Singlon
Singlon: 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. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Singlon
ATX code: R03DC03
Active ingredient: montelukast (montelukast)
Producer: Gedeon Richter JSC (Poland)
Description and photo updated: 22.11.2018
Prices in pharmacies: from 499 rubles.
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Singlon is a leukotriene receptor antagonist used to treat bronchial asthma and allergic rhinitis.
Release form and composition
Singlon dosage forms:
- film-coated tablets: round, biconvex, yellow, on one side there is an engraving of the letter R and the number "15" under it; the cross-section shows a white core (7 pieces in blisters, in a cardboard box 2, 4 or 8 blisters);
- chewable tablets: lenticular (4 mg) or round (5 mg), biconvex, pale yellow in color (inclusions of a darker color are possible), with a pronounced cherry aroma, engraving on one side of R13 (4 mg) or R14 (5 mg)) (7 pcs. in blisters, in a cardboard box 2, 4 or 8 blisters).
Composition of 1 film-coated tablet:
- active substance: montelukast sodium - 10.4 mg, which corresponds to 10 mg of montelukast;
- auxiliary components: microcrystalline cellulose 101, magnesium stearate, hyprolose, lactose monohydrate, croscarmellose sodium;
- composition of the film shell: opadry yellow 20B32427, including hyprolose, hypromellose 50cP, hypromellose 3cP, macrogol 400, titanium dioxide, iron oxide yellow dye.
Composition of 1 chewable tablet:
- active substance: montelukast sodium - 4.16 or 5.2 mg, which corresponds to 4 or 5 mg of montelukast, respectively;
- auxiliary components: microcrystalline cellulose 101, mannitol, aspartame, croscarmellose sodium, hyprolose, magnesium stearate, iron dye yellow oxide (E172), cherry flavor (powder).
Pharmacological properties
Pharmacodynamics
Singlon's active substance, montelukast, is a specific antagonist of leukotriene receptors. Even in low doses, it is able to arrest bronchospasm caused by inhalation of LTD4. The therapeutic effect develops after taking the first dose. Bronchodilation continues for 2 hours after oral administration of the drug.
Montelukast complements the bronchodilation effect caused by the beta-agonist. Inhibits the early and late phases of antigen-induced bronchospasm. Reduces the number of eosinophils in the respiratory tract (in sputum) and in the peripheral blood, improves control over the course of bronchial asthma.
The drug significantly improves the forced expiratory volume (OFV) in 1 second and the maximum expiratory flow rate (MOVV). Reduces the severity of night and daytime symptoms of bronchial asthma, including difficulty breathing, wheezing, coughing, restriction of activity. Significantly reduces the patient's need for beta-adrenergic agonists and glucocorticosteroids (GCS), used as needed (in case of deterioration).
Patients receiving Singlon have a longer remission compared to patients who do not take it.
Montelukast enhances the effect of inhaled glucocorticosteroids. Weakens bronchospasm that develops during exercise.
In children from 2 years of age with mild bronchial asthma and episodic exacerbations of the disease, the drug significantly improves respiratory function and reduces the frequency of exacerbations.
In patients with bronchial asthma, sensitive to acetylsalicylic acid (ASA), receiving inhaled and / or oral glucocorticosteroids, montelukast significantly improves the control of symptoms of bronchial asthma.
Pharmacokinetics
Basic pharmacokinetic characteristics of montelukast:
- absorption: after oral administration, montelukast is rapidly absorbed. The maximum plasma concentration is observed after 3 hours: in adult patients when taking the drug at a dose of 10 mg on an empty stomach, in children 2–5 years old after taking 4 mg on an empty stomach. Food intake does not significantly affect its bioavailability, which averages 64%;
- distribution: montelukast is characterized by a high bond with plasma proteins - more than 99%. The volume of distribution at equilibrium is approximately 8–11 liters. Poorly penetrates the blood-brain barrier. 24 hours after ingestion, the concentration of the substance in all tissues of the body is minimal;
- biotransformation: the substance is actively metabolized in the liver. When taken in therapeutic doses in an equilibrium state, plasma concentrations in adults and children are not determined. Metabolism of montelukast occurs, presumably, with the participation of cytochrome P450 CYP2 isoenzymes (A6, 2C9 and 3A4). At the same time, in therapeutic doses, the drug does not inhibit such cytochrome P450 CYP isozymes as 2A6, 2C9, 3A4, 1A2, and 2C19. The pharmacological activity of metabolites is negligible;
- Excretion: the plasma clearance of montelukast in healthy adults averages 45 ml / min. After oral administration of the labeled substance, 86% of the dose was excreted within 5 days mainly through the intestines and in a small amount by the kidneys - less than 0.2%. This indicates that montelukast and its metabolites are excreted mainly in the bile. The half-life in young patients is 2.7–5.5 hours. Pharmacokinetics remains practically linear when oral doses of more than 50 mg are taken.
