Oral melphalan pharmacokinetics--relation to dose in patients with multiple myeloma

Med Oncol Tumor Pharmacother. 1989;6(2):151-4. doi: 10.1007/BF02985238.

Abstract

The pharmacokinetics of melphalan have been studied after oral doses of 5, 10 and 20 mg, and 10 mg i.v. Seven patients with multiple myeloma received the drug on 4 consecutive days and the concentration of melphalan was determined by liquid chromatography. Melphalan was rapidly absorbed after p.o. administration. Absorption lag-time was less than 1 h. The median time for attaining the peak concentration was 1.12 h (97% confidence interval: 0.68-1.55), 1.21 h (0.85-1.43) and 1.08 h (0.84-1.29) after doses of 5, 10 and 20 mg. The bioavailability showed large interindividual variations, and was not significantly affected by the dose given. There was a significant decrease in bioavailability during the treatment course (P less than 0.05). Absorption of melphalan obeys first-order kinetics in the dose interval studied. The results indicate that it might be of benefit to administrate oral melphalan for fewer days than the usually used 4 day regimen, in an attempt to achieve a higher bioavailability.

MeSH terms

  • Administration, Oral
  • Aged
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Injections, Intravenous
  • Male
  • Melphalan / administration & dosage
  • Melphalan / pharmacokinetics*
  • Middle Aged
  • Multiple Myeloma / drug therapy
  • Multiple Myeloma / metabolism*

Substances

  • Melphalan