Montelukast Sodium 4 mg Granule, 15,000-count
🆔 Identity & classification
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🏭 Manufacturer & labeler
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🩺 Clinical
Montelukast is used to prevent wheezing, difficulty breathing, chest tightness, and coughing caused by asthma in adults and children 12 months of age and older. Montelukast is also used to prevent bronchospasm (breathing difficulties) during exercise in adults and children 6 years of age and older. Montelukast is also used to treat the symptoms of seasonal (occurs only at certain times of the year), allergic rhinitis (a condition associated with sneezing and stuffy, runny or itchy nose) in adults and children 2 years of age and older, and perennial (occurs all year round) allergic rhinitis in...
Read the full MedlinePlus article ↗- It does more than just treat allergies. Montelukast is used to help prevent and control asthma on a daily basis, to prevent breathing problems triggered by exercise, and to relieve...
- What is montelukast actually used for — is it just for allergies?
- This is a real and important concern — the FDA has placed its strongest warning on montelukast because of reported mental health side effects. These can include mood changes, agita...
- I heard montelukast can affect your mood. Should I be worried?
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII 0VUT3PMY82
Hypromellose 2910 is a plant-derived thickening agent made from cellulose. In medicines, it forms protective coatings on tablets or capsules, controls how fast the drug releases, and thickens liquid formulations.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 3OWL53L36A
A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
3 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.813 | $12,189.00 / 15000 granules |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Montelukast Sodium 4 mg/500mg 13668-0531-94 | Torrent | 30 packets | $0.813 | AB | Availability likely | — |
| Montelukast Sodium 4 mg 27241-0015-31 | Ajanta | 30 granules | $0.813 | AB | Availability likely | — |
| Montelukast Sodium 4 mg 59651-0329-30 | Aurobindo | 30 granules | $0.813 | AB | Availability likely | — |
| Montelukast Sodium 4 mgthis 55111-0763-03 | Dr.Reddy's | 15000 granules | $0.813 | AB | Discontinued | — |
| Singulair 4 mg 78206-0171-01 | Organon | 30 granules | — | — | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 55111-0763-03 You're viewing this | 30 PACKET in 1 CARTON (55111-763-03) / 500 GRANULE in 1 PACKET (55111-763-07) | 2012-09-20 | Inactivated by FDA |
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | ✓ Available |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Montelukast sodium is a leukotriene receptor antagonist indicated for: • Prophylaxis and chronic treatment of asthma in patients 12 months of age and older ( 1 .1 ). • Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 6 months of age and older (1.3 ).
1.1Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in pediatric patients 12 months of age and older.
1.3Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 6 months of age and older.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Administration (by indications): Asthma (2.1) : Once daily in the evening for patients 12 months and older. Seasonal allergic rhinitis (2.3) : Once daily for patients 2 years and older. Perennial allergic rhinitis (2.3) : Once daily for patients 6 months and older.
Dosage (by age) ( 2 ): 2 to 5 years: one packet of 4 mg oral granules. 6 to 23 months: one packet of 4 mg oral granules. Patients with both asthma and allergic rhinitis should take only one dose daily in the evening (2.4) .
For oral granules: Must administer within 15 minutes after opening the packet (with or without mixing with food) (2.5) .
2.1Asthma Montelukast sodium should be taken once daily in the evening. The following doses are recommended: For pediatric patients 2 to 5 years of age: one packet of 4 mg oral granules . For pediatric patients 12 to 23 months of age: one packet of 4 mg oral granules.
Safety and effectiveness in pediatric patients less than 12 months of age with asthma have not been established. There have been no clinical trials in patients with asthma to evaluate the relative efficacy of morning versus evening dosing. The pharmacokinetics of montelukast are similar whether dosed in the morning or evening.
Efficacy has been demonstrated for asthma when montelukast was administered in the evening without regard to time of food ingestion.
2.3Allergic Rhinitis For allergic rhinitis, montelukast sodium should be taken once daily. Efficacy was demonstrated for seasonal allergic rhinitis when montelukast was administered in the morning or the evening without regard to time of food ingestion. The time of administration may be individualized to suit patient needs.
