Comparative Pharmacology
Head-to-head clinical analysis: CEQUA versus NEORAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CEQUA versus NEORAL.
CEQUA vs NEORAL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Immunosuppressant; binds to cyclophilin D in mitochondria, inhibiting opening of mitochondrial permeability transition pore (mPTP), which reduces T-lymphocyte activation and cytokine release. Also forms complex with cyclophilin A to inhibit calcineurin, suppressing IL-2 production and T-cell proliferation.
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.
Instill one drop of 0.09% ophthalmic solution in each eye twice daily, approximately 12 hours apart.
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
None Documented
Terminal elimination half-life is approximately 8.4 hours (range 6-10 hours) in healthy adults; prolonged in hepatic impairment and pediatric patients.
Terminal elimination half-life: 8.4 hours (range 6–24 hours) in healthy volunteers; prolonged in hepatic impairment (up to 20 hours).
Primarily fecal (90%) with minor renal excretion (<1% unchanged drug). Biliary excretion is the major route for elimination of cyclosporine metabolites.
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 C
Category C
Immunosuppressant
Immunosuppressant