阿瑞匹坦预防顺铂化疗所致恶心和呕吐的疗效分析

目的:为明确阿瑞匹坦在预防含顺铂的化疗方案所致的化疗相关性恶心呕吐的临床疗效。方法:选取我院2014年1月1日–2014年10月1日接受含顺铂(75 mg·m-2)化疗方案的患者100例,接受阿瑞匹坦、5-HT3受体拮抗剂和地塞米松的患者为阿瑞匹坦组,同期使用5-HT3受体拮抗剂和地塞米松的患者为对照组,观察两组患者急性期(第1天)、延迟期(第2~5天)完全有效率(CR)及化疗期间(5 d)无严重恶心呕吐的发生率。结果:阿瑞匹坦组与对照组治疗急性呕吐的CR分别为70%和54%(P=0.149);而治疗迟发性呕吐两组有效率分别为78%和46%(P=0.002),阿瑞匹坦组显著优于对照组。化疗期间阿瑞匹坦组与对照组患者无严重恶心呕吐的发生率分别为86%、62%(P=0.012),阿瑞匹坦组优于对照组。两组止吐药物相关不良反应无明显差异。结论:阿瑞匹坦三联方案在预防顺铂诱发恶心和呕吐的疗效及耐受性方面表现良好,为提高患者生活质量提供了较好的选择方式。     

阿瑞匹坦联合托烷司琼预防顺铂化疗引起呕吐的临床观察

目的:观察阿瑞匹坦联合托烷司琼方案预防顺铂化疗引起呕吐的疗效及不良反应。方法:采用随机、自身交叉对照的方法,将60例接受两周期含顺铂联合化疗的患者,随机分为AB、BA组。AB组第1周期应用阿瑞匹坦联合托烷司琼,第2周期应用托烷司琼;BA组第1周期应用托烷司琼,第2周期应用阿瑞匹坦联合托烷司琼。结果:可评价疗效的59例患者中,阿瑞匹坦联合托烷司琼方案和托烷司琼方案对急性呕吐的完全缓解率分别为74.6%和57.6%,有效控制率分别为91.5%和81.4%(Z=-2.017,P=0.044);对延迟性呕吐的完全缓解率分别为69.5%和42.4%,有效控制率分别为86.4%和71.2%(Z=-3.112,P=0.002)。两种方案的主要不良反应为呃逆、便秘、头痛、头晕、口干等,不良反应发生率比较差异无统计学意义(P>0.05)。结论:阿瑞匹坦联合托烷司琼方案对顺铂化疗引起急性呕吐与延迟性呕吐均有很好的疗效,不良反应可以耐受。     

阿瑞匹坦在含顺铂方案化疗中的止吐疗效观察

目的:比较含顺铂化疗方案中常规止吐方案加用阿瑞匹坦与单用常规止吐方案的疗效差异。方法:106例肺癌患者均采用含顺铂的双药方案联合化疗,其中53例(对照组)予常规止吐治疗,另外53例(观察组)在常规止吐治疗的基础上加服NK-1受体拮抗剂阿瑞匹坦,观察两组的止吐效果。结果:对照组止吐有效率为77.36%,观察组止吐有效率为96.23%,两组比较差异有统计学意义(χ2=8.23,P<0.05)。结论:NK-1受体拮抗剂阿瑞匹坦联合5-HT3受体拮抗剂如托烷司琼及皮质类固醇类药物地塞米松可显著改善顺铂化疗所致的恶心、呕吐症状,明显改善化疗患者的生活质量,提高患者的依从性,从而保证化疗的顺利进行。     

