Abstract:

BACKGROUND: As an immunosuppressant of anti-metabolites, mycophenolic acid has been widely used in organ transplantation due to its relatively low toxicity. However, its pharmacokinetic properties are unclear when combined with other immunosuppressants such as calcineurin inhibitors (tacrolimus or cyclosporine A).
OBJECTIVE: To explore the optimal concentration of mycophenolic acid by dynamically monitoring its concentration in renal transplantation recipients, comparing the pharmacokinetic properties of mycophenolic acid when combined with other immunosuppressants, in order to guide personalized medicine, thereby improving the therapeutic effect and reducing adverse effects.
METHODS: The concentration of mycophenolic acid in the blood before drug administration (C0), 0.5 hour after drug administration (C0.5), and 2 hours after drug administration (C2) in the kidney recipients was determined using SyvaEmit-2000 drug concentration detection analyzer.
RESULTS AND CONCLUSION: Total 820 mycophenolic acid area under the concentration time curve values were determined from 340 recipients, among which 574 mycophenolic acid area under the concentration time curve values were determined from the recipients received mycophenolate mofetil+tacrolimus and 246 from the recipients received mycophenolate mofetil+cyclosporine A respectively. In mycophenolate mofetil+cyclosporine A, the value of mycophenolic acid area under the concentration time curve was significantly lower than that in the mycophenolate mofetil+tacrolimus group, and the difference was significant (P < 0.05). The concentration of mycophenolic acid at C0 and C0.5 in the mycophenolate mofetil+tacrolimus group was higher than that in the mycophenolate mofetil+cyclosporine A group (P < 0.05), and concentration of mycophenolic acid at C2 in the mycophenolate mofetil+cyclosporine A group was higher than that in the mycophenolate mofetil+tacrolimus group (P < 0.05). Furthermore, in mycophenolate mofetil+tacrolimus group, more patients reached their peak concentration of mycophenolic acid at C0.5. The results indicated that when mycophenolate mofetil was used in combination with other immunosuppressants, the drug administration should be based on their pharmacokinetics properties and the patients might be given a lower dose of mycophenolate mofetil. Three-point mycophenolate mofetil area under the concentration-time curve method for monitoring mycophenolic acid blood concentration was simple and convenient, and could meet the needs for the clinical use.