右美托咪啶复合瑞芬太尼在超声胃镜中的应用

目的:探讨使用右美托咪啶复合瑞芬太尼进行静脉麻醉在超声胃镜诊治中的可行性、有效性及安全性。方法:选取2015年10月至2017年10月南京市鼓楼医院接受超声胃镜检查的患者,随机将其分为研究组与对照组。对照组患者仅接受瑞芬太尼的辅助治疗,研究组患者在瑞芬太尼基础上接受右美托咪啶辅助治疗。对比2组患者的检查满意度、手术时间、术中知晓率、苏醒时间、不良反应发生情况。结果:研究组患者的检查满意度明显高于对照组(P<0.05),不良反应发生率明显低于对照组(P<0.05);研究组患者的呼吸抑制发生率以及麻醉药物消退时间明显小于对照组(P<0.05)。结论:右美托咪啶复合瑞芬太尼应用于胃镜超声辅助检查时能明显提高患者的检查满意度,安全有效,值得推荐使用。     

瑞芬太尼结合右美托咪啶腰硬麻醉应用于老年子宫肌瘤切除术中的效果及对患者应激反应和生命指征的影响

目的:探讨瑞芬太尼结合右美托咪啶腰硬麻醉应用于老年子宫肌瘤切除术中的效果及对患者应激反应和生命指征的影响。方法:选取我院2017年9月—2019年9月收治的老年子宫肌瘤切除术患者120例,采用随机数表法分成观察组和对照组,每组60例。对照组采用瑞芬太尼进行麻醉,观察组采用瑞芬太尼结合右美托咪啶腰硬麻醉,对两组围麻醉期的应激反应、平均动脉压(MAP)及心率(HR),术后1 h、12 h的视觉模拟评分法(VAS)评分及术后不良反应进行观察比较。结果:观察组HR和MAP在T1、T2时点明显低于对照组,观察组Cor、NE、E在T1、T2时点明显低于对照组,观察组VAS评分在术后1 h及12 h均明显低于对照组,差异具有统计学意义(P<0.05);观察组术后不良反应发生率为18.33%(11/60),对照组为23.33%(14/60),差异无统计学意义(P>0.05)。结论:将瑞芬太尼结合右美托咪啶腰硬麻醉应用于老年子宫肌瘤切除术,能够明显抑制应激反应,生命体征更加平稳,有效缓解疼痛,且不会增加不良反应。     

瑞芬太尼复合右美托咪定麻醉对冠状动脉搭桥患者术中血流动力学的影响

目的:探讨瑞芬太尼复合右美托咪定麻醉对冠状动脉搭桥患者的影响.方法:选取2015-09～ 2019-10我院冠状动脉搭桥患者60例,单独泵注瑞芬太尼麻醉的29例为对照组,泵注瑞芬太尼复合右美托咪定麻醉的31例为研究组,比较两组麻醉前1 h(T0)、麻醉诱导后3min(T1)、气管插管后3min(T2)、手术开始20min(T3)、拔管时(T4)平均动脉压(MAP)、心率(HR)变化及麻醉起效时间、麻醉维持时间、不良反应发生情况.结果:T1、T2 T3、T4时研究组MAP高于对照组,HR低于对照组(P＜0.05),研究组术中血流动力学波动小于对照组;研究组麻醉起效时间短于对照组,麻醉维持时间长于对照组(P＜0.05);研究组不良反应发生率6.45％低于对照组27.59％ (P ＜0.05).结论:瑞芬太尼复合右美托咪定麻醉应用于冠状动脉搭桥患者,能减小患者术中血流动力学波动,缩短麻醉起效时间,延长麻醉维持时间,降低不良反应发生率.     

舒芬太尼复合右美托咪啶在妇科腔镜手术术后镇痛的效果观察

目的:研究舒芬太尼复合右美托咪啶在妇科腔镜手术术后镇痛的效果.方法:选取2015年8月~2016年9月我院接收的88例行妇科腔镜手术医治的患者临床资料进行研究,按照不同的麻醉药物分为两组,对照组(44例)采取舒芬太尼镇痛,研究组(44例)采取右美托咪啶联合舒芬太尼镇痛,并对两组术后疼痛评分、舒适度评分、不良反应状况进行比较.结果:研究组术后疼痛评分、舒适度评分、不良反应状况较对照组优(P<0.05).结论:妇科腔镜手术后给予右美托咪啶联合舒芬太尼镇痛可提高舒适度,缓解术后疼痛.     

