Appendix A, Table 3. Characteristics of Nucleoside Reverse Transcriptase Inhibitors

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This 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. Oral zidovudine (ZDV) is no longer recommended by the Panel on Antiretroviral Guidelines for Adults and Adolescents due to the potential for serious adverse effects. 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
FormulationsDosing RecommendationsaElimination/ Metabolic PathwaySerum/ Intracellular Half-LivesAdverse Eventsb

Abacavir
(ABC)
Ziagen

Note: Generic products are available.

Ziagen

  • 20-mg/mL oral solution

Generic

  • 300-mg tablet
  • Also available as FDC with 3TC

FDC Tablets That Contain ABCc

  • ABC/3TC

STRs That Contain ABCd

  • Triumeq (DTG/ABC/3TC)

Tablet

  • ABC 600 mg PO once daily, or 
  • ABC 300 mg PO twice daily

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

ABC is contraindicated in people who test positive for HLA-B*5701 due to an increased risk of HSRs. HLA screening should be done before initiating ABC.

For people with a history of HSRs, rechallenge is contraindicated.

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).

Evidence increasingly supports a relationship between ABC and major CV events.

Emtricitabine
(FTC)
Emtriva

Note: Generic products are available.

Emtriva

  • 200-mg hard gelatin capsule
  • 10-mg/mL oral solution

Generic

  • 200-mg capsule
  • Also available as FDC with TDF

FDC Tablets That Contain FTCc

  • Descovy (TAF/FTC)
  • Truvada (TDF/FTC)

STRs That Contain FTCd

  • Biktarvy (BIC/TAF/FTC)
  • Complera (or generic) (RPV/TDF/FTC)
  • EFV/TDF/FTC (generic)
  • Genvoya (EVG/c/TAF/FTC)
  • Odefsey (RPV/TAF/FTC)
  • Stribild (EVG/c/TDF/FTC)
  • Symtuza (DRV/c/TAF/FTC)

 

Capsule

  • FTC 200 mg PO once daily

Oral Solution

  • FTC 240 mg (24 mL) PO once daily

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.

Islatravir
(ISL)
ISL is available only as a component of the STR Idvynso (DOR/ISL).d
  • One tablet PO once daily

See Appendix A, Table 1 for dosing information.

ADA-mediated metabolism (approximately 53%)21 hours/ 186 hoursDiarrhea

Lamivudine
(3TC)
Epivir

Note: Generic products are available.

Epivir

  • 150-mg and 300-mg tablets
  • 10-mg/mL oral solution

Generic

  • 100-mg, 150-mg, and 300-mg tablets
  • 10-mg/mL oral solution
  • Also available as FDC with ABC

FDC Tablets That Contain 3TCc

  • ABC/3TC (generic)
  • Cimduo (TDF/3TC)

STRs That Contain 3TCd

  • Delstrigo (DOR/TDF/3TC)
  • Dovato (DTG/3TC)
  • EFV/TDF/3TC (generic)
  • Triumeq (DTG/ABC/3TC)

Tablet

  • 3TC 300 mg PO once daily, or
  • 3TC 150 mg PO twice daily

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
(TAF)
Vemlidy

Note: Vemlidy is available as a 25-mg tablet for the treatment of HBV.

FDC Tablets That Contain TAFc

  • Descovy (TAF/FTC)

STRs That Contain TAFd

  • Biktarvy (BIC/TAF/FTC)
  • Genvoya (EVG/c/TAF/FTC)
  • Odefsey (RPV/TAF/FTC)
  • Symtuza (DRV/c/TAF/FTC)
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
(TDF)
Viread

Note: Generic products are available.

Viread

  • 150-mg, 200-mg, 250-mg, and 300‑mg tablets
  • 40-mg/g oral powder

Generic

  • 300-mg tablet
  • Also available as FDC with FTC

FDC Tablets That Contain TDFc

  • Cimduo (TDF/3TC)
  • Truvada (TDF/FTC) 

STRs That Contain TDFd

  • Complera (or generic) (RPV/TDF/FTC)
  • Delstrigo (DOR/TDF/3TC)
  • EFV/TDF/FTC (generic)
  • EFV/TDF/3TC (generic)
  • Stribild (EVG/c/TDF/FTC)

Tablet

  • TDF 300 mg PO once daily

Oral Powder

  • 7.5 level scoops of oral powder PO once daily (dosing scoop dispensed with each bottle; one level scoop contains 1 g of oral powder).

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 When no food restriction is listed, the antiretroviral drug can be taken with or without food.

b Also see Table 20.

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; ADA = adenosine deaminase; BIC = bictegravir; BMD = bone mineral density; CV = cardiovascular; DOR = doravirine; DRV/c = darunavir/cobicistat; DTG = dolutegravir; EFV = efavirenz; EVG/c = elvitegravir/cobicistat; FDC = fixed-dose combination; FTC = emtricitabine; HB = hepatitis B virus; HLA = human leukocyte antigen; HSR = hypersensitivity reaction; ISL = islatravir; PO = orally; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

 

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