Linezolid

CLINICAL USE

Antibacterial agent

DOSE IN NORMAL RENAL FUNCTION

600 mg twice daily

PHARMACOKINETICS

Molecular weight :337.3

%Protein binding :31

%Excreted unchanged in urine : 30

Volume of distribution (L/kg) :0.6

half-life – normal/ESRD (hrs) :5–7/Unchanged

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, but monitor closely.

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Likely to be dialysed. 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 :Dialysed. Dose as in normal renal functionCVVhdFDialysed. Dose as in normal renal function1

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antidepressants: increased risk of serotonergic syndrome with SSRIs and tricyclics; avoid concomitant use with MAOIs, moclobemideSelegiline: avoid concomitant use

Sympathomimetics: enhanced hypertensive effect with adrenaline, noradrenaline, dopamine, dobutamine, phenylpropanolamine and pseudoephedrine – use with caution

ADMINISTRATION

Reconstition

–

Route

Oral, IV

Rate of Administration

Over 30–120 minutes

Comments

–

OTHER INFORMATION

30% of dose is removed by a 3 hour haemodialysis sessionIn patients with GFR <10 mL/min, if platelet count drops on a dose of 600 mg twice daily, consider reducing dose to 600 mg once dailyTwo metabolites accumulate in renal failure which have MAOI activity but no antibacterial activity – monitor patients closelyThere is 5 mmol sodium per 300 mL infusionLinezolid is a weak, reversible non- selective inhibitor of MAO therefore can be used with drugs not normally given with MAOIs (e.g. SSRIs) but monitor closelyIn patients who have been on linezolid for longer than 28 days, there have been reports of peripheral neuropathy and/or optic neuropathy occasionally leading to loss of vision, anaemia requiring transfusions, and lactic acidosis – visual function should be monitored in these patientsAfter oral or IV administration, adequate drug concentrations can be found in PF fluid to treat VRE peritonitis. (Salzer W. Antimicrobial-resistant gram-positive bacteria in PD peritonitis.

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

Home