Understanding the Pharmacokinetics of Prodrug and Metabolite

Overview

Journal Transl Clin Pharmacol

Date 2020 Feb 15

PMID 32055540

Citations 11

Authors

Seungil Cho

Young-Ran Yoon

Affiliations

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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.

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