Losartan

Indications

• hypertension

  • reduction of renal disease progression in patients with type 2 diabetes, hypertension and microalbuminuria (>30 mg/24 hours) or proteinuria (>900 mg/24 hours)

Administration/Absorption

• • Well absorbed following oral administration

  • Undergoes significant first-pass metabolism to produce 5-carboxylic acid metabolite, designated as EXP3174.

  • This metabolite is a long-acting (6 to 8 hr), noncompetitive antagonist at the AT1 receptor and contributes to the pharmacological effects of Losartan.

  • This metabolite is 10-40 times more potent in blocking AT1 receptors than the original Losartan.

Distribution

• • bioavailability is about 32%.

Mechanism

• angiotensin II receptor antagonist

Excretion