Montelukast
Montelukast: 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: Montelukast
ATX code: R03DC03
Active ingredient: montelukast (montelukast)
Producer: Hetero Labs Limited (India), Vertex CJSC (Russia), N. B. Saniko (Belgium)
Description and photo updated: 22.11.2018
Prices in pharmacies: from 334 rubles.
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Montelukast is an anti-inflammatory anti-bronchoconstrictor drug, a blocker of leukotriene receptors.
Release form and composition
Dosage forms of Montelukast:
- film-coated tablets: depending on the manufacturer, they can be round, biconvex, with a yellow film shell and a white or almost white core, or square with rounded corners, with an engraving "I" on one side and "114" on the other, with film shell of a pale orange with a brownish tint and a white or almost white core (in a blister strip of 10, 14, 15, 20, 28 or 30 tablets, in a cardboard box of 1, 3 or 6 packs of 10 tablets, 1 or 2 packs 14 or 30 tablets, 1, 2 or 4 packs of 15 tablets, 3 packs of 20 tablets, 1 pack of 28 tablets; 10, 14 or 60 tablets in a jar, 1 jar in a cardboard box);
- chewable tablets: round, biconvex, white or almost white, with a cherry smell (10, 14, 15 or 30 tablets in a blister strip, in a cardboard box 1, 3 or 6 packs of 10 tablets, 1, 2 or 4 packs of 14 or 15 tablets, 1 or 2 packs of 30 tablets; 30 or 60 tablets in a jar, 1 jar in a cardboard box).
Composition of 1 film-coated tablet:
- active substance: montelukast sodium - 10.4 mg (in terms of montelukast - 10 mg);
- auxiliary components: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate;
- film shell (one of the options): I - hypromellose, hyprolose, talc, titanium dioxide, iron oxide yellow; II - dry mixture for film coating, including hypromellose, hyprolose, talc, titanium dioxide, yellow iron oxide; III - Opadry yellow 20A520007 (hypromellose, hyprolose, carnauba wax, titanium dioxide, dyes iron oxide yellow and iron oxide red).
Composition of 1 chewable tablet:
- active substance: montelukast sodium - 5.2 mg (in terms of montelukast - 5 mg);
- auxiliary components: mannitol, microcrystalline cellulose, hyprolose, magnesium stearate, aspartame, cherry flavor.
Pharmacological properties
Pharmacodynamics
When taken orally, Montelukast significantly improves the indicators of inflammation in patients with bronchial asthma. Biochemical and pharmacological analysis showed that it binds with high selectivity and chemical affinity to CysLT 1 receptors. The drug inhibits the physiological effect of the cysteinyl leukotrienes LTC 4, LTD 4, LTE 4 by binding to CysLT 1 receptors without stimulating these receptors.
Montelukast at a dose of 5 mg relieves bronchospasm caused by inhalation of cysteinyl-leukotriene LTD 4 in patients with bronchial asthma. The use of the drug leads to bronchodilation within 2 hours after administration, and can also supplement the bronchodilation caused by β2-adrenergic agonists.
Taking more than 10 mg of montelukast per day is not advisable, as this will not increase its effectiveness.
Pharmacokinetics
After oral administration, montelukast is almost completely absorbed within a short time. When adults take 10 mg of the drug (1 film-coated tablet), the maximum plasma concentration is reached within 3 hours, and when taken on an empty stomach, 5 mg of the drug (1 chewable tablet) - within 2 hours. The average bioavailability when taking film-coated tablets is 64%, chewable tablets - 73%.
Communication with plasma proteins - 99%. The volume of distribution at equilibrium concentration is 8–11 liters. The drug is actively metabolized. Its metabolism involves cytochrome P 450 isoenzymes - CYP 3A4, CYP 2A6, CYP 2C8 and CYP 2C9.
Plasma clearance of montelukast in healthy patients is 45 ml / min. It is excreted mainly through the intestines (86%). The half-life is 2.7-5.5 hours. When taking the drug at 10 mg per day, its cumulation remains moderate (about 14%).
