Davis's Lab & Diagnostic Tests

Immunosuppressants: Cyclosporine, Methotrexate, Everolimus, Sirolimus, and Tacrolimus

Immunosuppressants: Cyclosporine, Methotrexate, Everolimus, Sirolimus, and Tacrolimus is a topic covered in the Davis's Lab & Diagnostic Tests.

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Cyclosporine (Sandimmune), methotrexate (MTX, amethopterin, Folex, Metoject, Mexate, Rheumatrex), everolimus (Afinitor Disperz, Certican, Zortress), sirolimus (Rapamycin, Rapamune), tacrolimus (Advagraf, Prograf)

Common Use:
To monitor appropriate drug dosage of immunosuppressant related to organ transplant maintenance.

Whole blood collected in lavender-top tube for cyclosporine, everolimus; sirolimus; tacrolimus Serum collected in a red-top tube for methotrexate; specimen must be protected from light.

ImmunosuppressantRoute of AdministrationRecommended Collection Time
CyclosporineOral or intravenous12 hr after dose or immediately prior to next dose
MethotrexateOralVaries according to dosing protocol
IntramuscularVaries according to dosing protocol
EverolimusOralImmediately prior to next dose
SirolimusOralImmediately prior to next dose
TacrolimusOralImmediately prior to next dose
Leucovorin therapy, also called leucovorin rescue, is used in conjunction with administration of methotrexate Leucovorin, a fast-acting form of folic acid, protects healthy cells from the toxic effects of methotrexate

Normal Findings:
(Method: Immunoassay for cyclosporine and methotrexate; liquid chromatography with tandem mass spectrometry for everolimus, sirolimus, and tacrolimus)

Therapeutic DoseHalf-Life (hr)Volume of Distribution (L/kg)Protein Binding (%)Excretion
Conventional UnitsSI Units (Conventional Units × 0.832)
Cyclosporine100–300 ng/mL kidney transplant83–250 nmol/L8–244–690Renal
200–350 ng/mL cardiac, hepatic, pancreatic transplant166–291 nmol/L8–244–690Renal
100–300 ng/mL bone marrow transplant83–250 nmol/L8–244–690Renal
Conventional UnitsSI Units (Conventional Units × 1)
MethotrexateLow dose: Less than 0.5 micromol/L after 48 hrLow dose: Less than 0.5 micromol/L after 48 hr5–90.4–150–70Renal
High dose: Less than 5 micromol/L at 24 hr; less than 0.5 micromol/L at 48 hr; less than 0.1 micromol/L at 72 hrHigh dose: Less than 5 micromol/L at 24 hr; less than 0.5 micromol/L at 48 hr; less than 0.1 micromol/L at 72 hr
Conventional UnitsSI Units (Conventional Units × 1.04)
EverolimusTransplant: 3–8 ng/mLTransplant: 3–8 nmol/L18–35 (kidney); 30–35 (liver)128–58975Biliary
Oncology: 5–10 ng/mLOncology: 5–10 nmol/L18–35128–58975Biliary
Conventional UnitsSI Units (Conventional Units × 1.1)
SirolimusMaintenance phase: kidney transplant: 4–12 ng/mL; liver transplant: 12–20 ng/mLKidney transplant: 4–13 nmol/L; liver transplant: 13–22 nmol/L46–784–2092Biliary
Conventional UnitsSI Units (Conventional Units × 1.24)
TacrolimusMaintenance phase: Kidney transplant: 6–12 ng/mL; liver transplant: 4–10 ng/mL; pancreas transplant: 10–18 ng/mL; bone marrow transplant: 10–20 ng/mLKidney transplant: 7–15 nmol/L; liver transplant: 5–12 nmol/L; pancreas transplant: 12–22 nmol/L; bone marrow transplant: 12–25 nmol/L10–141.599Biliary
Therapeutic targets for the initial phase post-transplantation are slightly higher than during the maintenance phase and are influenced by the specific therapy chosen for each patient with respect to coordination of treatment for other conditions and corresponding therapies. Therapeutic ranges for everolimus, sirolimus, and tacrolimus assume concomitant administration of cyclosporine and steroids.

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