Comparative Pharmacology
Head-to-head clinical analysis: CYCLOSPORINE versus MYFORTIC.
Head-to-head clinical analysis: CYCLOSPORINE versus MYFORTIC.
CYCLOSPORINE vs MYFORTIC
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cyclosporine is a calcineurin inhibitor that binds to cyclophilin, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of nuclear factor of activated T-cells (NFAT), which reduces transcription of interleukin-2 and other cytokines, leading to immunosuppression.
Mycophenolic acid inhibits inosine monophosphate dehydrogenase (IMPDH), thereby depleting guanosine nucleotides in T and B lymphocytes, suppressing their proliferation and antibody production.
Initial oral dose: 3-5 mg/kg/day divided q12h; maintenance: 2-4 mg/kg/day divided q12h. IV dose: 3-5 mg/kg/day as continuous infusion or divided q8-12h.
720 mg orally twice daily, on an empty stomach, 1 hour before or 2 hours after meals.
None Documented
None Documented
Clinical Note
moderateCyclosporine + Norfloxacin
"The metabolism of Norfloxacin can be decreased when combined with Cyclosporine."
Clinical Note
moderateCyclosporine + Torasemide
"The risk or severity of adverse effects can be increased when Cyclosporine is combined with Torasemide."
Clinical Note
moderateCyclosporine + Etacrynic acid
"The risk or severity of adverse effects can be increased when Cyclosporine is combined with Etacrynic acid."
Clinical Note
moderateCyclosporine + Furosemide
Terminal elimination half-life ranges from 8.4 to 27 hours (mean ~19 hours) in adults with normal liver function. In patients with hepatic impairment, half-life may be prolonged. Pediatric patients typically have shorter half-lives (7–19 hours).
Terminal elimination half-life is approximately 12-18 hours (mean 17 hours) in healthy volunteers; longer in hepatic impairment (up to 40 hours).
Primarily hepatic metabolism via CYP3A4; eliminated in bile and feces. Renal excretion accounts for <6% of unchanged drug. Approximately 90% of metabolites are excreted in bile and feces.
Primarily renal (approximately 95% as metabolites, <3% as unchanged drug); biliary/fecal excretion accounts for <5%.
Category D/X
Category C
Immunosuppressant
Immunosuppressant
"The risk or severity of adverse effects can be increased when Cyclosporine is combined with Furosemide."