Antipyretics for children are prescribed by a pediatrician. But there are emergency situations with fever when the child needs to be given medicine immediately. Then the parents take responsibility and use antipyretic drugs. What is allowed to be given to infants? How can you lower the temperature in older children? What medications are the safest?
Bronchospasm is a phenomenon familiar to patients suffering from asthma. Against the background of obstructed bronchial passages, increased sputum production is observed, and the number of eosinophils increases. Symptoms of seasonal and year-round allergic rhinitis are swelling of the mucous membrane of the nasopharynx, lacrimation, headache, runny nose, itching, sneezing.
The American drug singular “turns off” cysteinyl leukotriene receptors in the epithelium of the patient’s respiratory organs, and also effectively relieves bronchospasms. Active substance The medicine contains montelukast.
The scope of application of the product includes the prevention of bronchospasms, treatment bronchial asthma in children and adults, as well as therapy for seasonal and regular allergic rhinitis. For children, the medication is approved from 6 years of age. Release form: tablets, chewable tablets.
The product is expensive, prices range from 1000–1300 rubles per package of 14 tablets. Cheap analogues Singular preparations contain the same active ingredient or have similar indications for use.
Russian-made analogues
Close substitutes for Singular, produced in Russia, are a high-quality replacement for the cheap medicine with montelukast. The table contains a list of similar products with prices and brief characteristics.
| Name of the drug | Average price in rubles | Characteristic |
| Moncasta | 750–840 | Chewable tablets with montelukast, causing bronchodilation within 2 hours after use. Used to relieve attacks of bronchial asthma and rhinitis of allergic origin. |
| Montelukast | 520–750 | The product has similar indications and contraindications to use as Singularia. |
| Ektalust | 440–520 | The cheapest synonym for singular from a domestic manufacturer. The composition of the drug includes montelukast. |
Ukrainian substitutes
Ukrainian-made medicines can be a worthy replacement for Singularia. Their cost is cheaper than the drug in question.
Medicines belong to pharmacological group medications for the treatment of obstructive diseases respiratory system, although not all products on the list contain montelukast.
- Montel. Inexpensive Ukrainian analogue with the same active ingredient. The drug is used to treat seasonal allergic rhinitis and bronchial asthma of varying severity. Available in the form of regular pills and chewable ones. The average price is 450–490 rubles.
- Allergomax. Medicine in the form of syrup, nasal spray or tablets. The drug effectively eliminates the symptoms of allergic rhinitis - lacrimation, itching, swelling, headache. The average price is 56–90 rubles.
- Bronchomax. Fenspiride hydrochloride syrup or tablets. The medication is indicated for otitis media, sinusitis, rhinitis, including allergic rhinitis, and bronchitis. The drug is also used in the treatment of bronchial asthma. The average price is 95–140 rubles.
- Teopek. Anti-asthmatic drug based on theophylline. Pills are taken for bronchial asthma, emphysema, obstructive bronchitis.
Contraindications include childhood up to 14 years, pregnancy, period breastfeeding, convulsive states, acute myocardial infarction, hyperfunction thyroid gland. The average price is 45–60 rubles.
Belarusian generics
The table brings together modern Belarusian generics of the singular. Antiasthmatic drugs are not its exact analogues, but are characterized by similar indications for use.
| Name of the drug | Average price in rubles | Characteristic |
| Eufillin | 15–35 | A bronchodilator that relaxes the muscles of the bronchi. The medicine effectively relieves bronchospasms. The indications for the medicine include bronchial asthma, obstructive bronchitis, Pickwick's syndrome, and chronic cor pulmonale. |
| Beclomethasone | 330–380 | An antiasthmatic drug used in the treatment of bronchial asthma for adults and children over 6 years of age. Release form: aerosol for inhalation. |
| Seleflu | 330–400 | Aerosol is used in therapeutic treatment mild, moderate and severe asthma. Not intended to relieve acute symptoms asthma. |
Other foreign analogues
Imported synonyms for singular will help you choose what to replace singular with. The list is given below.
- Single. The best substitute for singular with the same principle of action and active ingredient. The product has similar indications for use. Country of origin: Hungary. The average price is 440–870 rubles.
- Montelar. The drug is produced in Switzerland, Turkey, Slovenia. The active ingredient is montelukast. The average price is 440–1050 rubles.
- Montclair. The release form of the medication is chewable tablets. Country of origin: Croatia. The average price is 240–440 rubles.
- Almont. Used for asthma and allergic rhinitis. The medicine is produced in Switzerland. The average price is 700–960 rubles.
- Montelast. A close substitute for singular with a similar active substance. Sold in tablets. The product is produced in Switzerland and Malta. The average price is 640–2600 rubles.
Singulair and its analogues are popular medicines in the treatment of diseases specified in the instructions.
Allergic rhinitis, like bronchial asthma, are serious diseases that, in extreme cases, can lead to conditions incompatible with life, so they cannot be ignored. Montelukast is an effective substance that can not only treat, but also prevent dangerous symptoms.
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Singulair (montelukast sodium) is an anti-asthmatic drug, a leukotriene receptor antagonist. Used in pediatric practice for patients over six years of age. Taken orally once daily before going to bed. It is recommended to chew the tablet. Controlled multicenter randomized clinical studies have shown that Singulair relieves daytime and nighttime symptoms of bronchial asthma, improves the functional characteristics of the respiratory tract, reduces the number of acute episodes, reduces the consumption of bronchodilators, and reduces hypersensitivity bronchial tree, incl. during physical work, it is effective in patients with individual intolerance to acetylsalicylic acid. Taking the drug for two months improves external respiration parameters: respiratory rate, minute volume of breathing, pulmonary volume. For acute attacks of bronchial asthma, montelukast is not used. The drug is indicated for the treatment of patients with mild to moderate bronchial asthma. During the studies, it was found that with the same duration of pharmacotherapy (30 days), patients taking Singulair had attacks less frequently than those treated with Intal. A significant clinical effect of taking Singulair is a significant reduction in the incidence of allergic reactions (skin rashes, rhinoconjunctivitis).
Given the chronic nature of bronchial asthma, the duration of the drug course depends on the course of the disease. In some cases, continuous use of the drug is indicated. Singulair combines well with other preventive medications. The drug prevents constriction of the bronchi in response to provoking factors (physical work, allergens), and potentiates the bronchodilator effect of salbutamol. After oral administration, the drug is quickly and completely absorbed in the digestive tract. The presence of undigested food does not affect the bioavailability of montelukast. In patients over 2 years of age, after taking the drug on an empty stomach, the peak concentration of the active component in the blood is observed after 2 hours. The pharmacokinetic characteristics of Singulair do not change depending on the time of administration (morning, evening). Considering the fact that the drug is not indicated for the relief of acute attacks of bronchial asthma, patients should be warned about the need to have medications with them for emergency assistance(beta-2 agonists in spray form). During an exacerbation of the disease, Singulair is not stopped, combining it with inhaled beta-2 agonists. The amount of inhaled glucocorticosteroids taken together with Singulair can be progressively reduced under medical monitoring, however, abrupt discontinuation of their use and complete replacement with Singulair is not recommended.
Pharmacology
Leukotriene receptor antagonist. Cysteinyl leukotrienes LTC 4, LTD 4, LTE 4 are strong mediators of inflammation - eicosanoids that are released different cells, incl. mast cells and eosinophils. These important proasthmatic mediators bind to cysteinyl leukotriene receptors. Cysteinyl leukotriene receptors type I (CysLT 1 receptors) are present in respiratory tract humans (including in bronchial smooth muscle cells, macrophages) and other proinflammatory cells (including eosinophils and some myeloid stem cells). Cysteinyl leukotrienes correlate with the pathophysiology of bronchial asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchospasm, increased mucus secretion, increased vascular permeability, and increased eosinophil counts. In allergic rhinitis, after exposure to an allergen, cysteinyl leukotrienes are released from proinflammatory cells of the nasal mucosa during the early and late phases allergic reaction, which manifests itself as symptoms of allergic rhinitis. An intranasal test with cysteinyl leukotrienes demonstrated an increase in the resistance of the nasal airways and a symptom of nasal obstruction.
