The antianginal drug amiodarone (an amphiphilic cationic compound) causes a keratopathy in humans. In the present investigation the cytologic effects of amiodarone on ocular tissues of rats were studied. Ultrastructural alterations, which are typical of human keratopathy and characteristic of drug-induced lipidosis, could be experimentally reproduced in rats by local application of amiodarone. Repeated oral administration of high drug doses induced lipidosis-like alterations in many ocular cell types, particularly in retinal pigment epithelium. It is concluded that amiodarone has the potency to induce generalized lipidosis in rats, as do several other previously investigated amphiphilic cationic drugs. It is tentatively suggested that amiodarone-induced corneal alterations in humans might equally be interpreted as part of a generalized lipidosis.
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