Medical Pharmacology: Immunopharmacology Practice Questions
Proliferation-Signal Inhibitors II (Sirolimus (rapamycin) and
Everolimus)
Click on the correct answer.
Sirolimus (Rapamune) and drug interactions:
Serolimus doses may have to be adjusted if the drug is administered with other drugs that may induce synthesis of the P450 drug metabolizing enzyme isoform CYP3A4.
Serolimus dosage may have to be reduced if other drugs that inhibit CYP3A4 or P-glycoprotein activity (such as diltiazem, a calcium channel blocker)
Both
Either
Serolimus toxicity:
In the context of renal transplantation, serolimus exhibits
a dose-dependent increase in triglycerides in serum cholesterol (may require therapy).
The use of cyclosporine in combination with sirolimus may result in more renal dysfunction compared to cyclosporine as monotherapy.
Both
Neither
Serolimus administration may increase proteinuria and therefore should be used cautiously in those individuals exhibiting GFR <30% or have pre-existing proteinuria.
True
False
Toxicity/toxicities associated with the proliferation signal inhibitor class which includes both serolimus and everolimus.
Myelosuppression, notably thrombocytopenia
Liver toxicity
Both
Neither
mTOR Inhibitor/inhibitors:
Everolimus
Zotarolimus
Both
Neither
Everolimus (Zortress and others): clinical use/uses
Astrocytoma treatment
Breast cancer treatment
Both
Neither
Everolimus (mTOR inhibitor) administration, if given with a calcineurin inhibitor, may
result in reduced kidney function to greater extent than seen with calcineurin inhibitor treatment by itself.
True
False
Patients receiving serolimus exhibit:
Increased risk of infection
Increased risk of lymphoma
Both
Neither
Sirolimus administration especially when used in combination with an ACE inhibitor may cause angioedema.
True
False
Serolimus is contraindicated in pregnancy due to its antiproliferative action.
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Source Material:
Rothlin C Gutkind J Chapter 39
Immunosuppressants, Immunomodulation and Tolerance In
Goodman & Gilman's The Pharmacological Basis of Therapeutics
(Brunton LL Knollman BC eds) McGraw Hill LLC (2023).
Lake D & Briggs A Ch 55 Immunopharmacology
in Katzung's Basic & Clinical Pharmacology (Vanderah TW, ed)
16e McGraw Hill 2023.
Chrouos G Ch 39 Adrenocorticosteroids &
Adrenocortical Antagonists in Katzung's Basic & Clinical
Pharmacology (Vanderah TW, ed) 16e McGraw Hill 2023
Brezinski E Klickstein L Armstrong A Ch 46
Pharmacology of Immunosuppression in Principles of
Pharmacology: The Pathophysiologic Basis of Drug Therapy.
(Golan DE Armstrong EJ Armstrong AW, eds) 4e 2017 ls) 4e
2017
Ritter JM Flower R Henderson G Loke YK
MacEwan D Robinson E Fullerton J Ch 54 Anti-inflammatory and
Immunosuppressant Drugs Rang & Dale's Pharmacology 10e
Elsevier 2024.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 72 Immunosuppressants Elsevier 2022.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 75 Glucocorticoids in Nonendrocrine
Disorders Elsevier 2022.
Bass A Rogatsky Ch 32 Immunomodulatory Drugs
in Goldman-Cecil Medicine (Goldman L Schafer, eds) Elsevier
26e 2020
Leiva M Takemoto Ch 238 Immunosuppressants in
Lippincott Illustrated Reviews: Pharmacology 8e ((Walen et
al, eds) Wolters Kluwer 2023.
Hall J Hall M Ch 78 Adrenocortical
Hormones Guyton and Hall Textbook of Medical Physiology 14e
Elsevier 2021.