Montelukast is a highly active drug when taken orally that significantly improves inflammation in bronchial asthma. According to biochemical and pharmacological analysis, montelukast binds with high affinity and selectivity to CysLT 1 receptors, without interacting with other pharmacologically important receptors in the respiratory tract (such as prostaglandin receptors, cholinergic or β-adrenergic receptors). Montelukast inhibits the physiological effect of cysteinyl leukotrienes LTC 4, LTD 4, LTE 4 by binding to CysLT 1 receptors without having a stimulating effect on these receptors.
Montelukast inhibits CysLT receptors in the airways, as demonstrated by its ability to block the development of bronchospasm in response to inhaled LTD 4 in patients with asthma. A dose of 5 mg is sufficient to relieve bronchospasm induced by LTD 4 .
Montelukast causes bronchodilation within 2 hours after oral administration and may complement bronchodilation caused by β2-agonists.
The use of montelukast in doses of more than 10 mg/day once does not increase the effectiveness of the drug.
Pharmacokinetics
Suction
After oral administration, montelukast is rapidly and almost completely absorbed. Eating regular food does not affect plasma Cmax or the bioavailability of chewable tablets. In children aged 2 to 5 years, after taking chewable tablets on an empty stomach, 4 mg Cmax is achieved after 2 hours.
The pharmacokinetics of montelukast remains almost linear when administered orally in doses greater than 50 mg.
Distribution
The binding of montelukast to plasma proteins is more than 99%. V d in the equilibrium state is 8-11 liters.
Studies conducted in rats with radiolabeled montelukast indicate minimal penetration of the BBB. In addition, the concentration of labeled montelukast 24 hours after administration was minimal in all other tissues.
When taking montelukast at a dose of 10 mg 1 time/day, a moderate (about 14%) accumulation of the active substance in plasma is observed.
Metabolism
Montelukast is extensively metabolized. When used in therapeutic doses, the concentration of montelukast metabolites in plasma at steady state in adults and children is not determined.
In vitro studies using human liver microsomes have shown that isoenzymes of the cytochrome P450 system: CYP3A4, 2C8 and 2C9 are involved in the metabolism of montelukast. According to the results of studies conducted in vitro on human liver microsomes, montelukast at therapeutic concentrations in blood plasma does not inhibit the isoenzymes CYP3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Removal
T1/2 of montelukast in young healthy adults ranges from 2.7 to 5.5 hours. Plasma clearance of montelukast in healthy adults averages 45 ml/min. Following oral administration of radiolabeled montelukast, 86% is excreted in feces within 5 days and less than 0.2% is excreted in urine, confirming that montelukast and its metabolites are excreted almost exclusively in bile.
Pharmacokinetics in special clinical situations
When taking montelukast in the morning and evening hours, no differences in pharmacokinetics were observed.
The pharmacokinetics of montelukast are similar in women and men.
With a single oral dose of 10 mg of montelukast, the pharmacokinetic profile and bioavailability are similar in elderly and young patients. In elderly people, T1/2 of montelukast from plasma is slightly longer. No dose adjustment is required in elderly patients.
There were no differences in clinically significant pharmacokinetic effects in patients of different races.
In patients with mild to moderate liver failure and clinical manifestations liver cirrhosis, a slowdown in the metabolism of montelukast was observed, accompanied by an increase in AUC by approximately 41% after a single dose of 10 mg. The excretion of montelukast in these patients is slightly increased compared to healthy subjects (average T1/2 - 7.4 hours). No dose adjustment of montelukast is required for patients with mild to moderate hepatic impairment. Data on the nature of the pharmacokinetics of montelukast in patients with severe liver failure (more than 9 points on the Child-Pugh scale).
Release form
Chewable tablets are pink, oval, biconvex, embossed with the inscription "SINGULAIR" on one side and "MSD 711" on the other.
Excipients: mannitol - 161.08 mg, microcrystalline cellulose - 52.8 mg, hyprolose (hydroxypropylcellulose) - 7.2 mg, red iron oxide - 360 mcg, croscarmellose sodium - 7.2 mg, cherry flavor - 3.6 mg, aspartame - 1.2 mg, magnesium stearate - 2.4 mg.
7 pcs. - blisters (1) - cardboard packs.
7 pcs. - blisters (2) - cardboard packs.
7 pcs. - blisters (4) - cardboard packs.
Dosage
The drug is taken orally 1 time/day, regardless of meals.
For bronchial asthma, 4 mg (1 tablet) is prescribed at night.
For bronchial asthma and allergic rhinitis, 4 mg (1 tablet) is prescribed at night.
For allergic rhinitis, 4 mg (1 tablet)/day is prescribed individually, depending on the time of greatest exacerbation of symptoms.
For children, elderly patients, patients with renal failure and patients with mild/moderate liver dysfunction, no special dose selection is required.
Overdose
Symptoms of overdose were not identified during clinical studies of long-term (22 weeks) treatment with Singulair ® in adult patients with bronchial asthma in doses up to 200 mg/day, or during short (about 1 week) clinical studies when taking the drug in doses up to 900 mg/day. days
There have been cases of acute overdose of Singulair ® (taking at least 1000 mg/day) in the post-registration period and during clinical trials in adults and children. Clinical and laboratory data indicated comparable safety profiles of Singulair ® in children, adults and elderly patients. The most common symptoms were thirst, drowsiness, vomiting, psychomotor agitation, headache and abdominal pain. Data side effects are consistent with the safety profile of the drug Singulair ® .
Treatment: symptomatic therapy. There is no specific information on the treatment of overdose of Singulair ®. There are no data on the effectiveness of peritoneal dialysis or hemodialysis with montelukast.
Interaction
Singulair ® 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. Montelukast at the recommended therapeutic dose did not have a clinically significant effect on pharmacokinetics the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.
When taking phenobarbital concomitantly, the AUC value of montelukast is reduced by approximately 40%, but this does not require changes in the dosage regimen of Singulair ®.
In vitro studies have shown that montelukast inhibits the CYP2C8 isoenzyme. However, when researching drug interactions in vivo, montelukast and rosiglitazone (metabolized with the participation of the CYP2C8 isoenzyme) have not received confirmation of inhibition of the CYP2C8 isoenzyme by montelukast. Therefore, in clinical practice, the effect of montelukast on CYP2C8-mediated metabolism of a number of drugs is not expected. medicines, incl. paclitaxel, rosiglitazone, repaglinide.
In vitro studies have shown that montelukast is a substrate of the CYP2C8, 2C9 and 3A4 isoenzymes. Data from a clinical drug interaction study of montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times. Coadministration of itraconazole, a strong CYP3A4 inhibitor, with gemfibrozil and montelukast did not result in an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic exposure of montelukast may not be considered clinically significant based on safety data when used at doses greater than the approved dose of 10 mg in adult patients (eg, 200 mg/day for adult patients for 22 weeks and up to 900 mg/day for no clinically significant adverse effects were observed in patients taking the drug for approximately one week). Thus, when co-administered with gemfibrozil, no dose adjustment of montelukast is required. Based on the results of in vitro studies, no clinically significant drug interactions are expected with other known CYP2C8 inhibitors (for example, with trimethoprim). In addition, coadministration of montelukast with itraconazole alone did not significantly increase the effect of systemic exposure to montelukast.
Combination treatment with bronchodilators
Singulair ® is a reasonable addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. Once the therapeutic effect of treatment with Singulair ® is achieved, a gradual reduction in the dose of bronchodilators can begin.
Combined treatment with inhaled corticosteroids
Treatment with Singulair ® provides an additional therapeutic effect in patients using inhaled GCS. Once the condition has stabilized, you can begin a gradual reduction in the dose of GCS under the supervision of a physician. In some cases, complete abolition of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Singulair ® is not recommended.
