Abstract
The development of drugs which block the renin-angiotensin system (RAS) has been proven a major advance in cardiovascular medicine. Angiotensin converting enzyme (ACE) inhibitors, which block the formation of angiotensin II from the inactive angiotensin I, are widely used as first line treatment in hypertension, heart failure and diabetic nephropathy. More recently, selective antagonists of the angiotensin type-1 receptor (AT1R) have become available for clinical use. Accumulating evidence suggests that AT1R antagonists have similar effects to ACE inhibitors in hypertension, heart failure and diabetic nephropathy. Although ACE inhibitors and AT1R antagonists block the same system, experimental evidence suggest that their mechanisms of action differ in several respects, such as increased bradykinin and angiotensin 1-7 levels with ACE inhibitors and AT2R activation with AT 1R antagonists. Nevertheless, the clinical significance of these differences remains largely unknown and, in practice, the only clear advantage of AT1R antagonists over ACE inhibitors is the absence of cough as a side effect. Recent clinical data suggest that combined ACE inhibition and AT1R antagonism offer additive effects in reducing blood pressure in hypertension, in reducing proteinuria in nephropathy and in improving prognosis in heart failure. Further evidence suggests that some hypertensive patients may have a good antihypertensive response with ACE inhibition but not with AT1R antagonism, or the reverse. These data suggest that these two drug classes have important similarities, because they act on the same system, but they also appear to have important differences, which are not only of theoretical but also of clinical importance.
Keywords: Renin-angiotensin, AT1R antagonism, antihypertensive, nephropathy
Current Topics in Medicinal Chemistry
Title: Renin-angiotensin System Blockade at the Level of the Angiotensin Converting Enzyme or the Angiotensin Type-1 Receptor: Similarities and Differences
Volume: 4 Issue: 4
Author(s): George S. Stergiou and Irini I. Skeva
Affiliation:
Keywords: Renin-angiotensin, AT1R antagonism, antihypertensive, nephropathy
Abstract: The development of drugs which block the renin-angiotensin system (RAS) has been proven a major advance in cardiovascular medicine. Angiotensin converting enzyme (ACE) inhibitors, which block the formation of angiotensin II from the inactive angiotensin I, are widely used as first line treatment in hypertension, heart failure and diabetic nephropathy. More recently, selective antagonists of the angiotensin type-1 receptor (AT1R) have become available for clinical use. Accumulating evidence suggests that AT1R antagonists have similar effects to ACE inhibitors in hypertension, heart failure and diabetic nephropathy. Although ACE inhibitors and AT1R antagonists block the same system, experimental evidence suggest that their mechanisms of action differ in several respects, such as increased bradykinin and angiotensin 1-7 levels with ACE inhibitors and AT2R activation with AT 1R antagonists. Nevertheless, the clinical significance of these differences remains largely unknown and, in practice, the only clear advantage of AT1R antagonists over ACE inhibitors is the absence of cough as a side effect. Recent clinical data suggest that combined ACE inhibition and AT1R antagonism offer additive effects in reducing blood pressure in hypertension, in reducing proteinuria in nephropathy and in improving prognosis in heart failure. Further evidence suggests that some hypertensive patients may have a good antihypertensive response with ACE inhibition but not with AT1R antagonism, or the reverse. These data suggest that these two drug classes have important similarities, because they act on the same system, but they also appear to have important differences, which are not only of theoretical but also of clinical importance.
Export Options
About this article
Cite this article as:
Stergiou S. George and Skeva I. Irini, Renin-angiotensin System Blockade at the Level of the Angiotensin Converting Enzyme or the Angiotensin Type-1 Receptor: Similarities and Differences, Current Topics in Medicinal Chemistry 2004; 4 (4) . https://dx.doi.org/10.2174/1568026043451320
DOI https://dx.doi.org/10.2174/1568026043451320 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Renal Injury Following Intravitreal Anti-VEGF Administration in Diabetic Patients with Proliferative Diabetic Retinopathy and Chronic Kidney Disease - A Possible Side Effect?
Current Drug Safety Taurine-Diabetes Interaction: From Involvement to Protection
Current Diabetes Reviews Ex Vivo Gene Transfer for Improvement of Transplanted Pancreatic Islet Viability and Function
Current Pharmaceutical Design Pleiotropic Effects of Fenofibrate
Current Pharmaceutical Design Midkine: A Promising Molecule for Drug Development to Treat Diseases of the Central Nervous System
Current Pharmaceutical Design Role of Forkhead Transcription Factors of the O Class (FoxO) in Development and Progression of Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets Arterial Hypertension and Kidney Circulation
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Effect of Rosuvastatin on Non-alcoholic Steatohepatitis in Patients with Metabolic Syndrome and Hypercholesterolaemia: A Preliminary Report
Current Vascular Pharmacology Assessing Outcome of Diabetic Foot Ulcers and Multidisciplinary Foot Clinic
Current Diabetes Reviews Aliphatic and Aromatic Oxidations, Epoxidation and S-Oxidation of Prodrugs that Yield Active Drug Metabolites
Current Medicinal Chemistry Recent Studies of Aldose Reductase Enzyme Inhibition for Diabetic Complications
Current Medicinal Chemistry Simultaneous Assessment of MicroRNAs 126 and 192 in Diabetic Nephropathy Patients and the Relation of these MicroRNAs with Urinary Albumin
Current Molecular Medicine Biomarkers Determining Cardiovascular Risk in Patients with Kidney Disease
Current Medicinal Chemistry Oxidative Stress in Cardiovascular Disease: A New Avenue Toward Future Therapeutic Approaches
Recent Patents on Cardiovascular Drug Discovery The Application of Micro-Analytical Techniques to Biomedical Analysis
Current Pharmaceutical Analysis Matrix Metalloproteinases: New Routes to the Use of MT1-MMP As A Therapeutic Target in Angiogenesis-Related Disease
Current Pharmaceutical Design Curcumin: A Potential Neuroprotective Agent in Parkinson's Disease
Current Pharmaceutical Design Endocrinological Aspects of Proteinuria and Podocytopathy in Diabetes: Role of the Aldosterone/Mineralocorticoid Receptor System
Current Diabetes Reviews Managing Comorbidity in COPD: A Difficult Task
Current Drug Targets Curcumin: A Natural Product for Diabetes and its Complications
Current Topics in Medicinal Chemistry