薄荷醇对戊巴比妥中枢抑制作用的影响

研究薄荷醇经胃肠道给药戊巴比妥中枢抑制作用的影响，结果发现，薄荷对戊巴比妥的中枢抑制作具有一定的量效关系，含４．５％的薄荷醇溶中明显使小鼠的入睡时间短，并使急性死亡率增加，而含１．５％和０．５％的薄荷溶液对戊巴比妥的中枢抑制作用的无明显影响。     

酒对药物作用的干扰

酒能直接或间接地引起药物在体内的吸收、代谢、排泄的改变,对药物作用发生干扰,从而影响药物的治疗效果,或产生毒性反应。一、酒与药物并用使药物作用增加 1.巴比妥类:内服巴比妥、戊巴比妥、异戊巴比妥等,如同时饮酒可使巴比妥类中枢抑制作用加强。酒精可增加细胞膜的通透性,使巴比妥类易于进入细胞内而在中枢神经系达到更高浓度;酒精还可改变巴比妥类与脂类及蛋白质的结合。 2.吩噻嚓类:氯丙嗪等与乙醇同时使用可产生药物相加作用,加重中枢抑制作用,产生严重低血压,还可使昏迷加深,甚至发生深度呼吸抑制而死亡。     

巴比妥对地中海拟无枝酸菌的生长毒性及其与利福霉素B超产的关系

发展了一种筛选利福霉素Ｂ超产菌株的新方法。加有甘氨酸和巴比妥的合成培养基用诱变过的菌丝接种,培养 ４８ｈ后用溶菌酶处理。耐溶菌酶的菌丝用稀洗涤剂洗涤后种入含甘氨酸但不含巴比妥的合成培养基。所获得的原生质体再生后从中挑选菌落接种在加和不加巴比妥的Ｂｅｎｎｅｔ琼脂平板上。所挑选出的２株突变株对０．５％巴比妥敏感,其利福霉素产量比亲株高１倍。此外还分离出３０株耐巴比妥的突变株,但其产量均低于亲株。据此认为巴比妥对次级代谢（产生利福霉素）的影响与它对初级代谢的影响有关。     

药物相互作用

四、中枢抑制药处 理巴比妥类·口服抗凝药、口服避孕药、雌激素、皮质激素、三环抗抑郁药、洋地黄类(包括地高辛)、奎 尼丁、茶碱及其他经肝代谢药物:巴比妥类可诱导肝微粒体酶,促进这些药物的代谢和首 过作用,使之降效。·碳酸氢钠:使尿碱化、促进巴比妥类的尿排泄,使之降效。此作用可用来解救巴比妥类中 毒。·苯妥英钠:药效学上两者作用相加;药物动力学方面两者的代谢均可加速,出现复杂的相 互作用。·中枢抑制药、乙醇、全麻药、单胺氧化酶抑制药:药效相加。苯二氮堇类 ,·中枢抑制药:中枢抑制作用加强。·抗高血压药、利尿降压药:降压…     

关于巴比妥类药物中毒给予中枢兴奋剂的问题

关于巴比妥类药物中毒给予中枢兴奋剂的问题徐永昭（大连医科大学附属第一医院１１６０１１）巴比妥类药物是临床上常用的镇静、催眠、抗惊厥药，由于误服或其它原因，一次进入人体的量超过催眠剂量的５～６倍即可引起急性中毒，超过１５倍时，可出现致命的危险。关于巴比...     

巴比妥对地中海拟无枝酸菌的生长毒性及其与利福霉素B超？…

发展了一种筛选利福霉素Ｂ超产菌株的新方法。加有甘氨酸和巴比妥的合成培养基用诱变过的菌丝接种,培养４８ｈ后用溶菌酶处理,而溶菌酶的菌丝用稀洗涤剂洗涤后种入含甘氨酸但不含巴比妥的合成培养基。所获得的原生质体再生后从中挑选菌落接种在加和不加巴比妥的Ｂｅｎｎｅｔ琼脂平析上,所挑选出的２株突变株对０．５％巴比妥敏感,其利福霉素产量比新株高１倍。引外还分离同３０株耐巴比妥的突变株,但其产量均低于亲株。据此认为     

刺五加的药理与临床应用

1药理作用 1.1对中枢神经系统的作用:对中枢神经兴奋抑制过程均有影响.改善兴奋过程,加强抑制过程,兴奋与人参相似.使兔脑图呈现微兴奋,并降低水合氯醛、巴比妥、氯丙嗪的抑制作用.它的兴奋作用原理不同于苯丙胺类,不仅毒性小,而且不影响正常睡眠过程[1].     

