依托咪酯复合舒芬太尼在老年患者肠镜检查中的应用效果

目的：探讨依托咪酯复合小剂量舒芬太尼在老年患者无痛肠镜检查麻醉中应用的安全性及效果。方法选取2013年8月~2014年10月在本院行肠镜检查的老年患者60例,ASAⅡ~Ⅲ级,随机分为P组（丙泊酚组）、E1组（依托咪酯组）、E2组（依托咪酯复合小剂量舒芬太尼组）,P组予静脉缓慢注入丙泊酚1.5~2.5 mg/kg;E1组予静脉缓慢注入依托咪酯0.2~0.35 mg/kg;E2组先予静脉缓慢注入舒芬太尼0.1μg/kg,1 min后予依托咪酯0.1~0.3 mg/kg。记录麻醉前（T0）、给药后入镜前（T1）、入镜后2 min（T2）、入镜后5 min（T3）、检查结束（T4）、苏醒时（T5）的心率（HR）、平均动脉压（MAP）、血氧饱和度（SpO2）以及麻醉苏醒时间、不良反应、患者满意度。结果与T0、T5时点比较,P组患者的HR、MAP在T1、T2、T3、T4时点下降明显,差异有统计学意义（P<0.05）,与E1、E2组比较下降明显,差异有统计学意义（P<0.05）。 E1、E2组患者的注射痛发生率低于P组（P<0.05）,P、E2组患者的恶心呕吐、术中体动、肌颤发生率明显低于E1组（P<0.05）。结论依托咪酯复合小剂量舒芬太尼用于老年患者无痛肠镜检查术,对心率和血压影响小,患者的呼吸循环功能更稳定,更适用于老年患者无痛肠镜检查。     

依托咪酯与异丙酚在老年人无痛胃肠镜检查中的应用

目的观察依托咪酯与异丙酚静脉麻醉的效果及安全性。方法 60例实施无痛胃肠镜检查的老年患者,随机分成2组,P组用异丙酚+芬太尼,E组用依托咪酯+芬太尼;观察2组患者检查术中的心率、血压、脉搏、血氧饱和度的变化及苏醒时间。结果 P组在检查过程中血压、心率均下降25%左右,呼吸抑制发生率40%,E组则变化较小,血压下降5%左右,心率下降0～3%,无呼吸抑制病例。结论依托咪酯复合芬太尼麻醉在无痛胃肠镜检查中优于异丙酚复合芬太尼麻醉,对呼吸及循环抑制轻。     

瑞芬太尼复合依托咪酯脂肪乳在无痛胃镜检查中的研究

目的 研究瑞芬太尼和芬太尼复合依托咪酯脂肪乳注射液应用于无痛胃镜的临床效果和安全性.方法 选择进行无痛胃镜术的患者60例,随机分成瑞芬太尼组(R组)和芬太尼组(F组)各30例,R组:瑞芬太尼1.0μg/kg,依托咪酯脂肪乳注射液0.3mg/kg.F组:芬太尼1.0μg/kg,依托咪酯脂肪乳注射液0.3mg/kg.分别记录瑞芬太尼和芬太尼的用量,依托咪酯脂肪乳注射液的追加情况以及血压、心率、血氧饱和度、苏醒时间、定向力恢复时间以及检查术中术后的并发症情况.结果 两组患者的血压、心率、血氧饱和度变化差异无统计学意义,术中F组需追加依托咪酯的例数较R组多(P＜0.05),苏醒时间显著长于R组,不良反应如头晕、乏力发生率比R组高,但两组的恶心、呕吐发生率和对呼吸功能的影响相似.结论 瑞芬太尼复合依托咪酯脂肪乳注射液用于无痛胃镜的安全性与芬太尼相似,但苏醒快,留观时间短,更适于无痛胃镜检查.     

