Comparative Pharmacology
Head-to-head clinical analysis: PROGRAF versus TACROLIMUS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PROGRAF versus TACROLIMUS.
PROGRAF vs TACROLIMUS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Calcineurin inhibitor; binds to FKBP-12, inhibits calcineurin, preventing dephosphorylation and nuclear translocation of NF-AT, thereby inhibiting T-cell activation and cytokine gene transcription.
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: 0.1-0.15 mg/kg/day divided into 2 doses (every 12 hours). IV dose: 0.03-0.05 mg/kg/day as continuous infusion. Adjunct with corticosteroids.
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 8.7 hours (range 4-41 hours) in healthy volunteers; in liver transplant patients, half-life is approximately 11.7 hours (range 3.9-56 hours); 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 fecal (approximately 92%) with biliary excretion as the major route; renal excretion accounts for about 2.4% of the dose 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."