Mycophenolate mofetil:

• Prevention of rejection in allogeneic kidney, liver, and heart transplantation (used concurrently with cyclosporine and corticosteroids).

Mycophenolic acid:

• Prevention of rejection in allogenic renal transplantation (used concurrently with cyclosporine and corticosteroids).

Contraindicated in:

• Hypersensitivity
• Hypersensitivity to polysorbate 80 (for IV mycophenolate mofetil)
• OB: Pregnancy (↑ risk of congenital anomalies or spontaneous abortion).

Use Cautiously in:

• Active serious pathology of the GI tract (including history of ulcer disease or GI bleeding)
• Phenylketonuria (oral suspension contains aspartame)
• Severe chronic renal impairment (dose not to exceed 1 g twice daily [CellCept] if CCr <25 mL/min/1.73 m²); careful monitoring recommended
• Delayed graft function following transplantation (observe for ↑ toxicity)
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children <3 mo (mycophenolate mofetil) or <5 yr (mycophenolic acid)
• Geri: ↑risk of adverse reactions related to immunosuppression in older adults.

CV: edema, hypertension, hypotension, tachycardia.

Derm: rash.

Endo: hyperglycemia.

F and E: hyperkalemia, hypocalcemia, hypokalemia, hypomagnesemia.

GI: anorexia, constipation, diarrhea, nausea, vomiting, abdominal pain, GI BLEEDING.

GU: renal impairment.

Hemat: leukocytosis, leukopenia, thrombocytopenia, anemia, pure red cell aplasia.

Metab: hypercholesterolemia.

Neuro: anxiety, confusion, dizziness, headache, insomnia, paresthesia, sedation, tremor, PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY (PML).

Resp: cough, dyspnea.
Misc: fever, infection (including activation of latent viral infections such as Polyomavirus-associated nephropathy or Hepatitis B/C), acute inflammatory syndrome, MALIGNANCY.

Drug-Drug:

• Combined use with azathioprine is not recommended (effects unknown).
• Acyclovir and ganciclovir compete with MPA for renal excretion and, in patients with renal dysfunction, may ↑ each other’s toxicity.
• Magnesium and aluminum hydroxide antacids ↓ the absorption of MPA (avoid simultaneous administration).
• Proton pump inhibitors, including dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole may ↓ levels
• Cholestyramine and colestipol↓ the absorption of MPA (avoid concurrent use).
• May ↓ the effectiveness of oral contraceptives (additional contraceptive method should be used).
• May ↓ the antibody response to and ↑ risk of adverse reactions from live attenuated vaccines.
• Amoxicillin/clavulanic acid or ciprofloxacin may ↓ MPA trough levels.
• Cyclosporine may ↓ levels; use caution when discontinuing cyclosporine (may ↑ mycophenolate levels) or when switching from cyclosporine to another immunosuppressant, such as tacrolimus or belatacept
• Telmisartan may ↓ levels

(Generic available)

Mycophenolate Mofetil

• Tablets: 500 mg;
• Capsules: 250 mg;
• Oral suspension (fruit flavor): 200 mg/mL;
• Powder for injection : 500 mg/vial;

Mycophenolic Acid

• Delayed-release tablets: 180 mg; 360 mg;

Mycophenolate Mofetil

• PO, IV (Adults): 1 g twice daily; IV should be started 24 hr after transplantation and switched to PO as soon as possible (IV not recommended for 14 days).
• PO (Children 3 mo): 600 mg/m² twice daily (not to exceed 2 g/day).
Liver Transplantation
• PO, IV (Adults): 1 g twice daily IV, or 1.5 g twice daily PO. IV should be started 24 hr after transplantation and switched to PO as soon as possible (IV not recommended for 14 days).
• PO (Children 3 mo): 600 mg/m² twice daily; if well tolerated, can ↑ to 900 mg/m² twice daily (not to exceed 3 g/day).
Heart Transplantation
• PO, IV (Adults): 1.5 g twice daily; IV should be started 24 hr after transplantation and switched to PO as soon as possible (IV not recommended for 14 days).
• PO (Children 3 mo): 600 mg/m² twice daily; if well tolerated, can ↑ to 900 mg/m² twice daily (not to exceed 3 g/day).

