacokinetics of montelukast remains almost linear when ingested doses of over 50 mg. Pharmacokinetics in special groups of patients: Studies in patients with renal insufficiency were not conducted. Since montelukast and its metabolites are excreted in the bile, dose adjustment is not required in patients with renal insufficiency. Data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (score> 9 on the Child-Pugh scale) are not available.
Indications
Children 2-5 years old (chewable pills 4 mg) and children 6-14 years old (chewable pills 5 mg) for: - long-term treatment and prevention of bronchial asthma (including prevention of day and night symptoms of the disease) - treatment of bronchial asthma patients with hypersensitivity to acetylsalicylic acid and prevention of bronchospasm of physical effort.
Contraindications
- severe liver dysfunctions - phenylketonuria (the drug contains aspartame) - children's age up to 2 years (for 4 mg chewable pills) - children up to 6 years old (for 5 mg chewable pills) - hypersensitivity to the active substance or to any of the excipients . With caution should use the drug simultaneously with inducers of CYP3A4.
Use during pregnancy and lactation
The drug is used in children.
Dosage and administration
Children aged 2-5 years the drug is prescribed 1 tablet. chew 4 mg daily in the evening. Children aged 6-14 years, the drug Singlelon is prescribed on 1 tab. chewable 5 mg daily in the evening. The drug Singlelon should be taken 1 hour before or 2 hours after a meal. Dose adjustment within these age groups is not required. The safety and efficacy of chewable 4 mg pills for children under 2 years of age has not been established. General recommendations The therapeutic effect of the drug Singlelon develops within one day after administration. The patient should continue taking the drug Singlelon both during periods of controlled asthma and during periods of worsening course of the disease. In patients with renal insufficiency, mild or moderate liver failure, dose adjustment is not required. Data for patients with severe liver failure are not available. The dose of the drug does not depend on the gender of the patient. Therapy with the drug Singlelon in combination with other drugs for the treatment of asthma. If the drug Singlelon is prescribed in patients with inhaled GCS, it is not necessary to sharply replace the inhaled GCS with the drug Singlon.
Side effects
Below are the adverse reactions according to system-organ classes according to the MedDRA classification, which were often (> 1/100, less than 1/10) observed in patients who received montelukast. For 5 mg chewable pills: Nervous system: headache. For chewable pills 4 mg: On the part of the gastrointestinal tract: pain in the abdomen. Common disorders: thirst. During the post-marketing study, the following adverse events were identified: Blood and lymphatic system: increased tendency to bleed. Immune system disorders: hypersensitivity reactions, including anaphylaxis; eosinophilic infiltrates of the liver. Mentally: sleep disorders, including nightmares, hallucinations, psychomotor hyperactivity (including irritability, anxiety, agitation, including aggressive behavior, and tremor), depression and insomnia, suicidal thoughts and suicidal behavior. On the part of the nervous system: drowsiness, dizziness, paresthesia / hyperesthesia, seizures.Since the cardiovascular system: rapid heartbeat. On the part of the digestive tract: diarrhea, dry mouth, dyspepsia, nausea and vomiting. On the part of the hepatobiliary system: increased activity of hepatic transaminases in the blood serum (AST, ALT), cholestatic hepatitis, pancreatitis. From the skin and subcutaneous tissue: angioedema, the appearance of ecchymosis, urticaria, pruritus, rash, erythema nodosum, tendency to form bruises. On the part of the musculoskeletal system: arthralgia, myalgia, including muscle cramps. General disorders: asthenia / fatigue, discomfort, edema. In very rare cases, when receiving Montelukast, patients with bronchial asthma develop Churg-Strauss syndrome.
Overdose
There is no specific information on the treatment of overdose with the drug Singlelon. In clinical studies, adult patients with asthma took the drug in doses up to 200 mg / day for 22 weeks, and in short-term studies - in doses up to 900 mg / day for about a week without clinically significant adverse events. There have been cases of acute overdose of montelukast in adults and children when taken at a dose higher than 1000 mg (approximately 61 mg / kg for a child aged 42 months). The obtained clinical and laboratory results were consistent with the safety profile for adults and pediatric patients. Most overdose reports did not indicate adverse events. The most common adverse events corresponded to the safety profile of montelukast and included abdominal pain, drowsiness, thirst, headache, vomiting, psychomotor hyperactivity, mydriasis. There is no data on the possibility of elimination of montelukast with peritoneal dialysis or hemodialysis.
Interaction with other drugs
The drug Singlelon can be administered in conjunction with other drugs traditionally prescribed for the prevention and long-term treatment of bronchial asthma. In recommended doses, the drug did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethisterone 35/1), terfenadine, digoxin and warfarin.Monotelukast plasma AUC decreased by approximately 40% in patients who took montelukast and phenobarbital. Since CYP3A4 isoenzyme is involved in the metabolism of montelukast, caution should be exercised, especially in children, when using montelukast with such inducers of CYP3A4 as phenytoin, phenobarbital and rifampicin. In in vitro studies, it was found that montelukast is a potent inhibitor of the CYP2C8 isoenzyme. However, the results of a study of the clinical interaction of montelukast and rosiglitazone (an example of marker substrates for drugs whose main metabolism is performed by the CYP2C8 isoenzyme) did not reveal an inhibitory effect of montelukast on the CYP2C8 isoenzyme in vivo. Therefore, it is expected that montelukast will not significantly alter the transformations of drugs that are metabolized with the participation of this enzyme (for example, paclitaxel, rosiglitazone and repaglinide). When receiving high doses of montelukast (with a 20-and 60-fold excess of the recommended dose for adults) there is a decrease in plasma theophylline concentration. This effect is not observed when taking the drug in the recommended doses.
special instructions
One should not take the chewable pills Singlelon for the relief of acute asthma attacks. In the event of an attack, it is recommended to use inhaled beta adrenomimetics. With an increase in the need for short-acting beta-adrenomimetics, patients should consult a doctor as soon as possible. It is impossible to sharply replace inhalation or oral GCS drug Singleton. There is no evidence of the possibility of reducing the dose of oral GCS with the concomitant use of the drug Singlelon. In rare cases, patients taking drugs for the treatment of bronchial asthma, including montelukast, may experience systemic eosinophilia, sometimes accompanied by clinical manifestations of vasculitis and Churg-Strauss syndrome; This is an indication for the use of systemic GCS. Such cases are usually, but not always, associated with a dose reduction or withdrawal of oral corticosteroids. It is impossible neither to exclude, nor to confirm the probability that the taking of leukotriene receptor antagonists may be associated with the occurrence of Churg-Strauss syndrome.Physicians should be informed about the possibility of eosinophilia, vasculitic rash, increase in pulmonary symptoms, heart complications and / or neuropathy in their patients. Patients who have the above symptoms should be re-examined, and their treatment regimens revised. Chewable pills Singlelon contain aspartame - a source of phenylalanine. Patients with phenylketonuria should be borne in mind that each 4 mg chewable tablet contains 1.2 mg of aspartame, and each 5 mg chewable tablet contains 1.5 mg of aspartame. Impact on the ability to drive motor vehicles and control mechanisms When taking 5 mg chewable pills of the drug Singlelon, dizziness and drowsiness may develop, which should be considered when driving a vehicle or working with mechanisms is necessary. Chewable pills 4 mg prescribed for children 2-5 years.