Staub F, Stoffel M, Berger S, Eriskat J, Baethmann A
Institute for Surgical Research, Ludwig-Maximilians-University, Munich, Germany.
J Neurotrauma. 1994 Dec;11(6):679-90. doi: 10.1089/neu.1994.11.679.
The efficacy of the diuretic agent torasemide, which antagonizes the Na+/K+/Cl- cotransport and Cl- channels, was investigated to determine its inhibition of brain edema from a focal cerebral lesion. For this purpose, cold injury of the brain was induced in 50 Sprague-Dawley rats while monitoring arterial blood pressure. The brain was removed for gravimetric assessment of swelling of the traumatized hemisphere 24 h after trauma. The water content was also determined after drying the cerebral hemispheres for 24 h. Animals were divided into five groups. A control group with trauma received vehicle only; two other groups received 1.0 or 10.0 mg torasemide/kg body weight 30 minutes before and 6 h after trauma (n = 10-12). Administration of the drug after the insult was also investigated in animals with application of vehicle or 10.0 mg/kg of torasemide at 30 minutes and 6 h following the brain lesion (n = 8). Torasemide did not affect important physiologic variables, such as the arterial pO2, pCO2, pH, hemoglobin, hematocrit, or plasma osmolality, while increasing blood pressure (p < 0.01). The blood pressure response notwithstanding, treatment significantly attenuated hemispheric brain swelling from trauma. In control animals without treatment, cold injury led to hemispheric swelling of 8.89%. In animals with 1 mg torasemide/kg BW, brain swelling amounted to 8.51% and to 7.04% in animals receiving 10 mg/kg before and after the insult (p < 0.005). Treatment was also found to attenuate the increase in tissue water content from trauma, but without reaching statistical significance. Postinsult treatment with torasemide (10 mg/kg BW) at 30 minutes and 6 h after trauma was again associated with a significant reduction in hemispheric brain swelling, which in this group amounted to 7.46% compared with 9.76% in the untreated controls (p < 0.005). The increase in the cerebral water content from trauma was also significantly blunted in the latter experiments (p < 0.01). The present data indicate a remarkable therapeutic potential of the novel diuretic agent torasemide to reduce vasogenic brain edema from an acute cerebral lesion. It is surmised that the compound specifically interferes with Cl- transport mechanisms, which apparently are activated in edematous brain involving neuronal and glial cells, for example. This conclusion is supported by in vitro observations that torasemide inhibits the swelling of glial cells from acidosis. On the other hand, it is unlikely that gross dehydration of the brain secondary to the induction of diuresis by the agent played a role, because hematocrit and plasma osmolality were not found to be affected.
研究了具有拮抗Na+/K+/Cl-协同转运和Cl-通道作用的利尿剂托拉塞米抑制局灶性脑损伤后脑水肿的疗效。为此,在监测动脉血压的同时,对50只Sprague-Dawley大鼠进行脑冷损伤。创伤24小时后取出大脑,通过重量法评估受伤半球的肿胀情况。在将脑半球干燥24小时后还测定了含水量。动物被分为五组。创伤对照组仅给予赋形剂;另外两组在创伤前30分钟和创伤后6小时分别接受1.0或10.0mg托拉塞米/千克体重(n = 10 - 12)。还对创伤后给药的动物进行了研究,在脑损伤后30分钟和6小时分别给予赋形剂或10.0mg/kg托拉塞米(n = 八)。托拉塞米不影响重要的生理变量,如动脉血氧分压、二氧化碳分压、pH值、血红蛋白、血细胞比容或血浆渗透压,同时会使血压升高(p < 0.01)。尽管有血压反应,但治疗显著减轻了创伤引起的半球性脑肿胀。在未治疗的对照动物中,冷损伤导致半球肿胀8.89%。在接受1mg托拉塞米/千克体重的动物中,脑肿胀为8.51%,在创伤前后接受10mg/kg的动物中为7.04%(p < 0.005)。还发现治疗可减轻创伤引起的组织含水量增加,但未达到统计学显著性。创伤后30分钟和6小时用托拉塞米(10mg/kg体重)进行损伤后治疗再次与半球性脑肿胀的显著减轻相关,该组脑肿胀为7.46%,而未治疗的对照组为9.76%(p < 0.005)。在后者的实验中,创伤引起的脑含水量增加也显著减轻(p < 0.01)。目前的数据表明新型利尿剂托拉塞米在减轻急性脑损伤引起的血管源性脑水肿方面具有显著的治疗潜力。据推测,该化合物特异性地干扰Cl-转运机制,例如在涉及神经元和胶质细胞的水肿脑中这些机制显然被激活。这一结论得到了体外观察结果的支持,即托拉塞米抑制酸中毒引起的胶质细胞肿胀。另一方面,该药物诱导利尿继发的大脑严重脱水不太可能起作用,因为未发现血细胞比容和血浆渗透压受到影响。