Bicalutamide is a pure nonsteroidal antiandrogen. It is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analogue for the treatment of Stage D 2 metastatic carcinoma of the prostate.
藥理
Its long half-life enables once-daily dosing, an advantage over flutamide; it may also be less toxic than flutamide.
藥動學
Oral absorption is slow from the GI tract, with peak serum levels occurring 16 hours after doses of 50 mg; significant accumulation (tenfold) occurs with repeat daily doses.
禁忌症
Hypersensitivity to bicalutamide; pregnancy; women
懷孕分類
X
哺乳分類
副作用
Bicalutamide should not be used in women, especially in women who are or may become pregnant. Severe liver injury resulting in death has been reported. The predominant adverse effects of bicalutamide are hot flashes, breast tenderness, gynecomastia, pain (general, back, pelvic) asthenia and constipation. Loss of libido and impotence are relatively infrequent. Bicalutamide is not peripherally selective; increased luteinizing hormone and serum testosterone levels occur during therapy.