olmesartan (Benicar)
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Indications
- hypertension
- chronic heart failure
- delay &/or prevention of microalbuminuria in patients with diabetes mellitus type 2[5]
- nondiabetic proteinuric nephropathy[8]
Dosage
- start 20 mg PO QD[3]
- dosages above 40 mg QD have no additional benefit[3]
- no initial dosage adjustment recommended for elderly patients
Tabs: 5, 20 & 40 mg
Pharmacokinetics
- olemesartan medoxomil is rapidly hydrolyzed in the GI tract
- absolute oral bioavailability is 25%, not significantly affected by food
- peak plasma concentration is reached after 1-2 hours
- volume of distribution is 17 liters
- protein-binding is 99%
- does not penetrate erythrocytes
- poorly crosses the blood-brain barrier in rats
- no metabolism of olemesartan
- biphasic elimination with terminal 1/2life of 13 hours
- eliminated in the urine (35-50%) & in the bile/feces
- 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
elimination via kidney
Adverse effects
- similar to placebo in clinical trials[3]
- dizziness (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]
- sprue-like enteropathy[6][7][12][13][14]; average onset: 3 years
- duodenal villous flattening, intrapithelial lymphocytes
- avoid, use another ARB[11]
- drug adverse effects of angiotensin II receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Mechanism of action
Notes
- introduced 2002
- 1st generic versions of 4 drugs that contain olmesartan, Oct 2016
- Benicar, Benicar HCT, Azor, Tribenzor[10]
More general terms
Component of
- hydrochlorothiazide/olmesartan (Benicar HCT)
- amlodipine/olmesartan (Azor)
- amlodipine/hydrochlorothiazide/olmesartan (Tribenzor)
References
- ↑ Prescriber's Letter 9(5):30 2002
- ↑ Prescriber's Letter 9(6):34 2002
- ↑ 3.0 3.1 3.2 3.3 Sankyo Pharma Inc, 2002
- ↑ 4.0 4.1 4.2 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 - ↑ 5.0 5.1 5.2 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 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/21388309 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1007994
- ↑ 6.0 6.1 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
- ↑ 7.0 7.1 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
- ↑ 8.0 8.1 Deprecated Reference
- ↑ 9.0 9.1 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
- ↑ 10.0 10.1 Wendling P FDA Gives Green Light to First Olmesartan Generics. Medscape. Oct 27, 2016. http://www.medscape.com/viewarticle/871070
- ↑ 11.0 11.1 11.2 Therapeutics Letter #108. Therapeutics Initiative Drugs to Avoid. http://www.ti.ubc.ca/2018/01/04/108-drugs-avoid/
- ↑ 12.0 12.1 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: https://www.ncbi.nlm.nih.gov/pubmed/29359522 - ↑ 13.0 13.1 Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018
- ↑ 14.0 14.1 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: https://www.ncbi.nlm.nih.gov/pubmed/24805127 Free Article
- ↑ www.benicar.com