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Montelukast is an asthma medication. It belongs to a new class of substances: It prevents the attachment of certain tissue hormones (leukotrienes) to their binding site in the lungs and thus narrows the bronchi and provides increased mucus production. Montelukast is used as adjunctive therapy to prevent bronchial asthma when standard therapy (corticosteroids and beta-agonists) does not produce the desired result. It can also be used to prevent asthma during physical activity.
What is Montelukast?
Pharmacotherapeutic group: Anti-inflammatory antibronchoconstrictor agent – leukotriene receptor blocker.
ATX CODE: R03DC03
Form of production, composition and package
1 film-coated tablet 10 mg contains:
Active ingredient: Montelukast 10.00 mg (as Montelukast sodium 10.40 mg);
Excipients: The core is microcrystalline cellulose, type 102 89.30 mg, hyprolose 4.00 mg, croscarmellose sodium 6.00 mg, lactose monohydrate 89.30 mg, magnesium stearate 1.00 mg
Film Coating – Opadray II Beige 31F27012 (lactose monohydrate 1.440 mg, hypromellose 15cP 1.120 mg, titanium dioxide 1.011 mg, macrogol 4000 0.400 mg, iron oxide yellow dye 0.026 mg, iron oxide red dye 0.003 mg) 4.0 mg.
Shape: Square, rounded corners biconvex, beige colored film-coated tablets, labeled «М» on one side.
1 tablet 5 mg contains:
Active ingredient: montelukast sodium 5.2 mg, which corresponds to the content of Montelukast 5 mg.
Excipients: mannitol – 61.7 mg, sorbitol – 135 mg, low-substituted hyprolose – 6 mg, iron oxide red dye E172 – 1.5 mg, croscarmellose sodium – 24 mg, sodium cyclamate – 1.5 mg, microcrystalline cellulose – 60.3 mg, cherry flavoring – 1.8 mg, magnesium stearate – 3 mg.
Form: Pale pink, round, biconvex, chewable tablets with flecks of darker and white color.
1 tablet 4 mg contains:
Active ingredient: montelukast sodium 4.16 mg, which corresponds to the content of Montelukast 4 mg.
Excipients: mannitol – 49.36 mg, sorbitol – 108 mg, low-substituted hyprolose – 4.8 mg, iron oxide red dye E172 – 1.2 mg, croscarmellose sodium – 19.2 mg, sodium cyclamate – 1.2 mg, microcrystalline cellulose 48.24 mg, cherry flavoring – 1.44 mg, magnesium stearate – 2.4 mg.
Form: Pale pink, round, biconvex, chewable tablets with flecks of darker and white.
Indications for use Montelukast
- Prevention of daytime and nighttime symptoms of the disease;
- Treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid;
- Prevention of exercise-induced bronchospasm.
Management of daytime and nighttime symptoms of seasonal allergic rhinitis.
Prevention and long-term treatment of bronchial asthma in adults and children from 15 years of age, including prevention of daytime and nighttime symptoms of the disease, treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid and prevention of exercise-induced broychospasm; relief of daytime and nighttime symptoms of seasonal and/or year-round allergic rhinitis in adults and children from 15 years of age.
Contraindications
Hypersensitivity to any component of the drug — Childhood under 6 years old — phenylketonuria.
Dosage and administration of Montelukast
Montelukast, 4 mg chewable tablets, is indicated for use in children aged 2 to 5 years.
Montelukast, 5 mg chewable tablets, indicated for use in children 6 to 14 years of age.
Montelukast 10 mg
Orally once daily regardless of meals. For treatment of bronchial asthma the drug should be taken in the evening. For the treatment of allergic rhinitis the drug can be taken at any time of the day or night if the patient wishes. Patients with bronchial asthma and allergic rhinitis should take one tablet of Montelukast once daily in the evening. Adults and adolescents 15 years of age and older: one film-coated tablet (10 mg) per day. The therapeutic effect of montelukast on indicators reflecting the course of bronchial asthma develops within the first day. The patient should continue to take the drug both during the period of achieving control of bronchial asthma symptoms and during exacerbation of bronchial asthma. No special dosage adjustment is required for elderly patients, patients with renal insufficiency and for patients with mild or moderate hepatic impairment as well as for gender dependent patients. Montelukast can be added to a patient’s treatment with bronchodilators and inhaled glucocorticosteroids.
Montelukast 5 mg
Montelukast is taken orally once daily regardless of ingestion. The tablet may be swallowed whole or chewed before swallowing. For the treatment of bronchial asthma, the drug should be taken in the evening. In treatment of allergic rhinitis the drug can be taken at any time of day. Patients with bronchial asthma and allergic rhinitis should take 1 tablet once/day in the evening. Children ages 6 to 14 years 1 tablet chewable 5 mg once daily. No dose adjustment is required for this age group. Children over 15 years of age and adults The dose for adults and children over 15 years of age is 10 mg of Montelukast per day. The therapeutic effect of Montelukast on indicators reflecting the course of bronchial asthma develops within the first day. The patient should continue taking the drug both during the period of achieving control of bronchial asthma symptoms and during exacerbation of the disease. No special dosage adjustment is required for elderly patients, patients with renal insufficiency and patients with mild or moderate hepatic impairment. Montelukast may be added to treatment with bronchodilators and inhaled GCS.
Contraindications
Hypersensitivity to Montelukast or any other drug component; age under 15 years (for this dose of medicine); lactase deficiency, lactose intolerance and glucose-galactose malabsorption
Pharmacological action
Pharmacodynamics
Cysteinyl-leukotrienes (LTC4, LTD4, LTE4) are strong inflammatory mediators – eicosanoids – that are secreted by a variety of cells, including mast cells and eosinophils. These important proasthmatic mediators bind to cysteinyl leukotriene receptors. Cysteinyl-leukotriene type 1 receptors (CysLT1 receptors) are present in human airways (including bronchial smooth muscle cells, macrophages) and other pro-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 to an allergen, cysteinyl-leukotrienes are released from the pro-inflammatory cells of the nasal mucosa during the early and late phases of the allergic reaction, which manifests as symptoms of allergic rhinitis. An intranasal test with cysteinyl-leukotrienes demonstrated an increase in nasal airway resistance and symptoms of nasal obstruction.
Montelukast is a highly active oral medication that significantly improves inflammation in bronchial asthma. According to biochemical and pharmacological analysis, montelukast binds with high affinity and selectivity to CysLT1 receptors without interacting with other pharmacologically important receptors in the airways (such as prostaglandin, cholinergic or P-adrenergic receptors). Montelukast inhibits physiological action of cysteinyl-leukotrienes LTC4, LTD4, LTE4 by binding to CysLT1 -receptors, without having stimulating effect on these receptors. Montelukast inhibits CysLT1 receptors in the airways, as evidenced by its ability to block the development of bronchospasm in response to LTD4 inhalation in patients with bronchial asthma. A dose of 5 mg is sufficient to stop LTD4-induced bronchospasm. Montelukast induces bronchodilation within two hours after ingestion and may complement bronchodilation induced by beta2-adrenomimetics.
Use of montelukast in doses greater than 10 mg per day, taken once, does not increase the efficacy of the drug.
Pharmacokinetics
Montelukast is rapidly and almost completely absorbed after oral administration. In adults, when 10 mg film-coated tablets are taken on an empty stomach, the maximum concentration (Smah) is reached after 3 hours (Tmah). Average bioavailability when taken orally is 64%. Food intake does not affect the plasma Cmax and bioavailability of montelukast. Montelukast binds to plasma proteins by more than 99%. The volume of distribution of montelukast at equilibrium concentration averages 8-11 liters.
Studies with radioactively labeled montelukast in rats indicate minimal penetration through the blood-brain barrier. In addition, concentrations of labeled montelukast 24 hours after administration were minimal in all other tissues. Montelukast is actively metabolized. In therapeutic dose studies in adults and children, plasma concentrations of montelukast metabolites in equilibrium are undetectable. In vitro studies using human liver microsomes have shown that cygochrome P450 isoenzymes are involved in the metabolism of montelukast: WA4, 2A6 and 2C9. According to results of in vitro studies in human liver microsomes, in therapeutic concentration in blood plasma, Montelukast does not inhibit cytochrome P450 isoenzymes: ZA4, 2C9, 1A2, 2A6, 2C19 and 2D6. Plasma clearance of montelukast in healthy adults averages 45 mL/min. After oral administration of radioactively labeled montelukast, 86% of its amount is excreted through the intestine within 5 days and less than 0.2% – by the kidneys, which confirms that montelukast and its metabolites are excreted almost exclusively with bile. The half-life of montelukast in young healthy adults is 2.7 to 5.5 hours.
Montelukast pharmacokinetics remain nearly linear with oral doses over 50 mg. No differences in pharmacokinetics are observed when taking montelukast in the morning and evening hours. When taking 10 mg of montelukast once daily, a moderate (about 14%) accumulation of the active substance in blood plasma is observed.
