CLINICAL USE


Malaria prophylaxis and treatment

DOSE IN NORMAL RENAL FUNCTION

Prophylaxis: 250 mg weekly Treatment: Non-immune patients 20–25 mg/kg in —2–3 divided doses; maximum 1.5 gPartially-immune patients 15 mg/kg in —2–3 divided doses

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :414.8 (as hydrochloride)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :98
  • %Excreted unchanged in urine &nbsp &nbsp : 9 (+4% metabolites)
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :20
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :21 days

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Use with caution Prophylaxis: Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR=10–20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Anti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone – avoid concomitant use
  • Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin – avoid concomitant use
  • Anti-epileptics: antagonism of anticonvulsant effect
  • Antimalarials: increased risk of convulsions with chloroquine, hydroxychloroquine and quinine; avoid concomitant use with artemether and lumefantrine
  • Antipsychotics: increased risk of ventricular arrhythmias, avoid concomitant use with pimozide
  • Atomoxetine: increased risk of ventricular arrhythmiasIvabradine: increased risk of ventricular arrhythmias

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Start prophylaxis 1–3 weeks before arriving in malarial area and continue for 4 weeks after leaving the malarial areaIncreased risk of convulsions in patients with epilepsy.