Lack of a kinetic interaction between fluconazole and mexiletine.
OBJECTIVE
To investigate the effect of fluconazole on the kinetics of mexiletine.


METHODS
Six healthy male volunteers participated in a crossover study. On the 1st day, the subjects received 200 mg mexiletine alone. On days 2-7 they received 200 mg fluconazole orally, and on day 8 they received 200 mg mexiletine and 200 mg fluconazole concomitantly. In a third phase two subjects received 400 mg fluconazole daily.


RESULTS
No differences in concentrations were observed between the three phases. The area under the concentration curves (AUC) after administration of mexiletine alone and in combination with fluconazole 200 mg/day were 6.63 and 7.31 micrograms.h.ml-1, respectively.


CONCLUSIONS
These findings suggest that fluconazole does not inhibit mexiletine metabolism.
Ueno
K
K
Department of Pharmacy, National Sengokuso Hospital, Osaka, Japan.
Yamaguchi
R
R
Tanaka
K
K
Sakaguchi
M
M
Morishima
Y
Y
Yamauchi
K
K
Iwai
A
A
D000328:Adult; D000889:Anti-Arrhythmia Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D019388:Cytochrome P-450 CYP1A2; D065607:Cytochrome P-450 Enzyme Inhibitors; D004347:Drug Interactions; D004791:Enzyme Inhibitors / Q000494:pharmacology; D015725:Fluconazole / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D008297:Male; D008801:Mexiletine / Q000493:pharmacokinetics* / Q000494:pharmacology; D010088:Oxidoreductases / Q000037:antagonists & inhibitors
D000889:Anti-Arrhythmia Agents; D000935:Antifungal Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D008801:Mexiletine; D015725:Fluconazole; D010088:Oxidoreductases; D019388:Cytochrome P-450 CYP1A2