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mycophenolate (Cellcept, Myfortic)

Mycophenolate mofetil. Antibiotic substance produced by Penicillium brevi-compactum, P. stoloniferum & related species. Medication Guide to be distributed to every patient who fills a CellCept prescription. [7] Indications: 1) maintenance of immunosuppression after organ transplantation & for treatment of refractory rejection - renal graft rejection - liver transplantation [12] 2) used in conjunction with corticosteroids & cyclosporine 3) use in suppressing need for azathioprine 4) treatment of systemic lupus erythematosus, especially lupus nephritis [11] 5) polymyositis, dermatomyositis, vasculitis Contraindications: - pregnancy, pregnancy category: D [1,4,6] - women of childbearing potential should have a negative serum or urine pregnancy test with a sensitivity of at least 25 mIU/mL within one week prior to beginning therapy - women of childbearing potential taking mycophenolate must a) receive contraceptive counseling b) use effective contraception - begin using 2 chosen methods of contraception 4 weeks prior to starting mycophenolate therapy, unless abstinence is the chosen method - contraceptives should be used during & for 6 weeks after stopping mycophenolate Dosage: 1) 1 g PO BID 2) take on an empty stomach 3) do not crush or chew capsules 4) dose should be decreased or stopped in patients with neutropenia < 1300/mm3 Tabs: 250 mg. Myfortic: enteric coated Storage: - must be protected from light - product labeling for U.S. products does not instruct to dispense in original container [13] Dosage adjustment with renal failure: - doses > 2 g/day are not recommended Monitor: - baseline CBC, LFTs, serum creatinine - thereafter CBC, LFTs, serum creatinine every 3 months [1] Adverse effects: - commmon > 10% a) general - abdominal pain, fever, headache, infection from immunosuppression, asthenia, chest pain, back pain, hypertension b) central nervous system - tremor, insomnia, dizziness c) dermatology - acne, rash d) gastrointestinal - diarrhea, constipation, dyspepsia, nausea/vomiting e) hematologic - hypochromic anemia, leukopenia, thrombocytopenia, leukocytosis - pure red cell aplasia [9,10] f) metabolic - peripheral edema, hypercholesterolemia, hypophosphatemia, edema, hypokalemia, hyperkalemia, hyperglycemia g) respiratory - dyspnea, cough, pharyngitis, bronchitis, pneumonia h) urogenital - UTI, hematuria, renal tubular necrosis - progressive multifocal leukoencephalopathy ? [5] - congenital anomalies following exposure to mycophenolate mofetil during pregnancy, including microtia, cleft lip & cleft palate [6] - BK virus-associated nephropathy in renal transplant patients [8] Caution: 1) avoid inhalation or direct contact with skin or mucous membranes of powder in capsules; wash with soap & water if occurs 2) capsules should not be opened or crushed 3) teratogenic [6] Drug interactions: 1) antacids decrease absorption 2) cholestyramine decreases absorption 3) mycophenolate may increase levels of a) acyclovir b) ganciclovir 4) iron supplements may increase mycophenolate levels 5) probenecid may increase mycophenolate levels 7) salicylates may increase free fraction of mycophenolate Mechanism of action: 1) immunosuppressive agent 2) inhibits purine metabolism - inhibits inosine monophosphate dehydrogenase - antiproliferative - preferentially inhibits T-cells & B-cells [1]

Interactions

drug interactions drug adverse effects of immunosuppressive agents monitor with immunosuppressive agents

General

alkene; olefin antineoplastic agent (chemotherapeutic agent) carboxylate disease-modifying antirheumatic agent (DMARD) ester immunosuppressive agent inosine-5'-monophosphate dehydrogenase inhibitor; IMP dehydrogenase inhibitor phenol other antibiotic

Properties

MISC-INFO: elimination route KIDNEY pregnancy-category X

Database Correlations

PUBCHEM correlations

References

  1. Medical Knowledge Self Assessment Program (MKSAP) 11, 17. American College of Physicians, Philadelphia 1998, 2015
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Department of Veterans Affairs, VA National Formulary
  4. Prescriber's Letter 14(12): 2007 Pregnancy Category Change for Mycophenolate Motefil (CellCept) Detail-Document#: 231208 (subscription needed) http://www.prescribersletter.com
  5. FDA MedWatch http://www.fda.gov/medwatch/safety/2008/safety08.htm#mycophenolate
  6. FDA MedWatch http://www.fda.gov/medwatch/safety/2008/safety08.htm#MMF
  7. FDA MedWatch http://www.fda.gov/medwatch/safety/2009/safety09.htm#CellCept
  8. FDA Medwatch http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm171828.htm
  9. FDA Medwatch http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm177397.htm
  10. FDA MedWatch http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm181306.htm
  11. Kamanamool N, McEvoy M, Attia J et al Efficacy and adverse events of mycophenolate mofetil versus cyclophosphamide for induction therapy of lupus nephritis: systematic review and meta-analysis. Medicine (Baltimore). 2010 Jul;89(4):227-35. PMID: 20616662
  12. Deprecated Reference
  13. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  14. Myfortic: Novartis at (888) 669-6682