Pakes G E, Brogden R N, Heel R D, Speight T M, Avery G S
Drugs. 1980 Jun;19(6):397-411. doi: 10.2165/00003495-198019060-00001.
Flunisolide, a derivative of fluocinolone acetonide, is advocated for intranasal inhalation for the treatment of perennial and seasonal allergic rhinitis. It is rapidly absorbed by all routes of administration, but it quickly undergoes extensive first-pass metabolism to a 6 beta-hydroxylated metabolite, which possesses only weak corticosteroid effects. Intranasal flunisolide relieves nasal symptoms (but not eye symptoms) in both perennial and seasonal allergic rhinitis, being most effective in patients who have an allergic component to their rhinitis; and like other corticosteroids it may reduce the need for systemic antihistamines in such patients, expecially during peak pollen periods. A few well designed comparative studies have shown flunisolide to be as effective as intranasal beclomethasone, and (in a single study) more effective than intranasal sodium cromoglycate solution. Only transient side effects have occurred, including nasal stinging and throat irritation. No Candida infections have been clinically apparent in short or longer term trials. Resting morning plasma cortisol levels have not been suppressed by usual therapeutic doses of intranasal flunisolide, but the drug's effects on hypothalamo-pituitary-adrenal (HPA) axis integrity during conditions of stress have not been evaluated.
氟尼缩松是醋酸氟轻松的衍生物,被推荐用于鼻内吸入,以治疗常年性和季节性变应性鼻炎。它可通过所有给药途径迅速吸收,但很快会经历广泛的首过代谢,生成一种6β - 羟基化代谢物,该代谢物仅具有微弱的皮质类固醇作用。鼻内使用氟尼缩松可缓解常年性和季节性变应性鼻炎的鼻部症状(但对眼部症状无效),对鼻炎有过敏成分的患者最为有效;与其他皮质类固醇一样,它可能会减少此类患者使用全身性抗组胺药的需求,尤其是在花粉高峰期。一些设计良好的对照研究表明,氟尼缩松与鼻内使用倍氯米松效果相当,且(在一项研究中)比鼻内使用色甘酸钠溶液更有效。仅出现过短暂的副作用,包括鼻部刺痛和咽喉刺激。在短期或长期试验中,均未出现明显的念珠菌感染。鼻内使用氟尼缩松的常规治疗剂量未抑制静息状态下早晨的血浆皮质醇水平,但尚未评估该药物在应激状态下对下丘脑 - 垂体 - 肾上腺(HPA)轴完整性的影响。