Cowie Robert L, Giembycz Mark A, Leigh Richard
Faculty of Medicine, University of Calgary, Institute of Infection, Immunity and Inflammation, Department of Medicine, 3280 Hospital Drive NW, Calgary, Alberta, Canada.
Expert Opin Pharmacother. 2009 Aug;10(12):2009-14. doi: 10.1517/14656560903078428.
Mometasone furoate has been available for clinical use, starting with a dermatologic preparation, for nearly 20 years. An inhaled format of the drug for management of asthma had been in development during the last decade and has been available for clinical use for 6 years as a dry powder inhaler delivering either 100 mcg or 200 mcg per dose. It has a long half-life and is suitable for daily dosing. The drug is approved for use in the USA for the treatment of asthma in patients aged 4 years or over. Mometasone furoate is a topically potent glucocorticoid with a favorable risk-benefit profile. A wide variety of randomized clinical trials have shown the drug to have a clinically beneficial effect on asthma comparable to fluticasone propionate, and to permit the reduction or withdrawal of oral glucocorticoid therapy in patients with asthma. Mometasone furoate has approximately 1% oral bioavailability but does produce systemic glucocorticoid effects from the drug released from the lung and its metabolites. These effects are minimal when mometasone is used appropriately at low or moderate doses.
糠酸莫米松用于临床已有近20年,最初是一种皮肤科制剂。过去十年中一直在研发用于治疗哮喘的吸入剂型,作为一种每剂可提供100微克或200微克的干粉吸入器,已可供临床使用6年。它的半衰期长,适合每日给药。该药物在美国被批准用于治疗4岁及以上患者的哮喘。糠酸莫米松是一种局部强效糖皮质激素,具有良好的风险效益比。大量随机临床试验表明,该药物对哮喘具有与丙酸氟替卡松相当的临床有益效果,并可使哮喘患者减少或停用口服糖皮质激素治疗。糠酸莫米松的口服生物利用度约为1%,但确实会因肺部释放的药物及其代谢产物而产生全身性糖皮质激素效应。当以低剂量或中等剂量适当使用糠酸莫米松时,这些效应极小。