Guidelines
HIV ART Quick Guide

HIV ART Quick Guide

First Line

3 Drug Regimen

  • NRTI + NRTI + INSTI

TAF + FTC + BIC

  • Co-formulated in a single pill regimen:
    • Biktarvy

TAF + FTC + DTG

  • Co-formulated in a 2 pill regimen:
    • Descovy (TAF+FTC) & Tivicay (DTG)

TDF + FTC + DTG

  • Co-formulated in a 2 pill regimen:
    • Truvada (TDF+FTC) & Tivicay (DTG)

NRTI (Nucleoside Reverse Transcriptase Inhibitor)

+ Overall well tolerated drugs

  • Very similar in structure and are considered interchangeable. They are not used together.
  • Choose ONE of them to combine with a separate NRTI. Typically:
    • [Emtricitabine with Tenofovir]
    • [Lamivudine with Abacavir]
  • - Emtricitabine in rare circumstances can cause hyperpigmentation

  • Typically combined with FTC. 
  • TDF is a prodrug of TAF. 
  • Overall TAF used more frequently as it is less likely to cause renal & bone toxicity compared to TDF. 
  • Circumstances where TDF preferred: when also using rifampin (TAF interacts with rifamycins) & PreP as TDF is the only formulation that’s FDA approved for PrEP   
  • + Active against HBV
  • - Renal toxicity (Avoid TDF if GFR <50, TAF if GFR <30) 
  • - Decreased bone density 
  • - Possible weight gain with TAF

  • Typically combined with 3TC
  • + Not nephrotoxic
  • - Contraindicated in patients with HLA-B*5701 allele due to hypersensitivity reaction (must have negative result before starting)
  • - May increase risk of CVD events. Avoid in patients with CA

INSTI (Integrase Strand Transfer Inhibitors)

  • + High barrier to resistance
  • - Interact with rifampin
  • - Decrease in drug levels when taken with multivalent cations Ca2+, Mg2+, Fe (tell patients to avoid antacids!)

  •  BIKTARVY (with TAF/FTC) 
  • + Available in single tablet regimen 
  • - Emerging data on weight gain 
  • - Not much data/experience of its use in pregnancy

  • TRIUMEQ (with ABC/3TC) 
  • JULUCA (with RPV) 
  • DOVATO (with 3TC) 
  • +Higher barrier to resistance than EVG or RAL 
  • +If using rifamycins, preferred over BIC
  • - Emerging data on weight gain 
  • - Interacts with metformin- can’t exceed 1g metformin per day 
  • No co-formulations with TAF/TDF   

NOTE

Use at conception & in very early pregnancy has been associated with a slightly higher prevalence of neural tube defects. However, the overall prevalence was low & when compared to other ARTs, it was not meaningfully different (Zash et al., 2019). Dolutegravir based regimens are all considered first line in pregnancy

  • GENVOYA (with TAF/FTC) 
  • STRIBLID (with TDF/FTC) 
  • +Available in single tablet regimen with TAF/FTC 
  • - Low barrier to resistance (compared to BIC or DTG) 
  • - Needs boosting with Cobicistat (c) which increases drug interactions

  • + More data on its safety in pregnancy
  • - Low barrier to resistance (compared to BIC or DTG)
  • Virologic failure may lead to two-class resistance (INSTI plus NRTI)
  • - No co-formulations. Need to use BID dosing in pregnancy
  • - Some reports of rhabdomyolysis

+ Comes as a long acting injectable with rilpivirine

PI (Protease Inhibitors)

  • + High barrier to resistance 
  • - Side effects: metabolic syndrome (DM, HLD, lipodystrophy) 
  • - Interact with many medications. Avoid co-administration of rifampin. Can co-administer with rifabutin

  • SYMTUZA (with TAF/FTC/cobcistat) 
  • + Best tolerated PI 
  • - Needs boosting with Ritonavir(r) or Cobicistat (c) 
  • - Avoid in severe liver disease 
  • - Can increase risk of CVD

  • + Less metabolic syndrome effects
  • - Needs boosting with Ritonavir(r) or Cobicistat(c)
  • - Needs gastric acid and food for optimal absorption. Can’t use PPI >20 mg omeprazole with it
  • - Increased risk of kidney stones and AKI
  • - Can cause indirect hyperbilirubinemia
  • - Avoid in severe liver disease

NNRTI (Non-Nucleoside Reverse Transcriptase Inhibitors)

  • - Low barrier to resistance (especially 1st generation: EFV, NVP) 
  • - Not active against HIV-2

  • ATRIPLA (with TDF/FTC)
  • + Single pill coformulation with TDF/FTC
  • - Neuropsychiatric side effects (vivid dreams + may increase suicide risk + “hungover feeling”)
  • - Increase LFTs with risk of fulminant hepatitis (Child Pugh B and C)
  • - CYP450 inducer – > decreases methadone levels (may precipitate opioid withdrawal when initiated)
  • - Prolongs QT

  • ODEFSEY (with TAF/FTC) 
  • COMPLERA (with TDF/FTC) 
  • JULUCA (with DTG) 
  • + Less metabolic syndrome effects
  • - Needs food (400 calorie meal) for optimal absorption. 
  • - Needs gastric acid for optimal absorption. Caution with H2 blockers, avoid PPIs. 
  • - Not as good at a higher viral load. Use in PLWH with CD4 T-cell counts >200 cells/μL and HIV RNA <100,000 copies/mL 
  • - Neuropsychiatric side effects (vivid dreams + may increase suicide risk) 
  • - Prolongs QT

  • DELSTRIGO (with TDF/FTC)
  • + BEST IN CLASS 
  • + Unique resistance pathway from other NNRTIs

  • + One of the common meds used in the setting of drug resistance 
  • - Rash (can be mild, but SJS also reported) 
  • - Drug interactions

Additional Information

  • Resistance pattern
  • HLA-B*5701 allele status (for Abacavir)
  • Concomitant HBV infection (if HbSag +, include TAF/TDF in regimen)
  • Concomitant treatment for TB/LTBI (check drug-drug interactions especially when using rifampin)
  • Cardiovascular risk factors
  • Comorbid conditions (e.g. kidney disease, liver disease, osteoporosis, psychiatric illness, concern for weight gain, cancer/autoimmune disease)
  • Interaction with other medications (see table in DHHS guideline or Liverpool drug interaction website included below)
  • Pill burden (single tablet regimen vs. other regimens vs. long acting injectable)
  • Woman of child bearing age/ pregnancy

Paul Sax M.D. Selecting antiretroviral regimens for the treatment-naïve HIV-infected patient. Post TW, ed.  UpToDate. Waltham, MA: UpToDate Inc. hmps://www.uptodate.com (Accessed on Aug, 2021) 

Courtney Fletcher, PharmD. Overview of antiretroviral agents used to treat HIV. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. hmps://www.uptodate.com (Accessed on Aug 2021) 

John E. Bennett, Raphael Dolin, Martin J. Blaser. Mandell, Douglas, and Bennett's Principles and Practice of Infectious Diseases. Philadelphia, PA :Elsevier/Saunders, 2015. 

Spec, Andrej, et al. Comprehensive Review of Infectious Diseases. Elsevier, 2020

Created by Dr. Hawra Al Lawa 

Reviewed by Dr. Rajesh Gandhi and Dr. Robert Goldstein (MGH ID)