(mon te loo' kast)
P / L : Caution during pregnancy and lactation
|| See TERMINOLOGY & ABBREVIATIONS ||
|Indication(s) & Dosage||
Montelukast is indicated in the treatment of asthma as add-on therapy in those patients with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom 'as-needed' short acting Beta-agonists provide inadequate clinical control of asthma. In those asthmatic patients in whom Montelukast is indicated in asthma, Montelukast can also provide symptomatic relief of seasonal allergic rhinitis.
Montelukast is also indicated in the prophylaxis of asthma in which the predominant component is exercise-induced bronchoconstriction.
|RECENT MAJOR CHANGES||
Warnings and Precautions (US FDA)
See Brand Manufacturer's Prescribing Information for details.
No specific information is available on the treatment of overdose with montelukast. In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to patients for 22 weeks and in short term studies, up to 900 mg/day to patients for approximately one week without clinically important adverse experiences.
There have been reports of acute overdose in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1000 mg (approximately 61 mg/kg in a 42 month old child). The clinical and laboratory findings observed were consistent with the safety profile in adults and paediatric patients. There were no adverse experiences in the majority of overdose reports. The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.
It is not known whether montelukast is dialysable by peritoneal- or haemodialysis.
|Warning & Precautions||
|Adverse Drug Reaction(s)||Dizziness, fatigue, fever; rash; abdominal pain, dyspepsia, dental pain, gastroenteritis; increased AST; weakness; cough, nasal congestion. Aggression, agitation, angioedema, arthralgia, bleeding tendency, bruising, cholestasis, diarrhoea, dream abnormalities, drowsiness, oedema, eosinophilia, hallucinations, hepatic eosinophilic infiltration (rare), hepatitis, hypersensitivity, hypoaesthesia, insomnia, irritability, muscle cramps, myalgia, nausea, palpitation, pancreatitis, paraesthesia, pruritus, restlessness, seizure, urticaria, vasculitis, vomiting.
Potentially Fatal: Anaphylaxis, Churg-Strauss syndrome.
Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma. In drug-interactions studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following medicinal products: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/ norethindrone 35/1), terfenadine, digoxin and warfarin.
The area under the plasma concentration curve (AUC) for montelukast was decreased approximately 40% in subjects with co-administration of phenobarbital. Since montelukast is metabolised by CYP 3A4, 2C8, and 2C9, caution should be exercised, particularly in children, when montelukast is co-administered with inducers of CYP 3A4, 2C8, and 2C9, such as phenytoin, phenobarbital and rifampicin.
In vitro studies have shown that montelukast is a potent inhibitor of CYP 2C8. However, data from a clinical drug-drug interaction study involving montelukast and rosiglitazone (a probe substrate representative of medicinal products primarily metabolized by CYP 2C8) demonstrated that montelukast does not inhibit CYP 2C8 in vivo. Therefore, montelukast is not anticipated to markedly alter the metabolism of medicinal products metabolised by this enzyme (e.g., paclitaxel, rosiglitazone, and repaglinide.)
In vitro studies have shown that montelukast is a substrate of CYP 2C8, and to a less significant extent, of 2C9, and 3A4. In a clinical drug-drug interaction study involving montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) gemfibrozil increased the systemic exposure of montelukast by 4.4-fold. No routine dosage adjustment of montelukast is required upon co-administration with gemfibrozil or other potent inhibitors of CYP 2C8, but the physician should be aware of the potential for an increase in adverse reactions.
Based on in vitro data, clinically important drug interactions with less potent inhibitors of CYP 2C8 (e.g., trimethoprim) are not anticipated. Co-administration of montelukast with itraconazole, a strong inhibitor of CYP 3A4, resulted in no significant increase in the systemic exposure of montelukast.
|Food Interaction||Serum levels may be reduced with St John's wort.|
|Pregnancy Category (FDA)||
Pregnancy Category B.
Use during pregnancy
Animal studies do not indicate harmful effects with respect to effects on pregnancy or embryonal/foetal development.
Limited data from available pregnancy databases do not suggest a causal relationship between Montelukast and malformations (i.e. limb defects) that have been rarely reported in worldwide post marketing experience.
Montelukast may be used during pregnancy only if it is considered to be clearly essential.
Use during lactation
Studies in rats have shown that montelukast is excreted in milk. It is not known if montelukast is excreted in human milk.
