更新于：2024-07-01
Felodipine
非洛地平
更新于：2024-07-01
概要
基本信息
药物类型 小分子化药 |
别名 (±)-ethyl methyl 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate、3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylate、4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl ester + [15] |
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 |
在研机构 |
最高研发阶段临床1期 |
首次获批日期 美国 (1991-07-25), |
最高研发阶段(中国)临床1期 |
特殊审评优先审评 (中国) |
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结构
分子式C18H19Cl2NO4 |
InChIKeyRZTAMFZIAATZDJ-UHFFFAOYSA-N |
CAS号72509-76-3 |
关联
51
项与 非洛地平 相关的临床试验非洛地平缓释片在空腹及餐后条件下的人体生物等效性试验
中国健康受试者空腹和餐后单次口服非洛地平片的随机、开放、两序列、四周期、重复交叉设计的生物等效性试验
非洛地平缓释片（5mg）在中国健康受试者中空腹和餐后条件下给药的随机、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 非洛地平 相关的临床结果
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100 项与 非洛地平 相关的转化医学
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100 项与 非洛地平 相关的专利（医药）
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1,822
项与 非洛地平 相关的文献（医药）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 ; Giraudeau, Bruno ; Agier, Marie-Sara ; 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.
2024-01-01The Journal of pharmacology and experimental therapeutics
Gene Polymorphisms and Drug–Drug Interactions Determine the Metabolic Profile of Blonanserin
Article
作者: Hu, Guoxin ; Li, Xinyue ; Ye, Feng ; Qian, Jianchang ; Zhang, Yuqing ; Wang, Shiyu ; Luo, Jianchao ; Wang, Yahui ; Xu, Xiaoyu ; Ni, Jinhuan ; Zhong, Yunshan
This study aimed to evaluate the effects of cytochrome P450 3A4 (CYP3A4) gene polymorphism and drug interaction on the metabolism of blonanserin. Human recombinant CYP3A4 was prepared using the Bac-to-Bac baculovirus expression system. A microsomal enzyme reaction system was established, and drug-drug interactions were evaluated using Sprague-Dawley rats. Ultra-performance liquid chromatography-tandem mass spectrometry was used to detect the concentrations of blonanserin and its metabolite. Compared with wild type CYP34A, the relative clearance of blonanserin by CYP3A4.29 significantly increased to 251.3%, while it decreased notably with CYP3A4.4, 5, 7, 8, 9, 10, 12, 13, 14, 16, 17, 18, 23, 24, 28, 31, 33, and 34, ranging from 6.09% to 63.34%. Among 153 tested drugs, nimodipine, felodipine, and amlodipine were found to potently inhibit the metabolism of blonanserin. Moreover, the inhibitory potency of nimodipine, felodipine, and amlodipine varied with different CYP3A4 variants. The half-maximal inhibitory concentration and enzymatic kinetics assay demonstrated that the metabolism of blonanserin was noncompetitively inhibited by nimodipine in rat liver microsomes and was inhibited in a mixed manner by felodipine and amlodipine in both rat liver microsomes and human liver microsomes. When nimodipine and felodipine were coadministered with blonanserin, the area under the blood concentration-time curve (AUC)(0-t), AUC(0-∞), and C max of blonanserin increased. When amlodipine and blonanserin were combined, the C max of blonanserin C increased remarkably. The vast majority of CYP3A4 variants have a low ability to catalyze blonanserin. With combined administration of nimodipine, felodipine, and amlodipine, the elimination of blonanserin was inhibited. This study provides the basis for individualized clinical use of blonanserin. SIGNIFICANCE STATEMENT: The enzyme kinetics of novel CYP3A4 enzymes for metabolizing blonanserin were investigated. Clearance of blonanserin by CYP3A4.4, 5, 7-10, 12-14, 16-18, 23-24, 28, 31, 33, and 34 decreased notably, but increased with CYP3A4.29. Additionally, we established a drug interaction spectrum for blonanserin, in which nimodipine, felodipine, and amlodipine kinetics exhibited mixed inhibition. Moreover, their inhibitory potencies decreased with CYP3A4.4 and 5 compared to CYP3A4.1. This study provides essential data for personalized clinical use of blonanserin.
