Toxicity of high-dose carboplatin: ultrafiltered and not total plasma pharmacokinetics is of clinical relevance

J Clin Pharmacol. 2002 Jul;42(7):762-73. doi: 10.1177/009127002401102704.

Abstract

Combination chemotherapy containing high-dose carboplatin is a therapeutic option for patients with poor-risk germ cell tumors. Since such treatment is relatively toxic, pharmacokinetic characteristics of total and ultrafiltered platinum, representing different species of platinum complexes formed, were investigated in 29 patients in relation to toxicity. The goodness-of-fit parameters revealed that a two-compartment model with weighting (1/C2i) resulted in the best fit. The terminal half-life of total platinum > 5 days was fourfold longer than that of ultrafiltered platinum, indicating long-term retention. At stem cell rescue, an ultrafiltered concentration of < or = 0.223 microg/ml did not impair hematological recovery. Ultrafiltered but not total platinum concentrations or AUC values were significantly correlated to an increase in creatinine concentration and different types of toxicity associated with high-dose treatment. Since the fraction unbound is time dependent and highly variable among patients, measuring ultrafiltered concentrations is highly recommended as they represent the clinically relevant platinum complexes in high-dose treatment.

Publication types

  • Clinical Trial

MeSH terms

  • Aged
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / blood
  • Antineoplastic Agents / pharmacokinetics*
  • Antineoplastic Agents / toxicity*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Carboplatin / administration & dosage
  • Carboplatin / blood
  • Carboplatin / pharmacokinetics*
  • Carboplatin / toxicity*
  • Combined Modality Therapy
  • Dose-Response Relationship, Drug
  • Etoposide / administration & dosage
  • Germinoma / metabolism
  • Germinoma / therapy
  • Half-Life
  • Hematopoietic Stem Cell Transplantation
  • Humans
  • Ifosfamide / administration & dosage
  • Infusions, Intravenous
  • Male
  • Middle Aged
  • Models, Biological
  • Thiotepa / administration & dosage
  • Time Factors
  • Ultrafiltration

Substances

  • Antineoplastic Agents
  • Etoposide
  • Thiotepa
  • Carboplatin
  • Ifosfamide