The pharmacokinetics of the drug is not affected by the gender, age and race of the patient.
In patients with mild to moderate hepatic impairment, the metabolism of the drug is somewhat slowed down, and the area under the concentration-time curve (AUC) is increased by about 41% with a single dose of 10 mg of montelukast. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic impairment.
Indications for use
- long-term therapy of bronchial asthma and the prevention of its day and night symptoms;
- treatment of bronchial asthma with increased sensitivity to acetylsalicylic acid;
- relief of day and night symptoms of rhinitis (allergic and persistent);
- prevention of exercise-induced bronchospasm.
Contraindications
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption (for film-coated tablets);
- phenylketonuria (for chewable tablets);
- age up to 6 years (for chewable tablets), age up to 15 years (for film-coated tablets);
- increased sensitivity to the components of the drug.
Montelukast, instructions for use: method and dosage
Montelukast is taken orally, regardless of the meal. In case of bronchial asthma (in combination with or without allergic rhinitis), the drug is recommended to be taken in the evening, and in case of allergic rhinitis - at any time.
Film-coated tablets are intended for adolescents over 15 years of age and adults. The recommended dosage is 1 tablet once a day.
Recommendations for the use of chewable tablets:
- children 6-14 years old: 1 tablet once a day;
- adolescents over 15 years old and adults: 2 tablets 1 time per day.
The effect of the drug in patients with bronchial asthma begins to manifest itself during the first day of its administration. It is recommended to continue therapy while achieving control of symptoms, as well as during an exacerbation of the disease.
Side effects
- nervous system: dizziness, headache, drowsiness, paresthesia, hypesthesia, convulsions;
- cardiovascular system: heart palpitations;
- respiratory system, chest and mediastinal organs: epistaxis, pulmonary eosinophilia;
- psyche: agitation, aggression, hostility, anxiety, depression, impaired attention, disorientation, insomnia, pathological dreams, hallucinations, memory impairments, irritability, anxiety, tremors, somnambulism, tics, suicidal thoughts and behavior;
- gastrointestinal tract: nausea, vomiting, dyspepsia, pancreatitis, abdominal pain, thirst;
- liver and biliary tract: increased activity of alanine aminotransferase and aspartate aminotransferase, hepatitis;
- kidneys and urinary tract: enuresis (in children);
- musculoskeletal and connective tissue: myalgia (including muscle cramps), arthralgia;
- blood and lymphatic system: bleeding tendency, thrombocytopenia;
- skin and subcutaneous tissues: rash, itching, urticaria, a tendency to hematomas, erythema nodosum or multiforme, angioedema;
- immune system: allergic reactions, including anaphylaxis, eosinophilic liver infiltration.
In addition, infections of the upper tract, weakness, fatigue, edema and pyrexia are possible.
Usually side effects are fairly easy and do not require discontinuation of the drug.
Overdose
Symptoms of a Montelukast overdose (when taken at least 1000 mg per day): thirst, drowsiness, psychomotor agitation, vomiting, abdominal pain, mydriasis, headaches.
Symptomatic therapy is recommended.
special instructions
The appointment of Montelukast for acute attacks of bronchial asthma is not recommended, since its effectiveness in such cases has not been established. You should always carry emergency supplies for attacks of bronchial asthma (short-acting inhaled β2-agonists). During an exacerbation, you should continue taking the drug.
Patients with an allergy to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs are undesirable to take these drugs against the background of Montelukast therapy, since the drug is not able to completely prevent bronchoconstriction caused by their action.
Patients, as well as their parents and guardians, should take into account the possibility of developing neuropsychiatric symptoms that sometimes occur during therapy with Montelukast, although a causal relationship between its intake and these undesirable effects has not been established. If such symptoms appear, you should inform your doctor about them.
