Prodrugs pp 1305-1312 | Cite as

Case Study: Olmesartan Medoxomil: A Prodrug of Olmesartan

  • Bianca M. Liederer
Part of the Biotechnology: Pharmaceutical Aspects book series (PHARMASP, volume V)


Olmesartan is a durable, specific, and competitive nonpeptide angiotensin II receptor antagonist used to treat hypertension. To achieve better oral bioavailability its ester prodrug, olmesartan medoxomil, was developed. Olmesartan medoxomil is suitable for once daily oral administration and is available in tablet form.


Olmesartan Medoxomil Antihypertensive Efficacy Ambulatory Blood Pressure Measurement Ester Prodrug Daily Oral Administration 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Ball KJ, Williams PA, and Stumpe KO. Relative Efficacy of an Angiotensin II Antagonist Compared with Other Antihypertensive Agents. Olmesartan Medoxomil versus Antihypertensives. J Hypertens 2001; 19Suppl 1:S49–56Google Scholar
  2. Brunner HR. The New Oral Angiotensin II Antagonist Olmesartan Medoxomil: A Concise Overview. J Hum Hypertens 2002; 16Suppl 2:S13–16PubMedCrossRefGoogle Scholar
  3. Chrysant SG, Marbury TC, and Robinson TD. Antihypertensive Efficacy and Safety of Olmesartan Medoxomil Compared with Amlodipine for Mild-tomoderate Hypertension. J Hum Hypertens 2003; 17:425–432PubMedCrossRefGoogle Scholar
  4. Gardner SF, and Franks AM. Olmesartan Medoxomil: The Seventh Angiotensin Receptor Antagonist. Ann Pharmacother 2003; 37:99–105PubMedCrossRefGoogle Scholar
  5. Greathouse M. A Review of Olmesartan Medoxomil Monotherapy: Antihypertensive Efficacy Similar to that of Other Angiotensin II Receptor Blocker/Hydrochlorothiazide Combinations? Congest Heart Fail 2002; 8:313–320PubMedCrossRefGoogle Scholar
  6. Kobayashi N, Fujimori I, Watanabe M, and Ikeda T. Real-time Monitoring of Metabolic Reactions by Microdialysis in Combination with Tandem Mass Spectrometry: Hydrolysis of CS-866 In Vitro in Human and Rat Plasma, Livers, and Small Intestines. Anal Biochem 2000; 287:272–278PubMedCrossRefGoogle Scholar
  7. Lewis EJ. The Role of Angiotensin II Receptor Blockers in Preventing the Progression of Renal Disease in Patients with Type 2 Diabetes. Am J Hypertens 2002; 15:123S–128SPubMedCrossRefGoogle Scholar
  8. Laeis P, Puchler K, and Kirch W. The Pharmacokinetic and Metabolic Profile of Olmesartan Medoxomil limits the Risk of Clinically Relevant Drug Interaction. J Hypertens 2001;19Suppl 1:S21–32Google Scholar
  9. Miyazaki M, and Takai S. Anti-atherosclerotic Efficacy of Olmesartan. J Hum Hypertens 2002; 16Suppl 2:S7–12PubMedCrossRefGoogle Scholar
  10. Mizuno M, Sada T, Kato M, and Koike H. Renoprotective Effects of Blockade of Angiotensin II AT1 Receptors in an Animal Model of Type 2 Diabetes. Hypertens Res 2002; 25:271–278PubMedCrossRefGoogle Scholar
  11. Neutel JM, Elliott WJ, Izzo JL Jr., Chen CL, and Masonson HN. Antihypertensive Efficacy of Olmesartan Medoxomil, a New Angiotensin II Receptor Antagonist, as Assessed by Ambulatory Blood Pressure Measurements. J Clin Hypertens 2002;4:325–331CrossRefGoogle Scholar
  12. Oparil S. Comparative Antihypertensive Efficacy of Olmesartan: Comparison with Other Angiotensin II Receptor Antagonists. J Hum Hypertens 2002;16Suppl 2:S17–23PubMedCrossRefGoogle Scholar
  13. Oparil S, Williams D, Chrysant SG, Marbury TC, and Neutel J. Comparative Efficacy of Olmesartan, Losartan, Valsartan, and Irbesartan in the Control of Essential Hypertension. J Clin Hypertens 2001; 3:283–291CrossRefGoogle Scholar
  14. Puechler K, Laeis P, and Stumpe K. Blood Pressure Response, but no Adverse Event Incidence, Correlates with Dose of Angiotensin II Antagonist. J Hypertens 2001; 19Suppl 1:S41–48Google Scholar
  15. Schiffrin EL. Beyond Blood Pressure: The Endothelium and Atherosclerosis Progression. Am J Hypertens 2002; 15:115S–122SPubMedCrossRefGoogle Scholar
  16. Schwocho LR, and Masonson HN. Pharmacokinetics of CS-866, a New Angiotensin II Receptor Blocker, in Healthy Subjects. J Clin Pharmacol 2001;41:515–527PubMedCrossRefGoogle Scholar
  17. Simons WR. Comparative Cost Effectiveness of Angiotensin II Receptor Blockers in a US Managed Care Setting: Olmesartan Medoxomil Compared with Losartan, Valsartan, and Irbesartan. Pharmacoeconomics 2003; 21:61–74PubMedCrossRefGoogle Scholar
  18. Song JC, and White M. Olmesartan Medoxomil (CS-866). An Angiotensin II Receptor Blocker for Treatment of Hypertension. Formulary 2001; 36:487–499Google Scholar
  19. Stumpe KO, and Ludwig M. Antihypertensive Efficacy of Olmesartan Compared with Other Antihypertensive Drugs. J Hum Hypertens 2002; 16Suppl 2:S24–28PubMedCrossRefGoogle Scholar
  20. Takai S, Kim S, Sakonjo H, and Miyazaki M. Mechanisms of Angiotensin II Type 1 Receptor Blocker for Anti-atherosclerotic Effect in Monkeys Fed a Highcholesterol Diet. J Hypertens 2003; 21:361–369PubMedCrossRefGoogle Scholar
  21. von Bergmann K, Laeis P, Puchler K, Sudhop T, Schwocho LR, and Gonzalez L. Olmesartan Medoxomil: Influence of Age, Renal and Hepatic Function on the Pharmacokinetics of Olmesartan Medoxomil. J Hypertens 2001; 19Suppl 1:S33–40Google Scholar
  22. Yanagisawa H, Amemiya Y, Kanazaki T, Shimoji Y, Fujimoto K, Kitahara Y, Sada T, Mizuno M, Ikeda M, Miyamoto S, Furukawa Y, and Koike H. Nonpeptide Angiotensin II Receptor Antagonists: Synthesis, Biological Activities, and Structure-activity Relationships of Imidazole-5-carboxylic Acids Bearing Alkyl, Alkenyl, and Hydroxyalkyl Substituents at the 4-position and their Related Compounds. J Med Chem 1996; 39:323–338PubMedCrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Bianca M. Liederer
    • 1
  1. 1.Department of Pharmaceutical ChemistryThe University of KansasLawrenceUSA

Personalised recommendations