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Table of Contents

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents

Appendix B: Drug Characteristics Tables

Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

(Last updated: July 14, 2016; last reviewed: July 14, 2016)
Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors 
Generic Name
(Abbreviation)
Trade Name  		Formulations Dosing Recommendationsa
 Elimination  Serum/ Intracellular Half-Lives  Adverse Eventsb
Abacavir
(ABC)
Ziagen

Note: Generic available in tablet formulation

Also available as a component of fixed-dose combinations (by trade name and abbreviation):		 Ziagen:
  • 300 mg tablet
  • 20 mg/mL oral solution
 Ziagen:
  • 300 mg BID, or
  • 600 mg once daily
  • Take without regard to meals
 Metabolized by alcohol dehydrogenase and glucuronyl transferase

Renal excretion of metabolites: 82%

Dosage adjustment for ABC is recommended in patients with hepatic insufficiency (see Appendix B, Table 7).
 1.5 hours/
12–26 hours
  • HSRs: Patients who test positive for HLA-B*5701 are at highest risk. HLA screening should be done before initiation of ABC. 
  • For patients with history of HSR, re-challenge is not recommended.
  • Symptoms of HSR may include fever, rash, nausea, vomiting, diarrhea, abdominal pain, malaise, fatigue, or respiratory symptoms such as sore throat, cough, or shortness of breath.
  • Some cohort studies suggest increased risk of MI with recent or current use of ABC, but this risk is not substantiated in other studies.
Trizivir
(ABC/ZDV/3TC)

Note: Generic available		 Trizivir:
  • (ABC 300 mg plus ZDV 300 mg plus 3TC 150 mg) tablet
 Trizivir:
  • 1 tablet BID
Epzicom
(ABC/3TC) 		Epzicom:
  • (ABC 600 mg plus 3TC 300 mg) tablet
 Epzicom:
  • 1 tablet once daily
Triumeq
(ABC/3TC/DTG)
 Triumeq:
  • (ABC 600 mg plus 3TC 300 mg plus DTG 50 mg) tablet
 Triumeq:
  • 1 tablet once daily
Didanosine
(ddI)
Videx
Videx EC

Note: Generic available; dose same as Videx or Videx EC
 Videx EC:
  • 125, 200, 250, and 400 mg capsules
Videx:
  • 10 mg/mL oral solution
 Body Weight ≥60 kg:
  • 400 mg once daily
With TDF:
  • 250 mg once daily
Body Weight <60 kg:
  • 250 mg once daily
With TDF:
  • 200 mg once daily
Take 1/2 hour before or 2 hours after a meal.

Note: Preferred dosing with oral solution is BID (total daily dose divided into 2 doses).		 Renal excretion: 50%

Dosage adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 7). 		1.5 hours/
>20 hours
  • Pancreatitis
  • Peripheral neuropathy
  • Retinal changes, optic neuritis
  • Lactic acidosis with hepatic steatosis with or without pancreatitis (rare but potentially life-threatening toxicity)
  • Nausea, vomiting
  • Potential association with non-cirrhotic portal hypertension; in some cases, patients presented with esophageal varices
  • One cohort study suggested 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

Also available as a component of fixed-dose combinations (by trade name and abbreviation):		 Emtriva:
  • 200 mg hard gelatin capsule
  • 10 mg/mL oral solution
 Emtriva
Capsule:
  • 200 mg once daily
Oral Solution:
  • 240 mg (24 mL) once daily
Take without regard to meals.		 Renal excretion: 86%

