环索奈德与布地奈德治疗儿童支气管哮喘的临床观察

目的:比较环索奈德与布地奈德治疗儿童支气管哮喘的疗效、安全性及对患儿外周血单个核细胞Aiolos基因表达的影响。方法:将86例支气管哮喘患儿随机均分为对照组和观察组。对照组患儿给予布地奈德气雾剂维持治疗,200μg/次,bid;观察组患儿给予环索奈德气雾剂维持治疗,150μg/次,qd。两组患儿疗程均为1年。随访和记录两组患儿哮喘急性发作情况,观察治疗前及治疗1个月、6个月、1年后的临床症状评分和呼气高峰流量占预计值百分比(PEFR%),检测治疗前及治疗1年后血皮质醇浓度和外周血单个核细胞中Aiolos基因表达情况及不良反应发生情况。结果:对照组患儿哮喘急性发作例次显著多于观察组(P<0.05);治疗后两组患儿临床症状评分、PEFR%与治疗前比较均显著改善,且观察组患儿治疗6个月、1年后的改善程度优于对照组(P<0.05);治疗前后两组患儿血皮质醇浓度比较,差异无统计学意义(P>0.05);治疗后两组患儿Aiolos基因表达水平均显著高于治疗前,且观察组高于对照组(P<0.05);观察组患儿不良反应发生率显著低于对照组(P<0.05)。结论:环索奈德较布地奈德治疗儿童支气管哮喘安全、有效,同时能有效促进患儿外周血单个核细胞Aiolos基因表达。     

环索奈德气雾剂治疗轻中度哮喘疗效观察

目的:评价环索奈德(CIC)气雾剂治疗轻中度哮喘的有效性和安全性。方法:采用多中心、随机、单盲、平行、阳性药物对照研究方法。将229例轻中度哮喘患者随机分为试验组与对照组,试验组给予国产CIC200μgqd治疗8周,对照组给予国产布地奈德(BUD)200μgbid治疗8周。观察治疗前、后晨间最大呼气流量(PEF)、夜间PEF、第1秒用力呼气容积(FEV1)、哮喘症状评分及缓解症状药物用量等指标。结果:经8周治疗后,2组晨间PEF、夜间PEF、FEV1、哮喘症状评分及缓解症状药物用量等指标较治疗前均有显著改善(P<0.05),但2组间的改善值差异无统计学意义(P>0.05)。主要不良反应是咽部发痒、疼痛和声音嘶哑,2组不良事件发生率差异无统计学意义(P>0.05)。结论:每天200μgCIC治疗轻中度哮喘与每天使用400μgBUD的疗效相当,且患者依从性更好。     

环索奈德干粉吸入剂的研究及其对豚鼠哮喘的抑制作用(英文)

环索奈德是目前处于临床研究阶段,用于治疗哮喘的新糖皮质激素类药物。本研究的目的是制备小剂量环索奈德干粉吸入剂(DPIs,80μg),并探讨其抗哮喘作用。采用球型乳糖作为稀释剂,与微粉化环索奈德混匀,制备环索奈德胶囊,置于干粉吸入装置中供口服吸入用。建立豚鼠哮喘模型,评价环索奈德抗哮喘作用。结果表明:制备得到的环索奈德干粉吸入剂的肺部沉积率约为26%,含量均匀度符合中国药典要求。在建立的哮喘豚鼠模型中,哮喘豚鼠肺泡间隔增宽,肺泡腔缩小,支气管黏膜上皮部分坏死、脱落,伴杯状细胞增生及嗜酸性粒细胞侵润。给予环索奈德治疗后,肺部病理症状得到了有效缓解或恢复,肺泡灌洗液(BALF)中细胞总数及嗜酸性粒细胞明显减少,IL-5水平降低,IFN-γ水平升高,表现出明显的治疗哮喘效果。本研究成功的制备了新型抗哮喘环索奈德肺部给药系统,并在动物模型上证实了其对哮喘的抑制作用。     

吸入性皮质激素联合班布特罗治疗支气管哮喘的分析

目的观察吸入性皮质激素布地奈德联合班布特罗治疗支气管哮喘的疗效.方法将我院67例轻、中度哮喘患者随机分为两组,34例应用吸入性皮质激素布地奈德联合班布特罗与33例应用吸入性皮质激素布地奈德患者间治疗效果相比较得出结论.结果吸入性皮质激素布地奈德联合班布特罗能有效地控制哮喘急性发作及其相关症状和降低哮喘患者的住院率,减少布地奈德的吸入量.结论吸入性皮质激素布地奈德联合班布特罗治疗支气管哮喘优于单一吸入性激素布地奈德的疗效.     

