Comparative Pharmacology
Head-to-head clinical analysis: CYCLOSPORINE versus ZORTRESS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CYCLOSPORINE versus ZORTRESS.
CYCLOSPORINE vs ZORTRESS
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.
Inhibits mammalian target of rapamycin (mTOR) by binding to FKBP-12, blocking cell cycle progression from G1 to S phase, thereby suppressing cytokine-driven T-cell proliferation.
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.
1.5 mg orally twice daily, administered with cyclosporine and corticosteroids.
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 10-15 hours in renal transplant patients. In de novo liver transplant patients, half-life is ~13 hours. The effective half-life supports twice-daily dosing.
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 fecal (~78%) with <2.5% excreted unchanged in urine. Small amount via biliary elimination.
Category D/X
Category C
Immunosuppressant
Immunosuppressant
"The risk or severity of adverse effects can be increased when Cyclosporine is combined with Furosemide."