Cycloserine.JPG

Cycloserine

CLINICAL USE

Antibacterial agent:Tuberculosis

DOSE IN NORMAL RENAL FUNCTION

Initially 250 mg every 12 hours for 2 weeks; then increased according to blood concentration and response to maximum 500 mg every 12 hours

PHARMACOKINETICS

  • Molecular weight                           :102.1
  • %Protein binding                           :<20
  • %Excreted unchanged in urine     : 50–70
  • Volume of distribution (L/kg)       :0.11–0.26
  • half-life – normal/ESRD (hrs)      :8–12/Increased

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : 250–500 mg every 12–24 hours. Monitor blood levels weekly
  • 10 to 20     : 250–500 mg every 12–24 hours. Monitor blood levels weekly
  • <10           : 250–500 mg every 24 hours. Monitor blood levels weekly

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Dose as in GFR <10 mL/min
  • HD                     :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR
  • <10           : mL/min
  • CAV/VVHD      :Likely dialysability. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsAlcohol: Increased risk of seizures

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    _

    OTHER INFORMATION

    May cause drowsiness – increased cerebral sensitivity in patients with renal impairmentBlood concentration monitoring is required, especially in renal impairment, if dose exceeds 500 mg daily, or if signs of toxicity. Blood concentration should not exceed 30 mg/LContraindicated in severe renal insufficiencyCan cause CNS toxicity Pyridoxine has been used in an attempt to treat or prevent neurological reactions, but its value is unproven.