Department of Physiology, University of Puerto Rico-School of Medicine, GPO Box 365067, San Juan, 00936-5067, Puerto Rico.
Department of Anesthesiology, University of Puerto Rico-School of Medicine, GPO Box 365067, San Juan, 00936-5067, Puerto Rico.
Pharmacol Rep. 2020 Feb;72(1):126-134. doi: 10.1007/s43440-019-00038-5. Epub 2019 Dec 20.
Diabetics have a higher risk of developing cerebral vasospasms (CVSPs) than non-diabetics. Current therapies are ineffective in reducing CVSPs, but a a combination of dantrolene and nimodipine may be a viable treatment. Considering the potentially harmful secondary effects of dantrolene, however, we evaluated the efficacy of 10 μM dantrolene compared to 50 μM dantrolene alone or in combination with 50 nM nimodipine.
Dose-response curves for the phenylephrine (PHE)-induced contraction and acetylcholine (ACh)-induced relaxation were performed on aortic rings from diabetic and non-diabetic rats, before and after a 30-min incubation period with dantrolene (50 μM and 10 μM), alone or in combination with 50 nM nimodipine.
Whereas 50 μM dantrolene reduced PHE-induced contraction by 47% in diabetic rats and 29% in controls, 10 μM dantrolene failed to reduce this parameter in either group. Furthermore, 50 μM dantrolene reduced PHE-induced contraction by about 80% in both diabetic and controls when combined with nimodipine (N = 9, P < 0.05). The combination of 10 μM dantrolene and 50 nM nimodipine, however, was ineffective. Only 50 μM dantrolene improved endothelial dysfunction.
Improved endothelial-dependent relaxation and reduced vascular contractility with dantrolene are dose dependent. Thus, although dantrolene appears to be a promising alternative for the treatment of CVSPs when added to conventional therapies, careful titration should be performed to achieve a significant reduction in vascular hyperreactivity. Moreover, if our findings with rats are applicable to humans, the combined use of dantrolene and nimodipine at optimal doses may reduce CVSPs, especially in the diabetic population.
糖尿病患者发生脑血管痉挛(CVSP)的风险高于非糖尿病患者。目前的治疗方法无法有效降低 CVSP,但联合应用丹曲林钠和尼莫地平可能是一种可行的治疗方法。然而,考虑到丹曲林钠可能产生有害的副作用,我们评估了 10μM 丹曲林钠与单独使用 50μM 丹曲林钠或联合使用 50nM 尼莫地平相比的疗效。
在糖尿病和非糖尿病大鼠的主动脉环上进行了苯肾上腺素(PHE)诱导收缩和乙酰胆碱(ACh)诱导舒张的剂量反应曲线,在单独使用 50μM 和 10μM 丹曲林钠或联合使用 50nM 尼莫地平 30 分钟孵育期前后进行了这些实验。
50μM 丹曲林钠使糖尿病大鼠的 PHE 诱导收缩减少了 47%,对照组减少了 29%,而 10μM 丹曲林钠未能使两组的这一参数减少。此外,50μM 丹曲林钠与尼莫地平联合使用时,使糖尿病和对照组大鼠的 PHE 诱导收缩减少了约 80%(N=9,P<0.05)。然而,10μM 丹曲林钠与 50nM 尼莫地平联合使用时无效。只有 50μM 丹曲林钠改善了内皮功能障碍。
丹曲林钠对血管收缩性和内皮依赖性舒张的改善作用与剂量有关。因此,尽管丹曲林钠似乎是在常规治疗基础上加用的治疗 CVSP 的一种有前途的替代方法,但应仔细滴定以显著降低血管高反应性。此外,如果我们在大鼠身上的发现适用于人类,那么以最佳剂量联合使用丹曲林钠和尼莫地平可能会降低 CVSP,尤其是在糖尿病患者中。