预约演示
更新于：2025-08-27
Tizanidine Hydrochloride
盐酸替扎尼定
更新于：2025-08-27
概要
基本信息
简介盐酸替扎尼定是一种小分子药物，作用于ADRA2，是ADRA2激动剂。它的适应症包括多发性硬化、肌肉痉挛、瘫痪和肌强直症。盐酸替扎尼定最初由诺华制药公司研发，并于1988年1月20日获得首次批准。该药物通过作用于中枢神经系统，降低神经肌肉传递的敏感性，从而减轻肌肉痉挛和紧张。此外，它还可以改善运动协调和减轻疼痛等症状。虽然盐酸替扎尼定可以缓解症状，但也存在一些不良反应，如头晕、口干、疲劳等，需要在医生的指导下使用。总体而言，盐酸替扎尼定是一种有效的治疗肌肉痉挛和相关症状的药物。 |
药物类型 小分子化药 |
别名 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole、Tizanidine、Tizanidine hydrochloride (JP17/USP) + [20] |
靶点 |
作用方式 激动剂 |
作用机制 ADRA2激动剂(肾上腺素能受体α-2家族激动剂) |
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C9H9Cl2N5S |
InChIKeyZWUKMNZJRDGCTQ-UHFFFAOYSA-N |
CAS号64461-82-1 |
关联
82
项与 盐酸替扎尼定 相关的临床试验NCT07022353
Ultrasound-guided Bi-level Erector Spinae Plane Block and Pre-emptive Single-dose Oral Tizanidine for Postoperative Analgesia After Mastectomy Surgery: a Prospective, Randomized, Controlled Trial
CTR20252033
健康受试者空腹单次口服盐酸替扎尼定片的随机、开放、两序列、两制剂、两周期、交叉设计的生物等效性试验
CTR20252032
健康受试者餐后单次口服盐酸替扎尼定片的随机、开放、两序列、两制剂、四周期、完全重复交叉设计的生物等效性试验
100 项与 盐酸替扎尼定 相关的临床结果
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100 项与 盐酸替扎尼定 相关的转化医学
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100 项与 盐酸替扎尼定 相关的专利（医药）
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927
项与 盐酸替扎尼定 相关的文献（医药）2025-08-12JOURNAL OF ARTHROPLASTY
Efficacy of Muscle Relaxants on a Multimodal Analgesic Regimen in Total Knee Arthroplasty: A Prospective, Double-Blind, Placebo-Controlled, Randomized Trial.
Article
作者: Wang, Duan ; Zhou, Zongke ; Zhao, Long ; Zhu, Xiaoyan
BACKGROUND:
Postoperative muscle spasms markedly contribute to acute pain and restricted joint mobility after primary total knee arthroplasty (TKA). This study aimed to evaluate the efficacy of adding muscle relaxants as an adjunctive therapy in multimodal analgesic protocols for post-TKA pain management.
METHODS:
In this randomized trial with a 30-day follow-up, 120 patients undergoing TKA were assigned to receive either tizanidine (two mg three times daily for 14 days, starting on the first postoperative day) or placebo. The tizanidine group (n = 58) and placebo group (n = 56) had comparable baseline characteristics and surgical details (P > 0.05). Primary outcome was postoperative pain intensity, measured using the visual analog scale (VAS). Secondary outcomes included knee range of motion (ROM), Hospital for Special Surgery (HSS) score, morphine consumption during hospitalization, serum levels of inflammatory biomarkers (C-reactive protein and interleukin-6), and complications.
RESULTS:
Tizanidine significantly reduced VAS pain scores during ambulation on postoperative days three (mean difference: -1.56, P < 0.001), seven (mean difference: -2.40, P < 0.001), and 14 (mean difference: -1.47, P < 0.001), decreased the morphine prescription rate (24.1 versus 42.9%, P = 0.034), and improved knee ROM on day three (mean difference: 8.7°, P = 0.012) and day seven (mean difference: 6.7°, P = 0.038). Transient somnolence was significantly more frequent in the tizanidine group (20.7 versus 3.6%, P = 0.015). There were no significant intergroup differences observed in inflammatory biomarkers, resting pain scores, or HSS scores.
CONCLUSION:
Adding tizanidine to multimodal analgesia protocols provided clinically meaningful postoperative pain relief during ambulation, reduced the morphine prescription rate, and enhanced knee ROM recovery. These results may offer important implications for optimizing postoperative pain management strategies and inform future clinical practice guidelines for TKA recovery protocols.
2025-07-03Expert Opinion On Drug Safety
Evaluating potential unexpected adverse events and mortality after oral analgesics administration in fracture care-a cohort study
Article
作者: Ahmad, Tashfeen ; Muhammad, Zehra Abdul ; Rashid, Haroon
INTRODUCTION:
Analgesic selection per individual's tolerance is essential to avoid risks. The study evaluated current oral analgesic prescription practice, analgesic adverse effects-related factors, unexpected events, and mortality post-fracture surgery.