服药时为什么不能饮酒？

酒中含有乙醇。乙醇除了加速某些药物在体内的代谢转化,降低疗效外,也能诱发药品不良反应。长期饮酒可能引起肝功能损伤,影响肝脏对药物的代谢功能,使许多药品的不良反应增加。特别是服药时饮酒,可使消化道扩张,增加药物吸收,从而易引起不良反应。如服用巴比妥类药物时饮酒,则可增强巴比妥类药物的中枢抑制作用造成危害。头孢类抗菌药可影响乙醇代谢,出现双硫仑样反应,表现为面部潮红、头痛、眩晕、腹痛、恶心、呕吐、气促、     

高效毛细管电泳法分析血样尿样中巴比妥类药物

建立了血、尿样品中巴比妥类药物的高效毛细管电泳分离测定方法，测定条件为：运行缓冲液配比：１００ｍｍｏｌ／Ｌ十二烷基硫酸钠－１００ｍｍｏｌ／Ｌ磷酸二氢钠－甲醇－水＝７０∶１５∶５∶１０（ｐＨ值调至７．５５±０．０５），操作电压１７ｋＶ，检测波长２００和２８５ｎｍ，２０ｍｉｎ内７种巴比妥类药物全部得到分离。考察并选择了体液样品的预处理方法，测定了血浆和尿液中６种巴比妥类药物浓度（苯巴比妥、甲基苯巴比妥、异戊巴比妥、硫喷妥、戊巴比妥和速可眠）。测定血药浓度的线性范围为５．０～３５μｇ／ｍｌ，尿样药物浓度线性范围为１．０～８．０μｇ／ｍｌ，最低检测浓度为１．０μｇ／ｍｌ，方法重现性为ＲＳＤ小于１３％。     

联苯双酯多羟基酯的合成

联苯双酯(简称BDD)是根据中药五味子的有效成分之一丙素的合成中间体,经筛选而得到的。BDD的药理作用是能降低血清丙谷酶(SGPT)的活性,能促进部分切除肝脏的小鼠肝脏的再生,加速肝脏对戊巴比妥的代谢,具有保肝解毒作用。由于BDD的脂溶性强,较易于通过血脑屏障进入大脑产生中枢抑制作用,长期服用出现头晕、嗜睡等症状。另外,BDD的生物利用度仅为30％～39％,为减少BDD的中枢抑制作用,提高生物利用度,考虑降低它的亲脂性。首先,将BDD水解成钠盐,结果它的     

The effect methoxsalene on hypnotic and subhypnotic doses of pentobarbital.

The effect of several doses of methoxsalen on hypnotic action of 40 mg/kg of pentobarbital in mice was studied. Methoxsalen was injected 30 minutes before the barbiturate. The highest methoxsalen dose of 22 mg/kg extended the duration of the hypnotic action of pentobarbital about 10 times compared to the control. The effect decreased with time, and 96 hours after this single dose of methoxsalen it was not significantly different from that observed with the control animals receiving only 40 mg/kg pentobarbital. The other methoxsalen doses (10, 5, and 2 mg/kg) exhibited an equal effect on the hypnotic action of pentobarbital, and only in the first measuring time. The effect could not be detected after 24 hours, and no dose dependence was observed. Small doses of methoxsalen of 2 and 1 mg/kg injected 30 minutes before a subhypnotic pentobarbital dose of 30 mg/kg produced sleep in 75% of animals of the both groups. In the control group, this dose produced no sleep in none of the animals.     