The following doses for the treatment of symptoms of seasonal allergic rhinitis are recommended: For pediatric patients 2 to 5 years of age: one packet of 4 mg oral granules. Safety and effectiveness in pediatric patients younger than 2 years of age with seasonal allergic rhinitis have not been established. The following doses for the treatment of symptoms of perennial allergic rhinitis are recommended: For pediatric patients 2 to 5 years of age: one packet of 4 mg oral granules.
For pediatric patients 6 to 23 months of age: one packet of 4 mg oral granules. Safety and effectiveness in pediatric patients younger than 6 months of age with perennial allergic rhinitis have not been established.
2.4Asthma and Allergic Rhinitis Patients with both asthma and allergic rhinitis should take only one montelukast sodium dose daily in the evening.
2.5Instructions for Administration of Oral Granules Montelukast sodium 4 mg (montelukast) oral granules can be administered either directly in the mouth, dissolved in 1 teaspoonful (5 mL) of cold or room temperature baby formula or breast milk, or mixed with a spoonful of cold or room temperature soft foods; based on stability studies, only applesauce, carrots, rice, or ice cream should be used. The packet should not be opened until ready to use. After opening the packet, the full dose (with or without mixing with baby formula, breast milk, or food) must be administered within 15 minutes.
If mixed with baby formula, breast milk, or food, montelukast sodium oral granules must not be stored for future use. Discard any unused portion. Montelukast sodium oral granules are not intended to be dissolved in any liquid other than baby formula or breast milk for administration.
However, liquids may be taken subsequent to administration. Montelukast sodium oral granules can be administered without regard to the time of meals.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Montelukast sodium 4 mg (montelukast) oral granules are white to off white granular powder packed in aluminum foil packet. • Montelukast sodium 4 mg (montelukast) oral granules ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Hypersensitivity to any component of this product. Hypersensitivity to any component of this product ( 4 ).
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Do not prescribe montelukast sodium to treat an acute asthma attack ( 5.1 ). • Advise patients to have appropriate rescue medication available ( 5.1 ). • Inhaled corticosteroid may be reduced gradually. Do not abruptly substitute montelukast sodium for inhaled or oral corticosteroids ( 5.2 ). • Patients with known aspirin sensitivity should continue to avoid aspirin or non-steroidal anti-inflammatory agents while taking montelukast sodium ( 5.3 ). • Neuropsychiatric events have been reported with montelukast sodium.
Instruct patients to be alert for neuropsychiatric events. Evaluate the risks and benefits of continuing treatment with montelukast sodium if such events occur ( 5.4 and 6.2 ). • Systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, has been reported. These events have been sometimes associated with the reduction of oral corticosteroid therapy ( 5.5 and 6.2 ).
5.1Acute Asthma Montelukast sodium is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Patients should be advised to have appropriate rescue medication available. Therapy with montelukast sodium can be continued during acute exacerbations of asthma. Patients who have exacerbations of asthma after exercise should have available for rescue a short-acting inhaled β-agonist.
5.2Concomitant Corticosteroid Use While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, montelukast sodium should not be abruptly substituted for inhaled or oral corticosteroids.
5.3Aspirin Sensitivity Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking montelukast sodium. Although montelukast sodium is effective in improving airway function in asthmatics with documented aspirin sensitivity, it has not been shown to truncate bronchoconstrictor response to aspirin and other non-steroidal anti-inflammatory drugs in aspirin-sensitive asthmatic patients (see Clinical Studies (14.1) ].
5.4Neuropsychiatric Events Neuropsychiatric events have been reported in adult, adolescent, and pediatric patients taking montelukast sodium. Post-marketing reports with montelukast sodium use include, but are not limited to, agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, dysphemia (stuttering), hallucinations, insomnia, irritability, memory impairment, obsessive-compulsive symptoms, restlessness, somnambulism, suicidal thinking and behavior (including suicide), tic and tremor.
