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1.
噻托溴胺(tiotropiumbromide)是一个新型的用于治疗慢性阻塞性肺疾病(COPD)的吸入型支气管扩张药物,通过与M3受体结合,拮抗乙酰胆碱的作用,缓解支气管平滑肌的痉挛。吸入一次疗效持续24小时以上。几个大样本的临床试验结果表明,该药物对中重度COPD具有良好的疗效,在改善呼吸困难、生活质量、减少住院次数方面要优于沙美特罗,每日吸入一次噻托溴胺对支气管的舒张作用要明显好于每日吸入四次的溴化异丙托品和每日吸入两次的沙美特罗。而且该药物能够改善通气功能和肺容积,用药的耐受性和安全性也比较好。  相似文献   

2.
噻托溴铵治疗慢性阻塞性肺疾病作用机制研究进展   总被引:2,自引:0,他引:2  
曹玉海  张焕萍 《国际呼吸杂志》2008,28(21):1329-1332
噻托溴铵是一种新型长效抗胆碱类药物,是目前第一个能每日用药1次的吸人性药物,能高度选择性作用于胆碱M1和M3受体,表现出强大的支气管扩张作用,吸入一次疗效持续24 h以上.临床实验结果表明该药对中、重度慢性阻塞性肺疾病具有良好疗效,与其他常用抗胆碱能药物和β2受体激动剂相比较,噻托溴铵可显著改善肺功能、减少急性发作和改善生命质量,耐受性和安全性较好,主要不良反应为口干.  相似文献   

3.
目的观察不使用长效β2-激动剂情况下,应用噻托溴铵联合吸入糖皮质激素对哮喘-慢阻肺重叠综合征(ACOS)患者的治疗作用,并与单用噻托溴铵及单纯吸入糖皮质激素的治疗手段进行对比。方法根据"ACOS"诊断标准选择60例患者,分为噻托溴铵联合布地奈德粉吸入剂组、单用布地奈德粉吸入剂组、单用噻托溴铵组,三组分别进行肺功能、ACT、CAT及急性加重次数的比较。结果治疗后3组患者中噻托溴铵联合布地奈德(C)组肺功能改善率明显高于噻托溴铵(A)组、布地奈德粉吸入剂(B)组(P0.05)。治疗后三组患者用于哮喘症状评估的ACT评分噻托溴铵联合布地奈德(C)组较单用噻托溴铵、单用布地奈德治疗的两组症状改善更明显(P0.05),而治疗后三组患者CAT评分噻托溴铵联合布地奈德(C)组较单用噻托溴铵、单用布地奈德治疗的两组症状改善更明显。结论噻托溴铵联合糖皮质激素吸人治疗可以明显改善ACOS患者的肺功能和临床症状,减少急性发作次数,其疗效优于单用糖皮质激素吸入和单用噻托溴铵吸入治疗,可改善其短期预后。  相似文献   

4.
异丙托溴铵(ipratropium bromide,爱全乐)是临床上常用的一种抗胆碱药物,噻托溴铵(tiotropium,思力华)是一种新型、强力和长效的选择性吸入型胆碱能受体拮抗剂。噻托溴铵与异丙托溴铵同M1、M2和M3受体的亲和力大致相等,但是,噻托溴铵从M1、M3胆碱受体复合物上解离的速度要比从M2胆碱受体复合物上解离的速度慢3.5和8倍。异丙托溴铵与β2受体激动剂联合应用具有叠加、互补作用,与单独应用β2受体激动剂,前者能显著提高肺功能,缩短住院时间,且副作用无明显增加,目前推荐两者联合应用治疗重症哮喘。噻托溴铵可以明显缓解患者呼吸困难症状,改善生活质量及日常体力活动,减少短效β2受体激动剂的使用次数,适用于哮喘等气道痉挛及气道高反应性患者的长期使用。  相似文献   

