Erlotinib
Erlotinib.JPG

Erlotinib

CLINICAL USE

Antineoplastic agent:Treatment of locally advanced or metastatic non-small cell lung cancer after failure of at least 1 other regime

DOSE IN NORMAL RENAL FUNCTION

150 mg daily at least 1 hour before or 2 hours after foodOr see local protocol

PHARMACOKINETICS

  • Molecular weight                           :429.9 (as hydrochloride)
  • %Protein binding                           :93–95
  • %Excreted unchanged in urine     : 9 (<2% as unchanged drug)
  • Volume of distribution (L/kg)       :232 litres
  • half-life – normal/ESRD (hrs)      :36

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function 15–20 Dose as in normal renal function<15 Use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unlikely to be dialysed. Dose as in GFR<15 mL/min
  • HD                     :Unlikely to be dialysed. Dose as in GFR<15 mL/min
  • HDF/high flux   :Unlikely to be dialysed. Dose as in GFR<15 mL/min
  • CAV/VVHD      :Unlikely to be dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Analgesics: increased risk of bleeding with NSAIDs
  • Anticoagulants: increased risk of bleeding with coumarins
  • Antipsychotics: avoid concomitant use with clozapine, increased risk of agranulocytosis

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Has not been tried in patients with a GFR<15 mL/min; therefore use with caution, but drug has limited renal excretionMajor side effects are rash and diarrhoea Can cause interstitial lung disease and abnormal liver function testsSmoking may reduce erlotinib concentration by increasing clearance.



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

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