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Enprofylline kinetics in healthy subjects after single doses
Clinical Pharmacology and Therapeutics
|December 1, 1983
Summary
Enprofylline, an antiasthmatic drug, is primarily eliminated by the kidneys in healthy adults. Unlike theophylline, its elimination pathway involves significant active tubular secretion.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Drug Metabolism
Background:
- Enprofylline is a novel xanthine derivative developed for asthma treatment.
- Understanding its pharmacokinetic profile is crucial for effective therapeutic use.
Purpose of the Study:
- To investigate the pharmacokinetic properties of enprofylline in healthy subjects.
- To determine the primary routes of enprofylline elimination.
Main Methods:
- Single intravenous doses of enprofylline (0.5, 1, 1.5 mg/kg) were administered to eight healthy volunteers.
- Plasma and urine samples were collected over 24 hours to measure enprofylline concentrations.
- Pharmacokinetic parameters including half-life, volume of distribution, and clearance were calculated.
Main Results:
- Plasma half-life (t 1/2) ranged from 1.2 to 1.9 hours.
- Total body clearance averaged 0.25 L/hr/kg.
- Renal clearance was high (200-400 mL/min), with 89% of the dose recovered unchanged in urine, suggesting active tubular secretion.
Conclusions:
- Enprofylline is predominantly eliminated renally, mainly through active tubular secretion.
- This elimination pathway differs significantly from theophylline, another xanthine derivative.