Montelukast Sodium (2 brand names, 3 dosage forms, 1 route)
Available dosage forms: TABLET, CHEWABLE, TABLET, GRANULE.
Routes of administration: ORAL.
Brand Names
- MONTELUKAST SODIUM
- SINGULAIR
Related Health Topics
Boxed Warning
Seriousneuropsychiatric (NP) events have been reported with the use of montelukast sodium. The types of events reported were highly variable, and included, but were not limited to, agitation, aggression, depression, sleep disturbances, suicidal thoughts and behavior (including suicide). The mechanisms underlying NP events associated with montelukastsodium useare currently not well understood [see Warnings and Precautions (5.1)]. Because ofthe risk of NP events, the benefits of montelukast sodium may not outweigh the risks in some patients, particularly when the symptoms of disease may be mild and adequately treated with alternative therapies. Reserve use of montelukast sodium for patients with allergic rhinitis who have an inadequate response or intolerance to alternativetherapies [see Indications and Usage ( 1.3)]. In patients with asthma or exercise-induced bronchoconstriction, consider the benefits and risks before prescribing montelukast sodium. Discussthe benefits and risks of montelukast sodium with patients and caregivers when prescribing montelukast sodium. Advise patients and/or caregivers to be alert for changes in behavior or new NP symptoms when taking montelukast sodium. If changes in behavior are observed, or if new NP symptoms or suicidal thoughts and/or behavior occur, advisepatients todiscontinue montelukast sodium and contact a healthcare provider immediately [see Warnings and Precautions (5.1)].
Contraindications
Montelukast sodium tablets are contraindicated in patients with hypersensitivity to any of its components.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: • Neuropsychiatric Events [see Warnings and Precautions ( 5.1)]
Drug Interactions
No dose adjustment is needed when montelukast sodium is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, fexofenadine, 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)].
Mechanism 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 1receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or β-adrenergic receptor). Montelukast inhibits physiologic actions of LTD 4at the CysLT 1receptor without any agonist activity.
Overdosage
No specific information is available on the treatment of overdosage with montelukast sodium. 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. It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.