Active metabolites resulting from decarboxylation, reduction and ester hydrolysis of parent drugs

I. Hartyánszky, H. Kalász, E. Adeghate, Zs Gulyás, M. Y. Hasan, K. Tekes, A. Adem, P. Sótonyi

Research output: Contribution to journalReview article

2 Citations (Scopus)

Abstract

Decarboxylation, reduction and hydrolysis can yield active metabolites from the parent drug. Major therapeutic indications and metabolic routes of these drugs are reviewed. Changes in the logP values (determined and calculated) from the parent drug to the active metabolite show certain characteristics in comparison to other phase I metabolic alterations. Metabolic decarboxylation of parent drug is commonly associated with increase in lipophilicity. However, in some cases, decarboxylation may cause a reduction in lipophilicity. Ester hydrolysis generally unmasks either the polar carboxylic or hydroxyl group with the outcome of an increase in hydrophilicity. On the contrary, hydrolysis of phosphate ester means a huge increase in the lipophilic character of the drug, as the highly polar phosphate group is removed.

Original languageEnglish
Pages (from-to)835-862
Number of pages28
JournalCurrent Drug Metabolism
Volume13
Issue number6
DOIs
Publication statusPublished - Jul 1 2012

Keywords

  • Active metabolites
  • Metabolic decarboxylation
  • Metabolic reduction and metabolic hydrolysis

ASJC Scopus subject areas

  • Pharmacology
  • Clinical Biochemistry

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