Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV
The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.
Drug-Drug Interactions
Interactions between Integrase Inhibitors and Non-Nucleoside Reverse Transcriptase Inhibitors or Protease Inhibitors
Last Updated: October 25, 2018; Last Reviewed: October 25, 2018
Table 22b. Interactions between Integrase Strand Transfer Inhibitors and Non-Nucleoside Reverse Transcriptase Inhibitors or Protease Inhibitors
Recommendations for managing a particular drug interaction may differ depending on whether a new ARV is being initiated in a patient on a stable concomitant medication, or if a new concomitant medication is being initiated in a patient on a stable ARV regimen. The magnitude and significance of drug interactions are difficult to predict when several drugs with competing metabolic pathways are prescribed concomitantly.
ARV Drugs by Drug Class |
INSTIs | |||||
---|---|---|---|---|---|---|
BIC | DTG | EVG/c | RAL | |||
NNRTIs | ||||||
DOR |
PK Data |
↔ DOR, BIC expected | ↔ DOR
DTG AUC ↑ 36% and Cmin ↑ 27% |
↑ DOR expected
↔ EVG |
↔ DOR, RAL expected | |
Dose |
Standard doses | Standard doses | Standard doses | Standard doses | ||
EFV |
PK Data |
↓ BIC expected | With DTG 50 mg Once Daily:
|
↑ or ↓ EVG, COBI, EFV possible | With RAL 400 mg BID:
|
|
Dose |
Do not coadminister. | In Patients Without INSTI Resistance:
|
Do not coadminister. | Standard doses | ||
ETR | PK Data | ↓ BIC expected | ETR 200 mg BID plus DTG 50 mg Once Daily:
|
↑ or ↓ EVG, COBI, ETR possible | ETR 200 mg BID plus RAL 400 mg BID:
|
|
Dose | Do not coadminister. | Do not coadminister ETR and DTG without concurrently administering ATV/r, DRV/r, or LPV/r.
In Patients Without INSTI Resistance:
|
Do not coadminister. | RAL 400 mg BID
Coadministration with RAL 1200 mg once daily is not recommended. |
||
NVP | PK Data |
↓ BIC expected | With DTG 50 mg Once Daily:
|
↑ or ↓ EVG, COBI, NVP possible | No data | |
Dose |
Do not coadminister. | Standard doses | Do not coadminister. | Standard doses | ||
RPV | PK Data |
No data | With DTG 50 mg Once Daily:
|
↑ or ↓ EVG, COBI, RPV possible | ↔ RPV RAL Cmin ↑ 27% | |
Dose |
Standard doses | Standard doses | Do not coadminister. | Standard doses | ||
PIs | ||||||
ATV/c | PK Data | BIC AUC ↑ 305% | No data | No data | No data | |
Dose | Do not coadminister. | Standard doses | Do not coadminister. | Standard doses | ||
ATV +/- RTV |
PK Data |
BIC AUC ↑ 310% | Unboosted ATV plus DTG 30 mg Once Daily:
|
↑ or ↓ EVG, COBI, ATV possible | With Unboosted ATV:
|
|
Dose |
Do not coadminister. | Standard doses | Do not coadminister. | Standard doses | ||
DRV/c | PK Data |
BIC AUC ↑ 74% | DRV/c plus DTG Once Daily:
|
DRV/c plus EVG/c:
|
No data | |
Dose |
Standard doses | Standard doses | Do not coadminister. | Standard doses | ||
DRV/r |
PK Data |
No data | (DRV 600 mg plus RTV 100 mg) BID with DTG 30 mg Once Daily:
|
↑ or ↓ EVG, COBI, DRV possible | With (DRV 600 mg plus RTV 100 mg) BID:
|
|
Dose |
Standard doses | Standard doses | Do not coadminister. | Standard doses | ||
LPV/r | PK Data |
No data | With (LPV 400 mg plus RTV 100 mg) BID and DTG 30 mg Once Daily:
|
↑ or ↓ EVG, COBI, LPV possible
RTV and COBI have similar effects on CYP3A. |
↓ RAL
↔ LPV/r |
|
Dose |
Consider alternative combination. | Standard doses | Do not coadminister. | Standard doses | ||
TPV/r |
PK Data |
↓ BIC possible | With (TPV 500 mg plus RTV 200 mg) BID and DTG 50 mg Once Daily:
|
↑ or ↓ EVG, COBI, TPV possible
RTV and COBI have similar effects on CYP3A. |
With (TPV 500 mg plus RTV 200 mg) BID and RAL 400 mg BID:
|
|
Dose |
Do not coadminister. | In Patients Without INSTI Resistance:
|
Do not coadminister. | RAL 400 mg BID
Coadministration with RAL 1200 mg once daily is not recommended. |
||
a Refer to DTG product labeling for details. Key to Symbols: ↑ = increase ↓ = decrease ↔ = no change Key to Acronyms: ARV = antiretroviral; ATV = atazanavir; ATV/c = atazanavir/cobicistat; ATV/r = atazanavir/ritonavir; AUC = area under the curve; BIC = bictegravir; BID = twice daily; Cmin = minimum plasma concentration; COBI = cobicistat; CYP = cytochrome P; DOR = doravirine; DRV = darunavir; DRV/c = darunavir/cobicistat; DRV/r = darunavir/ritonavir; DTG = dolutegravir; EFV = efavirenz; ETR = etravirine; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; INSTI = integrase strand transfer inhibitor; LPV = lopinavir; LPV/r = lopinavir/ritonavir; NNRTI = non-nucleoside reverse transcriptase inhibitor; NVP = nevirapine; PI = protease inhibitor; PK = pharmacokinetic; RAL = raltegravir; RPV = rilpivirine; RTV = ritonavir; TPV = tipranavir; TPV/r = tipranavir/ritonavir |
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