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·专 题··脑卒中的治疗·盐酸替扎尼定对于脑卒中后肢体痉挛的疗效及耐受性万绍杰1 王运华2 陈洪国31烟台业达医院药剂科 264000；2烟台业达医院神经外科 264000；3烟台业达医院康复科 264000通信作者：万绍杰，Email：************** 【摘要】 目的 探讨盐酸替扎尼定对于脑卒中后肢体痉挛的疗效及耐受性。
方法 选取2018年1月至2019年1月在本院治疗的脑卒中后上肢痉挛患者92例，根据治疗方案分为观察组（n=47）和对照组（n=45）；对照组给予常规治疗，观察组在对照组基础上加用盐酸替扎尼定；观察两组治疗前后改良的Ashworth痉挛评定量表（MAS）、临床痉挛指数（CSI）、简化Fugl-Meyer运动量表（FMA）评分。
结果 治疗后，观察组MAS评级明显优于对照组，差异有统计学意义（P＜0.05）；治疗后，观察组CSI评分为（5.50±1.01）分，明显低于对照组（7.80±1.12）分，差异有统计学意义（P＜0.05）；治疗后，观察组FMA评分为（30.20±6.11）分，明显高于对照组（25.60±5.50）分，差异有统计学意义（P＜0.05）；观察组不良反应发生率为17.02%，其中有4例患者不能耐受不良反应。
结论 盐酸替扎尼定治疗脑卒中后肢体痉挛有较好的效果，值得临床使用。
【关键词】 盐酸替扎尼定；脑卒中；后肢体痉挛；临床疗效 DOI：10.3760/cma.j.issn.1007-1245.2020.16.018Therapeutic effect and tolerance of tizanidine hydrochloride for spasticity of limbs after strokeWan Shaojie1, Wang Yunhua2, Chen Hongguo31Department of Pharmacy, Yantai Yida Hospital, Yantai 264000, China; 2Department of Neurological Surgery,Yantai Yida Hospital, Yantai 264000, China; 3Department of Rehabilitation Medicine, Yantai Yida Hospital, Yantai264000, ChinaCorrespondingauthor:WanShaojie,Email:************** 【Abstract】Objective To investigate the effect and tolerance of tizanidine hydrochloride in the treatmentof limb spasm after stroke. Methods From January, 2018 to January, 2019, 92 patients with upper extremityspasm after stroke were selected and divided into an observation group (n=47) and a control group (n=45)according to the treatment plans. The control group was routinely treated; in addition, the observation group wastreated with tizanidine hydrochloride. The Modified Ashworth Spasticity Rating Scale (MAS), clinical spasticityindex (CSI), and Simplified Fugl Meyer Exercise Scale (FMA) were observed before and after the treatment.Results The MAS rating was significantly better in the observation group than in the control group (P＜0.05).After the treatment, the CSI score was lower and the FMA score was higher in the observation group than that ofthe control group [(5.50±1.01) vs. (7.80±1.12) and (30.20±6.11) vs. (25.60±5.50); both P＜0.05]. The incidenceof adverse reactions in the observation group was 17.02%; among which 4 patients could not tolerate the adversereactions. Conclusion Tizanidine hydrochloride has a good effect in the treatment of limb spasm after stroke,which is worth being clinically used. 【Key words】 Tizanidine hydrochloride; Stroke; Limb spasm; Clinical effect DOI：10.3760/cma.j.issn.1007-1245.2020.16.0182388 脑卒中后肢体痉挛是缺血性脑血管疾病所致的偏瘫或偏身感觉障碍性后遗症之一，肢体持续高痉挛状态可妨碍肢体功能康复训练，而常规的抗凝、改善微循环、促进脑代谢等药物治疗对肢体痉挛并无直接的改善效果[1]。
1替扎尼定有效治疗肌膜疼痛症候群Tizanidine Is Effective in the Treatment of Myofascial Pain SyndromeGerard A. Malanga, MD, Matthews W. Gwynn, MD, Rachael Smith, DO and Dorothy Miller肌膜疼痛症候群（Myofascial Pain Syndrome ，MPS ）治疗困难。
本试验对替扎尼定，一种在痉挛和疼痛治疗方面有效的α2肾上腺素能药物，在治疗MPS 方面的有效性和安全性进行了评估。
招募患MPS 持续9周至>50周的女性患者（n ＝29），平均年龄为37.5岁（范围：20－51岁），已降低了压痛阈值（pressure threshold ）。
