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Pefloxacin clinical pharmacokinetics
F Bressolle1, F Gonçalves, A Gouby
1Laboratoire de Pharmacocinétique, Faculté de Pharmacie, Montpellier, France.
Clinical Pharmacokinetics
|December 1, 1994
Summary
Pefloxacin exhibits broad-spectrum antibacterial activity and penetrates cells, making it effective against intracellular pathogens. Dosage adjustments are needed for liver insufficiency and elderly patients due to altered pharmacokinetics.
Area of Science:
- Pharmacology
- Microbiology
- Infectious Diseases
Background:
- Pefloxacin is a fluoroquinolone antibiotic with broad-spectrum activity.
- It demonstrates excellent penetration into cells and tissues, achieving high tissue-to-serum ratios.
- These properties suggest potential for treating intracellular bacterial infections.
Purpose of the Study:
- To review the pharmacokinetic properties of pefloxacin.
- To evaluate its tissue penetration and potential clinical implications.
- To identify factors affecting its metabolism and excretion.
Main Methods:
- Literature review of pharmacokinetic studies.
- Analysis of data on absorption, distribution, metabolism, and excretion.
- Evaluation of tissue and body fluid concentrations.
Main Results:
- Pefloxacin is well absorbed orally with an elimination half-life of 6.2–12.4 hours.
- Pharmacokinetics change with repeated dosing and are altered in liver insufficiency and elderly patients.
- Renal impairment minimally affects pharmacokinetic parameters.
- High tissue concentrations, particularly in lung and kidney, are achieved, exceeding plasma levels.
- Interactions with hepatic and gastrointestinal drugs occur.
Conclusions:
- Pefloxacin's pharmacokinetic profile supports its use against intracellular pathogens.
- Dosage adjustments are crucial for patients with liver insufficiency and the elderly.
- Monitoring for drug interactions is recommended.
- Its favorable tissue distribution highlights its therapeutic potential in various infections.