Pharmacokinetics of terbutaline in chronic kidney disease

Eur J Clin Pharmacol. 2013 Nov;69(11):1951-4. doi: 10.1007/s00228-013-1566-9. Epub 2013 Jul 31.

Abstract

Purpose: In healthy individuals upwards of 90 % of an injected dose of terbutaline is excreted in the urine. The purpose of this study is to determine the pharmacokinetic properties of terbutaline in patients with severe renal impairment as defined by a glomerular filtration rate (GFR) below 30 mL/min.

Methods: Ten patients were included in the study. GFR was measured with Cr-EDTA clearance. They were given an intravenous injection of 0.500 mg of terbutaline. Blood samples were collected at intervals for 60 h and urine samples were collected for 96 h. The concentration of terbutaline in the blood and in the urine was used to calculate pharmacokinetic parameters.

Results: In patients with normal renal function the total clearance of terbutaline is 2.23-3 mL/min/kg. In our population the total clearance of terbutaline was found to be 1.72 (SD: 0.49) mL/min/kg of which approximately 15 % (0.25 mL/min/kg) was renal clearance. We calculated a distribution volume at steady state of 0.74 (SD: 0.22) L/kg with a terminal half-life of 7.93 (SD: 4.06) hours. The mean residence time (MRT) was 8.35 (SD: 4.93) hours.

Conclusions: In healthy individuals the excretion of terbutaline is foremost renal but this study shows that severe renal impairment does not lower the total clearance of terbutaline to a degree that might be expected from the Cr-EDTA clearance. However, more research is needed to determine if dosage adjustment is warranted in patients with CKD.

Publication types

  • Clinical Trial

MeSH terms

  • Adrenergic beta-2 Receptor Agonists / blood
  • Adrenergic beta-2 Receptor Agonists / pharmacokinetics*
  • Adrenergic beta-2 Receptor Agonists / urine
  • Adult
  • Aged
  • Female
  • Humans
  • Male
  • Middle Aged
  • Renal Insufficiency, Chronic / metabolism*
  • Terbutaline / blood
  • Terbutaline / pharmacokinetics*
  • Terbutaline / urine
  • Young Adult

Substances

  • Adrenergic beta-2 Receptor Agonists
  • Terbutaline