布地奈德联合多索茶碱治疗老年支气管哮喘的疗效观察

目的观察布地奈德联合多索荼碱治疗老年支气管哮喘的疗效。方法96倒老年支气管哮喘患者随机分为治疗组（48例）和对照组（48例）,对照组采用常规方法治疗,治疗组在对照组基础上加用布地奈德和多索荼碱治疗,两组疗程均为14d,观察两组治疗总有效率和治疗前后患者肺通气功能变化。结果治疗组总有效率97．4％,对照组总有效率72．9％,差异具有统计学意义（P〈0．05）;治疗组治疗后肺通气功能较对照组治疗后明显缓解（P〈0．05）。治疗组治疗过程中未出现明显不良反应。结论布地奈德联合多索荼碱治疗老年支气管哮喘有良好的疗效,且安全性高。     

孟鲁司特联合布地奈德气雾剂治疗小儿轻度持续哮喘30例

目的探讨孟鲁司特联合布地奈德气雾剂治疗小儿轻度持续哮喘的临床疗效。方法观察比较孟鲁司特联合布地奈德气雾剂治疗52例患儿与单用布地奈德气雾剂治疗22例患儿的疗效。结果孟鲁司特联合布地奈德气雾剂组总有效率为96.67%,单用布地奈德气雾剂组总有效率为68.18%,差异有统计学意义（P〈0.05）。结论孟鲁司特联合布地奈德气雾剂治疗小儿轻度持续哮喘效果明显。     

观察布地奈德粉吸入剂与多索茶碱联合治疗中、重度支气管哮喘的效果

目的:分析和观察针对中、重度支气管哮喘应用布地奈德粉吸入剂和多索茶碱结合的临床疗效.方法:选取2014年1月~2016年3月来我院治疗的中、重度支气管哮喘患者68例作为研究对象,均分成两组,每组34例.对照组给予单纯的布地奈德粉吸入剂进行治疗,而试验组应用布地奈德粉吸入剂和多索茶碱结合进行干预.结果:试验组治疗后呼吸、酸碱值、心率等临床指标均优于对照组,差异显著,P<0.05.两组动脉血气指标分析,试验组动脉血氧分压、二氧化碳分压均优于对照组,P<0.05.试验组在用药治疗后出现恶心呕吐、头痛头晕、四肢无力等不良反应人数少于对照组,P<0.05.结论:布地奈德粉吸入剂和多索茶碱在临床治疗和控制中、重度支气管哮喘上都有较好的作用,但是两种药物联合应用可以明显改善患者治疗期间的各项指标,减少了不良反应.     

布地奈德联用孟鲁司特对比单用布地奈德治疗儿童轻度支气管哮喘的疗效观察

目的：对布地奈德联用孟鲁司特对比单用布地奈德对儿童轻度支气管哮喘的疗效及安全性进行研究。方法选取本院收治的轻度支气管哮喘患儿共194例,将患儿分为3～5岁组和5～12岁组。其中3～5岁组71例,随机分为治疗组34例和对照组37例。5～12岁组123例,随机分为治疗组63例和对照组60例。治疗组患儿给予布地奈德雾化吸入联合孟鲁斯特钠口服,对照组仅布地奈德雾化吸入,两组患儿均连续治疗2周。将两组患儿的治疗效果进行比较。结果治疗组与对照组患儿的总有效率差异不存在统计学意义。结论治疗儿童轻度支气管哮喘单用布地奈德疗效即可,不需联用孟鲁司特。     

布地奈德或丙酸倍氯米松联合特布他林治疗小儿轻中度哮喘急性发作的疗效和安全性比较

目的:比较布地奈德或丙酸倍氯米松联合特布他林治疗小儿轻中度哮喘急性发作的疗效和安全性。方法:110例轻中度哮喘急性发作患儿随机分为A组(55例)和B组(55例)。在常规治疗的基础上,A组患儿给予硫酸特布他林雾化液1 mL,雾化吸入,每日2次+吸入用布地奈德混悬液2 mL,雾化吸入,每日2次;B组患儿给予硫酸特布他林雾化液(用法用量同A组)+吸入用丙酸倍氯米松混悬液2 mL,雾化吸入,每日2次。两组疗程均为7 d。观察两组患儿的临床疗效、症状体征消失时间、住院时间、哮喘缓解率,治疗前后症状体征评分、呼气峰流速(PEF)及不良反应发生情况。结果:两组患儿总有效率、症状体征消失时间、住院时间、哮喘缓解率、不良反应发生率比较,差异均无统计学意义(P>0.05)。治疗后,两组患儿症状体征评分均显著低于同组治疗前,PEF均显著高于同组治疗前,差异均有统计学意义(P<0.05);但两组间比较差异均无统计学意义(P>0.05)。结论:在常规治疗的基础上,布地奈德或丙酸倍氯米松联合特布他林均可用于治疗小儿轻中度哮喘急性发作,且两者的疗效和安全性均相当。     

多索茶碱与布地奈德联合治疗支气管哮喘的临床分析

目的探讨多索茶碱与布地奈德联合治疗支气管哮喘的临床疗效。方法选取2010年4月至2011年4月期间在我院接受治疗的支气管哮喘患者56例,随机将所有患者分为对照组和研究组各28例。对照组采用脉滴注多索茶碱进行治疗,研究组在静脉滴注多索茶碱的同时加用布地奈德进行治疗。结果治疗后,对照组的总有效率为78.57%,研究的总有效率为92.86%,两组总有效率比较,差异显著具有统计学意义(P<0.05)。两组患者的FEV1、VC和FVC及等肺通气功能指标均比治疗前有明显改善(P<0.05);且研究的各项肺通气功能指标均比对照组改善更明显(P<0.05)。讨论采用多索茶碱与布地奈德联合治疗支气管哮喘可以有效缓解各项肺通气功能,提高治疗有效率,且无严重不良反应出现发生,具有临床推广价值。     

Ciclesonide

Ciclesonide is an inhaled corticosteroid (delivered via a hydrofluoroalkane metered-dose inhaler) that is converted to an active metabolite, desisobutyryl-ciclesonide, in the lung, thereby minimising effects on endogenous cortisol. In two 12-week, randomised studies in patients with asthma, ciclesonide 80 or 320 microg once daily was at least as effective as budesonide 400 microg/day at increasing forced expiratory volume in 1 second (FEV1) and forced vital capacity (FVC) from baseline; ciclesonide 320 microg daily was significantly more effective than budesonide 400 microg once daily in one study. In a randomised, double-blind study in patients with asthma controlled with high-dosages of inhaled corticosteroids, FEV(1) and FVC decreased significantly from baseline at 12 weeks in patients receiving ciclesonide 320 microg daily or budesonide 400 microg daily; peak expiratory flow values decreased significantly only in patients receiving budesonide. Inhaled ciclesonide 80 or 320 microg daily improved asthma symptom scores and decreased the use of rescue medication by a similar, significant amount to budesonide 400 microg/day in two 12-week studies. Inhaled ciclesonide was generally well tolerated in patients with asthma. Ciclesonide did not suppress biochemical markers of adrenal function in 52-week studies. The long-term (>52 weeks) systemic effects of ciclesonide remain unknown.     

布地奈德混悬液联合复方异丙托溴铵治疗儿童哮喘发作的疗效观察

目的评价布地奈德雾化悬浊液联合复方异丙托溴铵溶液治疗儿童哮喘急性发作的临床疗效。方法90例哮喘急性发作的患儿随机分为治疗组50例和对照组40例,治疗组采用布地奈德雾化悬浊液联合复方异丙托溴铵溶液雾化吸入治疗,每日2次;对照组静脉使用地塞米松联合氨茶碱,每日1次,疗程5 d。治疗组和对照组患儿均采用综合治疗如补液、抗生素及抗病毒药物等。结果布地奈德雾化悬浊液联合复方异丙托溴铵溶液雾化吸入和静脉使用地塞米松联合氨茶碱均能有效控制儿童哮喘急性发作,治疗组和对照组疗效比较差异无显著性（P〉0.05）。结论布地奈德雾化悬浊液联合复方异丙托溴铵溶液治疗儿童哮喘发作的疗效与静脉使用地塞米松联合氨茶碱相当,依从性好,值得临床推广应用。     

