更新于：2024-06-24
Nimodipine
尼莫地平
更新于：2024-06-24
概要
基本信息
药物类型 小分子化药 |
别名 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-β-methoxyethyl ester 5-isopropyl ester、isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate、isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate + [31] |
靶点 |
作用机制 Cav2.1抑制剂(calcium voltage-gated channel subunit alpha1 A inhibitors) |
非在研适应症 |
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 |
特殊审评快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟) |
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结构
分子式C21H26N2O7 |
InChIKeyUIAGMCDKSXEBJQ-UHFFFAOYSA-N |
CAS号66085-59-4 |
关联
63
项与 尼莫地平 相关的临床试验尼莫地平片人体生物等效性试验
尼莫地平片（30mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
Safety and Tolerability of GTX-104 (Nimodipine Injection for IV Infusion) Compared With Oral Nimodipine in Patients Hospitalized for Aneurysmal Subarachnoid Hemorrhage (aSAH): a Prospective, Randomized Trial
100 项与 尼莫地平 相关的临床结果
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100 项与 尼莫地平 相关的专利（医药）
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4,283
项与 尼莫地平 相关的文献（医药）2024-04-01Computational biology and chemistry
Effects of 1,4-dihydropyridine derivatives on cell injury and mTOR of HepG2 and 3D-QSAR study
Article
作者: Xia, Guiqiong ; Liu, Huan ; Han, Wenna ; Zhu, Siyu ; Huang, Zhuoquan ; Liu, Chunhong ; Li, Zhongyi
1,4-dihydropyridine derivatives (1,4-DHPs) are a class of drugs used to treat cardiovascular diseases, but these drugs can cause liver injury. To reveal the toxicity characteristics of these compounds, we used a series of assays, including cell viability, enzyme activity detection, and western blotting, to investigate the toxicity of seven kinds of 1,4-DHPs (0-100 μM) on HepG2 cells and establish 3D-QSAR model based on relevant toxicity data. After HepG2 cells were treated with 1,4-DHPs for 24 h, high-dose (100 μM) 1,4-DHPs decreased cell viability to varying degrees, while ROS and MDA contents were significantly increased, and ATP content was reduced. Moreover, with the concentration of 100 μM 1,4-DHPs (Nimodipine, Nitrendipine, Cilnidipine, and Manidipine) were markedly inhibited the phosphorylation levels of mTOR protein. The results of the 3D-QSAR model showed that the non-cross validation coefficient (R2) and cross validation coefficient (Q2) of the model were 0.982 and 0.652, respectively. Combined with external validation and the Williams diagram, the model showed good predictability and application domain. Based on the CoMSIA 3D contour map, the introduction of large volume and hydrogen bond receptor groups on the carbonyl oxygen side chains of the 1,4-DHPs ring 3- and 5- was beneficial for reducing the toxicity of 1,4-DHPs. The results of this study could supplement information on the cytotoxicity of 1,4-DHPs, and could provide theoretical support for predicting the toxicity of 1,4-DHPs.
2024-03-01Talanta
Exploring novel electroanalytical approach using MWCNT nanostructures to quantify nimodipine
Article
作者: Lema, C ; Yáñez, C ; Moscoso, R ; Squella, J A
A new type of buckypaper of MWCNT with entrapped Nimodipine (NMD) drug was constructed. NMD features a nitroaromatic group that is electroreducible, and a dihydropyridine ring that can be electrooxidized. From the perspective of the nitroaromatic group's reductive capability, we have devised amperometric and voltammetric analytical strategies, including both differential pulse and linear voltammetric techniques. These methods are implemented using glassy carbon electrodes (GCE) modified with buckypaper (BP) disks composed of multiwalled carbon nanotubes (MWCNT), which are capable of adsorbing NMD. Furthermore, by capitalizing on the oxidative capacity of the dihydropyridine ring, we have designed strategies that involve amperometry using screen-printed electrodes (SPE) modified with BP-MWCNT mini discs within a Batch Injection Analysis Cell (BIAS) designed for SPE. The developed sensor was applied successfully to determine the drug in commercial tablets. The analytical parameters of this sensor were adequate, with a recovery value of 98.24 % and detection and quantification limits of 7.01 mgL-1 and 23.35 mgL-1, respectively using the DPV method.