The clinical details of some post-marketing reports involving montelukast sodium appear consistent with a drug-induced effect. Patients and prescribers should be alert for neuropsychiatric events. Patients should be instructed to notify their prescriber if these changes occur.
Prescribers should carefully evaluate the risks and benefits of continuing treatment with montelukast sodium if such events occur (see Adverse Reactions (6.2) ].
5.5Eosinophilic Conditions Patients with asthma on therapy with montelukast sodium may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. These events have been sometimes associated with the reduction of oral corticosteroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients.
A causal association between montelukast sodium and these underlying conditions has not been established [see Adverse Reactions (6.2) ].
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Most common adverse reactions (incidence ≥5% and greater than placebo listed in descending order of frequency): upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy’s Laboratories, Inc. at 1-888-375-3784 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. In the following description of clinical trials experience, adverse reactions are listed regardless of causality assessment. The most common adverse reactions (incidence ≥5% and greater than placebo ; listed in descending order of frequency) in controlled clinical trials were: upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis.
Adults and Adolescents 15 Years of Age and Older with Asthma Montelukast sodium has been evaluated for safety in approximately 2950 adult and adolescent patients 15 years of age and older in clinical trials. In placebo-controlled clinical trials, the following adverse experiences reported with montelukast sodium occurred in greater than or equal to 1% of patients and at an incidence greater than that in patients treated with placebo: Table 1: Adverse Experiences Occuring in ≥ 1% of Patients with an Incidence Greater than that in Patients Treated with Placebo Montelukast Sodium 10 mg /day (montelukast) (%) (n=1955) Placebo (%) (n=1180) Body As A Whole Pain, abdominal 2.9
2.5Asthenia/fatigue 1.8
1.2Fever 1.5
0.9 Trauma 1
0.8Digestive System Disorders Dyspepsia 2.1
1.1Pain, dental 1.7 1 Gastroenteritis, infectious 1.5
0.5Nervous System/Psychiatric Headache 18.4
18.1Dizziness 1.9
1.4Respiratory System Disorders Influenza 4.2
3.9Cough 2.7
2.4Congestion, nasal 1.6
1.3Skin/Skin Appendages Disorder Rash 1.6
1.2Laboratory Adverse Experiences* ALT increased 2.1 2 AST increased 1.6
1.2Pyuria 1 0.9 * Number of patients tested (montelukast sodium and placebo, respectively): ALT and AST, 1935, 1170; pyuria, 1924, 1159. The frequency of less common adverse events was comparable between montelukast sodium and placebo. Cumulatively, 569 patients were treated with montelukast sodium for at least 6 months, 480 for one year, and 49 for two years in clinical trials.
With prolonged treatment, the adverse experience profile did not significantly change. Pediatric Patients 6 to 14 Years of Age with Asthma Montelukast sodium has been evaluated for safety in 476 pediatric patients 6 to 14 years of age. Cumulatively, 289 pediatric patients were treated with montelukast sodium for at least 6 months, and 241 for one year or longer in clinical trials.
The safety profile of montelukast sodium in the 8-week, double-blind, pediatric efficacy trial was generally similar to the adult safety profile. In pediatric patients 6 to 14 years of age receiving montelukast sodium, the following events occurred with a frequency ≥2% and more frequently than in pediatric patients who received placebo: pharyngitis, influenza, fever, sinusitis, nausea, diarrhea, dyspepsia, otitis, viral infection, and laryngitis. The frequency of less common adverse events was comparable between montelukast sodium and placebo.
With prolonged treatment, the adverse experience profile did not significantly change. In studies evaluating growth rate, the safety profile in these pediatric patients was consistent with the safety profile previously described for montelukast sodium. In a 56-week, double-blind study evaluating growth rate in pediatric patients 6 to 8 years of age receiving montelukast sodium, the following events not previously ob…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS No dose adjustment is needed when montelukast sodium is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, terfenadine, digoxin, warfarin, gemfibrozil, itraconazole, thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, decongestants, and Cytochrome P450 (CYP) enzyme inducers [see Clinical Pharmacology (12.3) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Available data from published prospective and retrospective cohort studies over decades with montelukast use in pregnant women have not established a drug-associated risk of major birth defects [see Data] . In animal reproduction studies, no adverse developmental effects were observed with oral administration of montelukast to pregnant rats and rabbits during organogenesis at doses approximately 100 and 110 times, respectively, the maximum recommended human daily oral dose (MRHDOD) based on AUCs [see Data] .
