CLINICAL USE


Acute treatment of migraine

DOSE IN NORMAL RENAL FUNCTION

10 mg, repeated after 2 hours if required; maximum of 2 doses in 24 hours

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :391.5 (as benzoate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :14
  • %Excreted unchanged in urine &nbsp &nbsp : 14

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :110 litres (females), 140 litres (males)

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :2–3/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Use with caution 5 mg, repeated after 2 hours; maximum 15 mg daily

    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 GR=
  • 10 to 20
    • mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Antidepressants: risk of CNS toxicity with MAOIs and linezolid – avoid for 2 weeks after discontinuation of MAOI; possibly increased serotonergic effects with duloxetine; increased serotonergic effects with St John’s wort – avoid concomitant use
  • Ergot alkaloids: increased risk of vasospasm – avoid concomitant use
    Propranolol: rizatriptan levels increased, reduce dose of rizatriptan to 5 mg (max 10 mg in 24 hours)

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Administration with food delays absorption by approximately 1 hour
    Metabolised to mainly inactive metabolites <1% excreted in the urine as active N-monodesmethyl metaboliteAUC increases by 44% in haemodialysis patients
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