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Author: Admin | 2025-04-28
Active metabolite. The pharmacokinetics of losartan and its active metabolite are linear with oral losartan potassium doses up to 200 mg. Following oral administration, plasma concentrations of losartan and its active metabolite decline polyexponentially, with a terminal half life of about 2 hours and 6-9 hours, respectively. During once daily dosing with 100 mg, neither losartan nor its active metabolite accumulates significantly in plasma. Both biliary and urinary excretions contribute to the elimination of losartan and its metabolites. Following an oral dose/intravenous administration of 14C labelled losartan in man, about 35% / 43% of radioactivity is recovered in the urine and 58%/ 50% in the faeces. Characteristics in patients In elderly hypertensive patients the plasma concentrations of losartan and its active metabolite do not differ essentially from those found in young hypertensive patients. In female hypertensive patients the plasma levels of losartan were up to twice as high as in male hypertensive patients, while the plasma levels of the active metabolite did not differ between men and women. In patients with mild to moderate alcoholinduced hepatic cirrhosis, the plasma levels of losartan and its active metabolite after oral administration were respectively 5 and 1.7 times higher than in young male volunteers (see sections 4.2 and 4.4). Plasma concentrations of losartan are not altered in patients with a creatinine clearance above 10 ml/minute. Compared to patients with normal renal function, the AUC for losartan is about 2 times higher in haemodialysis patients. The plasma concentrations of the active metabolite are not
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