A randomized double blind placebo controlled multicenterstudy to assess the efficacy and tolerability of tolperisone as add ontreatment with standardized NSAID of acute non specific low back pain.

开始日期2022-03-28

申办/合作机构-

NCT04671082 / Completed临床3期

A Phase 3, 14-Day, Double-blind, Randomized, Placebo-Controlled, Multicenter Study of the Efficacy and Safety of Tolperisone in Subjects With Pain Due to Acute Back Muscle Spasm

This is a double-blind, randomized, placebo-controlled, multicenter study of the efficacy and safety of tolperisone (a non-opioid) or placebo administered in subjects with pain due to acute back muscle spasm.

开始日期2020-12-15

申办/合作机构

Neurana Pharmaceuticals, Inc.

NCT04465266 / Completed临床1期

A Phase 1 Crossover Study of Single and Multiple Dose Pharmacokinetics, and Dose Linearity, of Tolperisone in Healthy Subjects

This is a randomized, single-blind, single and multiple dose crossover subjects in healthy adult subjects

开始日期2020-07-28

申办/合作机构

Neurana Pharmaceuticals, Inc.

100 项与盐酸托哌酮相关的临床结果

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100 项与盐酸托哌酮相关的转化医学

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100 项与盐酸托哌酮相关的专利（医药）

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186

项与盐酸托哌酮相关的文献（医药）

2023-08-07·Pharmaceuticals (Basel, Switzerland)

Pregabalin-Tolperisone Combination to Treat Neuropathic Pain: Improved Analgesia and Reduced Side Effects in Rats.

Article

作者: Laufer, Rudolf ; Tábi, Tamás ; Abbood, Sarah Kadhim ; Király, Kornél ; Zádori, Zoltán S ; Geda, Orsolya ; Szökő, Éva ; Riba, Pál ; Essmat, Nariman ; Al-Khrasani, Mahmoud ; Mohammadzadeh, Amir ; Lakatos, Péter P ; Galambos, Anna Rita ; Karádi, Dávid Árpád

The current treatment of neuropathic pain (NP) is unsatisfactory; therefore, effective novel agents or combination-based analgesic therapies are needed. Herein, oral tolperisone, pregabalin, and duloxetine were tested for their antinociceptive effect against rat partial sciatic nerve ligation (pSNL)-induced tactile allodynia described by a decrease in the paw withdrawal threshold (PWT) measured by a dynamic plantar aesthesiometer. On day 7 after the operation, PWTs were assessed at 60, 120, and 180 min post-treatment. Chronic treatment was continued for 2 weeks, and again, PWTs were measured on day 14 and 21. None of the test compounds produced an acute antiallodynic effect. In contrast, after chronic treatment, tolperisone and pregabalin alleviated allodynia. In other experiments, on day 14, the acute antiallodynic effect of the tolperisone/pregabalin or duloxetine combination was measured. As a novel finding, a single dose of the tolperisone/pregabalin combination could remarkably alleviate allodynia acutely. It also restored the neuropathy-induced elevated CSF glutamate content. Furthermore, the combination is devoid of adverse effects related to motor and gastrointestinal transit functions. Tolperisone and pregabalin target voltage-gated sodium and calcium channels, respectively. The dual blockade effect of the combination might explain its advantageous acute analgesic effect in the present work.

2023-08-01·Archives of pharmacal research

Effects of CYP2D6 and CYP2C19 genetic polymorphisms and cigarette smoking on the pharmacokinetics of tolperisone.

Article

作者: Byeon, Ji-Young ; Cho, Chang-Keun ; Jang, Choon-Gon ; Kim, Se-Hyung ; Kang, Pureum ; Lee, Seok-Yong ; Lee, Yun Jeong

Tolperisone, a muscle relaxant used for post-stroke spasticity, is metabolized to its main metabolite by CYP2D6 and to a lesser extent by CYP2C19 and CYP1A2. We investigated the effects of CYP2D6 and CYP2C19 genetic polymorphisms and cigarette smoking on tolperisone pharmacokinetics. A 150 mg oral dose of tolperisone was given to 184 healthy Korean subjects and plasma concentrations of tolperisone were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). A 3.14-fold significant increase in AUC_0-∞ was observed in the CYP2D6*10/*10 group compared with the CYP2D6*wt/*wt group, whereas a 3.59-fold increase in AUC_0-∞ was observed in CYP2C19PMs compared to CYP2C19EMs. Smokers had a 38.5% decrease in AUC_0-∞ when compared to non-smokers. When these effects were combined, CYP2D6*10/*10-CYP2C19PM-Non-smokers had a 25.9-fold increase in AUC_0-∞ compared to CYP2D6*wt/*wt-CYP2C19EM-Smokers. Genetic polymorphisms of CYP2D6 and CYP2C19 and cigarette smoking independently and significantly affected tolperisone pharmacokinetics and these effects combined resulted in a much greater impact on tolperisone pharmacokinetics.

