Bryson H M, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1992 May;43(5):760-75. doi: 10.2165/00003495-199243050-00009.
Fluticasone propionate is a potent topical anti-inflammatory corticosteroid with low systemic activity. Available pharmacodynamic data are only preliminary; however, large placebo- and drug-controlled clinical studies involving almost 4000 patients with seasonal allergic rhinitis and 1500 with perennial allergic and nonallergic rhinitis have confirmed the efficacy of intranasal fluticasone propionate in the control of nasal symptoms. Fluticasone propionate generally demonstrated similar efficacy compared with intranasal beclomethasone dipropionate, flunisolide acetonide and oral astemizole and better or a trend towards better efficacy compared with oral loratadine, terfenadine, cetirizine and intranasal sodium cromoglycate (cromolyn sodium) against nasal symptoms. The incidence of adverse effects in association with intranasal fluticasone propionate appears to be comparable to that observed with placebo; the most frequently reported effects are nasal dryness/burning, epistaxis and headache. Consistent with its minimal systemic availability, intranasal fluticasone propionate in a dosage of up to 4 mg/day does not cause adrenal suppression. Thus, based on early data from large clinical trials, fluticasone propionate administered once daily offers an effective and convenient treatment option in patients with seasonal and perennial allergic rhinitis, and is distinguished by its low oral bioavailability.
丙酸氟替卡松是一种强效的局部抗炎皮质类固醇,全身活性低。现有的药效学数据仅为初步数据;然而,涉及近4000例季节性变应性鼻炎患者和1500例常年性变应性和非变应性鼻炎患者的大型安慰剂对照和药物对照临床研究证实了鼻内使用丙酸氟替卡松在控制鼻部症状方面的疗效。与鼻内使用二丙酸倍氯米松、醋酸氟尼缩松和口服阿司咪唑相比,丙酸氟替卡松通常显示出相似的疗效;与口服氯雷他定、特非那定、西替利嗪和鼻内使用色甘酸钠(色甘酸二钠)相比,在控制鼻部症状方面疗效更好或有疗效更好的趋势。与鼻内使用丙酸氟替卡松相关的不良反应发生率似乎与安慰剂观察到的相当;最常报告的不良反应是鼻干燥/烧灼感、鼻出血和头痛。与其极低的全身利用率一致,每日剂量高达4mg的鼻内丙酸氟替卡松不会引起肾上腺抑制。因此,基于大型临床试验的早期数据,每日一次给药的丙酸氟替卡松为季节性和常年性变应性鼻炎患者提供了一种有效且方便的治疗选择,其特点是口服生物利用度低。