Olmesartan

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Olmesartan
Systematic (IUPAC) name
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[ [4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
Identifiers
CAS number 144689-63-4
ATC code C09CA08
PubChem 130881
DrugBank APRD00223
Chemical data
Formula C29H30N6O6 
Mol. mass 558.585 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 26% (olmesartan medoxomil)
Metabolism Hepatic (cannot be removed by hemodialysis)
Half life 13 hours
Excretion Renal 40%, biliary 60%
Therapeutic considerations
Pregnancy cat.

C (D if used in second or third trimester)
Legal status

℞ Prescription only
Routes Oral

Olmesartan (Benicar,Olmetec) belongs to the class of medicines called angiotensin II receptor antagonists to treat high blood pressure. It is marketed worldwide by Daiichi Sankyo, Ltd. and in the United States by Daiichi Sankyo, Inc. and Forest Laboratories. Olmesartan works by blocking the binding of angiotension II to the AT1 receptors in vascular muscle; it is therefore independent of angiotension II synthesis pathways, unlike ACE inhibitors. By blocking binding rather than synthesis of angiotension II, olmesartan inhibits the negative regulatory feedback on renin secretion. As a result of this blockage, olmesartan restricts vasoconstriction and the secretion of aldosterone. This lowers blood pressure by producing vasodilation, and decreasing peripheral resistance.

Contents

[edit] Administration

Olmesartan is available in 5, 20, and 40 mg tablets. A normal dose for an adult (including the elderly and mild renal or hepatic impairment) is 20 mg/day in one dosage. This may be increased after two weeks to 40 mg/day if further blood pressure reduction is needed.

[edit] Myocardial infarction

A recent meta-analysis published in the peer-reviewed journal Circulation demonstrated that angiotensin II receptor antagonist induce myocardial infarction compared to placebo.[1]

[edit] Side effects

Side effects include:

[edit] Notes

^1. Website of National Institute of Heath, US Government. http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a603006.html#side-effects

[edit] References

  1. ^ Strauss MH, Hall AS. (2006). "Angiotensin receptor blockers may increase risk of myocardial infarction: unraveling the ARB-MI paradox.". Circulation 8 (114): 838–54. doi:10.1161/CIRCULATIONAHA.105.594986. PMID 16923768. 

Hodgson, Barbara B., and Kizior, Robert J. Saunders Nursing Drug Handbook 2006. St. Louis, MO: Elsevier, Saunders, 2006.

[edit] External links

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Agents acting on the renin-angiotensin system (C09)
ACE inhibitors
Angiotensin II receptor antagonists (AIIRA)
Azilsartan • Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan
Renin inhibitors