Dosage adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 7). 		10 hours/
>20 hours
  • Minimal toxicity
  • Hyperpigmentation/skin discoloration
  • Severe acute exacerbation of hepatitis may occur in HBV-coinfected patients who discontinue FTC.
Atripla
(FTC/EFV/TDF)
 Atripla:
  • (FTC 200 mg plus EFV 600 mg plus TDF 300 mg) tablet
 Atripla:
  • 1 tablet at or before bedtime
  • Take on an empty stomach to reduce side effects.
Complera
(FTC/RPV/TDF)
 Complera:
  • (FTC 200 mg plus RPV 25 mg plus TDF 300 mg) tablet
 Complera:
  • 1 tablet once daily with a meal
Descovy
(FTC/TAF)		 Descovy:
  • (FTC 200 mg plus TAF 25 mg) tablet
 Descovy:
  • 1 tablet once daily
Genvoya
(FTC/EVG/c/TAF)		 Genvoya:
  • (FTC 200 mg plus EVG 150 mg plus COBI 150 mg plus TAF 10 mg) tablet
 Genvoya:
  • 1 tablet once daily with food
Odefsey
(FTC/RPV/TAF)		 Odefsey:
  • (FTC 200 mg plus RPV 25 mg plus TAF 25 mg) tablet
 Odefsey:
  • 1 tablet once daily with a meal
Stribild
(FTC/EVG/c/TDF)		 Stribild:
  • (FTC 200 mg plus EVG 150 mg plus COBI 150 mg plus TDF 300 mg) tablet
 Stribild:
  • 1 tablet once daily with food
Truvada
(FTC/TDF)		 Truvada:
  • (FTC 200 mg plus TDF 300 mg) tablet
 Truvada:
  • 1 tablet once daily
Lamivudine
(3TC)
Epivir 

Note: Generic available

Also available as a component of fixed-dose combinations (by trade name and abbreviation):		 Epivir:
  • 150 and 300 mg tablets
  • 10 mg/mL oral solution
Epivir:
  • 150 mg BID, or 
  • 300 mg once daily
  • Take without regard to meals.
 Renal excretion: 70%

Dosage adjustment in
patients with renal insufficiency is recommended (see Appendix B, Table 7). 		5–7 hours/
18–22 hours
  • Minimal toxicity
  • Severe acute exacerbation of hepatitis may occur in HBV-coinfected patients who discontinue 3TC.
Combivir
(3TC/ZDV)

Note: Generic available 		Combivir:
  • (3TC 150 mg plus ZDV 300 mg) tablet
 Combivir:
  • 1 tablet BID
Epzicom
(3TC/ABC)		 Epzicom:
  • (3TC 300 mg plus ABC 600 mg) tablet
 Epzicom:
  • 1 tablet once daily
Trizivir
(3TC/ZDV/ABC)

Note: Generic available		 Trizivir:
  • (3TC 150 mg plus ZDV 300 mg plus ABC 300 mg) tablet
 Trizivir:
  • 1 tablet BID
Triumeq
(3TC/ABC/DTG)		 Triumeq:
  • (3TC 300 mg plus ABC 600 mg plus DTG 50 mg) tablet
 Triumeq:
  • 1 tablet once daily
Stavudine
(d4T)
Zerit

Note: Generic available 		Zerit:
  • 15, 20, 30, and 40 mg capsules
  • 1 mg/mL oral solution
 Body Weight ≥60 kg: 
  • 40 mg BID
Body Weight <60 kg: 
  • 30 mg BID
Take without regard to meals.

Note: WHO recommends 30 mg BID dosing regardless of body weight.		 Renal excretion: 50%

Dosage adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 7). 		1 hour/
7.5 hours
  • Peripheral neuropathy
  • Lipoatrophy
  • Pancreatitis
  • Lactic acidosis/severe hepatomegaly with hepatic steatosis (rare but potentially life-threatening toxicity)
  • Hyperlipidemia
  • Insulin resistance/diabetes mellitus
  • Rapidly progressive ascending neuromuscular weakness (rare)
Tenofovir Alafenamide
(TAF)

Only available as a component of fixed-dose combinations (by trade name and abbreviation): 		See fixed-dose combinations below. See fixed-dose combinations below. Metabolized by cathepsin A; P-glycoprotein substrate

