PHOTOREACTIVITY AND SYSTEMIC SIDE-EFFECTS OF DRUGS Nitroaromatics (Photoreactivity of Nifedipine in vitro and in vivo ) Henk de Vries and Gerard M.J. Beijersbergen van Henegouwen Department of Medicinal Photochemistry Leiden/Amsterdam Center for Drug Research, University of Leiden P.O. Box 9502, 2300 RA Leiden, The Netherlands Key-words: Nifedipine, UVA, photodegradation, photoallergy, immunotoxicity, nitroso derivative. Abbreviations: BSA, Bovine serum albumin; GSH, glutathione; NHNIF, lactam derivative of NIF; NIF, nifedipine; NONIF, nitroso derivative of NIF; PEG, polyethylene glycol Abstract In this article reference is made to an extensive review on phototoxicity of drugs. The nitroaromatics are taken as an example and some emphasis is put on possible systemic phototoxic effects. More in detail, in vivo and in vitro experiments are described regarding nifedipine, a nitroaromatic as well. Both in vitro and in vivo with rats exposed to UVA, a lactam derivative of nifedipine is formed. From in vitro data, it is tentatively concluded that irreversible binding to biomacromolecules occurs as well.

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