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
|
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
|
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 |