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21 Cards in this Set
- Front
- Back
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Major inflamation mediator due to both COX enzymes?
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generation of Prostaglanding E2
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What's a COX2 selective drug currently in use?
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celecoxib (celebrix)
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DMARDs: Methotrexate (MTX)
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anti-inflammatory drug, most widely used DMARD, immunosupression may lead to infection, lymphomas.
Combo of MTX with cyclosporine or infliximab better than MTX alone |
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DMARDs: Gold preparation
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retard bone progression, and articular destruction.
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DMARDs: Gold sodium thiomalate
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i.m. gold accumulates in macrophages, depress macrophage activity, migration and immune response.
adv: dermatitis, thrombocytopenia, aplastic anemia, proteinuria. |
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DMARDs: drugs often given together with MTX
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Leflunamide, Etanercept, infliximab, abatercept, rituximab, Anakinra
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Etanercept
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TNF-alpha antagonist, prevents TNF-r stimulation
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Infliximab
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ab to TNF-alpha
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abatacept
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mimics CTLA-4, works upstream of infliximab and etanercept
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rituximab
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CD20 ab (spec B lymphocytes)
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Anakinra
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IL-1-r antagonist, natural, DON'T USE WITH TNF-ALPHA BLOCKERS
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DMARDs side effects
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serious infections, TB reactiviation, allergic rxn, malignancies
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Aspirin
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IRREVERSIBLE, nonselective cox inhibitor, through aceylation.
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older NSAIDS: ibuprofen, naproxen
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REVERSIBLE, non selective
gastric ulcerations, bleeding, impaired kideny function |
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Salicylate
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weak Cox inhibitor, NF-kB inhibition more important.
NF-kB normally induces IL-1, IL-6, IFN beta etc. |
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Celecoxib
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COX-2 selective, suppose to reduce gastric damage,
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Acetaminophen (Tylenol)
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not part of the NSAID group. good analgesic and antipyretic. LESS EFFECTIVE AS anti-inflammatory agent.
Weak COX inhibitor. Exact mechanism might include COX-2 inhibition in the brain. |
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Use of IRRVERSIBLE COX inhibiotor: Aspirin
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prophylactic for myocardial infarction in men and ischemic stroke in women.
Bartter's Syndrome: hyperplasia of renal JGA, increase renin, aldosterone, hypokalemia, normal BP. NSAIDS reverse these sx. Paten Ductus arteriosus: allows duct to close without suregery. |
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Aspirin metabolism
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dose dependant, deacylated to salicylate. Dose dependance due to saturation of conjugation pathway, glycine conjugation. >>> zero order elimination.
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NSAIDS with short half life
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aspirin, ibuprofen, indomethacin
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NSAIDS with long half life
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naproxen, phenylbutazone, salicylate.
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