Elimination kinetics of labetalol in severe renal failure

Br J Clin Pharmacol. 1982 Jun;13(1 Suppl):81S-86S. doi: 10.1111/j.1365-2125.1982.tb01893.x.


1 The pharmacokinetics of intravenously administered labetalol were studied in four patients with severe renal failure and in three normal subjects. 2 A new and sensitive method for the assay of plasma labetalol concentrations using high performance liquid chromatography is described. 3 Labetalol has a relatively large apparent volume of distribution (3.3-7.9 l/kg, two-compartment open model) and a relatively high plasma clearance (0.3-1.6 1 h-1 kg-1). 4 There were no significant differences between the patients with severe renal failure and the controls for any of the pharmacokinetic parameters measured. 5 In the presence of renal functional impairment, no modification of labetalol dosage is required. 6 In another study of 31 patients, glomerular filtration rate was measured at 3-month intervals for 3-18 months. In ten patients there was no change, in ten there was an improvement and in 11 there was deterioration, but in only three was this attributable to treatment. 7 In our experience with over 300 patients, we conclude that labetalol plus diuretic treatment is efficacious and safe in all grades of hypertension including those with all degrees of renal insufficiency.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Blood Urea Nitrogen
  • Creatinine / blood
  • Ethanolamines / metabolism*
  • Female
  • Glomerular Filtration Rate
  • Half-Life
  • Humans
  • Kidney Failure, Chronic / metabolism*
  • Kidney Failure, Chronic / physiopathology
  • Kinetics
  • Labetalol / metabolism*
  • Male
  • Middle Aged


  • Ethanolamines
  • Creatinine
  • Labetalol