Pharmacokinetics of montelukast in women and men are similar. With a single oral administration of 10 mg of montelukast, the pharmacokinetic profile and bioavailability are similar in elderly and younger patients. The plasma elimination half-life of montelukast is somewhat longer in elderly patients. No dose adjustment is required in elderly patients.
No differences in clinically relevant pharmacokinetic effects were found in patients of different races.
In patients with mild to moderate hepatic impairment and clinical manifestations of liver cirrhosis, a slowing of montelukast metabolism accompanied by an increase in the area under the pharmacokinetic curve has been noted «concentration – time» (AUC) by approximately 41% after a single oral dose of 10 mg of montelukast. The excretion of montelukast is slightly increased in these patients compared to healthy volunteers (mean elimination half time, 7.4 hours).
There is no need to change the dose of montelukast for patients with mild to moderate hepatic impairment. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic impairment (more than 9 points on the Child-Puo 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 for this group of patients. Pharmacokinetics of montelukast in patients with renal impairment has not been evaluated. Because montelukast and its metabolites are not excreted by the kidneys, no dose adjustment is required in this patient population. There are no data on the nature of montelukast pharmacokinetics in patients with severe hepatic impairment (more than 9 points on the Child-Pugh scale). When taking high doses of montelukast (20 and 60 times the recommended doses for adults), a decrease in plasma theophylline concentration is observed. This effect is not observed when taking montelukast in the recommended doses of 10 mg once a day.
Side effects
Nervous system and sensory organs:
Hallucinations, unusual vivid dreams, headache, sleep disturbances (including nightmares), somnambulism, drowsiness, agitation, irritability, aggressive behavior, insomnia, fatigue, paresthesias/hypesthesias, seizures, depression, anxiety, disorientation, tremor, suicidal thoughts and suicidal behavior, otitis.
Digestive system:
Nausea, dyspepsia, vomiting, abdominal pain, diarrhea, impaired liver function, jaundice and hepatitis (including fulminant), increased liver transaminases, cholestatic, hepatocellular and mixed forms of hepatitis, pancreatitis.
Musculoskeletal system:
Myalgia, arthralgia, muscle cramps.
Allergic reactions:
angioedema, anaphylaxis, rash, hypersensitivity reactions, urticaria, pruritus, eosinophilic liver infiltrates, erythema nodosa, erythema multiforme.
Other:
tendency to form subcutaneous hemorrhages, increased bleeding, nasal bleeding, palpitations, flu-like syndrome, edema, cough, pharyngitis, sinusitis, thrombocytopenia, upper respiratory infections, palpitations, pyrexia, Cerj-Strauss syndrome.
Special Indications
Montelukast is recommended for the treatment of acute attacks of bronchial asthma. Patients with bronchial asthma are always advised to carry emergency medications. Short-acting inhaled beta2-adrenomimetics should be used at the onset of an acute attack. Patients should consult their physician as soon as possible if they require more short-acting inhaled beta2-adrenomimetics than usual.
Montelukast should not be abruptly replaced with inhaled or oral GCS therapy. There is no evidence that a reduction in the dose of oral GCS with concomitant administration of montelukast is possible.
In rare cases, patients who receive anti-asthmatic drugs, including montelukast, may develop systemic eosinophilia, sometimes accompanied by clinical signs of vasculitis, the so-called Churg-Strauss syndrome, a condition that is treated by taking systemic GCS. These cases are usually associated with dose reduction or discontinuation of oral GCS therapy.
The possibility that leukotriene receptor antagonists may be associated with the development of Churg-Strauss syndrome cannot be excluded or established. Therefore, physicians should be alerted to the possibility of eosinophilia, vascular rash, increased severity of pulmonary symptoms, cardiac complications, and/or neuropathy in patients. Patients who have developed the above-mentioned symptoms should be reassessed and their treatment regimen reconsidered.
Treatment with Montelukast does not prevent bronchospasm in patients with hypersensitivity to acetylsalicylic acid when using acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.
The drug contains lactose monohydrate and should not be taken in patients with rare hereditary diseases: galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.
Effect on ability to operate motor vehicles and mechanisms
As a rule, taking montelukast does not affect the ability to drive or operate other machinery, but very rarely some patients have experienced drowsiness and dizziness. If these signs occur, patients should not drive vehicles or engage in other activities that require concentration and rapid psychomotor reactions.
Use in pregnancy and during breastfeeding
The use of Montelukast during pregnancy is possible if the expected benefits to the mother exceed the potential risk to the fetus. The decision to discontinue breastfeeding for the period of using Montelukast is taken on the basis of an assessment of the anticipated benefit to the mother and the potential risk to the child.