5.
目的观察长期吸入噻托溴铵及应用缓释茶碱对慢性阻塞性肺疾病(COPD)稳定期生存质量及肺功能的影响。方法对96例确诊为COPD稳定期患者随机分为两组,噻托溴铵组给予常规治疗加用长期吸入噻托溴铵,缓释茶碱组为常规治疗加用茶碱缓释片,对两组的生存质量及肺功能进行对比,评价噻托溴铵与缓释茶碱对COPD稳定期患者生存质量及肺功能的影响。结果噻托溴铵较缓释茶碱能提高生存质量及肺功能,有明显的差异性;噻托溴铵组用药1个月肺功能较治疗前无明显改善,3个月后能明显改善肺功能。结论长期吸入噻托溴铵较缓释茶碱能更好的改善患者生存质量及肺功能。  相似文献   

6.
目的探讨噻托溴铵治疗老年慢性阻塞性肺疾病(COPD)稳定期患者的临床疗效。方法 90例老年COPD稳定期患者均吸入噻托溴铵每日1粒,疗程3月,比较患者治疗前后肺功能、血气分析指标、慢性阻塞性肺疾病评估测试(CAT)评分。结果噻托溴铵治疗后血氧分压显著改善(P〈0.05),二氧化碳分压明显降低(P〈0.05);治疗前后CAT评分差异有统计学意义(P〈0.05)。结论噻托溴铵吸入治疗老年COPD稳定期患者,能明显改善肺功能、改善氧合,缓解症状,提高生活质量,是治疗老年COPD稳定期患者的有效选择。  相似文献   

7.
在大规模的COPD循证医学研究中,噻托溴铵对肺功能的潜在长期疗效(understanding potential long-term impacts on function with tiotropium,UPLIFT)研究内容较为丰富,影响意义深远[1-2].UPLIFT研究结果显示,噻托溴铵组吸入支气管舒张剂前后FEV1均值明显高于对照组,治疗30 d后两组吸入支气管舒张剂前后的FEV1年下降率无明显差别;噻托溴铵组的生命质量高于对照组,急性加重和住院次数及呼吸衰竭发生率均低于对照组,提示噻托溴钱有降低COPD患者病死率的趋势,对COPD临床进程有积极的治疗作用[1].  相似文献   

8.
目的 观察肺康复联合吸入噻托溴铵粉剂对中-重度COPD稳定期患者BODE指数的影响.方法 选择我院呼吸科门诊2013年10月至2015年7月确诊COPD稳定期患者60例,分为联合组(肺康复联合噻托溴铵)和对照组.对照组给予常规COPD药物基础上吸入单一噻托溴铵粉吸入剂治疗.联合组指在常规药物治疗基础上给予肺康复(包括呼吸功能锻炼、长期家庭氧疗、营养支持、心理疏导等综合治疗),联合每日吸入噻托溴铵粉吸入剂.对比2组治疗后3个月、6个月的BODE指标及BODE指数变化.结果 联合组与对照组比较治疗3个月后BODE指标(BMI、呼吸困难程度、6MWD、FEV1% pred)、BODE指数有改善,差异有统计学意义(t=2.23,P>0.05;t=2.44、7.78、4.36、2.61,P<0.05),治疗6个月后BODE指标(BMI、呼吸困难程度、6MWD、FEV2% pred)、BODE指数有显著改善,差异有统计学意义(t=4.26、3.25、23.74、9.73、4.78,P<0.05).结论 中-重度COPD稳定期患者实施肺康复联合吸入噻托溴铵粉剂治疗后,BODE相关指标及BODE指数显著改善,长期的肺康复及噻托溴铵使用有更大获益.  相似文献   

9.
陈淑娟 《临床肺科杂志》2010,15(9):1335-1336
目的观察噻托溴铵吸入剂(思力华吸入剂)治疗慢性阻塞性肺病(COPD)疗效;方法对13例COPD患者给予噻托溴铵吸入剂每日1粒,长期吸入一年,长期随访,并观察给药前及一年后肺功能,血气分析指标及临床症状的变化。结果治疗一年后,肺功能指标较治疗前均有明显的改善(P〈0.01),年平均住院次数,住院天数(分别为治疗前的33%,17.2%)与治疗前均有差异;患者咳嗽、气促的症状较治疗前减轻,结论噻托溴铵吸入剂长期吸入可明显改善喘鸣及气促的症状,显著提高肺功能,改善缺氧症状,提高患者的生活质量,具有良好的经济效益和社会效益。  相似文献   

