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Pharmacokinetics of cefoperazone after single and multiple doses
International Journal of Clinical Pharmacology Research
|January 1, 1986
Summary
Cefoperazone exhibits favorable pharmacokinetics with high bioavailability (~95%) via intramuscular injection and no accumulation with multiple doses. Its protein binding ensures effective serum concentrations for treating bacterial infections.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Drug Metabolism
Background:
- Understanding cefoperazone's pharmacokinetic profile is crucial for optimizing its therapeutic use.
- Previous studies may not have fully elucidated its behavior after both intravenous and intramuscular administration.
Purpose of the Study:
- To determine the pharmacokinetics of cefoperazone after single and multiple intravenous (IV) and intramuscular (IM) administrations in humans.
- To assess drug accumulation, serum concentrations, urinary excretion, and bioavailability.
Main Methods:
- Ten subjects received eleven successive doses (500 and 1000 mg) of cefoperazone at 12-hour intervals via IM and IV routes.
- Serum concentrations and urinary excretion were measured after the first, fifth, and eleventh doses.
Main Results:
- Peak serum levels were achieved rapidly after both IM (1.0 hr) and IV (5 min) administration.
- No significant drug accumulation was observed with multiple dosing.
- Terminal serum half-life was consistent (2.1-2.8 hours) across doses and routes.
- Absolute bioavailability of IM cefoperazone was approximately 95% compared to IV administration.
Conclusions:
- Cefoperazone demonstrates favorable pharmacokinetic properties, including high bioavailability and predictable elimination.
- High serum protein binding (90%) contributes to prolonged effective serum concentrations.
- These characteristics, combined with its antibacterial activity, suggest efficacy in treating human bacterial infections.