右美托咪啶在老年患者膝关节镜术后镇痛中的效果评价

目的 评价右美托咪啶在老年患者膝关节镜术后镇痛中的效果.方法 选取我院2014年2月~2016年7月我院收治的64例行膝关节手术治疗的老年患者作为观察对象,按照抽签法分为对照组和治疗组,每组32例患者,对照组采用舒芬太尼麻醉,治疗组在对照组基础上联合采用右美托咪定,比较两组术后镇痛效果.结果 两组术后48h内镇痛VAS评分比较,治疗组术后24h内的VAS评分情况显著优于对照组,差异具有统计学意义(P<0.05),但术后48h两组比较,差异不明显(WTBXP>0.05);治疗组48h按压次数及48h舒芬太尼总量均少于对照组,组间差异明显(P<0.05);两组术后各时间点Ramsay镇静评分比较,差异无统计学意义(P>0.05).结论 在老年患者膝关节镜术后应用舒芬太尼麻联合右美托咪定联合麻醉的方法,缩短疼痛时间,镇痛效果确切,值得临床使用和进一步推广.     

预防瑞芬太尼复合麻醉患者术后痛觉过敏采用地佐辛联合右美托咪定的临床研究

目的:探讨右美托咪定与地佐辛联用对瑞芬太尼复合麻醉患者术后痛觉过敏的预防效果.方法:选取80例行瑞芬太尼行复合麻醉的患者,均为我院2014年9月~2016年3月收治,随机分组,在结束手术前30min,就静注地佐辛(对照组,n=40)与静注右美托咪啶联合地佐辛(观察组,n=40)麻醉指标进行比较.结果:观察组术后不同时间点疼痛评分均低于对照组(P<0.05),均无严重不良反应.结论:针对瑞芬太尼行复合麻醉的患者,应用右美托咪啶联合地佐辛,可对术后痛觉过敏预防,有较高安全性.     

依托咪酯联合丙泊酚、瑞芬太尼麻醉对黏膜下子宫肌瘤患者术后定向力恢复时间及VAS评分的影响

目的：探究依托咪酯联合丙泊酚、瑞芬太尼麻醉对Ⅰ型以下黏膜下子宫肌瘤患者术后定向力恢复时间及VAS评分的影响。方法：选取本院Ⅰ型以下黏膜下子宫肌瘤患者52例，拟行宫腔镜下子宫肌瘤摘除术，其中研究组26例、对照组26例，分组原则：麻醉方案不同。对照组麻醉药物选择丙泊酚、瑞芬太尼，研究组选择依托咪酯联合丙泊酚、瑞芬太尼，统计两组麻醉诱导时间、苏醒时间、定向力恢复时间、疼痛程度(VAS评分)、不同时段心率(HR)、血氧饱和度(SpO₂)、平均动脉压(MAP)。结果：研究组麻醉诱导时间、苏醒时间、定向力恢复时间短于对照组(P<0.05);研究组VAS评分与对照组相比无显著性差异(P>0.05);研究组麻醉诱导后1min、术毕即刻心率高于对照组(P<0.05);麻醉诱导后1 min研究组MAP、SpO₂高于对照组(P<0.05),研究组HR、MAP、SpO₂波动幅度较小。结论：依托咪酯联合丙泊酚、瑞芬太尼麻醉应用于Ⅰ型以下黏膜下子宫肌瘤手术患者，可提高患者术后苏醒质量，缓解术后疼痛，血流动力学稳定。     

