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3.11 Terfenadine

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Terfenadine was marketed in 1985 in the United States as the first nonsedating antihistamine for the treatment of seasonal allergic rhinnitis. It was available as an OTC drug and was found to be associated with lethal cases of torsades de pointes, a form of ventricular arrythmia, in patients who were also taking macrolide antibiotics such as erythromycin [183–185], and the antifungal ketoconazole [184,186–188], and in patients with compromised liver functions [189]. A black box warning for terfenadine was issued by FDA in 1992 and the drug was eventually removed from the market in 1997. Terfeanadine was replaced by fexofenadine, the pharmacologically active metabolite of terfenadine without cardiotoxicity [190].

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity

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