Side effects
Children aged 2 to 5 years with bronchial asthma
Clinical studies of the drug Singulair ® involved 573 patients aged 2 to 5 years. In a 12-week placebo-controlled clinical trial, the only adverse event (AE) assessed as drug-related that occurred in >1% of patients treated with Singulair ® and more frequently than in the placebo group was thirst. The differences in the incidence of this AE between the two treatment groups were not statistically significant.
In total, in the studies, 426 patients aged 2 to 5 years were treated with Singulair® for at least 3 months, 230 for 6 months or more, and 63 patients for 12 months or more. With longer treatment, the AE profile did not change.
Children aged 2 to 14 years with seasonal allergic rhinitis
A 2-week, placebo-controlled clinical trial using Singulair ® for the treatment of seasonal allergic rhinitis included 280 patients aged 2 to 14 years. Patients took Singulair ® 1 time/day in the evening and was generally well tolerated. The safety profile of the drug in children was similar to that of placebo. In this clinical study, there were no AEs that were considered drug-related, occurred in ≥1% of patients taking Singulair, or more frequently than in the placebo group.
Children aged 6 to 14 years with bronchial asthma
The safety profile of the drug in children was generally similar to the safety profile in adults and comparable to the safety profile of placebo.
In an 8-week placebo-controlled clinical trial, the only AE assessed as drug-related occurring in >1% of patients treated with Singulair ® and more frequently than in the placebo group was headache. The difference in frequency between the two treatment groups was not statistically significant.
In growth rate studies, the safety profile in patients in this age group was consistent with the previously described safety profile of Singulair ® .
With longer treatment (more than 6 months), the AE profile did not change.
Adults and children aged 15 years and older with asthma
In two 12-week placebo-controlled clinical studies with a similar design, the only AEs assessed as drug-related that occurred in ≥1% of patients taking Singulair ® and more frequently than in the placebo group were abdominal pain and headache. The differences in the incidence of these AEs between the two treatment groups were not statistically significant. With longer treatment (for 2 years), the AE profile did not change.
Adults and children aged 15 years and older with seasonal allergic rhinitis
Patients took Singulair ® 1 time per day in the morning or evening; the drug was generally well tolerated, and the safety profile of the drug was similar to the safety profile of placebo. In placebo-controlled clinical trials, there were no AEs that were considered drug-related, occurring in ≥1% of patients taking Singulair, or more frequently than in the placebo group. In the 4-week placebo-controlled clinical study, the safety profile of the drug was similar to that in the 2-week studies. The incidence of drowsiness when taking the drug in all studies was the same as when taking placebo.
Adults and children aged 15 years and older with year-round allergic rhinitis
Patients took Singulair ® 1 time/day in the morning or evening; overall, the drug was well tolerated. The drug's safety profile was similar to that observed in patients with seasonal allergic rhinitis and placebo. In these clinical studies, there were no AEs that were considered drug-related, occurring in ≥1% of patients taking Singulair, or more frequently than in the placebo group. The incidence of drowsiness while taking the drug was the same as when taking placebo.
Generalized analysis of clinical trial results
A pooled analysis was conducted of 41 placebo-controlled clinical trials (35 studies involving patients aged 15 years or older, 6 studies involving patients aged 6 to 14 years) using validated methods for assessing suicidality. Among the 9929 patients receiving Singulair ® and the 7780 patients receiving placebo in these studies, 1 patient was identified as suicidal in the Singulair ® group. There were no suicides, suicide attempts, or other preparatory acts indicative of suicidal behavior in any of the treatment groups.
Separately, a pooled analysis of 46 placebo-controlled clinical trials (35 studies in patients aged 15 years and older; 11 studies in patients aged 3 months to 14 years) was conducted to assess adverse behavioral effects. Among the 11,673 patients treated with Singulair ® in these studies and the 8,827 patients treated with placebo, the percentage of patients experiencing at least one adverse behavioral effect was 2.73% among patients treated with Singulair ® and 2.27% among patients treated with placebo; the odds ratio was 1.12 (95% confidence interval).
AEs registered during post-registration use of the drug
From the blood coagulation system: increased tendency to bleeding.
From the outside immune system: hypersensitivity reactions, incl. anaphylaxis; very rarely (<1/10 000) - эозинофильная инфильтрация печени.
From the psyche: agitation (including aggressive behavior or hostility), anxiety, depression, disorientation, impaired attention, pathological dreams, hallucinations, insomnia, memory impairment, psychomotor activity (including irritability, restlessness and tremor), somnambulism, suicidal thoughts thoughts and behavior (suicidality).
From the nervous system: dizziness, drowsiness, paresthesia/hypesthesia; very rarely (<1/10 000) - судороги.
From the cardiovascular system: rapid heartbeat.
From the respiratory system: nosebleeds, pulmonary eosinophilia.
From the digestive system: diarrhea, dyspepsia, nausea, vomiting, pancreatitis.
From the liver and biliary tract: increased activity of ALT and AST in the blood; very rarely (<1/10 000) - гепатит (включая холестатические, гепатоцеллюлярные и смешанные поражения печени).
From the skin and subcutaneous tissues: tendency to form hematomas, erythema nodosum, erythema multiforme, itching, rash.
Allergic reactions: angioedema, urticaria.
From the musculoskeletal system: arthralgia, myalgia, including muscle cramps.
From the urinary system: enuresis in children.
General reactions: asthenia (weakness)/fatigue, edema, pyrexia.
In general, the drug Singulair ® is well tolerated by patients. Side effects are usually mild and, as a rule, do not require discontinuation of the drug. The overall frequency of side effects when treated with Singulair ® is comparable to their frequency when taking placebo.
Indications
- prevention and long-term treatment of bronchial asthma in children aged 2 years and older: to control daytime and nighttime symptoms of the disease;
- relief of symptoms of allergic rhinitis in children aged 2 years and older.
Contraindications
- children under 2 years of age;
- phenylketonuria;
- hypersensitivity to the components of the drug.
Features of application
Use during pregnancy and breastfeeding
Clinical studies of the drug Singulair ® have not been conducted in pregnant women. Singulair ® should be used during pregnancy and breastfeeding only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
During post-registration use of the drug Singulair ®, the development of congenital limb defects was reported in newborns whose mothers took Singulair ® during pregnancy. Most of these women also took other medications to treat asthma during pregnancy. A cause-and-effect relationship between taking Singulair ® and the development of congenital limb defects has not been established.
It is not known whether montelukast is excreted in breast milk. Since many drugs are excreted in breast milk, this must be taken into account when prescribing Singulair ® to breastfeeding mothers.
Use for liver dysfunction
For patients with mild or moderate liver dysfunction, no special dose selection is required.
There are no data on the nature of the pharmacokinetics of montelukast in patients with severe liver failure (more than 9 points on the Child-Pugh scale).
Use for renal impairment
For patients with renal failure, no special dose selection is required.Use in children
For children aged 2 to 5 years with bronchial asthma and/or allergic rhinitis, the dose is 4 mg (1 tablet)/day.
Contraindicated: children under 2 years of age.
special instructions
The effectiveness of oral Singulair ® for the treatment of acute attacks of bronchial asthma has not been established. Therefore, Singulair ® tablets are not recommended for the treatment of acute attacks of bronchial asthma. Patients should be instructed to always carry emergency medications to relieve asthma attacks (short-acting inhaled beta 2 agonists).
You should not stop taking Singulair ® during an exacerbation of asthma and the need to use emergency medications (short-acting inhaled beta 2 agonists) to relieve attacks.
Patients with a confirmed allergy to acetylsalicylic acid and other NSAIDs should not take these drugs during treatment with Singulair ®, since Singulair ®, while improving respiratory function in patients with allergic bronchial asthma, however, cannot completely prevent bronchoconstriction caused by NSAIDs.
The dose of inhaled corticosteroids used simultaneously with the drug Singulair ® can be gradually reduced under the supervision of a physician, however, an abrupt replacement of inhaled or oral corticosteroids with the drug Singulair ® cannot be carried out.
