Singular pills 10 mg 14 pcs
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Active ingredients
Montelukast
Release form
Pills
Composition
Active ingredient: Montelukast (montelukast) Active ingredient concentration (mg): 10
Pharmacological effect
Antagonist of leukotriene receptors. Cysteine leukotrienes LTC4, LTD4, LTE4 are strong inflammatory mediators - eicosanoids, which are secreted by different cells, including mast cells and eosinophils. These important prostatic mediators bind to cysteinyl with leukotriene receptors. Cysteine type I leukotriene receptors (CysLT1 receptors) are present in the human respiratory tract (including bronchial smooth muscle cells, macrophages) and other pro-inflammatory cells (including eosinophils and some myeloid stem cells). Cysteine leukotrienes correlate with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchospasm, an increase in mucus secretion, an increase in vascular permeability, and an increase in the number of eosinophils. In allergic rhinitis, after exposure to the allergen, leukotriene cysteinyl is released from pro-inflammatory cells of the nasal mucosa during the early and late phases of the allergic reaction, which is manifested by symptoms of allergic rhinitis. An intranasal test with cysteinyl leukotrienes has been shown to increase the resistance of the airways of the nasal tract and the symptom of nasal obstruction. Montelukast is a highly active drug when ingested, which significantly improves inflammation in bronchial asthma. According to biochemical and pharmacological analysis, Montelukast binds to CysLT1 receptors with high affinity and selectivity, without interacting with other pharmacologically important receptors in the airways (such as prostaglandin receptors, cholino or β adrenoreceptors). Montelukast inhibits the physiological effect of cysteinyl leukotrienes, LTC4, LTD4, LTE4 by binding to CysLT1-receptors without exerting stimulating action on data retseptory.Montelukast inhibit CysLT-receptors in the airways as evidenced by the ability to block bronchoconstriction in response to inhalation of LTD4 in patients with bronchial asthma.A dose of 5 mg is enough to relieve bronchospasm induced by LTD4. Montelukast causes bronchodilation within 2 hours after ingestion and may supplement bronchodilation caused by β2-adrenomimetic. The use of montelukast at doses of more than 10 mg / day does not increase the effectiveness of the drug once.
Pharmacokinetics
AbsorptionAfter oral administration, montelukast is rapidly and almost completely absorbed from the gastrointestinal tract. In adults, when taken on an empty stomach, coated pills in a dose of 10 mg Cmax in plasma are reached after 3 hours. The average bioavailability when administered is 64%. Food intake does not affect Cmax in plasma and the bioavailability of the drug. DistributionControl of montelukast with plasma proteins blood is over 99%. Vd is on average 8-11 l. Studies with radioactively labeled montelukast conducted on rats indicate minimal penetration through the BBB. In addition, the concentrations of the labeled drug 24 hours after the administration were minimal in all other tissues. When taking montelukast at a dose of 10 mg 1 time / day, a moderate (about 14%) accumulation of the active substance in plasma is observed. MetabolismMontelukast is actively metabolized in the liver. When used in therapeutic doses, the concentration of plasma metabolites of montelukast in equilibrium in adults and children is not determined. In vitro studies using human liver microsomes have shown that cytochrome P450: 3A4, 2C8 and 2C9 isoenzymes are involved in the metabolism of montelukast. According to the results of in vitro studies in human liver microsomes, montelukast at therapeutic plasma concentrations does not inhibit cytochrome P450: 3A4.2C9, 1A2, 2A6, 2C19 and 2D6 isoenzymes. ExcretionPlasma clearance of montelukast in healthy adults averages 45 ml / min . After oral administration of radiolabeled montelukast, 86% of its amount is excreted in the feces within 5 days and less than 0.2% in urine, which confirms that montelukast and its metabolites are excreted almost exclusively with bile. Monotelukast T1 / 2 in young healthy adults is from 2.7 up to 5.5 hours. The pharmacokinetics of Montelukast retains its almost linear character when ingestion of doses in excess of 50 mg. When taking montelukast in the morning and evening hours, no pharmacokinetic differences are observed. The pharmacokinetics in special clinical situations The pharmacokinetics of montelukast in women and men have a similar nature. No differences in clinically significant pharmacokinetic effects in patients depending on race are found. In case of ingestion of pills covered with a coating.at a dose of 10 mg 1 time / day, the pharmacokinetic profile and bioavailability are similar in elderly and young patients. In patients with mild to moderate hepatic insufficiency and clinical manifestations of cirrhosis, montelukast metabolism slowed down, accompanied by an increase in AUC by approximately 41% after a single dose of the drug in a dose of 10 mg. The withdrawal of montelukast in these patients is slightly increased compared with healthy subjects (T1 / 2 averages 7.4 hours). Changing the dose of montelukast for patients with mild and moderate hepatic insufficiency is not required. There are no data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (more than 9 points on the Child-Pugh scale). Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal insufficiency were not evaluated. Dose adjustment in this category of patients is not required.