瑞芬太尼联合依托咪酯乳剂用于老年人无痛胃镜麻醉的临床观察

目的 观察老年人无痛胃镜检查中应用瑞芬太尼联合依托咪酯乳剂静脉麻醉的效果及安全性.方法 80例实施无痛胃镜检查的老年患者,随机分成2组,E组患者静脉缓慢注射依托咪酯乳剂0.15-0.35 mg/kg,RE组患者静脉缓慢注射瑞芬太尼至0.3-0.5 μg/kg,然后静脉注射依托咪酯乳剂0.15-0.3 5 mg/kg,记录2组麻醉前,麻醉后,置胃镜后,苏醒时的SBP、DBP、HR、RR、SpO2,同时记录胃镜检查时间、苏醒时间、麻醉药用量、检查中体动、呛咳及检查后不良反应.结果 两组患者各时点生命体征差异无统计学意义.麻醉后RE组SBP和DBP下降（P〈0.05）;两组患者RR下降（P〈0.05）.两组患者均未出现严重的低血压、心动过缓,SpO2均高于90%.RE组苏醒时间较E组显著缩短（P〈0.05）,依托咪酯乳剂用量较E组显著减少（P〈0.05）,检查中呛咳、体动少于E组（P〈0.05）.结论 瑞芬太尼联合依托咪酯乳剂静脉注射用于老年人无痛胃镜检查麻醉更为安全、快捷.     

依托咪酯联合瑞芬太尼在老年患者无痛胃镜检查中的应用

目的观察依托咪酯联合瑞芬太尼在老年患者胃镜检查和治疗中的应用效果。方法将90例行胃镜检查的患者完全随机分为3组（各30例）,对照组接受常规胃镜检查;瑞芬太尼组静脉注射瑞芬太尼2μg／蝇,丙泊酚每次1．5—2．0mg／kg;联合组静脉注射瑞芬太尼2μg／kg,依托咪酯每次0．2～0．3ms／kg。监测并记录患者入室至检查结束不同时点的心率、血压、血氧饱和度及心电图,观察其苏醒时间及药物不良反应。结果瑞芬太尼组和联合组患者顺利完成胃镜检查,不良反应的发生率均明显低于对照组（P〈0．01）,对照组患者不适感明显;对照组和瑞芬太尼组在检查过程中血压及心率变化较大,与检查前相比较分别升高或降低（P〈0．05或P〈0．01）;联合组则变化较小,与对照组和瑞芬太尼组比较差异有统计学意义（P〈0．05）。瑞芬太尼组患者主诉症状局部疼痛者9例（30．0％）,联合组3例（10．0％）,差异具有统计学意义（P〈0．01）。结论依托咪酯联合瑞苏太尼静脉麻醉用于老年患者无痛胃镜检查安全有效。     

依托咪酯、芬太尼静脉复合麻醉在消化内镜诊疗中的应用

目的研究依托咪酯、芬太尼静脉复合麻醉用于电子肠镜检查的可行性。方法选择无电子肠镜检查禁忌症的需接受肠镜检查的患者116例,其中自愿接受麻醉的58例为组,静脉推注芬太尼,用量2ug/kg,依托咪酯用量0.15mg～0.3mg/kg/次;另58例为组,接受常规肠镜检查。两组病人术中常规监测血氧饱和度、血压及心电图,并记录患者入室至检查结束不同时点的SpO2及HR值,观察苏醒时间和不良反应并进行比较。结果组58例患者顺利完成肠镜检查,患者术中几无不适感,不良反应的发生率较对照组明显降低(P<0.01),组患者反应明显,有两例未完成手术。结论依托咪酯、苏太尼静脉复合麻醉用于电子肠镜检查是一种安全有效方法。     

舒芬太尼复合依托咪酯清醒镇静镇痛在无痛电子胃镜检查中的应用

目的研究舒芬太尼复合依托咪酯清醒镇静镇痛用于无痛胃镜检查中的有效性、安全性和可行性。方法选择ASAⅠ～Ⅱ级拟行无痛胃镜检查患者150例,随机分为三组：丙泊酚组（P组）、依托咪酯组（E组）、舒芬太尼复合依托咪酯组（SE组）,各50例。P组：丙泊酚1．0～2．0mg／kg,E组：依托咪酯0．1～0．2mg／kg,DE组：舒芬太尼0．1μg／kg＋依托咪酯0．1mg／kg。各组均以60秒匀速静脉推注完毕。检查中均视患者体动情况给予适量缓慢静脉追加注射丙泊酚0．25～0．5mg／kg或依托咪酯0．025．0．05mg／kg。观察记录三组患者术前、术中的平均动脉压（MAP）、心率（HR）、经皮脉搏血氧饱和度（SPO,）;记录定向力恢复时间、恢复质量及肌阵挛、心动过缓、血压过低等不良反应情况。结果三组患者在不同时点的平均动脉压（MAP）、心率（HR）、经皮脉搏血氧饱和度（SP02）组间比较差异无统计学意义（P〉0．05）,但与基础值比,P组T1、T2时点MAP、HR、SPO,下降明显,E组和sE组血流动力学明显比P组较平稳;三组定向力恢复时间和患者OAA／S评分结果比较,sE组和P组患者的神志恢复质量明显较E组好,患者术后嗜睡现象明显较少（P〈0．05）,且恢复时间也较E组迅速,但差异无统计学意义（P〉0．05）;E组出现肌阵挛4例,而sE组和P组均不超过2例发生,肌阵挛发生率三组间差异有统计学意义（P〈0．05）。结论舒芬太尼复合依托咪酯清醒镇静镇痛用于无痛电子胃镜检查能达到满意的麻醉效果,且不良反应少,是一种安全、有效、可靠的麻醉方法。     

