Comparative Pharmacology
Head-to-head clinical analysis: SANDIMMUNE versus TACROLIMUS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SANDIMMUNE versus TACROLIMUS.
SANDIMMUNE vs TACROLIMUS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cyclosporine is a calcineurin inhibitor. It binds to cyclophilin, forming a complex that inhibits calcineurin, thereby blocking the dephosphorylation and nuclear translocation of NF-AT, reducing T-cell activation and cytokine production.
Tacrolimus is a calcineurin inhibitor. It binds to FK506-binding protein 12 (FKBP12), forming a complex that inhibits calcineurin phosphatase activity. This prevents dephosphorylation and nuclear translocation of nuclear factor of activated T-cells (NFAT), thereby inhibiting transcription of interleukin-2 (IL-2) and other cytokines, leading to suppressed T-cell activation and proliferation.
Initial oral dose: 10-15 mg/kg/day divided q12h, then taper to 5-10 mg/kg/day. IV dose: 5-6 mg/kg/day continuous infusion or divided q12h.
0.1-0.2 mg/kg/day orally in two divided doses (immediate-release); 0.05-0.15 mg/kg/day orally once daily (extended-release); 0.01-0.05 mg/kg/day continuous IV infusion.
None Documented
None Documented
Clinical Note
moderateTacrolimus + Levofloxacin
"Tacrolimus may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderateTacrolimus + Benzydamine
"Tacrolimus may increase the nephrotoxic activities of Benzydamine."
Clinical Note
moderateTacrolimus + Budesonide
"The risk or severity of adverse effects can be increased when Tacrolimus is combined with Budesonide."
Clinical Note
moderateTacrolimus + Droxicam
Terminal elimination half-life is approximately 8.4 hours (range 6–24 hours) in adults; prolonged in patients with hepatic impairment.
Terminal elimination half-life is approximately 8.7-21.7 hours in healthy volunteers and 18-41 hours in liver transplant recipients. Prolonged half-life in hepatic impairment requires dose adjustments.
Primarily biliary/fecal (94% of metabolites); renal elimination is minimal (<6% as unchanged drug and metabolites).
Primarily fecal (approximately 93%), with renal excretion accounting for about 2.4% of the unchanged drug. Biliary excretion is a minor route for metabolites.
Category C
Category D/X
Calcineurin Inhibitor
Calcineurin Inhibitor
"Tacrolimus may increase the nephrotoxic activities of Droxicam."