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31 Cards in this Set
- Front
- Back
NSAIDS
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Reduce inflammation, do not slow disease progression
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Glucocorticoids
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Reduce inflammation, do not slow disease progression
Low dose-reduce joint destrruxn Long term-wt gain, diabetes, catarcts, osteoporosis |
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Methotrexate
-MOA |
Folic acid analogue (inhibits dihydrofolate reductase) not anti-RA mechanism..... Increases release of adenosine*-anti-inflammatory mediator
Renal metabolism |
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Methotrexate
-PK, uses |
MOST COMMONLY USED
1X/week Hepatic metabolism 7-hydroxymethotrexate-longer t1/2 PO, IM, IV Rapid onset/offset, improvement within weeks |
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Methotrexate
-AEs |
Reduced with leucovorin or folic acid
Mucosal ulcers N/D Liver disease Higher-bone marrow suppression Contraindicated in pregnancy Dont use with high dose ASA or probenecid |
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Hydroxychloroquine
-MOA |
Accumulates in lysosomal compartment of CT/WBCs, changes pH, inhibits sphingomyelinase, inhibits TNF signal, no NF-kB, proinflammatory mediators
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Hydroxychloroquine
-Uses |
2nd most used
PO 1X/day T1/2--40 days Long latency 2nd line drug for RA, malaria when NSAIDs dont work, may be used with NSAIDs, reduces RF, does not effect erosive bony lesions Safe for pregnancy |
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Hydroxychloroquine
-AEs |
Most transient, not serious
Rash GI Leukopenia Peripheral neuropathy Ocular EFX--basal eye exam |
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Sulfasalazine
-MOA |
Unknown
May prevent absorption of ag's from GI tract |
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Sulfasalazine
-PK, uses |
PO
2nd line drug for RA Early Rx of arthritis Can be used in low doses for pregnancy Sulfapyridine moiety is important |
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Etanercept (Enbrel)
-MOA |
2 soluble TNF p75 receptor moities linked to Fc of human IgG1
Binds two TNF-alpha molecules |
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Etanercept (Enbrel)
-PK/Uses |
SubQ injection
2X/week Alone or w/MTX RA, psoriatic arthritis, ankylosing arthritis |
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Etanercept (Enbrel)
-AEs |
Injxn site rxns
Increase in serious infxn DONT USE IN ME may reactivate latent TB |
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Infliximab (Remicade)
-MOA |
Chimeric monoclonal Ab
Binds w/high affinity to TNF-alpha |
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Infliximab (Remicade)
-PK/Uses |
IV @ 0.2.6 wk then every 4 or 8 wk
Alone or w/MTX Crohns |
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Infliximab (Remicade)
-AEs |
URI
Allergic rxn Not use in HF or PREGNANCY May reactivate latent TB |
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Adalimumab (Humira)
-MOA |
Fully human anti TF-alph Ab
Blacks TNF-alpha from interacting w/p55 and p75 TNF surface receptors |
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Adalimumab (Humira)
-PK/Uses |
Subqt, every other week
Alone or with MTX RA |
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Adalimumab (Humira)
-AEs |
Injxn site rxn
Opportunistic infxn: TB, fungal |
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Anakinra
-MOA |
Recombinant form of human IL-1R antagonist, blocks IL-1
decrease in cartilage degredation by inhibiting IL-1's indxn of loss of proteoglycans Inhibit stimulation of bone resorption |
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Anakinra (Kineret)
-PK/ Uses |
Daily SubQT injxn
Pt>18yo who have failed 1+DMARDs Alone or with other DMARDs Not with anti-TNF drugs |
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Anakinra (Kineret)
-AEs |
More injxn site rxns
Not for those with serious infxn LYMPHOMA |
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Leflunomide
-MOA |
Inhibits dihydroorotate dehydrogenase-decreased UMP concentration
Cells arrested in G1 Mostly reduces B cells, some T cells |
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Leflunomide
-PK/Uses |
Converted to active drug in intestines and liver
Average t1/2=15 days Cholestyramine can interrupt enterohepatic circulation/increase elimination RA, Wegner's granulomatosis, SLE, myasthenia gravis Similar efficacy to MTX |
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Leflunomide
-AEs |
Diarrhea
Reversible alopecia Elevated liver enzymes Contraindicated in pregnancy (Highly teratogenic) May incrase ibuprofen, other NSAIDs (Metabolite inhibits CYP2C9) |
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Abatacept
-MOA |
Recombinant fusion protein-binds CD80&CD86 on APCs, prevents binding with CD28 on T cells inhibits T cell co-activation
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Abatacept
-PK/Uses |
IV, every 2 wks
Moderate/severe RA w/inadequate response to other DMARDs CANNOT be used with other DMARDs Not used with TNF-a antagonist or anakinra |
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Abatacept
-AEs |
Increase in infxn, headache, nasopharyngitis, nausea
may exacerbate COPD |
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Rituximab
-MOA |
Monoclonal Ab binds CD20 on B cells
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Rituximab
-Uses/PK |
IV@day1,15
t1/2-19 days Relapsed or refractory non-hodgkin's Bcell lymphoma, diffuse large B-cell NHL, RA-when unresponsive to anti-TNFalpha, combined w/MTX |
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Rituximab
-AEs |
Chills
Fever Headache Nausea Long term: myelosuppression |