Mycophenolic Acid

Mycophenolate mofetil and mycophenolic acid should not be used interchangeably without the advice of a health care professional.

• PO (Adults): 720 mg twice daily.
• PO (Children 5–16 yr and 1.19 m²): 400–450 mg/m² twice daily (not to exceed 720 mg twice daily).

CellCept

mycophenolic acid: Myfortic

• Inhibits the enzyme inosine monophosphate dehydrogenase, which is involved in purine synthesis. This inhibition results in suppression of T- and B-lymphocyte proliferation.

• Prevention of heart, kidney, or liver transplant rejection.

Therapeutic Classification: Immunosuppressant agents

Absorption: Following oral and IV administration, mycophenolate mofetil is rapidly hydrolyzed to mycophenolic acid (MPA), the active metabolite. Absorption of enteric-coated mycophenolic acid (Myfortic) is delayed compared with mycophenolate mofetil (CellCept).

Distribution: Cross the placenta and enter breast milk.

Protein Binding: MPA: 97%.

Metabolism/Excretion: MPA is extensively metabolized; <1% excreted unchanged in urine. Some enterohepatic recirculation of MPA occurs.

Half-life: MPA: 8–18 hr.

(blood levels of MPA)

• Instruct patient to take medication as directed, at the same time each day. Take missed dose as soon as remembered, but not if within 2 hrs before next dose. Do not skip or double up on missed doses. Do not discontinue without consulting health care professional. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• REMS: Explain REMS program to patient.
• Reinforce the need for lifelong therapy to prevent transplant rejection. Review symptoms of rejection for the transplanted organ, and stress need to notify health care professional immediately if signs of rejection or infection occur.
• May cause somnolence, confusion, dizziness, tremor, or hypotension. Caution patient to avoid driving and other activities requiring alertness until response from medication is known.
• Instruct patient to notify health care professional immediately if signs and symptoms of infection (temperature 100.5°F, cold symptoms [runny nose, sore throat], flu symptoms [upset stomach, stomach pain, vomiting, diarrhea], earache or headache, pain during urination, frequent urination, white patches in mouth or throat, unexpected bruising or bleeding, cuts, scrapes, or incisions that are red, warm, and oozing pus) or PML.
• Advise patient to avoid contact with persons with contagious diseases.
• Advise patient to avoid vaccinations with live attenuated virus during therapy.
• Inform patient of the increased risk of lymphoma and other malignancies. Advise patient to use sunscreen and wear protective clothing to decrease risk of skin cancer.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Instruct patient to avoid donating blood during and for at least 6 wk after discontinuation of therapy.
• May cause fetal harm. Inform females of reproductive potential of the potential for pregnancy loss and fetal harm. Discuss importance of simultaneously using two reliable nonhormonal forms of contraception, unless abstinence is the chosen method, prior to beginning, during, and for 6 wk following discontinuation of therapy and to avoid breastfeeding. Discuss acceptable forms of contraception with health care professional. Mycophenolate may decrease effectiveness of hormonal contraceptives. Encourage patients who become pregnant during or within 6 wk after therapy to enroll in the Pregnancy Registry by calling 1-800-617-8191 or to monitor pregnancy outcomes in women exposed to mycophenolate during pregnancy. Instruct male patients with female partners of reproductive potential to use effective contraception during and for at least 90 days after discontinuing therapy. Advise male patients to avoid semen donation during and for at least 90 days after discontinuing therapy.
• Emphasize the importance of routine follow-up laboratory tests.

mye-koe-FEE-noe-late MOE-fe-til

mycophenolic acid: mye-koe-FEE-noe-lik