Double Blind, Randomized, Parallel Group, Multicentre Study to Evaluate the Effects of Manidipine 20 MG Vs. Amlodipine 10 MG and the Combination of Manidipine 10 MG Plus Delapril 30 MG Vs. Amlodipine 5 MG Plus Delapril 30 MG on Intraglomerular Pressure in Hypertensive Patients

Eight-week multi-national, multicenter, randomized, double blind, active control, two arms, parallel groups study with a 4-week single drug treatment (manidipine or amlodipine) phase followed by a 4-week combination treatment (manidipine + delapril or amlodipine + delapril) phase.

开始日期2007-11-01

申办/合作机构

Friedrich Alexander Universität Erlangen Nürnberg

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100 项与盐酸地拉普利相关的临床结果

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100 项与盐酸地拉普利相关的转化医学

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100 项与盐酸地拉普利相关的专利（医药）

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143

项与盐酸地拉普利相关的文献（医药）

2023-06-15·Toxicology 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.

2022-09-15·Maedica - A Journal of Clinical Medicine

The Effect of Commonly Used Fixed-Dose Single Pill Combinations of Renin-Angiotensin-System Blockers and Calcium Channel Blockers on HOMA-IR Index in Hypertensive Patients with Impaired Fasting Glucose: a 12-Week Randomized Open-Label Prospective Study

作者: Anastasiou, Georgia ; Liamis, George ; Elisaf, Moses ; Bakogiannis, Konstantinos ; Adamidis, Petros-Spyridon ; Liontos, Angelos ; Liberopoulos, Evangelos ; Milionis, Haralampos ; Biros, Dimitrios ; Papagiannopoulos, Christos

Backround: The effect of antihypertensive drugs on glucose homeostasis and insulin resistance remains an issue under investigation. There is evidence that renin-angiotensin system (RAS) blockers may favorably affect glucose metabolism, while treatment with calcium channel blockers (CCBs) is considered to have an overall neutral metabolic effect. However, the effects on glycemic indices may differ among agents within the same class of antihypertensive drugs. Objective: To evaluate the effects of different fixed-dose single pill combinations of RAS blockers with CCBs on homeostatic model assessment for insulin resistance (HOMA-IR). Methods: Drug-naive patients with arterial hypertension (AH) and impaired fasting glucose (IFG) were randomly allocated to open-label fixed, single pill combinations of valsartan 160 mg/day plus amlodipine 5 mg/day (VAL/AMLO group, n = 54), delapril 30 mg/day and manidipine 10 mg/day (DEL/MANI group, n = 53) or telmisartan 80 mg/day and amlodipine 5 mg/day (TEL/AMLO group, n = 51) for 12 weeks. Glycemic indices and HOMA-IR were determined at baseline and post-treatment. Results: A total of 158 patients were included. All treatment combinations effectively reduced blood pressure (systolic and diastolic) to similar levels (all p < 0.001). A decrease in the HOMA-IR index by 22.55% (p < 0.01) was noted following treatment with TEL/AMLO, while an increase by 1.4% (p = 0.57) and 12.65% (p = 0.072) was observed in the VAL/AMLO group and the DEL/MANI group, respectively. These changes were significantly different between TEL/AMLO and DEL/MANI (p < 0.05) as well as between TEL/AMLO and VAL/AMLO (p < 0.001). Conclusions: Despite similar antihypertensive action, the effect of fixed, single pill combinations with TEL/AMLO, VAL/AMLO and DEL/MANI on insulin resistance is in favor of TEL/AMLO. Trial registration: The study protocol was published online in https://diavgeia.gov.gr/ (No: ΒΘ6Σ46906Η-ΑΕΣ) via the Ministry of Digital Governance, after receiving approval from the Scientific Council and Administrative Council of University Hospital of Ioannina (No. of approval: 1/12-06-2014 (issue 150). https://diavgeia.gov.gr/decision/view/%CE%92%CE%986%CE%A346906%CE%97- %CE%91%CE%95%CE%A3 https://diavgeia.gov.gr/doc/%CE%92%CE%986%CE%A346906%CE%97- %CE%91%CE%95%CE%A3?inline=true

2021-12-12·Journal of Biomolecular Structure and Dynamics

Molecular docking, molecular dynamics simulations and reactivity, studies on approved drugs library targeting ACE2 and SARS-CoV-2 binding with ACE2

Article

作者: Khelfaoui, Hadjer ; Saleh, Basil A. ; Harkati, Dalal

The recent new contagion coronavirus 2019 (COVID-19) disease is a new generation of severe acute respiratory syndrome coronavirus-2 SARS-CoV-2 which infected millions confirmed cases and hundreds of thousands death cases around the world so far. Molecular docking combined with molecular dynamics is one of the most important tools of drug discovery and drug design, which it used to examine the type of binding between the ligand and its protein enzyme. Global reactivity has important properties, which enable chemists to understand the chemical reactivity and kinetic stability of compounds. In this study, molecular docking and reactivity were applied for eighteen drugs, which are similar in structure to chloroquine and hydroxychloroquine, the potential inhibitors to angiotensin-converting enzyme (ACE2). Those drugs were selected from DrugBank. The reactivity, molecular docking and molecular dynamics were performed for two receptors ACE2 and [SARS-CoV-2/ACE2] complex receptor in two active sites to find a ligand, which may inhibit COVID-19. The results obtained from this study showed that Ramipril, Delapril and Lisinopril could bind with ACE2 receptor and [SARS-CoV-2/ACE2] complex better than chloroquine and hydroxychloroquine. This new understanding should help to improve predictions of the impact of such alternatives on COVID-19.Communicated by Ramaswamy H. Sarma.

100 项与盐酸地拉普利相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01667	盐酸地拉普利	C09AA12	DB13312

研发状态

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适应症	国家/地区	公司	日期
心脏衰竭	意大利	CHIESI Farmaceutici SpA	2000-09-27
高血压	菲律宾	-	1995-03-02
肾血管性高血压	日本	Takeda Pharmaceutical Co., Ltd.	1989-04-01

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
高血压	临床2期	瑞士	Takeda Pharmaceutical Co., Ltd.	-
心脏衰竭	临床前	日本	Takeda Pharmaceutical Co., Ltd.	-
高血压	临床前	瑞士	Takeda Pharmaceutical Co., Ltd.	-

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


DEMAND (ASN2010)	N/A	2型糖尿病 albuminuria	380	Manidipine+Delapril	鹹積鑰網製廠衊壓積網(網鑰鹽壓壓餘廠觸構鑰) = was stable on combined therapy 鑰顧願鏇壓夢網簾糧網 (窪蓋夢糧艱選選壓壓淵 ) 更多	积极	2010-11-16
				Delapril