MERCK SHARP & DOHME B.V. Merck Sharp & Dome / Merck Sharp & Dome B.V. Merck Sharp and Dome B.V. Merck Sharp & Dome Ltd / Merck Sharp & Dome Ltd / Merck Sharp & Dome B.V.

Country of origin

UK/Netherlands UK/Russia Netherlands

Product group

Respiratory system

Leukotriene receptor antagonist. Drug for the treatment of bronchial asthma and allergic rhinitis

Release forms

• 7 - blisters (2) - packs of cardboard. 7 - blisters (2) - packs of cardboard. pack of 14 tablets

Description of the dosage form

• Coated chewable tablets

pharmachologic effect

Leukotriene receptor antagonist. Montelukast selectively inhibits CysLT1 receptors of cysteinyl leukotrienes (LTC4, LTD4, LTE4) of the respiratory epithelium, and also prevents bronchospasm in patients with bronchial asthma caused by inhalation of cysteinyl leukotriene LTD4. Doses of 5 mg are sufficient to relieve bronchospasm induced by LTD4. The use of montelukast in doses exceeding 10 mg 1 time / day does not increase the effectiveness of the drug. Montelukast causes bronchodilation within 2 hours of oral administration and may supplement bronchodilation induced by beta2-adrenergic agonists.

Pharmacokinetics

Absorption After oral administration, montelukast is rapidly and almost completely absorbed from the gastrointestinal tract. Eating a normal meal does not affect Cmax in blood plasma and the bioavailability of coated tablets and chewable tablets. In adults, when taking coated tablets on an empty stomach at a dose of 10 mg, Cmax in plasma is achieved after 3 hours. Bioavailability when taken orally is 64%. After oral administration on an empty stomach, the drug in the form of chewable tablets at a dose of 5 mg Cmax in adults is achieved after 2 hours. Bioavailability is 73%. Distribution The binding of montelukast to plasma proteins is more than 99%. Vd averages 8-11 liters. With a single dose of the drug in the form of coated tablets, at a dose of 10 mg 1 time / day, a moderate (about 14%) cumulation of the active substance in plasma is observed. Metabolism Montelukast is extensively metabolized in the liver. When used in therapeutic doses, the concentration of montelukast metabolites in plasma in an equilibrium state in adults and children is not determined. It is assumed that cytochrome P450 isoenzymes (3A4 and 2C9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. The elimination T1 / 2 of montelukast in young healthy adults ranges from 2.7 to 5.5 hours. The clearance of montelukast in healthy adults averages 45 ml / min. After oral administration 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 in the bile. Pharmacokinetics in special clinical situations The pharmacokinetics of montelukast remains almost linear when taken orally at doses greater than 50 mg. When taking montelukast in the morning and evening, no differences in pharmacokinetics are observed. The pharmacokinetics of montelukast in women and men is similar. When administered orally coated tablets 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 liver cirrhosis, a slowdown in the metabolism of montelukast was noted, accompanied by an increase in AUC of approximately 41% after a single dose of the drug at a dose of 10 mg. The excretion of montelukast in these patients is slightly increased compared with healthy subjects (T1 / 2 averages 7. 4 hours). Dose modification of montelukast is not required in patients with mild to moderate hepatic impairment. 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 have not been evaluated in patients with renal insufficiency. Dose adjustment in this category

Special conditions

Singular® is not recommended for the treatment of acute asthma attacks. In the acute course of bronchial asthma, patients should be prescribed medications for therapy that stops and prevents attacks of the disease. Patients with bronchial asthma are advised to always carry emergency drugs (short-acting inhaled beta-adrenergic agonists) with them. To stop an acute attack of bronchial asthma after exercise, a drug is used to stop an attack, i.e. short-acting inhaled beta-adrenergic agonists. Treatment with Singular® does not guarantee absolute prevention of exacerbations. During the period of exacerbation of bronchial asthma and the need to use emergency medications (short-acting inhaled beta-adrenergic agonists) to stop attacks, you should not stop taking the drug Singulair®. The dose of inhaled corticosteroids used simultaneously with Singulair can be gradually reduced under the supervision of a physician. You should not abruptly replace therapy with inhaled or oral corticosteroids with Singulair. Patients with confirmed allergy to acetylsalicylic acid and other NSAIDs should avoid contact with these drugs during the period of treatment with Singular®, since Singular®, while improving respiratory function in patients with allergic bronchial asthma, nevertheless does not prevent bronchoconstriction due to the action of NSAIDs. Reducing the dose of corticosteroids for systemic use in patients receiving anti-asthma drugs, including leukotriene receptor antagonists, was accompanied in rare cases by the appearance of one or more of the following phenomena: eosinophilia, hemorrhagic rash, worsening of pulmonary symptoms, cardiac complications and / or neuropathy, sometimes diagnosed as Churg-Ostrich syndrome (systemic eosinophilic vasculitis). Although a causal relationship of these adverse events with therapy with leukotriene receptor antagonists has not been established, when reducing the systemic dose of corticosteroids in patients taking Singulair®, care must be taken and appropriate clinical monitoring should be carried out. Patients with phenylketonuria should be informed that 1 chewable tablet contains at least 1.2 mg of aspartame.

Composition

• montelukast - 10 mg; Excipients: microcrystalline cellulose, lactose, croscarmellose sodium, hyprolose, magnesium stearate. The composition of the shell covering the tablet: hyprolose, hypromellose, titanium dioxide, iron dyes red oxide and yellow iron oxide and carnauba wax. montelukast - 4 mg; Excipients: mannitol, microcrystalline cellulose, hyprolose, iron dye red oxide, croscarmellose sodium, cherry flavor, aspartame and magnesium stearate. montelukast - 5 mg; Excipients: mannitol, microcrystalline cellulose, hyprolose, iron dye red oxide, croscarmellose sodium, cherry flavor, aspartame and magnesium stearate. montelukast (in the form of montelukast sodium) 4 mg Excipients: mannitol, microcrystalline cellulose, hyprolose, iron dye red oxide, croscarmellose sodium, cherry flavor, aspartame, magnesium stearate. montelukast 5 mg Excipients: mannitol, microcrystalline cellulose, hyprolose, iron oxide red dye, croscarmellose sodium, cherry flavor, aspartame, magnesium stearate.

Singulair indications for use

• Prevention and long-term treatment of bronchial asthma in adults and children aged 6 years and older, including: - prevention of day and night symptoms of the disease; - treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid; - prevention of bronchospasm caused by exercise. Relief of daytime and nighttime symptoms of seasonal allergic rhinitis (in adults and children aged 6 years and older) and persistent allergic rhinitis (in adults and children aged 6 years and older)

Singular contraindications

• Hypersensitivity to any of the components of the drug. Children's age up to 6 years.

Singular dosage

• 10 mg 4 mg 5 mg

Singulair side effects

• Children aged 2 to 5 years with bronchial asthma Clinical studies of the drug Singular® in this age group were conducted with the participation of 573 children. In a 12-week placebo-controlled study in the Singulair® treatment group, the only observed side effect occurring at a frequency of more than 1% compared with placebo was thirst. The difference between the two treatment groups was not statistically significant. At longer follow-up (12 months or more), the side effect profile did not change. Children aged 2 to 14 years with seasonal allergic rhinitis Clinical studies of the drug Singular® in this age group were conducted with the participation of 280 children. The safety profile of the drug in children was generally similar to that in adults and comparable to that of placebo. According to a 2-week, placebo-controlled study in the Singulair® treatment group, side effects occurring at a frequency of more than 1% compared with placebo were not registered.

drug interaction

SINGULAIR can be administered together with other medicines traditionally used for the prevention and long-term treatment of bronchial asthma. The recommended clinical dose of montelukast 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. AUC decreases in patients who simultaneously receive phenobarbital (by about 40%), however, correction of the dosing regimen of SINGULAIR in such patients is not required. Treatment with bronchodilators: SINGULAIR can be added to the treatment of patients whose asthma is not controlled by bronchodilators alone. When a therapeutic effect is achieved (usually after the first dose) during therapy with SINGULAIR, the dose of bronchodilators can be gradually reduced. Inhaled glucocorticosteroids: Treatment with SINGULAIR provides additional therapeutic effect to patients.

Overdose

overdoses of the drug Singular® in patients with chronic bronchial asthma when used at a dose exceeding 200 mg / day for 22 weeks and at a dose of 900 mg / day for 1 week have not been identified.

Storage conditions

• keep away from children

Information provided

active substance: montelukast;

1 film-coated tablet contains 10.4 mg montelukast sodium (equivalent to 10 mg montelukast);

Excipients: hydroxypropylcellulose, microcrystalline cellulose, lactose, croscarmellose sodium, magnesium stearate

tablet shell: hydroxypropylmethylcellulose, methylhydroxypropylcellulose, titanium dioxide (E 171), iron oxide red (E172), iron oxide yellow (E 172), carnauba wax.

Dosage form

Film-coated tablets.

Basic physical and chemical properties: Beige, square, rounded, film-coated tablets, debossed with "SINGULAIR" on one side and "MSD 117" on the other side.

