Gold chloroquine

Navarro, M., Vasquez, F., Sanchez-Delgado, R.A., Perez, H., Sinou, V. and Schrevel, J. (2004) Toward a Novel Metal-Based Chemotherapy against Tropical Diseases. 7. Synthesis and in Vitro Antimalarial Activity of New Gold-Chloroquine Complexes. Journal of Medicinal Chemistry, 47, 5204. 

Toward a novel metal-based chemotherapy against tropical diseases. 7. Synthesis and in vitro antima-larial activity of new gold-chloroquine complexes, M. Navarro, F. Vasquez, R. A. Sanchez-Delgado, et al. J. Med. Chem., 2004, 47, 5204. 

When added to methotrexate background therapy, cyclosporine, chloroquine, hydroxychloroquine, leflunomide, infliximab, adalimumab, rituximab, and etanercept have all shown improved efficacy. In contrast, azathioprine, auranofin, or sulfasalazine plus methotrexate results in no additional therapeutic benefit. Other combinations have occasionally been used, including the combination of intramuscular gold with hydroxychloroquine. 

Amiodarone Chloroquine Cisplatin Colchicine Dapsone Disulfiram Glutethimide Gold compounds Hydralazine Isoniazid Misonidazole Nitrous oxide Nitrofuratoin Nucleoside analogs (antiretrovirals) Paclitaxel (taxanes) Phenytoin... 

Lichenoid eruption e.g. p-adrenoceptor blockers, chloroquine, thiazides, frusemide (furosemide), captopril, gold, phenothiazines. 

Clinically important, potentially hazardous interactions with aluminum hydroxide, antacids, ascorbic acid, bone marrow suppressants, chloroquine, cytotoxic agents, food, gold, hydroxychloroquine, iron, magnesium, primaquine, probenecid... 

Answer C. Ocular toxicity is characteristic of chloroquine and hydroxychloroquine. Corneal deposits are reversible, but retinal pigmentation can ultimately lead to blindness. Patients will complain about GI distress, visual dysfunction, ringing in the ears (note that tinnitus aiso occurs in salicylism), and itchy skin. Hydroxychloroquine also promotes oxidative stress that can lead to hemolysis in G6PD deficiency. DMARDs include gold salts (e.g., auranofin), methotrexate, and etanercept, but thioridazine is a phenothiazine used as an antipsychotic it lacks anti-inflammatory effect, but does cause retinal pigmentation. 

Quinoline antimalarials such as hydroxychloroquine (Fig. 5-6) and chloroquine have been found to have antiarthritic properties however, the onset of clinical improvement, as with penicillamine and gold, takes months. Irreversible retinopathy, including retinal opacity, can be encountered. Lesser toxicities include skin pigmentation and alopecia. Proposals to possible mechanisms of action are speculative at best. It should be emphasized that none of the slow-action antiarthritic agents discussed earlier should be considered as initial therapy in RA. The salicylates and other NSAIDs deserve this distinction. If results are unsatisfactory gold may be considered as the subsequent therapeutic step. Penicillamine would be a logical alternate, as would short-term steroids or cytotoxic agents. 

The manufacturers say that the concurrent use of leflunomide and other DMARDs (they list azathioprine, chloroquine, hydroxychloroquine, intramuscular or oral gold and penicillamine) has not yet been studied but they say that combined use is not advisable because of the increased risk of serious adverse reactions (haemo- or hepatotoxicity). As the active metabolite of leflunomide has a long half life of 1 to 4 weeks the manufacturers say that a washout of colestyramine or activated charcoal should be given if patients are to be started on other DMARDs. See also Methotrexate, below. 

Penicillamine plasma levels are increased by chloroquine and an increase in penicillamine toxicity is possible. Penicillamine should not be used with gold. Indometacin slightly increases penicillamine levels, and its use with any NSAD) might increase the risk of renal damage. An isolated report describes penicillamine-induced breast enlargement in a woman taking a combined oral contraceptive. 

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