Olmesartan

Olmesartan medoxomil

File:Olmesartan.png
Systematic (IUPAC) name
(5-methyl-2-oxo-2H-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-imidazole-5-carboxylate
Clinical data
Pregnancy category	C (D if used in second or third trimester)
Routes of administration	Oral
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	26%
Metabolism	Hepatic (cannot be removed by hemodialysis)
Biological half-life	13 hours
Excretion	Renal 40%, biliary 60%
Identifiers
CAS Number	144689-63-4
ATC code	C09CA08 (WHO) C09DA08 (with diuretics) C09DB02 (with amlodipine)
PubChem	CID 130881
DrugBank	APRD00223
Chemical data
Formula	C29H30N6O6
Molar mass	558.585 g/mol[[]]
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olmesartan medoxomil (trade names Benicar (US), Olmetec (EU)) is an angiotensin II receptor antagonist used to treat high blood pressure. The prodrug olmesartan medoxomil is marketed worldwide by Daiichi Sankyo and in India by Zydus Cadila under the trade name Olmy and by Ranbaxy Laboratories Ltd. under the trade name Olvance.

Indications

Olmesartan is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Adverse effects

Adverse effects include headache, dizziness, diarrhea, hyperglycemia, Influenza-like illness, tachycardia, and upper respiratory tract infection. Olmesartan does not cause cough more frequently than placebo does. This medication may rarely cause a serious side effect called angiodema. Olmesartan may cause birth defects or fetal death if pregnant.

Structure

The olmesartan molecule includes one tetrazole group (a 5-member heterocyclic ring of four nitrogen and one carbon atom) and one imidazole group (a 5-membered planar heterocyclic aromatic ring of two nitrogen and three carbon atoms, classified as an alkaloid).

Mechanism of action

Olmesartan works by blocking the binding of angiotensin II to the AT₁ receptors in vascular muscle; it is therefore independent of angiotensin II synthesis pathways, unlike ACE inhibitors. By blocking binding rather than synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion. As a result of this blockage, olmesartan reduces vasoconstriction and the secretion of aldosterone. This lowers blood pressure by producing vasodilation, and decreasing peripheral resistance.

Interactions

Do not use non-prescription products that contain stimulants; including diet pills, and cold medicines. Consult your doctor before taking any potassium supplements, including salt substitutes.

Dosage and administration

The usual recommended starting dose of olmesartan is 20 mg once daily. The dose may be increased to 40 mg after 2 weeks of therapy, if further reduction in blood pressure is desirable. Doses above 40 mg do not appear to have greater effect, and twice-daily dosing offers no advantage over the same total dose given once daily. No adjustment of dosage is typically necessary for advanced age, renal impairment, or hepatic dysfunction. For patients with possible depletion of intravascular volume (e.g., patients treated with diuretics), olmesartan should be initiated with caution; consideration should be given to use of a lower starting dose in such cases. If blood pressure is not controlled by Benicar alone, a diuretic may be added. Benicar may be administered with other antihypertensive agents. Benicar may be administered with or without food.

Preparations

Benicar HCT is the brand name of a medication containing olmesartan medoxomil in combination with hydrochlorothiazide, a thiazide diuretic. Three dosage combinations are available: 20 mg or 40 mg of olmesartan medoxomil combined with 12.5 mg of hydrochlorothiazide, or 40 mg of olmesartan medoxomil combined with 25 mg of hydrochlorothiazide.

See also

• Discovery and development of angiotensin receptor blockers

External links

• Daiichi-Sankyo Benicar page
• Benicar HCT from RXlist.com

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