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olmesartan (Benicar)

Indications: - hypertension - chronic heart failure - delay &/or prevention of microalbuminuria in patients with diabetes mellitus type 2 [5] - nondiabetic proteinuric nephropathy [8] * avoid, use another ARB [11] Dosage: 1) start 20 mg PO QD [3] 2) dosages above 40 mg QD have no additional benefit [3] 3) no initial dosage adjustment recommended for elderly patients Tabs: 5, 20 & 40 mg Pharmacokinetics: 1) olemesartan medoxomil is rapidly hydrolyzed in the GI tract 2) absolute oral bioavailability is 25%, not significantly affected by food 3) peak plasma concentration is reached after 1-2 hours 4) volume of distribution is 17 liters 5) protein-binding is 99% 6) does not penetrate erythrocytes 7) poorly crosses the blood-brain barrier in rats 8) no metabolism of olemesartan 9) biphasic elimination with terminal 1/2life of 13 hours 10) eliminated in the urine (35-50%) & in the bile/feces 11) steady state levels achieved in 3-5 days with QD dosing Dosage adjustment with renal failure: -> no recommendations given but AUC tripled in patients with creatinine clearance < 20 mL/min Adverse effects: 1) similar to placebo in clinical trials [3] 2) dizziness (3%) 3) increased risk of cardiovascular death in patients with diabetes mellitus type 2 [4,5]; but potential benefits outweigh risks [4] - no clear evidence of increased cardiovascular risks [9] 4) sprue-like enteropathy [6,7,12,13,14]; average onset: 3 years - duodenal villous flattening, intrapithelial lymphocytes - avoid, use another ARB [11] Mechanism of action: - angiotensin 2 receptor antagonist Notes: - introduced 2002 - 1st generic versions of 4 drugs that contain olmesartan, Oct 2016 - Benicar, Benicar HCT, Azor, Tribenzor [10]

Interactions

drug interactions drug adverse effects (more general classes) monitor with ARBs

General

angiotensin II receptor antagonist (ARB)

Properties

MISC-INFO: elimination route KIDNEY pregnancy-category D

Database Correlations

PUBCHEM correlations

References

  1. Prescriber's Letter 9(5):30 2002
  2. Prescriber's Letter 9(6):34 2002
  3. Sankyo Pharma Inc, 2002
  4. FDA Medwatch Benicar (olmesartan): Ongoing Safety Review, 06/11/2010 http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm215249.htm - FDA Drug Safety Communication: Ongoing safety review of Benicar and cardiovascular events http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm215222.htm - Benicar (olmesartan): Ongoing Safety Review, UPDATED 04/14/2011 http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm215249.htm
  5. Haller H et al Olmesartan for the Delay or Prevention of Microalbuminuria in Type 2 Diabetes N Engl J Med 2011; 364:907-917March 10, 2011 PMID: 21388309 http://www.nejm.org/doi/full/10.1056/NEJMoa1007994
  6. Rubio-Tapia A et al Severe Spruelike Enteropathy Associated With Olmesartan Mayo Clinic Proceedings 2012 http://www.mayoclinicproceedings.org/webfiles/images/journals/jmcp/jmcp_ft87_7_1.pdf
  7. FDA MedWatch. July 3, 2013 Olmesartan Medoxomil: Drug Safety Communication - Label Changes To Include Intestinal Problems (Sprue-Like Enteropathy) http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm359528.htm
  8. Deprecated Reference
  9. FDA MedWAtch. June 24, 2014 Olmesartan: Drug Safety Communication - FDA Review Finds Cardiovascular Risks for Diabetics Not Conclusive. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm402616.htm
  10. Wendling P FDA Gives Green Light to First Olmesartan Generics. Medscape. Oct 27, 2016. http://www.medscape.com/viewarticle/871070
  11. Therapeutics Letter #108. Therapeutics Initiative Drugs to Avoid. http://www.ti.ubc.ca/2018/01/04/108-drugs-avoid/
  12. Walsh N. Sprue-like Events Seen with Olmesartan. Enteropathy identified more commonly than with other ARBs. MedPage Today. January 30, 2018 https://www.medpagetoday.com/gastroenterology/generalgastroenterology/70843 - Dong YH, Jin Y, Tsacogianis TN, He M, Hsieh PH, Gagne JJ. Use of olmesartan and enteropathy outcomes: a multi-database study. Aliment Pharmacol Ther. 2018 Jan 22. PMID: 29359522
  13. Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018
  14. Ianiro G, Bibbo S, Montalto M et al Systematic review: Sprue-like enteropathy associated with olmesartan. Aliment Pharmacol Ther. 2014 Jul;40(1):16-23. Review. PMID: 24805127 Free Article
  15. www.benicar.com

Component-of

amlodipine/hydrochlorothiazide/olmesartan (Tribenzor) amlodipine/olmesartan (Azor) hydrochlorothiazide/olmesartan (Benicar HCT)