2023-12-01Current organic synthesis
Practical Synthesis of 1,4-Dihydropyridines on Heterogeneous Sulfonicmodified
Silica (SBA-15-SO3H) Catalyst Under Mild Condition
Article
作者: Do, Dang Van ; Lan Nhi, Do Thi ; Nguyen, Hien ; Xuan Vu, Hoan ; Phuc, Ban Van ; Loan, Pham Thị Thanh ; Dang, Tuan Thanh ; Hung, Tran Quang
Aims::
Synthesis of 1,4-Dihydropyridines (1,4-DHP) using heterogeneous catalyst un-der mild condition
Objective::
Our objective is to explore new applications of non-metal heterogeneous catalysts in the synthesis of 1,4-DHP derivatives in a greener and more efficient approach.
Methods::
A greener and more efficient method for the synthesis of 1,4-DHPs and an asymmetric 1,4-DHP (Felodipine drug) was successfully developed in high yields using a heterogeneous SBA-15-SO3H catalyst.
Results::
A series of symmetric 1,4-DHP and an asymmetric 1,4-DHP (Felodipine drug) were suc-cessfully prepared in high yields using a heterogeneous SBA-15-SO3H catalyst
Conclusion::
The catalyst, SBA-15-SO3H, exhibited an efficient catalyst activity for the synthesis of 1,4-DHP derivatives in high yields from the aldehyde, β-ketoester, and NH4OAc as a nitrogen source under mild conditions and short reaction time. Bronsted acid sites of this solid catalyst were figured out to play a key role in this transformation. Interestingly, our catalyst is air-stable and can be recycled at least 5 times without losing catalytic activity.
100 项与 非洛地平 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 |
|---|---|---|---|
| 高血压 | 美国 | 1991-07-25 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 稳定型心绞痛 | 临床1期 | 中国 | - | 2013-10-11 |
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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 | 41 | 醖獵衊廠積壓廠壓繭餘(糧鬱簾醖繭願衊積膚簾) = 獵憲膚遞鏇鹹壓觸範繭 窪醖艱衊齋膚壓憲範襯 (築夢膚衊襯鏇選艱鹽簾, -40 ~ -22) | 积极 | 2018-05-18 | |||
Placebo | 醖獵衊廠積壓廠壓繭餘(糧鬱簾醖繭願衊積膚簾) = 獵醖餘餘繭鬱糧鹹壓齋 窪醖艱衊齋膚壓憲範襯 (築夢膚衊襯鏇選艱鹽簾, -57 ~ -39) | ||||||
N/A | 41 | 艱憲鬱鬱憲蓋襯夢糧齋(製選製憲蓋築鏇遞構蓋) = Hypotension occurred more frequently among felodipine-treated patients compared with placebo ( P <0.01) 淵遞艱鹹構範糧鹹製選 (鏇壓簾鹽壓願選觸遞齋 ) | 积极 | 2017-05-26 | |||
Placebo | |||||||
N/A | 529 | (Felodipine Tablet (Plendil)+Metoprolol Tablet (Betaloc ZOK)) | 糧蓋觸醖選醖鏇鏇願網(鏇鹹繭憲壓遞糧遞觸膚) = 齋齋觸繭顧齋醖膚獵廠 淵壓網網鑰範淵鏇顧鬱 (鑰憲糧積築繭襯網積鏇, 鬱繭遞遞積願襯衊選齋 ~ 製鬱醖積艱醖壓鏇構製) 更多 | - | 2015-03-23 | ||
(Felodipine Tablets (Plendil)+Lisinopril (Zestril)) | 糧蓋觸醖選醖鏇鏇願網(鏇鹹繭憲壓遞糧遞觸膚) = 範蓋鏇衊鹹網窪鹽醖壓 淵壓網網鑰範淵鏇顧鬱 (鑰憲糧積築繭襯網積鏇, 窪衊鹽製夢簾糧觸鑰廠 ~ 獵願鹽憲積餘夢鏇膚壓) 更多 | ||||||
临床4期 | 315 | 窪簾壓鏇廠憲範繭窪衊(鑰膚遞鑰憲選襯餘廠艱) = 鬱廠選網鬱壓鑰鏇鏇蓋 衊廠餘鬱築糧鹹蓋繭鑰 (鹹衊襯鏇憲選糧襯窪繭, 憲醖糧衊淵糧構醖繭鹹 ~ 選選鑰鹽艱鏇顧網願築) 更多 | - | 2012-04-02 |
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