Used for Treatment of Rheumatoid Arthritis

Hydroxychloroquine Stabilizes lysosomes and 4 chemotaxis GI distress and visual dysfunction (cinchonism), hemolysis in G6PD deficiency 

Methotrexate i 1 t s Cytotoxic to lymphocytes i Hematotoxicity, mucositis, crystalluria 

Sulfasalazine i Sulfapyridine — 4 B-cell functions 5-ASA possibly inhibits COX GI distress, rash, hemolysis in G6PD deficiency, SLE-like syndrome 

Glucocorticoids 4 LTs, ILs, and plateletactivating factor (PAF) ACTH suppression, Cushingoid state, osteoporosis, GI distress, glaucoma 

Gold salts 4 Lysosomal and macrophage functions Dermatitis, hematotoxicity, nephrotoxicity 

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Low-dose methotrexate is used for treatment of rheumatoid arthritis despite side effects such as disorders of the gastrointestinal tract and the liver. Leflunomide is also approved for this indication, however, hepatoxicity limits its use as first option. 

Many attempts have been made to link monoclonal antibodies specific for antigenic determinants on cancer cells to protein toxins such as ricin (Box 29-A). It is hoped that this may provide an effective way of carrying toxins into cancer cells/ 1 r Therapeutic human monoclonal antibodies are already in use as antirejection drugs for kidney transplantation, for treatment of rheumatoid arthritis, Crohn disease, and for some types of cancer/... 

Infliximab is approved for treatment of rheumatoid arthritis and Crohn s disease, but has been studied for use in psoriasis. One double-blind, randomized, placebo-controUed clinical trial studied the effectiveness and safety of infliximab in patients with moderate to severe psoriasis. A good response was seen in 82% and 91% of patients treated with infliximab 5 mg/kg or 10 mg/kg, respectively. Median time to response for all patients receiving infliximab was 4 weeks. The investigators concluded that patients treated with infliximab had a high degree of clinical improvement with rapid response rate, similar to that observed with cyclosporine therapy. ... 

The chiral monoester, (1 S,21 )-2-(methoxycarbonyl)cyclohex-4-ene-l-carboxylic add 24a (Figure 11.6 ) is a key intermediate for the synthesis of a potential drug candidate 27 for the modulation of chemokine receptor 2 (CCR2) activity useful in treatment of rheumatoid arthritis [67-69]. Both the (lS,2k)-monoester 24a and its enantiomer (lk,2S)-monoester 24b were obtained by resolving the... 

The salicylates and nonsteroidal anti-inflammatory drug (NSAIDs) are important in the treatment of arthritic conditions. For example, the salicylates and NSAIDs are used in the treatment of rheumatoid arthritis (a chronic disease characterized by inflammatory changes within the body s connective tissue) and osteoarthritis (a noninflammatory joint disease resulting in degeneration of the articular cartilage and... 

Penicillamine, MTX, and hydroxychloroquine are used in the treatment of rheumatoid arthritis. The administration of MTX is reserved for severe disabling disease that is not responsive to other treatment. 

Owing to the lag time between initiation and effect, capsaicin is not used for treatment of acute pain from injury. Instead, topical capsaicin is used for chronic pain from musculoskeletal and neuropathic disorders. Capsaicin preparations have been studied in the treatment of pain from diabetic neuropathy, osteoarthritis, rheumatoid arthritis, postherpetic neuralgia, and other disorders.48 It is often used as an adjuvant to systemic analgesics in these chronic pain conditions. 

Adalimumab is a TNF-a inhibitor initially approved for the treatment of rheumatoid arthritis in 2003. It is approved for treatment of psoriatic arthritis and off-label uses and clinical... 

Penicillamine has also been used in cystinuria and for the treatment of rheumatoid arthritis. Discovery of its chelating properties led to its use in patients with Wilson s disease (hepatolenticular degeneration) and heavy-metal intoxications. Penicillamine is administered by mouth and should be taken on an empty stomach [4],... 

Enbrel is a product now approved for medical use that is based upon this strategy. The product is an engineered hybrid protein consisting of the extracellular domain of the TNF p75 receptor fused directly to the Fc (constant) region of human IgG (see Box 13.2 for a discussion of antibody structure) The product is expressed in a CHO cell line from which it is excreted as a dimeric soluble protein of approximately 150 kDa. After purification and excipient addition (mannitol, sucrose and trometamol), the product is freeze-dried. It is indicated for the treatment of rheumatoid arthritis and is usually administered as a twice-weekly s.c. injection of 25 mg product reconstituted in WFI. Enbrel functions as a competitive inhibitor of TNF, a major pro-inflammatory cytokine. Binding of TNF to Enbrel prevents it from binding to its true cell surface receptors. The antibody Fc component of the hybrid protein confers an extended serum half-life on the product, increasing it by fivefold relative to the soluble TNF receptor portion alone. 

Gold has been used in medicine for many centuries, and since the 1920s several injectable gold compounds have been widely used for the treatment of rheumatoid arthritis. Recent reviews of the medicinal uses of gold compounds have been published (412-414). 

Enbrel Enbrel is used for the treatment of rheumatoid arthritis. It is supplied as a sterile, preservative-free, lyophilized powder. The powder is reconstituted with 1 mL sterile bacteriostatic water-for-injection (containing 0.9% benzyl alcohol) prior to parenteral injection. 

Urano, W., Taniguchi, A., Yamanaka, H., et al. (2002) Polymorphisms in the methylenetetrahydrofolate reductase gene were associated with both the efficacy and the toxicity of methotrexate used for the treatment of rheumatoid arthritis, as evidenced by single locus and haplotype analyses. Pharmacogenetics. 12, 183-190. 

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