药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201883001403532.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文替TAMOXIFENO处方资料(仅供参考)
药品名称(包括商品名、通用名)
他莫昔芬
用法用量
①乳腺癌等肿瘤:开始10mg,2次/d,口服。如1个月内无效,可增至20mg,2次/d。若80mg/d仍无效,再增剂量亦无意义;②不孕症:于月经周期第2~5天服10mg,2次/d,如果需要;以后周期可用至40mg,2次/d。
药理作用
本品是三苯乙烯非甾体抗雌激素类药物的典型代表。它能与雌二醇竞争与雌激素受体结合。当其与雌激素受体结合后,可诱导改变受体的三维空间形状,阻止受体与DNA上的雌激素反应成分相结合,使转录等过程不能进行,从而抑制激素依赖性乳腺肿瘤细胞的生长。近来研究表明,本品的抗癌作用可能还有其他机制,如:诱导癌细胞的周围细胞分泌生长抑制因子TGF-β,减少周围组织局部产生胰岛素样生长因子(IGF-1),该因子是一种乳腺癌细胞的胰生长因子。此外,本品还具有抑制蛋白激酶C和钙调蛋白依赖性cAMP磷酸二酯酶的作用,也能保护细胞膜和脂蛋白免受氧化损伤。除与雌激素受体作用外,本品也作用于其他生物大分子,尤其是对钙调素有拮抗作用,可延缓停经妇女骨质疏松的发生。本品还可降低血清胆固醇,降低低密度脂蛋白,减少心肌梗死发生的危险。本品为雌激素拮抗剂,能与雌二醇竞争靶细胞内雌激素受体的结合,从而阻断雌二醇的作用。此外,还能抑制细胞生长因子的产生和释放。
适应症
用于治疗晚期播散性乳腺癌,是停经后晚期乳腺癌的首选药物。本品对晚期卵巢癌、宫体癌等实体瘤也有效。还可用于晚期前列腺癌、晚期黑色素瘤、晚期肾癌、晚期胰腺癌。最近开始治疗脑瘤和肝癌。对绝经期妇女的疾病如乳腺癌、骨质疏松和心脏病等有预防作用。也可用其诱发排卵作用治疗不孕症。主要用于早期乳腺癌手术后的辅助治疗及晚期乳腺癌的姑息治疗,对雌激素受体水平高者疗效好,水平低者疗效很差。还用于治疗另一些恶性肿瘤:如卵巢癌、子宫内膜癌、肾癌和黑色素瘤。此外,亦用于无排卵性不育症。
不良反应
常见的不良反应有面部潮红、恶心、呕吐等,发生率约25%。较少见的有月经不规则、阴道出血、白带增多、外阴瘙痒和皮炎等。高剂量长期应用可致视力障碍,故眼药期间应定期作眼科检查。本品尚有部分雌激素激动作用,长期应用可引起继发性子宫内膜肿瘤。接受20mg/d治疗2年的患者,其肿瘤发生率至少比未用本品的对照组高2倍以上。因此,接受本品治疗者至少应每年进行盆腔检查和其他有关检查。本品还能增加其栓形成的危险。
制剂
片剂:每片含枸椽酸他莫昔芬15.2mg相当于他莫昔芬10mg。
注意事项
有月经的妇女慎用,以免引起月经不规则和卵巢囊肿增大,孕妇禁用。
Pharmaceutical name (including trade name, common name)
Tamoxifen
Usage and Usage
1 Tumors such as breast cancer: start 10mg, 2 times / d, orally. If it is invalid within 1 month, it can be increased to 20mg, 2 times / d. If 80mg / d is still invalid, it is meaningless to increase the dose; 2 infertility: 10mg, 2 times / d on the 2nd to 5th day of the menstrual cycle, if necessary; the later cycle can be used to 40mg, 2 times / d.
Pharmacological action
This product is a typical representative of tristyrene non-steroidal anti-estrogen drugs. It competes with estradiol for binding to the estrogen receptor. When it binds to the estrogen receptor, it can induce changes in the three-dimensional shape of the receptor, prevent the receptor from binding to the estrogen-responsive component on the DNA, and prevent transcription and other processes from proceeding, thereby inhibiting hormone-dependent breast tumor cells. Growing. Recent studies have shown that the anti-cancer effect of this product may have other mechanisms, such as: the peripheral cells that induce cancer cells secrete the growth inhibitory factor TGF-β, and reduce the local production of insulin-like growth factor (IGF-1) in the surrounding tissue. A pancreatic growth factor for breast cancer cells. In addition, this product also inhibits protein kinase C and calmodulin-dependent cAMP phosphodiesterase, and also protects cell membranes and lipoproteins from oxidative damage. In addition to the role of estrogen receptors, this product also acts on other biological macromolecules, especially antagonizing calmodulin, which can delay the occurrence of osteoporosis in menopausal women. This product can also lower serum cholesterol, reduce low-density lipoprotein, and reduce the risk of myocardial infarction. This product is an estrogen antagonist that competes with estradiol for the binding of estrogen receptors in target cells, thereby blocking the action of estradiol. In addition, it also inhibits the production and release of cell growth factors.
Indications
For the treatment of advanced disseminated breast cancer, it is the drug of choice for advanced breast cancer after menopause. This product is also effective for advanced ovarian cancer, uterine body cancer and other solid tumors. Can also be used for advanced prostate cancer, advanced melanoma, advanced kidney cancer, advanced pancreatic cancer. Recently, treatment of brain tumors and liver cancer has begun. It has preventive effects on diseases of menopausal women such as breast cancer, osteoporosis and heart disease. It can also be used to induce ovulation to treat infertility. It is mainly used for adjuvant therapy after early breast cancer surgery and palliative treatment of advanced breast cancer. It has good curative effect on patients with high estrogen receptor level, and low efficacy is low. Also used to treat other malignant tumors: such as ovarian cancer, endometrial cancer, kidney cancer and melanoma. In addition, it is also used for anovulatory infertility.
Adverse reactions
Common adverse reactions include facial flushing, nausea, and vomiting, with an incidence of about 25%. Less common are irregular menstruation, vaginal bleeding, increased vaginal discharge, genital itching and dermatitis. High-dose long-term application can cause visual impairment, so eye examination should be done regularly during eye drops. This product still has some estrogen stimulating effects, and long-term application can cause secondary endometrial tumors. Patients who received 20 mg/d for 2 years had a tumor incidence that was at least 2 times higher than that of the control group that did not use this product. Therefore, those who receive this product should have at least annual pelvic examinations and other related examinations. This product can also increase the risk of its formation.
Formulation
Tablets: Each tablet contains 15.2 mg of tamoxifen citrate equivalent to 10 mg of tamoxifen.
Notes
Women with menstruation should be used with caution to avoid irregular menstruation and enlarged ovarian cysts, and pregnant women should be banned.
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201883001403532.pdf)的“原文Priscribing Information”为准 ---------------------------------------------------------------
2011-4-7更新 |