Immunosuppression Flashcards Preview

Pharmacology > Immunosuppression > Flashcards

Flashcards in Immunosuppression Deck (12)
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1
Q

Prednisone (oral), Methylprednisolone (Solu-Medrol®; IV)

A

Glucocorticoid receptor agonists; inhibit synthesis of prostaglandins and leukotrienes, reduce expression of NF-κB, suppress inflammatory cytokine production, kill proliferating immune cells

Use: Organ transplantation, organ transplant rejection, autoimmune disease, chronic inflammatory disease

2
Q

Azathioprine (Imuran®)

A

After conversion to 6-mercaptopurine in the liver inhibits purine synthesis, blocks Rac1 activation

Use: Organ transplantation, autoimmune disease

3
Q

Methotrexate

A

Inhibits dihydrofolate reductase (high dose), inhibits AICAR transformylase thus increasing adenosine release (low dose)

Use: Rheumatoid arthritis (low dose), other autoimmune disease (low dose), cancer chemotherapy (high dose)

4
Q

Cyclophosphamide (Cytoxan®)

A

Alkylates guanine in DNA forming intrastrand and interstrand DNA crosslinks

Use: Acute crisis in autoimmune disease; cancer chemotherapy*

5
Q

Leflunomide

A

Inhibits dihydroorotate dehydrogenase thus inhibiting pyrimidine synthesis

Use: Rheumatoid arthritis*, other autoimmune disease

6
Q

Infliximab (Remicade®)

A

Monoclonal antibody directed against TNFα

Use: Rheumatoid arthritis, IBD, other autoimmune disease

7
Q

Rituximab

A

Monoclonal antibody directed against CD20 on B cells; kills B cells not long-lived plasma cells

Use: Autoimmune disease; cancer chemotherapy (B cell lymphomas)

8
Q

Abatacept (Orencia®)

A

Extracellular domain of CTLA4 fused to antibody constant regions; prevents B7 on APC from binding to CD28 on T cell (so no costimulation)

Use: Rheumatoid arthritis

9
Q

Cyclosporine

A

Binds to cyclophilin, complex inhibits calcineurin thus blocking T cell activation

Use: Organ transplantation

10
Q

Tacrolimus (FK506)

A

Binds to FKBP12, complex inhibits calcineurin thus blocking T cell activation

Use: Organ transplantation

11
Q

Sirolimus (rapamycin)

A

Binds to FKBP12, complex inhibits mTOR signalling thus blocking T cell activation

Use: Organ transplantation

12
Q

Mycophenolate mofetil (Cellcept®)

A

Inhibits IMP dehydrogenase thus inhibiting purine synthesis

Use: Organ transplantation, autoimmune disease