Immunosuppressive Drugs Pha 430
- 1.Which statement is incorrect regarding cyclosporine?
- A.
It is lipophilic
- B.
It binds to cyclophilins in the cytoplasm to form a complex
- C.
It inhibits IL-2 synthesis as well as secretion
- D.
The attenuation of IL-2 is achieved through decreased expression of transforming growth factor beta
- 2.The cyclosporine-cyclophilin complex serves as an inhibitor on what component in the cytoplasm:
- A.
Calcineurin
- B.
Neuricalcin
- C.
MTOR
- D.
None of the above
- 3.Phosphorylated NF-ATc binding with NF-ATn is what normally stimulates the release of IL-2
- A.
True
- B.
False
- 4.Which statement is the most correct regarding cyclosporine and cellular effects?
- A.
Causes lymphocyte death / does not cause apoptosis
- B.
Does not cause lymphocyte death / does not cause apoptosis
- C.
Causes lymphocyte death / causes apoptosis
- D.
Does not cause lymphocyte death / causes apoptosis
- 5.To prevent hemolytic disease of the newborn in Rh- mothers with Rh+ fetuses, RhoGAM needs to be administered when?
- A.
Within 72 hours before birth of the first child
- B.
Within 72 hours of birth of the first child
- C.
Within 72 hours of birth of every child after the first
- D.
Within 72 hours of birth of every child including the first
- 6.Cyclosporine is poorly orally bioavailable, with an oral F of 20-50%.
- A.
True
- B.
False
- 7.Cyclosporine metabolism primarily takes place how?
- A.
Renally
- B.
Hepatically
- C.
Fecally
- D.
Unknown
- 8.Which of these are toxicities associated with cyclosporine? [Select all that apply]
- A.
Nephrotoxicity
- B.
Hypertension
- C.
Neurological effects
- D.
Substantially decreased liver enzymes
- E.
Alopecia
- F.
Gingival hyperplasia
- 9.Cyclosporine is used for heart, kidney, and lung transplants, as well as GVHD, but not autoimmune disorders
- A.
True
- B.
False
- 10.Tacrolimus is a macrolide antibiotic
- A.
True
- B.
False
- 11.Tacrolimus is roughly 50-100x more potent than cyclosporine
- A.
True
- B.
False
- 12.The MOA of tacrolimus is identical to cyclosporine, with no deviations
- A.
True
- B.
False
- 13.What step of the MOA of tacrolimus is different from cyclosporine?
- A.
Ca2+ influx does not occur
- B.
Substrate complex; does not inhibit calcineurin
- C.
Substrate Complex; Tac binds and forms Tac-FK06 complex
- D.
NFATc/NFATn complex does not form
- 14.Tacrolimus is less orally bioavailable than cyclosporine
- A.
True
- B.
False
- 15.Nephrotoxicity associated with tac is equal to or worse than cyclosporine
- A.
True
- B.
False
- 16.Rarely, tacrolimus is associated with:
- A.
B-cell cancers
- B.
T-cell cancers
- C.
Both B- and T-cell cancers
- D.
None of the above
- 17.Rapamycin is similar to tacrolimus in that it is a macrolide, binds to FK in the cytoplasm, and inhibits calcineurin activation
- A.
True
- B.
False
- 18.The inhibition of mTOR by rapamycin has which downstream effect? Pick the most correct statement
- A.
Cell does not proceed to G2 phase of cell cycle
- B.
Cell does not proceed to S phase of cell cycle
- C.
Cell does not enter G1 phase of cell cycle
- D.
Cell undergoes spontaneous apoptosis unrelated to cell cycle
- 19.Rapamycin inhibits IL-2 receptor dependent cell cycling
- A.
True
- B.
False
- 20.Because rapamycin is associated with _____________, it should be started _________ a transplant
- A.
Impaired wound healing; after
- B.
Accelerated wound repair; before
- C.
Impaired wound healing; either before or after
- D.
None of the above - contraindicated in transplant surgeries
- 21.Select the correct statement(s) regarding rapamycin:
- A.
May be used with cyclosporine
- B.
Is not used in B-cell lymphoma
- C.
DDIs are similar to cyclosporine
- D.
Does not have a significant nephrotoxicity risk
- 22.Everolimus is similar to rapamycin except that it is used after tissue transplantation for the prevention of graft rejection
- A.
True
- B.
False
- 23.Everolimus is indicated for which of the following according to Dr. Khan's slides? Select all that apply
- A.
Cardiac allograft vasculopathy
- B.
Cardiac autograft vasculopathy
- C.
Post-transplant lymphosuppressive disorders
- D.
Post-transplant lymphoproliferative disorders
- E.
Breast cancers
- F.
Treatment of heart failure
- G.
Treatment of MS
- H.
Treatment of Parkinson's Disease
- 24.Fingolimod is a prodrug requiring dephosphorylation to work properly
- A.
True
- B.
False
- 25.Which is the most correct statement regarding the MOA of fingolimod
- A.
Increases peripheral blood lymphocyte count
- B.
Cells are hypersensitized to the presence of sphingosine-1 phosphate and respond overtly to its signal
- C.
It is associated with little to no adverse events
- D.
An internalization of G-protein linked receptors on thymocytes/lymphocytes
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