Table 1.
Medications | First used | Characteristics | Toxicity |
---|---|---|---|
Gold salts (Gold sodium thiomalate and gold sodium thioglucose) | 1928 | Longest onset of action, administered only by oral or by intramuscular injection.
Lack of sustained clinical activity, slow onset of action, cost, poor long-term compliance. |
High incidence of toxicity requiring drug discontinuation: mucocutaneous reations, proteinuria and cytopenias. |
Sulphasalazine | 1938 | the first DMARD specifically synthesized for the treatment of RA. Low cost. | GI-related complications, neutropenia, cytopenias. |
Antimalarials (Chloroquine, hydroxychloroquine) | 1940s | Less effective than other DMARDs, but also less toxic, readily absorbed orally, extended serum half-lives due to tissue depot effects. | Rare but potential renal toxicity |
Methotrexate | 1950s | Gold-standard therapy, sustained long-term action, high tolerability, low cost, antimetabolite and antifolate drug. | Hepatitis and cirrhosis, interstitial pneumonitis, cytopenias. |
Azathioprine | 1960s | An immunosuppressant used to treat severe rheumatoid arthritis. | Vomiting, diarrhea, muscle aches. Increasing risk of developing certain types of cancer, especially skin cancer and lymphoma. |
D-penicillamine | 1960s | A metabolite of penicillin. Used to treat active rheumatoid arthritis that has not responded to other measures. | Rashes, loss of appetite, nausea, abdominal pain, and loss of the sense of taste. bone marrow suppression and serious kidney disease |
Cyclosporine A | 1980s | Calcineurin inhibitor. Third-line drug in RA therapy. | Renal insufficiency, anemia, hypertension |
Leflunomide | 1988 | Inhibits de novo pyrimidine synthesis, similar efficacy with methotrexate and sulphasalazine. | Most important serious adverse reaction is hepatotoxicity |
Minocycline | 1990s | A member of the broad spectrum tetracycline antibiotics, mildly beneficial. | Autoimmune syndromes, headaches and a graying skin pigmentation. |