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

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