白花败酱草水提取液中枢抑制作用的研究

目的研究白花败酱草水提取液对小鼠中枢神经系统的抑制作用。方法取白花败酱草水提取液分别单独、配伍使用阈上或阈下剂量的戊巴比妥钠注入小鼠体内,观察小鼠的自发活动和睡眠时间,并将结果与对照组进行比较、分析。结果白花败酱草水提取液对小鼠自发活动有明显的抑制作用,可以缩短由戊巴比妥钠诱导的入睡时间及延长睡眠时间。结论白花败酱草水提取液具有明显的中枢抑制作用,与戊巴比妥钠的中枢抑制功能有协同作用。     

不同比例五味子宁神口服液镇静催眠作用研究

目的:寻找五味子宁神口服液镇静催眠作用的最佳配伍比例。方法:通过对小鼠自发活动的影响、对戊巴比妥钠的协同作用、对中枢神经递质的影响等3方面药理学研究,探讨五味子宁神口服液不同配伍比例的镇静催眠作用。结果:五味子宁神口服液以原方用药25%五味子比例作用最好。结论:五味子宁神口服液组方配伍是合理的。     

Interaction of alcoholic extracts of hops with pentobarbital and diazepam in mice.

The interaction of alcoholic extracts of Magnum, Aroma and wild genotype hops with drugs that lower the activity of the central nervous system (CNS) was studied in mice. Hops drying and preparation of extracts were performed according to standard pharmacological procedures for preparing total alcoholic extracts of medicinal plants, i.e. in a ratio of one part dry herbs to two parts of 70% alcohol, with evaporation to dryness so that the extracts no longer contained any alcohol. The mice received four doses intraperitoneally (i.p.) of 0.5% aqueous solutions of the above-mentioned extracts, which were dissolved in warm physiological solution to make up a 0.5% aqueous solution, 24, 16, 4 and 0.5 hours before pentobarbital (40 mg/kg) or diazepam (3 mg/kg) administration. The hypnotic action of pentobarbital and the effect of diazepam on the coordination of movements (rotating rod method) were measured. It was found that hops extracts influenced the action of the investigated drugs, and that the extracts of the Magnum and Aroma genotypes suppressed the hypnotic action of pentobarbital and diazepam. Tert-butanolic extracts also suppressed the action of these two drugs but to a lesser extent, whereas wild hops extracts did not exert any significant effects compared to controls.     

Interaction of alcoholic extracts of hops with pentobarbital and diazepam in mice.

The interaction of alcoholic extracts of Magnum, Aroma and wild genotype hops with drugs that lower the activity of the central nervous system (CNS) was studied in mice. Hops drying and preparation of extracts were performed according to standard pharmacological procedures for preparing total alcoholic extracts of medicinal plants, i.e. in a ratio of one part dry herbs to two parts of 70% alcohol, with evaporation to dryness so that the extracts no longer contained any alcohol. The mice received four doses intraperitoneally (i.p.) of 0.5% aqueous solutions of the above-mentioned extracts, which were dissolved in warm physiological solution to make up a 0.5% aqueous solution, 24, 16, 4 and 0.5 hours before pentobarbital (40 mg/kg) or diazepam (3 mg/kg) administration. The hypnotic action of pentobarbital and the effect of diazepam on the coordination of movements (rotating rod method) were measured. It was found that hops extracts influenced the action of the investigated drugs, and that the extracts of the Magnum and Aroma genotypes suppressed the hypnotic action of pentobarbital and diazepam. Tert-butanolic extracts also suppressed the action of these two drugs but to a lesser extent, whereas wild hops extracts did not exert any significant effects compared to controls.     

绒毛钩藤影响中枢神经系统的药理学研究

目的研究绒毛钩藤对中枢神经系统的药理作用。方法小鼠自主活动实验观察其镇静作用;戊巴比妥钠阁下催眠实验观察其催眠作用;士的宁致小鼠惊厥实验观察其抗惊厥作用。结果自主活动试验中．绒毛钩藤提取物（0．16g·kg^-1）灌胃给药后,小鼠60min时的自主活动计数与生理盐水组相比．明显减少（P〈0．01）。在戊巴比妥钠阁下催眠实验中,绒毛钩藤低（0．16g·kg^-1）,中（0．32g·kg^-1）剂量灌胃给药后,小鼠翻正反射消失的个数与生理盐水组比较。均明显增多（P〈0．01）。士的宁致小鼠惊厥实验中。绒毛钩藤提取物灌胃给药后．与生理盐水组比较,中（0．32g·kg^-1）剂量组小鼠死亡数目明显减少（P〈0．01）,高（0．64g·kg^-1）剂量组小鼠死亡数目明显增多（P〈0．01）。结论绒毛钩藤在低剂量和中剂量对中枢神经系统有抑制作用,在高剂量对中枢神经系统有兴奋作用。     

