Possible Interaction: Ketoconazole and Quinine

“ Ketoconazole , a potent inhibitor of CYP3A4, is known to markedly increase plasma concentrations of various co‐administered drugs including quinine.”

“ KTZ enhanced the therapeutic antischistosomal potential of QN and HF over each drug alone.”

“ KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone.”

“ QN and HF significantly (P<0.05) elevated malondialdehyde levels when used alone or with KTZ.”

“ Ketoconazole and troleandomycin inhibited the 3-hydroxylation of quinine in all species.”

“When the plasma/serum concentrations possibly attained after their usual therapeutic doses were taken into account, tetracycline, doxycycline, omeprazole, ketoconazole , nifedipine, troleandomycin and erythromycin are likely to be inhibitors of quinine metabolism in patients when these drugs are co-administrated with quinine.”

“ KTZ racemate and enantiomers showed differential inhibitory effects of quinine and alprazolam metabolism.”

“ Quinine metabolism catalyzed by HLM, CYP3A4 and CYP3A5 was potently inhibited by the trans-enantiomer KTZ 2S,4S, with IC50 value of 0.16 μM for HLM, 0.04 μM for CYP3A4 and 0.11 μM for CYP3A5.”

“Two inhibitors of CYP3A4, ketoconazole (1 microM) and troleandomycin (100 microM), inhibited quinine 3-hydroxylation by about 90% and 80%, and etoposide 3'-demethylation by about 75% and 65%, respectively.”

“ Ketoconazole and troleandomycin (inhibitors of … the 3-hydroxylation of quinine by human liver microsomes with respective mean IC50 values of 0.026 microM and 28.9 microM. Anti-CYP3A antibodies … inhibited quinine 3-hydroxylation, whereas weak inhibition was observed in the presence of S-mephenytoin or anti-CYP2C antibodies.”