Simultaneous pharmacokinetic modeling of gentamicin, tobramycin and vancomycin clearance from neonates to adults: towards a semi-physiological function for maturation in glomerular filtration

Pharm Res. 2014 Oct;31(10):2643-54. doi: 10.1007/s11095-014-1361-z. Epub 2014 May 2.

Abstract

Purpose: Since glomerular filtration rate (GFR) is responsible for the elimination of a large number of water-soluble drugs, the aim of this study was to develop a semi-physiological function for GFR maturation from neonates to adults.

Methods: In the pharmacokinetic analysis (NONMEM VI) based on data of gentamicin, tobramycin and vancomycin collected in 1,760 patients (age 1 day-18 years, bodyweight 415 g-85 kg), a distinction was made between drug-specific and system-specific information. Since the maturational model for clearance is considered to contain system-specific information on the developmental changes in GFR, one GFR maturational function was derived for all three drugs.

Results: Simultaneous analysis of these three drugs showed that maturation of GFR mediated clearance from preterm neonates to adults was best described by a bodyweight-dependent exponent (BDE) function with an exponent varying from 1.4 in neonates to 1.0 in adults (ClGFR = Cldrug*(BW/4 kg)(BDE) with BDE = 2.23*BW(-0.065)). Population clearance values (Cldrug) for gentamicin, tobramycin and vancomycin were 0.21, 0.28 and 0.39 L/h for a full term neonate of 4 kg, respectively.

Discussion: Based on an integrated analysis of gentamicin, tobramycin and vancomycin, a semi-physiological function for GFR mediated clearance was derived that can potentially be used to establish evidence based dosing regimens of renally excreted drugs in children.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Adolescent
  • Adult
  • Aging / blood
  • Aging / physiology*
  • Body Weight / physiology
  • Child
  • Child, Preschool
  • Creatinine / blood
  • Gentamicins / pharmacokinetics*
  • Glomerular Filtration Rate / physiology*
  • Humans
  • Infant
  • Infant, Newborn
  • Metabolic Clearance Rate
  • Models, Biological*
  • Tobramycin / pharmacokinetics*
  • Vancomycin / pharmacokinetics*

Substances

  • Gentamicins
  • Vancomycin
  • Creatinine
  • Tobramycin