Comparative Pharmacology
Head-to-head clinical analysis: ASTAGRAF XL versus TACROLIMUS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASTAGRAF XL versus TACROLIMUS.
ASTAGRAF XL vs TACROLIMUS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).
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 of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/day.
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 43 hours (range 15.8–68.6 hours) in adult kidney transplant recipients. This long half-life supports once-daily dosing. In liver transplant patients, half-life ranges from 12 to 42 hours.
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 (94.6%) via biliary elimination. Renal excretion accounts for approximately 2.4% of the dose, mainly as metabolites. Less than 1% is excreted unchanged in urine.
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
Immunosuppressant, Calcineurin Inhibitor
Calcineurin Inhibitor
"Tacrolimus may increase the nephrotoxic activities of Droxicam."