Antiretroviral Guidelines

US DHHS Guidelines with Australian commentary

Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Last Updated: October 25, 2018;

Last Reviewed: October 25, 2018

Generic Name
(Abbreviation)
Trade Name		 Formulations Dosing Recommendationsa Elimination/ Metabolic Pathway Serum/ Intracellular Half-Lives Adverse Eventsb
Abacavir
(ABC)
Ziagen

Note: Generic tablet formulation is available.		 Ziagen:
  • 300 mg tablet
  • 20 mg/mL oral solution
 Ziagen:
  • 600 mg once daily, or
  • 300 mg BID
Take without regard to meals.		 Metabolized by alcohol dehydrogenase and glucuronyl transferase 

Renal excretion of metabolites: 82% 

Dose adjustment for ABC is recommended in patients with hepatic insufficiency (see Appendix B, Table 8).		 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 a 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.
(ABC/3TC) 
Epzicom 

Note: Generic formulation is available.		 Epzicom:
  • (ABC 600 mg plus 3TC 300 mg) tablet
 Epzicom:
  • 1 tablet once daily
(ABC/DTG/3TC) 
Triumeq		 Triumeq:
  • (ABC 600 mg plus 3TC 300 mg plus DTG 50 mg) tablet
 Triumeq:
  • 1 tablet once daily
(ABC/ZDV/3TC) 
Trizivir 

Note: Generic formulation is available.		 Trizivir:
  • (ABC 300 mg plus ZDV 300 mg plus 3TC 150 mg) tablet
 Trizivir:
  • 1 tablet BID
Didanosine 
(ddI) 
Videx 
Videx EC 

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

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

Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 8).		 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 noncirrhotic 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		 Emtriva:
  • 200 mg hard gelatin capsule
  • 10 mg/mL oral solution
 Emtriva 
Capsule:
  • FTC 200 mg once daily
Oral Solution:
  • FTC 240 mg (24 mL) once daily
Take without regard to meals.		 Renal excretion: 86%

Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 8).		 10 hours/ >20 hours
  • Minimal toxicity
  • Hyperpigmentation/skin discoloration
  • Severe acute exacerbation of hepatitis may occur in HBV coinfected patients who discontinue FTC.
(FTC/TAF) 
Descovy		 Descovy:
  • (FTC 200 mg plus TAF 25 mg) tablet
 Descovy:
  • 1 tablet once daily
(FTC/TDF) 
Truvada		 Truvada:
  • (FTC 200 mg plus TDF 300 mg) tablet
 Truvada:
  • 1 tablet once daily
(FTC/BIC/TAF) 
Biktarvy		 Biktarvy:
  • (FTC 200 mg plus BIC 50 mg plus TAF 25 mg) tablet
 Biktarvy:
  • 1 tablet once daily
(FTC/DRV/c/TAF) 
Symtuza		 Symtuza:
  • (FTC 200 mg plus DRV 800 mg plus COBI 150 mg plus TAF 10 mg) tablet
 Symtuza:
  • 1 tablet once daily with food
(FTC/EFV/TDF) 
Atripla		 Atripla:
  • (FTC 200 mg plus EFV 600 mg plus TDF 300 mg) tablet
 Atripla:
  • 1 tablet once daily on an empty stomach, preferably at bedtime
(FTC/EVG/c/TAF) 
Genvoya		 Genvoya:
  • (FTC 200 mg plus EVG 150 mg plus COBI 150 mg plus TAF 10 mg) tablet
 Genvoya:
  • 1 tablet once daily with food
(FTC/EVG/c/TDF) 
Stribild		 Stribild:
  • (FTC 200 mg plus EVG 150 mg plus COBI 150 mg plus TDF 300 mg) tablet
 Stribild:
  • 1 tablet once daily with food
(FTC/RPV/TDF) 
Complera		 Complera:
  • (FTC 200 mg plus RPV 25 mg plus TDF 300 mg) tablet
 Complera:
  • 1 tablet once daily with a meal
Lamivudine 
(3TC) 
Epivir 

Note: Generic is available.		 Epivir:
  • 150 and 300 mg tablets
  • 10 mg/mL oral solution
 Epivir:
  • 3TC 300 mg once daily, or
  • 3TC 150 mg BID
 Renal excretion: 70%

Dose adjustment in patients with renal insufficiency is recommended (see Appendix B, Table 8).		 5–7 hours/ 18–22 hours
  • Minimal toxicity
  • Severe acute exacerbation of hepatitis may occur in HBV coinfected patients who discontinue 3TC.
(3TC/ABC) 
Epzicom 

Note: Generic is available.		 Epzicom:
  • (3TC 300 mg plus ABC 600 mg) tablet
 Epzicom:
  • 1 tablet once daily
(3TC/TDF) 
Cimduo		 Cimduo:
  • (3TC 300 mg plus TDF 300 mg) tablet
 Cimduo:
  • 1 tablet once daily
(3TC/ZDV) 
Combivir 

Note: Generic is available.		 Combivir:
  • (3TC 150 mg plus ZDV 300 mg) tablet
 Combivir:
  • 1 tablet BID
(3TC/ABC/ZDV) 
Trizivir 

