Olmesartan

From Anvita Health Wiki

Contents 1 Indications 2 Dosage 3 Pharmacokinetics 4 Adverse-effects 5 Mechanism-of-action 6 Notes 7 More General Terms 8 Internet Database 9 References

Indications

• hypertension
• delay &/or prevention of microalbuminuria in patients with diabetes mellitus type 2 [5]

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]
  
• drug adverse effects of angiotensin II receptor antagonists

Mechanism-of-action

• angiotensin 2 receptor antagonist

Notes

• introduced 2002

More General Terms

• angiotensin II receptor antagonist (ARB)

Internet Database

PubChem: 158781
PubChem: 130881

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 [1]
   - FDA Drug Safety Communication: Ongoing safety review of Benicar and cardiovascular events [2]
   - Benicar (olmesartan): Ongoing Safety Review, UPDATED 04/14/2011 [3]
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 <PubMed> PMID: [4] <Internet> [5]
6. www.benicar.com

olmesartan (Benicar)