Montelukast may be used in breast-feeding only if it is considered to be clearly essential.
|Storage||Oral: Store at 15-30°C (59-86°F). Protect from moisture and light.|
The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released from various cells including mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT1) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). CysLTs have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both early- and late-phase reactions and are associated with symptoms of allergic rhinitis. Intranasal challenge with CysLTs has been shown to increase nasal airway resistance and symptoms of nasal obstruction.
Montelukast is an orally active compound which binds with high affinity and selectivity to the CysLT1 receptor. In clinical studies, montelukast inhibits bronchoconstriction due to inhaled LTD4 at doses as low as 5 mg. Bronchodilation was observed within 2 hours of oral administration. The bronchodilation effect caused by aBeta-agonist was additive to that caused by montelukast. Treatment with montelukast inhibited both early- and late-phase bronchoconstriction due to antigen challenge. Montelukast, compared with placebo, decreased peripheral blood eosinophils in adult and paediatric patients. In a separate study, treatment with montelukast significantly decreased eosinophils in the airways (as measured in sputum) and in peripheral blood while improving clinical asthma control.
In studies in adults, montelukast, 10 mg once daily, compared with placebo, demonstrated significant improvements in morning FEV1 (10.4% vs 2.7% change from baseline), AM peak expiratory flow rate (PEFR) (24.5 L/min vs 3.3 L/min change from baseline), and significant decrease in total Beta-agonist use (-26.1% vs -4.6% change from baseline). Improvement in patient-reported daytime and nighttime asthma symptoms scores was significantly better than placebo.
Studies in adults demonstrated the ability of montelukast to add to the clinical effect of inhaled corticosteroid (% change from baseline for inhaled beclometasone plus montelukast vs beclometasone, respectively for FEV1: 5.43% vs 1.04%;Beta-agonist use: -8.70% vs 2.64%). Compared with inhaled beclometasone (200 Î¼g twice daily with a spacer device), montelukast demonstrated a more rapid initial response, although over the 12-week study, beclometasone provided a greater average treatment effect (% change from baseline for montelukast vs beclometasone, respectively for FEV1: 7.49% vs 13.3%;Beta-agonist use: -28.28% vs -43.89%). However, compared with beclometasone, a high percentage of patients treated with montelukast achieved similar clinical responses (e.g., 50% of patients treated with beclometasone achieved an improvement in FEV1 of approximately 11% or more over baseline while approximately 42% of patients treated with montelukast achieved the same response).
A clinical study was conducted to evaluate montelukast for the symptomatic treatment of seasonal allergic rhinitis in adult asthmatic patients 15 years of age and older with concomitant seasonal allergic rhinitis. In this study, montelukast 10 mg tablets administered once daily demonstrated a statistically significant improvement in the Daily Rhinitis Symptoms score, compared with placebo. The Daily Rhinitis Symptoms score is the average of the Daytime Nasal Symptoms score (mean of nasal congestion, rhinorrhea, sneezing, nasal itching) and the Nighttime Symptoms score (mean of nasal congestion upon awakening, difficulty going to sleep, and nighttime awakenings scores). Global evaluations of allergic rhinitis by patients and physicians were significantly improved, compared with placebo. The evaluation of asthma efficacy was not a primary objective in this study.
In an 8-week study in paediatric patients 6 to 14 years of age, montelukast 5 mg once daily, compared with placebo, significantly improved respiratory function (FEV1 8.71% vs 4.16% change from baseline; AM PEFR 27.9 L/min vs 17.8 L/min change from baseline) and decreased "as-needed"Beta-agonist use (-11.7% vs +8.2% change from baseline).
Significant reduction of exercise-induced bronchoconstriction (EIB) was demonstrated in a 12-week study in adults (maximal fall in FEV1 22.33% for montelukast vs 32.40% for placebo; time to recovery to within 5% of baseline FEV144.22 min vs 60.64 min). This effect was consistent throughout the 12-week study period. Reduction in EIB was also demonstrated in a short term study in paediatric patients (maximal fall in FEV1 18.27% vs 26.11%; time to recovery to within 5% of baseline FEV1 17.76 min vs 27.98 min). The effect in both studies was demonstrated at the end of the once-daily dosing interval.
In aspirin-sensitive asthmatic patients receiving concomitant inhaled and/or oral corticosteroids, treatment with montelukast, compared with placebo, resulted in significant improvement in asthma control (FEV1 8.55% vs -1.74% change from baseline and decrease in totalBeta-agonist use -27.78% vs 2.09% change from baseline).
