Allisartan isoproxil

Allisartan Isoproxil

Chemical structure of Allisartan isoproxil

Allisartan isoproxil is a prodrug of the active metabolite EXP3174, which is a potent angiotensin II receptor antagonist. It is used in the management of hypertension by blocking the effects of angiotensin II, a hormone that causes blood vessels to constrict, thereby lowering blood pressure.

Mechanism of Action

Allisartan isoproxil is converted in the body to its active form, EXP3174, after oral administration. EXP3174 selectively blocks the binding of angiotensin II to the angiotensin II receptor type 1 (AT1 receptor) in various tissues, including vascular smooth muscle and the adrenal gland. This blockade prevents the vasoconstrictor and aldosterone-secreting effects of angiotensin II, leading to vasodilation and a reduction in blood pressure.

Pharmacokinetics

After oral administration, allisartan isoproxil is rapidly absorbed and converted to its active form. The bioavailability of the active metabolite is influenced by factors such as food intake and individual metabolic differences. The drug is primarily excreted via the kidneys, and its half-life allows for once-daily dosing.

Clinical Use

Allisartan isoproxil is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. The drug is particularly useful in patients who require a reduction in blood pressure to prevent complications such as stroke, myocardial infarction, and heart failure.

Side Effects

Common side effects of allisartan isoproxil include dizziness, headache, and fatigue. These effects are generally mild and transient. Serious adverse effects are rare but may include renal impairment and hyperkalemia, particularly in patients with pre-existing kidney disease or those taking other medications that affect renal function.

Comparison with Other Angiotensin Receptor Blockers

Chemical structure of Losartan carboxylic acid

Allisartan isoproxil is similar to other angiotensin receptor blockers (ARBs) such as losartan, valsartan, and candesartan. Each ARB has unique pharmacokinetic properties and may be chosen based on patient-specific factors. Allisartan isoproxil's prodrug nature allows for effective oral administration and conversion to its active form, similar to the conversion of losartan to its active metabolite.

Related Pages

• Hypertension
• Angiotensin II receptor antagonist
• Losartan
• Valsartan
• Candesartan