依托咪酯脂肪乳剂在无痛人工流产术中的应用

目的探讨依托咪酯脂肪乳剂在无痛人工流产术中应用的可行性及最佳药物配合方案。方法选择60例择期行无痛人工流产术的妇女随机分为A、B、C三组,A组给予丙泊酚0.2mg/kg+芬太尼1μg/kg,B组静脉推注咪达唑仑1mg,依托咪酯脂肪乳剂0.2mg/kg+芬太尼1μg/kg,C组静脉推注丙泊酚1mg/kg+依托咪酯脂肪乳剂0.1mg/kg+芬太尼1μg/kg,观察不同时间点的呼吸循环变化及不良反应的发生。结果依托咪酯脂肪乳剂用在无痛人工流产术中无注射痛,患者呼吸循环稳定,各时点血压、心率、呼吸比较无显著性差异。A、C两组麻醉时间、麻醉诱导时间、麻醉恢复时间短于B组,但是差异无统计学意义。恶心呕吐发生情况三组无显著性差异。重度肌阵挛的发生率A、C组少于B组。结论丙泊酚1mg/kg+依托咪酯脂肪乳剂0.1mg/kg+芬太尼1μg/kg用在无痛人流术中患者呼吸循环稳定,恶心呕吐、肌阵挛的发生率低,用于门诊短小手术是个安全有效地麻醉方法。     

右美托咪定复合丙泊酚在无痛肠镜检查中的应用

目的：观察右美托咪定复合丙泊酚用于无痛肠镜检查的临床效果及安全性。方法：选择用肠镜检查患者66例,随机分成二组P组（n＝33）、D组（n＝33）,入室开放上肢静脉,吸氧,监测血压、心率、血氧饱和度,D组先0.1μg/kg/min静脉推注右美托咪定（0.1μg/kg）,P组静脉推注安慰剂（0.9%生理盐水）3ml后,再2 mg/kg/min静脉推注丙泊酚（1.5 mg/kg）,完成后待睫毛反射消失,开始插镜,检查中如有体动反应,追加丙泊酚30～50mg,并观察丙泊酚用量,及体动,循环、呼吸抑制等副作用。结果：丙泊酚总用药量,可唤醒时间P组明显高于D组,差异有统计学意义（ p〈0.05）;D组体动发生例数明显低于P组,差异有统计学意义（p〈0.05）;用丙泊酚实施无痛麻醉过程中均可导致循环抑制,心率加快,右美托咪定对循环影响小,能导致心率降低,可拮抗丙泊酚的心率加快作用,差异有统计学意义p〈0.05。结论：小剂量右美托咪定在无痛肠镜中的使用,方法简单,具有良好的安全性; 能协同丙泊酚的麻醉镇静作用,提供更佳的术中镇静效果。     

瑞芬太尼在无痛肠镜检查中的应用

目的观察瑞芬太尼加丙泊酚用于无痛肠镜检查的可行性,并与芬太尼加丙泊酚无痛肠镜检查比较。方法选择门诊ASAⅠ～Ⅱ级需行肠镜检查者50例,随机分2组,瑞芬太尼组(R组)和芬太尼组(F组),每组25例。R组,瑞芬太尼1.0μg/kg,60s内缓慢静脉推注,丙泊酚2mg/kg静脉推注后,术中以瑞芬太尼0.05μg/kg·min,加丙泊酚100mg/kg·h,持续输注至手术结束;F组,予芬太尼0.05μg,丙泊酚2mg/kg静脉推注后,术中以丙泊酚4mg/kg·h持续输注,必要时追加丙泊酚30mg。结果术后两组患者对镇痛效果均非常满意,其中F组2例出现肢体扭动征象,追加丙泊酚后缓解;R组出现1例肌僵和呼吸抑制,经面罩加压给氧后缓解。术中生命体征无明显变化。术毕清醒时间F组较R组明显延长(P<0.01)。结论瑞芬太尼加丙泊酚用于门诊无痛肠镜检查是一种安全可行的方法。     

Interindividual variability in metabolic activation in humans in vivo

In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.     

