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Drugs for Arthritic Disease
Dr. Turnbull - October 13, 2011 Semester 3, Mini 2
What are the drugs acting against circulating proinflammatory cytokines?
Etanercept, and Anakinra
What is infliximab and how does it work?
human/mouse chimeric monoclonal IgG1 Ab, w/ human Fc and murine variable regions that bind soluble and transmembrane TNF-α
What are the uses of infliximab?
, Ankylosing spondylitis, Psoratic arthritis, Crohn's Dis, Ulcerative colitis, IBD
What is usually used in combination w/ infliximab?
Why might a serious infection, like TB, occur as a result of infliximab administration?
↓ macrophage function
What are some common side effects of infliximab?
headache, fatique, abdominal pain, infusion reaction, upper respiratory/UTIs
What is a possible adverse effect when taking infliximab in combination w/ azathioprine?
What is the difference b/w infliximab and adalimumab structure?
Adalimumab is fully humanized monoclonal IgG1 ab
(no murine component)
What are the uses of adalimumab?
Psoriasis with arthropathy
How does adalimumab work?
Fully human ab that blocks the interaction of TNF-α with TNF receptors on cell surfaces.
Also: ↓ C reactive protein, ↓ ESR, ↓ IL-6, ↓ MMP-1 & MMP-3.
How might you have to adjust the dose of adalimumab after adding methotrexate to the drug regiment?
(methotrexate ↑ t½)
What is the black box warning for adalimumab?
At risk for TB, invasive fungal infections, and other opportunistic infections.
Adverse effects: exacerbates chronic CHF, serious infections, lupus-like syndrome.
How is adalimumab administered?
SQ every 14 days
What is the structure of Etanercept?
soluble, recombinant fully human TNF receptor fusion protein receptor
(extracellular domain of the TNF-α receptor coupled to human IgG1)
How does etanercept work?
It inhibits the binding of TNF-α and TNF-β to their
receptors, thus ↓ inflammation due to TNF-α.
What is etanercept used for?
moderate to severe RA
What drug against proinflammatory cytokines is C/I in pts w/ MS?
What is the structure of Anakinra?
recombinant form of Human IL-1 receptor antagonist
What is the main use of anakinra?
What is a serious adverse effect of anakinra?
infection, ↓ WBCs
What are the miscellaneous DMARDs?
Sulfonamide plus salicylate (sulfasalazine)
What patients are given miscellaneous DMARDs?
patients w/ serious GIT problems w/ NSAIDS and steroids
patients whose joints are deteriorating rapidly
What are some ways you evaluate the efficacy of a miscellaneous DMARD?
articular index (size of joint)
measure acute phase proteins
test joint movement
What is the MoA of penicillamine?
Penicillamine is rarely used in the tx of RA now, what is its main use?
How is penicillamine administered?
What are some major adverse effects of penicillamine?
Blood dyscrasias-bone marrow suppression which may be fatal
If a patient on penicillamine develops proteinuria, what is the best next step?
(unwise to substitute this DMARD w/ another)
What are the second line drugs used in the tx of RA?
What is chloroquines used for other than RA?
How does chloroquines work?
Suppresses the responsiveness of T- lymphocytes to mitogens
Decreases leukocyte chemotaxis
Stabilizes lysosomal membranes
Inhibits DNA and RNA synthesis
Reduce oxidative reactions
What is a major possible adverse effect of chloroquines?
irreversible retinal degeneration
(dose and frequency related)
Besides RA, what is another use of sulfasalazine?
Where is sulfasalazine metabolized to its active metabolite?
In the gut by bacteria.
What type of people would show increased effects with sulfasalazines?
How does sulfasalazines reduce inflammation?
cox inhibitor in the gut
What adverse effects of sulfasalazines occur in the first 3-6 months and then usually abate?
What are the most common side effects of sulfasalazine?
nausea and vomiting
diarrhea and anorexia
What are the major cytotoxic drugs?
What is the most commonly prescribed DMARD?
How does methotrexate work?
What is the difference in RA and cancer tx with methotrexate?
low dose in RA
What is given as an adjunct therapy in conjunction with methotrexate?
What are some of the most common toxicities associated with long-term methotrexate therapy?
Nausea, vomiting, diarrhea, anorexia
What tests are mandatory when a pt is on methotrexate?
CBC's and LFT's
(checking level of hepatoxicity)
How does azathioprine work?
inhibits PPRP synthase
How does leflunomide work?
inhibits dihydro-orotate DH
(RTL of de novo pyrimidine synthesis)
What are the uses of leflunomide
moderate to severe RA
Why does leftunomide decrease B and T cell proliferation?
B and T cells depend on de novo pyrimidine synthesis (can't recycle?). Leftunomide blocks this.
What are some adverse effects of leflunomide?
Rash and allergic reactions
What drug is second line following methotrexate?
What are both methotrexate and leflunomide C/I in?