右美托咪定在单孔胸腔镜肺癌根治术中的应用效果分析

目的 分析右美托咪定在单孔胸腔镜肺癌根治术中的应用效果。方法 选取100例行单孔胸腔镜肺癌根治术的患者,根据术中麻醉用药情况分为对照组(未使用右美托咪定)和实验组(使用右美托咪定),每组50例。对照组术中使用瑞芬太尼复合七氟烷麻醉,实验组术中使用右美托咪定、瑞芬太尼复合七氟烷麻醉。比较两组患者术前到术后共11个时间点血压、心率的波动情况,苏醒情况,术前、术后空腹血糖变化情况;观察两组患者并发症发生情况及追加药物情况。结果 (1)与本组术前(T1)比较,两组患者麻醉开始前(T2)收缩压显著升高(P<0.05)。(2)两组患者术后第1天(T11)舒张压低于本组T1时(P<0.05)。(3)麻醉开始后60 min (T4),实验组患者心率低于对照组(P<0.05)。(4)两组患者拔管时间、拔管后苏醒时间、总苏醒时间比较均无显著差异(P>0.05)。两组患者在麻醉后监测治疗室(PACU)的Steward评分均达到6分,安全送返普通病房。(5)两组术前、术后空腹血糖及血糖变化差值组间比较无显著差异(P>0.05);两组术后空腹血糖均高于本组术前(P<0.05)...     

右美托咪啶复合盐酸瑞芬太尼对高血压脑出血患者术后镇静镇痛中的应用研究

目的研究右美托咪啶复合盐酸瑞芬太尼对高血压脑出血患者术后镇静镇痛中的应用。方法本文研究对象为高血压脑出血患者90例,采取电脑随机分组方式分为两组,收取时间在2016年12月～2018年12月,观察组采用右美托咪啶复合盐酸瑞芬太尼,对照组采用咪达唑仑联合盐酸瑞芬太尼,将两组各项指标进行对比。结果观察组高血压脑出血患者术后6h镇静评分(4.21±0.81)分、术后24h(3.61±0.51)分、术后48h(3.10±0.91)分高于对照组(P 0.05);观察组高血压脑出血患者的HR、RR、MAP指标低于对照组患者(P 0.05);观察组高血压脑出血死亡率低于对照组(P 0.05);观察组高血压脑出血患者再出血手术率低于对照组(P 0.05)。结论通过对高血压脑出血患者应用右美托咪啶复合盐酸瑞芬太尼后,具有显著的镇静镇痛效果。     

瑞芬太尼联合右美托咪定对全麻下髋关节置换术患者脑氧代谢和认知功能的影响

目的 探讨髋关节置换术采用瑞芬太尼联合右美托咪定全麻对认知功能和脑氧代谢的影响。方法 选取2018年1月至2021年1月驻马店市第一人民医院收治行全麻髋关节置换术62例患者,根据麻醉方式不同,将瑞芬太尼麻醉的31例作为对照组,将瑞芬太尼联合右美托咪定麻醉的31例作为观察组。比较两组脑氧代谢、血流动力与认知功能变化。结果 两组T₁、T₂、T₃与术后4 h(T₄)的颈内静脉血氧含量(CjvO₂)与动脉血氧含量(CaO₂)均呈现逐渐降低趋势,且观察组低于对照组,差异有统计学意义(P<0.05);两组术后1 d、术后3 d与术后7 d的血清S100β蛋白水平与MMSE评分均低于术前,观察组术后1 d、术后3 d的血清S100β蛋白水平与MMSE评分高于对照组(P<0.05);两组不良反应发生率差异无统计学意义(P>0.05)。结论 瑞芬太尼联合右美托咪定可促使全麻下髋关节置换术患者血流动力学保持稳定,维持脑氧代谢,并减轻对认知功能产生的影响。     

Interaction of estrone and estradiol with DNA and protein of liver and kidney in rat and hamster in vivo and in vitro

