Singular
Singulair: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogues
- 16. Terms and conditions of storage
- 17. Reviews
- 18. Price in pharmacies
Latin name: Singulair
ATX code: R03DC03
Active ingredient: Montelukast (Montelukast)
Manufacturer: Merck Sharp and Dome B. V. (Netherlands)
Description and photo update: 2019-13-08
Prices in pharmacies: from 699 rubles.
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Singular is a leukotriene receptor blocker, anti-bronchospastic anti-inflammatory drug.
Release form and composition
Singularia dosage forms:
- chewable tablets: biconvex, pink, with SINGULAIR engraving on one side, on the other: for oval tablets - MSD 711, for round tablets - MSD 275 (7 pcs. in a blister, in a cardboard box 1, 2 or 4 blisters);
- coated tablets: square shape with rounded edges, light cream color, with SINGULAIR engraving on one side, on the other - MSD 117 (7 pcs. in a blister, in a cardboard box 1, 2 or 4 blisters).
1 chewable tablet contains:
- active substance: montelukast sodium - 4.16 mg or 5.2 mg, which corresponds to 4 mg or 5 mg of free acid;
- auxiliary components: cherry flavor, mannitol, hyprolose (hydroxypropyl cellulose), croscarmellose sodium, microcrystalline cellulose, iron oxide red, magnesium stearate, aspartame.
1 coated tablet contains:
- active substance: montelukast sodium - 10.4 mg, which corresponds to 10 mg of free acid;
- excipients: lactose monohydrate, hydroxypropyl cellulose (hyprolose), microcrystalline cellulose, magnesium stearate, croscarmellose sodium;
- shell composition: hypromellose (methylhydroxypropyl cellulose), hyprolose, yellow iron oxide (E172), red iron oxide (E172), titanium dioxide (E171), carnauba wax.
Pharmacological properties
Pharmacodynamics
Cysteinyl leukotrienes (LTC 4, LTD 4, LTE 4) are potent inflammatory mediators, eicosanoids, which can be secreted by a variety of cells (including eosinophils and mast cells). These important pro-asthmatic mediators are able to bind to the cysteinyl leukotriene receptors. CysLT 1 receptors (type I cysteinyl leukotriene receptors) are present in the human respiratory tract (including macrophages and bronchial smooth muscle cells) and other proinflammatory cells (including eosinophils and some myeloid stem cells).
Cysteinyl leukotrienes correlate with the pathophysiology of allergic rhinitis and bronchial asthma. The cause of allergic rhinitis symptoms is the release of cysteinyl leukotrienes from pro-inflammatory cells of the nasal mucosa during the early and late phases of an allergic reaction that develops when exposed to an allergen. Intranasal test with cysteinyl leukotrienes demonstrated an increase in nasal airway resistance and symptoms of nasal obstruction. In asthma, the following leukotriene-mediated effects develop: an increase in the number of eosinophils, an increase in vascular permeability, an increase in mucus secretion, bronchospasm.
When taken orally, montelukast is highly active and significantly improves inflammation in bronchial asthma. According to pharmacological and biochemical analysis, the substance selectively and with high affinity binds to CysLT 1 receptors, but does not interact with other pharmacologically important receptors in the respiratory tract (cholinergic, prostaglandin, or β-adrenergic receptors). Due to its ability to bind to CysLT 1 receptors, montelukast inhibits the physiological effect of the cysteinyl leukotrienes LTC 4, LTD 4 and LTE 4 and does not exert a stimulating effect on these receptors.
Montelukast is capable of inhibiting CysLT receptors in the airways, as evidenced by its ability to block the development of bronchospasm in response to LTD 4 inhalation in patients with bronchial asthma. A dose of 5 mg is sufficient to arrest the LTD 4 -induced bronchospasm.
Oral administration of montelukast causes bronchodilation within 2 hours and can complement β 2 -adrenomimetic-induced bronchodilation.
