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Fleroxacin clinical pharmacokinetics
1Veterans Affairs Medical Center, Geriatric Research, Education and Clinical Center, Sepulveda, California.
Clinical Pharmacokinetics
|February 1, 1992
Summary
Fleroxacin, a new fluoroquinolone antibiotic, shows broad-spectrum activity and excellent absorption. Dosage adjustments are needed for renal impairment, and antacids can reduce its effectiveness.
Area of Science:
- Pharmacology
- Microbiology
- Drug Metabolism
Background:
- Fleroxacin is a novel fluoroquinolone antibiotic.
- It exhibits broad-spectrum activity against Gram-positive and Gram-negative bacteria.
Purpose of the Study:
- To characterize the pharmacokinetic and metabolic profile of fleroxacin.
- To evaluate its efficacy and safety compared to other fluoroquinolones.
Main Methods:
- High-performance liquid chromatography (HPLC) for drug and metabolite quantification.
- Pharmacokinetic studies involving single and multiple dose regimens.
- Assessment of protein binding, tissue distribution, and elimination pathways.
Main Results:
- Rapid oral absorption with near 100% systemic availability and peak plasma concentrations in 1-2 hours.
- Extensive tissue distribution and predominantly renal elimination (60-70%).
- Metabolism yields active N-demethyl-fleroxacin and inactive N-oxide-fleroxacin; half-life of 10-12 hours.
Conclusions:
- Fleroxacin demonstrates favorable pharmacokinetics, including high bioavailability and a long half-life, surpassing ciprofloxacin.
- Dosage adjustments are crucial in renal impairment due to prolonged elimination.
- Potential drug interactions with antacids and adverse effects like photosensitivity and CNS reactions warrant consideration.