Pharmacological group

Means for systemic use in obstructive respiratory diseases. Leukotriene receptor blockers.

ATX code R03D C03.

Pharmacological properties

Pharmacodynamics.

Cysteinyl leukotrienes (LTC 4 , LTD 4 , LTE 4 ) are potent inflammatory eicosanoids secreted by various cells, including mast cells and eosinophils. These important pro-asthma mediators bind to cysteinyl leukotriene receptors (CysLT) present in the human airways and cause responses such as bronchospasm, mucus secretion, increased vascular permeability, and an increase in eosinophils.

Montelukast, when administered orally, is an active compound that binds with high selectivity and affinity to CysLT 1 receptors. According to clinical studies, montelukast suppresses bronchospasm after inhalation of LTD 4 at a dose of 5 mg. Bronchodilation is observed within 2:00 after oral administration, this effect was additive to bronchodilation caused by β-agonists. Treatment with montelukast depresses both the early and late phases of bronchoconstriction caused by antigenic stimulation. Montelukast, compared with placebo, reduces the number of peripheral blood eosinophils in adults and children. In a separate study, montelukast significantly reduced the number of eosinophils in the airways (as measured by sputum). In adults and children aged 2 to 14 years, montelukast, compared with placebo, reduces the number of peripheral blood eosinophils and improves the clinical control of asthma.

In adult studies, montelukast 10 mg once daily compared with placebo showed significant improvements in morning FEV1 (10.4% and 2.7% change from baseline), morning peak expiratory flow (MPF) ( change from baseline of 24.5 L/min and 3.3 L/min) and a significant decrease in total β-agonist use (change from baseline of -26.1% and -4.6%).

Improvement in patient-reported measures of daytime and nighttime asthma symptoms was significantly better than placebo.

A study in adults demonstrated the ability of montelukast to complement the clinical effect of inhaled corticosteroids (change (%) in baseline for inhaled beclomethasone plus montelukast compared with beclomethasone, respectively, for FEV 1: 5.43% and 1.04%, use of β-agonists: -8 , 70% and 2.64%). Compared to inhaled beclomethasone (200 mcg twice daily, spacer device), montelukast demonstrated a faster initial response, although during the 12-week study, beclomethasone resulted in a greater mean therapeutic effect (% change from baseline for montelukast compared to beclomethasone). respectively for FEV 1: 7.49% and 13.3%, the use of β-agonist: -28.28% and -43.89%). However, compared with beclomethasone, more patients treated with montelukast achieved a similar clinical response (i.e., 50% of patients treated with beclomethasone achieved an improvement in FEV 1 of about 11% or more compared to baseline, while 42% patients treated with montelukast achieved the same response).

In a 12-week placebo-controlled study in children aged 2 to 5 years, montelukast 4 mg once daily improved asthma control compared with placebo, regardless of concomitant control therapy (corticosteroids inhaled/nebulized, sodium cromoglycate for inhalation / in a nebulizer). 60% of patients received no other control therapy. Montelukast improved daytime symptoms (including cough, wheezing, difficulty breathing, and activity limitation) and nighttime symptoms compared with placebo. Montelukast also reduced the frequency of on-demand beta-agonist use and emergency corticosteroid use when asthma worsened, compared with placebo. Patients who use montelukast had more asthma-free days than patients who received placebo. The therapeutic effect was achieved after the first dose.

In a 12-month placebo-controlled study in children aged 2 to 5 years with mild asthma and episodic exacerbations, montelukast 4 mg once daily significantly (p≤0.001) reduced the summer exacerbation frequency (ER) of asthma compared with placebo (1.66 U and 2.34 U, respectively) [RU defined as ≥3 consecutive days of daytime symptoms requiring β-agonists or corticosteroids (oral or inhaled), or hospitalization for asthma].

The percentage decline in the annual rate of EH was 31.9%, with 95% CI 16.9, 44.1.

In a placebo-controlled study in children 6 months to 5 years of age with intermittent (but not persistent) asthma, treatment with montelukast was continued for 12 months on a 4 mg once daily regimen or in 12-day courses starting each course at the occurrence of an episode of intermittent symptoms. There was no significant difference between patients treated with montelukast 4 mg and those treated with placebo in terms of the number of asthma episodes progressing to an asthma attack (defined as an asthma episode requiring an unscheduled visit to a doctor, emergency room, or hospital; or treatment with oral, intravenous, or intramuscular corticosteroids).

In an 8-week study in children aged 6 to 14 years, montelukast 5 mg once daily compared to placebo significantly improved respiratory function (change from baseline FEV 1: 8.71% compared to 4, 16%, change in morning PSV: 27.9 L/min vs. 17.8 L/min) and reduced the frequency of on-demand beta-agonist use (-11.7% change from baseline vs. +8, 2%).

In a 12-month study comparing the efficacy of montelukast and inhaled fluticasone in controlling asthma in children aged 6 to 14 years with mild persistent asthma, montelukast was at least as effective as fluticasone in terms of increased (percentage) number of days without fast-acting rescue drugs (primary endpoint). On average, over the 12-month treatment period, the percentage of days without emergency treatment increased from 61.6 to 84.0 in the montelukast group and from 60.9 to 86.7 in the fluticasone group. Between groups, the difference in percent mean square (LS) increase in the number of days without the use of rapid-acting rescue drugs was statistically significant (-2.8 with 95% CI -4.7, -0.9), but within the clinically predetermined lesser efficiency.

Montelukast and fluticasone also improved asthma control with respect to secondary variables assessed over a 12-month treatment period.

FEV 1 increased from 1.83 L to 2.09 L in the montelukast group and from 1.85 L to 2.14 L in the fluticasone group. The intergroup difference in the LS index relative to the increase in FEV 1 was 0.02 l with 95% CI 0.06, 0.02. The mean percentage increase from baseline in the proper FEV 1 was 0.6% in the montelukast treatment group and 2.7% in the fluticasone treatment group. The difference in the LS score was significant: -2.2% with 95% CI -3.6, -0.7.

The number of days with β-agonist use decreased from 38.0% to 15.4% in the montelukast group and from 38.5% to 12.8% in the fluticasone group. The intergroup difference in LS score relative to the percentage of days with β-agonist use was significant 2.7 with 95% CI 0.9, 4.5.

The rate of patients with an asthma attack (an asthma attack is defined as a period of worsening asthma, requiring treatment with oral steroids, an unscheduled doctor's visit, emergency care or hospitalization) was 32.2% in the montelukast group and 25.6% in the fluticasone group; coefficient of discrepancy (95% CI) significant: equal to 1.38 (1.04, 1.84).

The rate of the number of patients who used systemic (mainly oral) corticosteroids during the study period was 17.8% in the montelukast group and 10.5% in the fluticasone group. The intergroup difference in LS was significant: 7.3% with 95% CI 2.9; 11.7.

A significant reduction in exercise-related bronchoconstriction (EIB) was demonstrated during a 12-week study in adults (maximum reduction in FEV 1 22.33% for montelukast compared with 32.40% for placebo, time to recovery within 5% from baseline FEV1 44.22 min compared to 60.64 min). This effect was observed during the 12-week study period. A reduction in ERF was also demonstrated in a short study in children aged 6 to 14 years (maximum reduction in FEV 1 18.27% compared to 26.11%, time to recovery within 5% of baseline FEV 1 17.76 min compared to 27.98 min). The effect in both studies was demonstrated at the end of the once-daily dosing interval.

In patients with aspirin sensitivity who were on current therapy with inhaled and/or oral corticosteroids, montelukast treatment compared with placebo resulted in a significant improvement in asthma control (change in baseline FEV 1 is 8.55% vs -1.74% and change from baseline in a reduction in total β-agonist use -27.78% vs. 2.09%).

Pharmacokinetics.

absorption

Montelukast is rapidly absorbed after oral administration. After the use by adults on an empty stomach of tablets, film-coated, 10 mg, the average maximum concentration (C max) in blood plasma was reached after 3:00 (T max). Bioavailability when administered orally is 64%. The intake of normal food does not affect the bioavailability and C max when administered orally. Safety and efficacy have been confirmed in clinical studies with the use of film-coated tablets, 10 mg, regardless of mealtime.

For 5 mg chewable tablets, Cmax in adults was reached 2 hours after ingestion on an empty stomach. Oral bioavailability is 73% and decreases to 63% when taken with a standard meal.

After taking 4 mg chewable tablets on an empty stomach at the age of 2 to 5 years, the Cmax is reached 2:00 after taking the drug. The mean C max is 66% higher and the mean C min lower than in adults after taking 10 mg tablets.

distribution

More than 99% of montelukast binds to plasma proteins. The volume of distribution of montelukast in the stationary phase averages from 8 to 11 liters. In studies in rats using radiolabeled montelukast, passage through the blood-brain barrier was minimal. In addition, in all other tissues, the concentrations of the radioisotope-designated material 24 hours after the dose were also minimal.

metabolism

Montelukast is actively metabolized. During studies using therapeutic doses, steady state plasma concentrations of montelukast metabolites in adults and pediatric patients are not determined.

