Mefloquine

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 :414.8 (as hydrochloride)

%Protein binding :98

%Excreted unchanged in urine : 9 (+4% metabolites)

Volume of distribution (L/kg) :20

half-life – normal/ESRD (hrs) :21 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 : Use with caution Prophylaxis: Dose as in normal renal function

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 :Not dialysed. Dose as in GFR <10 mL/min

CAV/VVHD :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

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Route

Oral

Rate of Administration

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Comments

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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.

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