Immunopharmacology Drugs Flashcards
Why is prednisone tapered off slowly?
Prednisone downregulates the HPA axis and sudden withdrawl from treatment causes adrenal insufficiency that can be fatal.
Name a drug that is an irreversible COX inhibitor. What is the significance of this?
Aspirin - works in platelets where there is little ability to make new cyclooxygenase enzyme
Ibuprofen
Non-specific COX inhibitor
SAEs: Nephrotoxicity, GI toxicity
Methotrexate
- Enzyme inhibition –> increased extracellular adenosine –> adenosine receptor activation –> cAMP –> PKA –> anti-inflammatory
- DHF reductase inhibitor (involved in thymidine biosynthesis)
SAE: Bone marrow depression
Prednisone
Prodrug; converted to prednisolone –> binds to glucocorticoid receptor –> changes gene expression to downregulate leukotriene and prostaglandin synthesis and inhibits leukocyte function and trafficking.
Also blocks NFkB to decrease cytokine production.
SAEs from chronic use: osteoporosis, muscle wasting, diabetes, adrenal suppression
Etanercept
Decoy receptor for TNF. Interception!
SAEs: injection site reactions, watch out for TB!
Anakinra
IL-1 receptor antagonist
SAE: increased infection risk
Aspirin
Non-specific COX inhibitor (irreversible)
SAEs: GI ulceration/bleeding, nephrotoxicity (rare)
Cyclosporine
Inhibits calcineurin (so no NFAT upregulation of IL-2 and IL-2R gene products)
SAEs: nephrotoxicity, neurotoxicity, hypertension
Mycophenolate mofetil
Inhibits IMP DH and GTP synthesis
SAE is bone marrow depression
Rituximab
Binds to CD20 on mature B cells –> lysis
SAEs are neutropenia and anemia
Sirolimus
Binds FKBP-12 and inhibits mTOR –> no T cell proliferation
SAEs are high cholesterol and triglycerides, bone marrow suppression, hepatotoxicity
Inhibits IMP DH and GTP synthesis
Mycophenolate mofetil
IL-1 receptor antagonist
Anakinra
Decoy receptor for TNF.
Etanercept
