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Methylxanthines: toxicity to humans. 1. Theophylline
1Food Research Division, Bureau of Chemical Safety, Health Protection Branch, Ottawa, Ontario, Canada.
Summary
This review summarizes the human toxicity of theophylline, a methylxanthine drug. It covers recent data on theophylline toxicity, benefits, mechanisms, and analytical challenges impacting dose-response findings.
Area of Science:
- Pharmacology
- Toxicology
- Clinical Medicine
Background:
- Methylxanthines like theophylline, caffeine, and theobromine have known toxic effects in animals.
- Comprehensive reviews on human methylxanthine toxicity are lacking.
- Theophylline is a widely used medication with a narrow therapeutic index.
Purpose of the Study:
- To provide an overview of the human toxicity of theophylline.
- To summarize recent and pertinent information on theophylline toxicity.
- To critically review analytical methodology issues affecting reported dose-response data.
Main Methods:
- Literature review focusing on recent publications.
- Synthesis of data on theophylline's human toxicity.
- Critical analysis of analytical methods for theophylline measurement.
Main Results:
- Theophylline exhibits significant human toxicity, with variability influenced by clearance and half-life.
- Information on theophylline's benefits and mechanisms of action is presented.
- Analytical method discrepancies may explain controversies in reported dose-response relationships.
Conclusions:
- This review consolidates current knowledge on theophylline's human toxicity.
- Understanding variability factors and analytical issues is crucial for safe theophylline use.
- Further research is needed to standardize analytical methods and clarify dose-response effects.