阿瑞匹坦在预防肺癌含铂化疗方案所致化疗相关性恶心呕吐的疗效研究

目的分析研讨阿瑞匹坦在预防肺癌含铂化疗方案所致化疗相关性恶心呕吐的疗效。方法随机抽取我院2015年9月~2017年10月期间收治的肺癌含铂化疗方案治疗而引发恶心呕吐患者80例,根据其所使用止吐药物进行分组,对照组40例接受地塞米松+托烷司琼治疗,研究组40例接受阿瑞匹坦+地塞米松+托烷司琼治疗,观察比较两组患者治疗疗效、不良反应,以及患者生活质量等。结果研究组治疗总有效率为90%高于对照组的72.50%,P0.05。研究组不良反应总发生率15%虽略低于对照组12.50%,P0.05。对比两组患者FLIE评分,治疗前P0.05,治疗后,研究组评分均高于对照组,P0.05。研究组首次呕吐时间晚于对照组,P0.05,表明阿瑞匹坦药物在预防化疗相关性恶心呕吐方面有应用价值。结论临床治疗肺癌含铂化疗而造成的恶心呕吐症状可在地塞米松联合托烷司琼治疗基础上,给予阿瑞匹坦药物,止吐效果更好,且可确保给药安全性,进而提升患者生活质量。     

阿瑞匹坦用于乳腺癌患者化疗的止吐效果观察

目的观察分析阿瑞匹坦用于乳腺癌患者化疗的止吐效果及安全性。方法选取我院经病理确诊的68例初诊化疗的乳腺癌患者,随机分为试验组及对照组。试验组34例,给予阿瑞匹坦联合托烷司琼、地塞米松;对照组给予安慰剂、格拉司琼、地塞米松,用药剂量及用法与试验组相同。观察两种治疗方案对化疗所致恶心、呕吐的疗效。结果 68例患者均纳入分析,阿瑞匹坦组患者完全缓解率明显优于对照组(61.8%vs.31.3%,P=0.029);阿瑞匹坦组与对照组的急性呕吐完全缓解率分别为85.3%和67.6%(P=0.086),呈降低趋势,但差异无统计学意义;阿瑞匹坦组迟发性呕吐的完全缓解率明显高于对照组(70.6%vs.44.1%,P=0.027),迟发性呕吐的发生率明显低于对照组(5.9%vs.29.4%,P=0.011)。本研究中未观察到阿瑞匹坦相关中重度不良反应,药物安全性良好。结论阿瑞匹坦对于乳腺癌化疗患者止吐效果良好,在迟发性呕吐的缓解方面尤其突出,且不良反应较轻,患者可耐受。     

阿瑞匹坦对乳腺癌AC方案化疗后中重度呕吐患者的二级预防

目的 观察分析联合应用阿瑞匹坦、盐酸托烷司琼、地塞米松二级预防乳腺癌术后蒽环类药物联合环磷酰胺（AC方案）化疗所致恶心呕吐的疗效及不良反应。方法 选取2015年1月至2016年5月在山东省德州市市立医院肿瘤科住院治疗的乳腺癌术后AC方案首次化疗相关性恶心呕吐（chemotherapy-induced nausea and vomiting,CINV）为中重度的患者72例,随机分为观察组35例,对照组37例。继续化疗过程中,观察组使用阿瑞匹坦+盐酸托烷司琼+地塞米松三联止吐药物预防CINV,对照组使用盐酸托烷司琼+地塞米松预防CINV。观察两组患者化疗后急性期（0~24 h）及延迟期（24~120 h）预防恶心呕吐的效果及不良反应发生情况。结果 两组患者急性期呕吐的完全控制率比较,差异无统计学意义（P>0.05）,观察组急性期呕吐的有效控制率较对照组明显升高,差异有统计学意义（P<0.05）;观察组延迟期呕吐的完全控制率及有效控制率均高于对照组,差异均有统计学意义（P<0.05）。两组患者不良反应主要为便秘、疲乏、面色潮红、焦虑及头晕等,均症状轻微。结论 对乳腺癌AC方案化疗后中重度呕吐患者,化疗过程中给予阿瑞匹坦三联止吐治疗效果好,经济效益较高,且不良反应轻微,患者可耐受。     

阿瑞吡坦在中国肺癌患者中预防高剂量顺铂引起恶心和呕吐的疗效(英文)