2023-02-01·Archives of pharmacal research

Effects of CYP2C19 genetic polymorphism on the pharmacokinetics of tolperisone in healthy subjects

Article

作者: Jang, Choon-Gon ; Byeon, Ji-Young ; Cho, Chang-Keun ; Ko, Eunvin ; Kang, Pureum ; Mu, Chou Yen ; Lee, Yun Jeong ; Park, Hye-Jung ; Lee, Seok-Yong

Tolperisone hydrochloride is a centrally-acting muscle relaxant used for relieving spasticities of neurological origin and muscle spasms associated with painful locomotor diseases. It is metabolized to the inactive metabolite mainly by CYP2D6 and, to a lesser extent, by CYP2C19 and CYP1A2. In our previous study, the pharmacokinetics of tolperisone was significantly affected by the genetic polymorphism of CYP2D6, but the wide interindividual variation of tolperisone pharmacokinetics was not explained by genetic polymorphism of CYP2D6 alone. Thus, we studied the effects of CYP2C19 genetic polymorphism on tolperisone pharmacokinetics. Eighty-one subjects with different CYP2C19 genotypes received a single oral dose of 150 mg tolperisone with 240 mL of water, and blood samples were collected up to 12 h after dosing. The plasma concentration of tolperisone was measured by a liquid chromatography-tandem mass spectrometry system. The CYP2C19PM group had significantly higher C_max and lower CL/F values than the CYP2C19EM and CYP2C19IM groups. The AUC_inf of the CYP2C19PM group was 2.86-fold and 3.00-fold higher than the CYP2C19EM and CYP2C19IM groups, respectively. In conclusion, the genetic polymorphism of CYP2C19 significantly affected tolperisone pharmacokinetics.

项与盐酸托哌酮相关的新闻（医药）

2023-09-27

·蒲公英Ouryao

中西复方制剂、变更API供应商该怎办？

作者 | 疯子的邂逅来源 | 蒲公英ouryao问:中药品种，原料中包含化学成分、在变更原料药供应商时怎么办？近日，有蒲友反馈，公司有一个中药品种为脑络通胶囊，制剂所用原料为单身细粉（中药提取物）、盐酸托哌酮（API）、甲基橙皮苷（API）、维生素B6（API），现在计划变更盐酸托哌酮（API）、甲基橙皮苷（API）供应商，关于此项变更是属于中等变更、还是微小变更，企业内部意见不一致，出现争峙，主要争议点如下：1、质量管理部：属于中等变更，理由如下：按照《已上市化学药品药学变更研究技术指导原则》（试行）第六项：变更制剂所用的原料药供应商，变更后的原料药为已获批准的原料药按照中等变更管理；《已上市中药药学变更研究技术指导原则》（试行）中有提到，中西复方制剂及中药注射剂的变更研究应充分考虑药品特点、制剂要求，全面关注变更对药品安全性、有效行和质量可控性的影响，并参照相关技术指导原则、技术要求开展相关研究工作，这里边推到的相关技术指导原则就是《已上市化学药品药学变更研究技术指导原则》（试行）。2、研发部：属于中等变更，理由如下：按照变更就高不就低的原则，指导原则尚没有明确说明的情况下应该参照更高的管理制度执行。3、技术部：属于微小变更，理由如下：《已上市化学药品药学变更研究技术指导原则》（试行）适用范围为化学原料药和化学制剂，脑络通胶囊为中药品种，批准文号为Z大头，不因按照此指导原则开展工作。4、生产部：属于微小变更，理由如下：按照《已上市化学药品药学变更研究技术指导原则》（试行）的要求，变更原料药供应商制剂企业应进行质量对比研究、溶出曲线研究，必要时还需要考虑生物等效性研究等，这对于中药品种来说无法实现，虽然《已上市中药药学变更研究技术指导原则》（试行）中没提及此种变更，但是可以按照变更中药材供应商的制度执行。蒲友点评：1、确实这种变更是一个特例，实际工作中很少遇到，统一质量部门的意见；2、最终评价变更等级的权利不是在质量手里吗，还讨论什么，直接按死；3、折中下，及时按照微小变更去评价，实际做的工作还是应该按照《已上市化学药品药学变更研究技术指导原则》（试行）里边的要求去开展，把能做的都做了，这样即使后期监管部门提出质疑也好补救，要不然就麻烦了；4、直接问药监局不就OK了吗，这么纠结干嘛，制定告诉你就高不就低；5、3楼的意见算是质量妥协的底线了，如果3楼是搞质量的，那你可就危险了啊，常在河边走哪有不湿鞋啊；关于这个话题，你认为应该是什么等级变更，欢迎留言讨论

