预约演示
更新于：2025-04-19
Nitrendipine
尼群地平
更新于：2025-04-19
概要
基本信息
原研机构- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (1987-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C18H20N2O6 |
InChIKeyPVHUJELLJLJGLN-UHFFFAOYSA-N |
CAS号39562-70-4 |
关联
6
项与 尼群地平 相关的临床试验NCT04931108
The Effect of Nitrendipine/Atenolol Combination on Blood Pressure Variability of Patients With Grade 1 Hypertension Compared With Nitrendipine or Atenolol Monotherapy.
CTR20210720
尼群地平片（10 mg）人体生物等效性研究
NCT02217852
A Randomized, Open-label, Positive Drug Controlled Clinical Trials to Compare the Efficacy of Nitrendipine and Hydrochlorothiazide , Captopril Plus Hydrochlorothiazide and Beijing Hypotensive No.0 in Tibetan Hypertension
100 项与 尼群地平 相关的临床结果
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100 项与 尼群地平 相关的转化医学
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100 项与 尼群地平 相关的专利（医药）
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3,949
项与 尼群地平 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.
2025-04-01BLOOD PRESSURE MONITORING
Effect of a calcium-channel blocker and β-blocker combination on reading-to-reading blood pressure variability: a randomized crossover trial
Article
作者: Xia, Jia-Hui ; Guo, Qian-Hui ; Wang, Ji-Guang ; Cheng, Yi-Bang ; Xu, Ting-Yan ; Chan, Chak-Ming ; Hu, Lei-Xiao ; Li, Yan
Objective:
The objective of this study was to investigate the efficacy of the nitrendipine/atenolol combination in comparison with standard-dose nitrendipine or atenolol monotherapy in reducing blood pressure (BP) and blood pressure variability (BPV) as assessed by ambulatory BP monitoring.
Methods:
In a randomized, crossover trial, 32 patients (30–65 years) with grade 1 hypertension and elevated daytime reading-to-reading BPV were randomly assigned to receive either the nitrendipine/atenolol combination (10/20 mg) or standard-dose nitrendipine (10 mg) or atenolol (25 mg) monotherapy for 6 weeks, followed by a crossover to another treatment for 6 weeks.
Results:
The final analysis included 31 patients (mean [±SD] age, 49.2 ± 9.6 years) and 12 men. The nitrendipine/atenolol combination significantly reduced from baseline clinic and ambulatory BP and pulse rate (P ≤ 0.002), and 24 h and daytime systolic and diastolic BPV as assessed by SD and average real variability (P ≤ 0.042), but not the coefficient of variation nor nighttime BPV indices (P ≥ 0.06). Significant differences between the nitrendipine/atenolol combination and nitrendipine or atenolol monotherapy at the end of treatment were observed in clinic BP and pulse rate (P ≤ 0.042), but not in 24 h, daytime and nighttime blood pressure and pulse rate, except for daytime DBP and 24 h and daytime pulse rate (P ≤ 0.049). There were no significant differences in BPV between the combination and monotherpy groups at the end of treatment (P ≥ 0.25).
Conclusion:
The nitrendipine/atenolol combination reduced daytime reading-to-reading BPV, but did not show superiority to nitrendipine or atenolol monotherapy.
2025-03-07ORGANIC LETTERS
Photoinduced Reductive [4 + 2] Cycloaddition of Nitroarenes
Article
作者: Okamura, Toshitaka ; Sato, Takaaki ; Kaneko, Taiki ; Ito, Rin
Direct C-N bond formation from nitroarenes is a valuable synthetic tool for quick access to aniline derivatives. Transformation via nitroso intermediates could be useful due to their unique properties, but the generation of nitrosoarenes in situ from nitroarenes is challenging due to the tendency for various side reactions. Herein we report the photoinduced reductive [4 + 2] cycloaddition of nitroarenes. The method begins with the photoinduced reduction of nitroarenes to give nitrosoarenes by hydrogen atom abstraction (HAA). The generated nitrosoarenes undergo a nitroso Diels-Alder (NDA) reaction. The key to success is the use of N-heterocyclic carbene (NHC) borane, which promotes efficient HAA, enabling the NDA reaction to proceed without the need for transition metals, strong bases, or elevated temperatures. The developed conditions allow high functional group tolerance, enabling late-stage functionalization and further derivatization of biologically active compounds.
100 项与 尼群地平 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肾性高血压 | 日本 | 1998-03-12 | |
| 心绞痛 | 日本 | 1990-01-23 | |
| 高血压 | 中国 | 1987-01-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 59 | Combined antihypertensive treatment with nitrendipine | 願糧齋築鬱構顧遞繭餘(簾蓋築簾艱鹹衊齋糧餘) = 構願顧鹹網憲醖衊遞壓 築廠襯鏇範淵艱艱夢鹽 (糧簾網鬱鏇築繭簾遞憲 ) | - | 2023-08-27 | ||
临床4期 | 1,405 | 積糧構蓋廠衊願襯範窪(網構鏇齋鏇築齋獵鑰築) = 餘願淵鬱鹹簾糧觸鹹構 壓繭鏇糧齋遞鹽窪鹹顧 (遞鏇簾繭夢壓製遞憲齋 ) | - | 2005-06-01 | |||
積糧構蓋廠衊願襯範窪(網構鏇齋鏇築齋獵鑰築) = 餘網構廠壓積遞糧齋憲 壓繭鏇糧齋遞鹽窪鹹顧 (遞鏇簾繭夢壓製遞憲齋 ) |
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