Azilsartan

Products

Azilsartan has been approved in the United States and the EU in tablet form since 2011 (Edarbi). In many countries, it was registered in August 2012 as the 8th member of the sartan drug group. In 2014, a fixed combination with chlortalidone was approved (Edarbyclor).

Structure

Azilsartan (C25H20N4O5, Mr = 456.5 g/mol) is present in drugs in the form of the ester prodrug azilsartan medoxomil, which is hydrolyzed to azilsartan during absorption. It is formulated as the potassium salt azilsartankamedoxomil, a white powder that is virtually insoluble in water. Important structural elements are the benzimidazole, the biphenyl, and the 4-oxadiazole ring.

Effects

Azilsartan (ATC C09CA09) 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.

Indications

For the treatment of high blood pressure (essential hypertension).

Dosage

According to the drug label. The tablets are taken once a day and independently of meals.

Contraindications

  • Hypersensitivity
  • Pregnancy
  • Combination with aliskiren in patients with diabetes mellitus or impaired renal function.

For complete precautions, see the drug label.

Interactions

Azilsartan is metabolized by CYP2C9. According to the drug label, no interactions have been noted with commonly used antihypertensive agents. Concomitant use of NSAIDs and COX-2 inhibitors is not recommended because the antihypertensive effect may be attenuated and renal function may be impaired. Other drug-drug interactions are possible with lithium, potassium-sparing diuretics, and potassium.

Adverse effects

Possible adverse effects include diarrhea, low blood pressure, nausea, fatigue, weakness, muscle cramps, dizziness, and cough.