Comparison of the pharmacokinetics of tacrolimus and cyclosporine at equivalent molecular doses
N Karamperis, JV Povlsen, C Højskov… - Transplantation …, 2003 - Elsevier
Even though calcineurin inhibitors, namely Tacrolimus (FK) and Cyclosporine (CsA) share
similar physicochemical properties and a common mechanism of action, their
pharmacokinetics (pk) are different and unpredictable. Both drugs are metabolized by
cytochrome P450-3A4 isoforms in the liver and in the mucosa of the upper gastrointestinal
tract. FK in clinical practice is given in doses up to 50-fold lower than those of CsA due to its
greater potency. It is often assumed that the diverse dosing contributes to the observed …
similar physicochemical properties and a common mechanism of action, their
pharmacokinetics (pk) are different and unpredictable. Both drugs are metabolized by
cytochrome P450-3A4 isoforms in the liver and in the mucosa of the upper gastrointestinal
tract. FK in clinical practice is given in doses up to 50-fold lower than those of CsA due to its
greater potency. It is often assumed that the diverse dosing contributes to the observed …