[6,7-³H] Estrone (E) and [6,7-³H]estradiol-17 (E₂) have been synthesized by reduction of 6-dehydroestrone and 6-dehydroestradiol with tritium gas. Tritiated E and E₂ were administered by oral gavage to female rats and to male and female hamsters on a dose level of about 300 g/kg (54 mCi/kg). After 8 h, the liver was excised from the rats; liver and kidneys were taken from the hamsters. DNA was purified either directly from an organ homogenate or via chromatin. The radioactivity in the DNA was expressed in the units of the Covalent Binding Index, CBI = (mol chemical bound per mol DNA-P)/(mmol chemical administered per kg b.w.). Rat liver DNA isolated via chromatin exhibited the very low values of 0.08 and 0.09 for E and E₂, respectively. The respective figures in hamster liver were 0.08 and 0.11 in females and 0.21 and 0.18 in the males. DNA isolated from the kidney revealed a detectable radioactivity only in the female, with values of 0.03 and 0.05 for E and E₂, respectively. The values for male hamster kidney were < 0.01 for both hormones. The minute radioactivity detectable in the DNA samples does not represent covalent binding to DNA, however, as indicated by two sets of control experiments. (A) Analysis by HPLC of the nucleosides prepared by enzyme digest of liver DNA isolated directly or via chromatin did not reveal any consistent peak which could have been attributed to a nucleoside-steroid adduct. (B) All DNA radioactivity could be due to protein contaminations, because the specific activity of chromatin protein was determined to be more than 3,000 times higher than of DNA. The high affinity of the hormone to protein was also demonstrated by in vitro incubations, where it could be shown that the specific activity of DNA and protein was essentially proportional to the concentration of radiolabelled hormone in the organ homogenate, regardless of whether the animal was treated or whether the hormone was added in vitro to the homogenate.Carcinogens acting by covalent DNA binding can be classified according to potency on the basis of the Covalent Binding Index. Values of 10³–10⁴ have been found for potent, 10² for moderate, and 1–10 for weak carcinogens. Since estrone is moderately carcinogenic for the kidney of the male hamster, a CBI of about 100 would be expected. The actually measured limit of detection of 0.01 places covalent DNA binding among the highly unlikely mechanisms of action. Similar considerations can be made for the liver where any true covalent DNA binding must be below a level of 0.01. It is concluded that an observable tumor induction by estrone or estradiol is unlikely to be due to DNA binding.Paper presented at the Satellite Symposium of the European Society of Toxicology, Rome, March 29, 1983     

Penetration and action of edoxudine in vitro and in vivo

The penetration of 5-ethyl-2'-deoxyuridine (edoxudine, Aedurid) from gel base with and without the addition of urea and other adjuvant has been studied in an in vitro model using guinea pig skin. The formulation of 3% edoxudine gel with 5% urea showed the best results. In vivo experiments on hairless mice infected intracutaneously with herpes simplex virus type 1 also showed this formulation's good efficacy as compared to other formulations.     

Extraction and determination of prednisolone in drugs and excipients in ointments and creams and the uniformity of distribution in prednisolone ointment

For the purpose of measuring the contents of prednisolone in low concentrated ointments and creams an instruction was elaborated that includes several steps of extraction, in the resulting solution of which the assay of the steroid by Blue Tetrazolium reaction will be done. The procedure permits the determination of prednisolone in presence of most of usual ingredients of ointment bases except wool alcohols. Also no influence is given by some remedies combined with prednisolone for topical application except coal tar solution. The results confirm a correct reflection of the steroid contents declared respectively the recovery of the steroid added to various ointment bases. Introducing discussion to content uniformity concerning low concentrated ointments is made, and some deviations are shown.     

Mechanisms of antiplatelet and antithrombotic activity of midazolam in in vitro and in vivo studies

Dopamine regulates various physiological functions in the central nervous system and the periphery. Dysfunction of the dopamine system is implicated in a wide variety of disorders and behaviors including schizophrenia, addiction, and attention-deficit hyperactivity disorder. Medications that modulate dopamine signaling have therapeutic efficacy on the treatment of these disorders. However, the causes of these disorders and the role of dopamine are still unclear. Studying the dopamine system in a model organism, such as Caenorhabditis elegans, allows the genetic analysis in a simple and well-described nervous system, which may provide new insight into the molecular mechanisms of dopamine signaling. In this review, we summarize recent findings on pharmacological and biochemical properties of the C. elegans dopamine receptors and their physiological role in the control of behavior.     

Comparative in vivo and in vitro studies of phenytoin protein binding and in vitro lipolysis in plasma of pregnant and nonpregnant rats

This investigation was designed to determine the cause of the changes in drug protein binding that occur in rat plasma, particularly in plasma from pregnant animals, during in vitro drug-protein binding measurements. In vivo estimates of phenytoin binding in plasma were obtained from steady-state CSF-plasma concentration ratios in pregnant and nonpregnant rats. Immediate ultrafiltration of heparin- or EDTA-anticoagulated plasma yielded phenytoin free fraction values that were in good agreement with in vivo estimates for nonpregnant rats but that were about one-third higher than in vivo estimates for pregnant animals. In vitro free fraction values tended to increase during incubation of plasma and/or during equilibrium dialysis. The concentrations of the four major endogenous free fatty acids were similar in plasma of pregnant and nonpregnant rats if determined immediately after blood collection. Six hours of incubation at 37 degrees C caused fatty acid concentrations to increase about fivefold and twofold in heparin-anticoagulated plasma from pregnant and nonpregnant animals, respectively. The corresponding increases in EDTA-anticoagulated plasma were only about twofold and 1.14-fold, respectively. These changes were associated with decreased plasma protein binding of phenytoin. The in vivo differences between pregnant and nonpregnant rats with respect to phenytoin binding in plasma are not due to differences in fatty acid concentrations, but the in vitro differences are due primarily to corresponding differences in free fatty acid concentrations if extensive in vitro lipolysis occurs.     

