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Terms in this set (45)
useful for reducing inflammation & pain but they cannot reverse pathological process
not used in osteoarthritis
What is usually elevated in RA?
rheumatoid factor & ACPA
Macrophages and lymphocytes secrete
cytokines (IL-1 & TNF)
What are the targets of DMARDs?
Why are DMARDs more effective if used early on?
most joint damage occurs early in disease
very commonly used agent for treatment of RA that inhibits dihydrofolate reductase & interferes with de novo purine biosynthesis
Methotrexate is used additionally for
leukemia & psoriasis
When do the effects of methotrexate become apparent?
What is often co-administered with methotrexate?
antimalarial agent, second line for mild RA, slow onset
Side effects of hydroxychloroquine
nausea & gastric pain, hemolysis with g6p deficiency, retinal damage
prodrug (5ASA) used to treat RA, mild to moderate ulcerative colitis, & Crohn's disease
Which drugs are used in triple therapy for RA?
methotrexate, hydroxychloroquine, & sulfalazine
oral pyrimidine synthesis inhibitor, effective in slowing progression of RA
What are the side effects of Leflunomide?
hepatic toxicity & liver failure, myelosuppression, teratogenic
The major target of the biologics at the moment
refers to fusion of a receptor to the Fc part of human immunoglobulin G1
indicates a monoclonal antibody
indicates a chimeric mAb
indicates a humanized mAb
indicates a fully human mAb
activates many kinases and nuclear signaling pathways
What is the therapeutic goal of TNF inhibitors?
reduce circulating levels of TNF-alpha
What is the main side effect of TNF inhibitors?
increased risk of infections
Which TNF inhibitor is a monoclonal antibody?
Which TNF inhibitor is a receptor analog?
fusion protein containing. the ligand-binding portion of the human TNF receptor linked to human IgG1, false receptor
may be used in combination with methotrexate, NSAIDs, or other agents
inhibits interaction of TNF with its receptors, used in RA, Crohn's disease, ankylosing spondylitis, psoriatic arthritis, and psoriasis, admin via IV, chimeric IgG1 monoclonal antibody, high affinity binding to TNF-alpha, highly stable complexes
Human monoclonal TNF-alpha antibody with human IgG, identical mechanism of action as Remicade (clears soluble & membrane bound TNF-alpha)
Remicade is prescribed for
ulcerative colitis only
What cannot be used to treat Chrohn's disease & ulcerative colitis?
TNF human monoclonal antibody, used in adults with moderate to severe RA, psoriatic arthritis, & ankylosing spondylitis, monthly SQ injections
TNF antibody conjugated to polyethylene glycol, monthly SQ injections
Considering the relative cost of drugs used in RA, what is the most affordable option?
methotrexate or triple therapy (as compared to biologics)
one amino acid difference from IL-1, blocks IL-1 by competitive inhibition (antagonist)
indicated for moderate to severe RA in pt who have failed 1 or more DMARDs, not used with TNF blocking agents, daily SQ injection
What is the most common side effect of Anakinra?
injection site reaction & increased risk of infection
What is effective in the treatment of RA?
pt not responsive to TNF inhibitor, T-cell costimulatory blocker, CTLA4 binds CD80 on APC & prevents interaction with CD28 on T cell which diminishes inflammatory response
pr who have failed to respond to TNF inhibitor, depletes B cells, chimeric monoclonal, Ab against CD20 on B cell surface
monoclonal antibody against IL-6 receptor, combination with methotrexate, infusion
small molecular inhibitor JAK (janus kinase), coadmin with methotrexate, also used in cancer
anti-inflammatory & immunosuppressive drugs, decrease circulating WBCs, inhibit cytokine production & TNF-alpha, provide relief until other, slower acting anti rheumatic drugs such as methotrexate take effect
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