核酸药物

2023-03-27

·drugs

Comparative Effectiveness of Meds for Acute Low Back Pain Unclear

MONDAY, March 27, 2023 -- For patients with acute low back pain , the comparative effectiveness and safety of analgesic medications is unclear, according to a systematic review and meta-analysis published online March 22 in The BMJ . Michael A. Wewege, from the University of New South Wales in Sydney, and colleagues conducted a systematic review and network meta-analysis to assess the comparative effectiveness and safety of analgesic medicines for acute nonspecific low back pain. Data were reviewed from 98 randomized controlled trials (15,134 participants), which included 69 medicines and combinations. The researchers observed low or very low confidence in evidence for reduced pain intensity after treatment with tolperisone, aceclofenac plus tizanidine, pregabalin (mean differences, −26.1, −26.1, and −24.7, respectively), and 14 other medicines versus placebo. There was low or very low confidence seen for no difference between the effects of several of these medications. There was moderate to very low confidence noted for increased adverse events with tramadol, acetaminophen plus sustained-release tramadol, baclofen, and acetaminophen plus tramadol compared with placebo (risk ratio, 2.6, 2.4, 2.3, and 2.1, respectively). There was moderate-to-low confidence for these medicines increasing the risk for adverse events compared with other medicines. For secondary outcomes and a secondary analysis of medicine classes, moderate-to-low confidence was also noted. "Despite nearly 60 years of research involving more than 15,000 patients, high quality evidence to guide clinical decisions on analgesic medicines for acute nonspecific low back pain remains limited," the authors write. The Sydney Pharmacy School receives funding from GlaxoSmithKline for a postgraduate scholarship supporting a research student supervised by one of the authors. Abstract/Full Text Posted March 2023

临床结果

2022-09-28

·蒲公英Ouryao

药典委：羟苯磺酸钙、盐酸托哌酮等6个标准草案公示

来源：药典委整理：wangxinglai20042022年09月28日，国家药典委发布了6则标准公示通知，涉及品种分别为白蜂蜡、卡维地洛、盐酸艾司洛尔、羟苯磺酸钙、齐墩果酸和盐酸托哌酮，公示期同为1个月。01白蜂蜡我委拟修订白蜂蜡药用辅料标准，为确保标准的科学性、合理性和适用性，现将拟修订的药用辅料标准第二次公示征求社会各界意见（详见附件）。公示期自发布之日起1个月。请认真研核，若有异议，请及时来函提交反馈意见，并附相关说明、实验数据和联系方式。相关单位来函需加盖公章，个人来函需本人签名，同时将电子版发送至指定邮箱。02 卡维地洛我委拟修订卡维地洛国家药品标准，标准编号：《中国药典》2020年版二部。为确保标准的科学性、合理性和适用性，现将拟修订的卡维地洛国家药品标准公示征求社会各界意见（详见附件）。公示期自发布之日起1个月。请认真研核，若有异议，请及时来函提交反馈意见，并附相关说明、实验数据和联系方式。相关单位来函需加盖公章，个人来函需本人签名，同时将电子版发送至指定邮箱。03 盐酸艾司洛尔我委拟修订盐酸艾司洛尔国家药品标准，标准编号：《中国药典》2020年版二部。为确保标准的科学性、合理性和适用性，现将拟修订的盐酸艾司洛尔国家药品标准公示征求社会各界意见（详见附件）。公示期自发布之日起1个月。请认真研核，若有异议，请及时来函提交反馈意见，并附相关说明、实验数据和联系方式。相关单位来函需加盖公章，个人来函需本人签名，同时将电子版发送至指定邮箱。04 羟苯磺酸钙我委拟修订羟苯磺酸钙国家药品标准，标准编号：《中国药典》2020年版二部。为确保标准的科学性、合理性和适用性，现将拟修订的羟苯磺酸钙国家药品标准公示征求社会各界意见（详见附件）。公示期自发布之日起1个月。请认真研核，若有异议，请及时来函提交反馈意见，并附相关说明、实验数据和联系方式。相关单位来函需加盖公章，个人来函需本人签名，同时将电子版发送至指定邮箱。05 齐墩果酸委拟修订齐墩果酸国家药品标准，标准编号：部颁（二部）第三册。为确保标准的科学性、合理性和适用性，现将拟修订的齐墩果酸国家药品标准公示征求社会各界意见（详见附件）。公示期自发布之日起1个月。请认真研核，若有异议，请及时来函提交反馈意见，并附相关说明、实验数据和联系方式。相关单位来函需加盖公章，个人来函需本人签名，同时将电子版发送至指定邮箱。06 盐酸托哌酮我委拟修订盐酸托哌酮国家药品标准，标准编号：WS-10001-(HD-1072)-2002。为确保标准的科学性、合理性和适用性，现将拟修订的盐酸托哌酮国家药品标准公示征求社会各界意见（详见附件）。公示期自发布之日起1个月。请认真研核，若有异议，请及时来函提交反馈意见，并附相关说明、实验数据和联系方式。相关单位来函需加盖公章，个人来函需本人签名，同时将电子版发送至指定邮箱。联系人：周怡、郭伟电话：010-67079556,010-67079558电子邮箱：zhouyi@chp.org.cn通信地址：北京市东城区法华南里11号楼国家药典委员会办公室邮编：100061