When taking more than 10 mg 1 time per day, the effectiveness of montelukast does not increase.
Pharmacokinetics
After oral administration, montelukast is absorbed quickly and almost completely. The average oral bioavailability is 64%. In adult patients taking 10 mg of montelukast on an empty stomach, the maximum concentration of the substance in the blood plasma is observed after 3 hours. Taking the drug with food does not affect bioavailability and maximum concentration.
Montelukast binds to blood plasma proteins by more than 99%. The volume of distribution in the state of equilibrium concentration is from 8 to 11 liters.
Studies carried out on rats with radioactively labeled montelukast revealed minimal penetration of the substance through the blood-brain barrier. In addition, 24 hours after administration, the concentrations of the labeled drug in all other tissues were minimal.
Montelukast is extensively metabolized. When studying therapeutic doses in children and adults, the concentration of montelukast metabolites in an equilibrium state in plasma is not determined.
In vitro studies using human liver microsomes have shown that cytochrome P 450 isoenzymes (2C8, 2C9 and 3A4) are involved in the metabolism of montelukast. Also, studies have shown that this substance in therapeutic concentration in blood plasma does not inhibit cytochrome P 450 isoenzymes (2C9, 2C19, 1A2, 2A6, 3A4 and 2D6).
In healthy adults, the plasma clearance of montelukast averages 45 ml / min. Montelukast and its metabolites are almost completely excreted by bile, which is confirmed in studies: with oral administration of radioactively labeled montelukast, 86% of the dose received is excreted within 5 days in feces and less than 0.2% in urine.
The half-life of montelukast in young healthy adults is 2.7–5.5 hours. When taken orally over 50 mg, the pharmacokinetics of this substance remains almost linear. When taken in the morning and evening hours, the pharmacokinetic parameters do not change. When taking more than 10 mg 1 time per day, there is a moderate accumulation of the active substance in the plasma (approximately 14%).
The pharmacokinetics of montelukast in men and women are similar. No differences in clinically significant pharmacokinetic effects in representatives of different races were identified.
With a single oral administration of montelukast at a dose of 10 mg, the bioavailability and pharmacokinetic profile in young and elderly patients are similar, however, in the elderly, the plasma half-life of the substance is slightly longer.
In patients with clinical manifestations of liver cirrhosis and mild to moderate hepatic insufficiency, the metabolism of montelukast slows down. With a single dose of 10 mg of the substance, the area under the pharmacokinetic curve AUC increases by about 41%. Compared with healthy people, in such patients, the elimination time of montelukast slightly increases (the average elimination half-life is 7.4 hours). There are no data on the pharmacokinetics of montelukast in persons with severe hepatic impairment (more than 9 points on the Child-Pugh scale).
Since montelukast and its metabolites are not excreted in the urine, there is no data on the pharmacokinetics of the substance in patients with renal insufficiency.
Indications for use
4 mg chewable tablets
- bronchial asthma - prevention and long-term treatment in order to control the day and night symptoms of the disease in children from two years of age and older;
- allergic rhinitis - symptom relief in children two years of age and older.
5 mg chewable tablets and film-coated tablets
- bronchial asthma - prevention and long-term treatment of adults and children from 6 years old (for chewable tablets 5 mg) or from 15 years old (for coated tablets) in order to prevent day and night symptoms of the disease, prevent bronchospasm during exercise, including treatment of patients with bronchial asthma with hypersensitivity to acetylsalicylic acid;
- relief of night and day symptoms of seasonal and perennial allergic rhinitis in patients over 6 years of age (for chewable tablets 5 mg) or from 15 years of age (for coated tablets).
Contraindications
- age up to 2 years;
- hypersensitivity to the components of Singular.
Additionally for chewable tablets:
- phenylketonuria;
- age up to 6 years (for chewable tablets 5 mg).
Additionally for coated tablets:
- age up to 15 years;
- syndrome of glucose-galactose malabsorption, lactase deficiency, lactose intolerance.