10.
目的:研究在长效β_2激动剂/吸入糖皮质激素(ICS/LABA)基础上加用噻托溴铵Respimat~(LAMA)治疗高龄慢性阻塞性肺疾病(COPD)患者的疗效和安全性。方法:54例肺功能GOLD 3级或4级、并使用ICS/LABA的高龄COPD患者随机分为2组,1组加用噻托溴铵Respimat~,另1组继续原治疗方案,比较用药12个月时2组的肺功能变化、COPD评估测试评分变化、年急性加重人数和次数、药物相关不良事件。结果:用药12个月时LAMA+ICS/LABA组的第1秒用力呼气容积(FEV_1)、用力肺活量(FVC)年下降值低于ICS/LABA组,COPD评估测试评分改善值高于ICS/LABA组(均P0.05);LAMA+ICS/LABA组急性加重的入院总次数低于ICS/LABA组(P0.05);2组均未发生严重心血管事件,药物相关不良事件无统计学差异。结论:在ICS/LABA基础上加用噻托溴铵Respimat~可改善老年COPD患者的肺功能和临床症状,安全性和依从性好。  相似文献   

11.
Anticholinergics are agents of first choice for the symptomatic treatment of patients with COPD. Tiotropium (Ba 679 BR, Spiriva) is a long-acting inhaled anticholinergic designed for once-daily bronchodilator treatment of COPD. Tiotropium is a selective antagonist of pulmonary M1 and M3 muscarinic receptor subtypes, that produces a long-lasting (24 hours), dose-dependent bronchodilation and bronchoprotection against constrictive stimuli, e. g. methacholine, following inhalation of single doses. Clinical trials with tiotropium in COPD patients over a maximum treatment duration of one year have confirmed a persisting bronchodilator effect of tiotropium compared with placebo and ipratropium, as well as meaningful clinical improvements in lung function, hyperinflation, exercise tolerance, symptom control and quality of life. Moreover, recent trials indicate that treatment with tiotropium also reduces the frequency of COPD exacerbations and hospitalizations. Comparative trials further suggest that the bronchodilator potency of tiotropium may be superior to those of available COPD treatments. Besides a higher incidence of dry mouth, the side effect profile was comparable to ipratropium bromide. In conclusion, present clinical data suggest that tiotropium has the potential of a first-line treatment for patients with COPD.  相似文献   

12.
目的探讨老年人COPD稳定期应用噻托溴铵治疗的疗效。方法选取58例慢性阻塞性肺疾病稳定期的患者,并随机分成两组即噻托溴铵组(30例)和异丙托溴铵组(28例),噻托溴铵组给予噻托溴铵治疗,异丙托溴铵组给予异丙托溴铵治疗,两组疗程均为60天,通过观察两组患者临床症状及肺功能改善情况等指标,分析对比两组疗效差别。结果噻托溴铵组的临床症状、肺功能改善情况明显优于异丙托溴铵组相关指标,P<0.05。结论噻托溴铵用于稳定期COPD的治疗效果优于异丙托溴铵。  相似文献   

13.
Bronchodilator therapy forms the mainstay of treatment for symptomatic patients with COPD. Long-acting bronchodilators, which maintain sustained airway patency over a 24-hour period, represent an advance in therapy. Tiotropium bromide is a new long-acting inhaled anticholinergic agent with superior pharmacodynamic properties compared with the short-acting anticholinergic, ipratropium bromide. Tiotropium bromide has been consistently shown to have a greater impact than ipratropium bromide on clinically important outcome measures such as health status. The mechanisms of clinical benefit with tiotropium bromide are multifactorial, but improved airway function, which enhances lung emptying and allows sustained deflation of over-inflated lungs, appears to explain improvements in dyspnea and exercise endurance in COPD. Inhaled tiotropium bromide therapy has also been associated with reduction in acute exacerbations of COPD as well as reduced hospitalizations. The safety profile of tiotropium bromide is impressive: dry mouth is the most common adverse event and rarely necessitates termination of the drug. No tachyphylaxis to tiotropium bromide has been demonstrated in clinical trials lasting up to 1 year. There is preliminary information that the combination of long-acting anticholinergics and long-acting beta2-adrenoceptor agonists provides additive physiological and clinical benefits. According to recent international guidelines, long-acting bronchodilators should be considered early in the management of symptomatic patients with COPD in order to achieve effective symptom alleviation and reduction in activity limitation. Tiotropium bromide, because of its once-daily administration and its established efficacy and tolerability profile, has emerged as an attractive therapeutic option for this condition.  相似文献   