Pharmacokinetic studies of montelukast with concomitant renal failure have not been conducted. Given the route of elimination of the drug (with bile), dose adjustment is not required for patients with impaired renal function, as well as for the elderly.
There are no pharmacokinetic data in patients with severe hepatic impairment (score> 9 on the Child-Pugh scale).
Indications for use
- long-term treatment and prevention of bronchial asthma, including prevention of night and daytime symptoms of the disease;
- therapy of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid, prevention of bronchospasm of physical effort.
Contraindications
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption - for film-coated tablets;
- phenylketonuria - for chewable tablets;
- hypersensitivity to any component of Singlon.
Age restrictions:
- film-coated tablets - up to 15 years;
- chewable tablets 4 mg - up to 2 years;
- chewable tablets 5 mg - up to 6 years.
According to the instructions, Singlon should be used with caution during pregnancy and lactation, as well as in the case of simultaneous administration of CYP3A4 inducers.
Instructions for the use of Singlon: method and dosage
Film-coated tablets are prescribed for adults and adolescents from 15 years of age: inside, regardless of meals, 1 tablet (10 mg) 1 time per day, in the evening.
Chewable tablets 4 mg are prescribed for children from 2 to 5 years old, chewable tablets 5 mg - for children 6-14 years old: 1 tablet 1 time per day, in the evening. It is recommended to take the drug 1 hour before or 2 hours after meals.
General recommendations:
- For female and male patients, the dose of montelukast is the same.
- The therapeutic effect of Singlon in relation to the symptoms of bronchial asthma is manifested within one day after taking the first dose. Patients are advised to continue taking the drug not only during the worsening of the course of the disease, but also during periods of a controlled course.
- Simultaneously with Singlon, you should not take other drugs containing montelukast as an active substance.
- Elderly patients with renal insufficiency of mild to moderate severity, as well as patients with hepatic insufficiency of mild and moderate severity, do not need to adjust the dose.
- Singlon can be incorporated into existing asthma treatment regimens.
- Singlon can be prescribed for bronchial asthma as an additional agent for patients in whom inhaled corticosteroids and short-acting beta-adrenomimetics used as needed do not provide the necessary control of the disease. It is important to take into account that montelukast does not replace inhaled GCS.
Side effects
- from the immune system: hypersensitivity reactions (including anaphylaxis);
- on the part of the blood and lymphatic system: increased tendency to bleeding;
- from the gastrointestinal tract: dry mouth, nausea, abdominal pain, vomiting, dyspepsia, diarrhea;
- from the hepatobiliary system: increased activity of hepatic enzymes in the blood serum, cholestatic hepatitis, eosinophilic liver infiltrates;
- from the side of the heart: palpitations;
- from the musculoskeletal system: muscle spasms, arthralgia, myalgia;
- from the skin and subcutaneous tissues: rash, itching, urticaria, erythema nodosum, ecchymosis, angioedema;
- from the nervous system: drowsiness, dizziness, headache, hypesthesia / paresthesia, seizures;
- from the psyche: sleep disturbances (including nightmares, insomnia), anxiety, irritability, hallucinations, tremors, agitation, aggressive behavior, depression, suicidality (suicidal thoughts and behavior);
- others: thirst, asthenia, increased fatigue, edema, Churg-Strauss syndrome (systemic eosinophilic vasculitis).
Overdose
In clinical studies, when adult patients took the drug in a daily dose of more than 200 mg for 22 weeks and in a daily dose of 900 mg for 1 week, overdose symptoms were not detected.
There are known cases of acute overdose in adults and children when taking montelukast in a dose of more than 1000 mg. The obtained clinical and laboratory data were consistent with the safety profile for adult patients and children. In most reports, there were no indications of the development of adverse manifestations. The most frequent adverse events corresponded to the safety profile of montelukast and were expressed by drowsiness, thirst, vomiting, abdominal pain, headache, mydriasis, and psychomotor hyperactivity.
There is no specific information on the treatment of an overdose of montelukast and the possibility of its elimination by hemodialysis or peritoneal dialysis.
special instructions
Singlon cannot replace inhaled or oral glucocorticosteroids. There is no data on the possibility of reducing the dose of oral corticosteroids in the case of concomitant administration of montelukast.
The drug should not be used to relieve acute attacks of bronchial asthma. In case of an attack, it is necessary to use short-acting inhaled beta-adrenomimetics. If the need for their use increases, you should immediately consult a doctor.
