CLINICAL USE


Antibacterial agent

DOSE IN NORMAL RENAL FUNCTION

Oral: 200–400 mg daily, increased if necessary to 400 mg twice dailyIV: 200–400 mg twice daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :361.4
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :25
  • %Excreted unchanged in urine &nbsp &nbsp : 65–80
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1.5–2.5
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :4–6/15–60

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : 200–400 mg once daily
  • 10 to 20 &nbsp &nbsp : 200–400 mg once daily
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 200 mg once daily

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not significantly dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min
  • HDF/high flux &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Dialysed. Dose as in GFR=10–20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Analgesics: increased risk of convulsions with NSAIDs
  • Anticoagulants: effect of acenocoumarol and warfarin enhanced
  • Antimalarials: manufacturer of artemether with lumefantrine advises avoid concomitant use
  • Ciclosporin: increased risk of nephrotoxicityTheophylline: possibly increased risk of convulsions

    ADMINISTRATION

    Reconstition

    Route

    Oral, IV

    Rate of Administration

    200 mg over 30 minutes

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