Note: Generic is available.		 Trizivir:
  • (3TC 150 mg plus ZDV 300 mg plus ABC 300 mg) tablet
 Trizivir:
  • 1 tablet BID
(3TC/DOR/TDF)
Delstrigo		 Delstrigo:
  • (3TC 300 mg plus DOR 100 mg plus TDF 300 mg) tablet
 Delstrigo:
  • 1 tablet once daily
(3TC/DTG/ABC) 
Triumeq		 Triumeq:
  • (3TC 300 mg plus ABC 600 mg plus DTG 50 mg) tablet
 Triumeq:
  • 1 tablet once daily
(3TC/EFV/TDF) 
Symfi		 Symfi:
  • (3TC 300 mg plus EFV 600 mg plus TDF 300 mg) tablet
 Symfi:
  • 1 tablet once daily on an empty stomach, preferably at bedtime
(3TC/EFV/TDF) 
Symfi Lo		 Symfi Lo:
  • (3TC 300 mg plus EFV 400 mg plus TDF 300 mg) tablet
 Symfi Lo:
  • 1 tablet once daily on an empty stomach, preferably at bedtime
Stavudine 
(d4T) 
Zerit 

Note: Generic is available.		 Zerit:
  • 15, 20, 30, and 40 mg capsules
  • 1 mg/mL oral solution
 Body Weight ≥60 kg:
  • d4T 40 mg BID
Body Weight <60 kg:
  • d4T 30 mg BID
Take without regard to meals. 

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

Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 8).		 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) 
Vemlidy 

Note: Available as a 25-mg tablet for the treatment of HBV.		 See FDCs for HIV treatment below. See FDCs for HIV treatment below. Metabolized by cathepsin A. 

Not recommended in patients with CrCl <30 mL/min.		 0.5 hours/ 150–180 hours
  • Renal insufficiency, Fanconi syndrome, proximal renal tubulopathy are less likely to occur with TAF than with TDF.
  • Osteomalacia, decrease in bone mineral density are less likely to occur with TAF than with TDF.
  • Severe acute exacerbation of hepatitis may occur in HBV coinfected patients who discontinue TAF.
  • Diarrhea, nausea, headache
(FTC/TAF) 
Descovy		 Descovy:
  • (FTC 200 mg plus TAF 25 mg) tablet
 Descovy:
  • 1 tablet once daily
(TAF/BIC/FTC) 
Biktarvy		 Biktarvy:
  • (TAF 25 mg plus BIC 50 mg plus FTC 200 mg) tablet
 Biktarvy:
  • 1 tablet once daily
(TAF/DRV/c/FTC) 
Symtuza		 Symtuza:
  • (TAF 10 mg plus DRV 800 mg plus COBI 150 mg plus FTC 200 mg) tablet
 Symtuza:
  • 1 tablet once daily with food
(TAF/EVG/c/FTC) 
Genvoya		 Genvoya:
  • (TAF 10 mg plus EVG 150 mg plus COBI 150 mg plus FTC 200 mg) tablet
 Genvoya:
  • 1 tablet once daily with food
(TAF/RPV/FTC) 
Odefsey		 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 

Note: Generic is available.		 Viread:
  • 150, 200, 250, and 300 mg tablets
  • 40 mg/g oral powder
Generic:
  • 300 mg tablet
 Viread:
  • TDF 300 mg once daily, or
  • 7.5 level scoops of oral powder once daily (dosing scoop dispensed with each prescription; 1 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. 

Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 8).		 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
(TDF/3TC) 
Cimduo		 Cimduo:
  • (TDF 300 mg plus 3TC 300 mg) tablet
 Cimduo:
  • 1 tablet once daily
(TDF/FTC) 
Truvada		 Truvada:
  • (TDF 300 mg plus FTC 200 mg) tablet
 Truvada:
  • 1 tablet once daily
  • Take without regard to meals.
(TDF/DOR/3TC) 
Delstrigo		 Delstrigo:
  • (TDF 300 mg plus DOR 100 mg plus 3TC 300 mg) tablet
 Delstrigo:
  • 1 tablet once daily
(TDF/EFV/FTC) 
Atripla		 Atripla:
  • (TDF 300 mg plus EFV 600 mg plus FTC 200 mg) tablet
 Atripla:
  • 1 tablet once daily on an empty stomach, preferably at bedtime
(TDF/EFV/3TC) 
Symfi		 Symfi:
  • (TDF 300 mg plus EFV 600 mg plus 3TC 300 mg) tablet
 Symfi:
  • 1 tablet once daily on an empty stomach, preferably at bedtime
(TDF/EFV/3TC) 
Symfi Lo		 Symfi Lo:
  • (TDF 300 mg plus EFV 400 mg plus 3TC 300 mg) tablet
 Symfi Lo:
  • 1 tablet once daily on an empty stomach, preferably at bedtime
(TDF/EVG/c/FTC) 
Stribild		 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.
(TDF/RPV/FTC) 
Complera		 Complera:
  • (TDF 300 mg plus RPV 25 mg plus FTC 200 mg) tablet
 Complera:
  • 1 tablet once daily
  • Take with a meal.
Zidovudine 
(ZDV) 
Retrovir 

Note: Generic is available.		 Retrovir:
  • 100 mg capsule
  • 300 mg tablet (only available as generic)
  • 10 mg/mL intravenous solution
  • 10 mg/mL oral solution
 Retrovir:
  • ZDV 300 mg BID, or
  • ZDV 200 mg TID
  • Take without regard to meals.
 Metabolized to GAZT

Renal excretion of GAZT 

Dose adjustment is recommended in patients with renal insufficiency (see Appendix B, Table 8).		 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
(ZDV/3TC) 
Combivir 

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

Note: Generic is 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 dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 8.
b Also see Table 15.

Key to Acronyms:3TC = lamivudine; ABC = abacavir; BIC = bictegravir; BID = twice daily; COBI = cobicistat; CrCl = creatinine clearance; d4T = stavudine; ddI = didanosine; DOR = doravirine; DRV = darunavir; DTG = dolutegravir; EC = enteric coated; EFV = efavirenz; EVG = elvitegravir; FDC = fixed-dose combination; 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