舒筋灵、唛酚生、地西泮对杀虫单中毒的保护作用

目的：探讨舒筋灵、唛酚生、地西泮三种中枢性肌松剂对杀虫单（ＳＣＤ）急性中毒的解救效果。方法：采用Ｂｌｉｓｓ法测定ＬＤ５０，并进行其显著性测定。结果：三种肌松剂能提高小鼠ＳＣＤ急性中毒ＬＤ５０３～４保，差异非常显著，二疏基丙磺酸钠（ＤＭＰＳ）与肌松剂合用效果更佳。先给中枢性肌松剂对大鼠ＳＣＤ急性中毒有良好的保护作用。结论：ＳＣＤ经口染毒主要是引起中枢性兴奋致惊厥最后衰竭而死，单用中枢性肌松剂有良好     

癫痫持续状态及其治疗--附86例报告

目的:本文报告86例癫痫持续状态,年龄12～80岁,平均(48.63±18.11)岁.男37例,女49例.其中强直-阵挛持续状态60例,阵挛-强直-阵挛持续状态21例,强直持续状态型3例及复杂性部分型癫痫持续状态-精神运动癫痫持续状态2例.方法:本组治疗分为苯巴比妥钠肌注组45例,安定静脉注射组41例.结果:两组在控制癫痫持续状态时为(28.53±10.95)min对(33.85±11.53)rmin,P＜0.05.结论:说明苯巴比妥和安定联合用药效果好.     

加锡果宁的中枢抑制作用与神经递质受体的关系

加锡果宁ip或ig后能诱发小鼠入睡,明显延长戊巴比妥钠小鼠的睡眠时间和入睡鼠数,对抗小鼠、大鼠MES,提高小鼠脑内DA、DOFAC、5-HT、HVA含量,并能从受体上置换出~3H-绳蕈醇,~3H-安定,其IC_(50)分别为5×10~(-4)M及4.4×10~(-5)M,提示加锡果宁的抗惊厥作用可能与其学兴奋DA、5-HT能神经元,提高DA、5-HT递质含量、激活苯二氮唑受体有关。     

Effects of benzodiazepines on laryngeal reflexes

Of 20 volunteers, five were given intravenous Diazemuls 15 mg over 15 seconds, and three groups of five were given lormetazepam 2 mg intravenously over 10, 20 and 60 seconds, respectively. Laryngeal reactivity and psychomotor function were tested at intervals from prior to injection until 4 hours after injection. For equivalent degrees of depression of psychomotor function, lormetazepam depressed the laryngeal reflex less than Diazemuls (p = 0.004). Lormetazepam give over 60 seconds depressed the laryngeal reflex more than when given over 10 seconds (p = 0.008) or over 20 seconds (p = 0.048), although a significant difference was not demonstrated between the 10-second and 20-second groups. These results concur with experimental evidence that benzodiazepine receptor multiplicity exists, which allows various members of the benzodiazepine group of drugs to exhibit differing therapeutic ratios for their various effects.     

Effects of diazepam on diaphragmatic functionand recovery in pentobarbital-anesthetized dogs: An open-label, dose-finding, pharmacologic study

Background:

Diazepam, a highly lipid-soluble benzodiazepine, is commonly used as a sedative agent during and after surgery. Based on a literature search, no published data are available concerning diaphragmatic function (as measured by contractility and electrical activity) during and after the administration of diazepam.

Objective:

The purpose of this study was to assess the effects of diazepam use on diaphragmatic function and recovery in pentobarbital-anesthetized dogs.

Methods:

This open-label, dose-finding, pharmacologic study was conductedat the Department of Anesthesiology, Institute of Clinical Medicine, University of Tsukuba, Tsukuba, Japan. Healthy adult mongrel dogs weighing 10 to 15 kg were assigned to 1 of 3 study groups: low dose (0.2-mg/kg) diazepam, high-dose (0.5-mg/kg) diazepam, or control (no study drug). Each dog was anesthetized with pentobarbital 2 mg/kg · h IV Study drug was administered IV for 1 hour. Diaphragmatic function was assessed before (baseline) and at 0 (immediately after), 1, and 2 hours after the end of study drug administration, using measurement of transdiaphragmatic pressure (Pdi), defined as the difference between gastric and esophageal pressures, and by integrated electrical activity (20- and 100-Hz stimulation) of the crural (Edi-cru) and costal (Edi-cost) parts of the diaphragm. The percentage changes from baseline in Edi-cru (%Edi-cru) and Edi-cost (%Edi-cost) were calculated.

