CLINICAL USE

Nucleoside reverse transcriptase inhibitor: Treatment of HIV in combination with other antiretroviral drugs Prevention of maternal-foetal HIV transmission

DOSE IN NORMAL RENAL FUNCTION

Oral: 500–600 mg daily in 2–3 divided doses IV: 1–2 mg/kg every 4 hours

PHARMACOKINETICS

  • Molecular weight                           : 267.2
  • %Protein binding                           : 34–38
  • %Excreted unchanged in urine     : 8–25
  • Volume of distribution (L/kg)       : 1.6
  • half-life – normal/ESRD (hrs)      : 1.1/1. 4–3

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Give 100% of normal dose every 8 hours
  • 10 to 20     : Give 100% of normal dose every 8 hours
  • <10           : Give 50% of normal dose every 8 hours1

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                : Not dialysed. Dose as in GFR <10 mL/min
  • HD                     : Not dialysed. Dose as in GFR <10 mL/min Give post dialysis
  • HDF/high flux   : Unknown dialysability. Dose as in GFR <10 mL/min Give post dialysis
  • CAV/VVHD      : Not dialysed. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: absorption reduced by clarithromycin; avoid concomitant use with rifampicin
  • Anti-epileptics: phenytoin levels may be raised or lowered; concentration possibly increased by valproate (increased risk of toxicity)
  • Antifungals: concentration increased by fluconazole
  • Antivirals: profound myelosuppression with ganciclovir – avoid if possible; extreme lethargy on administration of IV aciclovir; effects of stavudine inhibited – avoid concomitant use; concentration reduced by tipranavir

    ADMINISTRATION

    Reconstition

    –

    Route

    IV, oral

    Rate of Administration

    1 hour

    Comments

    Dilute with glucose 5% infusion to give a final concentration of 2 mg/mL or 4 mg/mL

    OTHER INFORMATION

    Dialysis has little effect on zidovudine, presumably because of rapid metabolism. The glucuronide metabolite (T½ =1 hour) has no antiviral activity and will be significantly removed by dialysis Patients with severe renal failure have 50% higher maximum plasma concentrations 90% of a dose is excreted renally, mostly as the glucuronide. There is substantial accumulation of this metabolite in renal failure Main risk in renal impairment is haematological toxicity

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