Overdose
Symptoms of drug overdose in patients with chronic bronchial asthma when administered at a dose greater than 200 mg per day for 22 weeks and at a dose of 900 mg per day for 1 week have not been identified.
There are reports of acute overdose of montelukast (when administered at least 1 g per day) in the post-marketing period and in clinical trials in adults and children. Clinical and laboratory data suggest a consistent safety profile in children, adults and elderly patients. The most common symptoms were feelings of thirst, drowsiness, vomiting, psychomotor agitation, headache, and abdominal pain.
Treatment: administration of symptomatic therapy. There are no data on the possibility of excretion of montelukast by peritoneal dialysis or hemodialysis.
Dosage and administration
Directly by mouth, once daily, with or without food. For the treatment of bronchial asthma, the drug should be taken in the evening. In the treatment of allergic rhinitis, the drug can be taken at any time of the day or night if the patient wishes.
Adults and children from 15 years of age: 1 tablet (10 mg) per day.
The therapeutic effect of the drug Montelukast on the symptoms reflecting the course of bronchial asthma is manifested within the first day. The patient should continue taking Montelukast both during the controlled course of bronchial asthma and during exacerbation of the disease.
For elderly patients, patients with renal insufficiency, patients with mild or moderate hepatic dysfunction, no dose adjustment is required. The dose of the drug is the same for female and male patients.
Interaction with other drugs
Administration of Montelukast at the same time as other asthma treatments
M-CAST can be used with other medications commonly used for prevention and long-term treatment of asthma. In studies of interactions with other drugs, the recommended clinical dose of montelukast had no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinylestradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.
Combined treatment with inhaled GCS
Treatment with Montelukast provides additional therapeutic benefit to patients using inhaled GCS. Once the condition has reached stabilization, a gradual reduction in the dose of GCS can be started under a physician’s supervision. In some cases, complete abolition of inhaled GCS is acceptable, but abrupt replacement of inhaled GCS with Montelukast is not recommended.In patients who simultaneously received phenobarbital, the area under the pharmacokinetic curve «Concentration-time» Montelukast decreased by about 40%, but no dosing regimen adjustment is required in these patients.
Combined treatment with bronchodilators
Montelukast is a reasonable adjunct to monotherapy with bronchodilators if the latter do not adequately control bronchial asthma. Once the therapeutic effect of treatment with Montelukast is achieved, a gradual reduction in the dose of bronchodilators may be initiated.
Since montelukast is metabolized by the CYP3A4 isoenzyme, caution should be exercised, especially in children, if montelukast is simultaneously used with CYP3A4 isoenzyme inducers, such as phenytoin, phenobarbital and rifampicin. Montelukast can be administered together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and/or allergic rhinitis.
Montelukast in recommended therapeutic dose had no clinically significant effect on pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinylestradiol/noretinodrel 35/1), terfenadine, digoxin and warfarin.
In vitro studies have shown that montelukast is a strong inhibitor of the CYP2C8 isoenzyme. However, in an in vivo drug interaction study of montelukast and rosiglitazone (a marker substrate, representative of drugs primarily metabolized by the CYP2C8 isoenzyme), there was no evidence of inhibition of the CYP2C8 isoenzyme by montelukast. Thus, in clinical practice, no effect of montelukast on the SUR2C8-mediated metabolism of a number of drugs, including.ч. paclitaxel, rosiglitazone, repaglinide.
In vitro studies have shown that montelukast is a substrate of the CYP2C8 isoenzyme, and to a lesser extent of the CYP2C9 and WA4 isoenzymes. Data from a clinical drug interaction study of montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the systemic effect of montelukast by 4.4 times. Co-administration of itraconazole, a strong CYP3A4 isoenzyme inhibitor, together with gemfibrozil and montelukast did not result in an additional increase in the systemic effects of montelukast. The effect of gemfibrozil on the systemic effects of montelukast cannot be considered clinically significant based on safety data when used at doses greater than the approved dose of 10 mg for adult patients (e.g., 200 mg/day for adult patients for 22 weeks and up to 900 mg/day for patients taking the drug for approximately one week no clinically significant adverse effects were observed).
Thus, no dose adjustment of montelukast is required when coadministered with gemfibrozil. In vitro studies suggest no clinically significant drug interactions with other known CYP2C8 isoenzyme inhibitors (e.g., trimethoprim). In addition, co-administration of montelukast with itraconazole alone did not significantly increase the systemic effects of montelukast.
In case of adverse reactions, including those not mentioned in the instructions for use, consult a physician.