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Appendix B, Table 1. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs) (Last
updated March 27, 2012; last reviewed March 27, 2012) (page 1 of 3)
Dosing
Recommendations
Generic Name Serum/ Adverse Events
(abbreviation)/ Formulations (For dosage adjustment Elimination Intracellular
Trade Name in renal or hepatic Half-lives (Also see Table 13)
insufficiency, see
Appendix B, Table 7.)
Abacavir Ziagen Ziagen Metabolized by 1.5 hrs/ • HSRs: Patients who test positive
(ABC)/Ziagen • 300-mg tablets 300 mg BID or alcohol 12–26 hrs for HLA-B*5701 are at highest
600 mg once daily dehydrogenase and risk. HLA screening should be
Also available as • 120-mg/mL oral glucuronyl done before initiation of ABC.
component of solution Take without regard to transferase Rechallenge is not
fixed-dose meals recommended.
combinations: Renal excretion of
metabolites 82% • Symptoms of HSR may include
Trizivir Trizivir Trizivir fever, rash, nausea, vomiting,
ABC (ABC 300 mg + 1 tablet BID Dosage adjustment diarrhea, abdominal pain, malaise,
for ABC
with ZDV+3TC ZDV 300 mg + or fatigue or respiratory symptoms
3TC 150 mg) tablet recommended in such as sore throat, cough, or
patients with hepatic shortness of breath.
insufficiency (See
Epzicom Epzicom Epzicom Appendix B, Table 7.) • Some cohort studies suggest
ABC with 3TC (ABC 600 mg + 1 tablet once daily increased risk of MI with recent or
3TC 300 mg) tablet current use of ABC, but this risk is
not substantiated in other studies.
Didanosine Videx EC Body weight ≥60kg: Renal excretion 50% 1.5 hrs/ • Pancreatitis
(ddI)/ 125-, 200-, 250-, 400 mg once daily >20 hrs
Videx EC 400-mg capsules With TDF: 250 mg once Dosage adjustment • Peripheral neuropathy
(generic available; daily in patients with renal • Retinal changes, optic neuritis
dose same as Videx Body weight <60kg: insufficiency
Videx EC) 10-mg/mL oral recommended (See • Lactic acidosis with hepatic
solution 250 mg once daily Appendix B, Table 7.) steatosis +/- pancreatitis (rare but
With TDF: 200 mg once
daily potentially life-threatening toxicity)
Take 1/2 hour before or 2 • Nausea, vomiting
hours after a meal
• Potential association with
Note: Preferred dosing with noncirrhotic portal hypertension,
oral solution is BID (total in some cases, patients presented
daily dose divided into 2 with esophageal varices
doses)
• 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
Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-1
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