Singular pill chewable 4 mg 14 pcs
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Active ingredients
Montelukast
Release form
Pills
Composition
Active ingredient: montelukast (montelukast) Concentration of the active ingredient: 4 mg
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 taking oral montelukast quickly and almost completely absorbed. Eating normal food does not affect Cmax in the blood plasma and the bioavailability of chewable pills. In children aged 2 to 5 years after ingestion of 4 mg Cmax chewable pills on an empty stomach, is achieved after 2 hours. The pharmacokinetics of montelukast remains almost linear when taken orally in doses over 50 mg. There is no difference in pharmacokinetics when taking montelukast in the morning and evening hours. DistributionThe binding of montelukast to plasma proteins is more than 99%. Vd in the equilibrium state is 8-11 l. Studies conducted on rats with radioactively labeled montelukast indicate minimal penetration through the BBB. In addition, the concentration of labeled montelukast 24 h after administration was minimal in all other tissues. When receiving montelukast at a dose of 10 mg 1 time / day, a moderate (about 14%) cumulation of the active substance in plasma is observed. MetabolismMontelukast is actively metabolized. When used in therapeutic doses, the concentration of plasma metabolites of montelukast in an equilibrium state in adults and children is not determined. In vitro studies using human liver microsomes have shown that cytochrome P450: CYP3A4, 2C8 and 2C9 isoenzymes are involved in the metabolism of montelukast. According to the results of in vitro studies on human liver microsomes, montelukast, at therapeutic plasma concentrations, does not inhibit CYP3A4, 2C9, 1A2, 2A6, 2C19, and 2D6 isoenzymes. The release of T1 / 2 of montelukast in young healthy adults ranges from 2.7 to 5.5 Montelukast clearance is a healthy 45 ml / min in healthy adults. After ingestion of labeled radioactivity of Montelukast, 86% is excreted in the feces within 5 days and less than 0.2% in the urine, which confirms that montelukast and its metabolites are excreted almost exclusively with bile. With a single dose of 10 mg of montelukast, the pharmacokinetic profile and bioavailability are similar in elderly and young patients.In older people, T1 / 2 of Montelukast from plasma is somewhat longer. Correction of the drug dose in elderly patients is not required. There were no differences in clinically significant pharmacokinetic effects in patients of various races. In patients with mild to moderate hepatic insufficiency and clinical manifestations of cirrhosis, montelukast metabolism slowed down 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 (average T1 / 2 - 7.4 h). Changes in the dose of montelukast are not required for patients with mild to moderate hepatic insufficiency. Data on the nature of 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 was not evaluated. Dose adjustment in this category of patients is not required.
Indications
prevention and long-term treatment of 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 aged 2 years and older.
Contraindications
children up to 2 years; phenylketonuria, hypersensitivity to the drug.
Precautionary measures
Chewable 4 mg pills contain aspartame - a source of phenylalanine. Patients with phenylketonuria should be informed that each 4 mg chewable tablet contains aspartame in an amount equivalent to 0.674 mg of phenylalanine. A singular tablet form of 4 mg is not recommended for patients with phenylketonuria.
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
The drug is taken orally 1 time / day, regardless of the meal. In bronchial asthma, 4 mg (1 tablet) is prescribed at night. In bronchial asthma and allergic rhinitis, 4 mg (1 tablet) is prescribed at night. In allergic rhinitis, it is prescribed 4 mg (1 tab.) / Day in an individual regimen, depending on the time of the greatest exacerbation of symptoms. For children aged 2 to 5 years with bronchial asthma and / or allergic rhinitis, the dose is 4 mg (1 tab.) / Day. For children, elderly patients, patients with renal insufficiency and patients with lung / Merenii dysfunction of liver specific dose adjustment is required.
Side effects
On the part of the blood coagulation system: increased bleeding. Allergic reactions: anaphylaxis, angioedema; very rarely - eosinophilic infiltration of the liver. For the central nervous system and peripheral nervous system: drowsiness, paresthesia / hypesthesia, irritability, aggressive behavior, anxiety, unusual dreams, hallucinations, depression, insomnia, irritability, suicidal thoughts and behavior, tremor; very rarely - convulsions. From the side of the cardiovascular system: palpitations. From the side of the digestive system: diarrhea, dyspepsia; rarely, cholestatic hepatitis, damage to hepatocytes, most often against the background of concomitant drug therapy or the existing pathology of the liver (alcoholic and other forms of hepatitis); very rarely - vomiting, pancreatitis. From the musculoskeletal system: arthralgia, myalgia, muscle spasms. Dermatological reactions: itching, urticaria, tendency to hematoma, erythema nodosum. In general, Singular is well tolerated. Side effects are usually mild and, as a rule, do not require discontinuation of treatment. The overall frequency of side effects reported when using the drug Singular is comparable to that for placebo.
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, repaglinide. In vitro studies have shown that montelukast is a substrate of CYP2C8, 2C9, and 3A4 isoenzymes.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 must be exercised in the dose of systemic corticosteroids in patients receiving Singular, and appropriate clinical observation is required. Effects on driving ability and control mechanisms This section does not apply to drug Singular tablet chewable 4 mg, since it is intended for the treatment of children from 2 to 5 years.Thus, the information presented below refers to the active substance of the drug montelukast. It is not expected that taking the drug Singulyar will affect the ability to drive a car and moving machinery. However, individual reactions to the drug may be different. Some side effects (such as dizziness and drowsiness), which have been reported to occur very rarely with the use of the drug Singular, can affect the ability of some patients to drive vehicles and moving mechanisms.