Neuropsychiatric disorders have been described in patients taking Singulair ® . Given that these symptoms could be caused by other factors, it is unknown whether they are related to the use of Singulair ® . Physicians should discuss these side effects with patients and/or their parents/guardians. Patients and/or their caregivers should be advised that if such symptoms occur, they should notify their 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 more of the following reactions: eosinophilia, rash, worsening of pulmonary symptoms, cardiac complications and/or neuropathy, sometimes diagnosed as Churg-Strauss syndrome, systemic eosinophilic vasculitis. Although the cause-and-effect relationship of these adverse reactions with therapy with leukotriene receptor antagonists has not been established, when reducing the dose of systemic corticosteroids in patients receiving Singulair ® , caution and appropriate clinical monitoring must be performed.
Chewable tablets 4 mg contain aspartame, a source of phenylalanine. Patients with phenylketonuria should be informed that each 4 mg chewable tablet contains aspartame equivalent to 0.674 mg phenylalanine. Singulair ® in the form of 4 mg chewable tablets is not recommended for use in patients with phenylketonuria.
Impact on the ability to drive vehicles and operate machinery
This section does not apply to the drug Singulair ® chewable tablets 4 mg, since it is intended for the treatment
children from 2 to 5 years old. Thus, the information presented below relates to the active substance of the drug montelukast.
Taking Singulair ® is not expected to affect the ability to drive or drive.
mechanisms. However, individual reactions to the drug may vary. Some side effects
(such as dizziness and drowsiness), which have been reported to occur very rarely with the use of the drug
Singulair ® may affect the ability of some patients to drive vehicles and operate machinery.
This page provides a list of all Singulair analogues by composition and indication for use. A list of cheap analogues, and you can also compare prices in pharmacies.
- The cheapest analogue of Singulair:
- The most popular analogue of Singulair:
- ATX classification: Montelukast
- Active ingredients/composition: montelukast
Cheap analogues of Singulair
When calculating the cost cheap analogs of Singulair the minimum price was taken into account, which was found in the price lists provided by pharmacies
Popular analogues of Singulair
The list of drug analogues based on statistics of the most requested drugs
All analogues of Singulair
Analogues in composition and indications for use
| Name | Price in Russia | Price in Ukraine |
|---|---|---|
| montelukast | -- | 284 UAH |
| -- | 66 UAH | |
| montelukast | -- | 152 UAH |
| montelukast | 299 RUR | 108 UAH |
| montelukast | -- | -- |
| montelukast | -- | 33 UAH |
| montelukast | -- | -- |
| montelukast | -- | 76 UAH |
| 1832 RUR | 700 UAH | |
| 284 RUR | 26 UAH | |
| -- | -- | |
| montelukast | 157 RUR | 750 UAH |
| montelukast sodium | 239 RUR | 412 UAH |
| montelukast sodium | -- | 103 UAH |
| montelukast | -- | 221 UAH |
| montelukast | 500 rub | 750 UAH |
The above list of drug analogues, which indicates substitutes Singulair, is the most suitable because they have the same composition of active ingredients and coincide in indications for use
Different composition, may have the same indication and method of use
| Name | Price in Russia | Price in Ukraine |
|---|---|---|
| theophylline | 9 RUR | 3 UAH |
| theophylline | -- | 13 UAH |
| theophylline | 124 rub. | 21 UAH |
| theophylline | 114 rub. | 28 UAH |
| theophylline | -- | 22 UAH |
| theophylline | -- | 24 UAH |
| theophylline | -- | 3 UAH |
| theophylline | 245 rub. | 39 UAH |
| -- | 117 UAH | |
| theophylline, potassium chloride, magnesium chloride | -- | 21 UAH |
| theophylline, guaifenesin | -- | -- |
| Belladonna, caffeine, paracetamol, theophylline, phenobarbital, cytisine, ephedrine | -- | 32 UAH |
| theophylline, phenobarbital, ephedrine | -- | -- |
| fenspiride | -- | 21 UAH |
| fenspiride | 218 RUR | 65 UAH |
| fenspiride | -- | 32 UAH |
| fenspiride | -- | 57 UAH |
| fenspiride | -- | 15 UAH |
| fenspiride hydrochloride | 147 RUR | -- |
| fenspiride hydrochloride | 158 RUR | -- |
| fenspiride hydrochloride | 146 RUR | 225 UAH |
| fenspiride hydrochloride | 150 rub. | -- |
| fenspiride hydrochloride | -- | -- |
| fenspiride | -- | 36 UAH |
| omalizumab | 17800 rub. | 6500 UAH |
| roflumilast | 1890 RUR | 480 UAH |
| 1480 RUR | 55 UAH |
To compile a list of cheap analogues of expensive drugs, we use prices that are provided to us by more than 10,000 pharmacies throughout Russia. The database of drugs and their analogues is updated daily, so the information provided on our website is always up to date as of the current day. If you have not found the analogue you are interested in, please use the search above and select the medicine you are interested in from the list. On the page of each of them you will find all possible analogues of the drug you are looking for, as well as prices and addresses of pharmacies where it is available.
How to find a cheap analogue of an expensive medicine?
To find an inexpensive analogue of a medicine, a generic or a synonym, first of all we recommend paying attention to the composition, namely the same active ingredients and indications for use. The same active ingredients of a drug will indicate that the drug is a synonym for the drug, pharmaceutically equivalent or a pharmaceutical alternative. However, we should not forget about the inactive components of similar drugs, which may affect safety and effectiveness. Do not forget about the instructions of doctors; self-medication can harm your health, so always consult a doctor before using any medication.Singular price
Use the websites below to find prices for Singulair and find out availability at your local pharmacy.Singular instructions
Release form
Film-coated tablets.
Chewable tablets.
Compound
- 1 film-coated tablet contains:
- Active substance: montelukast - 10 mg;
- Excipients: microcrystalline cellulose, lactose, croscarmellose sodium, hyprolose, magnesium stearate.
- The composition of the coating covering the tablet: hyprolose, hypromellose, titanium dioxide, dyes iron oxide red and iron oxide yellow and carnauba wax.
- 1 chewable tablet contains:
- Active substance: montelukast - 5 mg;
- Excipients: mannitol, microcrystalline cellulose, hyprolose, red iron oxide dye, croscarmellose sodium, cherry flavor, aspartame and magnesium stearate.
pharmachologic effect
Pharmacotherapeutic group: Leukotriene receptor blocker.
ATX code: R03DC03
Pharmacological properties:
Pharmacodynamics
Montelukast inhibits cysteinyl leukotriene receptors of the airway epithelium, thereby simultaneously having the ability to inhibit bronchospasm caused by inhaled cysteinyl leukotriene LTD4 in patients with bronchial asthma. A dose of 5 mg is sufficient to relieve bronchospasm induced by LTD4. The use of montelukast in doses exceeding 10 mg per day, taken once, does not increase the effectiveness of the drug.
Montelukast causes bronchodilation within 2 hours after oral administration; and may complement bronchodilation caused by β2-adrenergic agonists.
Pharmacokinetics
Suction
Montelukast is rapidly and almost completely absorbed after oral administration. Eating normal food does not affect the bioavailability and maximum plasma concentration (Cmax) of film-coated tablets and chewable tablets. In adults, when taking 10 mg film-coated tablets on an empty stomach, Cmax is achieved after 3 hours. Bioavailability when taken orally is 64%.
When taking 5 mg chewable tablets on an empty stomach, Cmax in adults is achieved after 2 hours. Bioavailability is 73%.
Distribution
Montelukast is more than 99% bound to plasma proteins. The volume of distribution of montelukast averages 8-11 liters.
Metabolism
Montelukast is actively metabolized in the liver. When using therapeutic doses, the concentration of montelukast metabolites in plasma at steady state in adults and children is not determined.
It is assumed that the cytochrome P450 CYP isoenzymes (3A4 and 2C9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit the cytochrome P450 CYP isoenzymes: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Removal
The clearance of montelukast averages 45 ml/min in healthy adults. After oral administration of montelukast, 86% of its amount is excreted in the feces within 5 days and less than 0.2% in the urine, confirming that montelukast and its metabolites are excreted almost exclusively in bile.
