mycophenolat

Mycophenolate refers to a class of immunosuppressive medicines whose active metabolite is mycophenolic acid (MPA). The two common formulations are mycophenolate mofetil (MMF), a prodrug, and enteric-coated mycopolate sodium (EC-MPS). Both deliver MPA after administration and are used to dampen immune responses.

Mechanism of action: MPA inhibits inosine monophosphate dehydrogenase (IMPDH), reducing de novo guanine nucleotide synthesis. This effect preferentially suppresses lymphocyte proliferation, since T and B cells rely on this pathway for growth, thereby lowering immune activity.

Medical uses: In solid organ transplantation, MMF or EC-MPS is used to prevent rejection, usually in combination with a calcineurin inhibitor (such as cyclosporine or tacrolimus) and corticosteroids. It is also employed for autoimmune diseases, notably lupus nephritis, and certain dermatologic conditions (for example pemphigus vulgaris) or other conditions in which immunosuppression is indicated.

Administration and dosing: MMF and EC-MPS are available as capsules or tablets. Dosing depends on the indication and formulation, with transplant regimens typically requiring twice-daily dosing and adjustments for kidney function and drug interactions. Formulations differ in their release profiles but aim to achieve similar MPA exposure per dose.

Adverse effects and monitoring: Common adverse effects include gastrointestinal symptoms (nausea, diarrhea), leukopenia, anemia, and increased infection risk. Long-term use carries a potential risk of malignancy. Mycophenolate is teratogenic; it is contraindicated in pregnancy, and effective contraception is required during treatment. Monitoring includes regular blood counts and liver and kidney function, as well as vaccination status; live vaccines are generally avoided during immunosuppression.

Interactions and cautions: Antacids with aluminum or magnesium may reduce MPA absorption; calcineurin inhibitors can alter MPA levels. Caution is advised when combining with azathioprine due to additive bone marrow suppression.