Effects of chloroquine in hematoporphyrin-treated animals.

Porphyrins and related compounds are useful in photodynamic therapy but can cause cutaneous photosensitivity. We determined whether chloroquine, which is effective in treating porphyria cutanea tarda, would mobilize an administered porphyrin from tissues and enhance its excretion. Hematoporphyrin with and without chloroquine was administered to chick embryos, mice, and rats. Tissue and plasma porphyrin levels were markedly increased after hematoporphyrin dosing. Porphyrin concentrations in liver, spleen, and kidney were not significantly affected by chloroquine. Total urinary and fecal porphyrin excretion in rats treated with hematoporphyrin (50 mg/kg, i.p.) was not influenced by chloroquine treatment (100 mg/kg, s.c.). Excretion of heptacarboxylporphyrin, normally a minor fraction of urinary porphyrins, was significantly increased in chloroquine-treated rats. These results suggest that chloroquine is unlikely to be useful after photodynamic therapy for mobilizing exogenous porphyrins from tissues such as liver, spleen, and kidney. Increased urinary excretion of heptacarboxylporphyrin may contribute to the beneficial effect of chloroquine in porphyria cutanea tarda.