Candesartan

Products

Candesartan is commercially available in tablet form (Atacand, Blopress, generics). It is also combined fixed with hydrochlorothiazide (Atacand plus, Blopress plus, generics). Candesartan has been approved in many countries since 1997. In 2020, a fixed combination with amlodipine was also released.

Structure and Properties

Candesartan (C₂₄H₂₀N₆O₃, M_r = 440.45 g/mol) is administered in the form of the prodrug candesartancilexetil, a white powder that is practically insoluble in water. Candesartancilexetil is an ester that is hydrolyzed to candesartan in the organism during absorption.

Effects

Candesartan (ATC C09CA06) has antihypertensive effects by abolishing the physiologic effects of angiotensin II. 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 effects of candesartan are due to selective blockade of AT₁ receptor.

Indications

For the treatment of essential hypertension (high blood pressure) and heart failure with impaired left ventricular systolic function.

Dosage

According to the SmPC. Candesartan may be administered once daily because of its long half-life of 9 hours. It is taken independently of meals. The usual daily dose for adults ranges from 8 to 32 mg.

Contraindications

Hypersensitivity
Severe liver dysfunction
Cholestasis
Pregnancy and lactation
Hereditary angioedema, previous angioedema on sartans or ACE inhibitors.
Combination with aliskiren in patients with diabetes mellitus or impaired renal function.

For complete precautions, see the drug label.

Interactions

Caution should be exercised with concomitant use of anticoagulants such as phenprocoumon. Lithium concentrations may potentially be increased. NSAIDs may attenuate the antihypertensive effects of candesartan, and other antihypertensive agents may potentiate the effects of candesartan.

Adverse Effects

The most common possible adverse effects include respiratory infections, drowsiness, dizziness, headache, low blood pressure (in heart failure), and back pain. Hyperkalemia, cough, renal impairment, and hepatic impairment occur rarely to very rarely.