European Journal of Clinical Pharmacology

, Volume 24, Issue 4, pp 453–456 | Cite as

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

  • H. Knauf
  • W. Möhrke
  • E. Mutschler
Originals

Summary

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 extrarenal elimination is less important. Administration of this antikaliuretic is therefore considered hazardous in patients with impaired kidney function.

Key words

triameteren renal failure hydroxytriamterene sulphate pharmacokinetics plasma protein binding urinary excretion renal tubular secretion 

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Copyright information

© Springer-Verlag 1983

Authors and Affiliations

  • H. Knauf
    • 1
  • W. Möhrke
    • 2
  • E. Mutschler
    • 2
  1. 1.Department of MedicineUniversity of FreiburgFreiburgFederal Republic of Germany
  2. 2.Pharmacological Institute, Department of Pharmacy and BiochemistryUniversity of FrankfurtFrankfurtFederal Republic of Germany

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