Montelukast is a selective leukotriene receptor antagonist that blocks the effects of cysteinyl leukotrienes in the airways.
|ATC Classification||R03DC03 - montelukast; Belongs to the class of other systemic drugs used in the treatment of obstructive airway diseases, leukotriene receptor antagonists.|
|Brand Name||Manufacturer/Marketer||Composition||Dosage Form||Pack Size & Price|
|AERON 10||Healthcare Pharmacuticals Ltd.||Montelukast Sodium INN equivalent to Montelukast 10mg||Tablet||30's MRP 450 Tk|
|AERON 4||Healthcare Pharmacuticals Ltd.||Montelukast Sodium INN equivalent to Montelukast 4mg||Tablet||30's MRP 180 Tk|
|AERON 5||Healthcare Pharmacuticals Ltd.||Montelukast Sodium INN equivalent to Montelukast 5mg||Tablet||30's MRP 240 Tk|
|AROKAST||Navana Pharmaceuticals Limited||Montelukast sodium INN 4mg & 5mg,10mg||Tablet||4mg & 5mg x30's, 10mg x10's: 150.00, 210.00 & 100.00 MRP|
|AROVENT 10||Orion Pharma Ltd.||Montelukast sodium INN 10mg||Tablet||10's: 200.80 MRP|
|ASMONT||Somatec Pharmaceuticals Ltd.||Montelukast sodium INN 5mg & 10mg||Tablet||10's each: 85.30 & 150.50 MRP|
|LUMENTA 10||Sandoz/Novartis||Montelukast Sodium INN equivalent to Montelukast 5mg||Tablet||2x14's, MRP 448.00|
|LUMENTA 5||Sandoz/Novartis||Montelukast Sodium INN equivalent to Montelukast 10mg||Chewable Tablet||20's, MRP 180.00|
|LUMONA 10||Eskayef Bangladesh Ltd||Montelukast Sodium INN equivalent to Montelukast 10mg||Tablet||10's & 20's MRP: 100.00 & 200.00|
|LUMONA 4||Eskayef Bangladesh Ltd||Montelukast Sodium INN equivalent to Montelukast 4mg granules||Granules||10's & 30's MRP: 60.00 & 180.00|
|LUMONA 5||Eskayef Bangladesh Ltd||Montelukast Sodium INN equivalent to Montelukast 5mg||Tablet||10's & 30's MRP: 60.00 & 180.00|
|M-KAST||Drug International Ltd||Montelukast sodium INN 4mg & 5mg,10mg||Tablet||4mg & 5mg x30's: 150.00 & 210.00; 10mg x20's: 240.00 MRP|
|M-LUKAS||Popular Pharmaceuticals Ltd.||Montelukast sodium INN 4mg & 5mg,10mg||Tablet||4mg & 5mg x30's: 180.00 & 240.00; 10mg x10's: 150.00 MRP|
|MOKAST||Alco Pharma Ltd||Montelukast sodium INN 4mg & 10mg||Tablet||4mg x20's, 10mg x10's: 120.00 & 100.00 MRP|
|MOLUKAT||Kemiko Pharmaceuticals Ltd||Montelukast sodium INN 4mg & 5mg,10mg||Tablet||20's each: 120.00, 160.00 & 240.00 MRP|
|MOLUS||Apex Pharmaceuticals Ltd.||Montelukast sodium INN 4mg & 10mg/||Tablet||10's each: 70.00 & 150.00 MRP|
|MONARK-10||Hallmark Pharmaceuticals Ltd||Montelukast sodium INN 10mg||Tablet||20's: 400.00 MRP|
|MONAS||The Acme Laboratories Ltd.||Montelukast sodium INN 4mg & 5mg,10mg||Tablet||4mg x5's & 30's: 30.10 & 180.60; 5mg x5's & 30's: 40.20 & 241.20; 10mgx 5's & 15's: 75.25 & 225.75 MRP|
|MONOCAST 10||Beximco Pharmaceuticals Ltd||Montelukast Sodium INN equivalent to Montelukast 10mg||Tablet||10's & 20's: 140.00 & 280.00 MRP|
|MONOCAST 4||Beximco Pharmaceuticals Ltd||Montelukast Sodium INN eq. to Montelukast 4mg||Tablet||20's: 110.00 MRP|
|MONOCAST 5||Beximco Pharmaceuticals Ltd||Montelukast Sodium INN eq. to Montelukast 5mg||Tablet||20's: 150.00 MRP|
