It is indicated for the prophylaxis of organ rejection in patients receiving allogeneic renal, cardiac or hepatic transplants. it should be used concomitantly with cyclosporine and corticosteroids. it Intravenous is an alternative dosage form to it capsules, tablets and oral suspension. it Intravenous should be administered within 24 hours following transplantation. it Intravenous can be administered for up to 14 days; patients should be switched to oral it as soon as they can tolerate oral medication.
Immunological Chemotherapy, Immunosuppressant
Mechanism of Action: Mycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid (MPA). MPA is a potent, selective, uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis. The mechanism by which MPA inhibits the enzymatic activity of IMPDH appears to be related to the ability of MPA to structurally mimic both nicotinamide adenine dinucleotide cofactor and a catalytic water molecule. This prevents the oxidation of IMP to xanthose-5’-monophosphate which is the committed step in de novo guanosine nucleotide biosynthesis. MPA has more potent cytostatic effects on lymphocytes than on other cells because T- and B lymphocytes are critically dependent for their proliferation on de novo synthesis of purines whereas other cell types can utilize salvage pathways.
Pharmacodynamics: Mycophenolic acid, the active metabolite of mycophenolate mofetil, is a non-competitive, reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). Inhibition of IMPDH blocks the de novo synthesis of guanosine nucleotides which are necessary substrates for DNA and RNA synthesis. Unlike other cell types which can use the salvage pathway, B and T lymphocytes are dependent upon the de novo pathway for the generation of guanosine. Data from in vitro studies indicate that mycophenolic acid and/or mycophenolate mofetil inhibit mixed lymphocyte responses and human peripheral blood lymphocyte proliferation induced by a variety of mitogens and antigens. Mycophenolic acid decreases intracellular pools of guanosine triphosphate (GTP) and deoxyguanosine triphosphate (dGTP) in mitogen-stimulated human peripheral blood monocytes or T lymphocytic cell lines but has no effect on GTP concentrations in human neutrophils.
Renal Transplantation: Adults: A dose of 1 gm administered orally or intravenously (over NO LESS THAN 2 HOURS) twice a day (daily dose of 2 gm) is recommended for use in renal transplant patients. Although a dose of 1.5 g administered twice daily (daily dose of 3 gm) was used in clinical trials and was shown to be safe and effective, no efficacy advantage could be established for renal transplant patients. Patients receiving 2 gm/day of Mycophenolate demonstrated an overall better safety profile than did patients receiving 3 gm/day of Mycophenolate . Pediatrics : The recommended dose of Mycophenolate oral suspension is 600 mg/m2 administered twice daily (up to a maximum daily dose of 2 gm/10 ml oral suspension). Patients with a body surface area of 1.25 m2 to 1.5 m2 may be dosed with Mycophenolate capsules at a dose of 750 mg twice daily (1.5 g daily dose). Patients with a body surface area >1.5 m2 may be dosed with Mycophenolate capsules or tablets at a dose of 1 gm twice daily (2 gm daily dose). Cardiac Transplantation: A dose of 1.5 g bid administered intravenously (over NO LESS THAN 2 HOURS) or 1.5 g bid oral (daily dose of 3 gm) is recommended for use in adult cardiac transplantpatients. Hepatic Transplantation: A dose of 1 gm bid administered intravenously (over NO LESS THAN 2 HOURS) or 1.5 g bid oral (daily dose of 3 gm) is recommended for use in adult hepatic transplantpatients.
Caution should be exercised with concomitant administration of Antacids, Azathioprine, Cyclosporin, Rifampin, Sevelamer, Cholestyramine, Acyclovir, Metronidazole, Hormonal contraceptives as these medicines may decrease Mycophenolic acid concentration.
Allergic reactions to it have been observed; therefore, it is contraindicated in patients with a hypersensitivity to mycophenolate mofetil, mycophenolic acid or any component of the drug product. CellCept Intravenous is contraindicated in patients who are allergic to Polysorbate 80 (TWEEN)
The principal adverse reactions associated with the administration of Mycophenolate Mofetil includes diarrhea, leukopenia, sepsis, gastrointestinal candidiasis, urinary tract infection, herpes simplex, vomiting and there is evidence of a higher frequency of certain types of infections eg. opportunistic infections.
Pregnancy, lactation. Rare hereditary deficiency of hypoxanthine-guanine phosphoribosyltransferase (HGPRT), including Kelley-Seegmiller or Lesch-Nyhan syndrome
In many of these cases no adverse events were reported. It is expected that an overdose of mycophenolate mofetil could possibly result in over suppression of the immune system and increase susceptibility to infections and bone marrow suppression. If neutropenia develops, dosing with Mycophenolate Mofetil should be interrupted or the dose reduced.
Store in a cool (below 30°C), dry place and away from light. Keep out of the reach of children.
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