January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 13 

Table 8. Antiretroviral Regimens or Components That Should Not Be Offered At Any Time 

(Updated January 10, 2011)

Rationale Exception

Antiretroviral Regimens Not Recommended

Monotherapy with NRTI (AII) • Rapid development of resistance

• Inferior ARV activity when compared with 

combination of three or more ARV agents

• No exception

Dual-NRTI regimens (AI) • Rapid development of resistance

• Inferior ARV activity when compared with 

combination of three or more ARV agents

• No exception

Triple-NRTI regimens (AI) except for 

ABC/ZDV/3TC (BI)

or possibly TDF + ZDV/3TC (BII)

• High rate of early virologic nonresponse seen 

when triple-NRTI combinations, including 

ABC/TDF/3TC and TDF/ddI/3TC, were used 

as initial regimen in ART-naïve patients.

• Other triple-NRTI regimens have not been 

evaluated.

• ABC/ZDV/3TC (BI) and possibly TDF 

+ ZDV/3TC (BII) in patients in whom 

other combinations are not desirable

Antiretroviral Components Not Recommended as Part of an Antiretroviral Regimen

ATV + IDV (AIII) • Potential additive hyperbilirubinemia • No exception

ddI + d4T (AII) • High incidence of toxicities: peripheral 

neuropathy, pancreatitis, and hyperlactatemia

• Reports of serious, even fatal, cases of lactic 

acidosis with hepatic steatosis with or 

without pancreatitis in pregnant women

• When no other ARV options are 

available and potential benefits 

outweigh the risks (BIII) 

ddI + TDF (AII) • Increased ddI concentrations and serious ddIassociated toxicities

• Potential for immunologic nonresponse 

and/or CD4 cell count decline

• High rate of early virologic failure

• Rapid selection of resistance mutations at 

failure

• Clinicians caring for patients who are 

clinically stable on regimens containing 

TDF + ddI should consider altering the 

NRTIs to avoid this combination.

2-NNRTI combination (AI) • When EFV combined with NVP, higher 

incidence of clinical adverse events seen 

when compared with either EFV- or NVPbased regimen.

• Both EFV and NVP may induce metabolism 

and may lead to reductions in ETR exposure; 

thus, they should not be used in combination 

with ETR.

• No exception

EFV in first trimester of pregnancy or in 

women with significant childbearing 

potential (AIII)

• Teratogenic in nonhuman primates • When no other ARV options are 

available and potential benefits 

outweigh the risks (BIII) 

FTC + 3TC (AIII) • Similar resistance profiles

• No potential benefit

• No exception

ETR + unboosted PI (AII) • ETR may induce metabolism of these PIs; 

appropriate doses not yet established

• No exception

ETR + RTV-boosted ATV or FPV (AII) • ETR may alter the concentrations of these 

PIs; appropriate doses not yet established

• No exception

ETR + RTV-boosted TPV (AII) • ETR concentration may be significantly 

reduced by RTV-boosted TPV

• No exception

NVP in ARV-naïve women with 

CD4 count >250 cells/mm3 or men with 

CD4 count >400 cells/mm3 (BI)

• High incidence of symptomatic 

hepatotoxicity

• If no other ARV option available; if 

used, patient should be closely 

monitored

d4T + ZDV (AII) • Antagonistic effect on HIV-1 • No exception

Unboosted DRV, SQV, or TPV (AII) • Inadequate bioavailability • No exception

Acronyms:

3TC = lamivudine, ABC = abacavir, ATV = atazanavir, d4T = stavudine, ddI = didanosine, DRV = darunavir, EFV = efavirenz, ETR = etravirine,

FPV = fosamprenavir, FTC = emitricitabine, IDV = indinavir, NVP = nevirapine, RTV = ritonavir, SQV = saquinavir, TDF = tenofovir, TPV = tipranavir, ZDV =

zidovudine