Immunosuppressants

Question 1

Sirolimus is synergistic with ___ and is also used in ___.

Answer 1

Cyclosporine

Drug-eluting stents

Question 2

Mechanism: Epoetin alfa

Answer 2

Recombinant EPO

Question 3

Other uses: Corticosteroids

Answer 3

Many autoimmune and inflammatory disorders

Adrenal insufficiency

Asthma

CLL

Non-hodgkin lymphoma

Question 4

Toxicity: Mycophenolate mofetil

Answer 4

GI upset

Pancytopenia

Hypertension

Hyperglycemia

Less nephrotoxic and neurotoxic

Question 5

Clinical use: IFN-beta

Answer 5

Multiple sclerosis

Question 6

6-MP (azathioprine) degraded by ___; increased toxicity by ___

Answer 6

Xanthine oxidase

Allopurinol and febuxostat

Question 7

Mechanism: Mycophenolate mofetil

Answer 7

Reversibly inhibits IMP dehydrogenase → inhibiting purine synthesis of B and T cells

Question 8

Other use: Cyclosporine

Answer 8

Psoriasis

RA

Question 9

Clinical use: Oprelvekin

Answer 9

Thrombocytopenia

Question 10

Clinical use: IFN-gamma

Answer 10

Chronic granulomatous disease

Question 11

Clinical use: Aldesleukin

Answer 11

Renal cell carcinoma

Metastatic melanoma

Question 12

Mechanism: Sirolimus (rapamycin)

Answer 12

Binds FKBP → inhibits mTOR

Blocks T-cell activation and B-cell differentiation by preventing response to IL-2 (blocks G1→S)

Question 13

Toxicity: Azathioprine

Answer 13

Myelosuppression → pancytopenia

Hepatotoxicity

GI distress

Question 14

Other uses: Basiliximab

Answer 14

Kidney transplant rejection prophylaxis specifically

Question 15

Mechanism: Azathioprine

Answer 15

Purine (thiol) analog → decreases de novo purine synthesis

Activated by HGPRT

Metabolized into 6-MP

Question 16

Mechanism: Eltrombopag

Answer 16

Thrombopoetin receptor agonist

Question 17

Toxicity: Corticosteroids

Answer 17

Cushing syndrome-like effects:

Osteoporosis

Hyperglycemia

Diabetes

Amenorrhea

Adrenocortical atrophy

Peptic ulcers

Psychosis

Cataracts

Avascular necrosis (femoral head)

Question 18

Mechanism: Sargramostim

Answer 18

Recombinant GM-CSF

Question 19

Mechanism: Oprelvekin

Answer 19

Recombinant IL-11

Question 20

Clinical use: Romiplostim

Answer 20

Thrombocytopenia

Question 21

Clinical use: IFN-alpha

Answer 21

Chronic hepatitis B and C

Kaposia sarcoma

Malignant melanoma

Hairy cell leukemia

Condyloma acuminata

Renal cell carcinoma

Question 22

Mechanism: Basiliximab

Answer 22

Monoclonal antibody → blocks IL-2R

Question 23

Clinical use: Epoetin alfa

Answer 23

Anemias (especially in renal failure)

Question 24

Mechanism: Tacrolimus

Answer 24

Binds FK506 binding protein (FKBP) → inhibits calcineurin

Blocks T-cell activation by preventing IL-2 transcription

Question 25

Mechanism: Cyclosporine

Answer 25

Binds cyclophilin → inhibits **calcineurin** Blocks T-cell activation by **preventing IL-2 transcription**

Question 26

Clinical use: Filgrastim

Answer 26

Recovery of BM and WBC counts by granulocyte stimulation

Question 27

Clinical use: Eltrombopag

Answer 27

Thrombocytopenia

Question 28

Mechanism: Corticosteroids

Answer 28

Inhibit NF-kB Suppress both B- and T-cell function by decreasing transcription of many cytokines Induce T-cell apoptosis

Question 29

Toxicity: Basiliximab

Answer 29

Edema Hypertension Tremor

Question 30

Toxicity: Sirolimus

Answer 30

Pancytopenia Insulin resistance Hyperlipidemia **NOT** nephrotoxic

Question 31

Use of ___ causes demargination of WBCs, which causes artificial leukocytosis. ___ may develop if drug is stopped abruptly after chronic use.

Answer 31

Corticosteroids Adrenal insufficiency

Question 32

Mechanism: Aldesleukin

Answer 32

Recombinant **IL-2**

Question 33

Mechanism: Romiplostim

Answer 33

Thrombopoetin analog

Question 34

Toxicity: Tacrolimus

Answer 34

**Similar to cyclosporine, but with increased risk for:** Diabetes (hyperglycemia) Neurotoxicity **NO:** Gingival hyperplasia Hirsutism

Question 35

Other use: Sirolimus

Answer 35

**Kidney transplant rejection prophylaxis** specifically

Question 36

Other uses: Azathioprine

Answer 36

RA Crohn disease Glomerulonephritis Other autoimmune conditions

Question 37

Toxicity: Cyclosporine

Answer 37

**Nephrotoxicity** **Gingival hyperplasia** **Hirsutism** Hypertension Hyperlipidemia Neurotoxicity

Question 38

Mycophenolate mofetil is associated with \_\_\_

Answer 38

Invasive CMV infection

Question 39

Other uses: Mycophenolate mofetil

Answer 39

Lupus nephritis

Question 40

Mechanism: Filgrastim

Answer 40

Recombinant **G-CSF**