14.
长效抗胆碱药物噻托溴铵的研究进展   总被引:1,自引:0,他引:1  
噻托溴铵是长效抗胆碱能药物,主要作用于M3受体,具有长效而持续的支气管扩张作用,在慢性阻塞性肺疾病患者管理中的应用获得肯定.还能抑制黏蛋白分泌、抑制气道重塑、具有抗炎作用.因此,对哮喘和其他黏液高分泌性疾病具有一定的治疗作用.  相似文献   

15.
尤宜  朱慕云 《临床肺科杂志》2010,15(10):1377-1379
目的研究吸入噻托溴铵联合舒利迭治疗稳定期中重度慢性阻塞性肺疾病(COPD)的治疗效果。方法 45例稳定期中重度COPD患者(完成实验43例,因病情加重退出实验2例)随机分成两组,治疗组给予噻托溴铵(商品名:思力华)及舒利迭(沙美特罗/氟替卡松)吸入治疗12周,对照组给予舒利迭吸入治疗12周,比较两组治疗前后临床症状、体征、血氧饱和度及肺功能主要指标。结果与对照组比较,治疗组FEV1/FVC以及FEV1占预计值百分比显著提高,临床症状体征及血氧饱和度明显改善(P0.05)。结论吸入噻托溴铵联合舒利迭可有效改善肺功能并缓解临床症状。  相似文献   

16.
17.
Bronchodilation with a long-acting muscarinic antagonist (LAMA) or long-acting β(2)-agonist is central to the management of chronic obstructive pulmonary disease (COPD). Tiotropium, the first LAMA available for use in COPD, has been shown to be an effective bronchodilator and is generally safe and well tolerated. However, tiotropium has limitations that include a high incidence of dry mouth, slow onset of action and, in some studies, a part of the patient population did not achieve clinically significant bronchodilation. It also remains unclear whether tiotropium reduces progressive deterioration of lung function in patients with COPD. An ideal LAMA would provide clinically meaningful bronchodilation, deliver symptom relief, prevent disease progression, improve exercise tolerance and health status, prevent and treat complications and exacerbations and reduce mortality risk. A 24-h duration of action, rapid onset of action and a good safety and tolerability profile are also desirable. The once-daily LAMA, NVA237 (glycopyrronium bromide), may meet some of these characteristics. NVA237 has high selectivity for the muscarinic type-3 (M(3)) receptor which might potentially result in a higher therapeutic index than tiotropium, which is less selective for M(3). Phase II studies showed that NVA237 once daily provides clinically significant 24-h bronchodilation with a rapid onset of action and a favourable safety and tolerability profile. Phase III studies are ongoing that will assess the long-term safety and efficacy of NVA237.  相似文献   

