Antiretroviral Agents in HIV-1

Antiretroviral Agents in HIV

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Selecting a Treatment Regimen Table 4. Antiretroviral Regimens or Components That Should NOT Be Offered At Any Time (Updated October 2011) ARV Drugs or Components (in alphabetical order) ABC/3TC/ZDV (coformulated) as triple- NRTI combination regimen (BI) ABC + 3TC + ZDV + TDF as quadruple-NRTI combination (BI) ABC + ddI (BIII) ABC + TDF (BIII) d4T + 3TC (BI) recommending as initial therapy Reasons for NOT ▶ Inferior virologic efficacy ▶ Inferior virologic efficacy ▶ Insufficient data in ART-naïve patients ▶ Insufficient data in ART-naïve patients ▶ Significant toxicities including lipoatrophy; peripheral neuropathy; and hyperlactatemia, including symptomatic and life-threatening lactic acidosis, hepatic steatosis, and pancreatitis ddI + 3TC (or FTC) (BIII) ▶ Inferior virologic efficacy, least clinical trial experience ddI + TDF (BII) ▶ Increased ddI drug exposure and toxicities DLV (BII) DRV (unboosted) ENF (BIII) ETR (BIII) FPV (unboosted) (BIII) IDV (unboosted) (BIII) ▶ Inferior virologic efficacy ▶ Inconvenient (three times daily) dosing ▶ Use without RTV has not been studied ▶ No clinical trial experience in ART-naïve patients ▶ Requires twice-daily subcutaneous injections ▶ Insufficient data in ART-naïve patients ▶ Less potent than RTV-boosted FPV ▶ Virologic failure with unboosted FPV-based regimen may select mutations that confer resistance to DRV ▶ Inconvenient dosing (three times daily with meal restrictions) ▶ Fluid requirement IDV (RTV-boosted) (BIII) ▶ High incidence of nephrolithiasis NFV (BI) ▶ Inferior virologic efficacy ▶ High incidence of diarrhea RTV as sole PI (BIII) SQV (unboosted) (BI) TPV (RTV-boosted) (BI) 6 ▶ High pill burden ▶ Gastrointestinal intolerance ▶ Inferior virologic efficacy ▶ Inferior virologic efficacy ▶ High rate of early virologic failure ▶ Rapid selection of resistance mutations ▶ Potential for immunologic nonresponse/CD4 T-cell decline

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