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Theophylline product and dosing interval selection for chronic asthma
The Journal of Allergy and Clinical Immunology
|August 1, 1985
Summary
Slow-release theophylline formulations offer stable serum concentrations, but significant absorption differences exist. Many products are clinically inadequate for once-daily dosing, especially in rapid metabolizers.
Area of Science:
- Pharmacology
- Clinical Pharmacy
Background:
- Conventional theophylline formulations cause significant serum concentration fluctuations.
- Slow-release (SR) theophylline aims for stable concentrations and improved compliance.
- Significant variability exists in absorption characteristics among available SR theophylline products.
Purpose of the Study:
- To evaluate the clinical implications of absorption variability among SR theophylline formulations.
- To identify appropriate dosing strategies based on patient elimination rates and product absorption profiles.
- To assess the impact of food on the absorption of different theophylline formulations.
Main Methods:
- Analysis of pharmacokinetic data for various SR theophylline products.
- Comparison of steady-state serum concentrations based on product absorption and patient elimination rates.
- Evaluation of food-drug interactions for specific theophylline formulations.
Main Results:
- Clinically relevant differences among SR theophylline products are not apparent in slow-eliminating patients with twice-daily dosing.
- In rapid-eliminating patients, only two SR products demonstrated sufficiently slow absorption for twice-daily use.
- Several "once-a-day" SR theophylline products are clinically inadequate; some require 8-hour dosing intervals.
- Food intake can cause dose dumping with Theo-24 and impair absorption with Theo-Dur Sprinkle.
Conclusions:
- Significant inter-product variability in SR theophylline absorption necessitates careful formulation selection.
- Current "once-a-day" SR theophylline products are not universally suitable, particularly for rapid metabolizers.
- Patient-specific factors (elimination rate) and food interactions significantly influence theophylline therapy effectiveness and safety.
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