Cytochrome P450 2C8 is the main enzyme in the metabolism of montelukast. In addition, cytochromes CYP 3A4 and 2C9 play a minor role in the metabolism of montelukast, although itraconazole (an inhibitor of CYP 3A4) did not change the pharmacokinetic parameters of montelukast in healthy volunteers who received montelukast 10 mg per day. According to research results in vitro using human liver microsomes, therapeutic plasma concentrations of montelukast do not suppress cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. The participation of metabolites in the therapeutic effect of montelukast is minimal.

output

The plasma clearance of montelukast in healthy adult volunteers averages 45 ml/min. After taking isotope-labeled montelukast, 86% is excreted in the feces within 5 days and less than 0.2% in the urine. Together with the oral bioavailability of montelukast, this fact indicates that montelukast and its metabolites are almost completely excreted in the bile.

Pharmacokinetics in different groups of patients

For patients with mild to moderate hepatic impairment, dose adjustment is not required.

No study has been conducted in patients with impaired renal function. Since montelukast and its metabolites are excreted in the bile, dose adjustment is not considered necessary in patients with impaired renal function. There are no data on the nature of the pharmacokinetics of montelukast in patients with severe liver dysfunction (more than 9 points on the Child-Pugh scale).

When taking large doses of montelukast (which is 20 and 60 times the dose recommended for adults), a decrease in the concentration of theophylline in blood plasma was observed. This effect is not observed when taking the recommended dose of 10 mg once a day.

Indications

As adjunctive treatment for asthma in patients with mild to moderate persistent asthma that is not adequately controlled with inhaled corticosteroids, and with inadequate clinical asthma control with short-acting β-adrenergic agonists, which are used as needed. In asthmatic patients taking SINGULAIR ® , this drug also relieves the symptoms of seasonal allergic rhinitis.

Prevention of asthma, the dominant component of which is exercise-induced bronchospasm.

Relief of symptoms of seasonal and perennial allergic rhinitis.

Contraindications

Hypersensitivity to the components of the drug. Age up to 15 years (for a dose of 10 mg).

Interaction with other medicinal products and other forms of interaction

Singulair ® can be given with other medicines that are commonly used for the prevention or long-term treatment of asthma. In a drug interaction study, the recommended clinical dose of montelukast had no important clinical effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin, and warfarin.

In patients who simultaneously took phenobarbital, the area under the concentration-time curve (AUC) for montelukast decreased by approximately 40%. Because montelukast is metabolized by CYP 3A4, 2C8 and 2C9, caution should be exercised, especially in children, when montelukast is given concomitantly with inducers of CYP 3A4, 2C8 and 2C9, such as phenytoin, phenobarbital and rifampicin.

Research in vitro showed that montelukast is a potent inhibitor of CYP 2C8. However, data from a clinical drug interaction study involving montelukast and rosiglitazone (marker substrate; drug metabolized by CYP 2C8) showed that montelukast is not an inhibitor of CYP 2C8 in vivo. Thus, montelukast does not significantly affect the metabolism of drugs metabolized by this enzyme (eg paclitaxel, rosiglitazone and repaglinide).

During research in vitro Montelukast has been found to be a substrate of CYP 2C8 and to a lesser extent 2C9 and 3A4. In a clinical drug interaction study using montelukast and gemfibrozil (an inhibitor of CYP2C8 and 2C9), gemfibrozil increased the systemic exposure of montelukast by 4.4 times. When co-administered with gemfibrozil or other potent inhibitors of CYP 2C8, dose adjustment of montelukast is not required, but the physician should take into account the increased risk of adverse reactions.

According to research results in vitro, clinically important interactions are not expected with less potent inhibitors of CYP2C8 (eg trimethoprim). Simultaneous use of montelukast with itraconazole, a strong CYP 3A4 inhibitor, did not lead to a significant increase in the systemic exposure of montelukast.

Application features

Patients should be warned that SINGULAIR ® oral is never used to treat acute asthma attacks and that they should always carry the appropriate rescue medication with them. In an acute attack, short-acting inhaled β-agonists should be used. Patients should consult their physician as soon as possible if they require more short-acting β-agonist than usual.

Do not abruptly replace montelukast therapy with inhaled or oral corticosteroids.

There is no evidence that the dose of oral corticosteroids can be reduced while the use of montelukast.

It was reported about the occurrence of neuropsychiatric phenomena in patients taking SINGULAIR ® (see section "Adverse reactions"). Since these events may be influenced by other factors, it is not known whether these events are associated with the use of the drug Singulair ® . Physicians should discuss these adverse events with their patients and/or their caregivers. Patients and/or caregivers should be instructed to notify their physician if such changes occur.

In rare cases, patients receiving anti-asthma drugs, including montelukast, may experience systemic eosinophilia, sometimes along with clinical manifestations of vasculitis, the so-called Churg-Ostrich syndrome, which is treated with systemic corticosteroids.

Such cases are usually (but not always) associated with dose reduction or withdrawal of the GCS drug. The possibility that leukotriene receptor antagonists may be associated with Churgah-Ostrich syndrome cannot be refuted or confirmed. Physicians should be aware of the possibility of patients developing eosinophilia, vasculitis, worsening pulmonary symptoms, cardiac complications, and/or neuropathy. Patients who develop these symptoms should be re-examined and their treatment regimen reviewed.

Treatment with montelukast prevents patients with aspirin-related asthma from taking aspirin or other non-steroidal anti-inflammatory drugs.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Use during pregnancy or lactation.

Pregnancy. Animal studies do not demonstrate harmful effects regarding effects on pregnancy or embryonic/fetal development.

The limited database information on pregnancies does not indicate a causal relationship between the use of Singulair ® and the occurrence of malformations (such as limb defects), which have rarely been reported during worldwide post-marketing experience.

Singular ® should only be used during pregnancy if it is considered absolutely necessary.

Lactation. Studies in rats have shown that montelukast passes into milk. It is not known whether montelukast is excreted in breast milk in women.

Singulair ® may only be used during breastfeeding if it is considered absolutely necessary.

The ability to influence the reaction rate when driving vehicles or operating other mechanisms.

Montelukast is not expected to affect the patient's ability to drive or use machines. However, drowsiness or dizziness have been very rarely reported.

Dosage and administration

The dose for patients (aged 15 years and older) with asthma or asthma and concomitant seasonal allergic rhinitis is 10 mg (1 tablet) per day, in the evening. To alleviate the symptoms of allergic rhinitis, the time of admission is selected individually.

General recommendations. The therapeutic effect of the drug Singular ® on asthma control occurs within 1 day. The drug can be used regardless of the meal. Patients should be advised to continue taking Singulair even if asthma is controlled and also during periods of asthma exacerbation. The drug should not be used simultaneously with drugs containing the active ingredient montelukast.

There is no need for dose adjustment for elderly patients with impaired renal function or with mild to moderate hepatic impairment. There are no data on patients with severe hepatic impairment. The dosage for men and women is the same.

Treatment with Singulair ® in relation to other asthma treatment.

SINGULAIR ® can be added to a patient's existing treatment regimen.

inhaled corticosteroids. Singulair ® can be used as adjunctive treatment in patients in whom inhaled corticosteroids, together with short-acting β-agonists, given as needed, do not provide satisfactory clinical control of the disease.

The drug SINGULAIR ® should not abruptly replace inhaled corticosteroids (see section "Peculiarities of use").

Children. Applied to children over the age of 15 years. Children under 15 years of age should use the drug in the form of chewable tablets.

Overdose

There is no specific information on the treatment of overdose with Singulair®. In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to adult patients for 22 weeks, and in short-term studies up to 900 mg/day for about one week, with no clinically important adverse reactions occurring.

In post-marketing use and in clinical studies, there have been reports of acute overdose of the drug Singulair ® . They included the use of the drug by adults and children in doses exceeding 1000 mg (approximately 61 mg/kg in a child aged 42 months). The obtained clinical and laboratory data were consistent with the safety profile in adult patients and children. In most cases of overdose, no adverse reactions have been reported. The most frequently observed adverse reactions were consistent with the safety profile of the drug Singular ® and included: abdominal pain, drowsiness, thirst, headache, vomiting and psychomotor hyperactivity.

It is not known whether montelukast is eliminated by peritoneal dialysis or hemodialysis.

Adverse reactions

Montelukast has been evaluated in clinical trials for:

film-coated tablets, 10 mg - in approximately 4000 patients with asthma aged 15 years and older;

film-coated tablets, 10 mg - in approximately 400 patients with asthma and seasonal allergic rhinitis aged 15 years and older;

During clinical studies, the following adverse reactions were reported frequently (from ≥1 / 100 to<1/10) у пациентов, получавших лечение монтелукастом, а также с большей частотой, чем у пациентов, получавших лечение плацебо.

Table 1

Classes of organ systems	adult patients, children 15 years and older (Two 12-week studies; n = 795)
From the side of the nervous system	Headache
From the gastrointestinal tract	abdominal pain

During clinical studies with prolonged treatment of a small number of adult patients for 2 years and children aged 6 to 14 years for 12 months, the safety profile did not change.

post-marketing period

Adverse reactions reported in the post-marketing period, listed according to organ system classes and specific terms, are presented in Table 2.