Respiratory effects of quazepam and pentobarbital

Quazepam is a new benzodiazepine that may provide good hypnotic action with negligible effect on motor coordination or respiration. Sleep laboratory studies on human volunteers have shown quazepam 15 mg to be an effective hypnotic dose, with the 30-mg dose being optimal. At these doses, there was no deterioration of motor performance, and the drug, when given nightly for two weeks, continued to exert hypnotic effects without serious adverse effects. Therefore, this study was designed to compare the respiratory effects of quazepam 15 and 30 mg to those of pentobarbital 50 and 150 mg and to placebo. Five adult male volunteers received each dose at separate times. A double-blind technique was employed for controlled rebreathing studies, to a ventilation of 40 L/min or a PETCO2 of 8%. Respiratory curves were compared with controls. The mean displacement curve at the 20-liter intercept showed a depressant effect for pentobarbital 150 mg at two hours and a stimulant effect for quazepam 15 mg at two hours but a slight depression effect for quazepam 30 mg at three hours compared with placebo. The slope of the respiratory curve was not affected.     

牛黄千金散对中枢的抑制作用

目的探讨牛黄千金散对中枢的抑制作用。方法给小白鼠灌胃牛黄千金散 ,分别采用苯甲酸钠咖啡因和电刺激引起惊厥 ,观察牛黄千金散的对抗作用 ;加用戊巴比妥钠给小白鼠灌胃 ,药后15min内观察翻正反射消失作为催眠指标 ;加用可待因给小白鼠灌胃 ,用扭体法观察小白鼠的镇痛作用 ;牛黄千金散小白鼠灌胃 ,用抖笼法观察对小白鼠自发活动的影响。结果牛黄千金散对药物和电刺激引起的惊厥均有对抗作用 ,并能加强戊巴比妥钠的催眠作用 ;加强可待因的镇痛作用 ;对小白鼠自发活动也有一定的抑制作用 ,与生理盐水对照组比较有非常显著的差异(P<0.01)。结论牛黄千金散有明显的中枢抑制作用。     

不同透皮促进剂对环吡酮胺和水杨酸体外经皮渗透性的影响

目的：以环吡酮胺和水杨酸为模型药物。研究透皮促进剂对外用抗真菌药的促透特性。方法：在离体透皮实验装置上进行透皮吸收试验和贮库效应的研究。结果：1%氮酮和1%薄荷醇联用对环吡酮胺经皮渗透的促进作用明显高于其它组，1%的薄荷醇对水杨酸促透效果最佳。而由1%氮酮。2.5%丙二酮，2.5%油酸，1%薄荷醇合用对环吡酮胺的体外经皮渗透虽具有明显的促进作用和时滞明显缩短。但是与二联使用透皮促进剂比较并无明显优点。结论：薄荷醇和氮酮对环吡酮胺和水杨酸体外经皮吸收具有显的促进作用。两联用对脂溶性化合物环吡酮胺的促透作用更明显。     

参芪五味子胶囊镇静、抗应激作用研究

目的:研究参芪五味子胶囊镇静、抗应激的作用。方法:采用戊巴比妥钠阈下剂量及催眠剂量观察参芪五味子胶囊对戊巴比妥钠小鼠催眠的协同作用;采用小鼠游泳、常压下耐缺氧实验观察参芪五味子胶囊对小鼠的抗应激作用。结果:参芪五味子胶囊能显著延长戊巴比妥钠小鼠的睡眠时间,增加阈下剂量戊巴比妥钠入睡小鼠只数;显著延长小鼠游泳时间和耐缺氧时间。结论:参芪五味子胶囊具有镇静、抗应激的作用。