Montelukast by aseem

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Montelukast by aseem

  1. 1. Montelukast
  2. 2. Introduction • MK-0476 ; Singulair (US) Montair (IN) Lukotas (IN) Monteflo (EU) C35H35ClNNaO3S • Developed by Merck in Montreal • Developed as a maintenance therapy for Asthma / Seasonal Allergies • Leukotriene Receptor Antagonist (LTRA)
  3. 3. Mechanism of Action • Blocks LTD4 action on Cys-LT1 receptors on Bronchi / Mast Cells / Eosinophils / Basophils • LT = ‘Slow Eicosanoid mediators of inflammation’ ; renamed as Leukotriene Modifiers • Others-in-Class  Zafirlukast (Acculate) / Pranlukast (Ultair) • 5-LOX-Inhibitors  Zileuton (Zyflo)
  4. 4. • aa
  5. 5. Role In Asthma • aa
  6. 6. Indications FDA-Approved • Prophylaxis of Chronic Asthma • Exercise-Induced Bronchoconstriction (EIB) Off-label uses • Allergic Rhinitis • Chronic Urticaria • COPD • Atopic Dermatitis • Migraine Prophylaxis • Sinonasal polyposis
  7. 7. Studies i/v/o CIU • Berkun and Shalit reported a case of successfully treated steroid- dependent delayed pressure urticaria with montelukast • Ellis reported 2 cases successfully treated with zileuton • Norris and Sullivan reported 9 of 15 steroid-requiring patients achieved control with zafirlukast • Chiu and Warren noted 8 of 15 subjects responded to zafirlukast • Spector and Tan noted one case controlled by zafirlukast and the other by zileuton • No RCTs published concerning treating chronic urticaria with leukotriene modifiers
  8. 8. • Bensch and Borish performed a retrospective chart review and identified 18 patients with chronic urticaria treated with leukotriene inhibitors • Ten had “dramatic” improvement – four with montelukast – five with zafirlukast – one with both zafirlukast and zileuton • Improvement seen within 1 week; resolution of urticaria within one month • ??? Better response to LOX-I > LTRA
  9. 9. Studies i/v/o AD • As of 2000, only two published papers address this issue • Carucci et al. reported a series of 4 cases using zafirlukast with observed subjective improvement • A pilot study using Montelukast recently concluded • • Woodmansee and Simon- Atopic Dermatitis Pilot Study using Zileuton on 14 pts (05 improved)
  10. 10. Pharmacology Absorption • Bioavailability: 64% (mean) • Peak plasma time: Tablet, 3-4 hr; chewable tablet, 2-2.5 hr; granules, 1-3 hr Distribution • Protein bound: >99% Metabolism • Metabolized by CYP3A4 and CYP2C9 Elimination • Half-life: 2.7-5.5 hr • Excretion: Feces (86%), urine (0.2%) Pregnancy Cat B Lactation – Unknown
  11. 11. Formulations Oral • Tablet (5/10mg) • Chewable (4/5mg) • Granules / Satchet
  12. 12. Dosage • > 15 yrs : 10 mg PO od • 6 -14 yrs: 5mg PO od (Chewable) • 2 - 5 yrs: 4mg chewable tablet / one packet of 4mg oral granules PO qd • 12- 23 mo : One satchet 4mg PO qd • < 12 mo : Safety-Efficacy not estabilished • Best taken in the evening ; No regard to food
  13. 13. ADRs • Headache (18.4%) • Abdominal pain (≥2%) Gastroenteritis (2%) • Laryngitis (≥2%) Pharyngitis (≥2%) • Dizziness (2%) • Elevated liver function tests (2%) • Urticaria (2%) Eczema (≥1%) • Cough (≥1%) Sinusitis (≥1%) • Churg-Strauss syndrome (AEGPA); rare • Aggressive behavior, suicidal thoughts
  14. 14. THANK YOU

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