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三苯氧胺(tamoxifen)具有拮抗雌激素受体的功能,在靶器官(包括一些肿瘤细胞)中竞争雌激素受体。乳癌是雌激素依赖的。胞浆中激素受体激活后,以雌激素(配基)—受体复合物的形式向细胞核内移动。三苯氧胺在进入细胞后,与胞浆中雌激素受体相结合,转移到细胞核内后停留时间延长。可能由于它的 t1/2长,或与受体形成的复合物不被破坏,从而抑制胞浆中雌激素受体的循环。对手术后乳癌病人防止癌肿的复发及对晚期乳癌病人的治疗中,均取得显著的疗效。乳癌病人在服药后,药物在休内广泛分布。口服药物3小时后,血浆药物浓度测得的
Tamoxifen antagonizes estrogen receptors and competes for estrogen receptors in target organs, including some tumor cells. Breast cancer is estrogen-dependent. Activation of the hormone receptor in the cytoplasm, the estrogen (ligand) - receptor complex in the form of movement to the nucleus. Tamoxifen, after entering the cell, binds to the estrogen receptor in the cytoplasm, and then stays in the nucleus for extended periods of time. It may be due to its t1 / 2 long, or complexes with the receptor is not destroyed, thereby inhibiting the circulating estrogen receptors in the cytoplasm. On postoperative breast cancer patients to prevent recurrence of cancer and treatment of advanced breast cancer patients, have achieved significant results. Breast cancer patients taking medicine, the drug widely distributed during the break. After 3 hours of oral medication, plasma drug concentrations were measured