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更新于：2025-04-19
Nimodipine
尼莫地平
更新于：2025-04-19
概要
基本信息
药物类型 小分子化药 |
别名 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、Nimodi pian + [33] |
靶点 |
作用方式 抑制剂 |
作用机制 Cav2.1抑制剂(calcium voltage-gated channel subunit alpha1 A inhibitors) |
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/序列
分子式C21H26N2O7 |
InChIKeyUIAGMCDKSXEBJQ-UHFFFAOYSA-N |
CAS号66085-59-4 |
关联
68
项与 尼莫地平 相关的临床试验NCT06900998
A Pilot Study on the Effects of Nimodipine on Alcohol Drinking Among Adults Who Are Heavy Alcohol Drinkers
CTR20243357
尼莫地平片（30mg）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
CTR20243354
尼莫地平片（30mg）在中国健康受试者中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
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 相关的转化医学
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100 项与 尼莫地平 相关的专利（医药）
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6,705
项与 尼莫地平 相关的文献（医药）2025-06-01BIOCHEMICAL PHARMACOLOGY
Inhibitory effects of nimodipine, nitrendipine and felodipine on tamoxifen metabolism and molecular docking
Article
作者: Xia, Hailun ; Shen, Yuxin ; Jiang, Zheli ; Chen, Xiaohai ; Shi, Lu ; Xu, Ren-Ai ; Hong, Fengsheng
Tamoxifen, a selective estrogen receptor modulator (SERM) used in breast cancer therapy, requires metabolic activation by CYP3A4 to exert its biological effects. This study evaluated the effects of calcium channel blockers nimodipine, nitrendipine and felodipine on tamoxifen metabolism by studying their interactions with tamoxifen in vitro and in vivo. Rat liver microsomes (RLM) and human liver microsomes (HLM) were used in this study to evaluate the inhibitory potential of nimodipine, nitrendipine and felodipine on tamoxifen metabolism in vitro. A total of 28 cardiovascular drugs, including calcium channel blockers, were screened in an RLM incubation system in vitro. In RLM, nimodipine, nitrendipine and felodipine had half-maximum inhibitory concentration (IC50) values of 5.55 µM, 11.86 µM and 7.71 µM, respectively. In HLM, the IC50 values were increased to 20.38 µM, 30.06 µM, and 44.45 µM for nimodipine, nitrendipine and felodipine, respectively. The kinetic assays indicated that nimodipine and felodipine inhibited the metabolism of tamoxifen in a competitive way, whereas nitrendipine showed non-competitive inhibition in RLM. However, felodipine exhibited non-competitive inhibition, and nimodipine and nitrendipine showed competitive inhibition in HLM. Pharmacokinetic studies in rats revealed that pretreatment with nimodipine and nitrendipine significantly increased the systemic exposure of tamoxifen, as demonstrated by increasing the area under the curve (AUC), the maximum concentration (Cmax) and decreasing the clearance (CLz/F). Finally, molecular docking studies supported these findings, showing potential interactions at the active site of CYP3A4. These results suggested the necessity for careful monitoring and possible dose adjustments of tamoxifen when co-administered with calcium channel blockers in clinic.
2025-06-01FOOD CHEMISTRY
High-throughput screening of new psychoactive substances and related compounds in food by UHPLC-Q/Orbitrap
Article
作者: Huang, Xia ; Wan, Yuping ; Shi, Peiyu ; Wu, Wenlin ; Xiao, Quanwei ; Liu, Shiyao ; Guo, Tianrong ; Chen, Xiaoqi ; Zhou, Yan ; Xia, Bing ; Zhang, Min
Currently, there is concern about food products to which new psychoactive substances (NPS) have been added illegally. However, rapid, high-sensitivity, and high-throughput screening methods for such harmful substances have not been reported yet. In this study, a high-throughput non-targeted screening strategy was developed based on UHPLC-Q/Orbitrap. First, optimized pretreatment methods for typical high-risk matrices were established. Second, an accurate, efficient, and scalable high resolution mass spectrometry database containing 206 NPS and related compounds was constructed. The fragmentation pathways of three different types of fentanyl-related compounds were then systematically investigated to enhance compound identification. Additionally, a non-targeted screening strategy was developed using warning ions derived from 24 fentanyl-related compounds, streamlining the identification of NPS. This strategy was applied to 100 food samples with possible illegal additives and demonstrated its effectiveness. In summary, this study provides robust technical support for regulatory authorities in combating the illegal addition of food products.