18.
Tiotropium bromide (Spiriva) is a long-acting anticholinergic bronchodilator that maintains bronchodilation for at least 24 hours, allowing once-daily administration. The active moiety is the tiotropium cation (tiotropium); tiotropium bromide 22.5 micrograms is equivalent to 18 micrograms of tiotropium cation. Greater improvements in lung function from baseline (primary endpoint mean trough FEV(1)) were observed with inhaled tiotropium 18 micrograms once daily than with placebo in 6-month and 1-year randomized, double-blind trials in patients with COPD. Tiotropium improved lung function (trough FEV(1) response) more effectively than ipratropium bromide (ipratropium) 40 micrograms four times daily in 1-year clinical trials, and was at least as effective as salmeterol 50 micrograms 12-hourly in 6-month trials. Preliminary data suggest that tiotropium alone or in combination with once-daily formoterol has a greater bronchodilator effect than twice-daily formoterol in patients with COPD. Improvements in patients' perception of health-related quality of life (HR-QOL) or dyspnea were greater with tiotropium than with placebo or ipratropium, and were similar to those with salmeterol. Reductions in the frequency and severity of acute exacerbations and in the use of rescue medication were also greater with tiotropium than with ipratropium or placebo. There was no evidence of tachyphylaxis with tiotropium during 1-year clinical trials. Inhaled tiotropium was generally well tolerated in clinical trials. Apart from dry mouth, the type and incidence of adverse events with tiotropium were similar to those with ipratropium, salmeterol or placebo in patients with COPD. In conclusion, inhaled tiotropium 18 micrograms once daily improved lung function, dyspnea, and HR-QOL, and decreased the incidence of acute COPD exacerbations and the use of rescue medication relative to placebo or ipratropium in clinical trials in patients with COPD. Tiotropium was at least as effective as salmeterol in terms of bronchodilator efficacy and improvements in dyspnea or HR-QOL. With the exception of dry mouth, the tolerability profile of tiotropium was similar to that with placebo, ipratropium, or salmeterol. Consequently, inhaled tiotropium is likely to be a valuable option for first-line, long-term maintenance therapy in the management of bronchoconstriction in patients with symptomatic COPD. Tiotropium bromide has a quaternary ammonium structure and acts as an anticholinergic bronchodilator; the active moiety is the tiotropium cation (tiotropium). A 22.5 micrograms dose of tiotropium bromide provides 18 micrograms of tiotropium. Orally inhaled tiotropium bromide antagonizes the muscarinic M(1), M(2), and M(3) receptors located in airway smooth muscle, reversing vagally mediated bronchoconstriction. Receptor binding assays and in vitro tests indicate that tiotropium bromide is kinetically selective for M(1) and M(3) receptors over the M(2) receptor, unlike ipratropium bromide, which is nonselective. Animal and in vitro studies showed that tiotropium bromide was more potent ( approximate, equals 20-fold) than ipratropium bromide in displacing [(3)H]N-methylscopolamine (NMS) from muscarinic receptors, and had a more sustained protective effect (>70% inhibition) against NMS binding. Tiotropium bromide was a more potent inhibitor of bronchial contraction than atropine ( approximate, equals 23-fold), and had a slower onset and markedly longer duration of action than atropine or an equipotent dose of ipratropium bromide. Aerosol particle penetration is improved with tiotropium, without delaying mucus clearance from the lungs. Tiotropium 4.5-36 micrograms once daily for 4 weeks increased mean trough and average FEV(1) and FVC and mean PEFR values from baseline compared with placebo, with no evidence of tachyphylaxis. Improvements in trough FEV(1) from baseline with tiotropium 4.5-36 micrograms were not dose dependent. Based on a lack of dose response, the optimal once-daily tiotropium dosage is 18 micrograms. Steady-state trough FEV(1) values are achieved within 48 hours of commencing tiotrochodilation (for >/=24 hours) and an attenuation of the nocturnal decline in FEV(1) that were unaffected by timing of the daily tiotropium dose were seen in randomized, double-blind, placebo-controlled studies in patients with stable COPD. The drug improved static and dynamic lung hyperinflation (evidenced by reduced trapped air volume and increased tidal volume and end-of-exercise inspiratory capacity), and improved exertional dyspnea (during activities of daily living and exertion) and exercise tolerance compared with placebo in randomized, double-blind studies. In patients with stable COPD, improved sleep-related oxygen desaturation that was unaffected by the timing of the daily dose was seen with tiotropium but not with placebo. Clinically significant treatment-related disorders of conduction or rhythm, or changes in heart rate were not observed with tiotropium in this patient group. Mean maximal plasma concentrations (C(max)) were observed within 5 minutes of inhalation of a single dose of tiotropium 