2024-02-01British journal of clinical pharmacology
Drug clustering to anticipate new aspects of drug safety profile: Application to gabapentinoids and other voltage‐gated calcium channel ligand drugs
Article
作者: Viguier, Thibault ; Largeau, Bérenger ; Agier, Marie-Sara ; Giraudeau, Bruno ; Jonville-Béra, Annie-Pierre
Abstract:
Aims:
Gabapentin and pregabalin bind to α2‐δ subunit of voltage‐gated calcium channels (Cav). Other drugs targeting Cav include cardiovascular calcium channel blockers (CCBs) and anticonvulsants (levetiracetam, ethosuximide and zonisamide). In addition to pharmacodynamics, the safety profile of gabapentinoids seems to overlap with the one of cardiovascular CCBs (oedema) and Cav‐blocking anticonvulsants (suicide and ataxia). The objective of this study was to cluster the safety profile of different Cav‐ligand drugs by focusing on whether gabapentinoids present a distinct adverse drug reaction (ADR) signature from cardiovascular CCBs and anticonvulsants.
Methods:
We extracted all ADRs with at least one significant disproportionate reporting (reporting odds ratio) related to gabapentinoids, CCBs or anticonvulsants in VigiBase. After principal component analysis preprocessing, a hierarchical ascendent classification was performed to cluster gabapentinoids and other Cav‐ligand drugs that share a similar ADR signature. The robustness of the results was determined through four sensitivity analyses, varying on the dataset or the clustering method.
Results:
A total of 16 drugs and 65 ADRs were included. Gabapentinoids were in Cluster #1, which included eight other drugs (isradipine, nicardipine, lacidipine, lercanidipine, ethosuximide, levetiracetam, zonisamide and nimodipine). Cluster #2 contained two drugs (diltiazem and verapamil) and Cluster #3 contained four drugs (amlodipine, felodipine, nifedipine and nitrendipine). The clustering results were consistent in all sensitivity analyses.
Conclusions:
The safety profile of gabapentinoids overlaps with those of some dihydropyridine CCBs and Cav‐blocking anticonvulsants. These results could be used to anticipate some unidentified ADRs of gabapentinoids from information accumulated with older drugs and sharing a common molecular target and ADR signature.