The use of Singular during pregnancy and breastfeeding is possible only if the expected effect of therapy for the mother outweighs the potential threat to the fetus or child.
Instructions for the use of Singular: method and dosage
The tablets are taken orally, regardless of food intake, 1 time per day.
In the treatment of bronchial asthma, the drug is used in the evening, allergic rhinitis - at any time convenient for the patient. In bronchial asthma with concomitant allergic rhinitis, the patient takes a dose in the evening 1 time per day.
Recommended daily dosage of Singular:
- patients over 15 years old: 1 coated tablet - 10 mg;
- children aged 6 to 14: 1 chewable tablet - 5 mg;
- children 2 to 5 years old: 1 chewable tablet - 4 mg.
The therapeutic effect of the drug develops during the first day.
The patient needs to continue taking pills not only with exacerbation of bronchial asthma, but also during the period of achieving control over the symptoms of bronchial asthma.
With renal failure, mild and moderate liver dysfunction, elderly patients do not need dose adjustment.
Side effects
Undesirable effects registered in the post-registration period of drug use:
- from the cardiovascular system: heart palpitations;
- infectious and parasitic pathologies: upper respiratory tract infections;
- on the part of the blood coagulation system: a tendency to increased bleeding;
- from the psyche: anxiety, agitation (including hostility, aggressive behavior), impaired attention, disorientation, pathological dreams, insomnia, hallucinations, psychomotor activity (including anxiety, irritability, tremors), memory impairments, somnambulism, depression, suicidal thoughts and behavior;
- from the immune system: hypersensitivity reactions, including anaphylaxis; very rarely - eosinophilic liver infiltration;
- from the digestive system: dyspepsia, nausea, vomiting, diarrhea, pancreatitis;
- from the nervous system: drowsiness, dizziness, paresthesia or hypesthesia; very rarely - convulsions;
- from the respiratory system: pulmonary eosinophilia, nosebleeds;
- from the liver and biliary tract: an increase in the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the blood; very rarely - hepatitis (including hepatocellular, cholestatic or mixed liver damage);
- allergic reactions: urticaria, angioedema;
- from the musculoskeletal system: myalgia, muscle cramps, arthralgia;
- on the part of the skin and subcutaneous tissues: itching, rash, tendency to hematomas, erythema multiforme, erythema nodosum;
- from the urinary system: in children - enuresis;
- general reactions: edema, asthenia (weakness) or increased fatigue, pyrexia.
Singular is well tolerated in most patients, side effects are usually mild and do not require discontinuation of therapy.
Overdose
In clinical studies of long-term (22 weeks) treatment of patients with bronchial asthma with a daily dose of the drug up to 200 mg and short (about 1 week) use of Singular with a daily dose of up to 900 mg, overdose symptoms were not identified.
In the post-registration period and in the course of clinical studies in children and adults, when taking at least 1000 mg of Singular per day, cases of acute overdose have been reported. Laboratory and clinical data indicate the comparability of the safety profiles of the drug in children, adults and elderly patients. The most common side effects (agitation, drowsiness, abdominal pain, thirst, vomiting, headache) are consistent with the safety profile of the drug.
There is no specific information on the treatment of Singular overdose. In acute overdose, symptomatic treatment is recommended. There are no data on the effectiveness of hemodialysis or peritoneal dialysis of montelukast.
special instructions
With a confirmed allergy to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (NSAIDs), their simultaneous use with montelukast is contraindicated, since it is not possible to completely prevent bronchoconstriction caused by NSAIDs.
Singular is not recommended for the treatment of acute attacks of bronchial asthma. To stop attacks of bronchial asthma, the patient should always have emergency medications with him - short-acting inhaled beta2-agonists. During an exacerbation of asthma, you should not stop taking the drug.