The frequency is established according to the data of relevant clinical studies.

table 2

Class of organ systems	Adverse reaction time	frequency *
Infections and infestations	Upper respiratory infections **	Often
From the blood and lymphatic system	tendency to increase bleeding
	thrombocytopenia	Very rarely
From the side of the immune system	Hypersensitivity reactions, including anaphylaxis
	Eosinophilic infiltration of the liver	Very rarely
From the side of the psyche	Sleep disturbance, including nightmares, insomnia, somnambulism, irritability, anxiety, restlessness, agitation, including aggressive behavior or hostility, depression.
	Psychomotor hyperactivity, tremor
	Hallucinations, suicidal thoughts and behavior (suicidality), disorientation, impaired attention, memory impairment.	Very rarely
From the side of the nervous system

In modern pharmacies, you can find quite a few remedies that are more or less effective against rhinitis, allergies and asthma. The description, instructions for the drug "Singulair", reviews are of rather high interest among the townsfolk. The average price of this medication this year is about a thousand rubles per pack. However, some outlets offer medicine for only 800 rubles, while in others the cost is close to one and a half thousand. The difference in price is explained not only by the specifics of the pharmacy, but also by the peculiarities of the release form.

What will help?

Based on the description in the instructions for use of "Singular", we can conclude that the tool has a positive effect on the following health disorders:

• asthma;
• rhinitis provoked by allergies.

Bronchial asthma is not only treated with a long course, but can also be prevented by the use of the described medication. As a preventive measure, the use of Singulair should be monitored by the attending physician. How can Singulair be used for children? 4 mg of medication per day can be eaten by a baby if he is already two years old. In general, this dose is intended for children from 2 to 5 years. And 5 mg per day can already be used by kids from 6 years and older.

Asthma: how will it help?

If bronchial asthma is diagnosed, already at a dose of 4 mg chewable tablets "Singulair" will have the following positive effect on the body:

• provide assistance to patients suffering from hypersensitivity to aspirin;
• prevent the development of seizures (regardless of the time of day);
• eliminate;
• will help prevent the development of asthma against the background of increased physical activity.

As for rhinitis provoked by an allergic reaction of the body, then, as follows from the reviews, instructions for use, for children "Singulair" (in the form of chewable tablets of 10 mg) is allowed from the age of 15 and has a pronounced positive effect. The use of the drug alleviates the condition of patients with both seasonal allergies and intolerance reactions that do not depend on the time of year. Symptoms are eliminated regardless of the time of day.

What can be replaced?

It must be said that there are relatively few reviews about the Singulair tool in the Russian-speaking sector of the Internet. Presumably, this is due to the difference in price (instructions for use for children "Singular" in general terms are similar to the prescriptions of other chewable tablets) in comparison with analogues. On average, medicines that have a similar effect in Russian pharmacies cost about 500 rubles per pack. Most popular titles:

• "Montelukast";
• "Montelast";
• "Singlon".

Of course, instructions for the use of "Singular" and analogues may differ, as well as the main active substance. At will, it is categorically not recommended to replace the remedy recommended by the doctor with a cheaper one, since cases of individual intolerance are possible, and the patient's condition will only get worse. This is especially true if the medication is selected for the treatment of a child.

However, if there is a desire to save money, then you can do without unnecessary risk if you agree on the replacement with your doctor. Reviews about the analogues of "Singular" (instructions for the use of these drugs are usually no more difficult - either they chew the tablets or use an inhaler) are generally positive, patients who underwent therapy note the high effectiveness of the drugs.

"Singular": how does it work?

The main active substance that ensures the effectiveness of the described drug is montelukast. This substance belongs to the category of leukotriene receptor antagonists. On sale, the medication is presented in tablets for chewing. Each tablet is coated with an easily digestible coating. Description of the drug "Singulair", the full composition and features of use are indicated in the attached instructions.

The tablets are packed in blisters, packaged in cardboard boxes. Each box is equipped with a paper insert containing complete information about the medication. Here, without fail, in detail, the description of the "Singular", indications, instructions for use are indicated in detail.

In some cases, you can use Singular only very carefully, under the supervision of your doctor, or even better to refrain from using the medication, find a replacement for it. Instructions for use of 5-, 10-milligram "Singular" for children / adults mention the following groups of people:

• children under six years of age;
• persons who do not tolerate the components of the drug;
• pregnant women;
• women during lactation;
• patients with phenylketonuria.

How to use?

So, you already know that all usage patterns are necessarily prescribed in the instructions for use of Singulair. Are you interested in reviews, the price of this drug? Many people say that this medicine is effective, but too expensive. The manufacturer indicates that the remedy is best used in the evening (it has the maximum effect in bronchial asthma). Tablets are chewed, the moment of use does not depend on the time of eating.

For patients over 15 years of age, the recommended daily dose is 10 mg (taken at a time). It is recommended to use in the evening, before going to sleep. Instructions for use "Singular" for children must be studied before purchasing this medication.

And when will it work?

Instructions for the medical use of the drug "Singulair" draws attention to the fact that only one day is needed to achieve a pronounced therapeutic effect. At the same time, interrupting treatment as soon as the first positive results are obtained is categorically not recommended.

The manufacturer advises to continue treatment in order to achieve maximum control over the situation and prevent the development of asthma attacks. If the disease has passed into an acute form, the use of the medication involves the control of the attending physician and lasts the entire period of exacerbation. This moment is indicated in the instructions for use of "Singular" for children and adults.

It is allowed to combine the described chewable tablets with GCS in the form of inhalations. The tool does not conflict with bronchodilators, which also allows simultaneous use in therapy.

Pharmacology

When ingested, the active component of the Singulair drug has a depressing effect on the CysLT1 receptors. This allows you to influence the mediators that accompany inflammatory processes. These same mediators are associated with the increased activity of the functioning of the bronchi, which is characteristic of asthma. Proper use of the drug allows you to reduce the amount of secretion generated in the bronchi.

As a result, the swelling of the airways becomes weaker. In general, this has a positive effect on the condition of the mucous membrane covering the respiratory tract. Proper use of the medication can reduce the frequency and number of seizures. The disease progresses more easily. Always try to carefully read the instructions for use of "Singular" for children / adults.

On the first day from the moment the active component enters the human body, the bronchodilator effect increases, which then for a long time period is maintained sufficiently pronounced so that the asthmatic condition stabilizes. The greatest positive effect is observed if persistent asthma is diagnosed, and bronchodilators do not allow to control the patient's condition sufficiently.

Negative effects: what to be prepared for?

According to the instructions for the use of "Singular" for children / adults, you may encounter a number of side effects. Some of them are fixed in a large percentage of cases. Patients complain about:

• cough;
• runny nose;
• headaches;
• nausea;
• sore throat;
• abdominal pain;
• allergy.

Laboratory tests show that liver transaminases are activated.

In some cases, infection of the respiratory system is possible. The upper paths suffer first.

In some patients, bleeding was observed when using the medication. There are known cases of intolerance, explained by the individual characteristics of the organism. This can lead to anaphylaxis. With a frequency of less than one case out of ten thousand, those who practiced treatment with Singulair may have liver damage - eosinophilic infiltration.

Some patients complain of a change in character under the influence of the drug: they become irritable, aggressive. There may be manifestations of hostility, sometimes - agitation. In some cases, side effects are manifested by tachycardia, a headache may occur, and convulsions rarely begin. Many patients complained that during the period of treatment with the use of "Singulair" they constantly want to sleep. Extremely rare, but still recorded cases of hepatitis.

Rare, but apt: unpleasant side effects

If an allergic reaction develops when using Singulair, not only a relatively safe urticaria is possible, but also an angioedema that poses a danger to the health and life of the patient.

Patients undergoing treatment with this drug are more prone to the appearance of hematomas, erythema. The skin may become covered with a rash or begin to itch. In some patients, the nose bleeds, a pulmonary form of eosinophilia develops. From the gastrointestinal tract, the following side effects may occur:

• stool disorder;
• pancreatitis;
• dyspepsia;
• nausea, vomiting.

Some patients complain of pain, aching sensations in the muscles, joints, turning into convulsions (extremely rare). In younger children, therapy is sometimes accompanied by urinary incontinence. At any age, patients treated with Singulair sometimes complain of fatigue, general weakness, asthenic syndrome and swelling.

Application features

Based on the possible side effects and taking into account the likelihood of their manifestation, "Singular" is considered a drug that is characterized by good tolerance, regardless of age. Most of the adverse events accompanying therapy are not serious enough to require a correction of the treatment strategy. The need to cancel the drug "Singular" is rare.

The manufacturer (and at the same time doctors) draws attention to the fact that even if improvements in the patient's condition are achieved, it is very important to continue treatment using Singulair, despite tangible progress. The tool is not intended for stopping seizures, its use is not a reason to refuse bronchodilators, since Singulair does not replace this group of medicines. The manufacturer also draws attention to the fact that there is no information on the effectiveness of the described drug in acute attacks, therefore, therapy with the use of Singulair is not recommended for a patient with such a diagnosis.