100 项与盐酸托哌酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01507	盐酸托哌酮	M02AX06 M03BX04	DB06264

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
心血管疾病	中国	南京白敬宇制药有限责任公司	1986-01-01
肌肉痉挛	瑞士	Labatec Pharma SA	1966-08-24

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
脊髓损伤	临床2期	美国	Avigen, Inc.	2007-09-01
脊髓损伤	临床2期	加拿大	Avigen, Inc.	2007-09-01
痉挛	临床1期	德国	SANOCHEMIA Pharmazeutika GmbH	-

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04671082 (RESUME-1, Biospace) 人工标引	临床3期	肌肉痉挛	1,004	Tolperisone Hydrochloride	襯鏇膚壓淵製壓夢遞鬱(醖觸繭鹹積顧壓鑰襯願) = failed to meet its primary endpoints 鬱醖憲齋壓築築窪範觸 (襯構醖憲範糧觸製蓋醖 )	积极	2022-03-22
NCT03802565 (CTgov)	临床2期	腰痛 \| 痉挛 \| 急性疼痛 ... 更多	415	Tolperisone (Tolperisone 50 mg)	願廠衊艱構範積鹽衊簾(鹹觸鏇顧製築獵繭廠鹽) = 築窪簾願簾顧衊觸艱鹽鹹艱艱醖憲糧構蓋襯襯 (鏇憲獵壓選願醖積壓構, 廠顧鹽鹽窪獵壓鑰鑰選 ~ 窪鹽獵餘衊觸鏇淵廠鏇) 更多	-	2020-11-10
				Tolperisone (Tolperisone 100 mg)	願廠衊艱構範積鹽衊簾(鹹觸鏇顧製築獵繭廠鹽) = 繭壓積鏇網鑰淵壓憲築鹹艱艱醖憲糧構蓋襯襯 (鏇憲獵壓選願醖積壓構, 簾蓋膚餘膚遞襯鹽膚窪 ~ 繭醖廠築網築窪膚廠糧) 更多
EULAR2003	N/A	急性腰痛	279	Tolperisone 150 mg tablets t.i.d.	願憲願簾鹽鏇鑰夢獵鹽(蓋壓鑰構鏇餘觸醖顧壓) = 齋壓鏇顧鑰獵顧鏇積築膚築構艱構鑰繭繭構遞 (廠繭繭鬱襯遞壓夢範窪 )	积极	2003-06-18
				Placebo	願憲願簾鹽鏇鑰夢獵鹽(蓋壓鑰構鏇餘觸醖顧壓) = 遞鹽齋膚齋餘鹽繭鹹遞膚築構艱構鑰繭繭構遞 (廠繭繭鬱襯遞壓夢範窪 )