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液相色谱-质谱-质谱方法同时测定抗疲劳保健食品中伐地那非、西地那非、他达那非
西地那非、伐地那非、他达那非是用于治疗男性功能障碍的处方药,严禁添加在保健食品中.西地那非柠檬酸盐(sildenafil citrate)俗称伟哥,早进入中国市场;他达那非即西力士(cialis),是第2代磷酸二酯酶(PED-5)选择性抑制剂,药效更快、更持久;伐地那非是继西地那非、他达那非之后第3种男性性功能障碍用药[1],它与西地那非在结构上只有微小差异.3种药物常见副反应都是头痛、面部泛红、鼻溢和消化不良等,对于心血管患者,有可能导致突然死亡[1].一些不法厂家为检测时蒙混过关,往往加入后两种更快、更持久的药物,严重威胁到服用者的健康,所以有必要建立能同时对这3种药物快速鉴定并且准确定量的方法.我们采用液相色谱-质谱-质谱(LC-MS-MS)联用技术,集LC的高分离能力及MS的强定性能力于一体,对这3种药物同时进行检测.
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西地那非的分析方法研究进展
西地那非(Sildenafil)是一种哌嗪类衍生物,于1998年首次在美国上市,它的柠檬酸盐是由美国FDA批准用于治疗性功能障碍的第一个口服药物,商品名Viagra,中文译名为万艾可,是对环磷酸鸟苷(cGMP)特异的5型磷酸二酯酶(PDE5)选择性抑制剂,在临床上已广泛应用,主要用途有:能增强阴茎勃起的生理反应、治疗男性不育与阳痿、妇女性功能障碍以及心血管疾病等.
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西地那非联合多沙唑嗪缓释剂治疗勃起功能障碍合并良性前列腺增生相关下尿路症状患者疗效的开放对照多中心临床评估
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比较西地那非与连续气道正压通气治疗阻塞性睡眠呼吸暂停患者的勃起功能障碍:疗效、安全性和患者满意度
Aim: To assess the efficacy of sildenafil and continuous positive airway pressure (CPAP) in the treatment of concurrent erectile dysfunction (ED) with obstructive sleep apnea (OSA), and to gauge the level of treatment satisfaction in patients and their partners. Methods: Forty men were treated for 12 weeks with sildenafil 100 mg (20 men) or CPAP during nighttime sleep (20 men). Treatment efficacy was assessed by the rate of successful intercourse attempts,and satisfaction with treatment was assessed by patients' and partners' answers to question 1 of the Erectile Dysfunction Inventory of Treatment Satisfaction. Results: Under sildenafil, 128 of 249 (51.4%) intercourse attempts were successful; under CPAP, 51 of 193 (26.9%) attempts were successful (Cp < 0.001). Erectile function was improved in both groups. After sildenafil and CPAP treatment, the mean International Index for Erectile Function domain scores were 14.3 and 10.8, respectively (Bp = 0.025), compared to 7.8 and 7 at baseline, respectively. CPAP and sildenafil were well tolerated. Sporadic episodes of nasal dryness under CPAP and transient headache and flushing under sildenafil were not significant. Fifty percent of patients treated with sildenafil and 25% with CPAP were satisfied with the treatment, and their partners were equally satisfied. The satisfaction scores for both patients and partners under sildenafil were superior to those under CPAP (Cp < 0.002). Conclusion: Both sildenafil 100 mg and CPAP, used separately, had positive therapeutic impact but sildenafil was superior. Patients and their partners were more satisfied with sildenafil for the treatment of ED. However, because of the high proportion of dissatisfied men and partners, new therapeutic agents or a combination of the two methods must be studied further.
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患者对ED治疗药物的偏爱度:一项荟萃分析
安全有效的ED治疗药物的不断出现使得对患者在选择治疗药物时的偏爱度的研究显得尤为重要.目前已经出现了多项关于治疗策略偏爱度的研究报告.本文旨在对涉及患者偏爱度和偏爱某种PDE5抑制剂的原因的研究进行回顾分析.通过PubMed检索过去10年间发表的包含下列关键词的文章:preference(偏爱度),sildenafil(西地那非),tadalafil(他达拉非)或者vardenafil(伐地那非).对检索结果进行细致的分析和总结(设计,缺陷和相关性).所有入选的研究均为在2000年以后发表的与患者偏爱度和ED有关的同行评审文章.涉及两种(他达拉非和西地那非)或者三种(他达拉非,西地那非和伐地那非)药物的偏爱度的研究结果显示:与伐地那非或西地那非相比,大部分的患者更偏爱他达拉非.由于ED治疗手段的改进,患者的偏爱度在ED治疗方案中显的愈发重要.经过分析后发现,有52%~65%的受试者偏爱他达拉非,而偏爱伐地那非和西地那非的比例仅有12%~20%和8%~30%.但人选的研究均有缺陷,特别表现在不同研究的剂量相差很大.在所有入选的研究中,与西地那非或伐地那非相比,患者对他达拉非的偏爱主要由于其长效性给予了患者更加自由的性生活时间.
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多种药理作用的西地那非
西地那非(sildenafil,Sil)作为治疗男性勃起功能障碍(简称勃起障碍erectile dysfunction,ED)的药物问世以来,已有11年的历史,从基础到临床,在全球范围内进行了广泛研究,通过Medline上网检索,截至2009年3月已发表论文3757篇,不仅肯定了Sil对ED的疗效,还发现其具有多种非ED方面的生物活性和药理作用[1,2,16].本文就有关的新研究成果,加以综合分析.
