Comparative Pharmacology
Head-to-head clinical analysis: CYCLOSPORINE versus NEORAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CYCLOSPORINE versus NEORAL.
CYCLOSPORINE vs NEORAL
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.
Cyclosporine, the active ingredient in Neoral, is a calcineurin inhibitor. It binds to cyclophilin, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NF-AT (nuclear factor of activated T-cells). This inhibits transcription of interleukin-2 and other cytokines, reducing T-cell activation and 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.
Initial dose 10-15 mg/kg/day orally divided q12h, then taper by 5% weekly to maintenance of 3-5 mg/kg/day divided q12h. For psoriasis: 2.5 mg/kg/day orally divided q12h. For rheumatoid arthritis: 2.5-5 mg/kg/day orally divided q12h. Administer consistently with or without food.
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
None Documented
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: 8.4 hours (range 6–24 hours) in healthy volunteers; prolonged in hepatic impairment (up to 20 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 biliary/fecal (94%): 94% of dose eliminated in feces via bile, 6% in urine (0.1% unchanged). Minimal renal elimination of parent drug.
Category D/X
Category C
Immunosuppressant
Immunosuppressant
"The risk or severity of adverse effects can be increased when Cyclosporine is combined with Furosemide."