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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 It was superceded by fexofenadine in the 1990s due to the risk cardiac arrhythmia.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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Fluticasone vs. terfenadine for allergic rhinitis treatment - Archives of Internal Medicine, December 12-26, 1994 - Tips from Other Journals
From American Family Physician, 4/1/95 by Barbara Apgar

Allergic rhinitis may substantially reduce work performance, produce physical symptoms and exacerbate asthma. Various treatments, including the use of antihistamines, corticosteroids, anticholinergic drugs and cromolyn, have been tried. Fluticasone, a corticosteroid formulated as an aqueous nasal spray, is as effective as intranasal beclomethasone in the treatment of seasonal allergic rhinitis. Van Bavel and associates performed a placebo-controlled, double-blind, randomized study to compare the efficacy and safety of intranasal fluticasone with that of oral terfenadine in patients with seasonal allergic rhinitis.

The study included 217 adults and adolescents who lived in central Texas during the mountain cedar pollination season. The substantial pollen exposure that occurs during this two-month period induces moderate to severe rhinitis in susceptible persons. Subjects underwent skin testing to determine their susceptibility to this allergen and were assigned to receive intranasal fluticasone (100 [mu]g per nostril each day), terfenadine tablets (60 mg twice daily) or placebo for two weeks. Pretreatment assessments indicated that the study subjects had moderately severe allergic rhinitis.

Clinician-rated total nasal symptom scores were significantly lower in the group treated with fluticasone. By day 15 of the study, scores had declined by 49 percent in the fluticasone group, compared with 27 percent in the terfenadine group and 19 percent in the placebo group. Patient-rated total nasal symptom scores were significantly lower in the fluticasone group, compared with the terfenadine group and the placebo group.

The data for individual symptoms were comparable with the total symptom scores. Improvement in rhinorrhea and nasal itching occurred by the third day in members of the fluticasone group. Subjects in the fluticasone group exhibited a significant improvement in sneezing by the end of the first day. Patient-rated scores for morning nasal obstruction in the fluticasone group were significantly lower than scores in the other groups. The frequency of eosinophils and basophils in nasal mucosal specimens was significantly lower in the fluticasone group than that in the other two groups. No serious adverse events occurred during the study period. Morning plasma cortisol concentrations did not differ among the three groups at baseline or at the end of the study.

The authors note that in their study population, use of fluticasone significantly reduced all nasal symptoms within 72 hours and reduced sneezing within 12 hours after initiation of therapy. The authors conclude that intranasal fluticasone is more effective and better tolerated than terfenadine in patients exhibiting symptoms of seasonal allergic rhinitis. (Archives of Internal Medicine, December 12/26,1994, vol. 154, p. 2699.)

COPYRIGHT 1995 American Academy of Family Physicians
COPYRIGHT 2004 Gale Group

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