hydroxychloroquine sulphate

CLINICAL USE

Rheumatoid arthritis Systemic lupus erythematosus Dermatological conditions caused or aggravated by sunlightMalaria (unlicensed in UK)

DOSE IN NORMAL RENAL FUNCTION

200–400 mg daily in divided doses; maximum of 6.5 mg/kg/dayProphylaxis of malaria: 400 mg weekly

PHARMACOKINETICS

Molecular weight :434

%Protein binding :30–40

%Excreted unchanged in urine : 3

Volume of distribution (L/kg) :Large

half-life – normal/ESRD (hrs) :5.9–504/–

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

30–50 Maximum 75% of dose10–30 25–50% of dose (equivalent of 150 mg daily)

<10 : 25– 50% of dose (equivalent of 50–100 mg daily) – use with caution

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 :Unknown dialysability. Dose as in GFR=10–30 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 mefloquine; avoid concomitant use with artemether/lumefantrine

Ciclosporin: increased ciclosporin concentration (increased risk of toxicity)Digoxin: possibly increased concentration of digoxinLanthanum: absorption possibly reduced by lanthanum – give at least 2 hours apart

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Take with a meal or a glass of milk Excretory patterns are not well characterised, but hydroxychloroquine and its metabolites are slowly excreted via the kidneysAttempt to avoid prolonged use in renal failureIn renal insufficiency, need more than annual eye examinationsDoses from Seyffart, probably not actually practical to give reduced dose so try giving longer dose intervals

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