CLINICAL USE

Malaria chemoprophylaxis

DOSE IN NORMAL RENAL FUNCTION

200 mg daily

PHARMACOKINETICS

  • Molecular weight                           :290.2
  • %Protein binding                           :75
  • %Excreted unchanged in urine     : 60
  • Volume of distribution (L/kg)       :No data
  • half-life – normal/ESRD (hrs)      :20

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    20–60 100 mg daily

  • 10 to 20     : 50 mg every 48 hours
  • <10           : 50 mg weekly

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anticoagulants: effect of warfarin possibly enhanced
  • Antimalarials: avoid concomitant use with artemether/lumefantrine; increased antifolate effect with pyrimethamine

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Rare reports of haematological changes (e.g. megaloblastic anaemia and pancytopenia) in patients with severe renal impairment

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