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Questions and Answers
What is Mycophenolate mofetil (CellCept)?
What is Mycophenolate mofetil (CellCept)?
An immunosuppressive antimetabolite and a morpholinoethyl ester of mycophenolic acid.
How does Mycophenolate mofetil metabolize in the body?
How does Mycophenolate mofetil metabolize in the body?
It undergoes rapid and complete metabolism to mycophenolic acid, the active metabolite.
What is the mechanism of action of Mycophenolate mofetil?
What is the mechanism of action of Mycophenolate mofetil?
The active metabolite inhibits inosine monophosphate dehydrogenase (IMPDH), affecting the synthesis of guanine.
What are the boxed warnings associated with Mycophenolate mofetil?
What are the boxed warnings associated with Mycophenolate mofetil?
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What are the common adverse drug reactions (ADRs) of Mycophenolate mofetil?
What are the common adverse drug reactions (ADRs) of Mycophenolate mofetil?
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Mycophenolate mofetil is a prodrug that metabolizes to ________.
Mycophenolate mofetil is a prodrug that metabolizes to ________.
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What happens when Mycophenolate mofetil is administered with antacids containing magnesium and aluminum hydroxides?
What happens when Mycophenolate mofetil is administered with antacids containing magnesium and aluminum hydroxides?
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Mycophenolate sodium requires activation to become effective.
Mycophenolate sodium requires activation to become effective.
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Which drug decreases the absorption of Mycophenolate mofetil?
Which drug decreases the absorption of Mycophenolate mofetil?
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Study Notes
Mycophenolate Mofetil (CellCept) Overview
- Mycophenolate mofetil (MPM) is an immunosuppressive antimetabolite, a morpholinoethyl ester of mycophenolic acid.
- MPM is a prodrug, offering enhanced oral bioavailability compared to mycophenolic acid.
- An alternative formulation, mycophenolate sodium (Myfortic), is enteric-coated to minimize gastrointestinal side effects.
Indications
- MPM is primarily indicated for preventing organ rejection in allogeneic transplantation.
Metabolism and Absorption
- MPM is rapidly and completely metabolized to mycophenolic acid (MPA), its active metabolite, predominantly by esterases in the upper GI tract.
- Oral absorption of MPM is quick and essentially complete.
Mechanism of Action
- MPA inhibits inosine monophosphate dehydrogenase (IMPDH), crucial in the synthesis of guanine.
- The inhibition of IMPDH leads to reduced GTP levels, affecting RNA and DNA synthesis, particularly in T and B cells.
Detailed Metabolism and Drug Interactions
- MPA is further metabolized by UDP-glucuronosyltransferases (UGTs) into an inactive form, mycophenolic acid glucuronide (MPAG).
- MPAG can undergo enterohepatic recirculation via the liver through MDRP2 transport.
- Cyclosporine interferes with MDRP2, decreasing MPAG recirculation, resulting in increased urinary excretion and lower systemic levels when coadministered.
Boxed Warnings
- Associated risks include heightened susceptibility to infections, lymphoma, and malignancies.
- Pregnant individuals are at increased risk for pregnancy loss and congenital malformations; effective contraception is essential for females of childbearing potential.
Adverse Drug Reactions (ADRs)
- Common gastrointestinal ADRs: nausea, vomiting, constipation, diarrhea, and dyspepsia.
- Hematologic ADRs: anemia and leukopenia are notable side effects.
- Increased risk of infections, particularly urinary tract infections and cytomegalovirus (CMV) infections.
Drug-Drug Interactions (DDIs)
- Co-administration of antacids containing magnesium or aluminum hydroxides reduces the absorption of MPM and MPA; separation in timing is recommended.
- Cholestyramine and similar bile acid-binding agents disrupt enterohepatic recirculation, diminishing MPA exposure and effectiveness.
- Sevelamer negatively impacts MPM absorption; it should not be given simultaneously, but can be administered two hours post-MPM.
- Rifampin may reduce MPM absorption and should only be used based on a favorable benefit-risk assessment.
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Description
This quiz covers the essential aspects of Mycophenolate Mofetil, a key immunosuppressive medication. It explores its indications, metabolism, absorption, and mechanism of action, particularly in organ transplantation. Test your knowledge on this vital pharmaceutical agent and its role in preventing organ rejection.