Theophylline kinetics in peripheral tissues in vivo in humans

Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (c_max, t_max, AUC) were calculated for plasma and tissue time courses. The mean AUC_tissue /AUC_plasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - t_max Time to peak concentration - c_max Peak concentration     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

休克时血中氧自由基的变化

本实验测定10名休克患者血浆和红细胞的丙二醛(MDA)、血浆总抗的氧化活性(AOA)的含量。结果表明:休克病人红细胞膜和血浆 MDA 含量(4.298±0.722;5.348±0.834)与对照组(3.235±0.682;4.356±1.081)比较明显增高(P<0.05);血浆 AOA(39.65±7.858)与对照组(48.21±10.81)比较明显降低(P<0.01)。提示:休克时,患者机体内自由基反应增强是引起组织细胞损伤的原因之一。     

Polymorphisms in genes involved in neurotransmission in relation to smoking

Smoking behavior is influenced by both genetic and environmental factors. The genetic contribution to smoking behavior is at least as great as its contribution to alcoholism. Much progress has been achieved in genomic research related to cigarette-smoking within recent years. Linkage studies indicate that there are several loci linked to smoking, and candidate genes that are related to neurotransmission have been examined. Possible associated genes include cytochrome P450 subfamily polypeptide 6 (CYP2A6), dopamine D₁, D₂, and D₄ receptors, dopamine transporter, and serotonin transporter genes. There are other important candidate genes but studies evaluating the link with smoking have not been reported. These include genes encoding the dopamine D₃ and D₅ receptors, serotonin receptors, tyrosine hydroxylase, trytophan 2,3-dioxygenase, opioid receptors, and cannabinoid receptors. Since smoking-related factors are extremely complex, studies of diverse populations and of many aspects of smoking behavior including initiation, maintenance, cessation, relapse, and influence of environmental factors are needed to identify smoking-associated genes. We now review genetic polymorphisms reported to be involved in neurotransmission in relation to smoking.     

Genotoxic effects of chlorophenoxy herbicide diclofop-methyl in mice in vivo and in human lymphocytes in vitro

Diclofop-methyl (DM) is a chlorophenoxy derivative used in large quantities for the control of annual grasses in grain and vegetable crops. In this study, the genotoxic effects of DM were investigated by measuring chromosomal aberrations (CAs) in mouse bone-marrow cells and CA and the comet assay in human peripheral lymphocytes. Mice were treated with 15.63, 31.25, 62.5, and 125?mg/kg body weight of DM intraperitoneally for 24 hours, and 15.63-, 31.25-, 62.5-, 125-, and 250-µg/mL concentrations were applied to human lymphocytes for both 24 and 48 hours. In in vivo treatments, DM significantly, but not dose dependently, increased the total chromosome aberrations, compared to both negative and solvent controls. Cell proliferation was significantly, but not dose dependently, affected by all doses. In in vitro treatments, DM (except 15.63 µg/mL) significantly and dose dependently increased the frequency of chromosome aberrations. Also, 250 µg/mL of 48-hour treatment was found to be toxic. Cell proliferation was significantly and dose dependently affected by DM applications, when compared to negative control. In in vitro treatments, DM significantly decreased the mitotic index only at the highest concentration for 24 hours, and 62.5- and 125-µg/mL concentrations for 48 hours. In the comet assay, a significant and dose-dependent increase in comet-tail intensity was observed at 62.5-, 125-, and 250-µg/mL concentrations. The mean comet-tail length was significantly increased in all concentrations. Our results demonstrate that DM is genotoxic in mammalian cells in vivo and in vitro.     

2010调脂治疗领域进展

2010年在调脂治疗领域针对他汀治疗心血管病的防治又进行了许多探索。本文通过综述他汀类药物的国际大规模临床试验结果,重新评价了他汀类药物在冠心病一级预防和冠心病二级预防中的地位,阐明了强化他汀治疗的意义;对他汀的心肾保护作用和安全性新证据进行了说明。     

Tramadol concentrations in blood and in cerebrospinal fluid in a neonate

Based on blood and cerebrospinal fluid samples collected in a full-term neonate, the penetration of tramadol in the central nervous system is described. Following intravenous administration of tramadol, a lag time of about 4 h was observed until full blood–brain equilibration was achieved. This pharmacokinetic observation is in line with a recent pharmacodynamic evaluation of the central opioid effects of tramadol in adults.