Inhibitor of Inosine Monophosphate Dehydrogenase (IMPDH): inhibits de novo guanosine nucleotide synthesis
Cytostatic Effect on Both T-Lymphocytes and B-Lymphocytes: since T/B-cells are dependent on this pathway for proliferation
Pharmacodynamics
Elimination Half-Life
Cellcept
PO: 18 hrs for MPA
IV: 17 hrs for MPA
Myfortic
PO: 8-16 hrs for MPA (13-17 hrs for MPAG)
Metabolism
Hepatic and Via Gastrointestinal Tract
Cellcept is completely hydrolyzed by the liver to mycophenolic acid (MPA), which is an active metabolite
Enterohepatic circulation of mycophenolic acid may occur
Mycophenolic acid is glucuronidated to MPAG (an inactive metabolite)
Administration
PO (Mycophenolate Mofetil = Cellcept)
Renal Transplant: 1 g BID
Cardiac Transplant: 1.5 g BID
Liver Transplant: 1.5 g BID
PO (Mycophenolic Acid = Myfortic)
Renal Transplant: 720 mg BID
IV (Mycophenolate Mofetil = Cellcept): limit use to max of 14 days
Renal Transplant: 1 g BID
Cardiac Transplant: 1.5 g BID
Liver Transplant: 1 g BID
Dose Adjustment
Hepatic: no dose adjustment required for renal patients with severe liver disease (unclear if dose adjustment is required in other settings with liver disease)
Renal
Renal Transplant
GFR <25 mL/min (Outside of Immediate Post-Transplant Period)
Cellcept: avoid doses >1 g
Myfortic: no dose adjustment required
Cardiac/Liver Transplant: no data available
Autoimmune Disease: no specific dose adjustment required (however, since mycophenolate exposure appears to be related to renal function, close monitoring in the setting of renal dysfunction, especially with end-stage renal disease, is recommended)
Hemodialysis: no dose adjustment required (as drug is not removed by hemodialysis)
Peritoneal Dialysis: no dose adjustment required
Pregnancy
Increased Risk of Congenital Malformations/First Trimester Pregnancy Loss
Adverse Effects
Cardiovascular Adverse Effects
Chest Pain (see Chest Pain, [[Chest Pain]]): occurs in 26% of cases
Hypertension (see Hypertension, [[Hypertension]]): occurs in 28-78% of cases
Hypotension (see Hypotension, [[Hypotension]]): occurs in 33% of cases
Sinus Tachycardia (see Sinus Tachycardia, [[Sinus Tachycardia]])): occurs in 20-22% of cases
Dermatologic Adverse Effects
Rash: occurs in 22% of case
Endocrinologic Adverse Effects
Hyperglycemia (see Hyperglycemia, [[Hyperglycemia]])): occurs in 44-47% of cases
Hyperlipidemia (see Hyperlipidemia, [[Hyperlipidemia]]): occurs in 41% of cases
Gastrointestinal Adverse Effects
Diarrhea (see Diarrhea, [[Diarrhea]]): occurs in 31-51% of cases
Elevated Liver Function Tests (LFT’s) (see Drug-Induced Hepatotoxicity, [[Drug-Induced Hepatotoxicity]]): occurs in 25% of cases
Vomiting (see Nausea and Vomiting, [[Nausea and Vomiting]]): occurs in 33% of cases
Hematologic Adverse Effects
Anemia/Pure Red Cell Aplasia (see Anemia, [[Anemia]])
Epidemiology: occurs in 26-43% of cases
Increased Risk of Malignancy
Post-Transplant Lymphoproliferative Disease
Skin Cancer
Leukopenia/Neutropenia (see Leukopenia, [[Leukopenia]])
Epidemiology: leukopenia occurs in 23-46% of cases
Physiology: xxx
Management: may require interruption or reduction of dosing
