Evaluation of the phototoxic properties of some hypolipidemics in vitro: fenofibrate exhibits a prominent phototoxic potential in the UVA and UVB region.
As some fibric acid derivatives have been reported to exhibit photosensitizing effects in vivo, the antilipemic drugs fenofibrate, bezafibrate, clofibrate, and gemfibrozil were tested for their phototoxic potential in vitro by a photohemolysis test using human erythrocytes and different irradiation sources. In this system only fenofibrate revealed strong phototoxic properties, which were dependent both on the drug concentration and the irradiation doses. Above a surface dose of 40 J/cm2 UVA of an UVA (320-400 nm)-rich irradiation source or 1.6 J/cm2 UVB/0.8 J/cm2 UVA of an UVB (280-320 nm)-rich irradiation source human red blood cells were completely photohemolysed in the presence of fenofibrate. Bezafibrate- and gemfibrozil-induced photohemolysis remained beneath 10%, and clofibrate showed no phototoxicity at all. As the phototoxic potential of fenofibrate lies in the UVB and UVA range, this might be of relevance with regard to clinical photosensitivity.
Diemer
S
S
Dermatologische Klinik und Poliklinik, Ludwig-Maximilians-Universität, München, Germany.
Eberlein-König
B
B
Przybilla
B
B
D001629:Bezafibrate / Q000009:adverse effects; D002994:Clofibrate / Q000009:adverse effects; D017484:Dermatitis, Phototoxic / Q000209:etiology*; D004353:Drug Evaluation, Preclinical; D011345:Fenofibrate / Q000009:adverse effects*; D015248:Gemfibrozil / Q000009:adverse effects; D006461:Hemolysis / Q000187:drug effects / Q000528:radiation effects; D006801:Humans; D000960:Hypolipidemic Agents / Q000009:adverse effects*; D066298:In Vitro Techniques; D014466:Ultraviolet Rays / Q000009:adverse effects
D000960:Hypolipidemic Agents; D002994:Clofibrate; D015248:Gemfibrozil; D011345:Fenofibrate; D001629:Bezafibrate