Results:

Twenty-four mongrel dogs were used in the study; 8 dogs were assigned to each treatment group. During diazepam administration in the low-dose group, significant decreases from baseline in Pdi were found with 20-Hz stimulation (15.6 [1.7] vs 13.3 [1.9] cm H₂O; P < 0.05) and 100-Hz stimulation (22.0 [2.1] vs 19.6 [1.8] cm H₂O; P < 0.05). In the high-dose group, the decreases in Pdi were significant with 20-Hz stimulation (15.5 [1.8] vs 10.0 [2.0] cm H₂O; P < 0.05) and 100-Hz stimulation (22.2 [1.9] vs 16.2 [ 2.0 ] cm H₂O; P < 0.05). In the low-dose group at 100-Hz stimulation, mean (SD) %Edi-cru and %Edi-cost were significantly lower compared with baseline (88.8% [6.6%] and 88.5% [5.9%], respectively; both, P < 0.05). In the high-dose group at 100-Hz stimulation, mean (SD) %Edi-cru and %Edi-cost were significantly lower compared with baseline (77.5% [4.3%] and 78.0% [5.0%], respectively; both, P < 0.05). The decreases in Pdi, %Edi-cru, and %Edi-cost were significantly greater in the high-dose group compared with the low-dose group (all, P < 0.05).

Conclusion:

The results of this experimental study of the effects of diazepamon diaphragmatic function and recovery in pentobarbital-anesthetized dogs suggest that diazepam inhibits diaphragmatic function in a dose-related manner and delays recovery.     

醒脑静治疗安定中毒的临床观察

目的:探讨醒脑静注射液联合纳络酮注射液在急性安定中毒治疗中的疗效。方法:本研究采用醒脑静注射液联合纳络酮注射液治疗急性安定中毒55例并与单纯纳络酮治疗的51例进行对照。106例患者均经静脉血毒物测定为安定中毒;来诊时均有意识障碍,平均年龄(30.35±7.95)合并酒精中毒及其他疾病20例,常规给予洗胃、补液、利尿促排泄、纠正电解质失衡、吸氧及抗感染等对症处理。结果:醒脑静注射液治疗组与对照组患者比较,神志恢复时间(h),治疗组(1.73±0.98)显著短于对照组(3.22±1.38)(P<0.01);同组患者就诊时与清醒后的神志、呼吸、血压、心率及瞳孔等临床指标比较差异有显著性(P<0.05)。结论:醒脑静注射液与纳络酮联合应用,治疗急性安定中毒与对照组比较起效快、疗效确定,临床应用安全可靠。     

Orofacial movements in phospholipase C‐related catalytically inactive protein‐1/2 double knockout mice: Effect of the GABAergic agent diazepam and the D1 dopamine receptor agonist SKF 83959

Orofacial movements are regulated by D₁‐like dopamine receptors interacting with additional mechanisms. Phospholipase C‐related catalytically inactive protein (PRIP) regulates cell surface expression of GABA_A receptors containing a γ2 subunit. Mutant mice with double knockout of PRIP‐1 and PRIP‐2 were used to investigate aspects of GABAergic regulation of orofacial movements and interactions with D₁ mechanisms. Vertical jaw movements, tongue protrusions and movements of the head and vibrissae were reduced in PRIP‐1/2 double knockouts. The GABA_Aergic agent diazepam reduced movements of the head and vibrissae; these effects were unaltered in PRIP‐1/2 double knockouts. The D₁‐like agonist SKF 83959 induced vertical jaw movements, incisor chattering, and movements of the head and vibrissae that were unaltered in PRIP‐1/2 double knockouts. However, SKF 83959‐induced tongue protrusions were reduced in PRIP‐1/2 double knockouts. PRIP‐mediated regulation of GABA_Aergic receptor mechanisms influences topographically distinct aspects of orofacial movement and interacts with D₁ receptor systems. Synapse 64:714–720, 2010. © 2010 Wiley‐Liss, Inc.     

高效液相色谱法测定人血浆中地西泮和咪达唑仑含量

目的 建立测定人血浆中地西泮和咪达唑仑质量浓度的高效液相色谱法.方法 色谱柱采用Waters C18柱(250 mm x4.6mm,5μm),流动相为乙腈-水(55∶45),柱温30℃,流速1.0 mL/min,检测波长220 nnl.结果 地西泮和咪迭唑仑的最低检测质量浓度为5 ng/mL,进样质量浓度的线性范围为O.05～10.0μg/mL(r＞0.990 0);咪达唑仑和地西泮日内精密度的RSD分别为3.09%～5.33%和1.56%～4.25%,日间精密度的JRSD分别为4.72%～6.52%和2.59%～6.22%,方法回收率分别为94.02%～97.19%和96.07%～105.64%.结论 所用方法简便、快速、准确,适用于地西泮和咪达唑仑体内血药浓度和生物等效性的测定.