预约演示
更新于：2025-07-25
Tizanidine Hydrochloride
盐酸替扎尼定
更新于：2025-07-25
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) |
登录后查看时间轴
结构/序列
分子式C9H9Cl2N5S |
InChIKeyZWUKMNZJRDGCTQ-UHFFFAOYSA-N |
CAS号64461-82-1 |
关联
80
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
登录后查看更多信息
100 项与 盐酸替扎尼定 相关的转化医学
登录后查看更多信息
100 项与 盐酸替扎尼定 相关的专利（医药）
登录后查看更多信息
1,137
项与 盐酸替扎尼定 相关的文献（医药）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.
2025-06-18Sudebno-meditsinskaia ekspertiza
Development of conditions for determination of imidazole derivatives in the blood using chromatography-mass spectrometry
Article
作者: Vasilenko, A.V. ; Krylova, E.A. ; Kataev, S.S. ; Dvorskaya, O.N.
The problem of clonidine, moxonidine, tizanidine determination in forensic studies of biological objects remains due to low therapeutic and toxic concentrations in biological material, that creates certain difficulties in detecting the use of these substances. The study objective is to develop chromato-mass-spectrometry conditions for imidazole derivatives determination in the blood for purposes of forensic chemical and chemical toxicological analysis. The conditions for reliable clonidine, moxonidine, tizanidine identification in the blood using solid-phase extraction and gas chromatography with mass-spectrometry detection are selected. Gas chromatographic and mass spectrometric characteristics of clonidine, moxonidine, tizanidine derivatives which can be used for the purposes of forensic chemical and chemical toxicological analysis were studied.
100 项与 盐酸替扎尼定 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | 壓鹹糧簾夢窪壓範襯網(夢鬱膚簾鑰獵餘蓋顧夢) = Transient elevation in metanephrines was likely related to the withdrawal syndrome. Clinician must be aware of current prescriptions and OTC drugs taken by patients. Prompt recognition is imperative and therapy must be started immediately. 廠鹽製積醖繭願廠範鹽 (廠積膚窪獵夢遞網網觸 ) 更多 | - | 2022-05-15 | |||
临床4期 | 320 | (Metaxalone) | 餘鏇醖襯遞廠鑰醖鏇築(鏇壓範襯構繭鑰憲選積) = 構觸選構鏇淵觸鬱願鑰 憲齋鬱廠襯壓廠膚淵衊 (網醖餘膚夢餘獵簾積簾, 窪鏇艱鏇窪積構繭獵積 ~ 壓觸鹹選蓋蓋糧襯鏇繭) 更多 | - | 2020-08-12 | ||
(Tizanidine) | 餘鏇醖襯遞廠鑰醖鏇築(鏇壓範襯構繭鑰憲選積) = 蓋壓範繭製顧鑰積糧製 憲齋鬱廠襯壓廠膚淵衊 (網醖餘膚夢餘獵簾積簾, 齋壓憲築鹽網夢壓繭獵 ~ 觸艱憲獵衊襯鬱選鹽夢) 更多 | ||||||
N/A | - | Tizanadine | 築獵齋淵壓壓範積簾鹹(觸艱壓顧衊窪築選襯窪) = 窪糧網積醖積淵鹹廠願 蓋繭衊構構鑰齋艱遞簾 (蓋顧壓鹹鹹壓壓鹹襯網 ) 更多 | - | 2010-11-14 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用