It is important!

Using "Singulair", it is forbidden to simultaneously undergo therapy with aspirin, other drugs of the same group, if an allergic reaction to drugs of the NSAID category has been established. When monitoring the condition of a patient using Singulair, it must be remembered that medical statistics describe cases of treatment accompanied by mental and neurological disorders.

One of the rare diseases that occurs in a small percentage of the population is galactose intolerance, due to genetic prerequisites. If an asthma patient suffers from this health disorder, he should not use Singulair in the form of chewable tablets, since each dose contains lactose in the form of monohydrate in an amount of 10 mg. Similar restrictions are imposed on asthmatics who suffer from lactase deficiency from birth. Serious restrictions on the possibility of therapy are imposed by glucose-galactose malabsorption, in which patients also cannot use tablets containing lactose monohydrate.

Caution is the key to health

If a patient with bronchial asthma has a history of phenylketonuria, the doctor must report (and the manufacturer indicates this fact in the instructions for use) that one tablet contains aspartame. Its volumes are similar to 0.842 mg of phenylalanine.

Studies of the effect on the human body of the components of the tablets "Singular" did not show an effect on the concentration. It is allowed to drive a car, other moving units during the course of a therapeutic course.

What if there are too many?

An overdose of the drug "Singulair" can lead to rather unpleasant consequences, so it is important to use the tablets correctly, following the recommendations of the manufacturer and the attending physician. Studies, clinical trials, as well as reviews of patients who have used the drug contain references to a feeling of thirst, a gag reflex, and overexcitation that accompany poisoning of the body. Your head and stomach may hurt. Many who have overdosed have complained of cravings for sleep.

There is no specific antidote. In case of poisoning of the body, it is necessary to carry out symptomatic therapy.

We combine with the mind

"Singulair" can be safely used with many medicines developed for patients with bronchial asthma suffering from rhinitis provoked by allergies. The agent is combined with both prophylactic drugs and drugs used for the long-term treatment of these disorders. Compatibility does not depend on the dosage form of the drug "Singulair".

If the patient was treated with corticosteroids in the form of aerosols, the manufacturer recommends switching to Singulair smoothly, under the supervision of the attending physician. A sharp change in treatment strategy can provoke negative reactions of the body. At will, it is not recommended to change one type of medication to another, without the recommendation of a doctor and his attentive attitude to the situation.

The tool is designed as a base for long-term therapy. Self-medication with its use can lead to unpredictable reactions. In an acute infectious process, the drug can be used when assessing the patient's condition by a doctor. In such a situation, a combination with other drugs, chosen by a specialist, based on the specifics of the disease, is usually practiced.

Some facts about the product:

Instructions for use

Price in the online pharmacy site: from 1 108

Composition

The active ingredient of the drug is a new generation substance Montelukast (montelukast), which has a bronchodilatory effect.

Additional Ingredients: Mannitol, Hydroxypropylcellulose, Magnesium Stearate.

Shell composition: titanium dioxide, hydroxypropyl cellulose, carnauba wax, hypromellose, dyes based on iron oxide.

Release form

Light beige film-coated tablets, square-shaped with rounded edges. Packed in blisters and cardboard packaging, which contains instructions for use

Tablets for chewing are convex on both sides, pink, oval type. On one side of the pill, the pressed name "Singulair" is applied, on the other - "Msd 117".

Pharmacotherapeutic group

The drug Singulair (Latin designation Singulair) is intended for systemic administration in obstructive diseases and lesions of the respiratory system. It is a selective leukotriene receptor blocker.

Pharmacology

Montelukast is the active pharmaceutical ingredient of the drug Singulair. This substance is included in a number of new drugs that can effectively expand the bronchi. It selectively disables leukotriene receptors in bronchial tissues and lungs, preventing their spasm, prevents the formation of sputum, capillary permeability, and an increase in the number of eosinophils. This fact is explained by the fact that cysteinyl leukotrienes are considered powerful meridians of inflammatory reactions. Proasthmatic mediators, by attaching to cysteinyl leukotriene receptors in the respiratory system, contribute to bronchospasm due to excessive secretion of mucus. Cysteinyl leukotrienes significantly affect the onset of rhinitis of allergic etiology.

Under the action of an allergen, any stage of an allergic reaction is accompanied by the release of cysteinyl leukotrienes on the mucous membranes of the respiratory tract. This leads to a violation of the patency of the nasal passages and the manifestation of asthmatic symptoms and allergic rhinitis.

Montelukast, which has a high affinity, selectively detects CysLT1 receptors from others, which contributes to the inhibition of the physiological action of LTD4. This achieves a bronchodilating effect, regardless of the stage of the disease.

Pharmacokinetics

Oral administration of montelukast is due to its immediate absorption by the walls of the digestive tract. The use of food does not slow down its bioavailability and the achievement of peak concentrations of the drug in blood plasma.

Reception by adult patients of tablets Singulair with a dosage of 10 mg contributes to the achievement of the highest concentration of the active element in plasma after 3-4 hours. Its volume at the site of exposure in the body reaches 64%.

When taken on an empty stomach, 5 mg chewable tablets, the maximum serum accumulation in adults is reached in about two hours, and the bioavailability is 73%.

When using 4 mg chewable tablets in children aged 2 to 5 years, the maximum accumulation in serum appears two hours after the use of the drug. The average bioavailability is 66% higher than in adult patients as a result of the use of Singulair tablets with a dosage of 10 mg.

Almost 99% of montelukast binds to blood serum proteins. The volume of dispersion of the substance, taking into account the average indicators, reaches 8 - 11 liters.

Metabolization of the active element of montelukast occurs dynamically in the liver, involving microsomal enzymes of cytochromes P450 3A4 and 2C9.

In adults, the excretion of montelukast from serum reaches 45 ml / min. The oral type of the drug is 86% excreted in the feces for about 5 days, and less than 0.2% of the substance is excreted in the urine.

The time of the process of removing half of the substance of montelukast from the body of adults varies from 2.7 to 5.5 hours. Violations of pharmacokinetics do not occur if the drug is used at different times of the day. A slight accumulation of the active element in the serum can be observed with a single use of tablets of 10 mg per day.

In elderly patients, when using a single dose of 10 mg, the maximum concentration of the active element in plasma and pharmacodynamics are indistinguishable from the category of young patients. Only the half-life of the drug differs in the elderly. The process is slower. But this fact does not provide for dosage correction.

Also, patients with an uncomplicated form of liver failure do not need to change the dosage. Studies of the pharmacokinetics of montelukast in patients with hepatitis and severe liver dysfunction syndrome have not been conducted.

Patients suffering from renal diseases also do not require dosage adjustment. Since the metabolites of the active ingredient are not excreted in the urine, therefore, studies in this area have not been conducted.

Indications and clinical characteristics

As an adjuvant treatment for bronchial asthma in patients with mild to severe persistent asthma not controlled by inhaled corticosteroids. Also, with a weak effect on the disease of β-adrenergic antagonists of short duration, used as needed.

It is used for preventive purposes, treatment of asthma in adults and children. The medicine eliminates the symptoms of the disease at any time of the day, is effective for patients sensitive to aspirin, reduces the likelihood of bronchospasm after physical labor.

Preventive and therapeutic agent for allergic rhinitis, both seasonal and permanent.

Dosage and administration

Regardless of the meal, the tablets are taken orally once a day. According to the instructions for the treatment of asthmatic syndrome, Singulair is preferably drunk after sunset. For the treatment of allergic rhinitis, the time of taking the medicine is not important. Patients with asthma and allergic rhinitis are required to take one tablet at bedtime to achieve the desired effect.

Adult patients and children from 15 years of age take the drug at a dosage of 10 mg per day.

In case of allergic rhinitis, the dosage period is determined by the attending physician.

Special instructions for use

Singulair is not recommended for use during an unexpected aggravation of asthma attacks. In the acute period of the course of the disease, patients should take medications that stop and stop asthmatic attacks. The dose of inhaled drugs used together with Singulair is reduced gradually and only after monitoring by a doctor. Montelukast-based preparations cannot be spontaneously replaced with other oral medications or inhaled glucocorticosteroids.

Reducing the main therapeutic dose for patients using anti-asthma drugs provokes their risk of onset of single or multiple adverse effects. Although the relationship between the cause and effect of adverse events in the combined treatment with leukotriene receptor blockers has not been indicated, it is important to be careful and timely undergo all clinical examinations in patients using Singulair in parallel when reducing the curative dose of corticosteroids.

Compatibility with other drugs

Singulair tablets are compatible with a wide range of pharmaceuticals prescribed for prophylactic purposes for long-term therapy of bronchial asthma. The recommended dose of montelukast does not interfere with the therapeutic effect of the following drugs: prednisolone, theophylline, prednisone, hormonal contraceptives, warfarin, terfenadine, and digoxin.

With a one-time therapy with glucocorticoids in the form of inhalations with this medication, the therapeutic effect is enhanced. After reducing the symptoms of the disease, the dose of glucocorticoids is reduced systematically under the supervision of a doctor. For some patients, complete cancellation of inhaled forms of treatment is allowed. It is impossible to sharply compensate for inhalations with glucocorticoids by taking Singulair.

