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. 2016 Oct 21;60(11):6813–6822. doi: 10.1128/AAC.01000-16

TABLE 3.

Plasma and urine metabolic ratios of EFV in healthy volunteers after a single 100-mg oral dose of EFV at baseline (control) and after treatment with voriconazole to steady state

PK parameter Mean ± SD for group:
% mean change P value
Control Voriconazoleb
Plasma AUC metabolic ratio (AUC of EFV/AUC of metabolite)
    8-OHEFV
        0–12 h 4.6 ± 3.1 12.0 ± 6.3 189 <0.001
        0–24 h 4.4 ± 3.1 10.7 ± 5.6 171 <0.001
        0–48 h 4.1 ± 3.3 9.1 ± 5.1 146 <0.001
    7-OHEFV
        0–12 h 156 ± 206 133 ± 126 18 0.09
        0–24 h 137 ± 209 109 ± 101 17 0.09
        0–48 h 126 ± 209 93 ± 83 16 0.09
    Di-OHEFV
        0–12 h 12.7 ± 10.2 56.2 ± 39.9 383 <0.001
        0–24 h 11.9 ± 10.7 48.5 ± 35.7 343 <0.001
        0–48 h 11.5 ± 12.6 40.2 ± 31.5 291 <0.001
0- to 48-h molar ratio (Ae of metabolite/Ae of EFV)a
    8-OHEFV/EFV 684 ± 386 304 ± 158 −49.1 <0.001
    7-OHEFV/EFV 169 ± 119 110 ± 62 −21.4 <0.001
    Di-OHEFV/EFV 516 ± 285 164 ± 90 −62.1 <0.001
    Di-OHEFV/8-OHEFV 0.8 ± 0.2 0.6 ± 0.5 −29.5 <0.001
    8- + di-OHEFV/EFV 1,200 ± 655 468 ± 240 −55.3 <0.001
a

Ratios are large because EFV excreted unchanged was relatively small.

b

Note that the effect of voriconazole on plasma MRs was larger than that on urine MRs.