January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 39 

Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Page 1 of 2 (Updated January 10, 2011) 

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

Also available 

as:

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

• Hypersensitivity reactions (HSR): 

Patients positive for HLA-B*5701 are 

at highest risk. HLA screening should 

be done prior to 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 myocardial infarction (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

Trizivir

1 tablet BID

Epzicom

ABC with 3TC

Epzicom

ABC 600 mg + 

3TC 300 mg

Epzicom

1 tablet once daily

Didanosine

(ddI)/

Videx EC

(generic 

available; dose 

same as Videx 

EC)

Videx EC

125-, 200-, 250-, 

400-mg capsules

Buffered tablets 

(non-EC) no 

longer available

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

*Preferred dosing with oral 

solution is BID (total daily 

dose divided into 2 doses)

Renal excretion 50%

Dosage adjustment in 

renal insufficiency 

recommended (See 

Appendix B, Table 7.)

1.5 hrs/

 >20 hrs

• Pancreatitis

• Peripheral neuropathy

• Retinal changes, optic neuritis

• Lactic acidosis with hepatic steatosis 

+/- pancreatitis (rare but potentially 

life-threatening toxicity)

• Nausea, vomiting

• Potential association with noncirrhotic 

portal hypertension, some cases 

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:

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

renal insufficiency 

recommended (See 

Appendix B, Table 7.)

10 hrs/

 >20 hrs

• 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

Atripla

1 tablet at or before bedtime

Take on an empty stomach to 

reduce side effects

Truvada

FTC with TDF

Truvada

FTC 200 mg + 

TDF 300 mg

Truvada

1 tablet once daily
January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 40 

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)

Lamivudine

(3TC)/

Epivir

Also available 

as:

Epivir

• 150-, 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 

renal insufficiency 

recommended (See 

Appendix B, Table 7.)

5–7 hrs/

 18–22 hrs

• Minimal toxicity

• Severe acute exacerbation of hepatitis 

may occur in HBV-coinfected patients 

who discontinue 3TC.

Combivir

3TC with ZDV

Combivir

3TC 150 mg + 

ZDV 300 mg

Combivir

1 tablet BID

Epzicom

3TC with ABC

Epzicom

3TC 300 mg + 

ABC 600 mg

Epzicom

1 tablet once daily

Trizivir

3TC with 

ZDV+ABC

Trizivir

3TC 150 mg + 

ZDV 300 mg + 

ABC 300 mg

Trizivir

1 tablet BID

Stavudine

(d4T)/

Zerit

Zerit

• 15-, 20-, 30-, 

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

*WHO recommends 30 mg 

BID dosing regardless of 

body weight.

Renal excretion 50%

Dosage adjustment in 

renal insufficiency 

recommended (See 

Appendix B, Table 7.)

1 hr/

7.5 hrs

• 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:

Viread

300-mg tablet

Viread

1 tablet once daily

Take without regard to meals

Renal excretion

Dosage adjustment in 

renal insufficiency 

recommended (See

Appendix B, Table 7.)

17 hrs/

>60 hrs

• Renal insufficiency, Fanconi syndrome

• Osteomalacia

• Potential decrease in bone mineral 

density

• Severe acute exacerbation of hepatitis 

may occur in HBV-coinfected patients 

who discontinue TDF.

• Asthenia, headache, diarrhea, nausea, 

Atripla vomiting, and flatulence

TDF with 

EFV+FTC

Atripla

TDF 300 mg + 

EFV 600 mg + 

FTC 200 mg

Atripla

1 tablet at or before bedtime

Take on an empty stomach to 

reduce side effects

Truvada

TDF with FTC

Truvada

TDF 300 mg + 

FTC 200 mg

Truvada

1 tablet once daily

Take without regard to meals

Zidovudine

(ZDV)/

Retrovir 

(generic 

available; dose 

same as 

retrovir)

Also available 

as:

Retrovir

• 100-mg capsules

• 300-mg tablets

• 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

renal insufficiency 

recommended (See 

Appendix B, Table 7.)

1.1 hrs/

7 hrs

• 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

Combivir

ZDV 300 mg +

3TC 150 mg

Combivir

1 tablet BID

Trizivir

ZDV with 

3TC+ABC

Trizivir

ZDV 300 mg + 

3TC 150 mg + 

ABC 300 mg

Trizivir

1 tablet BID

Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Page 2 of 2