Side effects

Most often, the drug is well tolerated. Side effects that appear during therapy are usually mild, which does not entail the need to interrupt the course of treatment. The following manifestations were often noted:

• eosinophilic infiltration of hepatic tissues;
• feeling of weakness, malaise;
• shortness of breath, cough;
• dyspeptic phenomena, accompanied by pain, vomiting, nausea;
• rash on the skin;
• urticaria, angioedema, anaphylactic reaction;
• the occurrence of hematomas, bleeding;
• puffiness;
• depression, sleep and memory disorders.

In rare cases, the following symptoms appear:

• psychomotor excitability, involuntary trembling;
• cephalgia, dizziness;
• disorientation in space, sleep disturbances, increased fatigue;
• aggression, hallucinations;
• dry mouth;
• Churg-Strauss syndrome, pulmonary eosinophilia;
• children's enuresis;
• pyrexia.

The effect of the drug on the ability to manage moving mechanisms and cars

There was no information confirming that the use of the drug leads to a violation of the ability to control driving mechanisms and vehicles.

Storage conditions

It is necessary to store the drug in its original packaging, not exceeding the temperature regime of 30 ° C, in a place restricted to children.

Singulair (montelukast). Composition, mechanism of action, release forms. Analogues. Indications, contraindications, instructions for use. Side effects, prices and reviews

Thanks

The site provides reference information for informational purposes only. Diagnosis and treatment of diseases should be carried out under the supervision of a specialist. All drugs have contraindications. Expert advice is required!

What is the drug Singulair ( montelukast)?

Singular ( montelukast) - a modern drug in the form of tablets, intended for the treatment and prevention of asthma attacks. It is intended for the treatment of patients of all ages, but is most often prescribed in pediatric practice ( children aged 6 years and older). The drug is taken 1 tablet at night, due to which the daytime and nighttime symptoms of bronchial asthma decrease, the quality of breathing improves, and the frequency of asthmatic attacks decreases.
Doctors recommend using Singular along with conventional asthma medications. The drug improves the quality of life of patients with bronchial asthma, reduces the doses of corticosteroids and other drugs, but their complete replacement with montelukast is not recommended. The patient should always carry inhalers that stop ( filming) acute attack of bronchial asthma ( salbutamol, clenbuterol). This is due to the fact that the singular does not act immediately and cannot provide immediate assistance during an attack.

The drug can also be used for some allergic diseases, such as allergic rhinitis. It reduces allergic swelling of the upper respiratory tract, reduces mucus secretion, sneezing. In addition, recent research data indicate good experience with the use of the drug in neurodegenerative diseases, Alzheimer's, Parkinson's diseases.

The drug is known under various trade names. Singulair, montelukast, montelar, almont, singlon - all these are the names of the same drug. Depending on the manufacturer, the cost of the drug may differ. However, the active substance, form of release, indications and method of application for the listed drugs are the same.

Pharmacological group of the drug. Leukotriene antagonists

Montelukast belongs to the group of leukotriene antagonists. This pharmacological group has a small number of representatives; it is used to treat bronchial asthma. Bronchial asthma is an allergic disease characterized by spasm ( reduction) smooth muscles of the bronchi, because of which the patient cannot take a normal breath and exhale. Many factors play a role in the development of bronchial asthma, including a violation of the autonomic nervous system, the participation of cells and inflammatory mediators.

One of the mechanisms of spasm of the bronchial tree is the release of inflammatory mediators in response to contact with an allergen. Histamine and leukotrienes are usually mediators of inflammation in the bronchi. If histamines cause short-term and instantaneous bronchospasm ( narrowing of the bronchial tree), then leukotrienes can cause bronchospasm, the duration of which is several days.

Leukotriene antagonists are drugs that compete with leukotriene for binding to receptors. As a result, this mediator loses its ability to exert all influence on the bronchial tree. Thus, the respiratory system is protected from attacks of bronchial asthma mediated by leukotriene. Unfortunately, this group of drugs is not able to protect against other options for the development of bronchospasm ( for example, from the action of histamine), so patients suffering from bronchial asthma have to take other drugs.

The main active ingredient of the drug. The mechanism of action of the drug

The main active ingredient of the drug Singular ( and a number of other trade names) is montelukast. The Latin name for this substance is montelukastum. The action of the drug lies in the specific blocking of receptors for three leukotrienes ( LTS4, LTD4, LTE4), which is the most powerful factor in the development of chronic inflammation in bronchial asthma. Taking the drug in an amount of 10 mg is sufficient to block leukotrienes during the day.

Taking montelukast in bronchial asthma has the following effects:

• relieves spasm of smooth muscles of the bronchi and blood vessels;
• expands the bronchial tree ( this effect lasts about 2 hours);
• reduces mucus secretion;
• improves bronchial cleansing;
• reduces the migration of cellular elements of the blood ( neutrophils, leukocytes) in the region of the bronchial wall.

The effect of montelukast is long-lasting, has the ability to accumulate. The drug is quite well tolerated, as it has a selective effect. However, this also has disadvantages, since the drug acts only on a part of the receptors through which bronchial asthma can develop. This necessitates the use of other drugs for bronchial asthma ( albeit in doses less than standard).

Forms of release of the drug Singular ( tablets 10 mg, chewable tablets 4 mg, 5 mg)

The drug is available in three dosage forms. The 10 mg film-coated tablets are intended for use by adults and adolescents over 15 years of age. They are taken 1 at a time before bedtime with a sufficient amount of water. The number of tablets in a package may vary depending on the manufacturer and trade name of the drug. The package may contain from 7 to 28 tablets.

The drug is also available in the form of chewable tablets. The dosage of 5 mg is intended for ages 6 to 15 years, and tablets containing 4 mg of montelukast are used for 2 to 6 years. Chewable tablets have a round or oval shape, white color, have a pleasant smell ( cherry or other). The appearance of the tablets may vary slightly depending on the manufacturer. Chewable tablets should be taken once a day in the evening, chewing in the mouth until completely dissolved.

Are there other forms of release of the drug ( drops, solution, spray, ointment)?

The drug is available only in the form of tablets for oral administration and in the form of chewable tablets. With this method of use, the drug enters the bloodstream and has a systemic effect. This is due to its beneficial effect in some other allergic diseases. In the form of nasal drops, ointment, oral solution, the drug is not available. To achieve local action in a pharmacy, you can purchase anti-allergic or corticosteroid drugs in the form of ointments, gels, nasal drops.

The composition of various dosage forms of the drug

The composition of montelukast necessarily includes the main medicinal substance and additional ( Excipients). Dosage of the main drug substance ( montelukast) is always indicated on the packaging and is standard for various trade names of the drug ( 4 mg, 5 mg or 10 mg). Various additives can be used as additional substances, the patient should pay attention to them in case of drug or food allergies.

The composition of the Singular tablets for oral administration includes the following excipients:

• hyprolosis;
• lactose monohydrate;
• magnesium stearate;
• titanium dioxide;
• iron oxide;
• wax.

Singulair chewable tablets contain the following excipients:

• mannitol;
• hyprolosis;
• microcrystalline cellulose;
• magnesium stearate;
• iron oxide;
• aspartame;
• cherry flavor.

Is Singulair a hormonal drug or an antibiotic?

The drug is not a hormonal drug. Even though hormones glucocorticosteroids) are really used in the treatment of bronchial asthma, this drug is not hormonal. Moreover, Singular allows you to reduce the doses of hormonal drugs used in curbing asthma attacks. Thus, the body experiences less stress and the risk of developing side effects from the treatment of bronchial asthma is significantly reduced.

Singulair is also not an antibiotic. Antibiotics are not used in the treatment of allergic diseases and bronchial asthma in particular. They help to cope with the bacterial flora that lives in the respiratory tract, but are not able to influence the mechanism of allergy development. That is why they should not be used in the treatment of bronchial asthma. Sometimes coughing, difficulty breathing caused by bacterial bronchitis, pneumonia, whooping cough, can mimic the symptoms of bronchial asthma. In these cases, a thorough medical examination is required. Antibiotics are sometimes prescribed for the treatment of such diseases.

Analogues of the drug Singular

Today there are a large number of analogues of the drug Singular, despite the fact that it appeared relatively recently. Three large groups of analogues of this tool can be distinguished. Depending on what purpose is pursued from the use of the singular, you can choose an analogue from a certain group. Before using Singulair or its analogues, it is necessary to consult a doctor or pharmacist.

There are the following groups of analogues of the drug singular:

• Direct analogues of the singular in composition. They contain the same active ingredient, but are produced by different manufacturers. The rules for using these analogues are almost completely the same.
• Glucocorticoids. They are used for bronchial asthma in the form of inhalations, they have anti-inflammatory, anti-allergic and immunosuppressive effects.
• Antihistamines. They are mainly used systemically, they can reduce the allergic manifestations of various diseases ( e.g. allergic rhinitis). Their disadvantage is the lack of effectiveness in bronchial asthma.

