Hepatotoxicity flutamide

Flutamide, an antiprostate cancer drug, is another example where inhibition of ETS, primarily at complex I, is associated with hepatotoxicity [56, 57]. Nefazodone, an antidepressant, also inhibits complex I activity and was discontinued in 2004 due to idiosyncratic hepatotoxicity [58]. 

Bicalutamide is a congener of flutamide, causing less hepatotoxicity and can be given once daily. 

Flutamide causes hepatotoxicity in some 0.36% of patients, and for this reason alone it should not be used in the absence of a serious indication. Whether bulimia nervosa in women justifies its use is open to doubt, since non-pharmacological methods of treatment are available. Furthermore, bulimia nervosa in women can be associated with raised serum testosterone concentrations. In a small double-blind study of the use of flutamide, citalo-pram, a combination of the two, or placebo in 31 women over 3 months, all the active treatments reduced the tendency to binge eating (47). However, there was a moderate and reversible increase in serum transaminase activities, leading to withdrawal in two of the 19 subjects who were taking flutamide either alone or in combination. 

Flutamide (EULEXIN, EUFLEX) Nonsteroidal LH increased T increased Monotherapy Combination therapy Potency spared Breast tenderness, nausea and vomiting, diarrhea, rectal bleeding, hot flashes, cystitis, increased appetite, sleep disturbances, hepatotoxicity, anemias, hemolysis, headache, dizziness, malaise, blurred vision, anxiety, depression, decreased libido, hypertension, complications in patients with cardiovascular disease... 

Cetin M, Demirci D, Unal A, et al. Frequency of flutamide induced hepatotoxicity in patients with prostate carcinoma. Hum Exp Toxicol 1999 18 137-140. 

Bruni V, Peruzzi E, Dei M, Nanninl S, SeravalH V, Sisti G, et al. Hepatotoxicity with low- and ultralow-dose flutamide a surveillance study on 203 hyperandrogenic young females. Fertil Steril 2012 98(4) 1047-52. 

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