The half-life of montelukast in young healthy adults ranges from 2.7 to 5.5 hours. The pharmacokinetics of montelukast remains almost linear when administered orally at doses above 50 mg. When taking montelukast in the morning and evening hours, no differences in pharmacokinetics were observed. When taking 10 mg film-coated tablets once a day, a moderate (about 14%) cumulation of the active substance in plasma is observed.
Features of pharmacokinetics in different groups of patients
The pharmacokinetics of montelukast are similar in women and men.
Elderly patients
When administered orally once daily as 10 mg film-coated tablets, the pharmacokinetic profile and bioavailability are similar in elderly and young patients.
Liver failure
In patients with mild to moderate hepatic impairment and clinical manifestations of cirrhosis, a slowdown in the metabolism of montelukast was observed, accompanied by an increase in the area under the concentration-time pharmacokinetic curve (AUC) by approximately 41% after a single dose of 10 mg. The elimination of montelukast in these patients is slightly increased compared to healthy subjects (average half-life of 7.4 hours). No dose adjustment of montelukast is required for patients with mild to moderate hepatic impairment. There are no data on the nature of the pharmacokinetics of montelukast in patients with severe liver failure (more than 9 points on the Child-Pugh scale).
There were no differences in clinically significant pharmacokinetic effects in patients of different races.
Kidney failure
Because montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal impairment have not been evaluated. No dose adjustment is required for this group of patients.
Singulair, indications for use
- Prevention and long-term treatment of bronchial asthma in adults and children from 6 years of age, including prevention of daytime and nighttime symptoms of the disease, treatment of aspirin-sensitive patients with bronchial asthma and prevention of exercise-induced bronchospasm.
- Relief of daytime and nighttime symptoms of seasonal allergic rhinitis (in adults and children over 6 years of age) and persistent allergic rhinitis (in adults and children over 6 years of age)
Contraindications
- Hypersensitivity to any of the components of the drug.
- Children's age up to 6 years.
Directions for use and doses
Orally 1 time per day, regardless of meals. To treat bronchial asthma, Singulair should be taken in the evening. When treating allergic rhinitis, the dose can be taken at any time of the day at the request of the patient. Patients suffering from bronchial asthma and allergic rhinitis should take one Singulair tablet once a day in the evening.
Adults aged 15 years and older
The dose for adults and children over 15 years of age is one 10 mg film-coated tablet per day.
Children aged 6 to 14 years
The dosage for children 6-14 years old is one chewable tablet 5 mg per day. No dosage adjustment is required for this age group.
The therapeutic effect of SINGULAR on indicators reflecting the course of bronchial asthma develops during the first day. The patient should continue to take SINGULAR both during the period of achieving control over the symptoms of bronchial asthma, and during periods of exacerbation of bronchial asthma.
For elderly patients, patients with renal failure, as well as patients with mild or moderate liver dysfunction, as well as depending on gender, no special dose selection is required.
Prescribing SINGULAR simultaneously with other types of treatment for bronchial asthma
SINGULAR can be added to the patient's treatment with bronchodilators and inhaled glucocorticosteroids (See Section "Interaction with other drugs").
Use during pregnancy and breastfeeding
Singulair should be used during pregnancy and lactation only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
Side effects
In general, SINGULAR is well tolerated. Side effects are usually mild and usually do not require discontinuation of treatment. The overall incidence of side effects reported with SINGULAR is comparable to that for placebo:
hypersensitivity reactions (including anaphylaxis, angioedema, rash, itching, urticaria and very rarely eosinophilic liver infiltrates); erythema nodosum, unusual vivid dreams; hallucinations; drowsiness; irritability; agitation, including aggressive behavior; fatigue; suicidal thoughts and suicidal behavior (suicidality); insomnia; paresthesia/hypesthesia and very rarely – seizures; nausea, vomiting, diarrhea, abdominal pain; headache; arthralgia; myalgia; muscle cramps; tendency to increased bleeding, the formation of subcutaneous hemorrhages; heartbeat; swelling.
special instructions
SINGULAR tablets are not recommended for the treatment of acute attacks of bronchial asthma. In acute cases of bronchial asthma, patients should be prescribed medications to relieve and prevent asthma attacks.
The dose of inhaled glucocorticosteroids used simultaneously with SINGULAR can be gradually reduced under the supervision of a physician. SINGULAR cannot be used as a substitute for inhaled or oral glucocorticosteroids.
Reducing the systemic dose of glucocorticosteroids in patients receiving antiasthmatic drugs, including leukotriene receptor blockers, was accompanied in rare cases by the appearance of one or more of the following phenomena: eosinophilia, vascular rash, worsening of pulmonary symptoms, cardiac complications and/or neuropathy, sometimes diagnosed as Charg syndrome - Ostrich – systemic eosinophilic vasculitis. Although a cause-and-effect relationship between these adverse events and leukotriene receptor antagonist therapy has not been established, caution and appropriate clinical monitoring should be used when reducing the systemic dose of glucocorticosteroids in patients taking SINGULAR.
Use in elderly patients
There were no age-related differences in the efficacy and safety profiles of SINGULAR.
Impact on the ability to drive a car or move machinery.
There is no evidence that taking SINGULAR affects the ability to drive a car or drive machinery.
Drug interactions
Singulair can be prescribed together with other drugs that are usually used for the prevention and long-term treatment of bronchial asthma and/or the 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/norethinodrel 35/1), terfenadine, digoxin and warfarin.
The AUC value of montelukast is reduced by simultaneous administration of phenobarbital by approximately 40%, which does not require changes in the dosing regimen of Singulair.
In vitro studies have shown that montelukast inhibits the cytochrome CYP2C8 isoenzyme system. However, when studying the drug-drug interaction in vivo of montelukast and rosiglitazone (metabolized with the participation of the CYP 2C8 isoenzyme of the cytochrome system), there was no confirmation of inhibition of the CYP 2C8 isoenzyme by montelukast. Thus, in clinical practice, the effect of montelukast on the CYP 2C8-mediated metabolism of a number of drugs, including paclitaxel, rosiglitazone, repaglinide, etc., is not expected.
Combination treatment with bronchodilators: Singulair is a reasonable addition to bronchodilator monotherapy if the latter do not provide adequate control of bronchial asthma. Once a therapeutic effect has been achieved (usually after the first dose) from treatment with Singulair, a gradual reduction in the dose of bronchodilators can begin.
Combined treatment with inhaled glucocorticosteroids: Treatment with Singulair provides an additional therapeutic effect for patients using inhaled glucocorticosteroids. Once stabilization is achieved, you can begin to reduce the dose of the corticosteroid - gradually and under the supervision of a physician. In some cases, complete withdrawal of inhaled glucocorticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Singulair is not recommended.
Overdose
Symptoms: symptoms of overdose of Singulair 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.
There are reports of acute overdose of montelukast in children (at a dose of at least 150 mg/day). Clinical and laboratory data indicate that the safety profile of Singulair in children corresponds to the safety profile in adults and elderly patients. The most common adverse events were thirst, drowsiness, mydriasis, hyperkinesis and abdominal pain.
Treatment: symptomatic therapy.
There are no data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis.
Storage conditions
List B.
At a temperature not exceeding 30°C, protected from moisture and light and out of the reach of children.
Best before date
The shelf life for 5 mg chewable tablets is 2 years.
The shelf life for 10 mg film-coated tablets is 3 years.
Do not use after the expiration date indicated on the package.
All information is presented for informational purposes and is not a reason for independent prescription or replacement of medication.Many people suffering from bronchial asthma or seasonal rhinitis are familiar with the drug Singulair firsthand. This is a truly effective medicine. It contains montelukast, a substance that quickly relieves spasms in the bronchi and eliminates swelling of the nasal mucosa. However, not all patients can use it due to its high price. Pharmacies sell cheaper, but equally effective analogues that have the same active ingredient.
