Rheumatoid Arthritis & Gout Flashcards
Indomethacin class?
Non-selective NSAID (eliminate pain, reduce inflammation)
Indomethacin for?
RA, gout
Indomethacin side effetcs?
Gastric and duodenal ulcers
Naproxen class?
Non-selective NSAID (eliminate pain, reduce inflammation)
Naproxen for?
RA, gout
Naproxen side effects?
Gastric and duodenal ulcers
COX-2 inhibitor class?
Selective NSAID (eliminate pain, reduce inflammation)
COX-2 inhibitors are____conventional NSAIDs for RA?
Superseding
COX-2 inhibitor side effects?
Gastric and duodenal ulcers, but 50% less than traditional NSAIDs
Quinolines class?
DMARDs (antimalarials)
Quinoline mxn?
Reduce T-cell activation & chemotaxis
Quinoline for?
RA & SLE, for patients who no longer respond to NSAIDs or cannot tolerate other DMARDs
Glucocorticoids (Corticosteroids) class & mxn?
DMARDs; Inhibit Phospholipase A2 (inhibit release of arachidonic acid and formation of prostaglandins) + Inhibit cytokine production and prevent induction of COX-2
Glucocorticoids for?
RA, Acute Gouty Arthritis
Glucocorticoid side effects?
Cushingoid symptoms
Glucocorticoid timing?
Fast acting
Sulfasalazine class and mxn?
DMARD; likely inhibition of IL-1 and TNF-a release
Sulfasalazine for?
RA
Sulfasalazine side effects?
N/V, HAs, Skin rashes, neutropenia, 30% discontinue drug
Sulfasalazine timing?
Fast acting
Methotrexate class and mxn?
DMARD (immunosuppressive). Inhibits aminoimidazolecarboxamide transformylase (AICAR) and thimidylate sunthase, with secondary effects on PMN chemotaxis; Causes adenosine accumulation which inhibits inflammation
Methotrexate for?
RA
Methotrexate side effects?
Nausea, stomatitis, hepatotoxicity (rare)
Methotrexate timing?
Takes several to start working
Leflunomide class and mxn?
DMARD (immunosuppressive). Inhibits dihydroorotate dehydrogenase (DHODH) (RLenzyme in de novo pyrimidine synthesis). T-lymphocyte response to stimuli.
Leflunomide for?
RA
Leflunomide side effects?
Diarrhea, hepatotoxicity (slightly more toxic than MTX)
Leflunomide timing?
Takes several weeks to start working
Leflunomide a prodrug?
Yes, an oral prodrug
Etanercept class and mxn?
BRM, blocks binding of TNF to TNFR (fusion protein of 2 TNF receptors with Fc portion of IgG)
Etanercept for?
RA
Etanercept dosing?
Twice weekly SubQ inection
Infliximab class and mxn?
BRM, blocks binding of TNF to TNFR (chimeric mouse/human IgG)
Infliximab for?
RA
Infliximab side effect?
Antigenic response to murine monoclonal Abs
TNF inhibitors?
Etanercept, Infliximab, Adalimumab, Golimumab, Certolizumab
Adalimumab mxn and class?
BRM, blocks binding of TNF to TNFR (fully human IgG)
Adalimumab for?
RA
Adalimumab dosing?
2 monthly injections
Adalimumab side effects?
Fully human so no antigenic response
Golimumab mxn and class?
BRM, blocks binding of TNF to TNFR
Golimumab for?
RA
Golimumab side effects?
Serious infections
Certolizumab mxn and class?
BRM, blocks binding of TNF to TNFR
Certolizumab for?
RA
Certolizumab side effects?
Serious infections
Quinolines efficacy and side effects?
Low side effects (except retinal damage with chloroquine), but low efficacy
Non-selective NSAIDs?
Indomethacin, Naproxen
Immunosuppressive DMARDs?
Methotrexate and Leflunomide
DMARD that inhibits IL-1 and TNFa release?
Sulfasalazine
IL-1 receptor antagonist?
Anakinra
Anakinra for?
RA
Anakinra timing?
Short (6 hr) half life, daily tx with high doses
Il-6 receptor antagonist?
Tocilizumab
Tocilizumab for?
RA
Tocilizumab side effects?
Serious infections
Rituximab class and mxn?
BRM, Anti-CD20 Ab, reducing circulating B cells
Rituximab for?
RA refractory to TNFa inhibitors
Rituximab side effects?
Infections, hypersensitivity reactions
Abatacept mxn and class?
BRM, inhibits T-cell activation and induces T-cell apoptosis
Abatacept for?
RA refractory to MTX or TNFa inhibitors
Abatacept side effects?
HAs, infections
Uricosuric agent?
Probenecid
Probenecid mxn?
Uricosuric agent. Competes with urate at the anionic transport side of the renal tubule and inhibits urate reabsorption.
Probenecid for?
Chronic tophaceous gout
Probenecid side effects?
GI irritation, urate crystal mobilization and acute gouty arthritis, secretion of weak acids (penicillin) reduced
For acute gouty arthritis?
NSAIDs, corticosteroids, colchicine
Colchicine for?
Acute gouty arthritis
Colchicine mxn?
Prevents tubulin polymerization and leads to inhibition of leukocyte migration, phagocytosis, and cytokine release
Colchicine timing?
works in 12-24 hours
Colchicine side effects?
N/V/D/Ab pain, Long-term use causes peripheral neuropathy and neutropenia, low therapeutic index
Allopurinal mxn?
Reduce uric acid synthesis by inhibiting xanthine oxidase (competitive inhibitor. It is converted to alloxanthine by XO, which is a non-competitive inhibitor of XO.
Allopurinol for?
Chronic tophaceous gout
Allopurinol side effects?
Acute attacks of gouty arthritis early in tx due to mobilization of urate crystals, hypersensitivity, maculopapular rash in 2%
Pegloticase is?
Recombinant stabilized uricase, converts uric acid to allantoin
Pegloticase for?
Chronic tophaceous gout
Non-purine, non-competitive antagonist of XO?
Febuxostat
Useful if allopurinol is not tolerable?
Febuxostat
Febuxostat for?
Chronic tophaceous gout
Febuxotat side effects?
Nausea, rash, arthralgias
Febuxostat is expensive?
Yes
TNF inhibitor conjugated to PEG for stabilization?
Certolizumab
“Classic” pharmacologic interventions for chronic gout?
Allopurinol, probenecid, febuxostat
Concerns for febuxostat remain for?
Cardiovascular safety