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LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-.
LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet].
Show detailsOVERVIEW
The leukotriene receptor antagonists are among the most prescribed drugs for the management of asthma, used both for treatment and prevention of acute asthmatic attacks. This class of drugs acts by binding to cysteinyl leukotriene (CysLT) receptors and blocking their activation and the subsequent inflammatory cascade which cause the symptoms commonly associated with asthma and allergic rhinitis.
The cysteinyl leukotrienes (C4, D4 and E4) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to CysLT receptors. The CysLT type-1 receptor is found in the human airway smooth muscle cells and airway macrophages and on other proinflammatory cells. In asthmatic patients, 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 and precipitate the symptoms of allergic rhinitis.
Two leukotriene receptor antagonists are available in the United States, zafirlukast (1996) and montelukast (1998). Both are oral agents used in management of asthma and allergic rhinitis. Both have been associated with rare cases of acute liver injury. While they have similar mechanisms of action, these two agents are structurally distinct, and the liver injury they cause does not appear to be similar in pattern of presentation or outcome. Indeed, several instances of hepatotoxicity due to one agent have been described in which the patient has tolerated the other agent without recurrence. For this reason, these two agents are discussed separately.
The following links are to individual drug records.
Drug Class: Antiasthmatic Agents
Last updated: 06 June 2019
- Expression of cysteinyl leukotriene synthetic and signalling proteins in inflammatory cells in active seasonal allergic rhinitis.[Clin Exp Allergy. 2003]Expression of cysteinyl leukotriene synthetic and signalling proteins in inflammatory cells in active seasonal allergic rhinitis.Figueroa DJ, Borish L, Baramki D, Philip G, Austin CP, Evans JF. Clin Exp Allergy. 2003 Oct; 33(10):1380-8.
- Review The role of leukotrienes in allergic rhinitis.[Ann Allergy Asthma Immunol. 2005]Review The role of leukotrienes in allergic rhinitis.Peters-Golden M, Henderson WR Jr. Ann Allergy Asthma Immunol. 2005 Jun; 94(6):609-18; quiz 618-20, 669.
- Review Pathophysiology of the cysteinyl leukotrienes and effects of leukotriene receptor antagonists in asthma.[Allergy. 2001]Review Pathophysiology of the cysteinyl leukotrienes and effects of leukotriene receptor antagonists in asthma.Bisgaard H. Allergy. 2001; 56 Suppl 66:7-11.
- Characterization of the human cysteinyl leukotriene 2 receptor.[J Biol Chem. 2000]Characterization of the human cysteinyl leukotriene 2 receptor.Heise CE, O'Dowd BF, Figueroa DJ, Sawyer N, Nguyen T, Im DS, Stocco R, Bellefeuille JN, Abramovitz M, Cheng R, et al. J Biol Chem. 2000 Sep 29; 275(39):30531-6.
- Review [Leukotrien antagonists in the treatment of allergic rhinitis and comorbidities].[Rev Alerg Mex. 2008]Review [Leukotrien antagonists in the treatment of allergic rhinitis and comorbidities].Sacre Hazouri JA. Rev Alerg Mex. 2008 Jul-Aug; 55(4):164-75.
- Leukotriene Receptor Antagonists - LiverToxLeukotriene Receptor Antagonists - LiverTox
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