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Description of the drug
Medicines with the main active ingredient - montelukast - can relieve spasms. This substance inhibits bronchoconstriction processes. One of the most famous drugs based on it is Singulair. It suppresses bronchospasms at any stage and eliminates swelling of the mucous membranes in allergic rhinitis. Even a small dose of the product is effective.
After taking the drug, the lumen in the bronchi expands.
The medicine is produced in Italy. Release form: chewable tablets. It belongs to anti-asthmatic drugs: it prevents and relieves spasms that occur in the bronchi when inhaling LTD4 - cysteinyl leukotriene.
Singulair is prescribed for both therapy and prevention for patients suffering from asthma. The main directions of action of the drug:
- treatment of patients with hypersensitivity to acetylsalicylic acid;
- prevention of spasm during physical activity;
- preventing the manifestation of daytime or nighttime symptoms of the disease.
Seasonal rhinitis is also an indication for the use of the medication.
The effect of taking Singulair is visible already on the first day of its use. The drug can be used simultaneously with other drugs that dilate the bronchi.
Despite all the obvious advantages, the product also has a significant drawback - its high price. For a pack of 14 tablets you will have to pay about 1000 rubles. The cost of tablets containing 10, 5 or 4 mg is practically the same. That is why many people think about analogues of this drug.
Analogues
Today, pharmacies offer several drugs with similar active ingredients. The difference between them is small, but with almost the same effect they are several times cheaper.
Substitutes for Singulair include: Montelar, Singlon, Ektalust, Montelast.
Single
The effect of using this medicine appears already on the first day of use. It is recommended to use the drug both during exacerbation of the disease and during remission.
Singlen is used for the treatment of bronchial asthma.
This drug has a number of side effects, including suicidal thoughts and actions.
Detailed characteristics are presented in the table:
Parameter Description Manufacturer
Release form
Tablets 10 mg (pack of 14, 28 or 56 pieces)
Reception features
In exceptional cases, children 6-14 years old are allowed to take 5 mg per day. Adolescents over 15 years of age and adults are prescribed 10 mg per day, regardless of food intake.
Cannot be used with other drugs containing the same active ingredient. The dose is the same for both men and women
Contraindications
It is forbidden to use during pregnancy and lactation. The drug is not recommended for children under 15 years of age
Side effects
- Bleeding;
- headache;
- sleep problems;
- thirst;
- stomach ache;
- tremor;
- hyperactivity;
- vomit:
- suicidal behavior
Montelar
Effective in the treatment of bronchial asthma, as well as in the treatment of allergic rhinitis. Not suitable for relieving acute attacks.
Montelar can be taken together with inhaled corticosteroids and bronchodilators.
The medication has a large list of side effects, including mental disorders. The effect of use during pregnancy has not been studied, so expectant mothers should avoid taking this medication.
Ektalust
The drug is made in Russia. After administration, the maximum concentration of the drug in the blood is observed after 2 hours. The use of Ektalust enhances the effect of inhaled corticosteroids.
Used for long-term treatment and prevention of asthma. Effective in the treatment of asthma caused by intolerance to acetylsalicylic acid, and in relieving the symptoms of rhinitis of an allergic nature.
The use of this medicine is recommended for children under 15 years of age. Older patients should take other montelukast-based drugs.
In general, the medication is tolerated quite well. Side effects usually develop in a mild form. This is largely due to the reduced concentration of montelukast compared to other drugs.
Characteristic:
Parameter Description Manufacturer
Release form
Chewable tablets 5 mg (7, 14, 20 or 30 pieces per pack)
Reception features
Take 60 minutes before or 2 hours after meals once a day. The tablet must be chewed.
Dosage for children 2-5 years old – 4 mg once a day. For children 6-14 years old, use 5 mg once a day. When treating bronchial asthma, it is recommended to take it in the evening.
Contraindications
Do not take if you have phenylketonuria or hypersensitivity to the components of the drug.
The drug is prohibited for children under 2 years of age, as well as pregnant women.
Side effects
- Anxiety;
- depression;
- insomnia;
- otitis;
- upper respiratory tract infections;
- cardiopalmus
Montelast
It is used for the treatment of asthma and its prevention, helps relieve the symptoms of seasonal rhinitis. Ineffective for acute spasms.
After taking it, you should refrain from driving, as using the medicine reduces attention and reaction speed.
The description is presented in the table:
Parameter Characteristic Manufacturer
Release form
- Chewable tablets 5 mg (14, 28 pcs.).
- Film-coated tablets, 10 mg (28, 98 pcs.)
Reception features
Instructions for use: consume 1 hour before meals. The tablet must be chewed thoroughly.
Doses:
- children 2-6 years old – 4 mg 1 time per day – in the evening;
- children 6-14 years old – 5 mg 1 time per day, in the evening
Contraindications
- Lactase intolerance.
- Phenylketonuria.
Patients under 2 years of age should not be treated
Side effects
- Increased likelihood of bleeding;
- anaphylaxis;
- insomnia;
- pancreatitis;
- hives;
- muscle cramps
Conclusion
Each of the analogues of the drug Singulair has its own advantages and disadvantages:
- 1. The best in the price category is Ektalust. This is a domestically produced medicine.
- 2. For the relief of acute spasms in the bronchi, the most effective is Singlon, but it should not be given to children under 2 years of age.
- 3. Each of the drugs has a wide range of side effects.
- 4. All medications are prohibited during pregnancy and breastfeeding.
- 5. Montelast and Ektalust should not be taken if you have phenylketonuria or lactase intolerance.
The attending physician must prescribe the use of this or that medication. It is he who will select the most suitable drug in accordance with the characteristics of the patient.
Active substance
Montelukast
Release form, composition and packaging
Chewable tablets pink, oval, biconvex, embossed with "SINGULAIR" on one side and "MSD 711" on the other.
Excipients: mannitol - 161.08 mg, microcrystalline cellulose - 52.8 mg, hyprolose (hydroxypropylcellulose) - 7.2 mg, red iron oxide - 0.36 mg, croscarmellose sodium - 7.2 mg, cherry flavor - 3.6 mg, aspartame - 1.2 mg, magnesium stearate - 2.4 mg.
7 pcs. - blisters (1) - cardboard packs.
7 pcs. - blisters (2) - cardboard packs.
7 pcs. - blisters (4) - cardboard packs.
pharmachologic effect
Leukotriene receptor antagonist. Cysteinyl leukotrienes LTC 4, LTD 4, LTE 4 are strong mediators of inflammation - eicosanoids, which are secreted by various cells, including. mast cells and eosinophils. These important proasthmatic mediators bind to cysteinyl leukotriene receptors. Cysteinyl leukotriene receptors type I (CysLT 1 receptors) are present in the human respiratory tract (including bronchial smooth muscle cells, macrophages) and other inflammatory cells (including eosinophils and some myeloid stem cells). Cysteinyl leukotrienes correlate with the pathophysiology of bronchial asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchospasm, increased mucus secretion, increased vascular permeability, and increased eosinophil counts. In allergic rhinitis, following exposure, cysteinyl leukotrienes are released from proinflammatory cells in the nasal mucosa during the early and late phases of the allergic reaction, resulting in symptoms of allergic rhinitis. An intranasal test with cysteinyl leukotrienes demonstrated an increase in the resistance of the nasal airways and a symptom of nasal obstruction.
Montelukast is a highly active drug when taken orally that significantly improves inflammation in bronchial asthma. According to biochemical and pharmacological analysis, montelukast binds with high affinity and selectivity to CysLT 1 receptors, without interacting with other pharmacologically important receptors in the respiratory tract (such as prostaglandin receptors, cholinergic or β-adrenergic receptors). Montelukast inhibits the physiological effect of cysteinyl leukotrienes LTC 4, LTD 4, LTE 4 by binding to CysLT 1 receptors without having a stimulating effect on these receptors.
Montelukast inhibits CysLT receptors in the airways, as demonstrated by its ability to block the development of bronchospasm in response to inhaled LTD 4 in patients with asthma. A dose of 5 mg is sufficient to relieve bronchospasm induced by LTD 4 .
Montelukast causes bronchodilation within 2 hours after oral administration and may complement bronchodilation caused by β2-agonists.
