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Related Experiment Videos

Interaction between theophylline and enoxacin.

K Takagi1, T Hasegawa, K Yamaki

  • 1Second Department of Internal Medicine, Nagoya University School of Medicine, Japan.

International Journal of Clinical Pharmacology, Therapy, and Toxicology
|June 1, 1988
PubMed
Summary
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Enoxacin significantly increases theophylline levels in the body by inhibiting its metabolism, leading to higher plasma concentrations. This interaction necessitates further study to understand theophylline dosage relationship with enoxacin-induced side effects.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Clinical Pharmacy

Background:

  • Theophylline is a widely used medication for respiratory diseases.
  • Enoxacin is an antibiotic that can potentially interact with other drugs.
  • Understanding drug-drug interactions is crucial for patient safety.

Purpose of the Study:

  • To investigate the pharmacokinetic and metabolic interactions between theophylline and enoxacin.
  • To assess the impact of enoxacin on theophylline plasma concentrations and its metabolic pathways.

Main Methods:

  • A pharmacokinetic study was conducted in seven healthy male volunteers.
  • Subjects received sustained-release theophylline alone and concurrently with enoxacin.
  • Plasma and urine samples were analyzed using high-performance liquid chromatography (HPLC).

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Main Results:

  • Enoxacin coadministration resulted in a threefold increase in mean steady-state theophylline plasma concentrations.
  • Total body clearance of theophylline decreased by 63% with no change in plasma protein binding.
  • Urinary theophylline concentrations increased, while 3-methylxanthine levels decreased, suggesting inhibition of 1-demethylation.

Conclusions:

  • Enoxacin significantly inhibits theophylline metabolism, primarily affecting the 1-demethylation pathway.
  • The observed increase in theophylline levels may be linked to enoxacin-induced side effects.
  • Further research is needed to correlate theophylline dosage and plasma levels with enoxacin-related adverse events.