目的探讨在中国肺癌患者中应用阿瑞匹坦减轻高剂量顺铂为主的化疗方案引起的恶心和呕吐的效果。方法纳入预接受高剂量顺铂为主化疗方案的肺癌患者291例,随机分为两组。阿瑞吡坦组139例,化疗第1日予阿瑞吡坦125 mg;第2,3日,予阿瑞吡坦80 mg,口服。标准治疗组152例,予安慰剂口服。两组均接受静脉注射格拉司琼和口服地塞米松。评估两组总完全反应率及在化疗第1日(急性期)和第2~5日(延迟期)的完全反应率,比较两组接受高度或中度致吐化疗方案患者的完全反应率。结果阿瑞吡坦组总完全反应率为69.1%(96/139),高于标准治疗组[57.2%(87/152),P=0.035],延迟期亦高于标准治疗组[72.7%(101/139)vs.59.9%(91/152),P=0.019],急性期组间无显著差异[79.9%(111/139)vs.80.9%(123/152),P=0.914]。阿瑞吡坦组接受高度或中度致吐化疗方案患者中完全反应率为60%(3/5),高于标准治疗组[33%(1/3),P=0.034]。结论阿瑞吡坦治疗可以预防中国肺癌患者接受高剂量顺铂化疗引起的恶心和呕吐,特别是在延迟期效果优于标准治疗。     

阿瑞匹坦联合托烷司琼防治铂类化疗药所致恶心呕吐的有效性及安全性分析

目的 探讨阿瑞匹坦联合托烷司琼对铂类化疗药所致恶心、呕吐、食欲下降、体质量下降等的防治作用,并评估其安全性。方法 选取100名给予铂类化疗的鼻咽癌患者,将其随机分为实验组和对照组,各50例。2组均常规使用托烷司琼,其中实验组在化疗前1 h及化疗后第2,3天口服阿瑞匹坦。观察2组患者恶心、呕吐、食欲下降、乏力、体质量下降、腹泻、便秘、皮疹、过敏、手足综合征及神经毒性感觉等方面的异同。结果 在呕吐方面,对照组的防治有效率为44%(22例),实验组的防治有效率为86%(43例)。对照组的体质量下降程度明显高于实验组(P<0.05)。2组患者在恶心、食欲下降、乏力、腹泻、便秘、皮疹、过敏、手足综合征及神经毒性感觉等方面差异无统计学意义。结论 阿瑞匹坦联合托烷司琼可安全、有效的防治铂类化疗药所致的呕吐,减轻鼻咽癌患者化疗期间的体质量下降,但对恶心及食欲下降等的防治作用不明显。     

昂丹司琼联合阿瑞匹坦胶囊及地塞米松治疗化疗致呕吐的效果分析

目的 探讨昂丹司琼联合阿瑞匹坦胶囊及地塞米松治疗化疗致呕吐的效果。方法 选择医院2020年3月～2021年3月诊治的乳腺癌化疗呕吐患者100例,采用简单随机化法将所有患者分成对照组(n=50)和联合组(n=50)。对照组患者使用昂丹司琼治疗,联合组患者使用昂丹司琼联合阿瑞匹坦胶囊及地塞米松治疗。比较两组患者止吐疗效、恶心呕吐分级及不良反应。结果 联合组患者止吐总有效率76%高于对照组48%(χ²=9.556,P <0.05)。两组患者经秩和检验发现,差异有统计学意义(Z=3.619,P <0.05)。两组患者不良反应发生率差异无统计学意义(χ²=0.391,P> 0.05)。结论 昂丹司琼联合阿瑞匹坦胶囊及地塞米松治疗化疗致呕吐患者可在不增加治疗不良反应基础上改善恶心呕吐程度,提升临床疗效。     

