Immunosuppressants

Question 1

What drug has a MoA: Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.

Answer 1

Cyclosporine

Question 2

What drug has ADR: Nephrotoxicity, hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism.

Answer 2

Cyclosporine

Question 3

What drug has a MoA: Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T-cell activation by preventing IL-2 transcription.

Answer 3

Tacrolimus (FK506)

Question 4

What drug has ADR: increased risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism.

Answer 4

Tacrolimus (FK506)

Question 5

Both calcineurin inhibitors are highly toxic to what organ?

Answer 5

kidneys

Question 6

How are Cyclosporine and Tacrolimus different from Sirolimus?

Answer 6

Sirolimus blocks T-cell activation AND B-cell differentiation by preventing RESPONSE to IL-2.
Cyclosporine/Tacrolimus block T-Cell Activation only and prevent IL-2 TRANSCRIPTION

Question 7

ADR of Sirolimus?

Answer 7

“PanSirtopenia” (pancytopenia), insulin resistance, hyperlipidemia; not nephrotoxic.

Question 8

Another name for Sirolimus?

Answer 8

Rapamycin

Question 9

What drug is synergistic with cyclosporine and also used in drug-eluting stents.

Answer 9

Sirolimus (Rapamycin)

Question 10

Daclizumab, basiliximab have what MoA?

Answer 10

Monoclonal antibodies; block IL-2R.

Question 11

Edema, hypertension, tremor are the side effects of what drug?

Answer 11

Daclizumab, basiliximab

Question 12

What drug is an antimetabolite precursor of 6-mercaptopurine.

Answer 12

Azathioprine

Question 13

Mechanism of Azathioprine

Answer 13

Inhibits lymphocyte proliferation by blocking nucleotide synthesis.

Question 14

Side effects of Azathioprine (3)

Answer 14

Leukopenia, anemia, thrombocytopenia.

Question 15

Relationship with Azathioprine and Allopurinol?

Answer 15

6-MP degraded by xanthine oxidase; toxicity increased by allopurinol.

Question 16

What drug has MOA: Reversibly inhibits IMP dehydrogenase, preventing purine synthesis of B and T cells.

Answer 16

Mycophenolate mofetil

Question 17

What drug can be used to treat lupus nephritis?

Answer 17

Mycophenolate mofetil

Question 18

What drug has the ADR: pancytopenia, hypertension, hyperglycemia.

Answer 18

Mycophenolate mofetil

Question 19

What drug is associated with invasive CMV infection?

Answer 19

Mycophenolate mofetil

Question 20

Corticosteroids inhibit what transcription factor?

Answer 20

Inhibit NF-κB.

Question 21

What drug has ADR: Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, avascular necrosis (femoral head).

Answer 21

Corticosteroids

Question 22

Cyclosporine MoA?

Answer 22

Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.

Question 23

Tacrolimus MoA?

Answer 23

Calcineurin inhibitor; binds FK506 binding protein (FKBP).

Blocks T-cell activation by preventing IL-2 transcription.

Question 24

Sirolimus (Rapamycin) MoA?

Answer 24

mTOR inhibitor; binds FKBP.

Blocks T-cell activation and B-cell differentiation by preventing response to IL-2.

Question 25

Aldesleukin (IL-2) use (2)

Answer 25

Renal cell carcinoma, metastatic melanoma

Question 26

Epoetin alfa (erythropoietin) use (1)

Answer 26

Anemias (especially in renal failure)

Question 27

Filgrastim (G-CSF) use (1)

Answer 27

Recovery of bone marrow

Question 28

Sargramostim (GM-CSF) use (1)

Answer 28

Recovery of bone marrow

Question 29

IFN-α use (3)

Answer 29

Chronic hepatitis B and C, Kaposi sarcoma, malignant melanoma

Question 30

IFN-β use (1)

Answer 30

Multiple sclerosis

Question 31

IFN-γ use (1)

Answer 31

Chronic granulomatous disease

Question 32

Romiplostim, eltrombopag (thrombopoietin receptor agonists) use (1)

Answer 32

Thrombocytopenia

Question 33

Oprelvekin (IL-11) use (1)

Answer 33

Thrombocytopenia