1007)
50 mg
once daily
0.88
(0.80, 0.98)
1.01
(0.93, 1.10)
0.92
(0.85, 0.99)
0.99
(0.97, 1.01)
NA
0.99
(0.97, 1.01)
Velpatasvir
100 mg once daily
50 mg
once daily
0.94
(0.86, 1.02)
0.91
(0.84, 0.98)
0.88
(0.82, 0.94)
a OCT2 or MATE1 substrate.
b Norelgestromin is the active metabolite of norgestimate.
No clinically significant differences in the pharmacokinetics of tenofovir (organic aniontransporter [OAT]1 and OAT3 substrates) or para-amino hippurate (OAT1 and OAT3 substrates)were observed when coadministered with dolutegravir.
No clinically significant differences in the pharmacokinetics of trimethoprim/sulfamethoxazolewere observed when coadministered with lamivudine.
Table 9. Effect of Coadministered Drugs on the Pharmacokinetics of Dolutegravir
Coadministered Drug(s)
and Dose(s)
Dose of
Dolutegravir
Geometric Mean Ratio (90% CI) of
Dolutegravir Pharmacokinetic
Parameters with/without Coadministered
Drugs
No Effect = 1.00
Cmax AUC Cau or C24
Antacid (MAALOX)
simultaneous administration
50-mg
single dose
0.28
(0.23 to 0.33)
0.26
(0.22 to 0.32)
0.26
(0.21 to 0.31)
Antacid (MAALOX)
2 h after dolutegravir
50-mg
single dose
0.82
(0.69 to 0.98)
0.74
(0.62 to 0.90)
0.70
(0.58 to 0.85)
Calcium carbonate 1,200 mg
simultaneous administration
(fasted)
50-mg
single dose
0.63
(0.50 to 0.81)
0.61
(0.47 to 0.80)
0.61
(0.47 to 0.80)
Calcium carbonate 1,200 mg
simultaneous administration
(fed)
50-mg
single dose
1.07
(0.83 to 1.38)
1.09
(0.84 to 1.43)
1.08
(0.81 to 1.42)
Calcium carbonate 1,200 mg
2 h after dolutegravir
50-mg
single dose
1.00
(0.78 to 1.29)
0.94
(0.72 to 1.23)
0.90
(0.68 to 1.19)
Carbamazepine
300 mg twice daily
50 mg
once daily
0.67
(0.61 to 0.73)
0.51
(0.48 to 0.55)
0.27
(0.24 to 0.31)
Daclatasvir
60 mg once daily
50 mg
once daily
1.29
(1.07 to 1.57)
1.33
(1.11 to 1.59)
1.45
(1.25 to 1.68)
Ferrous fumarate 324 mg
simultaneous administration
(fasted)
50-mg
single dose
0.43
(0.35 to 0.52)
0.46
(0.38 to 0.56)
0.44
(0.36 to 0.54)
Ferrous fumarate 324 mg
simultaneous administration
(fed)
50-mg
single dose
1.03
(0.84 to 1.26)
0.98
(0.81 to 1.20)
1.00
(0.81 to 1.23)
Ferrous fumarate 324 mg
2 h after dolutegravir
50-mg
single dose
0.99
(0.81 to 1.21)
0.95
(0.77 to 1.15)
0.92
(0.74 to 1.13)
Multivitamin (One-A-Day)
simultaneous administration
50-mg
single dose
0.65
(0.54 to 0.77)
0.67
(0.55 to 0.81)
0.68
(0.56 to 0.82)
Omeprazole
40 mg once daily
50-mg
single dose
0.92
(0.75 to 1.11)
0.97
(0.78 to 1.20)
0.95
(0.75 to 1.21)
Prednisone
60 mg once daily with taper
50 mg
once daily
1.06
(0.99 to 1.14)
1.11
(1.03 to 1.20)
1.17
(1.06 to 1.28)
Rifampina
600 mg once daily
50 mg
twice daily
0.57
(0.49 to 0.65)
0.46
(0.38 to 0.55)
0.28
(0.23 to 0.34)
Rifampinb
600 mg once daily
50 mg
twice daily
1.18
(1.03 to 1.37)
1.33
(1.15 to 1.53)
1.22
(1.01 to 1.48)
Rifabutin
300 mg once daily
50 mg
once daily
1.16
(0.98 to 1.37)
0.95 |
