Mycophenolate mofetil

Administration

• Type: Immunosuppressant
• Dosage Forms: 250,500; 200mg/mL; IV
• Routes of Administration: PO, IV
• Common Trade Names: CellCept

Adult Dosing

Kidney transplant rejection prophylaxis

• 1 g PO/IV bid
• Start: IV with in 24h post transplant, continue up to 14 days, switch to PO ASAP; Info: give on empty stomach; stable patients may take with food

Heart transplant rejection prophylaxis

• 1.5 g PO/IV bid
• Start: IV with in 24h post transplant, continue up to 14 days, switch to PO ASAP; Info: give on empty stomach

Liver transplant rejection prophylaxis

• 1.5 g PO BID or 1 g IV bid
• Info: start IV with in 24h post transplant, continue up to 14 days, switch to PO ASAP; Info: give on empty stomach

Lupus nephritis

• 1 g PO bid
• Info: use with prednisone, consider decease dose 50% after 6mo treatment

Pediatric Dosing

Kidney transplant rejection prophylaxis

• 3 mo-18 yo: Dose: 600mg/m^2 PO bid; Alt: 750mg PO BID for body surf. area = 1.25-1.5 m^2; 1 g PO BID for body surf. area >1.5 m^2; Max: 1 g/dose

Special Populations

• Pregnancy Rating: D
• Lactation risk: possibly unsafe

Renal Dosing

• Adult:
  • kidney transplant patients, delayed graft function immediate postop: no adjustment
  • kidney transplant patients, outside immediate post-transplant period:CrCl <25: max 1 g bid; HD/PD: no supplement
  • heart or liver transplant patients: CrCl <25: weigh risk/benefit; HD/PD: not defined
• Pediatric:
  • kidney transplant patients, delayed graft function immediate postop: no adjustment
  • kidney transplant patients, outside immediate post-transplant period: CrCl <30: max 600mg/m^2/day; HD/PD: no supplement

Hepatic Dosing

• Adult: renal transplant with severe hepatic parenchymal disease: no adjustment; other hepatic impairment: not defined
• Pediatric: renal transplant with severe hepatic parenchymal disease: no adjustment; other hepatic impairment: not defined

Contraindications

• Allergy to class/drug
• hypersens. to polysorbate 80 (IV form)
• Lesch-Nyhan syndrome
• Kelly-Seegmiller syndrome
• caution in elderly patients
• caution if GI disorder
• caution if renal disease, severe
• caution if bone marrow depression
• caution if PKU (phenylalanine-containing forms)

Adverse Reactions

Serious

• thrombocytopenia
• leukopenia
• neutropenia
• immunosuppression
• infection, severe
• opportunistic infection
• viral reactivation
• polyomavirus-assoc. nephropathy
• PML
• pure red cell aplasia
• lymphoma
• lymphoproliferative disorders
• malignancy
• GI bleeding
• GI perforation/ulcer
• colitis
• acute renal failure
• interstitial lung disease
• pregnancy loss, 1st trimester
• congenital malformations

Common

• hypertension
• infection
• diarrhea
• peripheral edema
• anemia
• abdominal pain
• constipation
• leukopenia
• fever
• headache
• nausea/vomiting
• dyspepsia
• hypotension (rapid IV use)
• dyspnea
• cough
• hypercholesterolemia
• hypokalemia
• tremor
• acne
• insomnia

Pharmacology

• Half-life: 17.9h (PO route), 16.6h (IV route)
• Metabolism: liver; CYP450: Info: prodrug converted to mycophenolic acid (MPA)
• Excretion: urine 93% (<1% unchanged), feces 6%

Mechanism of Action

inhibits B- and T-lymphocyte proliferation

References

epocrates