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Pharmacokinetics of organic nitrates in man: an overview

  • 0Heymans Institute of Pharmacology, University of Gent Medical School, Belgium.
European Heart Journal +

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January 1, 1988

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January 1, 1988

View abstract on PubMed

Summary

This summary is machine-generated.

The pharmacokinetics of glyceryl trinitrate and isosorbide dinitrate vary significantly. While plasma concentrations can be measured, they do not reliably predict therapeutic effects due to tolerance and counter-regulation.

Area Of Science

  • Pharmacology
  • Clinical Pharmacy

Background

  • The pharmacokinetics of glyceryl trinitrate (GTN) are not fully elucidated.
  • GTN is rapidly eliminated from plasma via extrahepatic pathways, metabolized into glyceryl dinitrates and mononitrates.

Purpose Of The Study

  • To review the current understanding of glyceryl trinitrate and isosorbide dinitrate pharmacokinetics.
  • To discuss the relationship between plasma concentrations and therapeutic effects of these nitrates.

Main Methods

  • Review of existing literature on nitrate pharmacokinetics.
  • Analysis of plasma concentration data following different administration routes.

Main Results

  • Transdermal GTN can maintain plasma concentrations, but significant inter- and intra-individual variability exists.
  • Isosorbide dinitrate exhibits slower elimination and more predictable plasma concentrations, especially with sustained-release formulations.
  • Measured plasma nitrate concentrations do not correlate with therapeutic effects due to rapid development of tolerance and counter-regulatory mechanisms.

Conclusions

  • Nitrate pharmacokinetics, particularly GTN, show considerable variability.
  • Predicting nitrate efficacy solely based on plasma concentrations is unreliable due to physiological responses like tolerance.