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Terfenadine

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 It was superceded by fexofenadine in the 1990s due to the risk cardiac arrhythmia.

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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Risky drug interaction confirmed - terfenadine and ketoconazole prescribed together may cause fatal heart-rhythm disturbance - Brief Article
From Science News, 4/3/93

Two commonly prescribed drugs, when taken together, can cause a rare type of heartbeat abnormality that may lead to a heart attack. One of the drugs is terfenadine (trade name Seldane), which doctors prescribe to clear up congestion. The other is ketoconazole (Nizoral), an antifungal agent.

In 1990, after reviewing reports of cardiac problems in people using both drugs, the Food and Drug Administration warned physicians about the risky combo. However, doctors continued to prescribe this potentially fatal combination, says Peter K. Honig of the Uniformed Services University of the Health Sciences in Bethesda, Md.

Honig and his colleagues have now confirmed the heart jeopardy posed by this drug duo. In the March 24/31 JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, they report that terlenadine is not metabolized properly when taken with the oral form of ketoconazole. The result: a buildup of a substance in the bloodstream that can cause a potentially fatal heart-rhythm disturbance in otherwise healthy people.

COPYRIGHT 1993 Science Service, Inc.
COPYRIGHT 2004 Gale Group

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