The use of montelukast in doses of more than 10 mg/day once does not increase the effectiveness of the drug.
Pharmacokinetics
Suction
After oral administration, montelukast is rapidly and almost completely absorbed. Eating regular food does not affect Cmax in the blood and the bioavailability of chewable tablets. In children aged 2 to 5 years, after taking chewable tablets on an empty stomach, 4 mg Cmax is achieved after 2 hours.
The pharmacokinetics of montelukast remains almost linear when administered orally in doses greater than 50 mg.
When taking montelukast in the morning and evening hours, no differences in pharmacokinetics were observed.
Distribution
The binding of montelukast to plasma proteins is more than 99%. V d in the equilibrium state is 8-11 liters.
Studies conducted in rats with radiolabeled montelukast indicate minimal penetration of the BBB. In addition, the concentration of labeled montelukast 24 hours after administration was minimal in all other tissues.
When taking montelukast at a dose of 10 mg 1 time/day, a moderate (about 14%) accumulation of the active substance in plasma is observed.
Metabolism
Montelukast is extensively metabolized. When used in therapeutic doses, the concentration of montelukast metabolites in plasma at steady state in adults and children is not determined.
In vitro studies using human liver microsomes have shown that isoenzymes of the cytochrome P450 system: CYP3A4, 2C8 and 2C9 are involved in the metabolism of montelukast. According to the results of studies conducted in vitro on human liver microsomes, montelukast at therapeutic concentrations in blood plasma does not inhibit the isoenzymes CYP3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Removal
T1/2 of montelukast in young healthy adults ranges from 2.7 to 5.5 hours. Plasma clearance of montelukast in healthy adults averages 45 ml/min. Following oral administration of radiolabeled montelukast, 86% is excreted in feces within 5 days and less than 0.2% is excreted in urine, confirming that montelukast and its metabolites are excreted almost exclusively in bile.
Pharmacokinetics in special clinical situations
The pharmacokinetics of montelukast are similar in women and men.
With a single oral dose of 10 mg of montelukast, the pharmacokinetic profile and bioavailability are similar in elderly and young patients. In elderly people, T1/2 of montelukast from plasma is slightly longer. No dose adjustment is required in elderly patients.
There were no differences in clinically significant pharmacokinetic effects in patients of different races.
In patients with mild to moderate hepatic impairment and clinical manifestations of cirrhosis, a slowdown in the metabolism of montelukast was observed, accompanied by an increase in AUC by approximately 41% after a single dose of 10 mg. The excretion of montelukast in these patients is slightly increased compared to healthy subjects (average T1/2 - 7.4 hours). No dose adjustment of montelukast is required for patients with mild to moderate hepatic impairment. Data on the nature of the pharmacokinetics of montelukast in patients with severe liver failure (more than 9 points on the Child-Pugh scale).
Because montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal impairment have not been evaluated. No dose adjustment is required in this category of patients.
Indications
- prevention and long-term treatment of bronchial asthma in children aged 2 years and older: to control daytime and nighttime symptoms of the disease;
- relief of symptoms of allergic rhinitis in children aged 2 years and older.
Contraindications
- children under 2 years of age;
- phenylketonuria;
- hypersensitivity to the components of the drug.
Dosage
Orally 1 time/day, regardless of meals.
For treatment bronchial asthma Singulair should be taken in the evening.
During treatment allergic rhinitis the drug can be taken at any time of the day at the request of the patient.
Patients with bronchial asthma and allergic rhinitis should take 1 tablet of Singulair once a day in the evening.
Children aged 2 to 5 years
For bronchial asthma and/or allergic rhinitis- 1 chewable tablet 4 mg per day.
The therapeutic effect of the drug Singulair on indicators reflecting the course of bronchial asthma develops during the first day. The patient should continue to take Singulair both during the period of achieving control over the symptoms of bronchial asthma, and during periods of exacerbation of bronchial asthma.
For elderly patients, patients with renal failure, as well as patients with mild or moderate liver dysfunction, or depending on gender, no special dose adjustment is required.
Prescribing Singulair simultaneously with other types of treatment for bronchial asthma
The drug Singulair can be added to the patient's treatment with bronchodilators and inhaled corticosteroids.
Side effects
In general, Singulair is well tolerated by patients. Side effects are usually mild and, as a rule, do not require discontinuation of the drug. The overall incidence of side effects when treated with Singulair is comparable to their frequency when taking placebo.
Children aged 2 to 5 years with bronchial asthma
Clinical studies of the drug Singulair involved 573 patients aged 2 to 5 years. In a 12-week placebo-controlled clinical trial, the only adverse event (AE) assessed as drug-related that occurred in >1% of Singulair-treated patients and more frequently than placebo-treated patients was thirst. The differences in the incidence of this AE between the two treatment groups were not statistically significant.
In total, in the studies, 426 patients aged 2 to 5 years were treated with Singulair for at least 3 months, 230 were treated for 6 months or longer, and 63 patients were treated for 12 months or longer. With longer treatment, the AE profile did not change.
Children aged 2 to 14 years with seasonal allergic rhinitis
A 2-week, placebo-controlled clinical trial using Singulair for the treatment of seasonal allergic rhinitis included 280 patients aged 2 to 14 years. Patients took Singulair 1 time/day in the evening and was generally well tolerated. The safety profile of the drug in children was similar to that of placebo. In this clinical study, there were no AEs that were considered drug-related, occurred in ≥1% of patients treated with Singulair, or occurred more frequently than in patients treated with placebo.
Children aged 6 to 14 years with bronchial asthma
The safety profile of the drug in children was generally similar to the safety profile in adults and comparable to the safety profile of placebo.
In an 8-week placebo-controlled clinical trial, the only AE assessed as drug-related occurring in >1% of Singulair-treated patients and more frequently than in placebo-treated patients was headache. The difference in frequency between the two treatment groups was not statistically significant.
In growth rate studies, the safety profile in patients in this age group was consistent with the previously described safety profile of Singulair.
With longer treatment (more than 6 months), the AE profile did not change.
Adults and children aged 15 years and older with asthma
In two 12-week placebo-controlled clinical trials with a similar design, the only AEs assessed as drug-related that occurred in ≥1% of patients taking Singulair and more frequently than in the placebo group were abdominal pain and headache. pain. The differences in the incidence of these AEs between the two treatment groups were not statistically significant. With longer treatment (for 2 years), the AE profile did not change.
Adults and children aged 15 years and older with seasonal allergic rhinitis
Patients took Singulair 1 time/day in the morning or evening; the drug was generally well tolerated, and the safety profile of the drug was similar to that of placebo. In placebo-controlled clinical trials, there were no AEs considered to be drug-related that occurred in ≥1% of patients taking Singulair or more frequently than in the placebo group. In the 4-week placebo-controlled clinical study, the safety profile of the drug was similar to that in the 2-week studies. The incidence of drowsiness when taking the drug in all studies was the same as when taking placebo.
Adults and children aged 15 years and older with year-round allergic rhinitis
Patients took Singulair 1 time/day in the morning or evening; overall, the drug was well tolerated. The drug's safety profile was similar to that observed in patients with seasonal allergic rhinitis and placebo. In these clinical studies, there were no AEs that were considered drug-related, were observed in ≥1% of patients taking Singulair, and were more common than in the group of patients taking placebo. The incidence of drowsiness while taking the drug was the same as when taking placebo.
Generalized analysis of clinical trial results
A pooled analysis was conducted of 41 placebo-controlled clinical trials (35 studies involving patients aged 15 years or older, 6 studies involving patients aged 6 to 14 years) using validated methods for assessing suicidality. Among the 9,929 patients receiving Singulair and the 7,780 patients receiving placebo in these studies, 1 patient was identified as suicidal in the Singulair group. There were no suicides, suicide attempts, or other preparatory acts indicative of suicidal behavior in any of the treatment groups.
