The following table includes dose recommendations for U.S. Food and Drug Administration (FDA)–approved nucleoside reverse transcriptase inhibitor products for adults with HIV. For information regarding the use of these medications in adolescents with HIV, including weight limitations and additional dosage forms, please consult FDA product labeling or Appendix A in the Pediatric Antiretroviral Guidelines. The older nucleoside reverse transcriptase inhibitors didanosine (ddI) and stavudine (d4T) have been discontinued in the United States. Zidovudine (ZDV) is no longer used commonly in clinical practice. Therefore, these antiretrovirals have been removed from this table. Please refer to the FDA product label for ZDV for information regarding this drug.
| Generic Name (Abbreviation) Trade Name | Formulations | Dosing Recommendationsa | Elimination/ Metabolic Pathway | Serum/ Intracellular Half-Lives | Adverse Eventsb |
|---|---|---|---|---|---|
Abacavir Note: Generic products are available. | Ziagen
Generic
FDC Tablets That Contain ABCc
STRs That Contain ABCd
|
See Appendix A, Tables 1 and 2 for dosing information for FDC tablets that contain ABC. | Metabolized by alcohol dehydrogenase and glucuronyl transferase 82% of ABC dose is excreted in the urine as metabolites of ABC. Dose adjustment is recommended in people with hepatic insufficiency (see Appendix B).
| 1.5 hours/12–26 hours | People who test positive for HLA-B*5701 are at the highest risk of experiencing HSRs. HLA screening should be done before initiating ABC. For people with a history of HSRs, rechallenge is not recommended. Symptoms of HSRs may include fever, rash, nausea, vomiting, diarrhea, abdominal pain, malaise, fatigue, or respiratory symptoms (e.g., sore throat, cough, or shortness of breath). Some cohort studies suggest an increased risk of MI with recent or current use of ABC, but this risk is not substantiated in other studies. |
Emtricitabine Note: Generic products are available. | Emtriva
Generic
FDC Tablets That Contain FTCc
STRs That Contain FTCd
|
Capsule
Oral Solution
See Appendix A, Tables 1 and 2 for dosing information for FDC tablets that contain FTC.
| 86% of FTC dose is excreted renally. See Appendix B for dosing recommendations in people with renal insufficiency.
| 10 hours/ >20 hours | Minimal toxicity Hyperpigmentation/skin discoloration Severe acute exacerbation of hepatitis may occur in people with HBV/HIV coinfection who discontinue FTC. |
Lamivudine Note: Generic products are available. | Epivir
Generic
FDC Tablets That Contain 3TCc
STRs That Contain 3TCd
|
See Appendix A, Tables 1 and 2 for dosing information for FDC tablets that contain 3TC.
| 70% of 3TC dose is excreted renally. See Appendix B for dose recommendations in people with renal insufficiency.
| 5–7 hours/18–22 hours | Minimal toxicity Severe acute exacerbation of hepatitis may occur in people with HBV/HIV coinfection who discontinue 3TC. |
Tenofovir Alafenamide Note: Vemlidy is available as a 25-mg tablet for the treatment of HBV. | FDC Tablets That Contain TAFc
STRs That Contain TAFd
| See Appendix A, Tables 1 and 2 for dosing information for FDC tablets that contain TAF. | Metabolized by cathepsin A
See Appendix B for dosing recommendations in people with renal insufficiency.
| 0.5 hour/150–180 hours | Renal insufficiency, Fanconi syndrome, and proximal renal tubulopathy are less likely to occur with TAF than with TDF. Osteomalacia and decreases in BMD are less likely to occur with TAF than with TDF. Severe acute exacerbation of hepatitis may occur in people with HBV/HIV coinfection who discontinue TAF. Diarrhea, nausea, headache Greater weight increase has been reported with TAF than with TDF. |
Tenofovir Disoproxil Fumarate Note: Generic products are available. | Viread
Generic
FDC Tablets that Contain TDFc
STRs that Contain TDFd
|
Mix oral powder with 2–4 ounces of a soft food that does not require chewing (e.g., applesauce, yogurt). Do not mix oral powder with liquid. See Appendix A, Tables 1 and 2 for dosing information for FDC tablets that contain TDF.
| Renal excretion is the primary route of elimination. See Appendix B for dose recommendations in people with renal insufficiency.
| 17 hours/ >60 hours | Renal insufficiency, Fanconi syndrome, proximal renal tubulopathy Osteomalacia, decrease in BMD Asthenia, headache, diarrhea, nausea, vomiting, flatulence Severe acute exacerbation of hepatitis may occur in people with HBV/HIV coinfection who discontinue TDF. |
a For dose adjustments in people with renal or hepatic insufficiency, see Appendix B. When no food restriction is listed, the antiretroviral drug can be taken with or without food. b Also see Table 21. c See Appendix A, Table 2 for information about these formulations. d See Appendix A, Table 1 for information about these formulations. Key: 3TC = lamivudine; ABC = abacavir; BIC = bictegravir; BMD = bone mineral density; DOR = doravirine; DRV/c = darunavir/cobicistat; DTG = dolutegravir; EFV = efavirenz; EVG/c = elvitegravir/cobicistat; FDC = fixed-dose combination; FTC = emtricitabine; HBV = hepatitis B virus; HLA = human leukocyte antigen; HSR = hypersensitivity reaction; MI = myocardial infarction; PO = orally; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate | |||||