CEFADROXIL, CEFACLOR, CEFUROXIME - INTERSTITIAL FLUID CONCENTRATIONS DETERMINED THROUGH A SKIN WINDOW

CEFADROXIL, CEFACLOR, CEFUROXIME - INTERSTITIAL FLUID CONCENTRATIONS DETERMINED THROUGH A SKIN WINDOW

Tan J S; Salstrom S J M; File T M

Advances in Therapy

1994

1994-05

The complex interaction between plasma and tissue concentrations of drug has significant implications for therapies that use beta-lactam antibiotics. This comparative, triple-crossover, open-label study enrolled 12 healthy adult male volunteers to determine interstitial fluid concentrations of cefadroxil, cefaclor, and cefuroxime. Each participant, by random assignment, received therapeutically equivalent (in skin and skin-structure infections) single oral doses of cefadroxil 500 mg, cefaclor 250 mg, and cefuroxime axetil 250 mg on separate occasions 1 week apart. Serum and interstitial fluid (by skin-window technique) concentrations were assayed sequentially to determine persistence and magnitude of antibiotic penetration into interstitial fluid. Statistically higher concentrations of cefadroxil (5.5 mug/mL) than of cefaclor (1.2 mug/mL) and cefuroxime (1.1 mug/mL) were documented in interstitial fluid. Cefadroxil (0.63) also demonstrated a tissue fluid:blood area under the curve ratio significantly greater than that achieved by cefaclor (0.48) and comparable to that of cefuroxime axetil (0.60). No significant adverse events occurred with any study medication. The distribution to interstitial fluids and reliable tissue penetration are fundamental principles of successful antibacterial therapy of skin and skin-structure infections. The excellent tissue and interstitial fluid penetration of cefadroxil may contribute to its high degree of efficacy when administered once daily.

cefaclor; cefadroxil; cefuroxime; interstitial fluid; pharmacokinetics; Pharmacology & Pharmacy; Research & Experimental Medicine; skin window

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Journal Article

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