Cyproterone acetate.JPG

Cyproterone acetate

CLINICAL USE

Control of libido in severe hypersexuality and sexual deviation in adult maleManagement of patients with prostatic cancer (LHRH ‘flare’, palliative treatment)Hot flushes post orchidectomy

DOSE IN NORMAL RENAL FUNCTION

Control of hypersexuality: 50 mg twice dailyProstatic cancer: 200–300 mg/day in 2–3 divided dosesHot flushes: 50–150 mg daily in 1–3 divided doses

PHARMACOKINETICS

  • Molecular weight                           :416.9
  • %Protein binding                           :Approx 96
  • %Excreted unchanged in urine     : <1
  • Volume of distribution (L/kg)       :10–30
  • half-life – normal/ESRD (hrs)      :32.1–56.7/–

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsNone known

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    May cause drowsiness – increased CNS sensitivity in patients with renal impairmentCSM has advised that in view of the hepatotoxicity associated with long-term doses of 300 mg daily, the use of cyproterone acetate in prostatic cancer should be restricted to short courses, to cover testosterone ‘flare’ associated with gonadorelin analogues, treatment of hot flushes after orchidectomy or gonadorelin analogues, and for patients who have not responded to (or are intolerant of) other treatmentsDirect hepatic toxicity including jaundice, hepatitis and hepatic failure have been reported. Liver function tests should be performed before treatment and whenever symptoms suggestive of hepatotoxicity occur