Horiguchi Takahiko, Kondo Rieko, Miyazaki Junichi, Fukumokto Koji, Torigoe Hiroshi
Department of Internal Medicine, Fujita Health University Second Hospital, Nagoya, Aichi, Japan.
Arzneimittelforschung. 2004;54(5):280-5. doi: 10.1055/s-0031-1296971.
Tulobuterol transdermal therapeutic system (TTS) is the world's first commercially available transdermal preparation of tulobuterol, a beta2-stimulant that can maintain effective blood tulobuterol (CAS 41570-61-0) levels for 24 h when applied once daily. In the present study, a total of 24 adult patients with mild persistent (Step 2) or moderate persistent (Step 3) bronchial asthma, consisting of 13 and 11 patients, who were or were not using inhalational steroids, respectively, used tulobuterol TTS (Hokunalin Tape) for one year and underwent measurement of peak expiratory flow (PEF) once daily. Peripheral eosinophil count, serum eosinophil cationic protein (ECP) level and airway responsiveness (Dmin) were evaluated at 6 months and 1 year, respectively, after the start of the study. PEF exhibited significant improvements after 6 months and 1 year in patients treated with or without inhalational steroids, while serum ECP was improved significantly only in the patients on inhalational steroids. Patients not using inhalational steroids exhibited significant exacerbation of Dmin at neither after 6 months nor after 1 year. One-year treatment with tulobuterol TTS did not appear to cause tachyphylaxis. The significant improvements in Dmin observed after 6 months and after 1 year in the patients using inhalational steroids suggested beneficial effects of inhalational steroids in controlling airway inflammation. Tulobuterol TTS is considered quite beneficial in improving quality of life (QOL) in patients with bronchial asthma because its incidence of adverse effects including palpitations and shivering is significantly lower than those of oral preparations because of its remarkable improvement of pulmonary function and symptoms of airway obstruction without increasing airway responsiveness even after repeated use, and because it is simple to use and ensures excellent clinical efficacy.
妥洛特罗透皮治疗系统（TTS）是世界上首个上市的妥洛特罗透皮制剂，妥洛特罗是一种β2激动剂，每日给药一次时可使妥洛特罗（CAS 41570-61-0）的有效血药浓度维持24小时。在本研究中，共有24例轻度持续性（第2级）或中度持续性（第3级）支气管哮喘成年患者，其中13例和11例患者分别正在或未使用吸入性糖皮质激素，使用妥洛特罗TTS（博利康尼透皮贴剂）治疗1年，且每天测量一次呼气峰值流速（PEF）。在研究开始后的6个月和1年时分别评估外周血嗜酸性粒细胞计数、血清嗜酸性粒细胞阳离子蛋白（ECP）水平和气道反应性（Dmin）。在接受或未接受吸入性糖皮质激素治疗的患者中，6个月和1年后PEF均有显著改善，而血清ECP仅在接受吸入性糖皮质激素治疗的患者中有显著改善。未使用吸入性糖皮质激素的患者在治疗6个月和1年后Dmin均未出现显著恶化。妥洛特罗TTS治疗1年似乎未引起快速耐受。使用吸入性糖皮质激素的患者在6个月和1年后观察到Dmin有显著改善，提示吸入性糖皮质激素在控制气道炎症方面具有有益作用。妥洛特罗TTS被认为对改善支气管哮喘患者的生活质量（QOL）非常有益，因为其包括心悸和寒战在内的不良反应发生率显著低于口服制剂，原因在于其能显著改善肺功能和气道阻塞症状，即使反复使用也不会增加气道反应性，且使用方便并确保了良好的临床疗效。