Indications
Prevention and long-term treatment of asthma in adults and children from 6 years old, including the prevention of day and night symptoms of the disease, the treatment of aspirin-sensitive patients with bronchial asthma and the prevention of bronchospasm caused by physical activity. The purchase of day and night symptoms of seasonal allergic rhinitis (in adults and children from 6 years) and persistent allergic rhinitis (in adults and children from 6 years)
Contraindications
Hypersensitivity to any of the components of the drug. Children up to 6 years.
Precautionary measures
10 mg coated pills contain lactose monohydrate. Patients with a rare form of hereditary intolerance to galactose, congenital lactase deficiency or glucose-galactose malabsorption should not be prescribed a singular in this dosage form.
Use during pregnancy and lactation
Clinical studies of the drug Singular with the participation of pregnant women has not been conducted. Singular 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 the drug, Singular was reported on the development of congenital defects of the extremities in newborns whose mothers took the Singular during pregnancy. Most of these women also took other drugs for the treatment of bronchial asthma during pregnancy.The causal relationship between taking the drug Singular and the development of congenital defects of the extremities 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 the drug Singular to breastfeeding mothers.
Dosage and administration
Inside once a day, regardless of the meal. For the treatment of asthma, Singular should be taken in the evening. When treating allergic rhinitis, the dose may be taken at any time of the day at the request of the patient. Patients suffering from asthma and allergic rhinitis should take one tablet Singingular once a day in the evening. Adults aged 15 years and over. The dose for adults and children over 15 years old is one coated tablet of 10 mg per day. Children aged 6 to 14 years Dosage for children 6-14 years old is one chewable tablet 5 mg per day. Dosage adjustment for this age group is not required. General recommendations The therapeutic effect of SINGULAIR on the indices reflecting the course of asthma develops during the first day. The patient should continue to take SINGULAIR, both in the period to achieve control over the symptoms of bronchial asthma, and in periods of exacerbation of bronchial asthma. For elderly patients, patients with renal insufficiency, as well as patients with mild or moderately impaired liver function, and also depending on the gender, a special dose selection is not required. Appointment of SINGULAR along with other types of treatment of bronchial asthma SINGULAIR can be added to the treatment of the patient with bronchodilators and inhaled glucocorticosteroids (See the Section "Interaction with other medicines").
Side effects
Hypersensitivity reactions (including anaphylaxis, angioedema, rash, pruritus, urticaria, and very rarely eosinophilic liver infiltrates); node erythema, unusual vivid dreams; hallucinations; drowsiness; irritability; excitement, including aggressive behavior; fatigue; suicidal thoughts and suicidal behavior (suicidality); insomnia; paresthesia / hypesthesia and very rarely seizures; nausea, vomiting, diarrhea, abdominal pain; headache; arthralgia; myalgia; muscle cramps; tendency to increased bleeding, the formation of subcutaneous hemorrhages; heartbeat; swelling.
Overdose
Overdose symptoms were not detected during clinical studies of prolonged (22 weeks) treatment of adult patients with asthma at doses up to 200 mg / day, or during short (about 1 week) clinical studies while taking the drug at doses up to 900 mg / day. . There have been cases of acute overdose of the drug Singular (taking at least 1000 mg / day) in the post-registration period and during clinical trials in adults and children. Clinical and laboratory data indicated that the safety profiles of the drug Singulyar were comparable in children, adults and elderly patients. The most frequent symptoms were thirst, drowsiness, vomiting, agitation, headache and abdominal pain. These side effects are consistent with the safety profile of the drug Singular. Treatment: symptomatic therapy. There is no specific information about the treatment of drug overdose Singular. There is no data on the effectiveness of peritoneal dialysis or hemodialysis of montelukast.
