Eletriptan

CLINICAL USE


Acute relief of migraine

DOSE IN NORMAL RENAL FUNCTION

40–80 mg repeated after 2 hours if migraine recurs (do not take 2nd dose for the same attack)Maximum 80 mg in 24 hours

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :463.4 (as hydrobromide)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :85
  • %Excreted unchanged in urine &nbsp &nbsp : 9
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :2–2.5
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :4/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    30–50 20 mg; maximum daily dose 40 mg10–30 20 mg; maximum daily dose 40 mg, use with caution
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 20 mg; maximum daily dose 40 mg, use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR=10–30 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Antibacterials: concentration increased by clarithromycin and erythromycin – avoid concomitant use
  • Antidepressants: possibly increased serotonergic effects with duloxetine; increased serotonergic effects with St John’s wort – avoid concomitant use
  • Antifungals: concentration increased by itraconazole and ketoconazole – avoid concomitant use
  • Antivirals: concentration increased by indinavir, nelfinavir and ritonavir – avoid concomitant use
  • Ergot alkaloids: increased risk of vasospasm

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Non-renal clearance accounts for about 90% of the total clearanceManufacturer advises to avoid in severe renal impairment due to enhanced hypertensive effect.