18 micrograms in patients with COPD. Plasma drug levels declined to minimum concentrations (C(min)) within 1 hour of treatment in healthy volunteers. Mean steady-state C(max) concentrations (16 ng/L) were achieved after 2-3 weeks of once-daily inhaled tiotropium 18 micrograms in elderly patients with COPD; tiotropium does not appear to accumulate once steady-state has been achieved.The estimated absolute bioavailability of tiotropium at steady state in healthy volunteers was approximately 20-25%, and approximately 72% of the drug is bound to plasma proteins. Excretion of tiotropium is predominantly renal (through active secretion by the kidneys), although in vitro studies suggest that cytochrome P450 (CYP) oxidation (possibly involving CYP2D6 and CYP3A4 enzymes) may have a minor role. In patients with COPD, renal excretion of the unchanged drug at 24 hours (Ae(24)) was approximately 7%. The mean plasma elimination half-life after single or multiple doses in healthy volunteers and elderly patients with COPD was approximately 5-6 days. The renal clearance and urinary excretion of tiotropium decrease with increasing age; however, these changes are not considered to be clinically significant. Because of altered steady-state C(max), C(min), area under the concentration-time curve, and Ae(24) values, caution is required with tiotropium administration in patients with moderate-to-severe renal impairment. The pharmacokinetics of tiotropium in patients with severe renal or hepatic impairment have not been studied. Tiotropium does not interact with drugs such as cimetidine or ranitidine, which are also eliminated by active renal secretion. Orally inhaled tiotropium bromide has been evaluated as a bronchodilator for the management of patients with COPD in randomized, double-blind 6-month and 1-year trials, and in several shorter studies. In clinical trials, COPD was diagnosed according to the American Thoracic Society guidelines. The bronchodilator effect was expressed as the trough FEV(1) response (the mean change in FEV(1) from baseline measured 1 hour prior to and immediately before a scheduled dose), and was the primary endpoint in all but two clinical trials. The bronchodilator effect with tiotropium 18 micrograms once daily was superior to that with placebo in several well designed trials in patients with COPD. Moreover, greater improvements in mean peak and average FEV(1) responses occurred with tiotropium but not with placebo. Mean trough, peak, and average FVC responses, and weekly mean morning and evening PEFR values were also improved to a greater extent with tiotropium than with placebo. Tiotropium demonstrated a greater bronchodilator effect than ipratropium bromide (hereafter referred to as ipratropium when used at approved dosages) 40 micrograms four times daily in two 1-year trials in patients with COPD. Mean peak and average FEV(1), mean trough FVC responses, and weekly mean morning and evening PEFR values were also increased to a greater extent with tiotropium than with ipratropium. In one of the two 6-month trials that compared the efficacy of tiotropium with that of inhaled salmeterol 50 micrograms twice daily, greater improvements from baseline in mean trough, peak, and average FEV(1) and FVC responses were seen with tiotropium than with salmeterol. Increases in weekly mean evening, but not morning, PEFR values were generally greater with tiotropium than salmeterol. In the second trial, improvement in the primary endpoint (mean trough FEV(1) response from baseline) with tiotropium or salmeterol was similar, although peak and average responses were superior with tiotropium. Preliminary results from a 6-week crossover study in patients with COPD suggested that tiotropium alone or in combination with once-daily formoterol improved mean trough and average FEV(1) and trough FVC values from baseline to a greater extent than twice-daily formoterol. More patients achieved a clinically important improvement (increase of >/=1 unit) in the transitional dyspnea index focal score (a measure of dyspnea-related impairment) with tiotropium than with placebo in the 1-year trials. Tiotropium was superior to ipratropium in 1-year trials, and was at least as effective as salmeterol in 6-month trials, in achieving a clinically important improvement in focal scores. Tiotropium recipients experienced fewer COPD exacerbations than placebo or ipratropium recipients and had fewer and shorter COPD-related hospitalizations compared with placebo recipients. Unlike salmeterol, tiotropium lengthened the time to onset of the first exacerbation and decreased the number of exacerbations compared with placebo in two 6-month trials. Similar proportions of tiotropium, salmeterol, and placebo recipients required COPD-related hospitalizations. (ABSTRACT TRUNCATED)  相似文献   

19.
目的 观察噻托溴铵联合沙美特罗替卡松对慢性阻塞性肺疾病(COPD)稳定期的治疗效果.方法 采用随机、双盲的方法将62例COPD患者分为观察组和对照组,观察组给予噻托溴铵和沙美特罗替卡松治疗,对照组给予沙美特罗替卡松治疗,分别对两组患者治疗前后呼吸困难评分和肺功能检测进行比较.结果 治疗两个月后,与对照组比较观察组肺功能FEV1、FVC、FEV1/FVC%,呼吸困难评分改善差异有统计学意义(P<0.05).结论 噻托溴铵与沙美特罗替卡松联合吸入治疗COPD,疗效优于沙美特罗替卡松单药治疗.  相似文献   

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