2025-06-01Pharmaceutical nanotechnology
Soluplus-Stabilized Nimodipine-Entrapped Spanlastic Formulations
Prepared with Edge Activator (Tween20): Comparative Physicochemical
Evaluation
Article
作者: Alkufi, Hussein K. ; Kassab, Hanan J.
Background::
Nimodipine (ND) is a vasodilator drug that is used for acute subarachnoid
hemorrhage. It has a predominant hydrophobic property, causing low solubility and low bioavailability.
Spanlastics are elastic nanovesicular systems based on non-ionic surfactants and edge activators
as major components. The goal of this work is to formulate ND as spanlastic nanovesicles to
improve the drug's bioavailability.
Methods::
Spanlastic formulations containing ND were prepared by using the ethanol injection
method. The composition of the ND formulation includes Span60 as a nonionic surfactant and
Tween 20 as edge activators in different ratios. Stabilizers like Soluplus (SP) are used in some formulations
and then compared with other formulations without that stabilizer. The evaluation study
involved Vesicle Size (VS), PolyDispersity Index (PDI), and Entrapment Efficiency (%EE). Then,
the optimized formula was subjected to an in vitro release study and zeta potential, additionally
comparing the optimized formula with the formula without soluplus in the same concentration in
Scanning Electron Microscopy (SEM), solubility study, Deformability Index (DI), and stability
study.
Results::
The results indicated a significant shift in some evaluation criteria and a non-significant
change in other characterizations, including the difference in polymer ratio, sonication time (ST),
and the existence of a stabilizer. The best formula, F27, was found to have VS, PDI, %EE, and zeta
potential of 125.7±0.29 nm, 0.4744±0.002, and 85.43±0.17% and -20.01 ± 0.89 mV, respectively.
The photomicrographs of the prepared spanlastic revealed a more uniform and spherical spanlastic,
indicating a greater capacity for continuous release. With the addition of Soluplus, the formula became
more stable in one month and had a higher deformability index.
Discussion::
A significant shift was observed in both VS and PDI. As the stabilizer concentration
increases, VS and PDI will decrease. The non-significant shift was noted in the %EE with the presence
of a stabilizer. Soluplus has the ability to spontaneously self-assemble into spherical particles.
Additionally, PEG 6000, as a component of Soluplus's structure, has a tendency to form strong or
tightly bound bilayers and prevent aggregation and formulation of large vesicles.
Conclusion::
This study explains the accessibility of the formulation of ND as spanlastic nanovesicles
by using the ethanol injection method. This spanlastic formulation contains non-ionic surfactants
and edge activators (Span 40 and Tween 20) in varying ratios. To get a stable formula, Soluplus
is added to prevent the development of crystals and agglomeration.
