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Flashcards in Immuno Pharm from FA Deck (30):
1

Immunosuppressants: generally what do they do?

Consequences of chronic use?

-Block lymphocyte activation and proliferation

-Reduce acute transplant rejection by suppressing cellular immunity

-May be combined -> greated efficacy and decr toxicity.

-Chronic use increases risk of infection and malignancy

2

Cyclosporine

Mech? Use? Toxicity? Notes?

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

Use: Transplant rejection prophy, psoriasis, RA

Tox: Nephrotoxic, HTN, Hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia 

Notes: BOTH calcineurin inhibitors are highly nephrotoxic (Cyclosporine & Tacrolimus)

3

Tacrolimus

Mech? Use? Toxicity? Notes?

Mech: Calcineurin inh (binds FK506 binding protein (FKBP). Blocks T cell activation by preventing IL-2 transcription

Use: Transplant rejection prophy

Tox: Nephrotoxic, incr risk of diabetes, NO gingival hyperplasia or hirsutism (compared to Cyclosporine)

Note: "-limus" drugs bind FKBP

4

Sirolimus

Mech? Use? Toxicity? Notes?

Mech: mTOR inhibitor, binds FKBP. Blocks T cell activation and B cell differentation by preventing IL-2 signal transduction

Use: kidney transplant rejection prophy, drug-eluting stents

Tox: Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipedemia, non-nephrotoxic

Notes: Kidney "sir"vives. Synergistic with cyclosporine. 

5

Basiliximab

Mech? Use? Toxicity?

Mech: monoclonal antibody; blocks IL-2R

Use: Kidney transplant rejection prophy

Tox: Edema, HTN, tremor

6

Azathioprine

Mech? Use? Toxicity? 

What Rx should you avoid using this with?

Mech: antimetabolite precursor of 6-mercaptopurine (6-MP). Inhibits lymphocyte proliferation by blocking nucleotide synthesis.

Use: Transplant rejection prophy; RA, Crohn's; glomerulonephritis; other autoimm diseases

Tox: Leukopenia, anemia, thrombocytopenia

Notes: 6-MP degraded by xanthine oxidase; toxicity incr by allopurinol. Think "azathiopurine"

7

Glucocorticoids (aka corticosteroids)

Mech? Use? Toxicity? Notes?

Mech: inhibit NF-kB. Suppress both B and T cell function by decr transcription of many cytokines

Use: Transplant rejection prophy; many autoimm disorders; inflammation

Tox: hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, HTN, cataracts, peptic ulcers

Notes: can cause iatrogenic Cushing's

8

Clinical use for Epoetin alfa (aka erythropoietin)?

Anemias, esp in renal failure

9

Clinical use for Thrombopoietin?

Thrombocytopenia

10

Clinical use for Oprelvekin (aka IL-11)?

Thrombocytopenia

11

Clinical use for Filgrastim (granulocyte colony-stimulating factor)

Recovery of bone marrow

12

Clinical use for Sargramostim (granulocyte-macrophage colony-stimulating factor)?

Recovery of bone marrow

13

Clinical use for Aldesleukin

(IL-2)

Renal cell carcinoma; metastatic melanoma

14

Clinical use for IFN-alpha?

Chronic Hep B and C

Kaposi sarcoma

hairy cell leukemia

condyloma acuminatum

renal cell carcinoma

malignant melanoma

15

Clinical use for IFN-beta?

Multiple sclerosis

16

Clinical use for IFN-gamma?

Chronic granulomatous disease

17

Alemtuzumab

Target? Use? Notes?

Target: CD52

Use: CLL

Notes: "Alymtuzumab": chronic lymphocytic leukemia

18

Bevacizumab

Target? Use?

Target: VEGF

Use: colorectal cancer, renal cell carcinoma

19

Cetuximab

Target? Use?

Target: EGFR

Use: Stage IV colorectal cancer; head and neck cancer

20

Rituximab

Target? Use?

Target: CD20

Use: B cell non-Hodgkin lymphoma; Rheum arthritis (with MTX); ITP

21

Trastuzumab

Target? Use?

Target: Her2/neu

Use: Breast cancer, gastric cancer

Note: HER2 - tras2zumab

22

Infliximab, adalimumab

Target? Use?

Target: TNF-alpha

Use: psoriasis, ank spond, IBD, rheumatoid arth

(similar to HLA-B27 associated diseases: PAIR - Psoriatic arth, Ank spond, arthritis of IBD, Reactive arthritis) 

Note: RA "inflix" pain in "da limbs"

23

Natalizumab

Target? Use?

Target: alpha4-integrin

Use: MS, Crohn's

Note: alpha4-integrin: leukocyte adhesion.

Risk of PML in patients with JC virus

24

Abciximab

Target? Use?

Target: Glycoprotein IIb/IIIA

Use: Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention

IIb x IIIa = absiximab

25

Denosumab

Target? Use?

Target: RANKL

Use: Osteoporosis; inhibits osteoclast maturation (mimics osteoprotegrin)

Denosumab affects osteoclasts

26

Digoxin immune Fab

Target? Use?

Target: Digoxin

Use: Antidote for digoxin toxicity

27

Omalizumab

Target? Use?

Target: IgE

Use: Allergic asthma; prevents IgE binding to FceRI

28

Palivizumab

Target? Use?

Target: RSV F protein

Use: RSV prophy for high risk infants

PaliVIzumab = VIrus

29

muromab

MoA

ADR

mAb binds CD3 that blocks T cell signaling

cytokine release storm

30

mycophenolate mofetil

MoA

ADR

blocks guanine nucleotide synthesis, thereby inhibiting lymphocyte proliferation

ADR: myelosuppression, Dramatic diarrhea