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Mycophenolate mofetil
Last reviewed: 04.07.2025
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[ When is mycophenolate mofetil indicated?
The drug is recommended as part of induction and maintenance therapy for lupus nephritis. There is evidence of effectiveness in extrarenal manifestations of SLE, in various forms of systemic vasculitis, SSc, and IVM.
The usual dose is 2-3 g/day. For children, mycophenolate mofetil is prescribed at a rate of 600 mg/m2 every 12 hours.
How does mycophenolate mofetil work?
After oral administration of mycophenolate mofetil, liver esterases completely convert it into the active compound, mycophenolic acid, which is a noncompetitive inhibitor of inosine monophosphate dehydrogenase, an enzyme responsible for the rate-limiting stage of de novo synthesis of guanosine nucleotides required for the synthesis of lymphocyte DNA. Inhibition of inosine monophosphate dehydrogenase type II by mycophenolic acid results in depletion of guanosine nucleotides, suppression of DNA synthesis, and cessation of lymphocyte replication in the S phase.
Pharmacological effects
Suppression of lymphocyte proliferation, inhibition of antibody formation, prevention of glycosylation of lymphocyte and monocytic glycoproteins, slowing down the migration of lymphocytes to the inflammation zone, blocking the effect of macrophages on DNA synthesis and proliferation.
Pharmacokinetics
After oral administration, mycophenolate mofetil is rapidly and completely converted to its active metabolite, mycophenolic acid. The average bioavailability of mycophenolic acid after oral administration is approximately 94%. Peak concentration of the active metabolite is achieved 60-90 minutes after oral administration. Mycophenolic acid undergoes enterohepatic recirculation, as indicated by the presence of a second peak concentration in plasma 6-12 hours after administration. When the drug is administered in therapeutic doses, 97% of mycophenolic acid is bound to plasma albumin. Administration of mycophenolate mofetil simultaneously with food does not significantly affect AUC (area under the concentration-time curves), but reduces the maximum concentration of mycophenolic acid in plasma (Cmax) by 40%.
Mycophenolic acid is metabolized in the liver, where it is converted to mycophenolic acid glycuronide, which is excreted primarily in the urine. A small amount of mycophenolic acid (less than 1%) is excreted in the urine. The half-life of mycophenolic acid after a single oral dose of 1.5 g of the drug is 17.9 h, and the clearance is 11.6 h.
Mycophenolate mofetil: additional information
It is necessary to take into account that the risk of developing lymphoproliferative processes may increase, regularly monitor the composition of peripheral blood. But effective contraception is required during treatment and for 6 weeks after the end of the course.
The patient should avoid exposure to sunlight and ultraviolet radiation, wear protective clothing and use sunscreens with effective sun protection (to reduce the risk of developing skin cancer).
During treatment with mycophenolate mofetil, vaccination with attenuated vaccines should be avoided. Influenza vaccination may be administered.
Medicines that are eliminated from the body through tubular secretion should be administered with caution, especially in the presence of chronic renal failure.
Mycophenolate mofetil should not be administered concomitantly with drugs that affect enteropathic circulation (reduced effectiveness of mycophenolate mofetil).
Antacids containing aluminum or magnesium hydroxide should not be administered concomitantly with mycophenolate mofetil.
Because mycophenolate mofetil is an inosine monophosphate dehydrogenase inhibitor, it should not be administered to patients with rare hereditary hypoxanthine-guanine phosphoribosyltransferase deficiency (Lesch-Nyhan syndrome and Kelley-Seegmiller syndrome).
More careful monitoring should be carried out in elderly patients (risk of increased incidence of adverse events).
Better tolerability of the drug can be achieved by gradually increasing the dose. To prevent exacerbations of the disease, it is advisable to reduce the dose of mycophenolate mofetil slowly.
When is mycophenolate mofetil contraindicated?
Mycophenolate mofetil is contraindicated in pregnancy, lactation, hypersensitivity to the drug and its components, exacerbation of gastrointestinal diseases, hypoxanthine-guanosine phosphoribosyltransferase deficiency, lymphoma.
Side effects
Common side effects include abdominal pain, constipation, diarrhea, dyspepsia, chest pain, general weakness, headache, hematuria, hypertension, infections, leukopenia, nausea, vomiting, swelling of the feet, shortness of breath.
Less common side effects include acne, arthralgia, colitis, dizziness, insomnia, fever, rash, gastrointestinal bleeding, pharyngitis, gingival hyperplasia.
Rare side effects - gingivitis, pancreatitis, septicemia, myalgia, oral candidiasis, stomatitis, thrombocytopenia. tremor.
Overdose
Increased incidence of gastrointestinal and hematological side effects.
Clinically significant interactions
A decrease in the concentration of mycophenolic acid is noted with combined use with cyclosporine, antacids, metronidazole, fluoroquinolones, and an increase in concentration is noted with a combination of mycophenolate mofetil with salicylates, antiviral drugs (acyclovir, ganciclovir).
Special instructions
Pregnancy
Mycophenolate mofetil is a category C drug (permitted for use only if the benefit to the mother outweighs the potential risk to the fetus).
Breastfeeding
Discontinuation of breastfeeding or discontinuation of mycophenolate mofetil (the drug is excreted in rat milk; there are no data for humans) is indicated.
Attention!
To simplify the perception of information, this instruction for use of the drug "Mycophenolate mofetil" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.