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Do nitrates differ?

H L Fung1

  • 1Department of Pharmaceutics, School of Pharmacy, State University of New York, Buffalo 14260.

British Journal of Clinical Pharmacology
|January 1, 1992
PubMed
Summary
This summary is machine-generated.

Organic nitrates share a common mechanism but vary in potency and pharmacokinetics. Tolerance limits sustained-release nitrate duration to approximately 12 hours.

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Development

Background:

  • Organic nitrates are widely used vasodilators.
  • Understanding their pharmacokinetic and pharmacodynamic profiles is crucial for effective clinical use.

Purpose of the Study:

  • To elucidate the common mechanism of action for organic nitrates.
  • To compare the pharmacologic potency and pharmacokinetic properties of various organic nitrates.
  • To investigate the factors limiting the duration of action for sustained-release nitrate formulations.

Main Methods:

  • Comparative analysis of in vitro and in vivo data for different organic nitrates.
  • Pharmacokinetic profiling of immediate-release and sustained-release formulations.
  • Assessment of pharmacologic tolerance development.

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Main Results:

  • All organic nitrates exhibit a unified biochemical and physiological mechanism.
  • Significant inter-drug variations in pharmacologic potency and pharmacokinetics were observed, with in vitro differences exceeding in vivo.
  • Pharmacokinetics dictate the duration of action for single doses, while tolerance limits sustained-release nitrates to ~12 hours.

Conclusions:

  • Organic nitrates share a common mechanism but differ in potency and pharmacokinetics.
  • Pharmacologic tolerance is a key limitation for sustained-release nitrate efficacy.
  • Nitrate formulations do not appear to differ in their adverse effect profiles.