Abstract
Decarboxylation, reduction and hydrolysis can yield active metabolites from the parent drug. Major therapeutic indications and metabolic routes of these drugs are reviewed.
Changes in the logP values (determined and calculated) from the parent drug to the active metabolite show certain characteristics in comparison to other phase I metabolic alterations. Metabolic decarboxylation of parent drug is commonly associated with increase in lipophilicity. However, in some cases, decarboxylation may cause a reduction in lipophilicity. Ester hydrolysis generally unmasks either the polar carboxylic or hydroxyl group with the outcome of an increase in hydrophilicity. On the contrary, hydrolysis of phosphate ester means a huge increase in the lipophilic character of the drug, as the highly polar phosphate group is removed.
Keywords: Active metabolites, metabolic decarboxylation, metabolic reduction and metabolic hydrolysis, Parent Drugs, Idarubicin, Prontosil, lipophilicity, half-life
Current Drug Metabolism
Title:Active Metabolites Resulting from Decarboxylation, Reduction and Ester Hydrolysis of Parent Drugs
Volume: 13 Issue: 6
Author(s): I. Hartyanszky, H. Kalasz, E. Adeghate, Zs. Gulyas, M. Y. Hasan, K. Tekes, A. Adem and P. Sotonyi
Affiliation:
Keywords: Active metabolites, metabolic decarboxylation, metabolic reduction and metabolic hydrolysis, Parent Drugs, Idarubicin, Prontosil, lipophilicity, half-life
Abstract: Decarboxylation, reduction and hydrolysis can yield active metabolites from the parent drug. Major therapeutic indications and metabolic routes of these drugs are reviewed.
Changes in the logP values (determined and calculated) from the parent drug to the active metabolite show certain characteristics in comparison to other phase I metabolic alterations. Metabolic decarboxylation of parent drug is commonly associated with increase in lipophilicity. However, in some cases, decarboxylation may cause a reduction in lipophilicity. Ester hydrolysis generally unmasks either the polar carboxylic or hydroxyl group with the outcome of an increase in hydrophilicity. On the contrary, hydrolysis of phosphate ester means a huge increase in the lipophilic character of the drug, as the highly polar phosphate group is removed.
Export Options
About this article
Cite this article as:
Hartyanszky I., Kalasz H., Adeghate E., Gulyas Zs., Y. Hasan M., Tekes K., Adem A. and Sotonyi P., Active Metabolites Resulting from Decarboxylation, Reduction and Ester Hydrolysis of Parent Drugs, Current Drug Metabolism 2012; 13 (6) . https://dx.doi.org/10.2174/138920012800840437
DOI https://dx.doi.org/10.2174/138920012800840437 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
Call for Papers in Thematic Issues
Interaction between drugs and endocrine diseases
The introduction of highly active antiretroviral therapy accelerated studies and our understanding on the interaction between pharmacological therapies and endocrine diseases. Drugs can precipitate endocrine via different mechanisms, including direct alteration of hormone production and secretion, dysregulation of hormonal axis, effects on hormonal transport, receptor-binding, and cellular signalling. Common drug-induced ...read more
Tissue Distribution and Metabolism of Micro- and Nanoparticles and Medical Implants
With the continuous advancement of modern science and engineering, numerous functional materials and active molecules have been developed and utilized in various industrial, medical, and food applications. Many of these can enter the body, either actively or passively, and have significant and intricate impacts on human health. For example, biomaterials ...read more
Related Journals
- 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
-
Arterial Duct Stenting in Congenital Heart Disease with Duct-Dependent Pulmonary Circulation
Current Pediatric Reviews Platelet-Derived Chemokines in Atherogenesis: What’s New?
Current Vascular Pharmacology Antifungal Therapy of Aspergillosis of the Central Nervous System and Aspergillus Endophthalmitis
Current Pharmaceutical Design A Review of the English and Russian Language Literature on the Osteoarticular Manifestations of Brucellosis Infection
Current Rheumatology Reviews Antithrombotic Therapy in Cardiac Embolism
Current Cardiology Reviews Prosthetic Valve Endocarditis: Diagnostic Approach and Treatment Options
Cardiovascular & Hematological Disorders-Drug Targets Synthesis, Structure and Antibacterial Evaluation of Some N-substituted 3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamides
Medicinal Chemistry Systemic Inflammatory Response as a Risk and Prognosis Factor in Ventilator-Associated Pneumonia
Current Respiratory Medicine Reviews Editorial [Hot topic: Infective Endocarditis (Guest Editor: Ioannis Starakis)]
Infectious Disorders - Drug Targets Disseminated TB in an Immunocompetent Patient: A Case Report
Infectious Disorders - Drug Targets Rashes, Sniffles, and Stroke: A Role for Infection in Ischemic Stroke of Childhood
Infectious Disorders - Drug Targets Prevalence of Nasal Colonization with Staphylococcus aureus in Patients with Rheumatoid Arthritis
Current Rheumatology Reviews New Developments in Antimicrobial Use in Sepsis
Current Pharmaceutical Design Cardiovascular Imaging in Thromboembolic Risk Stratification for Atrial Fibrillation: Recent Patents and Current Practice
Recent Patents on Medical Imaging ARC - Augmented Renal Clearance
Current Pharmaceutical Biotechnology The Use of Phages for the Removal of Infectious Biofilms
Current Pharmaceutical Biotechnology Levosimendan: A New Inodilatory Drug for the Treatment of Decompensated Heart Failure
Current Pharmaceutical Design Therapeutic Potential of γ -Secretase Inhibitors and Modulators
Current Topics in Medicinal Chemistry Current Indications for Infective Endocarditis Antibiotic Prophylaxis
Infectious Disorders - Drug Targets Kawasaki Disease and Its Treatment – An Update
Current Rheumatology Reviews