Immunopharmacology Flashcards
primary or secondary immune response which one is more easily and effectively affected
primary
when does immunosuppressive therapies work the best
used before rather then after exposure
name 3 clinical uses for immosupressive drugs
organ transplantation
Selective immunosuppression - Rh
autoimmune disease
name 2 limitations to therapy
- increase risk of infection
- increase risk of lymphomas and related cancers
Cyclosporine inhibits what
Calcineurin
MOA for Cyclosproine
- binds cyclophilin A in T cells
- complex binds to calcineurin
- inhibits synthesis of cytokines (IL2), protooncogenes, and cytokine receptors (IL-2R)
- Increase production of transforming growth factor B-(TGF-B)
Cyclosporine is selective for what lymphocyte
T lymphocytes
what is cyclosporine used for
- prevention and treatment of organ rejection
- autoimmune disorders
what is the toxicity for Cyclosporin
nephrotoxicity
hypertension
Tacrolimus (FK506) inhibits what
Calcineurin
MOA of Tacrolimus
binds FK506 binding protein-12 (FKBP)
-inhibits calcinerurin and calcineurin mediated events
difference between Tacrolimus and Cyclosporine
tacrolimus more potent
what is the toxicity for Tacrolimus
Nephrotoxicity
neurotoxicity
hypertension
diabetes
Sirolimus and Everolimus MOA
binds to FKBP
- does not inhibit calcineurin
- inhibits mTor
what is the role of mTor
kinase for T cell proliferation
Where does Sirolimus/Everolimus block the T cell cycle
G1 to S phase
Toxicities for Sirolimus and Everolimus
Not nephrotoxic
increase cholesterol and triglycerides in serum
Glucocorticoid MOA
unclear, inhibit T-cell proliferation, T-dependent immunity, and expression of genes encoding cytokines
what is the use for Glucocorticoid
prevent organ rejection
autoimmune disease
What are the cytotoxic drugs
Azathioprine
Mycophenolate mofeitl
What is the MOA for Azathioprine
6-MP metabolites inhibit purine biosynthesis, then inhibits DNA synthesis, inhibits T cell proliferation
What is Azathioprine used for
prevention of organ transplant rejection
what is the drug interaction for Azathioprine
Allopurinol is given, then reduce Azathioprine
- Allopurinol inhibits Xanthine oxidase
- Xanthine oxidase catabolizes Azathioprine metabolites
what is the toxicity for Azathioprine
bone marrow supression
leukopenia
thrombocytopenia
anemia
Mycophenolate mofetil MOA
prodrug converted to MPA
role of MPA
reversible inhibitor of IMPDH
-inhibits guanine nucleotide synthesis
What is Mycophenolate mofetil used for
prophylaxis of transplant reject
What is Mycophenolate Mofetil toxicity
GI effects
leukopenia
What should you not take Mycopheonolate mofetil with
antacids
Antithymocyte globulin (ATGAM) MOA
binds to circulating T lymphocytes which induces lymphonpenia and decreases T-cell function