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 :319.9 (515.9 as phosphate), (436 as sulphate)

%Protein binding :50–70

%Excreted unchanged in urine : 42–47

Volume of distribution (L/kg) :>100

half-life – normal/ESRD (hrs) :10–60 days/5–50 days

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Dose as in normal renal function

<10 : 50% of normal dose

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

HDF/high flux :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD :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

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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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