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棓酰苯胺与安定或香草醛相互作用的实验研究

EXPERIMENTAL STUDIES ON INTERACTION OF GALLANILIDE WITH DIAZEPAM OR VANILLIN

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【作者】 李端; 杨香媛; 王永铭; 王锦平; 竺心影; 韦容容; 袁保嘉;

【Author】 LI DUAN, YANG XIANGYUAN, WANG YONGMING,WANG JINPING, ZHTJ XINGYINGWEI RONGRONG, YUAN BAOJIA(Department of Pharmacology and Biochemistry, Faculty of Pharmacy, Shanghai First Medical College, Shanghai)

【机构】 上海第一医学院药学系药理生化教研室; 本系分析化学教研室; 本系分析化学教研室;

【摘要】 本文用实验动物研究安定或香草醛对棓酰苯胺(603)的抗心律失常作用、致惊厥毒性和药代动力学参数的影响。结果表明安定(1mg/kg)和香草醛(200mg/kg)均可拮抗603对小鼠的惊厥作用,而口服香草醛(300mg/kg)可显著增加603的抗心律失常作用。腹腔注射安定(1mg/kg)可显著减少603对大鼠乌头碱心律失常模型的治疗剂量,自23.29±1.25mg/kg(X±SE)减少到12.60±1.08mg/kg。合并用药对603药代动力学参数的影响,只安定组显示药物消除速率减小,半衰期延长(p<0.05),而在香草醛组未见显著变化。

【Abstract】 The effects of diazepam or vanillin on antiarrhythmio action, convulsive toxicity and pharmacokinetic parameters of gallanilide (603) were investigated on the experimental animals. The results, thereof, indicated that diazepam (1 mg/kg) or vanillin (200mg/kg) could antagonize 603-indueed convulsive toxicity in mice, while oral administration of vanillin (300 mg/kg) significantly increased the antiar-rhythmio effect of 603. On aoonitine-induced arrhythmias in rats, intraperitoneal injection of diazepam (1 mg/kg) would significantly reduce the therapeutic dose of 603 from 22.29±1.25mg/kg alone (X±SE) to 12.64±1.08mg/kg (p<0.001). In rabbits when intravenously injected with diazepam and 603 simultaneously, reduction in the elimination rate of 603 and prolongation of its half-life were significant (p<0.05), No obvious changes, however, were observed on the vanillin group.

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