Delayed elimination of triamterene and its active metabolite in chronic renal failure.

Abstract:

:The kinetics of triamterene and its active phase II metabolite were studied in 32 patients with various degrees of impaired renal function; the creatinine clearances ranged from 135 to 10 ml/min. The area under the plasma concentration-time curves (AUC) for triamterene were not influenced by kidney function, but the AUCs for the effective metabolite OH-TA-ester were significantly elevated in renal failure, indicating accumulation of the metabolite. Urinary recovery of triamterene and its metabolite over a 48 h collection period was significantly reduced in renal failure. This is considered to be due to delayed urinary excretion, corresponding to reduced renal clearance. The renal clearance of the native drug exceeded that of the metabolite, because of their different protein binding, 55% for triamterene and 91% for the metabolite. The latter is eliminated almost exclusively via tubular secretion and extra-renal elimination is less important. Administration of this antikaliuretic is therefore considered hazardous in patients with impaired kidney function.

journal_name

Eur J Clin Pharmacol

authors

Knauf H,Möhrke W,Mutschler E

doi

10.1007/BF00609885

subject

Has Abstract

pub_date

1983-01-01 00:00:00

pages

453-6

issue

4

eissn

0031-6970

issn

1432-1041

journal_volume

24

pub_type

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