Flashcards in Regal- Anti-inflammatory Steroids and Immunosuppressives Deck (34)
What drugs are anti-inflammatory steroids (glucocorticoids)?
What is the MOA of glucocorticoids?
Block steroid receptors that normally stimulate pathways that increase transcription of pro-inflammatory cytokines
• decrease COX2 expression (preferentially over COX 1)
•Inhibit AA release from phospholipids, affecting PG & LT formation
•Inhibit mast cell & basophil degranulation
•Inhibit synthesis & release of TNF (cachectin), IL-1, IL-2 & IFN → less immune cells circulating/functioning
How are glucocorticoids eliminated?
What toxicities are associated w/ glucocorticoids?
systemic therapy--> increased susceptibility to infections and OSTEOPOROSIS
What glucocorticoid has a short t 1/2?
What glucocorticoids have intermediate t 1/2?
What glucocorticoids have long t 1/2?
What SE are associated w/ glucocorticoids?
•Inhibition of growth
Discontinuation of long term use → adrenal insufficiency (fever, myalgia, arthralgia, malaise, death d/t hypotension & shock)
What glucocorticoid is good for tx ITP, AHA, acute glomulonephritis, autoimmune disease ?
What glucocorticoids have the best anti-inflammatory properties?
What drugs are the three categories of immunosuppressive drugs?
What drugs are calcineurin inhibitors?
What is the MOA of cyclosporine?
Binds cyclphillin to inhibit calcineuran phosphatase activity>
blocks cytokine gene expression and T cell activation
How is cyclosporine eliminated?
Extensive liver metabolism
What are the SE associated w/ cyclosporine?
nephrotoxicity (75% of pts)
What is the MOA of tacrolimus?
Binds FKBP to inhibit mTOR >
blocks cell cycle progression
What SE are assoicated w/ tacrolimus?
What drugs are anti-proliferative?
What is the MOA of siroliums?
Binds to FKBP to inhibit mTOR → blocks cell-cycle progression
What are the SE of sirolimus?
Dose dependent increase in cholesterol and triglycerides
Nephrotoxicity w/ cyclosporine
CYP34A drug intrxns
What drug is used in combination therapy for organ transplant rejection?
What is the MOA of mycophenolate?
Inhibits IMPDH in de novo guanine nucleotide synth pathway → blocks B & T cell proliferation preferentially
What are the SE of mycophenolate?
Hematological : leukopenia
GI: diarrhea, vomiting
When is mycophenolate used?
What drugs are Abs?
What is the MOA of ANti-thymocyte globulin?
Binds thymocytes in the circulation → lymphopenia & impaired T cell immune responses
What are the SE of anti-thymocyte globulin?
What is the MOA of muromonab CD-3?
Binds ε chain of CD3 of T-cells → TCR is internalized → prevents Ag recognition
What are the SE of muromonab CD-3?
Cytokine release syndrome: mild flu like illness to life-threatening shock
*Reduced w/ glucocorticoid admin 1st