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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:2/12/2013; last reviewed:2/12/2013)

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Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors
Generic Name (Abbreviation)/ Trade Name  Formulations Dosing Recommendations
(For dosage adjustment in renal or hepatic insufficiency, see
Appendix B, Table 7
.)
Elimination  Serum/ Intracellular Half-Lives  Adverse Events
(Also see Table 13.)
Abacavir
(ABC)/
Ziagen

Generic available in tablet formulation
Also available as component of fixed-dose combinations:
Ziagen
  • 300 mg tablets
  • 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 recommended in patients with hepatic insufficiency (See Appendix B, Table 7) 1.5 hrs /
12–26 hrs

  • HSRs: Patients who test positive for HLA-B*5701 are at highest risk. HLA screening should be done before initiation of ABC. Re-challenge is not recommended.
  • Symptoms of HSR may include fever, rash, nausea, vomiting, diarrhea, abdominal pain, malaise, or 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
with ZDV+3TC

Trizivir
(ABC 300 mg + ZDV 300 mg + 3TC 150 mg) tablet

Trizivir
1 tablet BID

Epzicom
ABC with 3TC

Epzicom
(ABC 600 mg + 3TC 300 mg) tablet
Epzicom
1 tablet once daily
Didanosine
(ddI)/
Videx EC
Generic available; dose same as Videx EC
Videx EC
125, 200, 250, and 400 mg capsules
Videx
10 mg/mL oral solution
Body weight ≥60kg:
400 mg once daily
With TDF: 250 mg once daily Body weight <60kg:
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 +/- 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:
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 co infected patients who discontinue FTC.
Atripla
FTC
with EFV + TDF
Atripla
(FTC 200 mg + EFV 600 mg + TDF 300 mg) tablet
Atripla
1 tablet at or before bedtime
Take on an empty stomach to reduce side effects.
Complera
FTC
with RPV+TDF
Complera
(FTC 200 mg +
RPV 25 mg +
TDF 300 mg) tablet
Complera
1 tablet once daily with a meal
Stribild
FTC
with EVG + COBI + TDF
Stribild
(FTC 200 mg +
EVG 150 mg +
COBI 150 mg +
TDF 300 mg)
tablet
Stribild
1 tablet once daily with food
Truvada
FTC with TDF
Truvada
(FTC 200 mg + TDF 300 mg) tablet
Truvada
1 tablet once daily
Lamivudine
(3TC)/
Epivir
Generic available in tablet formulation Also available as a component of fixed-dose combinations:
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 co infected patients who discontinue 3TC.
Combivir
3TC with ZDV
Generic available
Combivir
(3TC 150 mg + ZDV 300 mg) tablet
Combivir
1 tablet BID
Epzicom
3TC with ABC
Epzicom
(3TC 300 mg + ABC 600 mg) tablet
Epzicom
1 tablet once daily
Trizivir
3TC with ZDV+ABC
Trizivir
(3TC 150 mg + ZDV 300 mg + ABC 300 mg) tablet
Trizivir
1 tablet BID
Stavudine
(d4T)/
Zerit
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 hours/
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 Disoproxil Fumarate (TDF)/
Viread
Also available as a component of fixed-dose combinations:
Viread
  • 150, 200, 250, 300 mg tablets
  • 40 mg/g oral powder
Viread
300 mg once daily or
7.5 scoops once daily
Take without regard to meals

Mix oral powder with 2–4 ounces of soft food that does not require chewing (e.g., applesauce, yogurt). DO NOT MIX ORAL POWDER WITH LIQUID.
Renal excretion Dosage adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 7). 17 hours/
>60 hours
  • Renal insufficiency, Fanconi syndrome, proximal tubulopathy
  • Osteomalacia, decrease in bone mineral density
  • Potential decrease in bone mineral density
  • Severe acute exacerbation of hepatitis may occur in HBV-co-infected patients who discontinue TDF.
  • Asthenia, headache, diarrhea, nausea, vomiting, and flatulence
Atripla
TDF with EFV+FTC
Atripla
(TDF 300 mg +
EFV 600 mg + FTC 200 mg) tablet
Atripla
1 tablet at or before bedtime
Take on an empty stomach to reduce side effects
Complera
TDF with RPV+FTC
Complera
(TDF 300 mg + RPV 25 mg +
FTC 200 mg) tablet
Complera
1 tablet once daily
Take with a meal
Stribild
TDF with EVG+COBI+
FTC
Stribild
(TDF 300 mg +
EVG 150 mg +
COBI 150 mg +
FTC 200 mg)
tablet
Stribild
1 tablet once daily with food
Truvada
TDF with FTC
Truvada
(TDF 300 mg + FTC 200 mg) tablet
Truvada
1 tablet once daily
Take without regard to meals
Zidovudine
(ZDV)/
Retrovir
Generic available Also available as a component of fixed-dose combinations
Retrovir
  • 100 mg capsule
  • 300 mg tablet (generic only)
  • 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 with 3TC
Generic available
Combivir
(ZDV 300 mg +
3TC 150 mg) tablet
Combivir
1 tablet BID
Trizivir
ZDV with 3TC+ABC
Trizivir
(ZDV 300 mg + 3TC 150 mg + ABC 300 mg) tablet
Trizivir
1 tablet BID

Key to Abbreviations
: 3TC = lamivudine, ABC = abacavir, BID = twice daily, COBI = cobicistat, d4T = stavudine, ddI = didanosine, 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, TDF = tenofovir disoproxil fumarate, TID = three times a day, WHO = World Health Organization, ZDV = zidovudine