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25 Cards in this Set
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hydroxychloroquine
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antimalarial used to tx arthritis
DMARD mech of action is unclear more commonly used to tx rheumatoid arthritis and lupus erythematosus contraindicated in psoriatic arthritis b/c of possible development of exfoliative dermatitis can cause irreversible retinal damage (less of a prob w/ hydroxychloroquine than chloroquine) |
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chloroquine
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antimalarial used to tx arthritis
see hydroxychloroquine |
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aurothioglucose
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gold compounds used to tx arthritis
in general: alters macrophage morphology and function - decreases cytokine, chemokine, growth factor synthesis, decreases PG and LTB4, decreases histamine release from mast cells specific: adjunctive tx of early active cases of adult and uvenile RA administered IM cutaneous reactions include erythema (skin flush) and exfoliative deramtitis more serious side effects include blood dyscrasias and kidney toxicity --> use infrequently in general: should NOT be given with penicillamine (chelates gold) contraindications: previous gold tox, pregnancy, liver or kidney impairment, blood dyscrasia adverse effects: dermatitis and diarrhea, eosinophilia and other hematological disturbances, proteinuria may --> nephrotic syndrome, aplastic anemia (rare but fatal) |
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auranofin
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gold compounds used to tx arthritis
general: see aurothiglucose specific: only gold compound available for oral administration treats early active cases of both adult and juvenile types of RA |
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penicillamine
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other drugs used to tx arthritis
oral chelating agent treats patients with: Wilson's disease, cystinuria, R cases of RA |
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sulfasalazine
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other drugs used to tx arthritis
used for treatment of RA, ankylosing spondylitis, ulcerative colitis |
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leflunomaid
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other drugs used to tx arthritis
orally active, inhibits dihydroorotic acid dehydrogenase, an enzyme involved in ribonucleotide synthesis stimulates translocation of p53 to the nucleus - cells arrested in G1 phase of cell cycle inhibits autoimmune T cell production inhibits production of autoantibodies by B cells 1st agent for RA indicated for both symptomatic improvement and retardation of structural joint damage cause alopecia (hairloss), rash, and diarrhea |
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abatacept
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other drugs used to tx arthritis
a co-stimulatory or second signal blocker of T cell activation, blocks interaction b/t B7 and CTLA4 IV infusion used in pts unresponseive to DMARDs of TNF antagonists increased risk of infections |
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cochicine
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other drugs used to tx arthritis
used to tx gout reduces pain and inflammation of an acute attack of gouty arthritis produces anti-inflammatory effect by inhibiting leukocyte migration and phagocytosis adverse effects include: diarrhea, nausea, and vomiting |
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aspirin
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NSAID used to tx arthritis
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acetaminophen
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NSAID to tx arthritis; also: ibuprofen, naproxen, sulindac, celecoxib, etoricoxib, meloxicam, valdecoxib
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indomethacin
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NSAID to tx arthritis
very effective for inflammation, with acute gouty arthritis primary NSAID used to tx severe gout other NSAIDs used: ibuprofen, naproxen, sulindac |
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corticosteroids
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drug used to tx arthritis - immunosuppresive
anti-inflammatory properties make them useful in tx of acute gout side effects associated w/ prolonged use inhibits PG and LT synthesis cytotoxic to certain T cell subpopulations (helper and suppressor) suppresses both cellular and humoral immunity inhibition of leukocyte infiltration at site of inflammation interference in the fxn of mediators of inflammatory response NOT toxic to myeloid and erythroid stem cells adverse effects: predisposition to infection, adrenal gland suppression used as immunosupprssives: organ transplantation, autoimmune diseases, bronchial asthma |
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azathioprine
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cytotoxic agent, immunosuppressive drug to tx arthritis
well absorbed from GI tract converted to 6-mercaptopurine by glutathione-S-transferases and then to 6-thiouric acid by xanthine oxidase, reduce dose in pts with thiopurine methyltransferase def mech of action: interferes w/ nucleic acid metabolism and synthesis, inhibits cell proliferation adverse effects: bone marrow suppression - leukopenia, anemia, thrombocytopenia, high doses - skin rashes, fever, nausea, vomiting, diarrhea, and GI disturbance; occasional liver dysfxn and mild jaundice, increased by kidney disease and allopurinol (xanthine oxidase inhibitor) use: kidney transplant, autoimmune disease |
