Mometasone furoate dry powder inhaler: a once-daily inhaled corticosteroid for the treatment of persistent asthma

ABSTRACT

Background: 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.

Scope: 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.

Findings: 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 β₂?agonists for symptom relief. Once-daily dosing in the evening with MF-DPI 200?µg conferred a greater benefit than morning dosing with MF-DPI 200?µg. 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.

Limitations: 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.

Conclusion: Once-daily administration of MF-DPI 200–400?µg 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?µg BID permitted substantial reduction of oral corticosteroid use. All MF-DPI treatments were well tolerated and had minimal systemic effects.     

糠酸莫米松鼻喷剂在鼻内窥镜术后的疗效

目的:探讨糠酸莫米松鼻喷雾剂在功能性鼻内窥镜术后治疗慢性副鼻窦炎的疗效。方法:将接受鼻内镜术后的355例慢性鼻窦炎鼻息肉患者随机分为两组,治疗组180例,对照组175例。治疗组术前及术后局部使用糠酸莫米松鼻喷雾剂,观察其疗效。结果:根据鼻内窥镜手术疗效标准,治疗组治愈率及有效率与对照组比较治愈率及有效率有统计学意义(P<0.01),术后鼻腔黏膜上皮化时间:治疗组(40±5.06)d,对照组(47±29.4)d,差异有统计学意义(P<0.01)。结论:糠酸莫米松鼻喷雾剂在功能性鼻内窥镜术后缩短鼻腔粘膜上皮化时间及减少慢性鼻窦炎复发效果显著。     

糠酸莫米松鼻喷剂在儿童腺样体肥大治疗中的作用

目的探讨糠酸莫米松鼻喷剂在儿童腺样体肥大治疗中临床应用价值。方法对78例腺样体肥大患儿,分成两组:安慰剂组,35例每天用鼻腔冲洗器冲洗鼻腔1次;用药组43例,给予糠酸莫米松鼻喷剂50μg,1次/d。治疗3个月,随访12个月。在治疗前、治疗3个月和治疗后12个月,分别进行鼻声反射检查和症状评分。结果安慰剂组各时间段临床评分和鼻咽部体积无明显改变(P>0.05);用药组在用药后3个月,患儿临床评分为8.25±2.31,鼻咽部体积为20.87 cm3±3.56 cm3,与用药前临床评分10.30±1.51,及鼻咽部的体积15.21 cm3±2.17 cm3相比,具有统计学意义(P<0.01)。在随访12个月,临床评分和鼻咽部体积与治疗前相比有明显好转,具有统计学意义(P<0.01)。结论糠酸莫米松鼻喷剂能够减小肥大腺样体的体积,减轻慢性鼻阻塞的严重程度,为非手术治疗提供了新的途径。     

糠酸莫米松治疗小儿腺样体肥大的疗效观察

目的观察糠酸莫米松治疗小儿腺样体肥大的临床效果。方法将65例腺样体肥大病例随机分为治疗组35例和对照组30例,治疗组使用糠酸莫米松喷鼻+鼻腔冲洗,对照组用麻黄素滴鼻+鼻腔冲洗。随访3个月,比较两组的疗效。结果治疗组23例有效,总有效率65.7%,12例无效;对照组12例有效,总有效率40.0%,治疗组总有效率高于对照组,差异有统计学意义(P<0.05)。结论糠酸莫米松鼻腔局部用药可以改善临床症状,是治疗儿童腺样体肥大的有效方法,是部分腺样体肥大患儿保守治疗的一种选择。     

