CLINICAL USE

Nucleoside reverse transcriptase inhibitor:Treatment of HIV in combination with other antiretroviral drugs

DOSE IN NORMAL RENAL FUNCTION

<60 kg: 30 mg twice daily>60 kg: 40 mg twice daily

PHARMACOKINETICS

  • Molecular weight                           :224.2
  • %Protein binding                           :<1
  • %Excreted unchanged in urine     : 40
  • Volume of distribution (L/kg)       :0.5
  • half-life – normal/ESRD (hrs)      :1–1.5/5.5–8

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    26–50 <60 kg: 15 mg twice daily >60 kg: 20 mg twice daily<25 <60 kg: 15 mg daily >60 kg: 20 mg daily

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Dose as in GFR<25 mL/min
  • HD                     :Dialysed. Dose as in GFR<25 mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR<25 mL/min
  • CAV/VVHD      :Unknown dialysability. Dose as in GFR=26–50 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antivirals: zidovudine may inhibit intracellular activation – avoid concomitant use; increased risk of side effects with didanosine; effects possibly inhibited by ribavirinCytotoxics: effects possibly inhibited by doxorubicin; increased risk of toxicity with hydroxycarbamide – avoid concomitant use

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    Administer at least an hour before food

    OTHER INFORMATION

    Clearance by haemodialysis is 120 mL/min Lactic acidosis, sometimes fatal, has been reported with the use of nucleoside analoguesPatients with ERF are more likely to develop peripheral neuropathy.

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