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Phase I study of multiple-dose cefprozil and comparison with cefaclor.
R H Barbhaiya1, U A Shukla, C R Gleason
1Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Company, Syracuse, New York 13221-4755.
Antimicrobial Agents and Chemotherapy
|June 1, 1990
Summary
Cefprozil and cefaclor were well-tolerated cephalosporins. Cefprozil demonstrated a longer half-life and greater AUC, suggesting suitability for twice-daily dosing compared to cefaclor.
Area of Science:
- Pharmacology
- Clinical Pharmacy
Background:
- Cephalosporins are widely used antibiotics.
- Understanding the pharmacokinetic profiles of new cephalosporins is crucial for optimizing dosing regimens.
Purpose of the Study:
- To evaluate the safety and pharmacokinetics of cefprozil following multiple oral doses.
- To compare the pharmacokinetic parameters of cefprozil with those of cefaclor.
Main Methods:
- Healthy volunteers received multiple oral doses of cefprozil (250, 500, or 1,000 mg) or cefaclor (500 mg) every 8 hours for 10 days.
- Serial blood and urine samples were collected for pharmacokinetic analysis on days 1, 5, and 10.
- Safety and tolerance were assessed throughout the study.
Main Results:
- Both cefprozil and cefaclor were well tolerated.
- Cefprozil exhibited dose-linear Cmax, a terminal half-life of 1.2 hours, and dose-proportional AUC.
- Cefprozil had a longer half-life and greater AUC than cefaclor, with higher urine concentrations from 2-8 hours postdosing.
Conclusions:
- Cefprozil demonstrated favorable pharmacokinetic properties, including a longer half-life and greater AUC compared to cefaclor.
- These findings suggest cefprozil may be suitable for twice-daily administration.
- Cefaclor may require more frequent dosing (three to four times daily) to maintain therapeutic levels.