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Angiotensin II receptor antagonist

Drugs & Medication

Angiotensin II receptor antagonist

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Losartan, the first ARB
Losartan, the first ARB

Angiotensin II receptor antagonists, also known as angiotensin receptor blockers (ARBs), AT1-receptor antagonists or sartans, are a group of pharmaceuticals which modulate the renin-angiotensin-aldosterone system. Their main use is in hypertension (high blood pressure), diabetic nephropathy (kidney damage due to diabetes) and congestive heart failure.

Contents

Mode of action

These substances are AT1-receptor antagonists that is, they block the activation of angiotensin II AT1 receptors. Blockade of AT1 receptors directly causes vasodilation, reduces secretion of vasopressin, reduces production and secretion of aldosterone, amongst other actions the combined effect of which is reduction of blood pressure.

Uses

Angiotensin II receptor antagonists are primarily used for the treatment of hypertension where the patient is intolerant of ACE inhibitor therapy. They do not inhibit the breakdown of bradykinin or other kinins, and are thus only rarely associated with the persistent dry cough that commonly limits ACE inhibitor therapy. More recently, they have been used for the treatment of heart failure in patients intolerant of ACE inhibitor therapy, particularly candesartan. Irbesartan and losartan have trial data showing benefit in hypertensive patients with type II diabetes, and may delay the progression of diabetic nephropathy.

Adverse effects

This class of drugs is usually well-tolerated, with common adverse drug reactions (ADRs) including: dizziness, headache, and/or hyperkalaemia. Infrequent ADRs associated with therapy include: first dose orthostatic hypotension, rash, diarrhoea, dyspepsia, abnormal liver function, muscle cramp, myalgia, back pain, insomnia, decreased haemoglobin levels, renal impairment, pharyngitis, and/or nasal congestion. (Rossi, 2006)

While one of the main rationales for the use of this class is the avoidance of dry cough associated with ACE inhibitor therapy, it may still rarely occur. Additionally, there is also a small risk of cross-reactivity in patients who have experienced angioedema with ACE inhibitor therapy. (Rossi, 2006)

Members

  • Candesartan
    Eprosartan
    Irbesartan
    Losartan
    Olmesartan
    Telmisartan
    Valsartan

References

  • Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.

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