It should be borne in mind that when buying Singular analogues, advice from specialists is needed. So, for the treatment of bronchial asthma, you can use direct analogues of the singular in composition, glucocorticoids. With pollinosis ( seasonal allergic rhinitis) the best results show antihistamines . In most cases, the singular is used in combination with other drugs, including their counterparts.

Singular and montelar, singleon, almont. Which is better, montelukast, singular or another generic?

Montelukast is available under various brand names. There are many drugs that contain it in the same concentrations, have the same method of application and indications. Their only difference is the country of origin, and, accordingly, the cost. In terms of the quality of the therapeutic effect, they are all approximately comparable.

Montelukast as an active ingredient is found in the following trade names of drugs:

• montelukast;
• singular;
• Montelar;
• singleon;
• almont;
• Monler;
• ectalust;
• singulex and others.

Singulair is an original Canadian drug, first obtained in Montreal. The active substance montelukast has been registered and patented under the name "singular" in the United States. Today you can buy this drug at a relatively high price. Subsequently, cheaper generics have appeared that contain the same medicinal substance. The lower price is due to several reasons. Firstly, generics do not pass the full scope of clinical trials, and secondly, due to the transfer of the pharmaceutical industry to third world countries ( Pakistan, Bangladesh, India) the requirements for the level of the technological process are somewhat reduced. As a result, generics may have a higher percentage of impurities.

In Russian pharmacies, it is not always possible to find all existing drugs containing montelukast. Usually the patient can choose from 2 - 3 generics. It is very difficult to say for sure which of the drugs is the best in terms of price-quality ratio. It is worth noting that a generic called montelukast is several times cheaper than the original singular, and in terms of effectiveness it is quite comparable to it. The patient, knowing all the advantages and disadvantages of the original drug and generics, can make an independent decision on the purchase of a drug containing montelukast.

Singular and glucocorticoids. Singulair and Pulmicort ( budesonide). Singular and Nasonex ( mometasone)

Glucocorticoids, taken in the form of inhalations or systemically, have an anti-inflammatory effect in the bronchi. They are used in severe bronchial asthma for preventive purposes, as they reduce the frequency of attacks. This group of drugs reduces swelling of the bronchial mucosa, reduces the production of mucus and sputum. Despite all the advantages, this group of drugs is hormones, respectively, has a large number of side effects. Glucocorticoids reduce immunity, and also inhibit the human endocrine system, especially the adrenal cortex. These shortcomings are exacerbated by the need for long-term use of glucocorticoids in bronchial asthma. At the same time, these drugs are not able to stop an acute attack of bronchial asthma.

Pulmicort is a white suspension that is supplied in single doses for inhalation through a nebulizer. A nebulizer is a drug that mixes medicine with a liquid and sprays it into the air you breathe. The active ingredient in Pulmicort is budesonide. Treatment with glucocorticoids lasts a month or more. Singulair in bronchial asthma is used for the same purpose ( prevention of acute attacks), but it is not a hormonal drug, which makes it easier to tolerate and has fewer side effects. However, the combined use of Pulmicort and Singulair is not excluded.

Severe coughing fits are the main concern of parents with whooping cough and sometimes lead to misdiagnosis ( e.g. bronchial asthma). In addition to antibiotics for whooping cough, it is necessary to use sedatives, a diet rich in vitamins, and breathing exercises. Some doctors prescribe montelukast to reduce the frequency and duration of coughing. Unfortunately, its effectiveness in whooping cough is being questioned. Sometimes breathing moist air gives better results in stopping whooping cough than using montelukast. This drug is used only for bronchial asthma, with whooping cough and other bacterial infections, it brings very little benefit.

Is cough, fever an indication for the use of Singulair?

Cough and fever are not indications for the use of montelukast. The need to use this drug exists only if the specialist detects an allergic respiratory disease in the patient. For the diagnosis of bronchial asthma, special studies with the use of drugs are required. They can only be performed by a pulmonologist. Therefore, the appointment of montelukast can only be carried out by a doctor if there are reliable indications. In case of severe cough, high fever or other symptoms, it is recommended to seek help from medical specialists.

Contraindications to the use of Singulair

Singular is a relatively safe drug, it has a small number of contraindications and side effects. This advantage of the drug is especially noticeable in comparison with glucocorticoids, hormones used in the treatment of bronchial asthma. Singular can be used in the treatment of children older than 2 or 6 years ( depending on the release form). It should be used with caution during pregnancy and liver disease.

Singulair is contraindicated for use in the following cases:

• Phenylketonuria. This hereditary disease is associated with a congenital lack of enzymes that process the amino acid phenylalanine. Montelukast contains this amino acid ( in the form of aspartame), therefore its use for this category of patients is prohibited.

• Serious liver disease. In severe liver diseases, the drug is excreted from the body for a very long time, which can lead to toxic damage to various systems and undesirable side effects. For moderate and mild liver damage, the drug is allowed in a reduced dose under the supervision of medical specialists.
• Childhood ( up to 2 or 6 years). The drug is available for children in the form of chewable tablets. They contain less active ingredient than conventional tablets. Chewable tablets containing 4 mg of montelukast can be taken from 2 to 6 years, and with a content of 5 mg - from 6 to 15 years. Up to 2 years, the use of the drug is prohibited.
• Pregnancy and lactation. When using the drug during pregnancy or breastfeeding, various pathologies in the fetus and infant may be observed.
• Hypersensitivity to the components of the drug. Allergy to the components of the drug is very rare. Despite this, in case of hypersensitivity, the use of the drug should be discontinued.

Can I use the drug during pregnancy and lactation?

The drug is not recommended for use during pregnancy and lactation. Despite the fact that the use of montelukast is much safer than most drugs ( e.g. antibiotics), doctors recommend to refrain from using it during pregnancy. Animal studies have shown no particular teratogenicity ( disfiguring) effect of the drug, however, full-fledged clinical trials in humans have not been conducted. That is why doctors cannot guarantee the complete safety of using the drug during pregnancy, especially given the fact that the active substance of the drug is able to pass through the placenta.

There are no data on the use of the drug during breastfeeding in humans. It is not known if montelukast is excreted in breast milk. However, studies in rats have shown that in rodents it can actually pass into milk. Therefore, during lactation, doctors usually do not prescribe montelukast.

Can this drug be used in the treatment of children?

The drug is fully approved for use in children. The only restriction concerns the age from birth to 2 years. At this age, you should not use the drug at all. After two years of age, the child can be given chewable tablets with a dosage of 4 mg. After 6 years, doctors prescribe chewable tablets containing 5 mg of montelukast. If necessary, you can replace the 5 mg chewable tablet with half of the 10 mg adult dose by dividing the regular tablet into two parts.

It should be borne in mind that the original drug is available in three dosage forms, and generics do not always fully correspond to it. Therefore, in the absence of 4 mg chewable tablets in pharmacies, the drug can only be used from 6 years of age. When treating children with Singulair, it is recommended to consult with pediatrician ( enroll) .

Can I use the drug during vaccinations in children?

Vaccination is very important for today's population. Thanks to this, a person can avoid a large number of diseases. The bulk of vaccinations are carried out in childhood, but some of them continue to be performed until the age of 21 and beyond. The use of montelukast for the treatment of bronchial asthma does not change the vaccination schedule in any way and does not reduce their effectiveness.

It is worth noting that the drug may reduce the reliability of allergic tests, including the Mantoux test. This test is used to diagnose tuberculosis and involves the detection of a specific immune response ( redness and swelling of the skin) to the subcutaneous injection of tuberculin. When using montelukast, the immune response may be weaker, which theoretically can lead to false negative results. In order to avoid mistakes, it is necessary to warn the doctor about all the medicines that the patient is taking at the time of the allergy tests.

Instructions for use of the drug

Proper use of any drug is the basis of its effective use. Singular ( montelukast) is issued in a convenient form ( in the form of regular tablets and tablets for chewing), so that usually there are no special difficulties in its use. The drug has a pleasant taste and smell, which is important in the treatment of children. When using this medicine, it is very important to observe the duration of treatment recommended by the doctor, despite the high price of the drug. It is also not recommended to use an expired drug, as it has a reduced effectiveness and carries a higher potential harm.

How to take Singulair in the form of tablets?

The drug in the form of tablets containing 10 mg of montelukast should be taken 1 time per day ( in the morning or evening) regardless of the meal, drinking plenty of water. In the treatment of bronchial asthma and allergic rhinitis, it is recommended to use tablets at night, although the time of day does not play a special role. In a sense, this is due to the fact that during sleep the patient will not notice some of the possible side effects of the drug ( dizziness, drowsiness).

The use of this drug usually does not require dose adjustments. As a rule, patients with liver and kidney disease take standard doses of the drug. Individual selection of dosage is necessary only in case of severe liver failure. In general, Singulair is usually well tolerated and rarely causes side effects.

Can I split a montelukast tablet?

A montelukast tablet may well be divided to take half the 5 mg dose. This can be done to treat children 6 to 15 years of age instead of using chewable tablets. Significant savings can be achieved by dividing the tablets. The inconvenience lies in the fact that the tablet does not have a special risk for dividing into two equal parts. In addition, the integrity of the protective shell is violated, due to which the drug becomes less protected from the acidic environment of the stomach. A tablet divided in half cannot be stored for a long time, since the active substance of the drug, which is not coated, is destroyed by physical factors. Therefore, it is best to use standard 4 or 5 mg chewable tablets whenever possible for children.

