Immunopharmacology Flashcards Preview

POD Exam II > Immunopharmacology > Flashcards

Flashcards in Immunopharmacology Deck (23):
1

Cyclosporine:

- Calcineurin inhibitor.
- Binds to cyclophilin.
- Inhibits dephosphorylation of NFAT, synthesis of IL-2.
- Selective for T cells.
- Uses: prevent rejection, autoimmune disorders.
- Tox: *nephrotoxicity*, HTN, hepatotoxicity.

2

Tacrolimus:

- Calcineurin inhibitor.
- MOA: binds FKBP. Inhibits dephosphorylation of NFAT, synthesis of IL-2.
- Selective for T cells.
- Uses: prevent rejection, autoimmune disorders.
- Tox: *nephrotoxicity*, neurotoxicity, HTN, DM.

3

Sirolimus/Everolimus:

- MOA: binds to FKBP. Inhibits mTOR.
- Blocks T cell at the G1-->S transition, blocks T cell expansion.
- Use: stents used to inhibit restenosis of blood vessels, prevent rejection, autoimmune disorders.
- Tox: *hyperlipidemia*, delay in graft function and delayed wound healing, anemia, leukopenia, thrombocytopenia.

4

Azathioprine:

- Prodrug --> 6-MP.
- MOA: block the de novo pathway of purine synthesis.
- Uses: adjunct for prevention of rejection, RA.
- DI: if allopurinol is given then azathioprine dose reduced.
- Tox: bone marrow suppression, leukopenia, anemia, thrombocytopenia, increased risk of infection.

5

Mycophenolate mofetil:

- Prodrug --> MPA
- MOA: reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). Inhibits de novo synthesis of guanine.
- Use: prevent transplant rejection.
- DI: antacids decrease absorption.
- Tox: GI effects, leukopenia.

6

Antithymocyte globulin (ATGAM):

- Polyclonal antibody from serum of horses or rabbits.
- MOA: binds to circulating T cells which induces lymphopenia and decreases T cell function.
- Use: prevent rejection.
- Tox: serum sickness, nephritis, chills, fever and rashes.

7

Muromonab-CD3

- Mouse monoclonal antibody against CD3.
- MOA: induces internalization of the TCR complex.
- Use: prevent rejection.
- Tox: cytokine release syndrome, anaphylactic reactions, CNS tox, increased risk for infections and malignancy.

8

Daclizumab/basiliximab:

- MOA: bind the alpha subunit of IL-2R on T cells; inhibits T cell proliferation.
Use: D - relapsing MS. B - prevent rejection.

9

Alemtuzumab:

- Humanized anti-CD52 antibody.
- MOA: induces cytolysis upon binding CD 52 on the surface of B and T cells, monocytes, macrophages and NK cells.
- Use: relapsing remitting MS, chronic lymphoid leukemia.
- Tox: depletion of normal neutrophils and T cells, serious myelosuppression.

10

Tocilizumab:

- Humanized anti-IL-6 antibody.
- MOA: neutralizes IL-6, suppresses inflammation.
- Use: RA, juvenile RA.

11

Rituximab:

- Chimeric anti-CD20 antibody.
- MOA: induces B cell apoptosis by binding to CD20 on malignant B cells.
- Use: chronic lymphoid leukemia, non-Hodgkin's lymphoma and RA.

12

Infliximab:

- Chimeric anti-TNFalpha antibody.
- MOA: bind to and neutralize TNFalpha.
- Use: RA, psoriasis, ulcerative colitis, Crohn's disease.
- Tox: increased risk for infection, lymphomas and other cancers.

13

Certolizumab:

- Humanized PEGylated anti-TNFalpha antibody.
- MOA: bind to and neutralize TNFalpha.
- Use: RA, psoriasis, ulcerative colitis, Crohn's disease.
- Tox: increased risk for infection, lymphomas and other cancers.

14

Adalimumab:

- Human anti-TNFalpha antibody.
- MOA: bind to and neutralize TNFalpha.
- Use: RA, psoriasis, ulcerative colitis, Crohn's disease.
- Tox: increased risk for infection, lymphomas and other cancers.

15

Etanercept:

- Decoy TNFalpha receptor.
- MOA: bind to and neutralize TNFalpha.
- Use: RA, psoriasis, ulcerative colitis, Crohn's disease.
- Tox: increased risk for infection, lymphomas and other cancers.

16

Golimumab:

- Human anti-TNFalpha antibody.
- MOA: bind to and neutralize TNFalpha.
- Use: RA, psoriasis, ulcerative colitis, Crohn's disease.
- Tox: increased risk for infection, lymphomas and other cancers.

17

Abatacept/Belatacept:

- Fusion proteins CTLA-4 IgG1.
- Belatacept more potent.
- MOA: binds CD80/86 on APCs and prevents their binding with CD28 on T cells, inhibiting co-stimulation.
- Uses: A - juvenile arthritis, RA. B - prevent rejection.

18

Immune globulins:

- From pooled human plasma.
- Provide passive immunity.
- Use: immunodeficiency states, to prevent measles, hep-A and tetanus.

19

Bacillus Calmette-Guerin (BCG) vaccine:

- Viable attenuated strain of mycobacterium bovis.
- Muramyl dipeptide is active component.
- Stimulates NK cells and T cell activity.
- Use: bladder cancer.
- Tox: severe hypersensitivity reactions and shock.

20

Levamisole:

- Inhibits T-suppressor cells.
- Use: anthelminic agent, immunostimulant in colon ca.

21

INF-alpha:

- MOA: activates macrophages, T cells and NK cells.
- Use: cancers and Hep B/C
- Human recombinant INF-alpha used.
- Tox: flue like symptoms, pulmonary hypertension.

22

IL-2:

- MOA: activates cellular immunity.
- Use: metastatic melanoma, renal cell carcinoma and AIDS.
- Tox: severe hypotension, cardiovascular tox.
- Pulmonary edema is dose limiting.
- Natural or recombinant forms.

23

G-CSFs:

- Produced by monocytes, fibroblasts and endothelial cells.
- Stimulate increases in granulocytes and monocytes.
- Use: reduce neutropenia.