There are known cases of systemic eosinophilia, sometimes accompanied by symptoms of vasculitis and Churg-Strauss syndrome, in patients receiving therapy for bronchial asthma, including Singlon. Systemic glucocorticosteroids are prescribed to treat this condition. Most often, such cases are associated with dose reduction or cancellation of oral GCS. The possibility that the occurrence of Churg-Strauss syndrome is associated with the use of leukotriene receptor antagonists cannot be confirmed or excluded. The physician should warn the patient about the risk of vasculitis rash, increased pulmonary symptoms, eosinophilia, neuropathy, and / or heart complications. When these symptoms appear, the patient should consult a doctor for a second examination and revision of the treatment regimen.
Singlon has no effect on acetylsalicylic acid and other non-steroidal anti-inflammatory drugs in patients with bronchial asthma and hypersensitivity to ASA.
The coated tablets contain lactose, therefore Singlon is contraindicated in this dosage form in the presence of such rare hereditary diseases as glucose-galactose malabsorption, lactase deficiency and lactose intolerance.
Chewable tablets contain aspartame, which is a source of phenylalanine: in 1 tablet 4 mg - 1.2 mg, in 1 tablet 5 mg - 1.5 mg. Therefore, the drug in this dosage form is contraindicated in children with phenylketonuria.
Influence on the ability to drive vehicles and complex mechanisms
Some patients experience dizziness and / or drowsiness while taking Singlon. In this case, you should refrain from driving a car and performing potentially dangerous types of work.
Application during pregnancy and lactation
During pregnancy and lactation, Singlon should be used with caution.
Pediatric use
Chewable tablets 4 mg are contraindicated in children under 2 years of age (safety of use has not been established), chewable tablets 5 mg - for children under 6 years old, Singlon 10 mg coated tablets - up to 15 years.
With impaired renal function
If renal function is insufficient, there is no need to adjust the Singlon dose.
For violations of liver function
No dose adjustment is required in mild to moderate hepatic impairment. There is no information on the possibility of using Singlon in severe hepatic impairment.
Use in the elderly
Singlon 10 mg can be used in old age. No dose adjustment is required.
Drug interactions
Singlon can be combined with other drugs that are traditionally used for the prevention and long-term treatment of bronchial asthma.
When used in recommended doses, montelukast does not have a clinically significant effect on the pharmacokinetics of warfarin, terfenadine, theophylline, digoxin, prednisolone, prednisone and oral contraceptives (ethinylestradiol / norethisterone 35/1).
Montelukast is metabolized with the participation of the CYP3A4 isoenzyme, therefore, caution should be exercised with the simultaneous use of CYP3A4 inducers (such as rifampicin, phenytoin and phenobarbital), especially in the treatment of children.
In vitro studies have shown that montelukast is a potent inhibitor of the CYP2C8 isoenzyme. However, in the course of studies of its clinical interaction with rosiglitazone (an example of marker substrates for drugs, the main metabolism of which is carried out by the CYP2C8 isoenzyme), no inhibitory effect of montelukast on the CYP2C8 isoenzyme was revealed. In this regard, it is assumed that Singlon will not significantly affect the drugs in the metabolism of which this enzyme is involved (for example, rosiglitazone, repaglinide, paclitaxel).
When very high doses of montelukast are taken (20 and 60 times higher than recommended for adults), the plasma concentration of simultaneously used theophylline decreases. When Singlon is taken in recommended doses, this effect is absent.
Analogs
Singlon's analogues are Almont, Glemont, Montelar, Singular, Monkasta, Singulex, MONLER, Montelukast, Montelukast Zentiva, Ectalust.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a place protected from light, dry, out of reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of the Singleon
According to most reviews, Singlon is a very effective remedy for the treatment of bronchial asthma, which practically does not cause side effects.
Many reviews are left by parents who, as prescribed by a doctor, use the drug to treat not only bronchial asthma in their children, but also allergic diseases. Additional benefits include the availability of a dosage form for children from 2 years of age, the pleasant taste of chewable tablets and their good tolerance.
The cost of Singlon, in the opinion of the majority, is quite high, but still it is somewhat lower than that of similar medicines containing montelukast as an active substance.
Single negative reviews usually indicate the individual intolerance of Singlon.
Price for Singlon in pharmacies
Approximate prices for Singlon: 28 coated tablets - 680–835 rubles, 28 chewable tablets 4 mg - 770–840 rubles, 28 chewable tablets 5 mg - 785–830 rubles.
Singlon: prices in online pharmacies
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Drug name Price Pharmacy |
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Singlon 4 mg chewable tablets 28 pcs. RUB 499 Buy |
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Singlon 5 mg chewable tablets 28 pcs. RUB 500 Buy |
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Singlon 10 mg film-coated tablets 28 pcs. RUB 688 Buy |
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Singlon tablets chewable. 5mg 28 pcs. 823 RUB Buy |
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Singlon tablets p.o. 10mg 28 pcs. 848 RUB Buy |
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Singlon tablets chewable. 4mg 28 pcs. 863 RUB Buy |
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!