支气管哮喘急性发作期雾化吸入治疗

目的观察雾化吸入布地奈德和特布他林对门诊轻、中急性发作期支气管哮喘患者的疗效。方法48例急性发作期支气管哮喘患者随机分为治疗组（26例）和对照组（22例）。治疗组每天雾化吸入布地奈德和特布他林雾化液7d，7d后吸入布地奈德气雾剂；对照组吸入布地夺德气雾剂和沙丁胺醇气雾剂（分别增加2次的剂量）；均于治疗前和治疗后第3、7和14d给予症状评分。结果治疗组治疗后第3、7d症状评分较对照组明显降低，但第14d两组无明显差异。结论雾化吸入布地奈德和特布他林起效快，可为门诊轻、中度急性发作期哮喘的首选给药方法。     

Lower oropharyngeal deposition of inhaled ciclesonide via hydrofluoroalkane metered-dose inhaler compared with budesonide via chlorofluorocarbon metered-dose inhaler in healthy subjects

Objective Inhaled corticosteroids may cause oropharyngeal side effects if deposited in the oropharynx in active form. Ciclesonide, an inhaled corticosteroid with low glucocorticoid receptor affinity, is activated primarily in the lung by esterases to an active metabolite, desisobutyryl-ciclesonide (des-CIC), with high glucocorticoid receptor affinity. We studied oropharyngeal deposition of ciclesonide, des-CIC, and budesonide.Methods In an open-label, randomized, two-treatment (administered in sequence), five-period study, 18 healthy subjects received 800 g (ex-valve) inhaled ciclesonide via a hydrofluoroalkane-pressurized, metered-dose inhaler followed by 800 g budesonide (Pulmicort) by a chlorofluorocarbon-pressurized, metered-dose inhaler (four puffs of 200 g each, ex-valve) or vice versa. Oropharyngeal cavity rinsing was performed immediately, or 15, 30, 45, or 60 min after inhalation (one rinsing per study period), and the solutions were analyzed using liquid chromatography with tandem mass spectrometric detection.Results Ciclesonide and budesonide were detected in most oropharyngeal wash samples. Maximal concentration of each inhaled corticosteroid was reached immediately post-inhalation; maximal concentrations of ciclesonide and des-CIC were 30% and 0.67%, respectively, of budesonide. Oropharyngeal deposition of ciclesonide and budesonide decreased rapidly within 15 min post-inhalation, and less rapidly thereafter. Less than 10% of the residual ciclesonide in the oropharynx was converted to des-CIC. The molar dose-adjusted amount of des-CIC was 4% of budesonide (P < 0.0001). There were no significant adverse events.Conclusion Oropharyngeal deposition of des-CIC was more than one order of magnitude lower than that of budesonide when administered by the respective metered-dose inhalers. This may explain the low frequency of oropharyngeal side effects of ciclesonide in clinical studies.     

Pharmacokinetic disposition of inhaled ciclesonide and its metabolite desisobutyryl-ciclesonide in healthy subjects and patients with asthma are similar

OBJECTIVE: To evaluate whether the inflammatory process and bronchial constriction associated with asthma influence the pulmonary distribution and airway penetration of inhaled ciclesonide by investigating the pharmacokinetics of ciclesonide and its active metabolite, desisobutyryl-ciclesonide (des-CIC) in patients with asthma and matched healthy subjects. METHODS: 12 patients with asthma (8 males, 4 females) and 12 healthy subjects matched for age, sex, height, and weight received a single inhaled dose of 1,280 microg (ex-actuator, equivalent to 1,600 microg ex-valve) ciclesonide by metered-dose inhaler in a parallel-group study. Timed blood samples were collected for measurement of serum concentrations of des-CIC and ciclesonide by liquid chromatography with tandem mass spectrometry. RESULTS: There were no differences in the pharmacokinetics of des-CIC between healthy subjects and patients with asthma. Ratio analysis of the primary variable, the area under the concentration-time curve from time 0 to infinity (AUC(0 - inf)) showed equivalence for des-CIC in healthy subjects and patients with asthma, with a ratio of 1.003 (90% confidence interval between 0.815 and 1.234). The mean terminal half-life (t1/2) for des-CIC was also similar in patients with asthma (3.15 hours) and healthy subjects (3.33 hours). Furthermore, the pharmacokinetic parameter estimates for ciclesonide were comparable between the study groups. CONCLUSION: After administration of a single dose of ciclesonide, the pharmacokinetic parameter estimates for des-CIC were equivalent between patients with mild-to-moderate asthma and healthy subjects, suggesting that there is comparable lung deposition and activation of ciclesonide in the 2 populations.     