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly or moderately controlled asthma in pregnancy increases the maternal risk of perinatal adverse outcomes such as preeclampsia and infant prematurity, low birth weight, and small for gestational age. Data Human Data Published data from prospective and retrospective cohort studies have not identified an association with montelukast sodium use during pregnancy and major birth defects. Available studies have methodologic limitations, including small sample size, in some cases retrospective data collection, and inconsistent comparator groups.
Animal Data In embryo-fetal development studies, montelukast administered to pregnant rats and rabbits during organogenesis (gestation days 6 to 17 in rats and 6 to 18 in rabbits) did not cause any adverse developmental effects at maternal oral doses up to 400 and 300 mg/kg/day in rats and rabbits, respectively (approximately 100 and 110 times the AUC in humans at the MRHDOD, respectively).
8.2Lactation Risk Summary A published clinical lactation study reports the presence of montelukast in human milk. Data available on the effects of the drug on infants, either directly [see Use in Specific Populations ( 8.4 )] or through breast milk, do not suggest a significant risk of adverse events from exposure to montelukast sodium. The effects of the drug on milk production are unknown.
The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for montelukast sodium and any potential adverse effects on the breastfed infant from montelukast sodium or from the underlying maternal condition.
8.4Pediatric Use Safety and efficacy of montelukast sodium have been established in adequate and well-controlled studies in pediatric patients with asthma 6 to 14 years of age. Safety and efficacy profiles in this age group are similar to those seen in adults [see Adverse Reactions (6.1) , Clinical Pharmacology, Special Populations (12.3) , and Clinical Studies (14.1) ]. The efficacy of montelukast sodium for the treatment of seasonal allergic rhinitis in pediatric patients 2 to 14 years of age and for the treatment of perennial allergic rhinitis in pediatric patients 6 months to 14 years of age is supported by extrapolation from the demonstrated efficacy in patients 15 years of age and older with allergic rhinitis as well as the assumption that the disease course, pathophysiology and the drug’s effect are substantially similar among these populations.
The safety of montelukast sodium 4 mg (montelukast) oral granules in pediatric patients 12 to 23 months of age with asthma has been demonstrated in an analysis of 172 pediatric patients, 124 of whom were treated with montelukast sodium, in a 6-week, double-blind, placebo-controlled study [see Adverse Reactions (6.1) ]. Efficacy of montelukast sodium in this age group is extrapolated from the demonstrated efficacy in patients 6 years of age and older with asthma based on similar mean systemic exposure (A…
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and efficacy of montelukast sodium have been established in adequate and well-controlled studies in pediatric patients with asthma 6 to 14 years of age. Safety and efficacy profiles in this age group are similar to those seen in adults [see Adverse Reactions (6.1) , Clinical Pharmacology, Special Populations (12.3) , and Clinical Studies (14.1) ]. The efficacy of montelukast sodium for the treatment of seasonal allergic rhinitis in pediatric patients 2 to 14 years of age and for the treatment of perennial allergic rhinitis in pediatric patients 6 months to 14 years of age is supported by extrapolation from the demonstrated efficacy in patients 15 years of age and older with allergic rhinitis as well as the assumption that the disease course, pathophysiology and the drug’s effect are substantially similar among these populations.
The safety of montelukast sodium 4 mg (montelukast) oral granules in pediatric patients 12 to 23 months of age with asthma has been demonstrated in an analysis of 172 pediatric patients, 124 of whom were treated with montelukast sodium, in a 6-week, double-blind, placebo-controlled study [see Adverse Reactions (6.1) ]. Efficacy of montelukast sodium in this age group is extrapolated from the demonstrated efficacy in patients 6 years of age and older with asthma based on similar mean systemic exposure (AUC), and that the disease course, pathophysiology and the drug's effect are substantially similar among these populations, supported by efficacy data from a safety trial in which efficacy was an exploratory assessment.