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西地那非在儿童肺动脉高压的应用现状
西地那非(sildenafil)用于治疗男性勃起功能障碍的一线药,具有里程碑意义.近些年相关研究已证实西地那非通过选择性抑制5型磷酸二酯酶(PDE5),该酶是肺动脉血管中主要的磷酸二酯酶,抑制该酶可使环磷酸鸟苷(cGMP)维持在较高水平,后者促进内源性一氧化氮(NO)的血管扩张作用,具有治疗肺动脉高压(PAH)的功效.
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Sildenafil在慢性高原病预防中的实验研究
目的 探讨Sildenafil对慢性高原病的预防作用及与内皮素系统的关系.方法 随机分Wistar大鼠为3个组,雌雄各半,分常氧对照组,低氧对照组和Sildenafil组,将低氧对照组和Sildenafil组放入模拟海拔为5500m的低氧、低压舱中.常氧对照组和低氧对照组以灌胃方式灌注0.9%生理盐水,Sildenafil组用12.5mg/mL浓度的sildenafil水剂灌胃,每天2次.饲养15 d后,测量大鼠平均PAP、RV/(LV+S)比值.结果 药物组大鼠Hb、Hct与低氧对照组相比无差异,而PAP、PV/(LV+s)分别为(33.60±9.44)mmHg,(0.43%±0.05%)均显著低于低氧对照组:(46.30±8.25)rnmHg,(0.55%±0.05%)(P<0.01).结论 Sildenafil能有预防低氧性肺动脉压的升高,可缓解低氧对心肌细胞和血管平滑肌细胞的损伤,但不能抑制红细胞的过度增生.
关键词: sildenafil 预防 慢性高原病 -
西地那非治疗新牛儿持续性肺动脉高压研究进展
新生儿持续性肺动脉高压(persistent pulmonary hypertension of the newborn,PPHN)又称持续胎儿循环(persistent fetalcirculation,PFC),是指多种病因引起新生儿生后肺血管阻力持续性增高,肺动脉压超过体循环动脉压,使由胎儿型循环过渡至正常"成人"型循环发生障碍,引起的卵圆孔及(或)动脉导管水平血液的右向左分流,从而导致严重的低氧血症和青紫,甚至死亡.PPHN在活产新生儿中发病率为0.43%~6.8%,病死率10%~20%[1].因其病因复杂,发病机制尚不完全清楚,治疗难度较大.近年来PPHN的治疗手段有很大进展,但基本的治疗是高频通气、维持体循环、降低肺动脉压等,包括人工呼吸机高频通气、碱性药物应用、血管扩张剂应用、表面活性物质替代、一氧化氮(NO)吸入及体外膜氧合.不同方法各有利弊,佳治疗方法尚有争论.
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中西药在预防慢性高原病中的比较
目的:通过对藏药15味沉香散与西药Sildenafil的药效学比较,从中、西药物中寻找出更好的防治CMS的药物.方法对低氧对照组,15味沉香组,Sildenafd组Hb,Hct,平均PAP、RV/(LV+S),血清ET-1浓度进行比较.结果:15味沉香组大鼠Hb,Hct,PAP,RV/(LV+S)均低于低氧对照组(P<0.01),血浆内皮素-1浓度也明显比低氧对照组低(P<0.05),西药除PAP,RV/(LV+S)较低氧对照组低之外,Hb,Hct和ET-1水平与低氧对照组相比,均无显著性差异.结论:单纯从预防低氧性肺动脉高压形成方面,西药较藏药15味沉香好,但从整体预防CMS方面,藏药15味沉香散优于西药.
关键词: 沉香散 sildenafil 预防 CMs -
Background: Lung hypoplasia, pulmonary persistent hypertension of the newborn and its morphological changes are the main features in congenital diaphragmatic hernia (CDH). This study was undertaken to investigate if antenatal use of sildenafi l and/or bosentan attenuates vascular remodeling, promotes branching, and improves alveolarization in experimental nitrofeninduced CDH.
Methods: Nitrofen (100 mg) was gavage-fed to pregnant rats at post conception day (PCD) 9 to induce CDH. The rats were randomized to 5 groups: 1) control; 2) nitrofen; 3) nitrofen+sildenafil 100 mg/kg per day at PCD 16-20; 4) nitrofen+bosentan 30 mg/kg per day, at PCD 16-20, and 5) nitrofen+bosentan+sildenafil, same doses and administration days. After cesarean delivery, the offsprings were sacrifi ced. The diaphragmatic defect and pulmonary hypoplasia were identifi ed, and the lungs were dissected. Arterial wall thickness, bronchiolar density and alveolarization were assessed.
Results: The offsprings with CDH were characterized by severe pulmonary hypoplasia (lung weight-to-body weight ratio: 0.0263 [95% confidence interval (CI) 0.0242-0.0278)] in the nitrofen group versus 0.0385 (95% CI 0.0355-0.0424) in the control group (P=0.0001). Pulmonary arterial wall thickness was decreased to 3.0 (95% CI 2.8-3.7) μm in the nitrofen+sildenafil group versus 5.0 (95% CI 4.1-4.9) μm in the nitrofen group (P=0.02). Terminal bronchioles increased to 13.7 (95% CI 10.7-15.2) μm in the nitrofen+bosentan group in contrast to 8.7 (95% CI 7.2-9.4) μm in the nitrofen group (P=0.002). More significant differences (P=0.0001) were seen in terminal bronchioles in the nitrofen+sildenafil+bosentan group than in the nitrofen group [14.0 (95% CI 12.5-15.4) μm versus 8.5 (95% CI 7.1-9.3) μm]. Pulmonary arterial wall thickness was also decreased in the former group.
Conclusions: In this rat model, antenatal treatment with sildenafi l attenuates vascular remodeling. Bosentan promotes the development of terminal bronchioles in nitrofen-induced CDH.