|MONOCAST Granules||Beximco Pharmaceuticals Ltd||Montelukast Sodium INN equivalent to Montelukast 4mg granules sachet||Sachet||30's: 240.00 MRP|
|Montair 10||Incepta Pharmaceuticals Limited||Montelukast Sodium INN equivalent to Montelukast 10mg||Tablet||10x3's:MRP 450 Tk|
|Montair 4||Incepta Pharmaceuticals Limited||Montelukast Sodium INN equivalent to Montelukast 4mg||Chewable Tablet||10x3's:MRP 180 Tk|
|Montair 5||Incepta Pharmaceuticals Limited||Montelukast Sodium INN equivalent to Montelukast 5mg||Chewable Tablet||10x3's:MRP 240 Tk|
|MONTECAST 10||Pacific Pharmaceuticals Ltd.||Montelukast sodium INN 10mg||Tablet||20's: 300.00 MRP|
|MONTEK||Sun Pharmaceutical (Bangladesh) Ltd.||Montelukast sodium INN 4mg & 10mg/||Tablet||30's each: 210.00 & 450.00 MRP|
|MONTENE 10||Square Pharmaceuticals Ltd.||Montelukast 10mg||Tablet||2x10's: 301.00 MRP|
|MONTENE 4||Square Pharmaceuticals Ltd.||Montelukast 4mg||Chewable Tablet||2x10's: 120.4 MRP|
|MONTENE 5||Square Pharmaceuticals Ltd.||Montelukast 5mg||Chewable Tablet||2x10's: 160.60 MRP|
|MONTEX||IBN SINA Pharmaceutical Industry Ltd.||Montelukast sodium INN 5mg & 10mg||Tablet||5mg x20's, 10mg x10's: 160.00 IP each|
|MONTIFAST 10||Globe Pharmaceuticals Ltd||Montelukast sodium INN 10mg||Tablet||20's: 300.00 MRP|
|MONTIFAST 4 Chew||Globe Pharmaceuticals Ltd||Montelukast sodium INN 4mg||Tablet(chewable)||20's: 140.00 MRP|
|MONTRIL-10||Aristopharma Ltd.||Montelukast sodium INN 10mg||Tablet||20's: 300.00 MRP|
|MONTRIL-4 Oroflash||Aristopharma Ltd.||Montelukast sodium INN 4mg||Tablet(oroflash)||30's: 210.00 MRP|
|MONTRIL-5 Chew||Aristopharma Ltd.||Montelukast sodium INN 5mg||Tablet(chewable)||30's: 240.00 MRP|
|ODMON||Renata Limited||Montelukast sodium INN 5mg & 10mg||Tablet||10's each: 150.00 & 300.00 MRP|
|PROVAIR 10||Unimed & Unihealth Manufacturers Ltd.||Montelukast sodium INN 10mg||Tablet||20's: 300.00 MRP|
|PROVAIR Chew||Unimed & Unihealth Manufacturers Ltd.||Montelukast sodium INN 4mg & 5mg||Tablet(chewable)||20's each: 120.00 & 160.00 MRP|
|REVERSAIR||ACI Ltd.||Montelukast sodium INN 10mg||Tablet||20's: 301.20 MRP|
|REVERSAIR OD||ACI Ltd.||Montelukast sodium INN 4mg & 5mg||Tablet||20's each: 140.60 & 160.60 MRP|
|TELUKAST||General Pharmaceuticals Ltd||Montelukast sodium INN 10mg||Tablet||30's: 450.00 MRP|
|TRILOCK||Opsonin Pharma Limited||Montelukast sodium INN 4mg & 5mg,10mg||Tablet||30's each: 180.00, 240.00 & 450.00 MRP|
Why is this medication prescribed?
Montelukast is used to prevent wheezing, difficulty breathing, chest tightness, and coughing caused by asthma. Montelukast is also used to prevent bronchospasm (breathing difficulties) during exercise. Montelukast is also used to treat the symptoms of seasonal (occurs only at certain times of the year), and perennial (occurs all year round) allergic rhinitis (a condition associated with sneezing and stuffy, runny or itchy nose). Montelukast is in a class of medications called leukotriene receptor antagonists (LTRAs). It works by blocking the action of substances in the body that cause the symptoms of asthma and allergic rhinitis.
How should this medicine be used?