Comparison of in vitro and in vivo developmental toxicity and pharmacokinetics of phenytoin in the rat

The rat whole embryo culture was compared to an in vivo experiment with regard to embryotoxicity as well as exposure characteristics, using phenytoin as a model compound. Intra-embryonic concentrations and their embryotoxic effects were determined on gestation day 11 after in vitro administration of 50-150 microg/ml or in vivo gavage of 500-1500 mg/kg body-weight on gestation day 10. In addition, exposure kinetics were studied in vivo after a single oral dose on gestation day 10, and developmental defects on gestation day 21 were scored. The embryotoxic effects observed on gestation day 11 were more pronounced after in vitro exposure in comparison to in vivo exposure at similar intra-embryonic concentrations. Exposure of phenytoin on gestation day 10 in vitro via the culture medium resulted in general embryotoxicity on gestation day 11, whereas in vivo effects as determined on gestation day 11 were minimal. Plasma concentrations of phenytoin increased and plateaued around 35 microg/ml during the 48 hr monitoring period. Plasma concentration curves and pharmacokinetic parameters did not show remarkable differences between the dose groups, indicating that absorption is the limiting factor at the dose range used. Although the developmental effects were minimal as observed in vivo on gestation day 11, specific malformations (defects encompassing the urogenital. craniofacial and skeletal systems) were observed on gestation day 21. These findings show that with similar intra-embryonic concentrations of phenytoin the embryotoxicity in rat whole embryo culture was not comparable with the in vivo embryotoxicity as determined on gestation day 11. This discrepancy may at least partly be explained by differences in exposure characteristics.     

Mathematical modelling of in situ and in vitro efflux of ciprofloxacin and grepafloxacin

The efflux process due to p-glycoprotein-like mechanisms of ciprofloxacin (CIP) and grepafloxacin (GRX) has been studied "in situ" in rats and "in vitro" in Caco-2 cells. The results were modelled by a curve fitting procedure which allowed the characterization of the passive (Pd) and carrier mediated parameters (Vm and Km) from the raw data without initial velocities estimation. CIP absorption in rat was characterized as a passive diffusion at the assayed concentrations. Although the involvement of an efflux transporter cannot be ruled out, its relevance in the transport of the fluoroquinolone is negligible. In GRX absorption, an efflux process is implicated and it is detected in both absorption models. GRX permeability depends on the intestinal segment, reflecting the previously reported different expression level of the efflux transporters along the gut in rat. A first attempt to correlate the "in vitro" and the "in situ" data has been done. The mathematical model has been constructed using very simplistic assumptions and it will require further refinement but, nevertheless, the results are promising and demonstrate that a good modelling approach helps to identify the system critical parameters and how the system behaviour change when the parameters are modified as it happens when we move from the "in vitro" to the "in situ" level. Predicted versus experimental permeability values show a good correlation, demonstrating that the relevance of the secretion process "in situ" in rat can be predicted from the "in vitro" cell results.     

Comparison of pulmonary and hepatic glucuronidation and sulphation of ethanol in rat and rabbit in vitro

1. Pulmonary and hepatic UDP-glucuronyltransferase and sulphotransferase activities in subcellular fractions from rats and rabbits were determined, comparing ethanol with known substrates for these enzymes.

2. No ethyl glucuronide formation was detected with either hepatic or pulmonary microsomal incubations.

3. Chromatographic, autoradiographic and scintillation counting analysis indicated that ethanol is sulphated by rat and rabbit pulmonary cytosol, although this activity was approx. 2–6% of that in liver.

4. Rat hepatic and pulmonary sulphotransferase activities with β-naphthol were approx. 13 and 60 times higher than with ethanol, respectively.

5. Rabbit hepatic and pulmonary sulphotransferase activities with both substrates were higher than those in rat.