Pharmacokinetics: immunosuppressive drugs Allie Punke (apunke@uthsc.edu)

Immunosuppressive drugs cyclosporine Immunosuppressive drugs

The basics What is the half-life? What are the starting doses? What CYP enzyme metabolizes it? Is it affected by bile flow? What type of level do we get (i.e. peak or trough)? What is the conversion from oral to IV?

cyclosporine There are several formulations available: Sandimmune, Neoral, and Gengraf/Eon/Sidmak Which are bioequivalent to each other? If a patient is scheduled to receive Sandimmune 5 mg/kg/day PO divided BID. She has a T-tube draining into a bile bag. What, if any, modification would you make?

cyclosporine What effects (increased or decreased cyclosporine level) will the following medications cause: Erythromycin Grapefruit juice Rifampin Verapamil Carbamazepine Phenobarbital

cyclosporine A patient is receiving 325 mg BID cyclosporine, but needs to be converted to IV cyclosporine. What dosing regimen do you recommend? If changing to a liquid, what dosing regimen would you recommend? How long should cyclosporine be infused over? Why? Dose IV=0.3 (PO oral total dose) Dose (capsule)=Dose (liquid)

cyclosporine A patient was received her first dose of cyclosporine on 3/8 at 3/8 0705. Lab: Cyclosporine trough (3/9 at 0655 ): 140 ng/ml. Previous cyclosporine dose given on 3/8 at 1905. What do you recommend doing? A. Increasing the dose B. Decreasing the dose C. Leaving the dose alone

Immunosuppressive drugs tacrolimus Immunosuppressive drugs

tacrolimus What is the therapeutic range? What is the half-life? What are the starting doses? What CYP enzyme metabolizes it? What type of level do we get (i.e. peak or trough)? What is the conversion from oral to IV?

tacrolimus AR (67 kg) is a 16 YO African American male who received an intestinal transplant. The medical teams wants to initiate him on oral tacrolimus. What dosing regimen would you recommend? What if he was a 40 YO Caucasian male (94 kg) who was receiving verapamil? 0.15-0.3…..0.3 in this patient (young, african american, intestine transplant).

tacrolimus AR (67 kg) is a 16 YO African American male who is received an intestinal transplant. He is receiving 10 mg BID tacrolimus. He needs to be switched to IV tacrolimus. What dosing regimen do you recommend? How should tacrolimus be infused? Conversion: Oral dose= 4*IV dose

tacrolimus A patient has been accidentally “doubling up” on her tacrolimus dose. The 12 hour trough level drawn was 80. How long will it take for the level to be reach 10?

tacrolimus A patient has been receiving 5 mg BID with the most recent trough level of 10. If a trough of 15 is targeted, what should the new dosing regimen be?

Immunosuppressive drugs sirolimus Immunosuppressive drugs

The basics What is the therapeutic range? What is the half-life? What are the starting doses? What CYP enzyme metabolizes it? What type of level do we get (i.e. peak or trough)?

sirolimus DJ is a 80 YO Caucasian female who needs to be initiated on sirolimus. What maintenance dose would you recommend for her? If a loading dose is needed, what dose would be appropriate?

sirolimus When do we need to check a trough level?

Immunosuppressive drugs everolimus Immunosuppressive drugs

everolimus What is the therapeutic range? What is the half-life? What CYP enzyme metabolizes it? What type of level do we get (i.e. peak or trough)?

everolimus A patient had her blood drawn to check the everolimus level at the appointment with you. The level was 12 (goal is 3-8). She did note that she forgot to take it her last dose at 9 pm, so she took it when she remembered at 6 am this morning. How should we adjust her dosing?

Summary Be able to recognize drug interactions and how they can affect dosing (i.e. higher doses will be needed with inducers) Know the half life and starting doses of the medications Know how to convert oral IV Know how to interpret a level Know the factors that can affect absorption (i.e. T tube)

Questions? Enjoy your weekend!