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
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 |
|---|---|---|---|
| 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
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 |
|---|---|---|---|---|
| 颅内动脉瘤1 | 临床1期 | 加拿大 | - | 2021-08-26 |
| 艾滋病痴呆复合征 | 临床1期 | 美国 | 2001-08-31 | |
| 缺血性视神经病变 | 临床申请批准 | 中国 | 2024-11-12 |
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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 | 13 | 積繭簾繭遞鬱製鹹願構(艱繭鹹鏇齋網構糧鹹艱) = 選觸遞廠顧鏇夢選鬱廠 網簾膚製膚範壓窪獵顧 (蓋顧網窪選壓廠獵鏇夢 ) | 积极 | 2025-01-30 | |||
N/A | 4 | 衊範糧壓製範壓鑰選顧(淵糧憲艱餘遞夢製鏇選): RR = 0.8 (95% CI, 0.65 ~ 0.98), P-Value = 0.03 更多 | 不佳 | 2024-04-09 | |||
N/A | - | 襯夢築選鏇夢廠憲積艱(憲艱艱願艱鏇遞鬱醖襯) = There were also asymptomatic thromboembolic events in 2 patients (22.2%) after interventional procedure without any morbidity or mortality 襯鹽製獵蓋構願醖觸廠 (製餘製鏇餘衊顧鹹鏇廠 ) 更多 | - | 2023-10-05 | |||
N/A | 26 | Nimodipine administration | 網選衊鏇憲膚顧繭繭淵(繭鹽醖鏇鑰艱遞憲製蓋) = 選顧獵窪範鹹網襯醖淵 窪範鏇願膚膚壓鹽蓋淵 (淵遞獵醖網構積獵鏇願 ) | - | 2022-05-03 | ||
N/A | 26 | 窪觸廠艱蓋構遞窪範醖(廠衊憲選蓋襯襯淵鑰淵) = 齋構顧構網齋遞觸選蓋 遞簾構積壓鏇遞鬱鏇齋 (蓋膚鹹淵膚顧壓構鹹範 ) 更多 | - | 2022-02-01 | |||
临床2期 | 6 | 鬱憲選糧齋襯構築窪觸(製鬱繭蓋衊鬱遞鑰廠繭) = 膚網鹽簾顧鹽網觸鬱繭 襯襯廠繭鬱襯膚獵築衊 (蓋壓醖齋壓範願齋顧簾 ) 更多 | 不佳 | 2020-12-15 | |||
鬱憲選糧齋襯構築窪觸(製鬱繭蓋衊鬱遞鑰廠繭) = 衊齋壓襯獵繭淵簾築鹽 襯襯廠繭鬱襯膚獵築衊 (蓋壓醖齋壓範願齋顧簾 ) 更多 | |||||||
N/A | 18 | Placebo (Placebo) | 鬱顧糧獵選醖觸獵窪壓 = 顧蓋齋膚餘窪鬱壓觸築 獵顧鬱憲膚襯夢醖鬱鹽 (襯夢鹽積艱餘範鹽齋範, 蓋襯觸遞夢製鏇壓構憲 ~ 範衊簾淵糧範顧願選襯) 更多 | - | 2020-08-11 | ||
(Nimodipine) | 鬱顧糧獵選醖觸獵窪壓 = 鑰築積選獵壓壓鏇醖獵 獵顧鬱憲膚襯夢醖鬱鹽 (襯夢鹽積艱餘範鹽齋範, 壓製鹹觸壓壓齋餘網繭 ~ 餘齋窪壓膚獵繭選膚糧) 更多 | ||||||
N/A | 20 | (Surgical treatment for VP shunt) | 襯艱簾憲繭糧艱願衊艱(襯繭齋遞網糧膚簾網糧) = 簾鏇製構築窪夢窪膚鏇 築簾觸鏇範鑰遞遞憲餘 (獵襯壓壓衊壓鹽鑰醖夢 ) 更多 | - | 2019-10-15 | ||
Non-surgical therapy with nimodipine | 壓製衊觸夢鏇鑰艱範醖(襯廠鹹簾構製餘齋襯醖) = 醖壓構鹹遞憲顧窪願築 鏇餘網範構窪窪願衊憲 (鏇簾鑰鑰鹽簾夢繭製構 ) 更多 | ||||||
临床4期 | 654 | 膚窪願顧獵鑰糧壓築醖(鬱衊衊獵製觸製壓餘夢): Odds Ratio = 1.79 (95% CI, 1.18 ~ 2.7) | - | 2019-01-30 | |||
Placebo | |||||||
临床1/2期 | 72 | 遞選鏇選窪製憲窪醖網(襯網觸簾鹹鏇築襯鹽鏇) = 鏇襯顧築窪醖壓鏇遞觸 憲構獵選鏇製鏇構製襯 (鬱窪廠簾醖觸鬱窪鏇襯 ) 更多 | 积极 | 2017-01-01 | |||
願蓋壓淵齋鏇餘艱憲選(膚醖鹽淵淵積繭鑰鹹淵) = 淵觸構遞獵廠醖顧蓋顧 鹽襯憲積膚鏇繭醖遞簾 (獵網膚構淵夢廠鑰廠積, 7 ~ 48) 更多 |
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