The safety of montelukast sodium 4 mg (montelukast) oral granules in pediatric patients as young as 6 months of age with perennial allergic rhinitis is supported by extrapolation from safety data obtained from studies conducted in pediatric patients 6 months to 23 months of age with asthma and from pharmacokinetic data comparing systemic exposures in patients 6 months to 23 months of age to systemic exposures in adults. The safety and effectiveness in pediatric patients below the ageof 12 months with asthma and 6 months with perennial allergic rhinitis have not been established.
Growth Rate in Pediatric Patients A 56-week, multi-center, double-blind, randomized, active- and placebo-controlled parallel group study was conducted to assess the effect of montelukast sodium on growth rate in 360 patients with mild asthma, aged 6 to 8 years. Treatment groups included montelukast sodium 5 mg (montelukast) once daily, placebo, and beclomethasone dipropionate administered as 168 mcg twice daily with a spacer device. For each subject, a growth rate was defined as the slope of a linear regression line fit to the height measurements over 56 weeks.
The primary comparison was the difference in growth rates between montelukast sodium and placebo groups. Growth rates, expressed as least-squares (LS) mean (95% CI) in cm/year, for the montelukast sodium, placebo, and beclomethasone treatment groups were 5.67 (5.46, 5.88), 5.64 (5.42, 5.86), and 4.86 (4.64, 5.08), respectively. The differences in growth rates, expressed as least-squares (LS) mean (95% CI) in cm/year, for montelukast sodium minus placebo, beclomethasone minus placebo, and montelukast sodium minus beclomethasone treatment groups were 0.03 (-0.26, 0.31), -0.78 (-1.06, -0.49); and 0.81 (0.53, 1.09), respectively.
Growth rate (expressed as mean change in height over time) for each treatment group is shown in FIGURE 1. Figure 1: Change in Height (cm) from Randomization Visit by Scheduled Week(Treatment Group Mean ± Standard Error* of the Mean) *The standard errors of the treatment group means in change in height are too small to be visible on the plot.
🆘 Overdosage ▾
10 OVERDOSAGE No specific information is available on the treatment of overdosage with montelukast sodium. In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to adult patients for 22 weeks and, in short-term studies, up to 900 mg/day to patients for approximately a week without clinically important adverse experiences. In the event of overdose, it is reasonable to employ the usual supportive measures; e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required.
There have been reports of acute overdosage in post-marketing experience and clinical studies with montelukast sodium. These include reports in adults and children with a dose as high as 1000 mg. The clinical and laboratory findings observed were consistent with the safety profile in adults and pediatric patients.
There were no adverse experiences in the majority of overdosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of montelukast sodium and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity. It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action The cysteinyl leukotrienes (LTC 4 , LTD 4 , LTE 4 ) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT 1 ) 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 airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. 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.
Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT 1 receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or β-adrenergic receptor). Montelukast inhibits physiologic actions of LTD 4 at the CysLT 1 receptor without any agonist activity.
12.2Pharmacodynamics Montelukast causes inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD 4 in asthmatics. Doses as low as 5 mg cause substantial blockage of LTD 4 -induced bronchoconstriction. In a placebo-controlled, crossover study (n=12), montelukast sodium inhibited early- and late-phase bronchoconstriction due to antigen challenge by 75% and 57%, respectively.
The effect of montelukast sodium on eosinophils in the peripheral blood was examined in clinical trials. In patients with asthma aged 2 years and older who received montelukast sodium, a decrease in mean peripheral blood eosinophil counts ranging from 9% to 15% was noted, compared with placebo, over the double-blind treatment periods. In patients with seasonal allergic rhinitis aged 15 years and older who received montelukast sodium, a mean increase of 0.2% in peripheral blood eosinophil counts was noted, compared with a mean increase of 12.5% in placebo-treated patients, over the double-blind treatment periods; this reflects a mean difference of 12.3% in favor of montelukast sodium.
