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Mycophenolate mofetil
Last reviewed: 23.04.2024
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[When is mycophenolate mofetil?
The drug is recommended as part of induction and maintenance therapy for lupus nephritis. There is evidence of effectiveness in extrarenal manifestations of SLE, with various forms of systemic vasculitis, SSD, and IVM.
The usual dose is 2 to 3 g / day. To children of mycophenolate, mofetil is administered at a rate of 600 mg / m 2 every 12 hours.
How does mycophenolate mycophenolate?
After taking mycophenolate mycophenolate mofetil inside liver esterases completely turn it into an active compound - mycophenolic acid, which is a noncompetitive inhibitor of inosine monophosphate dehydrogenase enzyme responsible for the limiting stage of de novo synthesis of guanosine nucleotides necessary for the synthesis of lymphocyte DNA. Suppression of inosine monophosphate dehydrogenase type II under the influence of mycophenolic acid leads to the depletion of guanosine nucleotides, suppression of DNA synthesis, and termination of lymphocyte replication in the S phase.
Pharmacological effects
Suppression of proliferation of lymphocytes, inhibition of the formation of antibodies, prevention of glycosylation of lymphocytic and monocytic glycoproteins, slowing the migration of lymphocytes into the inflammation zone, blocking the effects of macrophages on DNA synthesis and proliferation.
Pharmacokinetics
After ingestion of mycophenolate, mycophenolate quickly and completely turns into its active metabolite, mycophenolic acid. The average bioavailability of mycophenolic acid after taking the drug inside is approximately 94%. The peak concentration of the active metabolite is achieved 60 to 90 minutes after ingestion. Mycophenolic acid undergoes enterohepatic recirculation, indicated by the presence of a second peak in plasma concentration 6-12 hours after admission. When the drug is administered at therapeutic doses, 97% of mycophenolic acid is bound to plasma albumin. The administration of mycophenolate mofetil simultaneously with food intake has no significant effect on AUC (area under the curves "concentration time"), but reduces the maximum concentration of mycophenolic acid in the plasma (Cmax) by 40%.
Metabolism of mycophenolic acid occurs in the liver, where it is converted into glycuronide of mycophenolic acid, which is excreted mainly 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 intake of 1.5 g of the drug is 17.9 hours, and the clearance is 11.6 hours.
Mycophenolate mofetil: additional information
It should be taken into account that the risk of developing lymphoproliferative processes may increase, and the composition of peripheral blood can be regularly monitored. But the time of treatment and for 6 weeks after the end of the course is required effective contraception.
The patient should avoid exposure to sunlight and ultraviolet radiation, wear protective clothing and use sunscreens with effective protective action (to reduce the risk of skin cancer).
Mycophenolate treatment with mycophenolate should avoid vaccination with weakened vaccines. It is possible to carry out influenza vaccination.
It is necessary to prescribe with caution the medicines withdrawn from the body through tubular secretion, especially in the presence of chronic renal failure.
Do not prescribe mycophenolate mofetil concomitantly with drugs that affect the zosteropathic circulation (a decrease in the effectiveness of mycophenolate mofetil).
It should not be simultaneously with mycophenolate mofetil appoint antacid agents containing aluminum or magnesium hydroxide.
Since mycophenolate mofetil is an inhibitor of inosine monophosphate dehydrogenase, it should not be administered to patients with a rare inherited deficiency of hypoxanthine-guanine phosphoribosyltransferase (Lesch-Nichin syndrome and Kelly-Zygmiller syndrome).
Greater monitoring of the elderly should be carried out (risk of an increase in the incidence of adverse events).
The best tolerability of the drug can be achieved with a gradual increase in the dose. To prevent exacerbations of the disease, the dose of mycophenolate mofetil should be reduced slowly.
When is mycophenolate mycophenolate contraindicated?
Mycophenolate mofetil is contraindicated in pregnancy, lactation, hypersensitivity to the drug and its components, exacerbation of digestive tract diseases, insufficiency of hypoxanthine-guanosine phosphoribosyltransferase, lymphoma.
Side effects
Frequent side effects - abdominal pain, constipation, diarrhea, dyspepsia, pain in the chest, general weakness, headache, hematuria, hypertension, infections, leukopenia, nausea, vomiting, edema of the feet, dyspnea.
Less common side effects are acne, arthralgia, colitis, dizziness, insomnia, fever, rash, gastrointestinal bleeding, pharyngitis, gingival hyperplasia.
Rare side effects - gingivitis, pancreatitis, septicemia, myalgia, candidiasis of the mouth, stomatitis, thrombocytopenia. Tremor.
Overdose
Increased frequency of gastrointestinal and hematological side effects.
Clinically Significant Interactions
Decrease in the concentration of mycophenolic acid is noted against the background of combined administration with cyclosporine, antacids, metronidazole, fluoroquinolones, and an increase in concentration - with the combination of mycophenolate mofetil with salicylates, antiviral drugs (acyclovir, ganciclovir).
Special instructions
Pregnancy
Mycophenolate mofetil is a C category drug (it is only allowed to apply the case of the superiority of the mother's benefit over the potential risk to the fetus).
Lactation
An interruption of breastfeeding or a break in taking mycophenolate mofetil is indicated (the drug is excreted into the milk of rats, there is no data for humans).
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.