Rheumatoid, Gout Flashcards
Class;Mechanism;Therapeutics;SideEffects
Indomethacin (Indocin)
Non-selective NSAID Eliminate pain; reduce inflammation (but does not slow disease progression) Rheumatoid arthritis; acute gouty arthritis Gastric and duodenal ulcers — —
Class;Mechanism;Therapeutics;SideEffects
Naproxen (Aleve)
Non-selective NSAID Eliminate pain; reduce inflammation (but does not slow disease progression) Rheumatoid arthritis; acute gouty arthritis Gastric and duodenal ulcers — —
Class;Mechanism;Therapeutics;SideEffects
COX-2 inhibitors
Selective NSAID Eliminate pain; reduce inflammation (but does not slow disease progression) Superseding conventional NSAIDs for rheumatoid arthritis 50% fewer gastric and duodenal ulcers than traditional NSAIDs — —
Class;Mechanism;Therapeutics;SideEffects
Gold Salts
DMARD Antipruritic; represses immune responsiveness (inhibits functional capabilities of macrophages) Rheumatoid arthritis Serious side effects in 30% of pts — Rarely used today
Class;Mechanism;Therapeutics;SideEffects
Quinolones
DMARD (antimalarial) Reduces T-cell activation & chemotaxis Rheumatoid arthritis, SLE Retinal damage (chloroquine) — Used for patients who no longer respond to NSAIDS or can’t tolerate gold or penillamine
Class;Mechanism;Therapeutics;SideEffects
Glucocorticoids
(Corticosteroids)
DMARD 1. Inhibits phospholipase A2 (inhibiting release of arachidonic acid and, thus, formation of prostaglandins)
2. Inhibits cytokine production (which prevents induction of COX-2) Rheumatoid arthritis; acute gouty arthritis (intraarticular injection for relief of acute monoarticular gout) Cushingoid symptoms — Started initially (fast acting) before other drugs become effective
Can give orally or intra-articularly
Class;Mechanism;Therapeutics;SideEffects
Sulfasalazine (Azulfidine)
DMARD Likely inhibition of IL-1 & TNF-alpha release Rheumatoid arthritis N/V, skin rashes, neutropenia (30% of patient discontinue drug) Headaches Acts more quickly than other drugs
Class;Mechanism;Therapeutics;SideEffects
Methotrexate (Trexall)
DMARD
(Immunosuppressive) 1. Inhibition of aminoimidazolecarboxamide (AICAR) transformylase and
thymidylate synthetase, with secondary effects on PMN chemotaxis
2. Causes adenosine accumulation, which inhibits inflammation Rheumatoid arthritis Nausea, stomatitis, hepatotoxicity (rare) — Takes several weeks to start working; “gold standard” of therapy
Class;Mechanism;Therapeutics;SideEffects
Leflunomide (Arava)
DMARD
(Immunosuppressive) Inhibits dihydroorotate dehydrogenase (DHODH), which inhibits T-lymphocyte response to stimuli Rheumatoid arthritis Diarrhea, hepatotoxity — Takes several weeks to start working; oral prodrug
Class;Mechanism;Therapeutics;SideEffects
Etanercept (Enbrel)
Biologic Response Modifiers Blocks binding of TNF to TNF receptors Rheumatoid arthritis — — Twice weekly subcutaneous injections
Class;Mechanism;Therapeutics;SideEffects
Infliximab (Remicade)
Biologic Response Modifiers Blocks binding of TNF to TNF receptors Rheumatoid arthritis Antigenic response to murine monoclonal Ab — —
Class;Mechanism;Therapeutics;SideEffects
Adalimumab (Humira)
Biologic Response Modifiers Blocks binding of TNF to TNF receptors Rheumatoid arthritis — — Fully human, so no antigenic response; twice monthly injections
Class;Mechanism;Therapeutics;SideEffects
Golimumab
Biologic Response Modifiers Blocks binding of TNF to TNF receptors Rheumatoid arthritis Risk of serious infections
Class;Mechanism;Therapeutics;SideEffects
Certolizumab
Biologic Response Modifiers Blocks binding of TNF to TNF receptors Rheumatoid arthritis Risk of serious infections Conjugated to PEG for stabilization
Class;Mechanism;Therapeutics;SideEffects
Anakinra (Kineret)
Biologic Response Modifiers IL-1 Receptor Antagonist Rheumatoid arthritis — — Short (6 hr) plasma half-life; daily treatment with high doses
Class;Mechanism;Therapeutics;SideEffects
Tocilizumab (Actemra)
Biologic Response Modifiers IL-6 Receptor Antagonist Rheumatoid arthritis — — —
Class;Mechanism;Therapeutics;SideEffects
Rituximab (Rituxan)
Biologic Response Modifiers Anti-CD20 mAb, reduces circulating B cells Rheumatoid arthritis Infections; hypersensitivity reactions — Used for RA refractory to TNF-alpha inhibitors
Class;Mechanism;Therapeutics;SideEffects
Abatacept (Orencia)
Biologic Response Modifiers Inhibits T-cell activation and induces T-cell apoptosis Rheumatoid arthritis Headaches; infections — Used in patients for RA refractory to MTX or TNF-alpha inhibitors
Class;Mechanism;Therapeutics;SideEffects
Colchicine (Colcrys)
— Prevents tubulin polymerization & leads to inibition of leukocyte migration, phagocytosis, and release of cytokines Acute gouty arthritis Long-term use causes peripheral neuropathy & neutropenia Nausea, vomiting, abdominal pain, troublesome diarrhea Works in 12-24 hours!
Class;Mechanism;Therapeutics;SideEffects
Probenecid (Benemid)
Uricosuric Agent Compete with urate at the anionic transport site of the renal tubule and inhibit urate reabsorption Chronic tophaceous gout Urate crystal mobilization and acute gouty arthritis Gastrointestinal irritation Secretion of some weak acids (e.g., penicillin) is reduced
Class;Mechanism;Therapeutics;SideEffects
Allopurinol (Zyloprim)
— 1. Reduces uric acid synthesis by inhibiting xanthine oxidase (competitive inhibition) –> alloxanthine
2. Alloxanthine is a non-competitive inhibitor of xanthine oxidase Chronic tophaceous gout Acute attacks of gouty arthritis early in treatment due to mobilization of urate crystals — —
Class;Mechanism;Therapeutics;SideEffects
Febuxostat (Uloric)
— Non-purine, non-competitive antagonist of xanthine oxidase Chronic tophaceous gout Nausea, rash, arthralgias — Expensive
Class;Mechanism;Therapeutics;SideEffects
Pegloticase (Krystexxa)
Recombinant, stabilized uricase Converts uric acid to allantoin Chronic tophaceous gout