糠酸莫米松鼻喷雾剂与孟鲁司特钠联合治疗儿童季节性变应性鼻炎的临床疗效分析

目的 :探讨糠酸莫米松鼻喷雾剂与孟鲁司特钠联合治疗儿童季节性变应性鼻炎的临床疗效.方法 :收集医院2012年1月~2015年9月的64例季节性变应性鼻炎患儿作为研究对象,依据随机对照原则分两组.对照组患儿糠酸莫米松鼻喷雾剂治疗,联合组给予糠酸莫米松鼻喷雾剂+孟鲁司特钠联合治疗,对两组临床疗效、临床症状积分和炎性因子变化进行对比观察.结果 :联合组临床治疗有效率优于对照组(96.9%Vs75.0%),数据比较差有统计学意义.治疗后两组患儿喷嚏、流涕、鼻塞和鼻痒四项评分均较治疗前明显的降低,而IL-10、IL-4和IFN-γ 以及IgE均较治疗前明显的改善,联合组优于对照组,数据比较差有统计学意义.结论 :临床中对于儿童季节性变应性鼻炎患儿应用糠酸莫米松鼻喷雾剂与孟鲁司特钠联合治疗效果显著,改善临床症状,减轻炎性因子作用,更值得临床中应用推广.     

Nasal allergies and beyond: a clinical review of the pharmacology, efficacy, and safety of mometasone furoate

Mometasone furoate nasal spray (MFNS; Nasonex^®, Schering-Plough Corporation, Kenilworth, NJ, USA) is an effective and well-tolerated intranasal corticosteroid approved for the prophylactic treatment of seasonal allergic rhinitis, and the treatment of perennial allergic rhinitis. MFNS is a potent molecule with a rapid onset of action and excellent safety and efficacy profiles. Having recently received approval for the treatment of nasal polyposis, data indicate that MFNS may also be effective in rhinosinusitis.     

Fluticasone furoate nasal spray: a single treatment option for the symptoms of seasonal allergic rhinitis

BACKGROUND: Fluticasone furoate (USAN-approved name) is a novel, enhanced-affinity glucocorticoid administered in a unique side-actuated device for the management of seasonal allergic rhinitis (SAR). OBJECTIVE: We sought to evaluate the efficacy and safety of once-daily fluticasone furoate nasal spray, 110 microg, in patients aged 12 years or older with fall SAR. METHODS: Patients (n = 299) received fluticasone furoate or placebo for 2 weeks in this double-blind, parallel-group randomized study. Patients evaluated nasal and ocular symptoms using a 4-point categoric scale. Efficacy was assessed on the basis of the mean change from baseline in reflective and instantaneous total nasal symptom scores and reflective total ocular symptom scores. RESULTS: Fluticasone furoate produced significantly greater improvements than placebo in daily reflective total nasal symptom score (-1.473, P < .001; primary end point), morning predose instantaneous total nasal symptom score (-1.375, P < .001), daily reflective total ocular symptom score (-0.600, P = .004), and patient-rated overall response to therapy (P < .001). The onset of therapeutic effect occurred at 8 hours after initial administration. Fluticasone furoate was well tolerated. CONCLUSION: Fluticasone furoate, 110 microg once daily, was effective and well tolerated for the treatment of nasal symptoms of SAR in patients aged 12 years and older. Treatment also produced significant improvements in ocular symptoms. Fluticasone furoate was fast acting, as indicated by an 8-hour onset of action, and provided 24-hour symptom control. CLINICAL IMPLICATIONS: New treatments for the bothersome symptoms of SAR are needed. One such treatment, fluticasone furoate nasal spray, provides effective relief of the symptom profile of SAR.     

RPLC Determination of Tinidazole and Diloxanide Furoate in Tablets

A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of tinidazole and diloxanide furoate. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and 0.2 M potassium dihydrogen phosphate (pH 5) in the ratio 2:3:2.The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 282 nm. The described method was linear over a concentration range of 10-70 μg/ml and 10-90 μg/ml for the assay of diloxanide furoate and tinidazole, respectively. The mean recovery was found to be 100-101% for tinidazole and 97-103% for diloxanide furoate when determined at three different levels.     

Sensitization studies with mometasone furoate, tixocortol pivalate, and budesonide in the guinea pig

Mometasone furoate is a new corticosteroid, synthesized to have an improved ratio of anti-inflammatory potential to adverse effects. The guinea pig maximization test was used to determine the sensitizing capacity of mometasone furoate, and also to investigate cross-reaction patterns in animals sensitized to tixocortol pivalate and budesonide, respectively. Tixocortol pivalate was shown to be a sensitizer in the guinea pig, but cross-reactions to other tested corticosteroids wore not observed. Furthermore, no sensitizing capacity could be demonstrated for budesonide or mometasone furoate.