Interaction with other drugs
Singular can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and / or treatment of allergic rhinitis. The recommended therapeutic dose of Montelukast did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethindrone 35/1), terfenadine, digoxin and warfarin. , but this does not require changes in the dosage regimen of the drug Singular. In vitro studies have established that montelukast inhibits the CYP2C8 isoenzyme. However, in the study of drug interaction in vivo of montelukast and rosiglitazone (it is metabolized with the participation of the CYP2C8 isoenzyme), there is no evidence of montelukast inhibition of the CYP2C8 isoenzyme. Therefore, in clinical practice, montelukast is not supposed to affect CYP2C8 mediated metabolism of a number of drugs, including paclitaxel, rosiglitazone, repaglinida. In vitro studies have shown that montelukast is a substrate of CYP2C8, 2C9 and 3A4.Data from a clinical study of drug interactions for montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the effect of the systemic effect of montelukast 4.4 times. Joint administration of itraconazole, a potent inhibitor of CYP3A4, together with gemfibrozil and montelukast did not lead to an additional increase in the effect of the systemic effect of montelukast. The effect of gemfibrozil on the systemic effect of montelukast cannot be considered clinically significant based on 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 patients taking the drug for about one week were not observed clinically significant adverse effects). Thus, when combined with gemfibrozil, a dose adjustment of montelukast is not required. According to the results of in vitro studies, no clinically significant drug interaction with other known inhibitors of CYP2C8 (for example, with trimethoprim) is expected. In addition, co-administration of montelukast with itraconazole alone did not lead to a significant increase in the effect of the systemic effect of montelukast. Combined treatment with bronchodilatorsThe singular is a valid supplement to monotherapy with bronchodilators, if the latter do not provide adequate control of asthma. Upon reaching the therapeutic effect of treatment with the drug Singular, you can begin to gradually reduce the dose of bronchodilators. Combined treatment with inhaled GCS. Treatment with the drug Singulyar provides an additional therapeutic effect in patients using inhaled GCS. Upon reaching stabilization, you can begin a gradual reduction in the dose of GCS under the supervision of a physician. In some cases, the complete abolition of inhaled corticosteroids is permissible, however, abrupt replacement of inhaled corticosteroids with Singular is not recommended.
special instructions
The effectiveness of the drug Singular for oral administration in relation to the treatment of acute attacks of bronchial asthma has not been established. Therefore, Singular pills are not recommended for the treatment of acute attacks of bronchial asthma.Patients should be instructed to always carry emergency medications to relieve bronchial asthma attacks (short-acting inhaled beta2-agonists). Do not stop taking the drug Singulyar in the period of exacerbation of asthma and the need for emergency medications (inhaled beta-2 agonists) short-acting). Patients with confirmed allergies to acetylsalicylic acid and other NSAIDs should not take these drugs during the period of treatment with the drug Singul p, since Singular, improving respiratory function in patients with allergic bronchial asthma, however, cannot completely prevent bronchoconstriction caused by their NSAIDs. The dose of inhaled corticosteroids used simultaneously with the drug Singularis can be gradually reduced under the supervision of a doctor, but by abrupt substitution of inhaled or oral GCS cannot be administered with the drug Singulyar. Neuropsychiatric disorders were described in patients taking Singulyar. Considering that these symptoms could have been caused by other factors, it is not known whether they are associated with taking the drug Singular. The physician should discuss these side effects with patients and / or their parents / guardians. Patients and / or their caregivers should be explained that if such symptoms occur, they should be reported to their attending physician. Reducing the dose of systemic corticosteroids in patients receiving anti-asthma drugs, including leukotriene receptor blockers, was accompanied in rare cases by the appearance of one or several of the following reactions: eosinophilia , rashes, worsening of pulmonary symptoms, cardiac complications and / or neuropathy, sometimes diagnosed as Chardzha-Strauss syndrome, systemic eosinophilic vasculitis. Although the causal relationship between these adverse reactions and therapy with leukotriene receptor antagonists has not been established, caution should be exercised in reducing the dose of systemic corticosteroids in patients receiving Singularis and conducting appropriate clinical observation. The effect on the ability to drive and work with data mechanisms that the use of the drug Singular affects the ability to drive a car or moving machinery was not detected.