预约演示
更新于：2025-01-14
Lisinopril
赖诺普利
更新于：2025-01-14
概要
基本信息
简介Lisinopril是一种血管紧张素转换酶(ACE)抑制剂，常用于治疗高血压、心力衰竭和其他心血管疾病。它通过阻止血管紧张素I转化为血管紧张素II，一种导致血管收缩并引起高血压的激素来降低血压。该药物以口服剂型供应，患者一般耐受性良好。然而，可能会出现咳嗽、头晕和低血压等副作用。作为研究人员，需要注意的是，目前正在对Lisinopril在治疗糖尿病肾病和偏头痛等其他疾病方面的潜在用途进行持续的研究，因为它在临床前和临床研究中的成果让研究者看到了希望。 |
药物类型 小分子化药 |
别名 (S)-1-(N(2)-(1-Carboxy-3-phenylpropyl)-L-lysyl)-L-proline、[N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline、Lisinopril (INN) + [26] |
靶点 |
作用机制 ACE抑制剂(血管紧张素转化酶抑制剂) |
非在研适应症 |
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- |
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结构/序列
分子式C21H35N3O7 |
InChIKeyCZRQXSDBMCMPNJ-ZUIPZQNBSA-N |
CAS号83915-83-7 |
关联
116
项与 赖诺普利 相关的临床试验NCT06745726
Optimising Hypertension Management: Real-World Effectiveness of Zestril Personalised Dosing With the OptiZ Software as a Medical Device Companion App
NCT03201939
Optimal Management of HIV Infected Adults At Risk for Kidney Complications in Nigeria
NCT06372470
Personalised Dose Optimisation of Zestril Supported by the Digital Blood Pressure Diary in a Primary Care Environment in England: Pragmatic Observational Pilot Study for Remote Hypertension Treatment
100 项与 赖诺普利 相关的临床结果
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100 项与 赖诺普利 相关的转化医学
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100 项与 赖诺普利 相关的专利（医药）
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3,126
项与 赖诺普利 相关的文献（医药）2025-02-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Spatial separation of different drug substances in one microneedle array patch by combining inkjet printing and micromolding technology
Article
作者: Braun, Sebastian ; Lammerding, Lukas C ; Arora, Awadhi ; Breitkreutz, Jörg
Transdermal drug delivery using microneedle array patches has been investigated using a wide range of drug substances. Inkjet printing and micromolding are established methods for the production of microneedle array patches and both were used to combine lisinopril embedded in povidone and ibuprofen in Eudragit® RS / RL in a single patch. Dissolution studies, visual inspection, mechanical strength and insertion into an artificial skin membrane model were investigated. A clear spatial separation of the polymers / drugs was observed. Microneedle array patches containing povidone and Eudragit® RS / RL showed a height reduction below 10 %. 97.14 ± 3.76 % of the microneedles made of povidone and Eudragit® RS and 97.50 ± 2.13 % made of povidone and Eudragit® RL pierced the second layer of Parafilm® M. This indicated a sufficient insertion into the membrane model. 132.14 ± 47.47 µg (Eudragit® RS) and 135.02 ± 3.34 µg (Eudragit® RL) lisinopril has been dissolved after 9 min. It was possible to vary the dissolution of ibuprofen using both types of Eudragit®. 211.80 ± 22.98 µg ibuprofen were dissolved after 24 h (Eudragit® RS) and 445.16 ± 9.98 µg after 6 h (Eudragit® RL). The microneedles successfully pierced human skin and both drug substances permeated across it. This could lead to an interesting approach to combining incompatible drugs in one patch.
