Lim Ji-Hey, Muguet-Chanoit Audrey C, Smith Daniel T, Laber Eric, Olby Natasha J
Department of Clinical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, North Carolina, United States of America; Center for Comparative Medicine and Translational Research, North Carolina State University, Raleigh, North Carolina, United States of America.
Department of Clinical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, North Carolina, United States of America.
PLoS One. 2014 Dec 31;9(12):e116139. doi: 10.1371/journal.pone.0116139. eCollection 2014.
4-Aminopyridine (4-AP) blocks voltage gated potassium channels, restoring conduction to demyelinated axons and improving function in demyelinating conditions, but its use is associated with adverse effects and benefit in spinal cord injury is limited. Derivatives of 4-AP have been developed to improve clinical efficacy while reducing toxicity. We compared the therapeutic effects of orally administered 4-AP and its t-butyl carbamate derivative (t-butyl) with placebo in dogs that had suffered an acute spinal cord injury that left them chronically paralyzed. Nineteen dogs were entered into the trial, conducted in two-week treatment blocks starting with placebo, followed by random assignment to 4-AP or t-butyl, a washout and then the opposite medication followed by placebo. Investigators and owners were blinded to treatment group. Primary outcome measures included open field gait score (OFS), and treadmill based stepping score and regularity index, with additional secondary measures also considered. Thirteen of 19 dogs completed the protocol. Two were euthanized due to unrelated heath problems, two developed side effects and two were unable to complete for unrelated reasons. Dogs showed significant improvement in supported stepping score (from 17.39 to 37.24% with 4-AP; 16.85 to 29.18% with t-butyl p<0.0001) and OFS (from 3.63 to 4.73 with 4-AP; 3.78 to 4.45 with t-butyl, p = 0.005). Response was individually variable and most dramatic in three dogs that were able to walk without support with treatment. No significant difference was found between 4-AP and t-butyl. No adverse effects were reported with t-butyl but gastrointestinal upset and seizures were observed in two dogs with 4-AP. In conclusion, both 4-AP and t-butyl significantly improved supported stepping ability in dogs with chronic spinal cord injury with no adverse effects noted with t-butyl. Drug response varied widely between individuals, highlighting the need to understand the factors that influence canine and human patients' response to therapy.
4-氨基吡啶(4-AP)可阻断电压门控钾通道,恢复脱髓鞘轴突的传导并改善脱髓鞘疾病中的功能,但它的使用会带来不良反应,且对脊髓损伤的益处有限。已开发出4-AP的衍生物以提高临床疗效并降低毒性。我们在遭受急性脊髓损伤并导致长期瘫痪的犬中,比较了口服4-AP及其氨基甲酸叔丁酯衍生物(叔丁基)与安慰剂的治疗效果。19只犬进入试验,试验以两周的治疗周期进行,从安慰剂开始,然后随机分配至4-AP或叔丁基组,经过洗脱期后再给予相反的药物,最后再给予安慰剂。研究者和犬主对治疗组情况不知情。主要结局指标包括旷场步态评分(OFS)、基于跑步机的步幅评分和规律性指数,同时也考虑了其他次要指标。19只犬中有13只完成了试验方案。2只因无关健康问题实施安乐死,2只出现副作用,2只因无关原因未能完成试验。犬的辅助步幅评分(4-AP组从17.39%提高到37.24%;叔丁基组从16.85%提高到29.18%,p<0.0001)和OFS(4-AP组从3.63提高到4.73;叔丁基组从3.78提高到4.45,p = 0.005)有显著改善。反应存在个体差异,在3只经治疗后能够独立行走的犬中最为显著。4-AP和叔丁基之间未发现显著差异。叔丁基组未报告不良反应,但4-AP组有2只犬出现胃肠道不适和癫痫发作。总之,4-AP和叔丁基均显著改善了慢性脊髓损伤犬的辅助步幅能力,且叔丁基未出现不良反应。个体间药物反应差异很大,这突出表明有必要了解影响犬类和人类患者对治疗反应的因素。