Montelukast comes as a tablet, a chewable tablet, and granules to take by mouth. Montelukast is usually taken once a day with or without food. When montelukast is used to treat asthma, it should be taken in the evening. When montelukast is used to prevent breathing difficulties during exercise, it should be taken at least 2 hours before exercise. If you are taking montelukast once a day on a regular basis, you should not take an additional dose before exercising. When montelukast is used to treat allergic rhinitis, it may be taken at any time of day. Take montelukast at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor to explain any part you do not understand. Take montelukast exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
If you are giving the granules to your child, you should not open the foil pouch until your child is ready to take the medication. There are several ways that you can give the granules to your child, so choose the one that works best for you and your child. You may pour all of the granules directly from the packet into your child's mouth to be swallowed immediately. You may also pour the entire packet of granules onto a clean spoon and place the spoonful of medication in your child's mouth. If you prefer, you may mix the entire packet of granules in 1 teaspoon (5 mL) of cold or room temperature baby formula, breastmilk, applesauce, soft carrots, ice cream, or rice. You should not mix the granules with any other foods or liquids, but your child may drink any liquid right after he or she takes the granules. If you mix the granules with one of the allowed foods or drinks, use the mixtures within 15 minutes. Do not store unused mixtures of food, formula, or breast milk and the medication.
Do not use montelukast to treat a sudden attack of asthma symptoms. Your doctor will prescribe a short-acting inhaler to use during attacks. Talk to your doctor about how to treat symptoms of a sudden asthma attack. If your asthma symptoms get worse or if you have asthma attacks more often, be sure to call your doctor.
If you are taking montelukast to treat asthma, continue to take or use all other medications that your doctor has prescribed to treat your asthma. Do not stop taking any of your medications or change the doses of any of your medications unless your doctor tells you that you should. If your asthma is made worse by aspirin, do not take aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs) during your treatment with montelukast.
Montelukast controls the symptoms of asthma and allergic rhinitis but does not cure these conditions. Continue to take montelukast even if you feel well. Do not stop taking montelukast without talking to your doctor.
Other uses for this medicine
This medication may be prescribed for other uses; ask your doctor for more information.
What special precautions should I follow?
Before taking montelukast,
- tell your doctor if you are allergic to montelukast or any other medications.
- tell your doctor what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention phenobarbital and rifampin. Your doctor may need to change the doses of your medications or monitor you more carefully for side effects.
- tell your doctor if you have or have ever had liver disease.
- tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking montelukast, call your doctor.
- you should know that your mental health may change in unexpected ways while you are taking montelukast. You should call your doctor right away if you experience any of the following symptoms: agitation, aggressive behavior, anxiety, irritability, unusual dreams, hallucinations (seeing things or hearing voices that do not exist), depression, difficulty falling asleep or staying sleep, restlessness, sleep walking, suicidal thoughts or actions (thinking about harming or killing yourself or planning or trying to do so), or tremor (uncontrollable shaking of a part of the body). Your doctor will decide if you should continue taking montelukast.
- if you have phenylketonuria (PKU, an inherited condition in which a special diet must be followed to prevent mental retardation), you should know that the chewable tablets contain aspartame that forms phenylalanine.
What special dietary instructions should I follow?
Unless your doctor tells you otherwise, continue your normal diet.
What should I do if I forget a dose?
Skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one. Do not take more than one dose of montelukast in a 24 hour period.
What side effects can this medication cause?
Montelukast may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
Some side effects can be serious. If you experience any of the following symptoms or those listed in the SPECIAL PRECAUTIONS section, call your doctor immediately:
difficulty breathing or swallowing
swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
pins and needles or numbness in the arms or legs
pain and swelling of the sinuses
Montelukast may cause other side effects. Call your doctor if you have any unusual problems while you are taking this medication.
What should I know about storage and disposal of this medication?
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
In case of emergency/overdose
In case of overdose, consult your doctor. If the victim has collapsed or is not breathing, consult local medical emergency services.
Symptoms of overdose may include:
restlessness or agitation
What other information should I know?
Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests to check your response to this medicine.
Do not let anyone else use your medication. If you still have symptoms and need further treatment, consult your doctor.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
Ref: U.S. National Library of Medicine.
This information is provided for reference only and not a replacement for and should only be used in conjunction with full consultation with a registered medical practitioner. It may not contain all the available information you require and cannot substitute professional medical care, nor does it take into account all individual circumstances. Although great effort has been made to ensure content accuracy, mph-bd shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise.
|| See FDA approved Brand Manufacturer's Prescribing Information |
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