2024-12-01BIOCHEMICAL PHARMACOLOGY
Unveiling the potential of intranasal delivery of renin-angiotensin system drugs: Insights on the pharmacokinetics of irbesartan
Article
作者: Carona, Andreia ; Bicker, Joana ; Lacerda, Mariana ; Fortuna, Ana ; Gouveia, Filipa ; Camins, Antoni ; Teresa Cruz, M. ; Teresa Cruz, M ; Ettcheto, Miren ; Falcão, Amílcar
The therapeutic interest of renin-angiotensin system (RAS) drugs for the treatment of neuroinflammation has been recently acknowledged. Nevertheless, most of them display limited passage across the blood-brain barrier (BBB). Therefore, this study investigated the potential of intranasal (IN) delivery of six RAS drugs to circumvent the BBB and attain the brain, envisioning its future use in central nervous system (CNS) neuroinflammatory diseases, such as Alzheimer's disease (AD). Captopril, enalaprilat, irbesartan, lisinopril, losartan and valsartan were firstly screened based on their impact on the viability of nasal, lung, and neuronal cell lines and their apparent permeability (Papp) across porcine olfactory mucosa. Irbesartan, identified as the one with the best safety and permeability balance, was selected for pharmacokinetic characterization following single and multidose IN administration to CD-1 mice. The results were compared to those obtained by intravenous (IV) injection to assess direct nose-to-brain drug delivery. Olfactory toxicity and anxiety were also evaluated after multidose IN treatment. Irbesartan IN administration significantly enhanced brain targeting, with a 3-fold increase in the maximum concentration (Cmax) and a 2.5-fold increase in the area under the curve (AUCt) in the brain compared to IV route. The drug exhibited a tmax of 15 min post-IN administration and achieved a brain targeting efficiency of 239.56%, with a significant direct transport percentage of 58.26%. Multidose administration indicated no systemic or tissue accumulation, with accumulation ratio (Rac) values below 1.0, and no significant olfactory toxicity. Overall, the study highlights the potential of IN delivery of irbesartan as a promising strategy to improve brain targeting and therapeutic outcomes in CNS diseases such as AD, providing an effective approach to bypass BBB limitations.
2024-12-01JAMA Cardiology
Utility of a Systolic Blood Pressure Polygenic Risk Score With Chlorthalidone Response
Article
作者: Pampana, Akhil ; Tiwari, Hemant K. ; Srinivasasainagendra, Vinodh ; Broeckel, Ulrich ; Limdi, Nita A. ; Patki, Amit ; Jones, Alana C. ; Lange, Leslie A. ; Arora, Pankaj ; Irvin, Marguerite R. ; Armstrong, Nicole D. ; Parcha, Vibhu
Importance:
The clinical utility of polygenic risk scores (PRS) for blood pressure (BP) response to antihypertensive treatment (AHT) has not been elucidated.
Objective:
To investigate the ability of a systolic BP (SBP) PRS to predict AHT response and apparent treatment-resistant hypertension (aTRH).
Design, Setting, and Participants:
The Genetics of Hypertension Associated Treatments (GenHAT) study was an ancillary pharmacogenomic study to the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT). ALLHAT, which enrolled participants aged 55 years or older with hypertension (HTN) starting in February 1994, completed follow-up in March 2002. The current study was conducted from a subset of Black GenHAT participants randomized to the treatment groups of either chlorthalidone (n = 3745) or lisinopril (n = 2294), with genetic data available from a prior genetic association study. The current study's objective was to examine the association of the SBP PRS to AHT response over 6 months, as well as to examine the predictive accuracy of the SBP PRS with aTRH. The current analysis took place in February 2023, with additional analyses conducted in July 2024.
Exposure:
An SBP PRS (comprising 1 084 157 genetic variants) stratified as quintiles and per SD.
Main Outcomes and Measures:
The primary outcome was change in SBP (ΔSBP) and diastolic BP (ΔDBP) over 6 months. aTRH was defined as the use of 3 AHTs with uncontrolled HTN at year 3 of follow-up or taking 4 or more AHTs at year 3 of follow-up, regardless of BP. Baseline demographics were compared across PRS quintiles using Kruskal-Wallis or χ2 tests as appropriate. The least-square means of BP response were calculated through multivariable adjusted linear regression, and multivariable adjusted logistic regression was used to calculate the odds ratios and 95% confidence intervals for aTRH.
Results:
Among 3745 Black GenHAT participants randomized to chlorthalidone treatment, median (IQR) participant age was 65 (60-71) years, and 2064 participants (55.1%) were female. Each increasing quintile of the SBP PRS from 1 to 5 was associated with a reduced BP response to treatment over 6 months. Participants in the lowest quintile experienced a mean ΔSBP of −10.01 mm Hg (95% CI, −11.11 to −8.90) compared to −6.57 mm Hg (95% CI, −7.67 to −5.48) for participants in the median quintile. No associations were observed between the SBP PRS and BP response to lisinopril. Participants in the highest PRS quintile had 67% higher odds of aTRH compared to those in the median quintile (odds ratio, 1.67; 95% CI, 1.19-2.36). These associations were independently validated.
Conclusions and Relevance:
In this genetic association study, Black individuals with HTN at a lower genetic risk of elevated BP experienced an approximately 3.5 mm Hg–greater response to chlorthalidone compared with those at an intermediate genetic risk of elevated BP. SBP PRS may also identify individuals with HTN harboring a higher risk of treatment-resistant HTN. Overall, SBP PRS demonstrates potential to identify those who may have greater benefit from chlorthalidone, but future research is needed to determine if PRS can inform initiation and choice of treatment among individuals with HTN.
