Guidelines for the Use of Antiretroviral Agents in

HIV-1-Infected Adults and Adolescents

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Table 20a. Interactions between Non-Nucleoside Reverse Transcriptase Inhibitors and Protease
Inhibitorsa (Last updated September 9, 2016; last reviewed April 8, 2015) (Page 1 of 3)
Note: DLV, IDV, and NFV are not included in this table. Refer to the DLV, IDV, and NFV Food and Drug Administration
package inserts for information regarding drug interactions.

NNRTIs
PIs a
EFV ETR NVP RPV
PK Data EFV: no significant ETR AUC 50% and ATV possible RPV possible
change Cmin 58%
ATV ATV AUC 74% ATV AUC 17% and
Unboosted
Cmin 47%

Dose Do not coadminister. Do not coadminister. Do not coadminister. Standard doses

PK Data ATV ATV COBI RPV possible
COBI COBI n ATV expected
Dose EFV standard dose Do not coadminister. Do not coadminister. Standard doses
In ART-Naive Patients:
ATV/c
ATV 400 mg plus COBI
150 mg Once Daily
Do not coadminister in
ART-experienced
patients.
PK Data (ATV 300 mg plus RTV (ATV 300 mg plus RTV (ATV 300 mg plus RTV RPV possible
100 mg) Once Daily: 100 mg) Once Daily: 100 mg) Once Daily:
ATV concentrations are ETR AUC and Cmin ATV AUC 42% and
similar to those with both ~30% Cmin 72%
unboosted ATV without
EFV. ATV AUC n and Cmin NVP AUC 25%
18%
ATV/r Dose EFV standard dose ETR standard dose Do not coadminister. Standard doses
In ART-Naive Patients: (ATV 300 mg plus RTV
(ATV 400 mg plus RTV 100 mg) Once Daily
100 mg) Once Daily
Do not coadminister in
ART-experienced
patients.
PK Data DRV possible Effect on DRV unknown Effect on DRV unknown n DRV expected

DRV/c COBI possible COBI possible COBI possible RPV possible

Dose Do not coadminister. Do not coadminister. Do not coadminister. Standard doses

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Table 20a. Interactions between Non-Nucleoside Reverse Transcriptase Inhibitors, and Protease
Inhibitorsa (Last updated September 9, 2016; last reviewed April 8, 2015) (Page 2 of 3)

NNRTIs
PIs a
EFV ETR NVP RPV
PK Data With (DRV 300 mg plus ETR 100 mg BID with With (DRV 400 mg plus RPV 150 mg Once Daily
RTV 100 mg) BID: (DRV 600 mg plus RTV RTV 100 mg) BID: with (DRV 800 mg plus
EFV AUC 21% 100 mg) BID: NVP AUC 27% and RTV 100 mg) Once Daily:
DRV AUC 13% and ETR AUC 37% and Cmin 47% RPV AUC 130% and
Cmin 31% Cmin 49% DRV AUC 24%
b Cmin 178%
DRV: no significant DRV: no significant
change change
DRV/r
Dose Clinical significance Standard doses Standard doses Standard doses
unknown. Use standard
doses and monitor Safety and efficacy of this
patient closely. Consider combination, despite
monitoring drug levels. reduced ETR
concentration, have been
established in a clinical
trial.
PK Data With (FPV 1400 mg plus With (FPV 700 mg plus With Unboosted FPV With Boosted and
RTV 200 mg) Once Daily: RTV 100 mg) BID: 1400 mg BID: Unboosted FPV:
APV Cmin 36% APV AUC 69% and NVP AUC 29% RPV possible
Cmin 77% APV AUC 33%
With (FPV 700 mg plus
FPV
RTV 100 mg) BID:
+/-
NVP Cmin 22%
RTV
Dose (FPV 1400 mg plus RTV Do not coadminister (FPV 700 mg plus RTV Standard doses
300 mg) Once Daily or with FPV +/ RTV. 100 mg) BID
(FPV 700 mg plus RTV
100 mg) BID NVP standard dose

EFV standard dose

PK Data With LPV/r Tablets With LPV/r Tablets: With LPV/r Capsules: RPV 150 mg Once Daily
c
500/125 mg BID: ETR AUC 35% LPV AUC 27% and with LPV/r Capsules:
LPV concentration (comparable to the Cmin 51% RPV AUC 52% and
similar to that with LPV/r decrease with DRV/r) Cmin 74%
400/100 mg BID without LPV AUC 13% LPV no significant
LPV/r EFV change
Dose LPV/r tablets 500/125 Standard doses LPV/r tablets 500/125 Standard doses
c
mg BID; LPV/r oral mgc BID; LPV/r oral
solution 520/130 mg BID solution 533/133 mg BID
EFV standard dose NVP standard dose

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Table 20a. Interactions between Non-Nucleoside Reverse Transcriptase Inhibitors, and Protease
Inhibitorsa (Last updated September 9, 2016; last reviewed April 8, 2015) (Page 3 of 3)

NNRTIs
PIs a
EFV ETR NVP RPV
PK Data With SQV 1200 mg TID: With (SQV 1000 mg plus With SQV 600 mg TID: RPV possible
EFV AUC 12% RTV 100 mg) BID: NVP: no significant
SQV AUC 62% ETR AUC 33% and change
SQV Cmin 29% SQV AUC 24%
Always SQV AUC n
use with
RTV ETR levels similar to
reduction with DRV/r
Dose (SQV 1000 mg plus RTV (SQV 1000 mg plus RTV Dose with SQV/r not Standard doses
100 mg) BID 100 mg) BID established

PK Data With (TPV 500 mg plus With (TPV 500 mg plus With (TPV 250 mg plus RPV possible
RTV 100 mg) BID: RTV 200 mg) BID: RTV 200 mg) BID or with
EFV no significant ETR AUC 76% and (TPV 750 mg plus RTV
change Cmin 82% 100 mg) BID:
TPV AUC 31% and TPV AUC 18% and NVP: no significant
Cmin 42% Cmin 24% change
TPV
Always TPV: no data
With (TPV 750 mg plus
use with RTV 200 mg) BID:
RTV
EFV: no significant
change
TPV: no significant
change

Dose Standard doses Do not coadminister. Standard doses Standard doses

a
Approved dose for RPV is 25 mg once daily. Most PK studies were performed using 75 mg to 150 mg RPV per dose.
b
Based on between-study comparison.
c
Use a combination of two LPV/r 200 mg/50 mg tablets plus one LPV/r 100 mg/25 mg tablet to make a total dose of LPV/r 500 mg/125 mg.
Key to Symbols: = increase, = decrease, n = no change
Key to Acronyms: APV = amprenavir; ART = antiretroviral therapy; ATV = atazanavir; ATV/c = atazanavir/cobicistat; AUC = area under the
curve; BID = twice daily; Cmax = maximum plasma concentration; Cmin = minimum plasma concentration; CYP = cytochrome P; DLV =
delavirdine; DRV = darunavir; DRV/c = darunavir/cobicistat; DRV/r = darunavir/ritonavir; EFV = efavirenz; ETR = etravirine; FDA = Food
and Drug Administration; FPV = fosamprenavir; IDV = indinavir; LPV = lopinavir; LPV/r = lopinavir/ritonavir; NFV = nelfinavir; NVP =
nevirapine; PK = pharmacokinetic; RPV = rilpivirine; RTV = ritonavir; SQV = saquinavir; SQV/r = saquinavir/ritonavir; TID = three times a
day; TPV = tipranavir

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