When prescribing the drug, it is impossible to abruptly cancel inhalation or oral glucocorticosteroids (GCS), it is allowed to gradually reduce the dose of simultaneously used GCS under the supervision of a physician. A sharp decrease in the dose of systemic corticosteroids can cause a rash, worsening pulmonary symptoms, the development of eosinophilia, cardiac complications and / or neuropathy, systemic eosinophilic vasculitis.
Since against the background of the use of Singular there is a risk of neuropsychiatric disorders, the patient should be warned about the possibility of their development and the need to immediately contact the attending physician if unwanted symptoms appear.
Adult patients are advised to be careful when driving vehicles and mechanisms due to the risk of side effects such as dizziness and drowsiness.
Application during pregnancy and lactation
Clinical studies of the effect of Singular on pregnancy have not been conducted. According to the data of post-registration use, cases of the development of congenital defects of the limbs in newborns, whose mothers took the drug during pregnancy, were recorded. Also, most of these women took other drugs for the treatment of bronchial asthma, therefore, a causal relationship between the development of congenital defects of the extremities and the use of Singular has not been established.
There are no data on the excretion of the drug in breast milk.
The use of Singular during pregnancy and breastfeeding is possible only in cases where the potential benefit to the mother outweighs the possible risk to the fetus / child.
Pediatric use
According to the instructions, Singular is used in the treatment of children of the following age categories:
- chewable tablets 4 mg - from 2 years;
- chewable tablets 5 mg - from 6 years old;
- film-coated tablets - from 15 years.
With impaired renal function
No dose adjustment of Singular is required in patients with impaired renal function.
For violations of liver function
When treating people with mild to moderate hepatic impairment, dose adjustment of Singular is not required.
Use in the elderly
When treating elderly patients, dose adjustment of Singular is not required.
Drug interactions
Singulair is indicated for simultaneous use with medicines intended for the prevention and long-term treatment of bronchial asthma and / or the treatment of allergic rhinitis.
The recommended therapeutic dose of montelukast does not have a clinically significant effect on the pharmacokinetics of theophylline, prednisolone, prednisone, terfenadine, warfarin, digoxin, oral contraceptives (norethindrone or ethinyl estradiol).
A decrease in the AUC value of montelukast by approximately 40% with concomitant phenobarbital therapy does not require correction of the drug dosing regimen.
The drug can be administered in combination with paclitaxel, rosiglitazone, repaglinide and other drugs that are metabolized with the participation of the CYP2C8 isoenzyme.
The inhibitor of CYP2C8 and CYP2C9 isoenzymes gemfibrozil increases the systemic effect of montelukast by 4.4 times. However, this effect is not considered clinically significant and does not require dose adjustment of montelukast.
Clinical studies have shown that being a substrate of isoenzymes CYP2C8, CYP3A4 and CYP2C9, montelukast does not cause therapeutically significant interactions with other CYP2C8 inhibitors, including trimethoprim, itraconazole.
When monotherapy with bronchodilators that do not provide adequate control of bronchial asthma, the use of Singular is a reasonable addition to therapy. After achieving the therapeutic effect of the combined treatment, the dose of bronchodilators can be gradually reduced.
Analogues
Singular analogs are: Almont, Glemont, Monax, Monkasta, Montler, Montelar, Singlon, Ectalust.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 30 ° C. Keep out of the reach of children.
Shelf life: chewable tablets - 2 years, coated tablets - 3 years.
Reviews of Singular
Reviews of Singular testify to its effectiveness in the treatment of children of different ages. Among the advantages of the drug are often mentioned speed, safety for health and low likelihood of side effects. Reported side effects are extremely rare.
According to doctors, Singular, which is a non-hormonal drug, in some cases can become a full-fledged replacement for inhaled corticosteroids.
The price of Singular in pharmacies
The approximate price for Singulair is: 14 chewable tablets 4 mg - 1059 rubles, 14 chewable tablets 5 mg - 1060 rubles, 14 coated tablets, 10 mg - 1079 rubles.
Singulair: prices in online pharmacies
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Drug name Price Pharmacy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
