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Call for Scientific/Clinical Member and Community Member Nominations
The Department of Health and Human Services (HHS) Panel on Antiretroviral Guidelines for Adults and Adolescents is accepting nominations for new scientific/clinical members with expertise in HIV medicine, as well as nominations for a community representative. Nominations should be submitted to Alice Pau, Pharm.D., electronically (apau@niaid.nih.gov) by no later than January 10, 2020.
For more information on the scientific/clinical member nomination requirements, please read this news announcement.
For more information on the community member nomination requirements, please read this news announcement.
Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV
- Home
- Guidelines
- Adult and Adolescent ARV
- Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.
- Table of Contents
- What's New in the Guidelines?
- Panel Roster
- Financial Disclosure
- Introduction
- Baseline Evaluation
- Laboratory Testing
- Treatment Goals
- Initiation of Antiretroviral Therapy
- What to Start
- What Not to Use
- Management of the Treatment-Experienced Patient
- Special Patient Populations
- Considerations for Antiretroviral Use in Patients with Coinfections
- Limitations to Treatment Safety and Efficacy
- Drug-Drug Interactions
- Conclusion
- Appendix A: Key to Acronyms
- Appendix B: Drug Characteristics Tables
Download Guidelines
- Section Only PDF (236 KB)
- Full Guideline PDF (4.7 MB)
- Recommendations Only PDF (88.9 KB)
- Tables Only PDF (563 KB)
Appendix B: Drug Characteristics Tables
Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Last Updated: July 10, 2019; Last Reviewed: July 10, 2019
|
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
Renal excretion of metabolites: 82% Dose adjustment is recommended in patients with hepatic insufficiency (see Appendix B, Table 10). |
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, re-challenge 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. |
| Didanosine (ddI) Videx Videx EC Note: Generic delayed-release capsules are available; the dose for these is the same as for Videx EC. |
Videx EC:
|
Body Weight ≥60 kg Without TDF:
Without TDF:
Oral solution should be administered twice daily, with the total daily dose divided into two doses. |
Renal excretion: 50%
Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 10). |
1.5 hours/>20 hours | Pancreatitis
Peripheral neuropathy Retinal changes, optic neuritis Lactic acidosis with hepatic steatosis with or without pancreatitis (this is a rare, but potentially life-threatening, toxicity) Nausea, vomiting Potential association with noncirrhotic portal hypertension; in some cases, patients presented with esophageal varices One cohort study suggested an increased risk of MI with recent or current use of ddI, but this risk is not substantiated in other studies. Insulin resistance/diabetes mellitus |
| Emtricitabine (FTC) Emtriva |
Emtriva:
|
Emtriva Capsule:
|
Renal excretion: 86% Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 10). |
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 is available. |
Epivir:
|
Epivir:
|
Renal excretion: 70%
Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 10). |
5–7 hours/18–22 hours | Minimal toxicity
Severe acute exacerbation of hepatitis may occur in patients with HBV/HIV coinfection who discontinue 3TC. |
| Stavudine (d4T) Zerit Note: Generic is available. |
Zerit:
|
Body Weight ≥60 kg:
|
Renal excretion: 50%
Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 10). |
1 hour/7.5 hours | Peripheral neuropathy
Lipoatrophy Pancreatitis Lactic acidosis/severe hepatomegaly with hepatic steatosis (this is a rare, but potentially life-threatening, toxicity) Hyperlipidemia Insulin resistance/diabetes mellitus Rapidly progressive ascending neuromuscular weakness (rare) |
| Tenofovir Alafenamide (TAF) Vemlidy Note: Vemlidy is available as a 25-mg tablet for the treatment of HBV. |
STRs that Contain TAF:d
|
See Appendix B, Tables 1 and 2 for dosing information for FDC tablets that contain TAF. | Metabolized by cathepsin A.
Not recommended in patients with CrCl <30 mL/min. |
0.5 hours/150–180 hours | Renal insufficiency, Fanconi syndrome, and proximal renal tubulopathy are less likely to occur with TAF than with TDF.
Osteomalacia and decrease in bone mineral density are less likely to occur with TAF than with TDF. Severe acute exacerbation of hepatitis may occur in patients with HBV/HIV coinfection who discontinue TAF. Diarrhea, nausea, headache |
| Tenofovir Disoproxil Fumarate (TDF) Viread Note: Generic 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.
Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 10). |
17 hours/>60 hours | Renal insufficiency, Fanconi syndrome, proximal renal tubulopathy
Osteomalacia, decrease in bone mineral density Severe acute exacerbation of hepatitis may occur in patients with HBV/HIV coinfection who discontinue TDF. Asthenia, headache, diarrhea, nausea, vomiting, flatulence |
| Zidovudine (ZDV) Retrovir Note: Generic is available. |
Retrovir:
|
Retrovir:
|
Metabolized to GAZT
Renal excretion of GAZT Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 10). |
1.1 hours/7 hours | Bone Marrow Suppression: Macrocytic anemia or neutropenia
Nausea, vomiting, headache, insomnia, asthenia Nail pigmentation Lactic acidosis/severe hepatomegaly with hepatic steatosis (this is a rare, but potentially life-threatening, toxicity) Hyperlipidemia Insulin resistance/diabetes mellitus Lipoatrophy Myopathy |
| a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 10. 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; c = cobicistat; CrCl = creatinine clearance; d4T = stavudine; ddI = didanosine; DOR = doravirine; DRV = darunavir; DTG = dolutegravir; EC = enteric coated; EFV = efavirenz; EVG = elvitegravir; FDC = fixed-dose combination; FTC = emtricitabine; GAZT = azidothymidine glucuronide; HBV = hepatitis B virus; HLA = human leukocyte antigen; HSR = hypersensitivity reaction; IV = intravenous; MI = myocardial infarction; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; WHO = World Health Organization; ZDV = zidovudine |
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Download Guidelines
- Section Only PDF (236 KB)
- Full Guideline PDF (4.7 MB)
- Recommendations Only PDF (88.9 KB)
- Tables Only PDF (563 KB)
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