Mycophenolate

CLINICAL USE

Mycophenolate sodium: for renal transplantationMycophenolate mofetil: prophylaxis against acute transplant rejection; autoimmune renal diseases

DOSE IN NORMAL RENAL FUNCTION

Mycophenolate sodium: 720 mg twice dailyMycophenolate mofetil: 1–1.5 g twice a day

PHARMACOKINETICS

Molecular weight :320.3 (mycophenolic acid) 433.5 (as mofetil) 342.3 (as sodium)

%Protein binding :97

%Excreted unchanged in urine : <1

Volume of distribution (L/kg) :3.6–4

half-life – normal/ESRD (hrs) :12–17.9/–

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Mycophenolate mofetil: 1 g twice a day; mycophenolate sodium: dose as in normal renal function

<10 : Mycophenolate mofetil: 1 g twice a day; mycophenolate sodium: dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Not dialysed. Dose as in GFR <10 mL/min

HD :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD :Not dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antipsychotics: avoid concomitant use with clozapine (increased risk of agranulocytosis)

Antivirals: higher concentrations of both mycophenolate acid and aciclovir or ganciclovir when the two are prescribed concomitantlyAntacids: absorption of mycophenolate decreased in presence of magnesium and aluminium saltsColestyramine: 40% reduction in oral bioavailability of mycophenolate

Ciclosporin: some studies show that ciclosporin decreases plasma MPA AUC levels; other studies show increases – no dose change requiredIron preparations: may significantly reduce absorption of mycophenolateSevelamer: reduced levels of mycophenolate

Tacrolimus: increases MPA concentrations– no dose change required but monitor closely

ADMINISTRATION

Reconstition

Add 14 mL of glucose 5% per 500 mg vial

Route

Oral, IV

Rate of Administration

Over 2 hours

Comments

Dilute reconstituted solution further with glucose 5% to achieve a concentration of 6 mg/mL

OTHER INFORMATION

Mycophenolate mofetil (MMF) rapidly undergoes complete presystemic absorption to mycophenolic acid (MPA) which in turn is metabolised to MPA glucuronide. This undergoes extensive enterohepatic recirculation, hence a secondary increase in MPA plasma levels is seen 6–12 hours post doseIf neutrophil count drops below 1.3 × 10 3/μL, consider suspending MMF therapyNo dosage reduction is required in the event of a transplant rejection episodeMycophenolate sodium 720 mg is approximately equivalent to 1 g mycophenolate mofetil.

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