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Tacrolimus, sold under the brand name Prograf among others, is an immunosuppressive drug. After allogenic organ transplant , the risk of organ rejection is moderate. To lower the risk of organ rejection, tacrolimus is given.
a Moderate inhibitor causes at least a 2-fold increase in the plasma AUC values, or 50–80% decrease in clearance. [39] a Weak inhibitor causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20–50% decrease in clearance. [39] The inhibitors of CYP3A4 are the following substances.
Tacrolimus: Efonidipine inhibits metabolic enzymes involved in Tacrolimus metabolism and reduces its clearance. So, increase in blood concentration of Tacrolimus can ...
TDM interpretation: an anticancer drug is given to a patient at a dosage of 400 mg every day at 8:00 am. A TDM sample is obtained at 6:00 am, showing a drug concentration of 0.46 mg/L. 1) Regarding “normality”, the result is around the 25th percentile, suggesting a rather high drug clearance in this patient.
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Two studies consisting of 26 and 17 patients who developed BKVAN on a three-drug regimen of tacrolimus, MMF, and steroids had their MMF replaced with leflunomide 20–60 mg daily. 84 and 88% of patients, respectively had clearance or a progressive reduction in viral load and a stabilization or improvement of graft function (7).
LCP-Tacro (tacrolimus) is a once-daily dosage version of tacrolimus for prevention of rejection in organ transplant patients in two Phase 3 clinical trials in kidney transplant patients. The first study in stable transplant patients showed that LCP-Tacro was non-inferior in efficacy and safety compared to twice-daily tacrolimus (Prograf ...
Tacrolimus: potential pharmacokinetic interactions; Other systemic antimycotic agents: with amphotericin B, itraconazole and mycophenolate, no interactions have been seen; Inducers of drug clearance (e.g. carbamazepine, phenytoin, rifampin, dexamethasone): consider 70 mg intravenous as maintenance dose instead of 50 mg
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