Montelukast


Introduction

Montelukast is Selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene receptor. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. Cysteinyl leukotrienes are also released from the nasal mucosa following allergen exposure leading to symptoms associated with allergic rhinitis.

Montelukast manufactured by Faran Shimi Pharmaceutical Company_ is available in 5mg chewable and 10mg coated tablets. 10 tablets are packed in a blister and 3 blisters are packaged in one box with a leaflet.

Indications

Labeled Indications

• Allergic rhinitis (perennial or seasonal)
• Asthma, persistent (maintenance therapy)
• Bronchoconstriction, exercise-induced (prevention)

Off-Label: Adult

• Aspirin-exacerbated respiratory disease (including aspirin challenge/desensitization)
• Hypersensitivity reactions, rapid chemotherapy/biologics desensitization (premedication)
• Infusion related reactions, daratumumab-based regimens (premedication)
• Urticaria, chronic and delayed pressure


Important Information

Dosing

Adult


Allergic rhinitis, perennial or seasonal Allergic rhinitis (alternative agent):
Oral: 10 mg once daily

Aspirin-exacerbated respiratory disease, including aspirin challenge/desensitization (adjunct) (off-label use):
Chronic management
Oral: 10 mg once daily in the evening

Aspirin challenge/desensitization procedures:
Oral: 10 mg once daily starting 3 days before challenge/desensitization or
10 mg twice daily the day before challenge/desensitization followed by 10 mg
once daily on each day of the challenge/desensitization.

Introduction of aspirin before cardiovascular interventions for myocardial infarction:
Oral: 10 mg once ≥1 hour prior to the first aspirin dose

Asthma, persistent, maintenance therapy (alternative agent)
Oral: 10 mg once daily in the evening

Bronchoconstriction, exercise-induced (prevention):
Oral: 10 mg ≥2 hours prior to exercise; limit to 1 dose every 24 hours

Note: May be used as an adjunctive agent or alternative monotherapy
in patients with persistent symptoms on or who cannot take a short-acting beta agonist
or in patients who exercise frequently (e.g., >3 hours/day or more than once per day).
In patients receiving daily montelukast for another indication, additional montelukast
should not be administered for exercise-induced bronchoconstriction.

Hypersensitivity reactions, rapid chemotherapy/biologics desensitization (premedication) (off-label use):
Oral: 10 mg once daily for 1 to 2 days before the desensitization procedure,
then 10 mg 1 hour before the start of the procedure.

Infusion-related reactions, daratumumab-based regimens (premedication) (off-label use):
Oral: 10 mg administered 30 to 60 minutes prior to the first infusion; for split-dose infusion,
administer 10 mg before start of daratumumab on day 1 and day 2; administer as part of an appropriate premedication regimen.

Urticaria, chronic and delayed pressure (adjunct) (off-label use):
Oral: 10 mg once daily
Note: May be used as an adjunctive therapy in patients with persistent symptoms despite appropriately titrated antihistamine therapy

Renal Impairment:


No dosage adjustment necessary.

Hepatic Impairment:


• Mild-to-moderate impairment: No dosage adjustment necessary
• Severe impairment: There are no dosage adjustments provided in manufacturer’s labeling; has not been studied.

Pediatric

Allergic rhinitis:

Perennial
Children ≥6 years and Adolescents <15 years: Oral: 5 mg once daily
Adolescents ≥15 years: Oral: 10 mg once daily
Seasonal
Children ≥6 years and Adolescents <15 years: Oral: 5 mg once daily.
Adolescents ≥15 years: Oral: 10 mg once daily

Asthma, maintenance therapy:


6 to 14 years: Oral: 5 mg once daily in the evening.
≥15 years: Oral: 10 mg once daily in the evening.

Exercise-induced bronchospasm, prevention:


Children ≥6 years and Adolescents <15 years: Oral: 5 mg at least 2 hours prior to exercise.
Adolescents ≥15 years: Tablet: Oral: 10 mg at least 2 hours prior to exercise

Urticaria (nonsteroidal anti-inflammatory drug-induced):


Limited data available: Adolescents ≥15 years: Oral: 10 mg once daily

Renal Impairment:

No dosage adjustment necessary.

Hepatic Impairment:


• Mild-to-moderate impairment: No dosage adjustment necessary
• Severe impairment: There are no dosage adjustments provided in manufacturer’s labeling; has not been studied.

Administration:


Adult


In patients with asthma or who require chronic management of aspirin-exacerbated respiratory disease,
administer dose in the evening regardless of the presence of other indications for montelukast; for all
other indications, may individualize administration time. May administer without regard to food or meals.

Pediatric


May administer without regard to food or meals. When treating asthma, administer dose
in the evening. Patients with allergic rhinitis may individualize administration time (morning or evening).
Patients with both asthma and allergic rhinitis should take their dose in the evening.

Missed dose: The missed dose should be skipped and therapy resumed at next scheduled doses;
two doses should not be administered at the same time to catch up.

Interactions


Gemfibrozil: May increase the serum concentration of Montelukast.
Risk C: Monitor therapy

Pregnancy

an increased risk of teratogenic effects has not been observed with montelukast use in pregnancy.
Montelukast should not be withheld during pregnancy when clinically indicated

Breast-Feeding

Montelukast is present in breast milk, the decision to breastfeed during therapy should consider the risk and benefits.

Contraindications


Hypersensitivity to montelukast or any component of the formulation

Warnings/Precautions


• Serious neuropsychiatric (NP) events: have been reported with the use of montelukast.
If changes in behavior are observed, or if new NP symptoms or suicidal thoughts and/or behavior occur,
advise patients to discontinue montelukast and contact a health care provider immediately.
• Acute asthma/bronchospasm: Montelukast is not FDA approved for use in the reversal of bronchospasm
in acute asthma attacks, including status asthmaticus.
• Chewable tablet(5mg): Contains phenylalanine. Avoid use in phenylketonuria
• Eosinophilia and vasculitis: In rare cases, patients may present with systemic eosinophilia,
sometimes presenting with clinical features of vasculitis consistent with eosinophilic granulomatosis
with polyangiitis (formerly known as Churg-Strauss); these clinical features may include eosinophilia,
vasculitis rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy.
A causal association between montelukast and these underlying conditions has not been established.

Side Effects

1% to 10%:
Dermatologic: Atopic dermatitis, dermatitis, eczema, skin infection, skin rash, urticaria
Gastrointestinal: Abdominal pain, diarrhea, dyspepsia, gastroenteritis, nausea, tooth infection, toothache
Genitourinary: Pyuria
Hepatic: Increased ALT, AST
Infection: Influenza, varicella zoster infection, viral infection
Nervous system: Dizziness, fatigue, headache
Neuromuscular & skeletal: Asthenia
Ophthalmic: Conjunctivitis, myopia
Otic: Otalgia, otitis, otitis media
Respiratory: Acute bronchitis, cough, epistaxis, laryngitis, nasal congestion, pharyngitis,
pneumonia, rhinitis, rhinorrhea, sinus headache, sinusitis, upper respiratory tract infection
Miscellaneous: Fever, trauma

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