Singular 4mg chewable tablets, No. 28

Singular 4mg chewable tablets, No. 28; 'SingularЃ prevention and long-term treatment of bronchial asthma in children aged 2 years and older: in order to control day and night symptoms of the disease; relief of symptoms of allergic rhinitis in children aged 2 years and older.

Inside 1 time / day, regardless of food intake. For the treatment of bronchial asthma, SingularЃ should be taken in the evening. In the treatment of allergic rhinitis, the drug can be taken at any time of the day at the request of the patient. Patients with bronchial asthma and allergic rhinitis should take 1 tablet of SingularЃ 1 time per day in the evening. Children aged 2 to 5 years With bronchial asthma and / or allergic rhinitis - 1 chewable tablet 4 mg per day.

1 coated tablet contains:

Active substance: montelukast

Excipients:

microcrystalline cellulose, lactose, croscarmellose sodium, hyprolose, magnesium stearate.

• children under 2 years of age;

• phenylketonuria;

• hypersensitivity to the components of the drug.

pharmachologic effect

Leukotriene receptor antagonist. Cysteinyl leukotrienes LTC4, LTD4, LTE4 are potent inflammatory mediators - eicosanoids, which are secreted by various cells, incl. mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl leukotriene receptors. Cysteinyl leukotriene receptors type I (CysLT1 receptors) are present in the human respiratory tract (including bronchial smooth muscle cells, macrophages) and other proinflammatory cells (including eosinophils and some myeloid stem cells). Cysteinyl leukotrienes correlate with the pathophysiology of bronchial asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchospasm, increased mucus secretion, increased vascular permeability, and increased eosinophil count.In allergic rhinitis, after exposure to an allergen, cysteinyl leukotrienes are released from pro-inflammatory cells of the nasal mucosa during the early and late phases of an allergic reaction, which is manifested by symptoms of allergic rhinitis. An intranasal test with cysteinyl leukotrienes showed an increase in nasal airway resistance and a symptom of nasal obstruction. Montelukast is a highly active oral drug that significantly improves inflammation in bronchial asthma. According to biochemical and pharmacological analysis, montelukast binds with high affinity and selectivity to CysLT1 receptors without interacting with other pharmacologically important receptors in the respiratory tract (such as prostaglandin receptors,choline or? -adrenergic receptors). Montelukast inhibits the physiological effect of cysteinyl leukotrienes LTC4, LTD4, LTE4 by binding to CysLT1 receptors without stimulating these receptors.

Indications of the drug

SingularЃ prevention and long-term treatment of bronchial asthma in children aged 2 years and older: in order to control the day and night symptoms of the disease; Relief of symptoms of allergic rhinitis in children 2 years of age and older.

Dosage regimen

Inside 1 time / day, regardless of food intake. For the treatment of bronchial asthma, SingularЃ should be taken in the evening. In the treatment of allergic rhinitis, the drug can be taken at any time of the day at the request of the patient. Patients with bronchial asthma and allergic rhinitis should take 1 tablet of SingularЃ 1 time per day in the evening.

Children aged 2 to 5 years With bronchial asthma and / or allergic rhinitis - 1 chewable tablet 4 mg per day.

Side effect

In general, SingularЃ is well tolerated by patients. Side effects are usually mild and usually do not require discontinuation of the drug. The overall incidence of side effects during treatment with SingularЃ is comparable to their incidence with placebo.

Contraindications for use

children under 2 years of age;

phenylketonuria; hypersensitivity to the components of the drug.

Application during pregnancy and lactation

Clinical trials of the drug SingularЃ with the participation of pregnant women have not been carried out. SingularЃ should be used during pregnancy and during breastfeeding only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child. During the post-registration use of SingularЃ, it was reported about the development of congenital defects of the extremities in newborns whose mothers took SingularЃ during pregnancy. Most of these women also took other asthma medications during pregnancy. The causal relationship between taking SingularЃ and the development of congenital limb defects has not been established. It is not known whether montelukast is excreted in breast milk. Since many drugs are excreted in breast milk,it is necessary to take this into account when prescribing SingularЃ for breastfeeding mothers.

Application for violations of liver function

For patients with mild or moderately impaired liver function, a special dose adjustment is not required. There are no data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic impairment (more than 9 points on the Child-Pugh scale).

Application for impaired renal function

For patients with renal insufficiency, a special dose adjustment is not required.

Application in children

For children aged 2 to 5 years with bronchial asthma and / or allergic rhinitis, the dose is 4 mg (1 tab.) / Day. Contraindicated: children under 2 years of age.

Use in elderly patients

For elderly patients, special dose selection is not required.

Overdose

Overdose symptoms were not identified during clinical trials of long-term (22 weeks) treatment with SingularЃ in adult patients with bronchial asthma at doses up to 200 mg / day, or during short (about 1 week) clinical studies when taking the drug in doses up to 900 mg / day. days There have been cases of acute overdose of SingularЃ (taking at least 1000 mg / day) in the post-registration period and during clinical trials in adults and children. Clinical and laboratory data indicated the comparability of the safety profiles of SingularЃ in children, adults and elderly patients. The most common symptoms were thirst, drowsiness, vomiting, agitation, headache, and abdominal pain. These side effects are consistent with the safety profile of SingulairЃ. Treatment:carrying out symptomatic therapy. There is no specific information on the treatment of SingularЃ overdose. There are no data on the effectiveness of peritoneal dialysis or montelukast hemodialysis.

Drug interactions

SingularЃ can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and / or the treatment of allergic rhinitis. Montelukast at the recommended therapeutic dose did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinylestradiol / norethindrone 35/1), terfenadine, digoxin and warfarin. With the simultaneous administration of phenobarbital, the AUC value of montelukast decreases by about 40%, but this does not require changes in the dosage regimen of SingularЃ. In vitro studies have shown that montelukast inhibits the CYP2C8 isoenzyme.However, in a study of drug interactions in vivo between montelukast and rosiglitazone (metabolized with the participation of the CYP2C8 isoenzyme), no confirmation of the inhibition of the CYP2C8 isoenzyme was obtained by montelukast. Therefore, in clinical practice, the effect of montelukast on the CYP2C8-mediated metabolism of a number of drugs is not expected, incl. paclitaxel, rosiglitazone, repaglinide. In vitro studies have shown that montelukast is a substrate of isoenzymes CYP2C8, 2C9 and 3A4. Data from a clinical study of drug interactions in relation to montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the systemic effect of montelukast by 4.4 times. Co-administration of itraconazole, a potent CYP3A4 inhibitor,together with gemfibrozil and montelukast did not lead to an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on systemic exposure to montelukast cannot be considered clinically significant on the basis of safety data when used in doses exceeding the approved dose of 10 mg for adult patients (for example, 200 mg / day for adult patients for 22 weeks and up to 900 mg / day for no clinically significant adverse effects were observed in patients taking the drug for about one week). Thus, when taken together with gemfibrozil, dose adjustment of montelukast is not required. According to the results of in vitro studies, clinically significant drug interactions with other known inhibitors of CYP2C8 (for example, with trimethoprim) are not expected. Besides,co-administration of montelukast with itraconazole alone did not lead to a significant increase in the effect of systemic exposure to montelukast.

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