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 部分中文他莫昔芬处方资料（仅供参考）
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    他莫昔芬也叫枸橼酸他莫昔芬（tamoxifen），英文商品名为Nolvadex®。其为一种选择性雌激素受体调节剂（SERM）。这种药物能干扰雌激素（estrogen）的某些活动，模拟其它雌激素作用。他莫昔芬用于治疗某些乳腺癌和卵巢癌。目前，科研人员正在比较他莫昔芬与雷洛昔芬（raloxifene）（另一种SERM），比较它们在降低高危人群的乳腺癌发病率方面的作用。 　　

药理作用机制
    该药为雌二醇竞争性拮抗剂，能与乳腺细胞的雌激素受体结合，不刺激转录或作用微弱。药物-受体复合物不易解离，组织受体的循环应用，也是作用机制之一。他莫昔芬能上调转化生长因子β生成，此因子减少与恶性肿瘤的发展有关。还对蛋白激酶C有特异性抑制作用。这些作用都对依赖雌激素才能继续生长的肿瘤细胞有抑制作用。多用于绝经期前雌激素（ER+）和孕激素受体（PR+）呈进行性发展的乳癌的治疗。他莫昔芬对血浆脂代谢、子宫内膜和骨的作用则仍是雌激素性质，不呈拮抗作用。他莫昔芬的抗骨质疏松作用也可能与上调转化生长因子β有关，因为此因子能够控制成骨细胞和破骨细胞间的平衡。
    可以作为基因敲除基础的一个研究工具，可以构建条件敲除小鼠模型，调节特定基因表达表达或不表达。 　　

药动学 　　
    本药口服20mg后，4～7h达血药峰浓度，为0.14μg/ml。给药4天或更长时间后可由于肠肝循环出现第二次高峰。半衰期β相大于7天，α相为7～14h。给药后4～10周，客观体征有改善，如果有骨转移，数月才有效。单次剂量抗雌激素作用约持续数周。本药在肝内代谢，主要代谢物为N-去甲基三苯氧胺和4-羟基三苯氧胺，也有与雌激素受体结合的作用。本药大部分以结合物形式由粪便排出，少量从尿中排出。本品母体化合物清除半衰期为5～7天，代谢产物氮-去甲基他莫昔芬为14天。 　　

适应证 　　
1.乳腺癌术后辅助治疗，用于雌激素受体阳性者，特别是绝经后年龄60岁以上的患者疗效较好。
2.晚期乳腺癌，或治疗后复发者。对皮肤、淋巴结及软组织转移疗效较好。子宫内膜癌。 　　

禁忌证 　　
1.孕妇及有血栓栓塞性疾病者。
2.有深部静脉血栓史者。
3.有肺栓塞史者。 　　

注意事项 　　
1.用药前检查有视力障碍、肝肾功能不全者慎用。
2.对长期服用本品并有血栓栓塞危险的患者，治疗期间应定期检查血象。如有骨转移，在治疗初期需定期检查血钙。在用本品进行2年以上长期治疗期间，要定期对肝功能进行检测。
3.当出现异常的阴道出血时，应立即就诊，并进行全面检查。阴道大量出血时应停药。
4.用本品治疗的患者有增加子宫内膜癌发生的危险，所以应当进行仔细的妇科检查。
5.使用本品可出现突发性卵巢功能性囊肿和月经过多及不规则子宫出血。因此，若绝经前必须使用本药，应同时服用抗促性腺激素药物 　　

不良反应 　　
1.胃肠道反应：食欲减退、恶心、呕吐、腹泻。
2.继发性抗雌激素作用：面部潮红、外阴瘙痒、月经失调、闭经、白带增多、阴道出血等。
3.神经精神症状：头痛、眩晕、抑郁等。
4.大剂量长期应用可导致视力障碍，如白内障。
5.骨髓抑制：少数患者可有一过性白细胞和血小板减少。
6.其他：皮疹、脱发、体重增加、肝功有异常等。

Benefits of tamoxifen
.Cell with estrogen receptors blocked by tamoxifen and helper proteins.
Larger Version...Since its approval in 1998, tamoxifen has been used to treat millions of women and men diagnosed with hormone-receptor-positive breast cancer. While an aromatase inhibitor is the first hormonal therapy medicine choice for post-menopausal women, tamoxifen is the first choice for pre-menopausal women and is still a good choice for post-menopausal women who can't take an aromatase inhibitor.

Tamoxifen can:
reduce the risk of breast cancer coming back by 40% to 50% in post-menopausal women and by 30% to 50% in pre-menopausal women
reduce the risk of a new cancer developing in the other breast by about 50%
shrink large, hormone-receptor-positive breast cancers before surgery
slow or stop the growth or advanced (metastatic) hormone-receptor-positive breast cancer in both pre- and post-menopausal women

lower breast cancer risk in women who have a higher-than-average risk of disease but have not been diagnosed
Tamoxifen offers other health benefits that aren't related to treating cancer. Because it's a SERM, it selectively either blocks or activates estrogen's action on specific cells. While tamoxifen blocks estrogen's action on breast cells, it activates estrogen's action in bone and liver cells. So tamoxifen can:
help stop bone loss after menopause
lower cholesterol levels

Side effects of tamoxifen
Tamoxifen's selective estrogen activation effects can cause some serious side effects, including blood clots, stroke, and endometrial cancer. If you and your doctor are considering tamoxifen as part of your treatment plan, tell your doctor if you smoke or have a history of blood clots or heart attack. If you're taking tamoxifen, call your doctor immediately if you have any of these symptoms:
abnormal vaginal bleeding or discharge
pain or pressure in the pelvis
leg swelling or tenderness
chest pain
shortness of breath
weakness, tingling, or numbness in your face, arm, or leg
difficulty speaking or understanding
vision problems
dizziness
sudden severe headache

The most common side effects of tamoxifen are:
increased tumor or bone pain
hot flashes
nausea
fatigue
mood swings
depression
headache
hair thinning
constipation
dry skin
loss of libido

Hot flashes or night sweats from taking tamoxifen can be troubling. But a 2008 British study suggests that women who experienced hot flashes and night sweats while taking hormonal therapy medicine were less likely to have the breast cancer come back (recur). Knowing that this side effect might indicate a reduced risk of the cancer coming back may help some people stick with treatment despite the side effects.

Some women on tamoxifen have reported memory problems while taking the medicine. While no definitive results are available yet, the ongoing Co-STAR (Cognition in the Study of Tamoxifen and Raloxifene) trial is looking at the effects tamoxifen and Evista (chemical name: raloxifene), another SERM, have on memory and thinking.

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