Understanding the pharmacokinetics of prodrug and metabolite

Seungil Cho, Young Ran Yoon

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

This tutorial explains the pharmacokinetics of a prodrug and its active metabolite (or parent drug) using a two-step, consecutive, first-order irreversible reaction as a basic model for prodrug metabolism. In this model, the prodrug is metabolized and produces the parent drug, which is subsequently eliminated. The mathematical expressions for pharmacokinetic parameters were derived step by step. In addition, we visualized these expressions to help understand the relationship between pharmacokinetic parameters easily. For the elimination rate-limited and formation rate-limited metabolism, we analyzed the plasma drug concentration versus time curve of a prodrug administered intravenously.

Original languageEnglish
Pages (from-to)1-5
Number of pages5
JournalTranslational and Clinical Pharmacology
Volume26
Issue number1
DOIs
StatePublished - 2018

Keywords

  • Elimination rate-limited
  • Formation rate-limited
  • Metabolism
  • Pharmacokinetics
  • Prodrug

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