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

TABLE 2.

Urinary excretion parameters of EFV and metabolites in healthy volunteers after a single 100-mg oral dose of EFV alone (control) and after treatment with voriconazole to steady state

Parameter Mean ± SD for group:
% mean change P value
Control Voriconazole
Amt (Ae0–48, nmol) recovered in urine over 48 h
    EFV 27.0 ± 12.8 36.0 ± 20.3 50.1 <0.001
        % dose 0.009 ± 0.004 0.012 ± 0.006 <0.001
    8-OHEFV 15,733 ± 6,362 9,334 ± 5,015 −33.3 <0.001
        % dose 5.0 ± 2.0 3.0 ± 1.6 <0.001
    7-OHEFV 4,030 ± 2,459 3,363 ± 1,501 8.5 <0.01
        % dose 1.3 ± 0.8 1.1 ± 0.5 <0.01
    Di-OHEFV 11,871 ± 4,803 5,088 ± 3,245 −48.8 <0.001
        % dose 3.8 ± 1.5 1.6 ± 1.0 <0.001
    8- + di-OHEFV 27,603 ± 10,681 14,422 ± 8,021 −41.1 <0.001
        % dose 8.7 ± 3.4 4.6 ± 2.5 <0.001
        Total % of dose 10.0 ± 3.9 5.6 ± 2.6 <0.001
CLfa of EFV to metabolite (ml/min)
    EFV to 8-OHEFV 558 ± 272 219 ± 209 −61.5 <0.001
        % total CLf 49.0 ± 6.4 51.5 ± 7.2 6.2 <0.01
    EFV to 7-OHEFV 141 ± 99 74 ± 34 −39.8 <0.001
        % total CLf 12.4 ± 5.6 19.8 ± 8.4 70.1 <0.001
    8-OHEFV to di-OHEF 1,505 ± 649 940 ± 784 −37.1 <0.001
    EFV to 8- + di-OHEFV 996 ± 468 345 ± 349 −66.5 <0.001
        % total CLf 87.6 ± 5.6 80.2 ± 8.4 −9.0 <0.001
a

CLf, 0- to 48-h formation clearance.