IV. Comparison of Effects of Two Antimalarial Agents, Hydroxychloroquine Sulfate and Chloroquine Phosphate, in Patients with Rheumatoid Arthritis

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SOME of the antimalarial agents that have a valuable anti-inflammatory action in patients having discoid or systemic lupus erythematosus have been found to have a similar effect in patients having rheumatoid arthritis.34,35 However, these drugs have not been used widely for rheumatoid arthritis because of their undesirable side effects.

The first antimalarial agent used in the treatment of discoid lupus erythematosus was quinacrine hydrochloride*, an acridine derivative,36 but the undesirable side effects of this drug often were serious and sometimes fatal; they included nausea, anorexia, vomiting, dermatitis, nervousness, insomnia, headache, blurring of vision, agranulocytosis, and aplastic anemia. Primaquine diphosphate**, an 8-aminoquinoline, also was found to have anti-inflammatory activity, but its side effects, as reported by Steck and his group,37 prevented its widespread clinical use. They found methemoglobinemia and pallor in all, anorexia in 14, and leukopenia in 7 of 21 patients having rheumatoid arthritis who were given the drug for two weeks.

Chloroquine phosphate, a 4-aminoquinoline, has been reported to be effective in the treatment of both systemic lupus erythematosus and rheumatoid arthritis. Dubois and Martel38 believe that chloroquine phosphate is as effective as quinacrine hydrochloride in the treatment of moderately active systemic lupus erythematosus. Freedman39 reported the effect in 50 patients with rheumatoid arthritis who received 300 mg. of chloroquine sulfate daily for two years. Apparently 43 patients became entirely or nearly asymptomatic, although some continued to have elevated sedimentation rates, which indicated that disease activity persisted. Of the other seven patients, three continued to have slight joint inflammation . . .



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