Immunopharmacology Flashcards
1
Q
Cyclosporine:
A
- 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
Q
Tacrolimus:
A
- 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
Q
Sirolimus/Everolimus:
A
- 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
Q
Azathioprine:
A
- 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
Q
Mycophenolate mofetil:
A
- 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
Q
Antithymocyte globulin (ATGAM):
A
- 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
Q
Muromonab-CD3
A
- 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
Q
Daclizumab/basiliximab:
A
- MOA: bind the alpha subunit of IL-2R on T cells; inhibits T cell proliferation.
Use: D - relapsing MS. B - prevent rejection.
9
Q
Alemtuzumab:
A
- 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
Q
Tocilizumab:
A
- Humanized anti-IL-6 antibody.
- MOA: neutralizes IL-6, suppresses inflammation.
- Use: RA, juvenile RA.
11
Q
Rituximab:
A
- 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
Q
Infliximab:
A
- 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
Q
Certolizumab:
A
- 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
Q
Adalimumab:
A
- 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
Q
Etanercept:
A
- 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
Q
Golimumab:
A
- 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
Q
Abatacept/Belatacept:
A
- 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
Q
Immune globulins:
A
- From pooled human plasma.
- Provide passive immunity.
- Use: immunodeficiency states, to prevent measles, hep-A and tetanus.
19
Q
Bacillus Calmette-Guerin (BCG) vaccine:
A
- 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
Q
Levamisole:
A
- Inhibits T-suppressor cells.
- Use: anthelminic agent, immunostimulant in colon ca.
21
Q
INF-alpha:
A
- 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
Q
IL-2:
A
- 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
Q
G-CSFs:
A
- Produced by monocytes, fibroblasts and endothelial cells.
- Stimulate increases in granulocytes and monocytes.
- Use: reduce neutropenia.