更新于：2024-11-08
Imidapril Hydrochloride
盐酸咪达普利
更新于：2024-11-08
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (1993-10-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C20H28ClN3O6 |
InChIKeyLSLQGMMMRMDXHN-GEUPQXMHSA-N |
CAS号89396-94-1 |
关联
13
项与 盐酸咪达普利 相关的临床试验盐酸咪达普利片在健康受试者中的随机、开放、两制剂、单次给药、部分重复/双交叉的空腹/餐后生物等效性研究
盐酸咪达普利片在健康受试者中的随机、开放、两制剂、单次给药、部分重复/双交叉的空腹/餐后生物等效性研究
The effects of imidapril on aspiration and naso-pharyngeal reflux - The effects of imidapril on aspiration and naso-pharyngeal reflux
100 项与 盐酸咪达普利 相关的临床结果
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100 项与 盐酸咪达普利 相关的转化医学
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100 项与 盐酸咪达普利 相关的专利（医药）
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274
项与 盐酸咪达普利 相关的文献（医药）2023-09-01Chemical & pharmaceutical bulletin
Potential Interaction between Sodium Polystyrene Sulfonate and Prescription Drugs in Artificial Intestinal Juice
Article
作者: Uematsu, Yugo ; Ogata, Fumihiko ; Kawasaki, Naohito ; Nishida, Kyohei ; Mizuno, Yuri
This study evaluated the interaction between sodium polystyrene sulfonate (SPS) and several commonly used concomitant drugs, such as carvedilol, bisoprolol, imidapril, atorvastatin and azilsartan. The residual rate of adsorption 6 h after starting the experiment followed the order carvedilol (0.36%) < bisoprolol (19.7%) < imidapril (81.2%) < atorvastatin (86.5%) < azilsartan (87.9%) in artificial intestinal juice (pH 6.8). In addition, the pKa of carvedilol and bisoprolol was 8.0 and 9.6 and that of atorvastatin, azilsartan, and imidapril was 4.5, 6.1, and 2.4, respectively. These results indicate that the form (ionic or uncharged) of each drug is important to its reaction with SPS. Moreover, we demonstrated the effect of potassium ions (concentration of 1000 or 2000 mg/L) on the adsorption of concomitant drugs onto SPS in artificial intestinal juice. Our results show that the residual rate of adsorption of carvedilol and bisoprolol increases with increasing concentration of potassium ions whereas adsorption of potassium ions onto SPS was unaffected by carvedilol and bisoprolol under our experimental conditions. Finally, the obtained results revealed that interactions between SPS and carvedilol or bisoprolol readily occur in artificial intestinal juice.
2023-06-15Toxicology and applied pharmacology
In silico and in vitro screening for carcinogenic potential of angiotensin-converting enzyme inhibitors and their degradation impurities.
Article
作者: Regulska, Katarzyna ; Mikolajczyk, Aleksandra ; Matera-Witkiewicz, Agnieszka ; Stanisz, Beata J.
According to some clinical observations, the use of angiotensin-converting enzyme inhibitors (ACEI) may be associated with an increased risk of cancer. The aim of the present study was to screen for the potential carcinogenicity, mutagenicity and genotoxicity of these drugs using in silico methodology. Delapril, enalapril, imidapril, lisinopril, moexipril, perindopril, ramipril, trandolapril, spirapril were thereby analyzed. In parallel, the corresponding degradation impurities, the diketopiperazine (DKP) derivatives, were also investigated. (Q)SAR computer software (VEGA-GUI and Lazar), available in the public domain, was employed. The obtained predictions suggested that none of the compounds tested (from the group of ACE-Is and DKPs) was mutagenic. Moreover, none of the ACE-Is was carcinogenic. The reliability of these predictions was high to moderate. In contrast, in the DKP group, ramipril-DKP and trandolapril-DKP were found to be potentially carcinogenic, but the reliability of this prediction was low. As for the genotoxicity screening, all compounds tested (ACE-I and DKP) were predicted to be active and genotoxic, with moexipril, ramipril, spirapril, and all DKP derivatives within the highest risk group. They were prioritized for experimental verification studies to confirm or exclude their toxic activity. On the other hand, the lowest risk of carcinogenicity was assigned to imidapril and its DKP. Then, a follow-up in vitro micronucleus assay for ramipril was performed. It showed that this drug was genotoxic via aneugenic activity, but only at concentrations exceeding real-life levels. At concentrations found in human blood after standard dose, ramipril was not genotoxic in vitro. Therefore, ramipril was considered safe for human use with a standard dosing regimen. The other compounds of concern (spirapril, moexipril and all DKP derivatives) should be subjected to analogous in vitro studies. We also concluded that the adopted in silico software was applicable for ACE-I toxicity prediction.
2021-05-01Atherosclerosis2区 · 医学
Bleeding associated with co-administration of clopidogrel and ACEi in patients undergoing PCI and DAPT
2区 · 医学
Article
作者: Chi-Ching Kuo ; Victor Chien-Chia Wu ; Chang-Fu Kuo ; Hui-Tzu Tu ; Chun-Li Wang ; Shang-Hung Chang ; Yu-Tung Huang ; Ming-Shien Wen ; Shao-Wei Chen
BACKGROUND AND AIMS:
The coprescription of an angiotensin-converting enzyme inhibitor (ACEi) with clopidogrel reportedly increases bleeding risk. However, studies have not described such an increase in cases of dual antiplatelet therapy (DAPT) after percutaneous coronary intervention (PCI).
METHODS:
We analyzed electronic medical records of patients with discharge records of having undergone DAPT after PCI from a national health insurance claims database for January 1, 2006 to December 31, 2014. The date of PCI was the index date, and the primary outcome was major bleeding. The unit of analysis was one person-quarter. We compared patients who were prescribed with those not prescribed an ACEi in the cohort. A Poisson model with inverse probability of treatment weighting was fitted using generalized estimating equations to measure the risk of outcomes.
RESULTS:
In total, 193,258 patients underwent DAPT after PCI; 46% had a coprescription of an ACEi. After screening, 170,775 patients (479,263 person-quarters) remained for analysis. The mean patient age was 65 ± 13 years, and 73.43% were men. In total, 79,739 prescriptions of an ACEi were written: 57%, 14.21%, 8.88%, 7.17%, and 4.68% were for captopril, ramipril, enalapril, perindopril, and imidapril, respectively. A concomitant prescription of an ACEi with clopidogrel was not associated with increased bleeding risk (adjusted rate ratio: 1.08, 99% confidence interval: 0.99-1.17).
CONCLUSIONS:
The coadministration of an ACEi with clopidogrel after PCI is common. In this real-world cohort study, such coadministration was not associated with an increased risk of major bleeding in patients undergoing DAPT after PCI.
100 项与 盐酸咪达普利 相关的药物交易
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 糖尿病肾病 | 日本 | 2002-01-17 | |
| 高血压 | 日本 | 1993-10-01 |
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