Abstract
Olprinone, a phosphodiesterase (PDE) 3 inhibitor, is used to treat heart failure due to its positive inotropic and vasodilative effects. Selective inhibition of the PDE 3 isozyme increases intracellular adenosine 35-cyclic monophosphate and enhances Ca2+ influx into cardiac muscle cells. The most significant advantage of PDE 3 inhibitors is their ability not only to enhance myocardial contraction, but to reduce, through vasodilatory action, the stress to which the heart is subjected. In peripheral vessels, the decrease of cytosolic free Ca2+ induces the vasorelaxation of vascular smooth muscle cells. In this way, olprinone reduces mean aortic and pulmonary artery pressures. Additionally, olprinone exerts differential vasodilatory effects on peripheral vessels in each organ, based on the differences in the distribution of PDE 3 among the organs. With respect to the cerebral circulation, olprinone augments blood flow in the cerebral cortex through direct vasodilatory effects on small cerebral arter ies or arterioles. Olprinone increases hepatosplanchnic blood flow and improves oxygen supply. While long-term therapy with PDE 3 inhibitors in patients with chronic heart failure may accelerate the progress of the underlying disease and provoke serious ventricular arrhythmia, olprinone shows good potential for short-term treatment in patients who have experienced severe heart failure or patients who have undergone cardiac surgery.
Keywords: Phosphodiesterase 3 inhibitor, olprinone, cardiac function, cerebral circulation, arterial distensibility, renal function, splanchnic circulation, bronchodilator
Current Vascular Pharmacology
Title: The Effects of Olprinone, a Phosphodiesterase 3 Inhibitor, on Systemic and Cerebral Circulation
Volume: 4 Issue: 1
Author(s): Takashi Ueda and Katsufumi Mizushige
Affiliation:
Keywords: Phosphodiesterase 3 inhibitor, olprinone, cardiac function, cerebral circulation, arterial distensibility, renal function, splanchnic circulation, bronchodilator
Abstract: Olprinone, a phosphodiesterase (PDE) 3 inhibitor, is used to treat heart failure due to its positive inotropic and vasodilative effects. Selective inhibition of the PDE 3 isozyme increases intracellular adenosine 35-cyclic monophosphate and enhances Ca2+ influx into cardiac muscle cells. The most significant advantage of PDE 3 inhibitors is their ability not only to enhance myocardial contraction, but to reduce, through vasodilatory action, the stress to which the heart is subjected. In peripheral vessels, the decrease of cytosolic free Ca2+ induces the vasorelaxation of vascular smooth muscle cells. In this way, olprinone reduces mean aortic and pulmonary artery pressures. Additionally, olprinone exerts differential vasodilatory effects on peripheral vessels in each organ, based on the differences in the distribution of PDE 3 among the organs. With respect to the cerebral circulation, olprinone augments blood flow in the cerebral cortex through direct vasodilatory effects on small cerebral arter ies or arterioles. Olprinone increases hepatosplanchnic blood flow and improves oxygen supply. While long-term therapy with PDE 3 inhibitors in patients with chronic heart failure may accelerate the progress of the underlying disease and provoke serious ventricular arrhythmia, olprinone shows good potential for short-term treatment in patients who have experienced severe heart failure or patients who have undergone cardiac surgery.
Export Options
About this article
Cite this article as:
Ueda Takashi and Mizushige Katsufumi, The Effects of Olprinone, a Phosphodiesterase 3 Inhibitor, on Systemic and Cerebral Circulation, Current Vascular Pharmacology 2006; 4 (1) . https://dx.doi.org/10.2174/157016106775203072
DOI https://dx.doi.org/10.2174/157016106775203072 |
Print ISSN 1570-1611 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6212 |
Call for Papers in Thematic Issues
Advancements in Arterial Stiffness: Novel Therapeutic Frontiers
Arterial stiffness, a hallmark of cardiovascular disease, poses significant challenges in contemporary healthcare. This thematic issue delves into the multifaceted landscape of arterial stiffness and explores cutting-edge therapeutic interventions aimed at mitigating its adverse effects. Within these pages, readers will find a comprehensive overview of the mechanisms underlying arterial stiffness, ...read more
Ischemic Cardiovascular Diseases: Mechanisms, Diagnosis and Therapy
Ischemic cardiovascular disease includes myocardial infarction, coronary atherosclerotic heart disease, angina pectoris, etc., constitute the leading cause of patient mortality by preventing tissues from getting sufficient oxygen and nutrients. Ischemic heart disease, as a clinical condition, is characterized by myocardial ischemia, causing an imbalance between myocardial blood supply and demand, ...read more
TREATMENT OF CARDIOVASCULAR DISEASE IN CHRONIC AND END STAGE KIDNEY DISEASE
Cardiovascular disease still remains the leading cause of death in Chronic and End Stage Kidney Disease, accounting for more than half of all deaths in dialysis patients. During the past decade, research has been focused on novel therapeutic agents that might delay or even reverse cardiovascular disease and vascular calcification, ...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
-
Efficacy and Cardiovascular Safety of Alpha Glucosidase Inhibitors
Current Drug Safety Wide Pulse Pressure in the Elderly
Current Cardiology Reviews Lipid Modulation of Intravascular and Cellular Sodium Handling:Mechanistic Insights and Potential Clinical Implications
Current Vascular Pharmacology Potential of Taming MicroRNA on Driver Seat to Control Mitochondrial Horses in Breast Carcinoma
MicroRNA Structure-Activity Relationships of Flavonoids
Current Organic Chemistry Oxidative Stress-Induced Caspases are Regulated in Human Myeloid HL-60 Cells by Calcium Signal
Current Signal Transduction Therapy Novel Target Sites for Drug Screening: A Special Reference to Cancer, Rheumatoid Arthritis and Parkinson’s Disease
Current Signal Transduction Therapy FDG-PET Scan in Sarcoidosis: Clinical and Imaging Indications
Current Medical Imaging Pharmacogenomics of Cardiovascular Complications in Diabetes and Obesity
Recent Patents on Biotechnology Small Molecule Inhibitors of NF-κB and JAK/STAT Signal Transduction Pathways as Promising Anti-Inflammatory Therapeutics
Mini-Reviews in Medicinal Chemistry Advances in the Physiology of GPR55 in the Central Nervous System
Current Neuropharmacology Heart Failure Epidemiology: European Perspective
Current Cardiology Reviews Improved Pharmacokinetic Profile and Anti-Inflammatory Property of a Novel Curcumin Derivative, A50
Letters in Drug Design & Discovery Pulmonary Disease in Beta-Thalassemia
Current Respiratory Medicine Reviews Editorial: New Therapetic Approaches in the Management of Ischemia Reperfusion Injury and Cardiometabolic Diseases: Opportunities and Challenges
Current Drug Targets Chronic Inflammation and Oxidative Stress as a Major Cause of Age- Related Diseases and Cancer
Recent Patents on Inflammation & Allergy Drug Discovery Metabolic Therapy of Heart Failure
Current Pharmaceutical Design Cell Cycle Checkpoint Genes and Aneuploidy: A Short Review
Current Genomics Antimicrobial Drug Interactions in the Critically Ill Patients
Current Clinical Pharmacology The Emerging Roles of Leptin and Ghrelin in Cardiovascular Physiology and Pathophysiology
Current Vascular Pharmacology