Table 1. Blood levels of various NNRTIs.
Drug (in vitro EC 50) | Author | Daily Dose | Limitations | Measured after intake | Measured samples | C mean (ng/ml) | C max (ng/ml) | Number of blood levels > EC50 | Ratio EC50 / C mean |
---|---|---|---|---|---|---|---|---|---|
EFV | Manosuthi 2005 [19] | 1x600mg | concurrent Rifampicin | 12h | 42 | 3020 | 12210 | 1 (2.4%) | 3.3 |
(31.5μmol/l = | “ | 1x800mg | concurrent Rifampicin | 12h | 42 | 3390 | 21310 | 6 (14.3%) | 2.9 |
9944ng/ml) | Marzolini 2001 [20] | 1x600mg | 14h | 171 | 2188 | 15230 | 6 (3.5%) | 4.5 | |
Gutierrez 2005 [21] | 1x600mg | 12h | 58 | 4120 | 12590 | 3 (5.2%) | 2.4 | ||
NVP | Ratanasuwan 2012 [22] | 2x200mg | Post-dose | 108 | 6671 | ~25000 | 0 | 9.6 | |
(239μmol/l = | Nafrialdi 2012 [23] | 2x200mg | 24 | 7950 | ~15000 | 0 | 8.0 | ||
63786ng/ml) | Wang 2011 [17] | 2x200mg | CR group | 2h | 87 | 6850 | ~15000 | 0 | 9.3 |
“ | 2x200mg | CR group | 12h | 34 | 5180 | 12.3 | |||
ETR | DeJesus 2010 [24] | 1x400mg | 4h | 20 | 801 | 1410 | 0 | 48.4 | |
(89.0μmol/l = | Kakuda 2009 [25] | 2x800mg | early formulation | 3h | 15 | 935 | 41.5 | ||
38740ng/ml) | Gruzdev 2003 [26] | 2x900mg | early formulation | 3h | 12 | 418 | 92.7 | ||
LSV | Vourvahis 2012 [27] | 1x2400mg | healthy volunteers | 4h | 48 | 1727 | ~3000 | 0 | 97.6 |
(543μmol/l = | Vourvahis 2010 [28] | 1x750mg | healthy volunteers | 4h | 14 | 1524 | 111 | ||
168523ng/ml) | Vourvahis 2012 [29] | 2x1000mg | healthy volunteers | 4h | 16 | 1328 | 127 | ||
DLV (171μmol/l | Justesen 2004 [30] | 2x1000mg | healthy volunteers | 1h | 3 | 14890 | 24840 | 0 | 5.2 |
= 78072ng/ml) | Cheng 1997 [31] | 3x400mg | 1h | 8 | 12144 | 6.4 | |||
RPV (24.4μmol/l | Goebel 2006 [32] | 1x150mg | 4h | 9 | 922 | 9.7 | |||
= 8941ng/ml) | Ford 2013 [33] | 1x25mg | healthy volunteers | 4h | 16 | 148 | 60.4 |
Several studies about blood concentrations of NNRTIs in patients are compared to the in vitro EC50 of cytotoxicity against cancer cells. (C mean: mean of all measured blood concentrations in a cohort; C max: highest blood concentration measured in one patient in a cohort)