From the Guidelines
Olmesartan medoxomil is an angiotensin II receptor blocker (ARB) with a target dose of 40 mg, once daily, as recommended by the 2020 ACC/AHA clinical performance and quality measures for adults with heart failure 1. The medication works by relaxing blood vessels, allowing blood to flow more easily and lowering blood pressure.
- Key points about olmesartan medoxomil include:
- It is used to treat high blood pressure (hypertension)
- The typical starting dose is 20 mg once daily, which may be increased to a maximum of 40 mg daily if needed for blood pressure control
- Olmesartan blocks the action of angiotensin II, a natural substance that narrows blood vessels and causes sodium and water retention, both of which contribute to high blood pressure
- This medication is usually taken once daily with or without food and may be prescribed alone or in combination with other blood pressure medications like diuretics
- Common side effects include dizziness, back pain, and upper respiratory infections
- Patients should be aware that olmesartan should not be taken during pregnancy as it can cause harm to the developing fetus, particularly in the second and third trimesters
- Regular monitoring of blood pressure and kidney function is important while taking this medication, as recommended by the ACC/AHA guidelines 1.
From the FDA Drug Label
Olmesartan medoxomil, a prodrug, is hydrolyzed to olmesartan during absorption from the gastrointestinal tract. Olmesartan is a selective AT1 subtype angiotensin II receptor antagonist. Olmesartan medoxomil is described chemically as 2,3-dihydroxy-2-butenyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-carboxylate, cyclic 2,3-carbonate Its molecular formula is C29H30N6O6 and its structural formula is: [Chemical Structure] Olmesartan medoxomil USP is a white to off-white, crystalline powder with a molecular weight of 558. 59.
Olmesartan medoxomil is a prodrug that is hydrolyzed to olmesartan during absorption, and olmesartan is a selective AT1 subtype angiotensin II receptor antagonist. Key characteristics of olmesartan medoxomil include:
- Molecular formula: C29H30N6O6
- Molecular weight: 558.59
- Appearance: White to off-white, crystalline powder 2
From the Research
Definition and Mechanism of Action
- Olmesartan medoxomil is a new orally active angiotensin II (Ang II) type 1 receptor antagonist 3.
- It is a prodrug that is rapidly de-esterified during absorption to form olmesartan, the active metabolite 3, 4.
- Olmesartan is a potent, competitive and selective Ang II type 1 receptor antagonist that inhibits the actions of angiotensin II on the renin-angiotensin-aldosterone system 5, 6.
Pharmacokinetics and Pharmacodynamics
- Olmesartan medoxomil is rapidly absorbed from the gastrointestinal tract and converted during absorption to olmesartan, which is subsequently excreted without further metabolism 4.
- Peak plasma concentrations of olmesartan occur 1-3 h after administration, after which concentrations decrease with an elimination half-life of 10-15 h 4.
- The absolute bioavailability of olmesartan from olmesartan medoxomil tablets is 28.6% 4.
Clinical Efficacy and Safety
- Olmesartan medoxomil has been shown to be effective in reducing blood pressure in patients with hypertension, with a favorable adverse-event profile 3, 4, 5, 6, 7.
- It is recommended for the treatment of adult patients with hypertension, with a usual dose of 20 mg once daily, increasing to 40 mg if needed 4, 6.
- Olmesartan medoxomil has been compared to other antihypertensive agents, including losartan, valsartan, and irbesartan, and has been shown to be at least as effective in reducing blood pressure 3, 6, 7.