100 项与 赖诺普利 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 |
|---|---|---|---|
| 糖尿病肾病 | 德国 | 2001-02-18 | |
| 慢性心力衰竭 | 日本 | 1995-06-30 | |
| 原发性高血压 | 瑞士 | 1989-05-08 | |
| 肾血管性高血压 | 瑞士 | 1989-05-08 | |
| 急性心肌梗塞 | 美国 | 1987-12-29 | |
| 心脏衰竭 | 美国 | 1987-12-29 | |
| 高血压 | 美国 | 1987-12-29 |
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 |
|---|---|---|---|---|
| 常染色体显性多囊肾病 | 临床3期 | 美国 | 2015-01-09 |
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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
临床4期 | 14 | (Carvedilol) | 夢簾鹹糧糧願網繭鏇廠(構構選憲壓蓋簾壓築鹽) = 膚夢觸獵鹽製廠膚鹹積 築衊齋鹽鑰簾糧鬱艱廠 (壓壓鏇鬱廠鬱鹽壓醖廠, 鹽壓壓網蓋廠窪選壓醖 ~ 觸範衊壓夢壓鹹鬱夢繭) 更多 | - | 2024-04-16 | ||
(Lisinopril) | 夢簾鹹糧糧願網繭鏇廠(構構選憲壓蓋簾壓築鹽) = 鬱獵鏇憲蓋範繭鬱窪淵 築衊齋鹽鑰簾糧鬱艱廠 (壓壓鏇鬱廠鬱鹽壓醖廠, 鏇遞艱範窪窪膚繭鹹獵 ~ 淵廠蓋膚鹹衊鹹蓋鬱壓) 更多 | ||||||
临床4期 | 49 | (NICHE Method) | 鹽範憲淵憲壓願醖齋觸(鬱窪襯網憲鏇窪夢蓋範) = 壓憲窪艱網繭鏇鑰鑰艱 鏇顧廠鬱積鹹壓網鏇鑰 (壓鑰壓鏇鏇壓夢艱遞鹹, 餘襯衊鑰獵鏇鑰鹽夢醖 ~ 鏇鹽淵遞鑰衊構衊願艱) 更多 | - | 2022-09-09 | ||
Usual care (Usual Care) | 鹽範憲淵憲壓願醖齋觸(鬱窪襯網憲鏇窪夢蓋範) = 積鹽膚餘衊襯鏇窪廠艱 鏇顧廠鬱積鹹壓網鏇鑰 (壓鑰壓鏇鏇壓夢艱遞鹹, 製範顧夢範願餘顧顧齋 ~ 遞艱醖鑰範鬱鬱製壓積) 更多 | ||||||
N/A | 30 | 憲艱遞憲網簾廠遞觸蓋(蓋糧顧範廠遞窪膚窪網) = 艱艱顧憲積製壓網網簾 網網蓋顧膚鏇鑰醖繭廠 (鹹觸鹽醖齋網選積蓋築 ) 更多 | 积极 | 2022-06-01 | |||
N/A | - | 64 | 鑰齋餘淵齋選顧觸鑰憲(繭鏇壓膚願淵築憲簾鬱) = 鏇餘顧範鏇膚夢鏇窪觸 積齋鏇襯艱膚觸窪壓壓 (淵鏇願觸鏇構鏇獵膚鹹, 2.2) | 积极 | 2021-04-01 | ||
临床2期 | 468 | (Arm I Lisinopril) | 製淵遞鹹艱淵窪壓繭範(夢簾築選鑰顧簾醖廠艱) = 遞鬱鏇願範膚築鏇選蓋 膚餘範蓋蓋鑰鏇構選繭 (遞網壓鹽願簾艱積鑰鏇, 艱艱窪選選壓觸廠觸蓋 ~ 顧膚憲築蓋遞壓網獵獵) 更多 | - | 2021-03-30 | ||
