B / 27 : Immunopharmacology II - inhibitors of cytokine gene expression, 5-ASA derivatives Flashcards
1
Q
What are inhibitors of cytokine gene expression mainly used for?
A
Primarily for graft rejection and some autoimmune disorders
2
Q
What is calcineurin?
A
Ca and calmodulin dependant phosphatase : plays a role in activation of T cells
3
Q
What are the 2 calcineurin inhibitors?
A
- Cyclosporin A
- Tacrolimus
4
Q
Cyclosporin A
- MOA
- Effect
- Indication
- SE
- ROA
A
- Calcineurin inhibitor
- Binds to cyclophilin to form a complex that inhibits calcineurin inside the cell : inhibit gene production and decrease T cell transcription factors
- For BM transplantation, GVH disease, RA
- Nephrotoxic, hepatotoxic, hypertension
- Oral, parenteral
5
Q
Tacrolimus
- MOA
- Effect
- Indication
- SE
- ROA
A
- Calcineurin inhibitor
- Binds to FK-binding protein to inhibits calcineurin : inhibits gene prod
- For solid organ transplant and autoimmune diseases
- Nephrotoxic, hepatotoxic, hypertension
- Oral, parenteral
6
Q
What is mTOR?
A
A regulator of IC signaling pathway involved in cell growth and proliferation
7
Q
What is an example of an mTOR inhibitor?
A
Sirolimus
8
Q
Sirolimus
- MOA
- Effect
- Indication
- SE
- ROA
A
- Macrolide antibiotic
- Inhibits kinase activity of mTOR : inhibition of T cell proliferation
- For kidney, breast and endocrine cancers + solid organ transplantation
- BM suppression, hepatotoxicity
- Oral, parenteral
9
Q
Tofacitinib
- MOA
- Effect
- Indication
- SE
- ROA
A
- Inhibitor of JAK-1 and JAK-3
- blocks the IL-2 mediated pathways in T cells
- For RA
- Infections, hyperlipidemia, liver enzyme elevation
- Oral
10
Q
What is an example of a 5-ASA derivative?
A
Sulfasalazine
11
Q
Sulfasalazine
- MOA
- Effect
- Indication
- SE
- ROA
A
- Uncertain mechanism
- Cleaved to 5-ASA in the colon
- For RA, IBD
- Nausea, vomiting, headache
- Oral, topical
