Montelukast

Montelukast Brand Name– Singulair

What is Montelukast

Montelukast is an oral leukotriene receptor antagonists (LTRA).

Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and has not been found to affect the hepatic clearance of drugs metabolized by these enzymes.

Montelukast is primarily used for the chronic maintenance treatment of asthma, to prevent exercise-induced bronchoconstriction (EIB), and for the treatment of perennial and seasonal allergic rhinitis.

In general, montelukast is well tolerated; however, serious psychiatric effects (e.g., suicidal behaviors, aggression, depression) have been prevalent in postmarketing reports.

A boxed warning exists in the product label because of serious neuropsychiatric effects.

Montelukast should not be used for mild symptoms of allergic rhinitis, but should be reserved for patients who are not treated effectively with or cannot tolerate other allergy medication.

For asthma maintenance therapy, LTRAs are less effective than inhaled corticosteroids (ICSs); however, they may be of benefit in patients who are unwilling or unable to use ICS, experience intolerable ICS side effects, or have concomitant allergic rhinitis.

LTRAs are add-on therapy for severe asthma in adolescents and adults. In young children with asthma, LTRA therapy reduces symptoms and the need for oral corticosteroids when compared with placebo.

For the prevention of exercise-induced bronchoconstriction (EIB), montelukast may be considered a first-line choice to add as a controller agent to an inhaled short-acting beta-2 agonist (SABA) to control EIB symptoms in patients who cannot be controlled by an inhaled SABA alone.

Expert opinions regard the LTRAs as options in the treatment of allergic rhinitis, particularly when the patient has comorbid asthma.

Montelukast has the most substantial evidence for seasonal and perennial allergies of the LRTAs. However, in patients with allergic rhinitis (seasonal or other) alone, intranasal corticosteroids are generally considered first-line therapy, since treatment results with LTRAs appear to be similar to standard treatments such as antihistamines, and inferior to intranasal corticosteroids.

Montelukast is FDA-approved for use in patients as young as 1 year of age for the maintenance treatment of asthma, as young as 2 years of age for treatment of seasonal allergic rhinitis, and in infants as young as 6 months with perennial allergic rhinitis.

Montelukast is also used for preventing exercise-induced bronchoconstriction (EIB) in patients 6 years and older.

Indications

  1. allergic rhinitis
  2. aspirin-induced asthma
  3. asthma
  4. atopic dermatitis
  5. chronic idiopathic urticaria
  6. exercise-induced bronchospasm prophylaxis
  7. perennial allergies
  8. seasonal allergies
  9. sleep apnea
  10. urticaria

For the chronic treatment and prevention of the symptoms of asthma, either as monotherapy or as add-on therapy in patients whose persistent mild-moderate asthma is inadequately controlled with inhaled corticosteroids

NOTE: Montelukast is not a rescue medication; it should not be used for the treatment of an acute asthmatic attack or acute bronchospasm. However, montelukast may be continued during the treatment of an acute asthmatic event.

Side Effects

  1. abdominal pain
  2. abnormal dreams
  3. agitation
  4. anaphylactoid reactions
  5. angioedema
  6. anxiety
  7. arthralgia
  8. asthenia
  9. atopic dermatitis
  10. bleeding
  11. Churg-Strauss syndrome
  12. confusion
  13. conjunctivitis
  14. cough
  15. depression
  16. diarrhea
  17. dizziness
  18. drowsiness
  19. dyspepsia
  20. dysphemia
  21. ecchymosis
  22. edema
  23. elevated hepatic enzymes
  24. eosinophilia
  25. epistaxis
  26. erythema multiforme
  27. erythema nodosum
  28. fatigue
  29. fever
  30. gastritis
  31. hallucinations
  32. headache
  33. hepatitis
  34. hostility
  35. hypoesthesia
  36. impulse control symptoms
  37. infection
  38. influenza
  39. insomnia
  40. irritability
  41. laryngitis
  42. memory impairment
  43. muscle cramps
  44. myalgia
  45. myopia
  46. nasal congestion
  47. nausea
  48. nightmares
  49. palpitations
  50. pancreatitis
  51. paresthesias
  52. pharyngitis
  53. pruritus
  54. pyuria
  55. rash
  56. restlessness
  57. rhinitis
  58. rhinorrhea
  59. seizures
  60. sinusitis
  61. somnambulism
  62. Stevens-Johnson syndrome
  63. suicidal ideation
  64. thrombocytopenia
  65. toxic epidermal necrolysis
  66. tremor
  67. urinary incontinence
  68. urticaria
  69. vasculitis
  70. vomiting
  71. weight loss
  72. wheezing

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • acute bronchospasm
  • alcoholism
  • behavioral changes
  • breast-feeding
  • corticosteroid withdrawal
  • depression
  • geriatric
  • hepatic disease
  • hepatitis
  • infants
  • jaundice
  • neonates
  • neurologic events
  • phenylketonuria
  • pregnancy
  • psychiatric event
  • status asthmaticus
  • suicidal ideation

Interactions

  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Carbamazepine
  • Enzalutamide
  • Gemfibrozil
  • Hydantoins
  • Lumacaftor; Ivacaftor
  • Mitotane
  • Phenobarbital
  • Primidone
  • Rifamycins
  • St. John’s Wort, Hypericum perforatum
  • Warfarin
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