Hochhaus Günther
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, USA.
Clin Ther. 2008 Jan;30(1):1-13. doi: 10.1016/j.clinthera.2008.01.005.
Mometasone furoate nasal spray (MFNS) is recommended as a first-line therapy for allergic rhinitis. The purpose of intranasal administration is to deliver maximally effective therapy to the affected nasal tissues while minimizing systemic exposure.
This article reviews the pharmacokinetic and pharmacodynamic properties of MFNS, highlighting the potential clinical relevance of data concerning its glucocorticoid receptor binding, bioavailability, and metabolism, and its role in activating and suppressing transcription of steroid-dependent genes.
A search of the MEDLINE and EMBASE databases (January 1995-July 2007) was undertaken to identify in vitro, preclinical, and clinical studies and review articles concerning MFNS. Searches were also conducted to identify articles on the pharmacokinetics, pharmacodynamics, and adverse effects of the intranasal corticosteroids discussed in this article. Pertinent abstracts from allergy society meetings and data from the author's research experience were also included.
The data reviewed indicate that MFNS has a number of qualities that are important in achieving nasal selectivity with minimal systemic adverse effects. For example, MFNS is stable in nasal tissues and is efficiently metabolized in the liver (AUC for a 400-microg dose: 127 fmol/mL x h). Its systemic bioavailability (0.46%) is one of the lowest among currently available intranasal corticosteroids. Bioactive glucocorticoid metabolites have not been observed in humans. The results of immunologic studies suggest that MFNS may reverse the exaggerated T-helper cell type 2 (Th2)-related cytokine response seen in allergic disease through preferential inhibition of Th2 over the T-helper cell type 1-related cytokine.
MFNS is an intranasal corticosteroid with a low potential for systemic adverse effects. The efficacy and safety profiles of MFNS seen in clinical use are consistent with its pharmacokinetic and pharmacodynamic properties.
糠酸莫米松鼻喷雾剂（MFNS）被推荐作为变应性鼻炎的一线治疗药物。鼻内给药的目的是在尽量减少全身暴露的同时，为受影响的鼻组织提供最大有效的治疗。
本文综述了MFNS的药代动力学和药效学特性，强调了有关其糖皮质激素受体结合、生物利用度和代谢的数据的潜在临床相关性，以及其在激活和抑制类固醇依赖性基因转录中的作用。
检索MEDLINE和EMBASE数据库（1995年1月至2007年7月），以识别关于MFNS的体外、临床前和临床研究以及综述文章。还进行了检索以识别本文中讨论的鼻用糖皮质激素的药代动力学、药效学和不良反应的文章。过敏学会会议的相关摘要和作者研究经验的数据也包括在内。
所综述的数据表明，MFNS具有许多重要特性，有助于在尽量减少全身不良反应的情况下实现鼻腔选择性。例如，MFNS在鼻组织中稳定，在肝脏中有效代谢（400μg剂量的AUC：127fmol/mL×h）。其全身生物利用度（0.46%）是目前可用鼻用糖皮质激素中最低的之一。在人类中未观察到生物活性糖皮质激素代谢产物。免疫学研究结果表明，MFNS可能通过优先抑制辅助性T细胞2型（Th2）相关细胞因子，而非辅助性T细胞1型相关细胞因子，来逆转变应性疾病中过度的Th2相关细胞因子反应。
MFNS是一种全身不良反应可能性低的鼻用糖皮质激素。临床使用中观察到的MFNS的疗效和安全性与其药代动力学和药效学特性一致。
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