Artemether with lumefantrine

CLINICAL USE

Treatment of malaria

DOSE IN NORMAL RENAL FUNCTION

>35 kg: 6 doses of 4 tablets, i.e. 24 tablets
given over 60 hours
Give 4 tablets at 0, 8, 24, 36, 48 and 60 hours

PHARMACOKINETICS

  • Molecular weight                           :
    Artemether: 298.4;
    lumefantrine: 528.9
  • %Protein binding                           :
    Artemether: 95.4;
    lumefantrine: 99.9
  • %Excreted unchanged in urine     :
    No data
  • Volume of distribution (L/kg)       :
    Artemether: 5.4–8.6;
    lumefantrine: 3.8
  • half-life – normal/ESRD (hrs)      :
    Artemether 0.8–7;
    lumefantrine: 48–72
    (4–6 days in people
    with falciparum
    malaria)

    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           :
    Dose as in normal renal function.
    Use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :
    Unknown dialysability. Dose as in
    GFR <10 mL/min
  • HD                     :
    Unknown dialysability. 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
    normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anti-arrhythmics: avoid concomitant usewith amiodarone, disopyramide, flecainide
    and procainamide – risk of ventricular
    arrhythmias
    Antibacterials: avoid concomitant use with

    macrolides and quinolones.

  • Antidepressants: avoid concomitant use
  • Antifungals: avoid concomitant use withimidazoles and triazoles.
    Antimalarials: increased risk of ventricular

    arrhythmias with quinine – avoid
    concomitant use.

  • Antipsychotics: avoid concomitant use
  • Antivirals: avoid concomitant use withamprenavir, atazanavir, indinavir, lopinavir,
    nelfinavir, ritonavir and saquinavir;
    possibly increased risk of ventricular
    arrhythmias with tipranavir – avoid
    concomitant use
    Beta-blockers: avoid concomitant use with

    metoprolol and sotalol

  • Grapefruit juice: may increasebioavailability and inhibit metabolism –
    avoid concomitant use
    Ulcer-healing drugs: avoid concomitant

    use with cimetidine

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    Take with food to increase absorption

    If patient vomits within 1 hour of taking

    the tablet the dose should be repeated

    OTHER INFORMATION

  • In renal impairment monitor ECG andpotassium levels
  • Undergoes extensive metabolism by theliver
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