患者用3周时间将服用替扎尼定的剂量逐渐增加到12mg ，并维持剂量2周。
睡眠通过视觉模拟量表（visual analog scale ，V AS ）评估，疼痛强度通过包括基线水平、第3和5周、停用替扎尼定后1周的V AS 、残疾/功能水平、压痛阈值（通过痛觉计测试）的简易McGill 调查问卷表进行评估。
在第5周时，报告患者和医生的治疗总体评价。
24例患者完成了研究。
从基线水平到第3周、第5周和停药后，疼痛强度和残疾明显减少（P <.001）。
在全部研究阶段，压痛阈值和睡眠得到改善（P <.001）。
89％的患者和79％的医生将替扎尼定缓解疼痛分级为“好”到“极好”。
没有严重副作用发生。
替扎尼定治疗MPS 有效。
关键词：替扎尼定，肾上腺素能的，肌膜疼痛症候群Myofascial pain syndrome (MPS) is difficult to treat. The efficacy and safety of tizanidine, an alpha2-adrenergic agent with effects on spasticity and pain, in treating MPS was evaluated. Female subjects (n = 29) with MPS of 9 to > 52 weeks’ duration and mean age 37.5 (range 20–51) years, who also had reduced pressure thresholds, were enrolled. Subjects were titrated up to 12 mg of tizanidine over 3 weeks and maintained for 2 weeks. Sleep was assessed via visual analog scale (VAS), pain intensity via short form McGill questionnaire including VAS, disability/level of function, and pressure threshold (tested by algometry) at baseline, weeks 3 and 5, and 1 week after tizanidine was discontinued. Patient and physician global assessments of treatment were reported at week 5. Twenty-four subjects completed the study. Pain intensity and disability decreased significantly from baseline at weeks 3 and 5 and after washout (P < .001). Pressure threshold and sleep improved for all study periods (P < .001). Tizanidine was rated as good to excellent in relieving pain by 89% of subjects and 79% of physicians. No serious adverse events occurred. Tizanidine was effective in the treatment of MPS.Key words: Tizanidine, adrenergic, myofascial pain syndrome肌膜疼痛症候群（Myofascial Pain Syndrome ，MPS ）是一种普通人群中非常常见的疾病；患病率为12％[1]。
盐酸替扎尼定联合坦度螺酮治疗纤维肌痛综合征临床疗效观察林长艺;吴培埕;徐朝焰【期刊名称】《中国现代医药杂志》【年(卷),期】2016(0)5【摘要】Objective To evaluate the efficacy and safety of tizanidine hydrochloride combined with tandospirone in fi-bromyalgia symdrome(FS). Methods 46 cases up to the stardard of the American College of rheumatology (CAR) FS patients were randomly divided into two groups, group A for tizanidine hydrochloride, group B for tizanidine hydrochloride combined with tandospirone. After 12 weeks of treatment,compared VAS score,FIQ score,HAMA score and HAMD score of two groups. Results VAS score,ADL score, FIQ score,HAMA score and HAMD score of two groups after 12 weeks of treatment were lower than that before treatment, ADL score was higher than that before treatment, the difference was statistically significant (P<0.05). Compared the difference value of VAS score, ADL score, HAMA score, HAMD score, FIQ score of two groups before and after the treatment, the differences were statistically significant (P<0.05). Conclusion Tizanidine hydrochloride com-bined with tandospirone in the treatment of fibromyalgia syndrome can significantly improve the clinical efficacy. There is no se-rious adverse reaction.%目的：探讨盐酸替扎尼定联合坦度螺酮治疗纤维肌痛综合征（FS）的有效性及安全性。