Separately, a pooled analysis of 46 placebo-controlled clinical trials (35 studies in patients aged 15 years and older; 11 studies in patients aged 3 months to 14 years) was conducted to assess adverse behavioral effects. Among the 11,673 patients treated with Singulair and the 8,827 patients treated with placebo in these studies, the percentage of patients experiencing at least one adverse behavioral effect was 2.73% among patients treated with Singulair and 2.27% among patients treated with placebo; the odds ratio was 1.12 (95% confidence interval).
AEs registered during post-registration use of the drug
From the blood coagulation system: increased tendency to bleed.
From the immune system: hypersensitivity reactions, incl. anaphylaxis; very rarely (<1/10 000) - эозинофильная инфильтрация печени.
From the mental side: agitation (including aggressive behavior or hostility), anxiety, depression, disorientation, impaired attention, pathological dreams, hallucinations, insomnia, memory impairment, psychomotor activity (including irritability, restlessness and tremors), somnambulism, suicidal thoughts and behavior ( suicidality).
From the nervous system: dizziness, drowsiness, paresthesia/hypesthesia; very rarely (<1/10 000) - судороги.
From the cardiovascular system: cardiopalmus.
From the respiratory system: nosebleeds, pulmonary eosinophilia.
From the digestive system: diarrhea, dyspepsia, nausea, vomiting, pancreatitis.
From the outside liver and biliary tract: increased activity of ALT and AST in the blood; very rarely (<1/10 000) - гепатит (включая холестатические, гепатоцеллюлярные и смешанные поражения печени).
For the skin and subcutaneous tissues: tendency to form hematomas, erythema nodosum, erythema multiforme, itching, rash.
Allergic reactions: angioedema, urticaria.
From the musculoskeletal system: arthralgia, myalgia, including muscle cramps.
From the urinary system: enuresis in children.
General reactions: asthenia (weakness)/fatigue, edema, pyrexia.
Overdose
Symptoms overdoses were not identified during clinical studies of long-term (22 weeks) treatment with Singulair in adult patients with bronchial asthma in doses up to 200 mg/day, or during short (about 1 week) clinical studies when taking the drug in doses up to 900 mg/day.
There have been cases of acute overdose of Singulair (taking at least 1000 mg/day) in the post-registration period and during clinical trials in adults and children. Clinical and laboratory data indicated comparable safety profiles of Singulair in children, adults and elderly patients. The most common symptoms were thirst, drowsiness, vomiting, psychomotor agitation, headache and abdominal pain. These side effects are consistent with the safety profile of Singulair.
Treatment: carrying out symptomatic therapy. There is no specific information on the treatment of overdose of Singulair. There are no data on the effectiveness of peritoneal dialysis or hemodialysis with montelukast.
Drug interactions
Singulair can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and/or the treatment of allergic rhinitis. Montelukast at the recommended therapeutic dose did not have a clinically significant effect on the pharmacokinetics of the following drugs: prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.
When co-administered with phenobarbital, the AUC of montelukast is reduced by approximately 40%. , but this does not require changes in the dosage regimen of Singulair.
In vitro studies have shown that montelukast inhibits the CYP2C8 isoenzyme. However, in an in vivo drug interaction study between montelukast and rosiglitazone (metabolized via the CYP2C8 isoenzyme), no evidence was obtained of montelukast inhibiting the CYP2C8 isoenzyme. Therefore, in clinical practice, the effect of montelukast on the CYP2C8-mediated metabolism of a number of drugs, incl. paclitaxel, rosiglitazone, repaglinide.
In vitro studies have shown that montelukast is a substrate of the CYP2C8, 2C9 and 3A4 isoenzymes. Data from a clinical drug interaction study of montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times. Coadministration of itraconazole, a strong CYP3A4 inhibitor, with gemfibrozil and montelukast did not result in an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic exposure of montelukast may not be considered clinically significant based on safety data when used at doses greater than the approved dose of 10 mg in adult patients (eg, 200 mg/day for adult patients for 22 weeks and up to 900 mg/day for no clinically significant adverse effects were observed in patients taking the drug for approximately one week). Thus, when co-administered with gemfibrozil, no dose adjustment of montelukast is required. Based on the results of in vitro studies, no clinically significant drug interactions are expected with other known CYP2C8 inhibitors (for example, with trimethoprim). In addition, coadministration of montelukast with itraconazole alone did not significantly increase the effect of systemic exposure to montelukast.
Combination treatment with bronchodilators
Singulair is a reasonable addition to bronchodilator monotherapy if the latter do not provide adequate control of bronchial asthma. Once the therapeutic effect of treatment with Singulair is achieved, you can begin to gradually reduce the dose of bronchodilators.
Combined treatment with inhaled corticosteroids
Treatment with Singulair provides an additional therapeutic effect in patients using inhaled corticosteroids. Once the condition has stabilized, you can begin a gradual reduction in the dose of GCS under the supervision of a physician. In some cases, complete abolition of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Singulair is not recommended.
special instructions
The effectiveness of oral Singulair for the treatment of acute attacks of bronchial asthma has not been established. Therefore, Singulair tablets are not recommended for the treatment of acute attacks of bronchial asthma. Patients should be instructed to always carry emergency medications to relieve asthma attacks (short-acting inhaled beta 2 agonists).
You should not stop taking Singulair during an exacerbation of asthma and the need to use emergency medications (short-acting inhaled beta 2 agonists) to relieve attacks.
Patients with confirmed allergies to and other NSAIDs should not take these drugs during treatment with Singulair, since Singulair, while improving respiratory function in patients with allergic bronchial asthma, however, cannot completely prevent bronchoconstriction caused by NSAIDs.
The dose of inhaled corticosteroids used concomitantly with Singulair can be gradually reduced under the supervision of a physician, however, an abrupt replacement of inhaled or oral corticosteroids with Singulair should not be carried out.
Neuropsychiatric disorders have been described in patients taking Singulair. Given that these symptoms could be caused by other factors, it is unknown whether they are related to taking Singulair. Physicians should discuss these side effects with patients and/or their parents/guardians. Patients and/or their caregivers should be advised that if such symptoms occur, they should notify their 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 more of the following reactions: eosinophilia, rash, worsening of pulmonary symptoms, cardiac complications and/or neuropathy, sometimes diagnosed as Churg-Strauss syndrome, systemic eosinophilic vasculitis. Although the cause-and-effect relationship of these adverse reactions with therapy with leukotriene receptor antagonists has not been established, when reducing the dose of systemic corticosteroids in patients receiving Singulair, caution and appropriate clinical monitoring must be performed.
Chewable tablets 4 mg contain aspartame, a source of phenylalanine. Patients with phenylketonuria should be informed that each 4 mg chewable tablet contains aspartame equivalent to 0.674 mg phenylalanine. Singulair in the form of 4 mg chewable tablets is not recommended for use in patients with phenylketonuria.
Impact on the ability to drive vehicles and operate machinery
This section does not apply to the drug Singulair chewable tablets 4 mg, since it is intended for the treatment
children from 2 to 5 years old. Thus, the information presented below relates to the active substance of the drug montelukast.
Singulair is not expected to affect the ability to drive or drive.
mechanisms. However, individual reactions to the drug may vary. Some side effects
(such as dizziness and drowsiness), which have been reported to occur very rarely with the use of the drug
Singulair may affect the ability of some patients to drive vehicles and operate machinery.
Pregnancy and lactation
Clinical studies of the drug Singulair have not been conducted in pregnant women. Singulair should be used during pregnancy and breastfeeding only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
During post-marketing use of Singulair, the development of congenital limb defects has been reported in newborns whose mothers took Singulair during pregnancy. Most of these women also took other medications to treat asthma during pregnancy. A cause-and-effect relationship between taking Singulair and the development of congenital limb defects has not been established.
For patients with mild or moderate liver dysfunction, no special dose selection is required.
There are no data on the nature of the pharmacokinetics of montelukast in patients with severe liver failure (more than 9 points on the Child-Pugh scale).
Use in old age
For elderly patients no special dose selection is required.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
The drug should be stored out of the reach of children, in a dry place, protected from light at a temperature of 15° to 30°C. Shelf life - 2 years.