阿瑞匹坦和托烷司琼及柠檬皮片联合使用防治卵巢癌化疗患者恶心呕吐的效果分析

目的：探讨阿瑞匹坦联合柠檬皮片和托烷司琼防治卵巢癌化疗患者恶心呕吐的效果。方法：选择2021年6月—2023年6月收治的卵巢癌化疗患者110例,随机分为对照组和观察组,每组55例。对照组给予托烷司琼注射液联合柠檬皮片闻味治疗,观察组在对照组基础上口服阿瑞匹坦,比较两组的化疗相关性恶心、呕吐的预防效果及用药不良反应。结果：治疗后,观察组患者的恶心预防有效率、急性呕吐预防有效率和延迟性呕吐预防有效率均高于对照组,差异有统计学意义(P<0.05);两组用药不良反应发生率比较,差异无统计学意义(P>0.05)。结论：阿瑞匹坦、托烷司琼及柠檬皮片联合使用可提高卵巢癌患者化疗期间恶心呕吐预防效果,改善患者化疗耐受性,且不会加重止吐药的不良反应。     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Synthesis and anti-nociceptive and anti-inflammatory effects of gaultherin and its analogs

The synthesis of gaultherin (1) and its analogs was carried out to provide 11 glycosides under phase-transfer catalytic conditions. The activities of all synthesized compounds were evaluated by nitric oxide production inhibitory assay in vitro. Methyl 2-O-(4-O-β-d-galactopyranosyl)-β-d-glucopyranosylbenzoate (5f) showed significantly anti-nociceptive and anti-inflammatory effects by the evaluation in vivo. Structure–activity relationships within these compounds were discussed.     

Modelling and simulation of variability and uncertainty in toxicokinetics and pharmacokinetics

Two important methodological issues within the framework of the variability and uncertainty analysis of toxicokinetic and pharmacokinetic systems are discussed: (i) modelling and simulation of the existing physiologic variability in a population; and (ii) modelling and simulation of variability and uncertainty when there is insufficient or not well defined (e.g. small sample, semiquantitative, qualitative and vague) information available. Physiologically based pharmacokinetic models are especially suited for separating and characterising the physiologic variability from the overall variability and uncertainty in the system. Monte Carlo sampling should draw from multivariate distributions, which reflect all levels of existing dependencies in the intact organism. The population characteristics should be taken into account. A fuzzy simulation approach is proposed to model variability and uncertainty when there is semiquantitative, qualitative and vague information about the model parameters and their statistical distributions cannot be defined reliably.     

成骨细胞的功能与损伤和骨质疏松的防治

骨质疏松是一种全身性骨骼疾病,导致骨折风险增加。成人的骨量通过破骨细胞的骨吸收和成骨细胞的骨形成作用来维持动态平衡,治疗骨质疏松症的理想策略是抑制破骨细胞的骨吸收和/或增强成骨细胞的骨形成功能。目前针对保护成骨细胞及增强其功能的骨质疏松疗法相对较少。因此,本文针对成骨细胞相关功能蛋白、各种细胞损伤机制（内质网应激、氧化应激、机械过载、微小RNA和长链非编码RNA的影响等）及骨质疏松的治疗与预防作一综述,以期为针对增强成骨细胞功能的骨质疏松治疗策略提供新思路。     

益生菌与肿瘤防治

益生菌广泛存在于自然界中,通过维持宿主体内菌群平衡、影响肠屏障功能和调节免疫应答等作用,提高宿主健康水平,被公认为"肠道健康卫士".一些益生菌可以增强机体的免疫功能,抑制致癌物质,影响肿瘤细胞的基因表达,对肿瘤具有拮抗作用.大量研究表明,益生菌在未来的肿瘤防治中有很好的应用和发展前景.     

Self-stimulation and amphetamine: Tolerance to d and l isomers and cross tolerance to cocaine and methylphenidate

The effects of the d and l isomers of amphetamine on self-stimulation responding were tested following acute and chronic administration. Tolerance and post-drug depression of responding occurred in tests with both isomers, indicating no role for p-hydroxynorephedrine (PHN) which is one of the metabolites of d-amphetamine. In the second experiment, d-amphetamine, methylphenidate and cocaine all produced quantitatively and qualitatively similar effects on self-stimulation responding following acute administration. Following chronic administration of d-amphetamine, animals showed tolerance to all three drugs, indicating cross-tolerance among them. These data are consistent with an hypothesis that tolerance and post-drug depression following chronic amphetamine treatment are the result of decreases in postsynaptic receptor sensitivity, which would lead to a decreased effectiveness of all three drugs, regardless of their pre-synaptic mechanisms.     

