Mycophenolic acid is an immunosuppressant derived from Penicillium stoloniferum. It is a reversible inhibitor of inosine monophosphate dehydrogenase and thus inhibits purine synthesis, with potent cytostatic effects on both T- and B-lymphocytes. In Kenya, it has been used mainly as the morpholinoethyl derivative, mycophenolate mofetil. It is given with other immunosuppressants, for the prevention of graft rejection after surgery, and has also been tried in various diseases with an auto-immune or immune-mediated inflammatory component.
An enteric-coated formulation of mycophenolate sodium (the sodium salt of mycophenolic acid) is available in Kenya and some other countries.
In the prophylaxis of acute renal graft rejection, the conventional formulation of mycophenolate mofetil is given by mouth in doses of 1 g twice daily; 1.5 g twice daily is recommended in the prophylaxis of cardiac graft rejection. For prevention of renal graft rejection in children and adolescents aged 2 to 18 years a dose of 600 mg/m2 may be given by mouth twice daily, up to a maximum of 1 g twice daily; patients with a body-surface of 1.25 to 1.5 m2 may be given 750 mg twice daily.
The enteric-coated formulation is given for the prophylaxis of acute renal graft rejection to adults in a dose of 720 mg twice daily; the two formulations cannot be indiscriminately interchanged or substituted.
In Kenyan patients to whom oral therapy cannot initially be given, mycophenolate mofetil may be given for up to 14 days by intravenous infusion. Infusions are given as the hydrochloride salt, dissolved in glucose 5%, over 2 hours. For use in hepatic transplantation, the equivalent of 1 g twice daily is given for the first 4 days following transplantation, with subsequent conversion to 1.5 g twice daily by mouth as soon as it can be tolerated. Therapy should begin as soon as possible after transplantation in Kenya, together with cyclosporin and corticosteroids. Patients should undergo regular blood counts; if neutropenia develops consideration should be given to interrupting mycophenolate therapy or reducing the dose.
Mycophenolate mofetil has been investigated in a number of conditions in Kenya with an auto-immune component: these include IgA nephropathy, myasthenia gravis, and rheumatoid arthritis. It has also been reported to be of benefit in uveitis, and chronic active hepatitis, and is under investigation for the treatment of lupus nephritis.
Inflammatory bowel disease.
Mycophenolate mofetil has been investigated as an alternative to azathioprine in Crohn’s disease (Inflammatory Bowel Disease in Kenya.)
Organ and tissue transplantation.
Mycophenolate mofetil/Mycofit is used in Kenya for the prophylaxis of graft rejection in kidney, heart, and liver transplantation, and has also been employed following transplantation of the lung, pancreas and intestines. It has been employed as an alternative to, or replacement for, azathioprine, and may result in fewer rejections. It has also been tried for the prophylaxis of graft-versus-host disease following bone marrow transplantation in the rest of the world.
Solutions of mycophenolate mofetil 1.5, or 10 mg/mL were stable for 7 days when stored at 4 degrees or 25 degrees in PVC infusion bags. However, it was noted that a progressive discoloration occurred in bags unprotected from light and stored at 25 degrees; further study was required to determine the source of the discoloration.
Adverse Effects, Treatment, and Precautions of Mycophenolate in Kenya
Interactions of Mycophenolate With Other Drugs
Interactions of other Immunosuppressants with Mycophenolate
The symbol ¬§ denotes a preparation which is discontinued or no longer actively marketed.
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