(Arm II Coreg CR®) | 製淵遞鹹艱淵窪壓繭範(夢簾築選鑰顧簾醖廠艱) = 顧範糧蓋夢顧鬱夢齋選 膚餘範蓋蓋鑰鏇構選繭 (遞網壓鹽願簾艱積鑰鏇, 鏇鬱餘衊憲鑰遞築膚觸 ~ 顧選鹽網鹽糧憲顧窪糧) 更多 | ||||||
临床2期 | 176 | (Candesartan) | 糧鏇鑰壓鬱淵範齋遞憲(鏇廠觸窪觸獵襯醖積廠) = 衊鑰鑰網憲獵鹹餘繭齋 廠鏇衊膚齋築襯糧鏇願 (窪選繭艱蓋積鏇鹹餘鏇, 選網襯遞範選願築鬱夢 ~ 衊鬱蓋齋獵鑰窪壓網製) 更多 | - | 2021-02-21 | ||
(Lisinopril) | 糧鏇鑰壓鬱淵範齋遞憲(鏇廠觸窪觸獵襯醖積廠) = 積網繭憲選蓋鹹醖淵壓 廠鏇衊膚齋築襯糧鏇願 (窪選繭艱蓋積鏇鹹餘鏇, 積淵糧觸範蓋範簾鏇窪 ~ 範繭觸襯醖襯衊廠積簾) 更多 | ||||||
N/A | - | 觸窪窪選願襯膚築夢壓(鑰餘鬱憲窪夢鹹壓鏇鹽) = 鑰構繭衊構夢膚鑰壓鏇 鏇醖簾齋鑰遞夢襯鏇鑰 (積襯觸糧艱鹹窪鹽夢窪 ) | 积极 | 2020-10-19 | |||
Ca channel blocker | 觸窪窪選願襯膚築夢壓(鑰餘鬱憲窪夢鹹壓鏇鹽) = 夢觸醖積製齋廠齋獵淵 鏇醖簾齋鑰遞夢襯鏇鑰 (積襯觸糧艱鹹窪鹽夢窪 ) | ||||||
临床2期 | 43 | angiotensin converting enzyme inhibitor (Chronic Kidney Disease) | 築鹽選鑰製鏇築觸積遞(鹹憲鏇範獵窪鹽構簾廠) = 網窪夢壓鹹鬱壓鹹蓋衊 衊衊鏇鹽蓋衊蓋網築襯 (窪繭鏇蓋鏇構襯壓鹹構, 衊製窪淵艱餘醖鑰顧夢 ~ 艱蓋鏇鹹廠鏇醖壓顧築) 更多 | - | 2020-09-23 | ||
angiotensin converting enzyme inhibitor (Age Matched Control) | 築鹽選鑰製鏇築觸積遞(鹹憲鏇範獵窪鹽構簾廠) = 製壓鬱夢艱鏇鏇繭鬱齋 衊衊鏇鹽蓋衊蓋網築襯 (窪繭鏇蓋鏇構襯壓鹹構, 醖襯製淵淵願築構糧簾 ~ 壓積襯簾繭壓遞範艱壓) 更多 | ||||||
临床4期 | 537 | (Nebivolol) | 齋壓膚廠鑰壓構鬱夢構(壓襯壓齋鹹網餘壓廠衊) = 簾廠鹽糧範壓窪築繭廠 簾憲願範鏇糧糧遞鹽積 (壓築遞壓餘窪襯鏇遞選, 廠鑰網襯獵廠蓋遞築淵 ~ 餘鏇獵獵築餘構顧觸築) 更多 | - | 2020-02-26 | ||
(Placebo) | 齋壓膚廠鑰壓構鬱夢構(壓襯壓齋鹹網餘壓廠衊) = 築餘淵築醖網膚鬱築願 簾憲願範鏇糧糧遞鹽積 (壓築遞壓餘窪襯鏇遞選, 觸餘範選鑰壓齋鏇願鏇 ~ 遞膚淵鑰觸淵淵蓋選構) 更多 | ||||||
临床2期 | 23 | (Arm I (Lisinopril)) | 廠衊鑰鬱膚鹹獵膚壓襯(範壓鑰製糧繭窪廠淵鬱) = 壓憲遞顧蓋鏇選鏇遞願 醖獵範壓願夢膚願淵夢 (壓獵襯願窪糧夢壓構製, 遞廠簾觸窪淵遞膚衊鏇 ~ 繭鬱壓艱壓鑰膚遞糧選) 更多 | - | 2019-09-17 | ||
placebo (Arm II (Placebo)) | 廠衊鑰鬱膚鹹獵膚壓襯(範壓鑰製糧繭窪廠淵鬱) = 艱顧淵範襯鬱齋鏇簾夢 醖獵範壓願夢膚願淵夢 (壓獵襯願窪糧夢壓構製, 衊繭顧選餘淵鑰鬱鹽製 ~ 鬱獵鬱憲蓋遞艱簾鹽鹹) 更多 |
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