CLINICAL USE

MAOI antidepressant

DOSE IN NORMAL RENAL FUNCTION

15 mg 3 times daily; maximum: 30 mg 3 times daily

PHARMACOKINETICS

  • Molecular weight                           :136 (234.3 as sulphate)
  • %Protein binding                           :No data
  • %Excreted unchanged in urine     : 0.25–1.1
  • Volume of distribution (L/kg)       :No data
  • half-life – normal/ESRD (hrs)      :1.2/–

    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

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Possibly dialysed. Dose as in normal renal function
  • HD                     :Possibly dialysed. Dose as in normal renal function
  • HDF/high flux   :Possibly dialysed. Dose as in normal renal function
  • CAV/VVHD      :Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Alcohol: some alcoholic and dealcoholised drinks contain tyramine which can cause hypertensive crisisAlpha-blockers: avoid concomitant use with indoramin; enhanced hypotensive effect
  • Anaesthetics: avoid concomitant use
  • Analgesics: CNS excitation or depression with pethidine, other opioids and nefopam – avoid concomitant use
  • Antidepressants: enhancement of CNS effects and toxicity. Care with all antidepressants including drug free periods when changing therapies
  • Anti-epileptics: antagonism of anticonvulsant effect; avoid carbamazepine with or within 2 weeks of MAOIs
  • Antimalarials: avoid concomitant use with artemether/lumefantrine
  • Antipsychotics: effects enhanced by clozapine
  • Atomoxetine: avoid concomitant use and for 2 weeks after useBupropion: avoid with or for 2 weeks after MAOIs
  • Dopaminergics: avoid concomitant use with entacapone and tolcapone; hypertensive crisis with levodopa and rasagiline – avoid for at least 2 weeks after stopping MAOI; hypotension with selegiline5HT 1 agonist: risk of CNS toxicity with sumatriptan, rizatriptan and zolmitriptan – avoid sumatriptan and rizatriptan for 2 weeks after MAOIMethyldopa: avoid concomitant use
  • Sibutramine: increased risk of CNS toxicity – avoid concomitant use
  • Sympathomimetics: hypertensive crisis with dexamfetamine, other amphetamines, dopamine, dopexamine, ephedrine, isometheptene, methylphenidate, phenylephrine, phenylpropanolamine, pseudoephedrine or sympathomimeticsTetrabenazine: risk of CNS excitation and hypertension

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments