Bernstein D I, Schoenwetter W F, Nathan R A, Storms W, Ahlbrandt R, Mason J
Division of Immunology, University of Cincinnati, College of Medicine, Ohio, USA.
Ann Allergy Asthma Immunol. 1997 Nov;79(5):443-8. doi: 10.1016/S1081-1206(10)63041-4.
H1-receptor antagonists are effective for the treatment of seasonal allergic rhinitis. In rare circumstances, some second-generation H1-receptor antagonists have been associated with prolongation of the corrected QT interval (QTc), thus increasing the risk of ventricular arrhythmias. Fexofendine HCl, the carboxylic acid metabolite of terfenadine, is a new second-generation antihistamine that is nonsedating and does not cause electrocardiographic effects.
To investigate the clinical efficacy and safety of fexofenadine HCl in the treatment of ragweed seasonal allergic rhinitis and to characterize the dose-response relationship of fexofenadine HCl at dosages of 60, 120, and 240 mg bid.
A multicenter, 14-day, placebo-controlled, double-blind trial was conducted with patients suffering from moderate to severe ragweed seasonal allergic rhinitis who met symptom severity criteria after a 3-day placebo baseline period. Patients with minimal or very severe symptoms during the baseline period were excluded. Patients were randomized to receive fexofenadine HCl (60, 120, or 240 mg bid) or placebo at 12-hour dosing intervals (7:00 AM and 7:00 PM). The primary efficacy measure was patient-assessed 12-hour reflective total symptom score before the evening dose (trough).
Five hundred seventy patients completed the trial. Fexofenadine HCl at each dosage provided significant improvement in total symptom score (P < or = .003) and in all individual nasal symptoms compared with placebo. The frequency of adverse events was similar among fexofenadine HCl and placebo groups, with no dose-related trends. No sedative effects or electrocardiographic abnormalities, including prolongations in QTc were detected.
Fexofenadine HCl is both effective and safe for the treatment of ragweed seasonal allergic rhinitis. Because there was no additional efficacy at higher dosages, 60 mg bid appears to be the optimal therapeutic dosage for these patients.
H1受体拮抗剂对季节性变应性鼻炎有效。在罕见情况下，一些第二代H1受体拮抗剂与校正QT间期（QTc）延长有关，从而增加室性心律失常的风险。特非那定的羧酸代谢产物盐酸非索非那定是一种新型第二代抗组胺药，无镇静作用且不引起心电图改变。
研究盐酸非索非那定治疗豚草季节性变应性鼻炎的临床疗效和安全性，并确定60、120和240mg bid剂量的盐酸非索非那定的剂量反应关系。
对中度至重度豚草季节性变应性鼻炎患者进行了一项多中心、为期14天、安慰剂对照、双盲试验，这些患者在3天安慰剂基线期后符合症状严重程度标准。排除基线期症状轻微或非常严重的患者。患者随机接受盐酸非索非那定（60、120或240mg bid）或安慰剂，给药间隔为12小时（上午7:00和晚上7:00）。主要疗效指标是患者评估的晚上给药前（谷值）12小时反射性总症状评分。
570名患者完成了试验。与安慰剂相比，各剂量的盐酸非索非那定在总症状评分（P≤0.003）和所有个体鼻部症状方面均有显著改善。盐酸非索非那定组和安慰剂组不良事件的发生率相似，无剂量相关趋势。未检测到镇静作用或心电图异常，包括QTc延长。
盐酸非索非那定治疗豚草季节性变应性鼻炎有效且安全。由于高剂量时无额外疗效，60mg bid似乎是这些患者的最佳治疗剂量。
