简介：

部分中文他莫昔芬处方资料（仅供参考）
【药品类别】激素类及抗激素类抗肿瘤药
【性状】本品为白色片。
【药理毒理】他莫昔芬为非固醇类抗雌激素药物。其结构与雌激素相似，存在Z型和E型两个异构体。两者物理化学性质各异，生理活性也不同，E型具有弱雌激素活性，Z型则具有抗雌激素作用。如果乳癌细胞内有雌激素受体（ER），则雌激素进入肿瘤细胞内，与其结合，促使肿瘤细胞的DNA和m-RNA的合成，刺激肿瘤细胞生长。而他莫昔芬Z型异构体进入细胞内，与ER竞争结合，形成受体复合物，阻止雌激素作用的发挥，从而抑制乳腺癌细胞的增殖。
【药代动力学】本品为口服，吸收迅速。口服20mg后6～7.5小时，在血中达最高浓度，T1/2?:7～14小时，4天或4天后出现血中第二高峰，可能是肝肠循环引起，T1/2?大于7天。其排泄较慢，主要从粪便排泄，约占4/5，尿中排泄较少，约1/5。口服后13天时仍可从粪便中检测得到。
【适应症】
1、治疗女性复发转移乳腺癌；
2、用作乳腺癌手术后转移的辅助治疗，预防复发。
【用法用量】
每次10mg口服，每天2次，也可每次20mg,每天2次。
【不良反应】
治疗初期骨和肿瘤疼痛可一过性加重，继续治疗可逐渐减轻。少数病人有不良反应。其中胃肠道反应食欲不振，恶心，呕吐，腹泻；生殖系统：月经失调，闭经，阴道出血，外阴搔痒，子宫【内膜增生，内膜息肉和内膜癌；皮肤：颜面潮红，皮疹，脱发。骨髓：偶见白细胞和血小板减少；肝功：偶见异常；眼睛：长时间（17个月以上）大量（每天240～320mg）使用可出现视网膜病或角膜浑浊。罕见的需引起注意的不良反应：精神错乱，肺栓塞（表现为气短），血栓形成，无力，嗜睡。
【禁忌症】
有眼底疾病者禁用。
【注意事项】
有肝功能异常者应慎用。如有骨转移，在治疗初期需定期查血钙。
孕妇及哺乳期妇女用药 对胎儿有影响，妊娠，哺乳期妇女禁用。
【药物相互作用】
雌激素可影响本品治疗效果；抗酸药，西米替丁，雷尼替丁等在胃内改变pH值，使本品肠衣提前分解，对胃有刺激作用。
【贮藏】
遮光、密闭保存.
Nolvadex(Tamoxifen Citrate)
Nolvadex and Gynocomastia
This drug is used as a first line defense against breast cancer. In the late 80s, Dan Duchaine speculated that it could also be used by
bodybuilders to halt the development of another type of tumor in the mammary gland, Gynocomastia. He introduced this find to the Steroid-using-community in his "Contest Prep" issue of the UnderGround Steroid Handbook Update Newsletters (the contest prep-issue was actually 3 issues in one, for those who had a subscription to the newsletter).
Nolvadex is commonly referred to in quite a few ways: as a SERM(Selective Estrogen Receptor Modulator), as an anti-estrogen (that is actually incorrect, as we will later see), and finally as a triphenylethylene. I happen to stick with calling Nolvadex a SERM, because out of my three options, it happens to be correct (as we know that calling it an anti-estrogen is incorrect), and pronouncable (as we know that I have no idea how to say "triphenylethylene"). Selective estrogen receptor modulators (SERMs) act as either estrogen receptor agonists or antagonists in a tissue-selective manner, lets see what that means to us& Nolvadex actually has quite a few applications for the steroid using athlete.
First and foremost, its most common use is for the prevention of gynocomastia. Nolvadex does this by actually competing for the receptor site in breast tissue, and binding to it. Thus, we can safely say that the effect of tamoxifen is through estrogen receptor blockade of breast tissue (1), especially since total body estradiol increases with use of tamoxifen. Clearly, if you are on a cycle which includes steroids which convert to estrogen, you may want to consider nolvadex as a good choice to run along side them.
Nolvadex Cycle
Nolvadex, however, is not the most potent ancillary compound we can use on a cycle, but it is probably the safest considering it doesnt
actually reduce estrogen in your body keeping some estrogen floating around could have many benefits on muscle growth, as well. Estrogen
is also important for a properly functioning immune system, and not only that, but your lipid profile (both HDL and LDL) should also show marked improvement with administration of tamoxifen (4). Many bodybuilders actually use this stuff during their cycle for the health benefits provided by it. If, however, you are preparing for a bodybuilding contest, you need to use something which will suck most(if not all) of the estrogen out of your body. I am speculating that you may be able to use Nolvadex for the majority of a contest prep cycle, to keep yourself relatively healthy, and then switch over to Letrozole for the last 8 weeks.
Nolvadex also has some important features for the steroid using athlete. In hypogonadic and infertile men given nolvadex, increases in the serum levels of LH, FSH, and most importantly, testosterone were all observed (2)(3). The best (rough) estimate I can give you from my research is that 20mgs of Nolvadex will raise your testosterone levels about 150% (5)...and this would of course greatly aid post-cycle-recovery.
What this means to us is that if you take Nolvadex after a cycle, when you are trying to raise your levels of testosterone, LH, and FSH back to normal, it will greatly aid recovery. In fact, if I were limited to just one compound to aid me in post-cycle-recovery, Nolvadex would be my choice. If you want a comparison, it would require 150mgs of Clomid to accomplish that type of elevation in testosterone, but nolvadex also significantly increased the LH (Leutenizing Hormone) response to LHRL (5), after 6 weeks.
Some of the more harsh ancillary compounds available today will give you a more "dry" look that nolvadex cant, but nolvadex is simply
safer to use in long (over 16 week) cycles.
Nolvadex Side Effects
Unfortunately, Nolvadex isnt perfect. Anecdotally, it has been linked to reduced gains in some bodybuilders. This isnt due, as
previously thought, to its reducing estrogen levels (which it doesnt), but rather to its ability to possibly reduce IGF (Insulin-like-Growth-Factor) levels, which are important for muscle growth.
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