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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: May 1, 2014; last reviewed: May 1, 2014)

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Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
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.
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. Rechallenge 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
Note: Generic available
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

Note: Generic available; dose same as 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 +/- 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-coinfected 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 

Note: 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-coinfected patients who discontinue 3TC.
Combivir
3TC with ZDV


Note: 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
Note: Generic available
Trizivir:
  • 3TC 150 mg + ZDV 300 mg + ABC 300 mg tablet
Trizivir:
  • 1 tablet BID
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 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 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 – 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 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
  • Take 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

Note: Generic available

Also available as a component of fixed-dose combinations.
Retrovir:
  • 100 mg capsule
  • 300 mg tablet
  • 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 

Note: Generic available
Combivir:
  • ZDV 300 mg + 3TC 150 mg tablet
Combivir:
  • 1 tablet BID
  • Take without regard to meals.
Trizivir
ZDV with 3TC + ABC

Note: Generic available
Trizivir:
  • ZDV 300 mg + 3TC 150 mg + 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; 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 

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