|
EFV
|
ETR
|
NVP
|
RPVa
|
ATV
+/-
RTV |
PK data |
With unboosted ATV
ATV: AUC ↓ 74%
EFV: no significant change
With (ATV 300 mg + RTV 100 mg) once daily with food
ATV concentrations similar to those with unboosted ATV without EFV
|
With unboosted ATV
ETR: AUC ↑ 50%, Cmax ↑ 47%, and Cmin ↑ 58%
ATV: AUC ↓ 17% and
Cmin ↓ 47%
With (ATV 300 mg + RTV 100 mg) once daily
ETR: AUC, Cmax, and Cmin ↑ approximately 30%
ATV: AUC ↓ 14% and
Cmin ↓ 38%
|
With (ATV 300 mg + RTV 100 mg) once daily
ATV: AUC ↓ 42%
and
Cmin ↓ 72%
NVP: AUC ↑ 25% |
With boosted and unboosted ATV
↑ RPV possible |
Dose |
Do not co-administer with unboosted ATV.
In ART-naive patients
(ATV 400 mg + RTV 100 mg) once daily
Do not co-administer in ART experienced patients.
|
Do not co-administer with
ATV +/− RTV. |
Do not co-administer with ATV +/− RTV. |
Standard |
DRV
(always use with RTV) |
PK Data |
With (DRV 300 mg + RTV 100 mg) BID
DRV: AUC ↓ 13%, Cmin ↓ 31%
EFV: AUC ↑ 21% |
ETR 100 mg BID with (DRV 600 mg + RTV 100 mg) BID
DRV: no significant change
ETR: AUC ↓ 37%, Cmin ↓ 49% |
With (DRV 400 mg + RTV 100 mg) BID
DRV: AUC ↑ 24%b
NVP: AUC ↑ 27% and
Cmin ↑ 47% |
RPV 150 mg once daily with (DRV 800 mg + RTV 100 mg) once daily
DRV: no significant change
RPV: AUC ↑ 130% and Cmin ↑ 178% |
Dose |
Clinical significance unknown. Use standard doses and monitor patient closely. Consider monitoring drug levels. |
Standard (ETR 200 mg BID).
Safety and efficacy of this combination, despite decreased ETR concentration, have been established in a clinical trial.
|
Standard |
Standard |
EFV |
PK Data |
•
|
↓ ETR possible |
NVP: no significant change
EFV: AUC ↓ 22% |
↓ RPV possible |
Dose |
Do not co-administer.
|
Do not co-administer.
|
Do not co-administer.
|
ETR |
PK Data |
↓ ETR possible |
•
|
↓ ETR possible |
↓ RPV possible |
Dose |
Do not co-administer. |
Do not co-administer. |
Do not co-administer. |
FPV |
PK Data |
With (FPV 1400 mg + RTV 200 mg) once daily
APV: Cmin ↓ 36% |
With (FPV 700 mg + RTV 100 mg) BID
APV: AUC ↑ 69%, Cmin ↑ 77% |
With unboosted FPV 1400 mg BID
APV: AUC ↓ 33%
NVP: AUC ↑ 29%
With (FPV 700 mg + RTV 100 mg) BID
NVP: Cmin ↑ 22%
|
With boosted and unboosted FPV
↑ RPV possible
|
Dose |
(FPV 1400 mg + RTV 300 mg) once daily or (FPV 700 mg + RTV 100 mg) BID
EFV standard |
Do not co-administer with
FPV +/− RTV. |
(FPV 700 mg + RTV 100 mg) BID
NVP standard |
Standard |
LPV/r |
PK Data |
With LPV/r tablets 500/125 mg BIDc + EFV 600 mg
LPV levels similar to
LPV/r 400/100 mg BID without EFV |
With LPV/r tablets
ETR: AUC ↓ 35% (comparable to the decrease with DRV/r)
LPV: AUC↓ 13% |
With LPV/r capsules
LPV: AUC ↓ 27% and Cmin ↓51% |
RPV 150 mg once daily with LPV/r capsules
LPV: no significant change
RPV: AUC ↑ 52% and
Cmin ↑ 74% |
Dose |
LPV/r tablets 500/125 mgc BID; LPV/r oral solution 533/133 mg BID
EFV standard
|
Standard |
LPV/r tablets 500/125 mgc BID; LPV/r oral solution 533/133 mg BID
NVP standard
|
Standard |
NVP |
PK Data |
NVP: no significant change
EFV: AUC ↓ 22% |
↓ ETR possible |
•
|
↓ RPV possible |
Dose |
Do not co-administer. |
Do not co-administer. |
Do not co-administer. |
RPV |
PK Data |
↓ RPV possible |
↓ RPV possible |
↓ RPV possible |
•
|
Dose |
Do not co-administer. |
Do not co-administer. |
Do not co-administer. |
RTV |
PK Data |
Refer to information for boosted PI. |
Refer to information for boosted PI. |
Refer to information for boosted PI. |
Refer to information for boosted PI. |
Dose |
SQV
(always use with RTV) |
PK Data |
With SQV 1200 mg TID
SQV: AUC ↓ 62%
EFV: AUC ↓ 12% |
With (SQV 1000 mg + RTV 100 mg) BID
SQV: AUC unchanged
ETR: AUC ↓ 33%, Cmin ↓ 29%
Reduced ETR levels similar to reduction with DRV/r |
With 600 mg TID
SQV: AUC ↓ 24%
NVP: no significant change |
↑ RPV possible |
Dose |
(SQV 1000 mg + RTV 100 mg) BID |
(SQV 1000 mg +
RTV 100 mg) BID |
Dose with SQV/r not established |
Standard |
TPV
(always use with RTV) |
PK Data |
With (TPV 500 mg +
RTV 100 mg) BID
TPV: AUC ↓ 31%, Cmin ↓ 42%
EFV: no significant change
With (TPV 750 mg +
RTV 200 mg) BID
TPV: no significant change
EFV: no significant change
|
With (TPV 500 mg +
RTV 200 mg) BID
ETR: AUC ↓ 76%, Cmin ↓ 82%
TPV: AUC ↑ 18%, Cmin ↑ 24% |
With (TPV 250 mg +
RTV 200 mg) BID and with (TPV 750 mg +
RTV 100 mg) BID
NVP: no significant change
TPV: no data |
↑ RPV possible |
Dose |
Standard |
Do not co-administer. |
Standard |
Standard |