PHARMACOKINETIC INTERACTION BETWEEN
LINEZOLID AND GRAPEFRUIT JUICE IN RATS.
RODICA CUCIUREANU1*, L. VLASE2, DANA MUNTEAN2,
MAGDALENA CUCIUREANU 3
University of Medicine and Pharmacy “Gr.T.Popa”, Iasi, 16,
Universităţii street, 700115, Romania
1Department of Environmental and Food Chemistry
3Department of Pharmacology
2University of Medicine and Pharmacy “Iuliu Haţieganu”, Cluj-Napoca,
13 Emil Isac street, 400023, Romania Department of Pharmaceutical
Technology and Biopharmaceutics,
*corresponding author: rcuciur@yahoo.com
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Abstract:

Grapefruit juice has been reported to increase the oral availability of many cytochrome P450 substrates, mainly by inhibiting the first-pass metabolism of the drugs metabolized by cytochrome P450 3A in the gut wall rather than in liver. Linezolid is the first of a new class of antimicrobial drugs, is indicated for the treatment of nosocomial pneumonia and complicated skin infections. It was developed a fast and simple liquid chromatography/ mass spectrometry/ mass spectrometry (LC/MS/MS) method able to quantify linezolid in rat plasma after oral administration. Finally, the developed and validated method was applied for the investigation of the pharmacokinetic interaction between linezolid and grapefruit juice.

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