Drugs for RA, Gout, and Osteoporosis

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Created by:

birdsvsworms  on April 10, 2012

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MSS 2

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Drugs for RA, Gout, and Osteoporosis

First line DMARD
methotrexate; fastest onset about 2-6 wks
1/39
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First line DMARD methotrexate; fastest onset about 2-6 wks
Side effects of methotrexate. Which may be irreversible? nausea, mucosal ulcers
At high doses, WBC depression, liver cirrhosis, pneumonitis (may be irreversible)
Leflunomide: MOA inhibit TK activity and inhibit de novo pyrimidine synthesis
Lefluonomide: side effects elevated liver enzymes
suppression of high-turnover cells (so GI sx, alopecia)
Abatacept: MOA binds CD80 and CD86, which are costimulation modulators in T cell activation
Abatacept: indications for mod-severe RA not responding to TNF-inhibitors or methotrexate
Abatacept should not be used with ---- TNF-alpha inhibitors, b/c increases risk of infection
Abatacept contraindicated in ppl with COPD
Rituximab: MOA targets CD20 B lymphocytes
Rituximab: side effect and first-time effects side effect: flu-like sx
first time effects: may cause breathing difficulties, cardiac rhythm disturbances, cardiogenic shock
Sulfasalazine: pharmacokinetic properties prodrug; is poorly absorbed, gets modified by gut bacterial to sulfpyradine and 5-aminosalicylate (the anti-inflammatory)
Sulfasalazine: indications usually used after methotrexate fails, or in pts with liver dz who can't take methotrexate
Also used in IBD, seronegative spondyloarthropathies
Hydroxychloroquine: toxicities usually ocular: corneal deposits, extraocular muscle weakness, retinopathy--can lead to irreversible vision loss
Gold salts: side effects skin rash, blood dyscrasias, kidney damage
D-penicillamine: MOA cysteine analog
D-penicillamine: side effects and indication derm problems, nephritis, aplastic anemia
Usually used last-resort when others fail
Infliximab: MOA Ab binding to TNF-alpha
Infliximab: side effects URIs, immune rxn
Etancercept: MOA two TNF receptors + Fc portion of IgG, so sequesters two molecules of TNF-alpha per molecule of drug
Adalimumab: MOA murine anti-TNF antibody
usually less immunoreactive
Anakinra: MOA IL-1ra: analog of IL-1 human receptor antagonist, so blocks the IL-1 receptor
Anakinra: not recommended in combo with ---- TNF-alpha inhibitors, b/c increases infections
Tocilizumab: MOA IL-6 receptor Ab
Tocilizumab: indication for pts who fail TNF-alpha; usually used in combo with methotrexate
Tocilizumab: adverse effects URI, H/A, HTN, elevated LFTs, increased LDL, decreased neutrophils and platelets--infection, GI perforation, hypersensitivity, may increase risk of CA
Cyclosporine: MOA and adverse effect inhibits T cell activity
renal toxicity
Azathioprine: MOA and adverse effect purine antimetabolite, interferes with purine biosynthesis causing DNA damage
can cause bone marrow suppression and hepatotoxicity
Cyclophosphamide: MOA alkylating agent, suppressing B cells, T cells, and any rapidly dividing cells
Capsacin: MOA causes local depletion of substance P (usually a local cream for RA)
Two drugs used for acute gout NSAIDs
Colchicine
Colchicine: MOA and adverse effects binds tubulin so arrests granulocyte migration
n/v/d, abd pain; long term use leads to myopathy, agranulocytosis, aplastic anemia, alopecia
3 drugs used for chronic gout allopurinol/febuxostat
probenecid
sulfinpyraxole
Allopurinol/febuxostat: MOA and side effect inhibits xanthine oxidase
hypersensitivity
Probenecid: MOA and side effects blocks PCT reabsorption of uric acid
GI irritation, GI bleeding, hypersensitivity
Probenecid: contraindications in pts with impaired renal function or those predisposed to getting urate stones
Sulfinpyrazole: MOA and drug interactions blocks PCT reabsorption of uric acid
may inhibit metabolism of oral hypoglycemic agents and hepatic metabolism of warfarin
Side effects of bisphosphonates esophagitis and osteonecrosis of jaw (alendronate especially)
What diuretic increases plasma concentrations of urate? thiazides
Anytime you increase excretion of sodium, the PCT will reabsorb calcium, sodium, urate. However, even if hyperuricemia results, pt is likely not to have an attack of gout
Maintain pH of urine at what level when using uricosuric agent? alkaline urine--maintains ionic form

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