Medical Pharmacology: Immunopharmacology Practice Questions

Medical Pharmacology: Immunopharmacology Practice Questions

Calcineurin Inhibitors II (Cyclosporin, Tacrolimus)


Cyclosporine	Tacrolimus

Click on the correct answer.

Cyclosporine:
1. Binds to cyclophilin A which is the prominent immunophilin localized in T cells.
2. Binding of cyclosporine to cyclophilin A Increases cyclophilin-mediated inhibition of calcineurin.
3. Both
4. Neither
T-cell activation increases calcineurin activity leading to activation of nuclear factor of activated T cells (NFAT). This enhancement of NFAT promotes interleukin-2 (IL-2) in addition to other cytokines associated with the immune response.
1. True
2. False
Calcineurin promotes activation of NFκB which is very important for T-cell function and survival.
1. True
2. False
Cyclosporine:
1. After oral administration, ciclosporine is absorbed incompletely (20%-50%) and slowly.
2. Absorbed drug is mainly metabolized by the cytochrome P450 drug metabolizing system and is associated with drug-drug interactions.
3. Both
4. Neither
Drug-drug interactions associated with cyclosporine administration is an important factor in interpatient bioavailability differences.
1. True
2. False
Ophthalmic cyclosporine solution maybe clinically useful for:
1. Dry eye syndrome (severe)
2. Ocular graft-versus-host disease (GVH) disease
3. Both
4. Neither
The primary use of cyclosporine is in preventing rejection associated with allogenic kidney, liver, and heart transplantation. Prednisone in this context is often given at the same time.
1. True
2. False
Which one(s) of the following agents inhibit transcription of IL-2 thus decreasing clonal T-helper cell clonal proliferation?
1. Tacrolimus (Envarsus)
2. Sirolimus (Rapamune)
3. Both
4. Either
Clinical use/uses for cyclosporine (FDA approved uses):
1. For treating severe plaque psoriasis
2. Treating active rheumatoid arthritis (not typically used for this indication)
3. Both
4. Neither
Cyclosporine is considered a first-line treatment for pure red cell aplasia.
1. True
2. False

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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.