Abstract
Artemisinin and its derivatives were discovered to be highly effective antimalarial drugs, which combine potent, rapid antimalarial activity with a wide therapeutic index and an absence of clinically important resistance. Artemisinins as a group are poorly efficacious at curing malaria as monotherapy. However, this shortfall is being overcome by using oral artemisinin-based combination therapy (ACT) and intravenous artesunate (AS) in sequential administration with slower acting antimalarial drugs. Pharmacokinetic and pharmacodynamic (PK/PD) evaluations demonstrate that the rapid efficacy of artemisinins is principally due to the drug peak concentration (Cmax), and other pharmacokinetic parameters, such as drug exposure level (AUC) and drug exposure time (half-life) tend to be of minor significance. The evaluation also demonstrated that AS is a superior in PK/PD achievements either following oral or intravenous administration when compared to other four artemisinin drugs. Most recently, a decrease in mortality (34.7%) has been demonstrated in a large study using intravenous AS, as opposed to the standard of care quinine injection. The fast efficacy and less mortality show that current artemisinins have great advantage over other antimalarials in ACTs for uncomplicated malaria and in sequential therapy of AS injection for severe and complicated malaria.
Keywords: Artemisinin, artesunate, dihydroartemisinin, arteether, artemether, artelinate, pharmacokinetics, pharmacodynamics, efficacy
Current Drug Therapy
Title: Pharmacokinetic and Pharmacodynamic Profiles of Rapid-Acting Artemisinins in the Antimalarial Therapy
Volume: 2 Issue: 3
Author(s): Qigui Li, Peter J. Weina and Wilbur K. Milhous
Affiliation:
Keywords: Artemisinin, artesunate, dihydroartemisinin, arteether, artemether, artelinate, pharmacokinetics, pharmacodynamics, efficacy
Abstract: Artemisinin and its derivatives were discovered to be highly effective antimalarial drugs, which combine potent, rapid antimalarial activity with a wide therapeutic index and an absence of clinically important resistance. Artemisinins as a group are poorly efficacious at curing malaria as monotherapy. However, this shortfall is being overcome by using oral artemisinin-based combination therapy (ACT) and intravenous artesunate (AS) in sequential administration with slower acting antimalarial drugs. Pharmacokinetic and pharmacodynamic (PK/PD) evaluations demonstrate that the rapid efficacy of artemisinins is principally due to the drug peak concentration (Cmax), and other pharmacokinetic parameters, such as drug exposure level (AUC) and drug exposure time (half-life) tend to be of minor significance. The evaluation also demonstrated that AS is a superior in PK/PD achievements either following oral or intravenous administration when compared to other four artemisinin drugs. Most recently, a decrease in mortality (34.7%) has been demonstrated in a large study using intravenous AS, as opposed to the standard of care quinine injection. The fast efficacy and less mortality show that current artemisinins have great advantage over other antimalarials in ACTs for uncomplicated malaria and in sequential therapy of AS injection for severe and complicated malaria.
Export Options
About this article
Cite this article as:
Li Qigui, Weina J. Peter and Milhous K. Wilbur, Pharmacokinetic and Pharmacodynamic Profiles of Rapid-Acting Artemisinins in the Antimalarial Therapy, Current Drug Therapy 2007; 2 (3) . https://dx.doi.org/10.2174/157488507781695649
DOI https://dx.doi.org/10.2174/157488507781695649 |
Print ISSN 1574-8855 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3903 |
Call for Papers in Thematic Issues
Novel Therapeutic Approaches and Biomarkers for Chronic Kidney Disease (CKD)
The thematic issue on "Novel Therapeutic Approaches and Biomarkers for CKD" aims to provide a comprehensive exploration of cutting-edge strategies for the management of chronic kidney disease (CKD). This issue will delve into emerging therapeutic targets, focusing on critical aspects such as podocyte injury, endothelial dysfunction, and tubulointerstitial fibrosis, which ...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
Related Articles
-
A Review of Preclinical Experiments Toward Targeting M2 Macrophages in Prostate Cancer
Current Drug Targets Germ Cell Apoptosis: Relevance to Infertility and Contraception
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Current Advances on Different Kinases Involved in Tau Phosphorylation, and Implications in Alzheimers Disease and Tauopathies
Current Alzheimer Research The Effect of Modified-Release Ketoconazole on Insulin Resistance in Patients with Severe Metabolic Syndrome
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Recent Advances in Antigen-Based Generation of Monoclonal Antibodies
Current Immunology Reviews (Discontinued) Biomedical Applications of Zinc Oxide Nanomaterials
Current Molecular Medicine Metabolic Routes in Inflammation: The Citrate Pathway and its Potential as Therapeutic Target
Current Medicinal Chemistry Dihydrotestosterone Induces Chemo-Resistance of Triple-Negative Breast MDA-MB-231 Cancer Cells Towards Doxorubicin Independent of ABCG2 and miR-328-3p
Current Molecular Pharmacology Progress of Oral Insulin and Related Drug Delivery Systems and their Pharmacokinetics
Current Drug Metabolism Development of Repaglinide Loaded Solid Lipid Nanocarrier: Selection of Fabrication Method
Current Drug Delivery Poor Response to Antiplatelet Drugs. An Important Issue in Drug-Eluting Stents.
Current Clinical Pharmacology Acknowledgements to Reviewers
Endocrine, Metabolic & Immune Disorders - Drug Targets Meet Our Editorial Board Member
Current Aging Science Immune Aging and Autoimmune Diseases in Children
Current Immunology Reviews (Discontinued) Perforated One Anastomosis Gastric Bypass, How we Managed and Review of Literature
New Emirates Medical Journal Expression and Function of Cytochrome P450 in Brain Drug Metabolism
Current Drug Metabolism Processed Foods, Dysbiosis, Systemic Inflammation, and Poor Health
Current Nutrition & Food Science Plant Coumestans: Recent Advances and Future Perspectives in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Immunology Behind Tumors: A Mini Review
Current Cancer Therapy Reviews Melittin: A Natural Peptide with Expanded Therapeutic Applications
The Natural Products Journal