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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :102.1

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :<20

%Excreted unchanged in urine &nbsp &nbsp : 50–70

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.11–0.26

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :8–12/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : 250–500 mg every 12–24 hours. Monitor blood levels weekly

10 to 20 &nbsp &nbsp : 250–500 mg every 12–24 hours. Monitor blood levels weekly

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : 250–500 mg every 24 hours. Monitor blood levels weekly

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 :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

HDF/high flux &nbsp :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

CAV/VVHD &nbsp &nbsp &nbsp: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

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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.

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