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Updated Adult and Adolescent ARV Guidelines

The Adult and Adolescent ARV Guidelines were updated on February 12, 2013. 

Please send your comments with the subject line "Comments on Adult and Adolescent ARV Guidelines" to ContactUs@aidsinfo.nih.gov by February 26, 2013.

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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

(Last updated:2/12/2013; last reviewed:2/12/2013)

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Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors
Click here to view this table as an image 

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