Karpel Jill P, Nelson Harold
North Shore-Long Island Jewish Health System, New Hyde Park, NY 11040-1101, USA.
Curr Med Res Opin. 2007 Nov;23(11):2897-911. doi: 10.1185/030079907x242485.
Mometasone furoate (MF), a potent synthetic inhaled corticosteroid (ICS) with a high affinity for the glucocorticoid receptor, is approved for use in the treatment of asthma.
Publications reviewed in this article were identified via searches of MEDLINE and EMBASE databases using the terms 'mometasone furoate AND pharmacology' and 'mometasone furoate AND asthma AND clinical trial'. Data from abstracts presented at respiratory society meetings, and relevant background information, are also reviewed.
In clinical studies, MF, administered by dry powder inhaler (MF-DPI), was effective in treating all severities of persistent asthma, improving pulmonary function, reducing asthma symptoms, and reducing or eliminating the need for oral corticosteroids. Once-daily dosing of MF-DPI was effective in patients with mild or moderate persistent asthma previously taking twice-daily regimens of inhaled corticosteroids (ICSs), and in patients taking only inhaled beta2-agonists for symptom relief. Once-daily dosing in the evening with MF-DPI 200 microg conferred a greater benefit than morning dosing with MF-DPI 200 microg. Patients with severe asthma who were dependent on oral corticosteroids (OCSs) and high doses of ICSs were able to achieve greater asthma control and reduce or even eliminate OCSs when switched to MF-DPI. In trials of up to 1 year in duration, MF-DPI was well tolerated, with the majority of adverse events considered mild or moderate in intensity. MF had low systemic bioavailability and no clinically significant hypothalamic-pituitary-adrenal-axis suppression at therapeutic doses. The DPI device is a multiple-dose inhaler with a counter containing agglomerates of MF and lactose. Patients of all severities of persistent asthma were able to generate and maintain airflow profiles necessary to provide a uniform and accurate dose.
Only one study evaluated both morning and evening administration of once-daily doses, and one of the comparative clinical trials was an open-label study.
Once-daily administration of MF-DPI 200-400 microg in patients with mild to moderate persistent asthma effectively improved lung function and asthma control. In patients with severe persistent asthma dependent on oral corticosteroids, treatment with MF-DPI 400 microg BID permitted substantial reduction of oral corticosteroid use. All MF-DPI treatments were well tolerated and had minimal systemic effects.
糠酸莫米松(MF)是一种强效合成吸入性糖皮质激素(ICS),对糖皮质激素受体具有高亲和力,已被批准用于治疗哮喘。
本文所综述的出版物是通过检索MEDLINE和EMBASE数据库确定的,检索词为“糠酸莫米松与药理学”以及“糠酸莫米松与哮喘与临床试验”。还对在呼吸学会会议上发表的摘要数据以及相关背景信息进行了综述。
在临床研究中,通过干粉吸入器(MF-DPI)给药的MF对治疗各种严重程度的持续性哮喘有效,可改善肺功能、减轻哮喘症状,并减少或消除口服糖皮质激素的需求。对于先前采用每日两次吸入性糖皮质激素(ICS)治疗方案的轻度或中度持续性哮喘患者,以及仅使用吸入性β2受体激动剂缓解症状的患者,MF-DPI每日一次给药有效。与MF-DPI 200微克早晨给药相比,MF-DPI 200微克晚上每日一次给药带来的益处更大。依赖口服糖皮质激素(OCS)和高剂量ICS的重度哮喘患者在改用MF-DPI后能够实现更好的哮喘控制,并减少甚至停用OCS。在长达1年的试验中,MF-DPI耐受性良好,大多数不良事件的强度被认为是轻度或中度。MF的全身生物利用度低,在治疗剂量下对下丘脑-垂体-肾上腺轴无临床显著抑制作用。DPI装置是一种多剂量吸入器,带有一个计数器,含有MF和乳糖的聚集体。各种严重程度的持续性哮喘患者都能够产生并维持所需的气流分布,以提供均匀且准确的剂量。
只有一项研究评估了每日一次剂量的早晨给药和晚上给药,并且其中一项比较性临床试验是开放标签研究。
对于轻度至中度持续性哮喘患者,MF-DPI每日一次给予200 - 400微克可有效改善肺功能和哮喘控制。对于依赖口服糖皮质激素的重度持续性哮喘患者,MF-DPI每日两次给予400微克可大幅减少口服糖皮质激素的使用。所有MF-DPI治疗耐受性良好,全身影响极小。