The relationship between these observations and the clinical benefits of montelukast noted in the clinical trials is not known [see Clinical Studies (14) ].
12.3Pharmacokinetics Absorption Montelukast is rapidly absorbed following oral administration. After administration of the 10 mg film-coated tablet to fasted adults, the mean peak montelukast plasma concentration (C max ) is achieved in 3 to 4 hours (T max ). The mean oral bioavailability is 64%.
The oral bioavailability and C max are not influenced by a standard meal in the morning. For the 5 mg chewable tablet, the mean C max is achieved in 2 to 2.5 hours after administration to adults in the fasted state. The mean oral bioavailability is 73% in the fasted state versus 63% when administered with a standard meal in the morning.
For the 4 mg chewable tablet, the mean C max is achieved 2 hours after administration in pediatric patients 2 to 5 years of age in the fasted state. The 4 mg oral granule formulation is bioequivalent to the 4 mg chewable tablet when administered to adults in the fasted state. The co-administration of the oral granule formulation with applesauce did not have a clinically significant effect on the pharmacokinetics of montelukast.
A high fat meal in the morning did not affect the AUC of montelukast oral granules; however, the meal decreased C max by 35% and prolonged Tmax from 2.3± 1 hours to 6.4 ± 2.9 hours. The safety and efficacy of montelukast sodium in patients with asthma were demonstrated in clinical trials in which the 10 mg film-coated tablet and 5 mg…
🧬 Mechanism of Action ▾
12.1Mechanism of Action The cysteinyl leukotrienes (LTC 4 , LTD 4 , LTE 4 ) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT 1 ) 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 airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. 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.
Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT 1 receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or β-adrenergic receptor). Montelukast inhibits physiologic actions of LTD 4 at the CysLT 1 receptor without any agonist activity.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Montelukast sodium oral granules, 4 mg (montelukast), are white to off white granular powder packed in aluminum foil packet. They are supplied as follows: Unit Dosage Package of 30 (1x30) NDC 55111-763-03 Storage Store montelukast sodium oral granules, 4 mg (montelukast), at 20°–25°C (68°–77° F), excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature]. Protect from moisture and light.
Store in original package.
📋 Description ▾
11 DESCRIPTION Montelukast sodium USP, the active ingredient in montelukast sodium oral granules, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinylleukotriene CysLT 1 receptor. Montelukast sodium USP is described chemically as [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid, monosodium salt. The molecular formula is C 35 H 35 CINNaO 3 S, and its molecular weight is 608.18.
The structural formula is: Montelukast sodium USP is white or almost white amorphous powder, hygroscopic in nature. Montelukast Sodium USP is freely soluble in water, methylene chloride and ethanol (96%). Each packet of montelukast sodium 4 mg oral granules contains 4.2 mg montelukast sodium USP, which is equivalent to 4 mg of montelukast.
The oral granule formulation contains the following inactive ingredients: hypromellose, magnesium stearate, and mannitol.
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information) Information for Patients • Patients should be advised to take montelukast sodium daily as prescribed, even when they are asymptomatic, as well as during periods of worsening asthma, and to contact their physicians if their asthma is not well controlled. • Patients should be advised that oral montelukast sodium is not for the treatment of acute asthma attacks. They should have appropriate short-acting inhaled β-agonist medication available to treat asthma exacerbations.
Patients who have exacerbations of asthma after exercise should be instructed to have available for rescue a short-acting inhaled β-agonist. Daily administration of montelukast sodium for the chronic treatment of asthma has not been established to prevent acute episodes of EIB. • Patients should be advised that, while using montelukast sodium, medical attention should be sought if short-acting inhaled bronchodilators are needed more often than usual, or if more than the maximum number of inhalations of short-acting bronchodilator treatment prescribed for a 24-hour period are needed. • Patients receiving montelukast sodium should be instructed not to decrease the dose or stop taking any other anti-asthma medications unless instructed by a physician. • Patients should be instructed to notify their physician if neuropsychiatric events occur while using montelukast sodium. • Patients with known aspirin sensitivity should be advised to continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking montelukast sodium.