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cyclophosphamide
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cytotoxic agent, immunosuppressive drug to tx arthritis
most potent immunosuppressive agent destroys proliferating lymphoic cells in addition to some quiescent cells use: organ transplantation, autoimmune diseases |
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methotrexate
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cytotoxic agent, immunosuppressive drug to tx arthritis
low dose inhibits AICAR transformylase --> AICA ribose, AICA ribose inhibits adenosine deaminase, increases extracellular adenosine --> inhibits IL-2R expression on T cells Dihydrofolate reductase inhibitor - blocks reactions requiring folate (biosynt of nucleotides for cell prolif) cytotoxic to proliferating lymphocytes following antigen exposure uses: prophylaxis for GvH for bone marrow transplantation in leukemia pts, acute rheumatoid arthritis, psoriasis |
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cyclosporine
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other immunosuppressive agent to tx arthritis
one of several polypeptid antibiotics produced by certain fungi that has immunosuppressive activity complexes with cyclophilin, which inhibits the phosphatase calcineurin blocks production of cytokines by antigen-stimulated T-helper cells that otherwise stimulate T-cell growth and differentiation does NOT affect suppressor T cells or T cell independent, antibody-mediated immunity immunosuppressive actions involve: inhibition of the production and/or release of various lymphokines including IL-1 and IL-2 in turn; impaired actions of helper T-cells --> impaired cellular immunity administered orally (20-50% absorbed) and IV - high 1st metabolism in liver metabolized extensively in liver by CYP3A4 to at least 25 metabolites inhibition of hepatic microsomal enzymes: decreased clearance (cyclosporine toxicity - nephrotoxicity, seizures); increased clearance of cyclosporine by stimulating its metabolism may lead to graft rejection adverse effects: nephrotoxicity - most common, most pts, minimized by clonidine additional nephrotoxicity - coadministratino of others - amphotericin B, acyclovir, aminoglycosides, foscarnet, NSAIDs, and vancyomycine seizures used as immunosuppressive: prevent allograft rejection tx autoimmune conditions |
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tacrolimus (FK-506)
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other immunosuppressive agent to tx arthritis
macrolide derived from a fungus with similar pharmacokinetics to cyclosporin more effective than cyclosporine in acute rejection, than in chronic rejection - more potent immnosuppressant than cyclosporine overall adverse effects are greater than cyclosporine, but kidney toxicity is less oral parenteral immunosuppressive agent approved for prophylaxis of hepatic allograft rejection but also effective for other organ transplantation |
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etanercept
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other immunosuppressive agent to tx arthritis
anti-TNFalpha agent - also, there is infliximab and adalimumab dimeric fusion protein that binds to TNF - soluble TNFreceptor, treatment of RA, given by injection |
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anakinra
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other immunosuppressive agent to tx arthritis
IL-1 receptor antagonist reduces the signs and symptoms and slows the progression of structural damage of moderate to severe active rheumatoid arthritis in patients who failed one or more DMARDS given sc once a day |
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infliximab
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monoclonal antibody used to tx arthritis
a chimeric monoclonal antibody that binds TNFalpha IV infusion - half-life of 8-12 days given w/ methotrexate for RA use for Crohn's disease when conventional therapy fails patients may develop serious infections |
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adalimumab
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monoclonal drug use dto tx arthritis
binds and neutralizes TNFalpha by blocking its interaction with the p55 and p75 TNF receptors given sc every other week to patients who have had inadequate response to at least one other DMARD methotrexate, glucocorticoids, salicylates, NSAIDs, or DMARDs may be continued during treatment |
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allopurinol
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drug used to tx gouty arthritis
inhibits xanthine oxidase and thus inhibits synthesis of uric acid effective in both primary and secondary forms of gout serious side effects including vasculitis, agranulocytosis, hypersensitivity reactions inhibits conversion of mercaptopurine and azathioprine to their inactive form - dosing considerations |
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probenicid
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uricosuric agent used to tx gouty arthritis
tx hyperuricemia assoc w/ chronic gout or secondary to other causes (drug-induced hyperuricemia) not effective for: acute attacks of gout, can aggravate inflammation if administered during initial stages |
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sulfinpyrazone
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uricosuric agents to tx gouty arthritis
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