How to use Singulair chewable tablets?

Singulair chewable tablets are available in a dosage of 4 mg ( for children from 2 to 6 years old) and 5 mg ( for children from 6 to 15 years old). Chewable tablets should be thoroughly chewed in the mouth or sucked. Due to the presence of flavoring in the composition of the tablets, they have a pleasant taste and smell. Singulair chewable tablets are preferably used at night, before going to bed. Communication of the use of the drug with food intake is not required. When treating with chewable tablets, it is important to monitor the frequency of taking tablets by a child ( no more than 1 tablet per day).

What is the duration of taking Singulair?

The duration of taking Singulair is not regulated by the instructions, it depends on the clinical symptoms and the nature of the development of the disease. After an objective improvement in the symptoms of bronchial asthma, it is necessary to undergo an examination by the attending physician, who decides on the need to continue treatment. As a rule, it continues even after the normalization of the functions of the respiratory system. Treatment of asthma with Singular can take several months.

How quickly does the drug start to work?

The drug is absorbed from the gastrointestinal tract into the blood quickly and almost completely. Despite this, it cannot be said that the effect of its use appears almost immediately. The drug should not be used in case of an acute attack of bronchial asthma, as its action is delayed. The maximum concentration of the drug after taking on an empty stomach is reached only after 2 hours. It is by this time that the bronchial tubes expand, caused by taking the drug. Thus, the drug acts remotely and shows itself much better in protecting against potential exacerbations of bronchial asthma.

How long does the singular last? Does the drug have a cumulative effect?

The duration of action of the drug is enough to take only 1 tablet of the drug per day. Studies show that after 24 hours its concentration in all tissues becomes minimal. It is excreted almost entirely through the liver and gallbladder. Removal of the drug from the body of an elderly person takes a little longer. It has been established that with daily intake of montelukast, a cumulative effect of taking the drug is observed. This means that its effect is increased by 10 - 20% with constant use.

How to combine Singular with other drugs for the treatment of bronchial asthma?

The drug is well combined with other drugs used to treat bronchial asthma. So, montelukast does not affect the rate of excretion of glucocorticoids and bronchodilators from the body ( drugs that dilate the bronchi), so it does not increase their toxicity. It is a reasonable addition to the named groups of medicines. After achieving a pronounced therapeutic effect from Singulair, doctors usually reduce the doses of hormonal drugs and beta-agonists, thereby reducing the negative impact of these groups of drugs on the body. They are known to be much more harmful to the body than montelukast. However, the complete and abrupt abolition of glucocorticoids in bronchial asthma is still not recommended.

What should I do if I missed one of the Singularity tricks?

If you skip one of the doses of Singular, do not take a double dose at the next dose. Skipping, of course, somewhat reduces the effectiveness of the drug, but is not a big problem. A positive aspect in the treatment of Singulair is that it has a cumulative effect, due to which a certain amount of the drug continues to remain in the body even when one tablet is missed. However, skipping montelukast should not be abused, as this may worsen the course of bronchial asthma or allergic rhinitis.

Shelf life and storage conditions of the singular

The shelf life of Singulair chewable tablets is 2 years, and the coated tablets for oral administration are 3 years. The release date and expiry date are always indicated on the drug packaging. The drug is suitable for the specified period only if all conditions were observed during its storage. It is strongly not recommended to buy and use an expired drug, as this can be dangerous to health.

Singulair is recommended to be stored in its original packaging in a dark, dry place out of direct sunlight. Storage temperature - room temperature, from 15 to 25 degrees. The drug should be kept out of the reach of children, as they are attracted by the pleasant taste of the tablets, which can lead to an overdose.

Side effects of the drug

The drug, according to the manufacturer, is characterized by a small number of side effects. However, due to the fact that it is new and has little experience in the application. In the course of its use, new, rather rare cases of side effects are described. Practice shows that, in general, the drug is well tolerated and does not cause serious side effects that would force its use to be discontinued.
Side effects of montelukast include violations of the following systems:

• Nervous system. If any side effects occur, you should consult a doctor and, if necessary, stop using the drug.

  The effect of the drug on the central nervous system and psyche

  Singulair can really have a negative impact on the nervous system and psyche. This phenomenon is the most common side effect of the drug. Doctors recommend taking the drug at night, just before bed, in order to reduce the likelihood of developing these side effects. Negative effects on the nervous system can have different manifestations, from anxiety and agitation to hallucinations and suicidal tendencies. Unfortunately, it is impossible to predict the effect of the drug in this regard. In case of serious mental disorders, mood deterioration, depression, the drug should be discontinued and other drugs should be used to treat bronchial asthma.

  Does the drug affect the ability to drive vehicles and other mechanisms?

  It is believed that the drug does not affect the ability to drive vehicles and other mechanisms. However, it is not fully researched and does not have much clinical experience. That is why individual reactions to the drug can be unpredictable. In addition, there are cases of a negative effect of the drug on the nervous system and mental state. Therefore, when treating with montelukast, it is recommended to take precautions when driving mechanical means and transport.

  Does the drug cause addiction, addiction, withdrawal syndrome?

  Cases of dependence on montelukast have not been observed. The drug, although it has an effect on the nervous system, does not cause physical or mental dependence. This feature is important, since the drug is intended for long-term use. Compared with montelukast, hormonal drugs for the treatment of bronchial asthma ( budesonide) have a significant drawback, since their use cannot be abruptly terminated. This can lead to a deterioration in the production of one's own hormones.

  Is it possible to combine Singulair treatment with alcohol intake?

  The combination of Singulair and alcohol is not recommended, despite the fact that no particular interaction between the active ingredient of the drug and alcohol has been found. The disadvantage of taking Singular and alcohol at the same time is the increased risk of toxic effects of the drug on the liver. As you know, Singulair is almost completely excreted through the liver, which is why its use creates an increased load on this organ. Additional alcohol consumption further wears out the liver and can lead to hepatitis.

  Singular overdose

  Clinical trials have not revealed cases of drug overdose. During a five-month treatment with the drug ( when using 200 mg per day, which is 20 times the recommended dose) patients showed no symptoms of overdose. It has been proven that an overdose of montelukast can occur only at a hundredfold excess of the usual dose ( taking 1000 mg per day). Overdose is characterized by thirst, drowsiness, nausea, vomiting, and abdominal pain.

  Singularity price ( montelukast) in Russian cities

  The active substance montelukast is sold in pharmacies under various trade names. The original American drug Singular is quite expensive. Fortunately, there are various generics that have a more affordable price. So, for example, Russian-made montelukast costs 2 times cheaper and contains 2 times more tablets per package. Considering that a patient with bronchial asthma must take the drug for a sufficiently long time, buying a cheaper generic brings good savings.
  The cost of regular and chewable tablets is about the same. When buying, it should be borne in mind that chewable tablets are intended for children, and regular tablets are for adults. The price of the drug may differ depending on the general price level in the region of Russia, on the cost of transporting and storing the drug. In addition, in some pharmacies drugs are sold at a significantly lower price than in others within the same city.

  The cost of various dosage forms of the drug Singular ( montelukast)
  

  City	Manufacturer, dosage forms
  	Singular ( USA), tablets 10 mg, 14 pieces	Singular ( USA), chewable tablets 5 mg, 14 pieces	Montelukast ( Russia), tablets 10 mg, 30 pieces	Montelukast ( Russia), chewable tablets 5 mg, 28 pieces
  Moscow		940 rubles	499 rubles	599 rubles
  St. Petersburg	900 rubles	928 rubles	567 rubles	612 rubles
  Novosibirsk	1098 rubles	1017 rubles	510 rubles	627 rubles
  Ekaterinburg	1040 rubles	980 rubles	498 rubles	537 rubles
  Voronezh	1113 rubles		569 rubles	576 rubles
  Chelyabinsk	905 rubles	807 rubles		537 rubles
  Krasnoyarsk	1140 rubles	1050 rubles	625 rubles	675 rubles
  Kazan	1010 rubles		458 rubles	512 rubles
  Samara	1038 rubles	998 rubles	510 rubles	580 rubles
  Rostov-on-Don			539 rubles

  Can I buy the drug without a doctor's prescription?

  To buy a drug be it singular or its generic) requires a doctor's prescription. However, this is not due to the peculiarities of its interaction with the human body. The drug has no particularly serious contraindications or side effects. The requirement of a prescription when buying this drug is explained by the fact that the treatment of bronchial asthma requires supervision by a doctor. If necessary, only a doctor can correctly adjust the treatment regimen.

  Can I get the drug for free?

  The drug is not included in the list of essential medicines, so it cannot be obtained free of charge in the usual way. However, there is the possibility of preferential treatment at the place of permanent treatment. To do this, you must write a statement to the pulmonologist, in which the patient is undergoing therapy for bronchial asthma. Further, the issue of its free provision is decided by a special commission.