Acamprosate and naltrexone treatment effects on ethanol and sucrose seeking and intake in ethanol-dependent and nondependent rats

Rationale  Two pharmacotherapies are approved for treating alcohol craving (acamprosate and naltrexone), but both have shown mixed findings in animals and humans. Objectives  The present experiments utilized a “reinforcer blocking” approach (i.e., rats were able to consume ethanol during treatment) to better understand the efficacy of these treatments for ethanol seeking and drinking using ethanol-dependent and nondependent rats. Materials and methods  In “nondependent” experiments, drugs (acamprosate 50, 100, and 200 mg/kg; naltrexone 0.1, 0.3, and 1.0 mg/kg) were administered over 3-week periods prior to operant sessions with a low response requirement to gain access to reinforcers for 20 min. For “dependent” experiments, rats were made dependent in vapor/inhalation chambers. Results  Acamprosate and naltrexone had similar effects on intake in nondependent and dependent rats; neither drug was selective for ethanol over sucrose drinking. In nondependent animals, naltrexone was more efficacious at more doses than acamprosate, and acamprosate’s effects were limited to a dose that also had adverse effects on body weight. Both pharmacotherapies showed more selectivity when examining reinforcer seeking. In nondependent rats, acamprosate and naltrexone had response-attenuating effects in ethanol, but not sucrose, groups. In dependent animals, acamprosate had selective effects limited to a decrease in sucrose seeking. Naltrexone, however, selectively decreased ethanol-seeking in nondependent rats. Conclusions  The naltrexone-induced decreases in seeking suggested a change in incentive motivation which was selective for ethanol in nondependent rats. The “nondependent” paradigm may model early stages of “problem drinking” in humans, and the findings suggest that naltrexone could be a good intervention for this level of alcohol abuse and relapse prevention.     

Antiinfective and encrustation-inhibiting materials--myth and facts

Catheters, urethral and ureteral stents and other urological implants are frequently affected by encrustration and infection due to their permanent contact with urine. Indwelling urinary catheters provide a haven for microorganisms and thus require extensive monitoring. Several surface modification techniques have been proposed to improve the performance of devices including the immobilization of biomolecules, the incorporation of hydrophilic grafts to reduce protein adsorption, the creation of hydrophobic surfaces, the creation of microdomains to regulate cellular and protein adhesion, new polymers and antimicrobial coatings. Physico-chemical explanation to elucidate the mechanism of such encrustation or infection inhibiting materials is still not available. Our series of experiments showed a marked decrease of silver-activity in biological fluids which corresponds with the controversial clinical results obtained with silver coated urinary catheters. Rifampicin/minocycline coated catheters had very low activity against Gram-negative rods, enterococci and Candida spp., the main causing organisms of urinary catheter infection. Surface engineered materials and antimicrobial drug delivery systems will be the next generation of sophisticated urinary catheters and stents, if both efficacy as well as efficiency has been proved clinically.     

Alprazolam and lorazepam single and multiple-dose effects on psychomotor skills and sleep

Summary The effects of alprazolam 0.5 mg and lorazepam 2 mg on cognitive and psychomotor skills were assessed in twelve normal volunteer subjects in a randomised, double-blind, crossover design. Single and multiple dose effects were monitored using a battery of tests comprising critical flicker fusion threshold (CFFT), choice reaction time (CRT), simulated car tracking, and subjective ratings of perceived sedation (LARS) and of sleep behaviour (LSEQ). Compared with placebo baseline scores, treatment with lorazepam 2 mg (both single and multiple doses) resulted in a widespread impairment of CRT, tracking accuracy, and CFFT. Single doses of alprazolam 0.5 mg reduced CFFT with respect to the placebo baseline. Single and multiple dose treatment with both drugs resulted in subjective reports of sedation, a reduction of sleep onset latency, and improved sleep quality. Only lorazepam 2 mg significantly disrupted the integrity of behaviour on waking from sleep. These results suggest important pharmacodynamic differences between the two drugs in the doses used.