替扎尼定治疗三叉神经痛有效性及安全性评析翟伟奇【摘要】ObjectiveTo analyze the tizanidine treatment efficacy and safety of trigeminal neuralgia.Methods94 patients with trigeminal neuralgia were treated in our hospital from February March to 2012, 47 cases of the observation group and 47 cases in control group were divided into observation group and control group with cases. The observation group were treated with Tizanidine treatment; the control group was treated with C Masi Bing therapy. Comparison and analysis of the two groups of patients with treatment efficacy and safety. Results After different treatment, the observation group of patients 21 cases cured, 14 cases markedly effective, 10 cases effective, 2 cases ineffective, the total effective rate was 95.7% (45/47); the control group of patients with 10 cases, 13 cases were effective, 10 cases ineffective, the total effective rate was 78.7% (37/47); the treatment effect of the observation group was significantly better than the control group (P<0.05), the difference was significant between the two groups.Conclusion Needle for patients with trigeminal neuralgia, in the course of treatment choice use of tizanidine has satisfactory therapeutic effect, and tizanidine was well tolerated.%目的：分析替扎尼定治疗三叉神经痛有效性及安全性。
替扎尼定联合综合康复疗法治疗偏瘫肌痉挛疗效观察作者：尉伟滕以亮刘克岩来源：《中外女性健康研究》2015年第07期【摘要】目的：观察替扎尼定结合综合康复疗法治疗脑卒中后偏瘫肌痉挛的疗效。
方法：将60例脑卒中所致偏瘫合并偏瘫侧肢体痉挛（Ashoworth分级≥1级）患者随机分为治疗组和对照组，每组各30例。
对照组仅应用综合康复治疗。
治疗组在综合康复治疗的同时口服替扎尼定，替扎尼定为开始剂量每次2mg，2次/日，以后逐渐加量直至增加到最佳有效剂量并维持，采用改良的Ashworth分级法和Barthel氏ADL（日常生活活动评定量表）指数评定法，对两组患者治疗前后肌张力及ADL能力进行评定。
结果：治疗后，两组患者肌张力较治疗前均有明显降低（P【关键词】卒中；肌痉挛；替扎尼定；康复疗法脑血管病所致的肢体瘫痪，如果早期未进行康复治疗，大部分患者会出现瘫痪肢体肌张力增高或痉挛，严重影响了肢体功能的恢复，直接影响患者的生活质量，其中偏瘫对日常生活的影响尤为严重。
这类功能障碍的康复是一个综合的、整体的治疗过程，除康复治疗外，药物治疗也是一种积极有效的治疗方法。
盐酸替扎尼定（凯莱通）是一种咪唑啉间二氮杂环戊烯衍生物，作用于脑和脊髓的α2受体，通过减少脊髓兴奋性神经递质的释放和降低这些兴奋性神经递质对其受体的作用而减少脊髓α和γ运动神经原的兴奋性。
国外研究证实，替扎尼定对于脑损伤后痉挛具有较好的疗效[1]。
但国内尚未有相关的研究，本文对患者进行了替扎尼定联合综合康复疗法治疗偏瘫肌痉挛的疗效观察。
1 资料与方法1.1 病例选择60例患者均为2010年7月至2012年7月在我院住院治疗的伴有肌痉挛的脑血管病的患者（Ashoworth分级≥1级），除外有意识障碍、失语症、严重的认知障碍等。
年龄42～68岁（平均55±5.4岁），男36例，女24例，病程2～6个月（平均4个月）。
病种有脑出血18例，脑梗塞42例，病变部位经CT或MRI检查，基底节36例，脑叶15例，脑干6例，丘脑3例。
替扎尼定在治疗痉挛方面的研究进展替扎尼定是一种中枢镇痉药，常用于治疗各种类型的痉挛，例如帕金森综合症、多发性硬化、脑损伤、肌张力障碍、白色痴呆症等等。
随着科技的不断进步，替扎尼定在治疗痉挛方面的研究也得以不断深入，本文将对替扎尼定的治疗机制、副作用以及研究进展等方面进行探讨。
一、替扎尼定的治疗机制替扎尼定是一种GABA_A受体正向调节剂，也就是说，它通过增强GABA_A受体的作用来抑制中枢神经系统的兴奋性，从而达到镇静、抗惊厥、抗癫痫和镇痉的效果。
研究表明，替扎尼定主要通过增强中枢GABA能系统的抑制作用来发挥镇痉作用。
具体来说，替扎尼定可增强GABA_A受体的Cl-通道活性，从而增加GABA的抑制性作用，抑制中枢神经元的兴奋性，从而达到镇痉的效果。
此外，替扎尼定还能降低中枢神经系统的谷氨酸水平，从而进一步抑制神经元的兴奋性。
二、替扎尼定的副作用虽然替扎尼定具有较好的镇痉作用，但它也有一系列的副作用，例如头晕、嗜睡、注意力不集中、情绪波动、失眠、恶心、便秘、视幻觉等等。
其中，嗜睡是替扎尼定使用中最常见的副作用之一，大约有30％的患者会出现嗜睡现象。
此外，长期应用替扎尼定还可能导致依赖性和耐受性，甚至出现药物滥用和戒断症状等问题。
三、替扎尼定在治疗痉挛方面的研究进展随着对替扎尼定的进一步研究，人们也在探索它在治疗痉挛方面的新途径和新方法。
下面将分别从以下几个方面进行阐述：1. 替扎尼定的药代动力学替扎尼定的药代动力学主要包括吸收、分布、代谢和排泄等过程。
研究表明，替扎尼定的口服生物利用度很低，只有25％左右，而且受食物的影响较大。
因此，口服替扎尼定尤其是与高脂食物一起服用时需要注意。
此外，替扎尼定主要由CYP3A4代谢，因此与CYP3A4抑制剂和诱导剂合用时需要密切监测。
2. 替扎尼定在癫痫治疗中的应用替扎尼定在癫痫治疗方面也有一定的应用价值。
研究表明，替扎尼定可以有效地控制部分性和全面性癫痫，且不良反应较小。
