Products
Olmesartan is commercially available in the form of film-coated tablets (Olmetec, Votum, fixed combinations with amlodipine and hydrochlorothiazide). It has been approved in many countries since 2005. Generics were registered in 2016 and went on sale in 2017.
Structure and properties
Olmesartan is present in drugs as olmesartan medoxomil (C29H30N6O6, Mr = 558.6 g/mol), a prodrug that is rapidly converted in the intestine to the active metabolite olmesartan. Relevant structural elements include the imidazole, the tetrazole, and the biphenyl. Olmesartan medoxomil exists as a white crystalline powder that is practically insoluble in water.
Effects
Olmesartan (ATC C09CA08) has antihypertensive properties. It is a selective antagonist of angiotensin II at the AT1 receptor. Angiotensin II is a peptide hormone directly involved in the development of hypertension. It has a potent vasoconstrictor effect and increases aldosterone release, which in turn causes increased water and sodium retention. The half-life of olmesartan is between 10 and 15 hours.
Indications
For the treatment of hypertension (essential hypertension).
Dosage
According to the SmPC. The film-coated tablets are taken once daily, usually in the morning, always at the same time and regardless of meals.
Contraindications
- Hypersensitivity
- Pregnancy
- Severely impaired liver function
- Biliary obstruction
- Inherited angioedema
- Previous angioedema while taking ACE inhibitors or sartans.
- Combination with aliskiren in patients with diabetes mellitus or impaired renal function.
For complete precautions, see the drug label.
Interactions
Potassium-sparing diuretics and potassium may increase the risk of hyperkalemia. Other drug interactions are possible with antihypertensives, NSAIDs, antacids, lithium, and immunosuppressants, among others.
Adverse effects
The most common possible adverse effects include headache, flu-like symptoms, and dizziness.
