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Generic Name (Abbreviation) Trade Name |
Formulations | Dosing Recommendationsa | Elimination/ Metabolic Pathway | Serum/ Intracellular Half-Lives | Adverse Eventsb |
---|---|---|---|---|---|
Abacavir (ABC) Ziagen Note: Generic tablet formulation is available. |
Ziagen:
|
Ziagen:
|
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 patients with hepatic insufficiency (see Appendix B, Table 11). |
1.5 hours/12–26 hours | Patients who test positive for HLA-B*5701 are at the highest risk of experiencing HSRs. HLA screening should be done before initiating ABC. For patients 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 (FTC) Emtriva |
Emtriva:
|
Emtriva Capsule:
|
86% of FTC dose is excreted renally See Appendix B, Table 11 for dosing recommendations in patients with renal insufficiency. |
10 hours/>20 hours | Minimal toxicity Hyperpigmentation/skin discoloration Severe acute exacerbation of hepatitis may occur in patients with HBV/HIV coinfection who discontinue FTC. |
Lamivudine (3TC) Epivir Note: Generic products are available. |
Epivir:
|
Epivir:
|
70% of 3TC dose is excreted renally See Appendix B, Table 11 for dose recommendations in patients with renal insufficiency. |
5–7 hours/18–22 hours | Minimal toxicity Severe acute exacerbation of hepatitis may occur in patients with HBV/HIV coinfection who discontinue 3TC. |
Tenofovir Alafenamide (TAF) Vemlidy Note: Vemlidy is available as a 25-mg tablet for the treatment of HBV. |
FDC Tablets that Contain TAF:c
|
See Appendix B, Tables 1 and 2 for dosing information for FDC tablets that contain TAF. | Metabolized by cathepsin A See Appendix B, Table 11 for dosing recommendations in patients with renal insufficiency. |
0.5 hours/150–180 hours |
Renal insufficiency, Fanconi syndrome, and proximal renal tubulopathy are less likely to occur with TAF than with TDF. Greater weight increase has been reported with TAF than with TDF. |
Tenofovir Disoproxil Fumarate (TDF) Viread Note: Generic product is available. |
Viread:
|
Viread:
See Appendix B, Tables 1 and 2 for dosing information for FDC tablets that contain TDF. |
Renal excretion is the primary route of elimination. See Appendix B, Table 11 for dose recommendations in patients with renal insufficiency. |
17 hours/>60 hours | Renal insufficiency, Fanconi syndrome, proximal renal tubulopathy Osteomalacia, decrease in BMD Severe acute exacerbation of hepatitis may occur in patients with HBV/HIV coinfection who discontinue TDF. Asthenia, headache, diarrhea, nausea, vomiting, flatulence |
a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the ARV drug can be taken with or without food. b Also see Table 17. c See Appendix B, Table 2 for information about these formulations. d See Appendix B, 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; EVG/c = elvitegravir/cobicistat; EFV = efavirenz; 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 |