Trade Names: CellCept, Myfortic
Synonyms: Mycophenolate mofetil, Mycophenolic acid
Drug Class: Immunosuppressant
Preparations
Tablet: 500 mg (CellCept), 180 mg (Myfortic), 360mg (Myfortic)
Capsule: 250 mg (CellCept)
Dose: In lupus nephritis usually started at 500/360 mg twice daily for a week and, if tolerated, increased to 1000/720 mg twice daily for a week and then increased to a target of 1.5/1.08 g twice daily. For maintenance therapy after remission lower doses (2/1.44 g/day) are used.
Indications: Treatment of SLE, vasculitis, inflammatory muscle disease
Mechanism of Action: Inosine monophosphate dehydrogenase inhibitor, inhibits guanine and de novo purine synthesis, inhibits T and B lymphocyte proliferation
Contraindications: Hypersensitivity to mycophenolate or mycophenolic acid, pregnancy, avoid live virus vaccines
Precautions: The patient must understand the risks and benefits of treatment and the requirement for monitoring. Pregnant women must not receive mycophenolate. Contraceptive methods should be reviewed and be in place before starting therapy. Because mycophenolate may affect the efficacy of estrogen contraceptives, two methods of contraception are recommended. Avoid live virus vaccines.
Monitoring
CBC, platelets, LFTs, creatinine at baseline; check CBC every 2 weeks till stable and and once stable CBC and LFTs every 4–8 weeks.
Pregnancy Risk: D; increased congenital malformations
Adverse Effects
Common: Nausea, GI cramps, diarrhea, headache
Less common: Vomiting, leukopenia, neutropenia, pure red cell aplasia, elevated liver enzymes, hypertension,edema, rash, hyperglycemia, tremor, increased risk of infection, skin cancer, herpes zoster, lymphoma, reactivation of hepatitis B or C, gastrointestinal perforation or bleeding
Drug Interactions
Antacids and cholestyramine: Decreased serum concentrations
Azathioprine: Increased toxicity, avoid this combination
Rifampin: Decreased serum concentrations
Oral contraceptives: Decreased contraceptive efficacy
Patient Instructions: Never increase the dose by yourself. Do not become pregnant. Protect skin from the sun.
Comments: Appears to be as effective as cyclophosphamide for induction therapy and more effective than azathioprine for maintenance therapy of lupus nephritis with a better side effect profile. In ANCA-associated vasculitis less effective than azathioprine in maintaining remission.
Clinical Pharmacology: Rapidly and completely absorbed, rapidly de-esterified to mycophenolic acid, the active drug, which is glucuronidated and excreted in the urine.
Adapted from: RheumaKnowledgy