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Bifluranol 是氟取代的联苄类抗雄激素药物,化学名为赤型-3,3′-二氟-4,4-二羟基-α-乙基-α′-甲基-联苄,商品名:‘Prostarex’。其抗雄激素作用与己烯雌酚相似,而在大鼠,雌激素样副作用仅为己烯雌酚的1/8。本品毒性低,临床正用于治疗前列腺肥大。给狗、鼬(ferret)和大鼠口服~3H-bifluranol 50、60和200μg/kg,药物很易吸收,胆汁中放射性很高,但血中放射性始终很低。静脉给药后血药浓度2～3小时内迅速下降,4小时内大部分从胆汁排泄。药物主要经粪排出,仅很少量在尿中出现。大鼠剂量的4％(雄性)和0.7％(雌性)的~3H 转变为~3H_2O 在尿中出现,而狗和鼬尿却缺如。大鼠和鼬的呼出气体中可见微量~3H。作者认为,动物给药后吸收良好,并迅速为肝脏摄取,使血药
Bifluranol is a fluorine-substituted bibenzyl anti-androgenic chemical having the chemical name erythro-3,3’-difluoro-4,4-dihydroxy-α-ethyl-α’-methylbibenzyl, : ’Prostarex’. Its anti-androgens are similar to diethylstibestrol, whereas in rats, estrogen-like side effects are only 1/8 that of diethylstilbestrol. This product is low toxicity, clinical treatment of benign prostatic hyperplasia. Oral administration of ~ 3H-bifluranol at doses of 50, 60 and 200 μg / kg to dogs, ferrets and rats resulted in high absorption of the drug, high radioactivity in bile but low radioactivity in the blood. After intravenous administration of plasma concentration 2 to 3 hours decreased rapidly within 4 hours most of the excretion from the bile. The main excretion of drugs, only a small amount appeared in the urine. 4% (male) and ~ 3H of 0.7% (female) to ~ 3H_2O in rats appeared in urine while dogs and weasels were absent. Exhaled gas from rats and Mustela can be seen trace ~ 3H. The authors believe that the animal is well absorbed after administration, and quickly for the liver to make blood medicine