Not recommended in patients with CrCl < 30 mL/min (see Appendix B, Table 7). 		0.5 hours/150–180 hours
  • Renal insufficiency, Fanconi syndrome, proximal renal tubulopathy; less likely than from TDF
  • Osteomalacia, decrease in bone mineral density; lesser effect than from TDF
  • Severe acute exacerbation of hepatitis may occur in HBV-coinfected patients who discontinue TAF.
  • Diarrhea, nausea, headache
Descovy
(TAF/FTC) 		Descovy:
  • (FTC 200 mg plus TAF 25 mg) tablet
 Descovy:
  • 1 tablet once daily
Genvoya
(TAF/EVG/c/FTC) 		Genvoya:
  • (TAF 10 mg plus EVG 150 mg plus COBI 150mg plus FTC 200 mg) tablet
 Genvoya:
  • 1 tablet once daily with food
Odefsey
(TAF/RPV/FTC) 		Odefsey:
  • (TAF 25 mg plus RPV 25 mg plus FTC 200 mg) tablet
 Odefsey:
  • 1 tablet once daily with a meal
Tenofovir Disoproxil Fumarate
(TDF)
Viread

Also available as a component of fixed-dose combinations (by trade name and abbreviation):		 Viread:
  • 150, 200, 250, and 300 mg tablets
  • 40 mg/g oral powder
 Viread:
  • 300 mg once daily or
  • 7.5 level scoops once daily (dosing scoop dispensed with each prescription; one level scoop contains 1 g of oral powder).
  • Take without regard to meals.
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.		 Renal excretion is primary route of elimination.

Dosage adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 7). 		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 HBV-coinfected patients who discontinue TDF.
  • Asthenia, headache, diarrhea, nausea, vomiting, and flatulence
Atripla
(TDF/EFV/FTC)		 Atripla:
  • (TDF 300 mg plus EFV 600 mg plus FTC 200 mg) tablet
 Atripla:
  • 1 tablet at or before bedtime
  • Take on an empty stomach to reduce side effects.
Complera
(TDF/RPV/FTC)		 Complera:
  • (TDF 300 mg plus RPV 25 mg plus FTC 200 mg) tablet
 Complera:
  • 1 tablet once daily
  • Take with a meal.
Stribild
(TDF/EVG/c/FTC)
 Stribild:
  • (TDF 300 mg plus EVG 150 mg plus COBI 150 mg plus FTC 200 mg) tablet
 Stribild:
  • 1 tablet once daily
  • Take with food.
Truvada
(TDF/FTC)		 Truvada:
  • (TDF 300 mg plus FTC 200 mg) tablet
 Truvada:
  • 1 tablet once daily
  • Take without regard to meals.
Zidovudine
(ZDV)
Retrovir

Note: Generic available

Also available as a component of fixed-dose combinations (by trade name and abbreviation):		 Retrovir:
  • 100 mg capsule
  • 300 mg tablet (only available as generic)
  • 10 mg/mL intravenous solution
  • 10 mg/mL oral solution
Retrovir:
  • 300 mg BID, or
  • 200 mg TID
  • Take without regard to meals.
 Metabolized to GAZT

Renal excretion of GAZT

Dosage adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 7). 		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 (rare but potentially life-threatening toxicity)
  • Hyperlipidemia
  • Insulin resistance/diabetes mellitus
  • Lipoatrophy
  • Myopathy
Combivir 
(ZDV/3TC)

Note: Generic available		 Combivir:
  • (ZDV 300 mg plus 3TC 150 mg) tablet
 Combivir:
  • 1 tablet BID
  • Take without regard to meals.
Trizivir
(ZDV/3TC/ABC)

Note: Generic available		 Trizivir:
  • (ZDV 300 mg plus 3TC 150 mg plus ABC 300 mg) tablet
 Trizivir:
  • 1 tablet BID
  • Take without regard to meals.
a For dosage adjustment in renal or hepatic insufficiency, see Appendix B, Table 7.
b Also see Table 14.

Key to Acronyms: 3TC = lamivudine; ABC = abacavir; BID = twice daily; c, COBI = cobicistat; CrCl = creatinine clearance; d4T = stavudine; ddI = didanosine; DTG = dolutegravir; EC = enteric coated; EFV = efavirenz; EVG = elvitegravir; FTC = emtricitabine; GAZT = azidothymidine glucuronide; HBV = hepatitis B virus; HLA = human leukocyte antigen; HSR = hypersensitivity reaction; MI = myocardial infarction; RPV = rilpivirine; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; TID = three times a day; WHO = World Health Organization; ZDV = zidovudine

                                                                                                                                                                                                                                           

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