Leukotriene receptor antagonist
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Authored by: Aahynes 20:01, 22 February 2007 (PST) Certified by : Khlee3 13:49, 25 February 2007 (PST) |
Contents |
Mechanism of Action
Leukotriene receptor antagonists exert their actions by binding to the active site of leukotriene receptors. Cysteinyl leukotrienes (LTC4, LTD4, LTE4) have been associated with airway edema, smooth muscle contraction, and inflammation. Inhibition of these phsyiologic actions has been shown to be effective for the maintenence treatment of asthma. In addition, cysteinyl leukotrienes are released in the nasal mucosa by immune cells during an allergic response. Administration of leukotriene receptor antagonists to patients with seasonal and perenial allergies has been shown to decrease nasal airway resistance and nasal obstruction.
Two leukotriene receptor antagonists are currently on the market: Montelukast and Zafirlukast. Montelukast is a selective inhibitior of leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor CysLT1. Zafirlukast selectively inhibits leukotriene D4 (LTD4) and leukotriene E4 (LTE4).
Medical Uses
FDA Approved Indications:
- Allergic Rhinitis(Montelukast only)[1][2][3]
- Asthma (maintenence ONLY)[1][4][5][6][7][8][9][10]
- Bronchospasm prophylaxis[1][4][11]
Non FDA Approved Indications:
- Allergic Rhinitis (Zafirlukast only)[12]
- Cystic fibrosis (Montelukast only)[13]
Churg-Strauss syndrome
Leukotriene receptor antagonist use has been associated with rare reports of Churg-Strauss syndrome]. This condition of eosinophilia and vasculitis usually occurs when the dosage of concomittant oral corticosteroid therapy is reduced. Patients with this syndrome often complain initially of flu-like symptoms such as fever, myalgia, and weight loss. As the condition develops, patients can experience worsening pulmonary symptoms, cardiac compliactions, and neuropathy. This condition can be life threatening. Treatment strategies often include oral corticosteroids. While a direct relationship has not been definitively shown, patients should be counseled to report flu-like symptoms to their physician while on montelukast therapy.[1]
Available Medications in this Class
- Montelukast (Singulair®)
- Zafirlukast (Accolate®]
Complete Medication Classification List
References
- ↑ 1.0 1.1 1.2 1.3 Singulair® (montelukast) package insert. Whitehouse Station, NJ: Merck & Co, Inc.; 2005 Sep.
- ↑ Virchow JC, Bachert C. Efficacy and safety of montelukast in adults with asthma and allergic rhinitis. Respiratory medicine. 2006 Nov;100(11):1952-9.
- ↑ Grainger J, Drake-Lee A. Montelukast in allergic rhinitis: a systematic review and meta-analysis. Clin Otolaryngol. 2006 Oct;31(5):360-7.
- ↑ 4.0 4.1 Accolate® (zafirlukast) package insert. Wilmington, DE: AstraZeneca; 2004 Jul.
- ↑ Ghosh G, Manglik AK, Roy S. Efficacy and safety of montelukast as monotherapy in children with mild persistent asthma. Indian pediatrics. 2006 Sep;43(9):780-5.
- ↑ Athavale A, Souza GA, Avasthi R, Singh NP, Kale M, Taneja A, et al. A clinical trial of the efficacy and safety of montelukast as monotherapy in patients with chronic stable bronchial asthma. Journal of the Indian Medical Association. 2004 Feb;102(2):109-11
- ↑ van Adelsberg J, Moy J, Wei LX, Tozzi CA, Knorr B, Reiss TF. Safety, tolerability, and exploratory efficacy of montelukast in 6- to 24-month-old patients with asthma. Current medical research and opinion. 2005 Jun;21(6):971-9.
- ↑ Virchow JC, Bachert C. Efficacy and safety of montelukast in adults with asthma and allergic rhinitis. Respiratory medicine. 2006 Nov;100(11):1952-9.
- ↑ Can M, Yuksel B, Demirtas S, Tomac N. The effect of montelukast on soluble interleukin-2 receptor and tumor necrosis factor alpha in pediatric asthma. Allergy Asthma Proc. 2006 Jul-Aug;27(4):383-6.
- ↑ Harmanci K, Bakirtas A, Turktas I, Degim T. Oral montelukast treatment of preschool-aged children with acute asthma. Ann Allergy Asthma Immunol. 2006 May;96(5):731-5.
- ↑ Hakim F, Vilozni D, Adler A, Livnat G, Tal A, Bentur L. The effect of montelukast on bronchial hyperreactivity in preschool children. Chest. 2007 Jan;131(1):180-6.
- ↑ Lacy C, Armstrong L, Goldman M, Lance L. Drug Information Handbook 11th edition: APhA 2003.
- ↑ Stelmach I, Korzeniewska A, Stelmach W, Majak P, Grzelewski T, Jerzynska J. Effects of montelukast treatment on clinical and inflammatory variables in patients with cystic fibrosis. Ann Allergy Asthma Immunol. 2005 Oct;95(4):372-80.

