+1 Recommend
1 collections
      • Record: found
      • Abstract: found
      • Article: found

      Rosuvastatin – A Highly Effective New 3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase Inhibitor: Review of Clinical Trial Data at 10–40 mg Doses in Dyslipidemic Patients



      S. Karger AG

      Diabetes, Hypercholesterolemia, Hypercholesterolemia, familial, Rosuvastatin, Statin, Dyslipidemia, Hyperlipidemia

      Read this article at

          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.


          Rosuvastatin (Crestor<sup>®</sup>; licensed to AstraZeneca, Macclesfield, UK from Shionogi, Osaka, Japan) is a new statin with pharmacologic characteristics that translate into selectivity of effect in hepatic cells and enhanced potency in 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition. It is approved for use at doses of 10–40 mg once daily to reduce low-density lipoprotein (LDL) cholesterol, increase high-density lipoprotein (HDL) cholesterol and improve other lipid measures in dyslipidemic patients. In a dose-ranging study in mild/moderate hypercholesterolemia, rosuvastatin reduced LDL cholesterol by 52–63% at 10–40 mg. Rosuvastatin 10 mg reduces LDL cholesterol significantly more than atorvastatin 10 mg, simvastatin 10–40 mg and pravastatin 10–40 mg, and enables significantly more patients to achieve National Cholesterol Education Program and Joint European Societies LDL cholesterol goals compared with each of these statins. Rosuvastatin also produces marked elevations in HDL cholesterol and maintains this effect across the dose range. Rosuvastatin favorably modifies triglycerides, LDL cholesterol and other lipid measures in patients with hypertriglyceridemia or mixed dyslipidemia, including diabetic patients, and may constitute a monotherapy option for many such patients. Rosuvastatin is well tolerated when used alone or in combination, exhibiting a safety profile similar to that of other available statins. Rosuvastatin offers considerable advantages for use in routine clinical practice.

          Related collections

          Most cited references 24

          • Record: found
          • Abstract: found
          • Article: not found

          Structural mechanism for statin inhibition of HMG-CoA reductase.

          HMG-CoA (3-hydroxy-3-methylglutaryl-coenzyme A) reductase (HMGR) catalyzes the committed step in cholesterol biosynthesis. Statins are HMGR inhibitors with inhibition constant values in the nanomolar range that effectively lower serum cholesterol levels and are widely prescribed in the treatment of hypercholesterolemia. We have determined structures of the catalytic portion of human HMGR complexed with six different statins. The statins occupy a portion of the binding site of HMG-CoA, thus blocking access of this substrate to the active site. Near the carboxyl terminus of HMGR, several catalytically relevant residues are disordered in the enzyme-statin complexes. If these residues were not flexible, they would sterically hinder statin binding.
            • Record: found
            • Abstract: not found
            • Article: not found

            Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Simvastatin Survival Study (4S)

              • Record: found
              • Abstract: found
              • Article: not found

              Lifestyle and risk factor management and use of drug therapies in coronary patients from 15 countries; principal results from EUROASPIRE II Euro Heart Survey Programme.

              The principal aim of the second EUROASPIRE survey was to determine in patients with established coronary heart disease whether the Joint European Societies' recommendations on coronary prevention are being followed in clinical practice. This survey was undertaken in 1999-2000 in 15 European countries: Belgium, Czech Republic, Finland, France, Germany, Greece, Hungary, Ireland, Italy, the Netherlands, Poland, Slovenia, Sweden, Spain and the U.K., in selected geographical areas and 47 centres. Consecutive patients, men and women or =140 mmHg and/or diastolic blood pressure > or =90 mmHg), 58% had elevated serum total cholesterol (total cholesterol > or =5 mmol x l(-1)) and 20% reported a medical history of diabetes. Glucose control in these diabetic patients was poor with 87% having plasma glucose >6.0 mmol x l(-1)and 72% > or =7.0 mmol x l(-1). Among the patients interviewed the use of prophylactic drug therapies on admission, at discharge and at interview was as follows: aspirin or other antiplatelets drugs 47%, 90% and 86%; beta-blockers 44%, 66% and 63%; ACE inhibitors 24%, 38% and 38%; and lipid-lowering drugs 26%, 43% and 61%, respectively. With the exception of antiplatelet drugs, wide variations in the use of prophylactic drug therapies exist between countries. This European survey of coronary patients shows a high prevalence of unhealthy lifestyles, modifiable risk factors and inadequate use of drug therapies to achieve blood pressure and lipid goals. There is considerable potential throughout Europe to raise the standard of preventive cardiology through more effective lifestyle intervention, control of other risk factors and optimal use of prophylactic drug therapies in order to reduce coronary morbidity and mortality. Copyright 2001 The European Society of Cardiology.

                Author and article information

                S. Karger AG
                June 2003
                27 June 2003
                : 99
                : 3
                : 126-139
                MDC, Humboldt University, Berlin, Germany
                70669 Cardiology 2003;99:126–139
                © 2003 S. Karger AG, Basel

                Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug. Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

                Page count
                Figures: 6, Tables: 3, References: 79, Pages: 14


                Comment on this article