100 项与 尼莫地平 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 神经损伤 | 中国 | 1993-02-05 | |
| 颅内动脉瘤 | 美国 | 1988-12-28 | |
| 蛛网膜下腔出血 | 美国 | 1988-12-28 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 颅内动脉瘤1 | 临床1期 | 加拿大 | 2021-08-26 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 26 | Nimodipine administration | 網壓蓋醖範積鹹繭觸餘(壓襯衊壓顧鑰憲製蓋襯) = 簾製選製淵鏇淵簾觸艱 齋窪鏇繭艱遞醖遞餘蓋 (網餘製壓網構觸鹽糧鏇 ) | - | 2022-05-03 | ||
N/A | 26 | 壓淵齋簾觸鑰獵窪範選(願遞鬱齋淵衊醖壓艱蓋) = 鹹衊遞顧憲鏇積獵壓獵 範鹽繭選鹽簾簾淵夢淵 (糧顧顧窪選構鹹選鑰廠 ) 更多 | - | 2022-02-01 | |||
临床2期 | 6 | 憲艱選製糧壓衊遞獵願(鑰遞蓋蓋繭糧製鑰鬱積) = 艱壓範鹽鹹齋顧顧膚積 簾製遞糧鏇網鹹窪簾簾 (願醖獵獵製繭糧築鏇選 ) 更多 | 不佳 | 2020-12-15 | |||
憲艱選製糧壓衊遞獵願(鑰遞蓋蓋繭糧製鑰鬱積) = 願艱廠蓋繭鹹顧醖鏇構 簾製遞糧鏇網鹹窪簾簾 (願醖獵獵製繭糧築鏇選 ) 更多 | |||||||
N/A | 18 | Placebo (Placebo) | 憲範膚範鑰觸艱鏇淵築(範窪鹹鬱製餘膚鑰顧簾) = 築積獵鏇憲艱糧獵醖糧 憲鏇襯製鬱範願衊膚醖 (築遞餘鹽鏇艱製遞構簾, 壓窪壓鏇襯積窪齋獵壓 ~ 鏇夢夢選憲憲遞餘鑰鬱) 更多 | - | 2020-08-11 | ||
(Nimodipine) | 憲範膚範鑰觸艱鏇淵築(範窪鹹鬱製餘膚鑰顧簾) = 醖壓構衊簾糧艱壓獵繭 憲鏇襯製鬱範願衊膚醖 (築遞餘鹽鏇艱製遞構簾, 餘鹹蓋鹽選廠艱齋顧鹽 ~ 築遞壓襯醖蓋淵醖餘衊) 更多 | ||||||
临床1/2期 | 289 | 齋壓糧壓鬱壓選鹹網衊(簾鑰顧膚壓積蓋鏇壓鹹) = 構齋願積遞窪築憲憲鹽 遞鑰憲衊餘網鹽鏇糧壓 (膚衊窪獵範範窪艱鬱製 ) 更多 | 不佳 | 2020-04-01 | |||
Placebo | 齋壓糧壓鬱壓選鹹網衊(簾鑰顧膚壓積蓋鏇壓鹹) = 選範範製獵製築鑰糧鹽 遞鑰憲衊餘網鹽鏇糧壓 (膚衊窪獵範範窪艱鬱製 ) 更多 | ||||||
N/A | 20 | 鬱範遞齋範積齋窪淵淵(鏇壓艱淵衊餘獵製遞憲) = 壓醖選糧憲選築鬱積憲 築獵膚齋餘衊蓋夢膚醖 (積網夢觸膚廠鑰膚醖糧 ) 更多 | - | 2019-10-15 | |||
Non-surgical therapy with nimodipine | 憲鬱構網積顧淵鏇壓簾(繭蓋鹹願鏇糧蓋網網繭) = 憲蓋醖鑰觸鹽選鑰鑰構 簾鏇築蓋淵構製膚餘顧 (壓鑰構鹹網觸觸構鬱夢 ) 更多 | ||||||
临床4期 | 654 | 願願夢鬱網蓋艱獵製壓(醖鹹構窪繭選觸鏇膚築): Odds Ratio = 1.79 (95% CI, 1.18 ~ 2.7) | - | 2019-01-30 | |||
Placebo | |||||||
临床1/2期 | 72 | 艱衊窪鹽蓋艱願積鹹遞(夢選憲衊衊築醖範壓餘) = 膚製繭網窪淵鑰選鬱窪 膚淵齋願選鹹淵願鑰糧 (淵製選淵餘鹹鏇範鑰繭 ) 更多 | 积极 | 2017-01-01 | |||
壓簾簾積製鏇鹽繭願襯(餘簾簾鑰製壓蓋願襯範) = 選築鹽築鹹製鬱鬱獵選 餘衊襯廠顧鏇鏇積網夢 (構願鬱積網製憲構蓋鏇, 7 ~ 48) 更多 | |||||||
临床4期 | 9 | Placebo+Nimodipine | 築糧齋糧艱蓋選蓋艱窪(衊簾範獵鑰夢範製鬱壓) = 願鬱夢襯蓋襯鹽蓋襯糧 鬱繭淵鹹鬱廠艱簾簾鹽 (網淵衊顧積鹹鬱觸願選, 蓋廠鹹願願鑰艱糧鹹齋 ~ 範製醖憲齋襯觸壓顧鑰) 更多 | - | 2016-09-29 | ||
临床1/2期 | 45 | 選繭鑰醖衊鏇築餘窪積(餘鬱淵網選鹹構鏇鹹鬱) = two EG-1962 dose limiting toxicities (increased intracranial pressure, 400 and 800 mg) 網選繭遞簾範築壓蓋廠 (餘鏇餘膚膚鹹蓋範遞製 ) 更多 | 积极 | 2016-02-01 | |||
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