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31 Cards in this Set

  • Front
  • Back
NSAIDS
Reduce inflammation, do not slow disease progression
Glucocorticoids
Reduce inflammation, do not slow disease progression
Low dose-reduce joint destrruxn
Long term-wt gain, diabetes, catarcts, osteoporosis
Methotrexate
-MOA
Folic acid analogue (inhibits dihydrofolate reductase) not anti-RA mechanism..... Increases release of adenosine*-anti-inflammatory mediator
Renal metabolism
Methotrexate
-PK, uses
MOST COMMONLY USED
1X/week
Hepatic metabolism
7-hydroxymethotrexate-longer t1/2
PO, IM, IV

Rapid onset/offset, improvement within weeks
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
Hydroxychloroquine
-MOA
Accumulates in lysosomal compartment of CT/WBCs, changes pH, inhibits sphingomyelinase, inhibits TNF signal, no NF-kB, proinflammatory mediators
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
Hydroxychloroquine
-AEs
Most transient, not serious
Rash
GI
Leukopenia
Peripheral neuropathy
Ocular EFX--basal eye exam
Sulfasalazine
-MOA
Unknown
May prevent absorption of ag's from GI tract
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
Etanercept (Enbrel)
-MOA
2 soluble TNF p75 receptor moities linked to Fc of human IgG1

Binds two TNF-alpha molecules
Etanercept (Enbrel)
-PK/Uses
SubQ injection
2X/week

Alone or w/MTX

RA, psoriatic arthritis, ankylosing arthritis
Etanercept (Enbrel)
-AEs
Injxn site rxns
Increase in serious infxn
DONT USE IN ME
may reactivate latent TB
Infliximab (Remicade)
-MOA
Chimeric monoclonal Ab
Binds w/high affinity to TNF-alpha
Infliximab (Remicade)
-PK/Uses
IV @ 0.2.6 wk then every 4 or 8 wk
Alone or w/MTX

Crohns
Infliximab (Remicade)
-AEs
URI
Allergic rxn
Not use in HF or PREGNANCY
May reactivate latent TB
Adalimumab (Humira)
-MOA
Fully human anti TF-alph Ab
Blacks TNF-alpha from interacting w/p55 and p75 TNF surface receptors
Adalimumab (Humira)
-PK/Uses
Subqt, every other week
Alone or with MTX

RA
Adalimumab (Humira)
-AEs
Injxn site rxn
Opportunistic infxn: TB, fungal
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
Anakinra (Kineret)
-PK/ Uses
Daily SubQT injxn

Pt>18yo who have failed 1+DMARDs
Alone or with other DMARDs
Not with anti-TNF drugs
Anakinra (Kineret)
-AEs
More injxn site rxns
Not for those with serious infxn
LYMPHOMA
Leflunomide
-MOA
Inhibits dihydroorotate dehydrogenase-decreased UMP concentration
Cells arrested in G1
Mostly reduces B cells, some T cells
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
Leflunomide
-AEs
Diarrhea
Reversible alopecia
Elevated liver enzymes
Contraindicated in pregnancy (Highly teratogenic)

May incrase ibuprofen, other NSAIDs (Metabolite inhibits CYP2C9)
Abatacept
-MOA
Recombinant fusion protein-binds CD80&CD86 on APCs, prevents binding with CD28 on T cells inhibits T cell co-activation
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
Abatacept
-AEs
Increase in infxn, headache, nasopharyngitis, nausea
may exacerbate COPD
Rituximab
-MOA
Monoclonal Ab binds CD20 on B cells
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
Rituximab
-AEs
Chills
Fever
Headache
Nausea
Long term: myelosuppression