Chloroquine

CLINICAL USE

  • Treatment and prophylaxis of malaria
  • Discoid and systemic lupus erythematosus
  • Rheumatoid arthritis

    DOSE IN NORMAL RENAL FUNCTION

  • Orally (as base)
  • Malaria treatment: 600 mg, followed by 300 mg 6–8 hours later, then 300 mg/day for 2 days
  • Malaria prophylaxis: 300 mg once a week on the same day each week (start 1 week before exposure to risk and continue until 4 weeks after leaving the malarial area
  • SLE: 150 mg daily
  • Rheumatoid arthritis: 150 mg daily; maximum 2.5 mg/kg

    PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :319.9 (515.9 as phosphate), (436 as sulphate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :50–70
  • %Excreted unchanged in urine &nbsp &nbsp : 42–47

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :>100

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :10–60 days/5–50 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 : 50% of normal dose

    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 :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

    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 mefloquine; avoid concomitant use with artemether/lumefantrine
  • Ciclosporin: increases ciclosporin concentration – increased risk of toxicity
  • Digoxin: possibly increased concentration of digoxin
  • Lanthanum: absorption possibly reduced by lanthanum, give at least 2 hours apart

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral, IV, IM/SC in rare cases

    Rate of Administration

    IV infusion :
  • Administer dose 10 mg/kg of chloroquine base in sodium chloride 0.9% by slow

    IV infusion

    over 8 hours followed by 3 further 8 hour infusions containing 5 mg base/kg (total dose 25 mg base/kg over 32 hours)

    Comments

  • Oral: Do not take indigestion remedies at the same time of day as this medicine
  • Chloroquine sulphate inj. is available: 5.45% w/v (equivalent to 40 mg chloroquine base per mL)

    OTHER INFORMATION

  • Excretion is increased in alkaline urine
  • Caution in patients with renal or hepatic disease
  • Bone marrow suppression may occur with extended treatment
  • 150 mg chloroquine base is equivalent to 200 mg of sulphate and 250 mg of phosphate
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