孟鲁司特治疗支气管哮喘临床疗效观察

目的观察孟鲁司特治疗支气管哮喘的临床疗效。方法轻、中度支气管哮喘患者64例,随机分为2组。治疗组32例使用孟鲁司特10mg,每晚1片;对照组32例使用吸入型皮质激素布地奈德400μg/d吸入。2组均每天给予沙丁胺醇吸入,每天3～4次,整个观察期为5d。比较2组患者呼吸困难、咳嗽、喘息、哮鸣音的病情评价、症状消失的时间及2组治疗有效率情况。结果2组患者呼吸困难、咳嗽、喘息、哮鸣音的病情评价及症状消失的时间比较,差异无统计学意义（P〉0.05）。结论孟鲁司特能明显改善轻、中度哮喘患者呼吸困难、咳嗽、喘息症状、肺功能,作为一种治疗支气管哮喘的抗炎和平喘的新型药物,具有较好临床价值。     

Two-dimensional and three-dimensional imaging show ciclesonide has high lung deposition and peripheral distribution: a nonrandomized study in healthy volunteers.

Drug deposition is an important factor that contributes to safety and efficacy outcomes of inhaled steroid therapy. Ciclesonide is a nonhalogenated, inhaled corticosteroid under investigation for the treatment of asthma. Therefore, this study was performed to assess lung deposition of ciclesonide. Technetium-99m (99mTc)-labeled ciclesonide (where the 99mTc-label is physically dissolved in the ciclesonide-hydrofluoroalkane [HFA] solution aerosol) inhaled by healthy volunteers was analyzed by two-dimensional (2-D) and three-dimensional (3-D) imaging to determine lung deposition. Six healthy volunteers inhaled one puff of 40 microg (exactuator, equivalent to 50 microg ex-valve) ciclesonide for 2-D imaging, and two healthy volunteers inhaled 10 puffs of 40 microg ciclesonide for 2-D and 3-D imaging. The ciclesonide aerosol was administered via metered-dose inhaler (MDI) containing HFA-134a as propellant. The ex-actuator mean (+/- standard deviation) deposition of ciclesonide in the lungs was higher (52% +/- 11%) than in the mouth/pharynx (38% +/- 14%). Two-dimensional and 3-D imaging showed that ciclesonide reached all regions of the lung. Mean percent deposition in peripheral regions (47% and 34%) was higher than in lower central regions (17% and 30%), as revealed by 3-D and 2-D imaging, respectively. Inhalation of up to 400 microg of ciclesonide produced no drug-related side effects. In conclusion, ciclesonide administered via metered-dose inhaler using HFA-134a as a propellant provided high lung deposition (>50%), greater distribution throughout peripheral regions of the lungs, and relatively low oropharyngeal deposition.     

我院儿科抗哮喘药物用药分析

目的：分析我院儿科门诊抗哮喘药物的用药情况,为临床合理用药提供参考。方法：采用回顾性研究方法,对我院儿科门诊2013年8月至2015年7月抗哮喘药物的用药金额、用药频度（DDDs）、合理用药情况等进行统计分析。结果：我院儿科2013年8月至2014年7月和2014年8月至2015年7月的抗哮喘药物总用药金额分别为122.86万元和175.31万元,后者比前者增加42.69%;两个时间段的吸入制剂用药金额构成比均>60%。用药金额排前3位的药品依次是孟鲁司特钠片、布地奈德福莫特罗粉吸入剂、吸入用布地奈德混悬液;DDDs排前3位的药品依次是布地奈德/福莫特罗粉吸入剂、孟鲁司特钠片、吸入用异丙托溴铵溶液。2013年8月至2014年7月和2014年8月至2015年7月的哮喘患儿分别为182例和276例,合理用药率分别为84.62%和90.22%,不合理用药情况主要是用量不当、联用不当、选药不当。结论：我院门诊主要为轻、中度哮喘患儿,治疗药物以布地奈德和孟鲁司特为主,主要采用吸入途径给药,抗哮喘药物的合理用药水平有待进一步提高。