Rarely, eosinophilia, worsening pulmonary symptoms, rash, neuropathy, or cardiac complications, sometimes diagnosed as systemic eosinophilic vasculitis, have occurred with anti-asthma drugs. Sometimes these symptoms have occurred with dose reduction or withdrawal of oral corticosteroids. In this regard, patients taking Montelukast should be under appropriate supervision.
Film-coated tablets contain lactose monohydrate.
Chewable tablets contain aspartame equivalent to 0.842 mg phenylalanine.
Influence on the ability to drive vehicles and complex mechanisms
In connection with the possible development of such undesirable effects as dizziness and drowsiness, care should be taken during Montelukast therapy when driving vehicles and other complex mechanisms that require the speed of psychomotor reactions.
Application during pregnancy and lactation
With the post-registration use of montelukast by pregnant women, there have been cases of the development of congenital limb defects in newborns. The causal relationship of this phenomenon with taking montelukast has not been established, it was usually taken in combination with other drugs for the treatment of bronchial asthma.
The use of the drug during pregnancy / lactation is allowed only if the expected benefit to the mother outweighs the possible risk to the fetus / child.
Pediatric use
Montelukast chewable tablets are approved for use by children from 6 years old. For adolescents over 15 years of age, the usual adult dose is indicated.
With impaired renal function
According to the instructions, Montelukast is not excreted by the kidneys, and therefore no dose adjustment is required for patients with impaired renal function.
For violations of liver function
Patients with mild and moderate hepatic impairment do not need dose adjustment.
Use in the elderly
Correction of the dose of the drug is not required for elderly persons.
Drug interactions
- prednisone, theophylline, prednisolone, oral contraceptives, terfenadine, digoxin, warfarin: combined use is permitted;
- phenobarbital: AUC of montelukast decreases by 40%, dose adjustment is not required;
- paclitaxel, rosiglitazone, repaglinide and other drugs metabolized with the participation of the CYP 2C8 isoenzyme: montelukast has no effect on them;
- gemfibrozil: increases the effect of systemic exposure to montelukast by 4.4 times; this effect has no clinical significance, no dose adjustment of montelukast is required;
- trimethoprim and other known inhibitors of the isoenzyme CYP 2C8: no clinically significant interactions were noted, dose adjustment of montelukast is not required.
It is allowed to use Montelukast in combination therapy with bronchodilators and inhaled glucocorticosteroids. After achieving a stable effect, a gradual decrease in their dose is allowed. In some cases, even a complete abolition of inhaled glucocorticosteroids is possible, but they should not be abruptly replaced with Montelukast.
Analogs
The analogues of Montelukast are: Almont, Glemont, Monax, Monkasta, Montler, Montelar, Singlon, Singular, Ectalust.
Terms and conditions of storage
Store away from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life - 3 years (for film-coated tablets), 2 years (for chewable tablets).
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Montelukast
Reviews of Montelukast indicate its effectiveness in the fight against allergic cough and rhinitis. In addition, among the advantages are the pleasant taste of chewable tablets, which children like, as well as a lower price than their counterparts. The disadvantage is the risk of side effects, as well as the lack of immediate action of the drug.
Price for Montelukast in pharmacies
The approximate price for Montelukast is 496-590 rubles. (film-coated tablets, 10 mg, 30 pcs. in a package) or 550-665 rubles. (chewable tablets 5 mg, 28 pcs. per pack).
Montelukast: prices in online pharmacies
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Drug name Price Pharmacy |
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Montelukast tab. chewable 4 mg 10 pcs. 334 r Buy |
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Montelukast 10 mg film-coated tablets 30 pcs. 378 r Buy |
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Montelukast 5 mg chewable tablets 28 pcs. 450 RUB Buy |
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Montelukast 5 mg chewable tablets 30 pcs. 455 RUB Buy |
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Montelukast tab. p.p. 10mg 30 pcs. RUB 471 Buy |
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Montelukast 10 mg film-coated tablets 30 pcs. RUB 499 Buy |
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Montelukast tab. chewable 5 mg 30 pcs. 576 r 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!