RESEARCH DESIGN AND METHODS:
The present prospective cohort study from June 2022 to July 2023 enrolled a total of 198 proximal femoral, ankle, and hindfoot trauma fracture patients. Stratification was done for oral analgesics prescribed at hospital discharge and 1 week with their accompanying toxicity assessed for 2 weeks. Analyzed Kaplan-Meier curve and the absolute risk for possible analgesics-related deaths.
RESULTS:
Following oral analgesic administration, 122 (62%) patients experienced adverse events. In seven expiries, five were possibly due to acetaminophen added tramadol combined with any of pregabalin, diclofenac, etoricoxib, or gabapentin (absolute risk 2.5%, 97.5% proportion 2 weeks survival). Three (2% of 122) patients taking acetaminophen added tramadol or diclofenac experienced unexpected serious adverse events. Elderly diabetic and hypertensive hip fracture patients expired or experienced unexpected events.
CONCLUSION:
Data suggest that oral acetaminophen added tramadol combined with any of pregabalin, diclofenac, etoricoxib, or gabapentin might increase the death risk or unexpected serious adverse events in elderly diabetic and hypertensives suffering from intertrochanteric/femoral neck fracture. Safe analgesic selection is necessitated for at-risk patients.
2025-07-01Drug Delivery and Translational Research
Intranasal trimethyl chitosan-coated emulsomes containing tizanidine as brain-targeted therapy in spasticity: formulation, optimization, and pharmacokinetic assessment
Article
作者: Ali, Adel A ; Elkomy, Mohammed H ; Aldosari, Basmah Nasser ; Zaki, Randa Mohammed ; Hendawy, Omnia M ; Tulbah, Alaa S ; Eid, Hussein M
Tizanidine HCl (TZN) is an FDA-approved medication for treating spasticity. However, its oral administration presents obstacles to its efficacy, as it has a short duration of action and a low rate of absorption into the circulation (less than 40%) due to its rapid breakdown in the liver. In addition, its hydrophilic properties limit its capacity to cross the blood-brain barrier, thereby prohibiting it from reaching the central nervous system, where it can exert its intended therapeutic effects. Furthermore, diet-dependent absorption leads to fluctuations in bioavailability. Thus, this work aimed to create TZN-loaded chitosan-coated emulsomes (TZN-CTS-EMS) for intranasal administration, bypassing hepatic metabolism and boosting brain bioavailability. TZN-CTS-EMS were made using a thin film hydration approach. The influence of the independent parameters on the vesicle characteristics was examined and optimized using a Box-Behnken experimental methodology. The optimized formulation expected by the experimental design exhibited a greater desirability factor, characterized by a smaller particle size (127.63 nm), higher encapsulation efficiency (67.36%), and higher zeta potential (32.49 mV). As a result, it was chosen for additional in vivo assessment. Histopathological examinations showed no structural injury or toxicity to the nasal mucosa. Compared to intranasal TZN solution (TZN-SOL), the pharmacokinetics analysis demonstrated that intranasal TZN-CTS-EMS had a relative bioavailability of 191.9% in the plasma and 459.3% in the brain. According to these findings, intranasal administration of the optimized TZN-CTS-EMS may represent a viable, noninvasive substitute for effective TZN delivery to brain tissues, potentially leading to improved safety and pharmacological efficiency.
100 项与 盐酸替扎尼定 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 偏头痛 | 中国 | 2025-06-30 | |
| 痉挛 | 美国 | 2024-12-12 | |
| 多发性硬化症 | 日本 | 1996-03-05 | |
| 肌肉痉挛 | 日本 | 1996-03-05 | |
| 肌张力障碍 | 日本 | 1988-04-18 | |
| 麻痹 | 日本 | 1988-04-18 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 先兆偏头痛 | 临床3期 | 中国 | 2023-06-01 | |
| 无先兆偏头痛 | 临床3期 | 中国 | 2023-06-01 | |
| 脊髓损伤 | 临床3期 | 美国 | 2002-06-01 | |
| 脑卒中 | 临床3期 | 美国 | 2002-06-01 | |
| 急性腰痛 | 临床2期 | - | 2016-11-01 | |
| 肌痛 | 临床2期 | - | 2016-11-01 | |
| 创伤性脑损伤 | 临床1期 | 以色列 | 2006-12-01 | |
| 肌强直 | 临床申请批准 | 中国 | 2022-09-01 | |
| 肌张力亢进 | 药物发现 | 美国 | 2021-11-16 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 320 | (Metaxalone) | 廠鹽積遞範獵積範襯廠(齋範鬱鑰鏇淵製鏇鏇餘) = 糧鬱鹹觸醖鹹選壓夢鑰 衊願顧鏇製餘選選積齋 (憲夢鹽範遞鬱觸觸淵餘, 襯糧鏇鑰繭簾憲糧範獵 ~ 衊網衊壓壓壓廠壓願構) 更多 | - | 2020-08-12 | ||
(Tizanidine) | 廠鹽積遞範獵積範襯廠(齋範鬱鑰鏇淵製鏇鏇餘) = 繭願壓遞憲積淵夢窪構 衊願顧鏇製餘選選積齋 (憲夢鹽範遞鬱觸觸淵餘, 艱範簾獵壓膚醖築積製 ~ 範壓餘積鑰憲窪鬱糧獵) 更多 |
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