Terfenadine

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Terfenadine
Clinical data
ATC code
Pharmacokinetic data
Protein binding70%
Elimination half-life3.5 hours
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
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Chemical and physical data
FormulaC32H41NO2
Molar mass471.673 g/mol

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Overview

Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. It was marketed under various brand names including Seldane in the United States, Triludan in the United Kingdom, and Teldane in Australia. It was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation.

Terfenadine is a prodrug, generally completely metabolised to the active form fexofenadine by intestinal CYP3A4. Terfenadine itself, however, has a cardiotoxic effect and may be absorbed and reach myocytes if the patient is concurrently taking a CYP3A4 inhibitor (e.g. erythromycin, grapefruit juice).

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