【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-D

Brand Names: Nolvadex-D, Nolvadex, Tamofen, Tamone, Tamotec
Generic Name: Tamoxifen Citrate
Manufacturer: Astra Zeneca

How does Nolvadex-D work?
Nolvadex D tablets contain the active ingredient tamoxifen citrate, which is a type of medicine known as an 'anti-oestrogen'. (NB. Tamoxifen is also available without a brand name, ie as the generic medicine.) Tamoxifen is mainly used to treat women with breast cancers that respond to the female sex hormone, oestrogen.

Most breast cancers are sensitive to oestrogen, and their growth is increased in the presence of this hormone. Oestrogen binds to oestrogen receptors on the breast cancer cells and causes changes within the cells that result in faster growth of the cancer. Breast cancers that are sensitive to oestrogen are called oestrogen receptor positive cancers.

Tamoxifen works by blocking the oestrogen receptors, thereby blocking the effect of oestrogen on the cancer. This starves the breast cancer cells and stops them from growing.

Tamoxifen helps prevent breast cancer from spreading to other areas of the body and also reduces risk of developing cancer in the other breast.

Tamoxifen is also used in the treatment of female infertility that is caused by problems with ovulation. Again, it acts by blocking oestrogen receptors, this time in a part of the brain called the hypothalamus. The effect of this is an increase in the levels of the hormones that control the development and release of an egg. These hormones are released from the pituitary gland and are known as follicle stimulating hormone (FSH) and luteinising hormone (LH). FSH stimulates the ovaries and LH causes the release of an egg from the ovaries (ovulation).

In the normal menstrual cycle, oestrogen acts on receptors in the hypothalamus after ovulation. This causes the pituitary gland to stop releasing FSH and LH. As tamoxifen blocks the oestrogen receptors in the hypothalamus, it prevents this action of oestrogen. FSH and LH levels therefore increase, which increases the chances of egg development and ovulation.

What is Nolvadex-D used for?
* Breast cancer
* Infertility in women caused by failure of ovulation

Warning!
* As this medicine may potentially cause harm to a developing baby, it should not be used during pregnancy. Women who have not yet passed the menopause should use a non-hormonal method of contraception to prevent pregnancy both during, and for two months following, treatment with this medicine.

* Tamoxifen is associated with a small increase in the risk of endometrial cancer. The benefits of taking tamoxifen to treat breast cancer outweigh this risk, however, to minimise the risk you should consult your doctor if you experience any abnormal gynaecological symptoms during or after treatment, so that they can be investigated. Symptoms to report include vaginal bleeding, menstrual irregularities, vaginal discharge, or symptoms such as pelvic pain or pressure. Consult your doctor for further information.

* Tamoxifen is associated with an increased risk of abnormal blood clots in the blood vessels (for example deep vein thrombosis or pulmonary embolism), particularly during periods of immobilisation and following surgery. The benefits of taking tamoxifen to treat breast cancer outweigh this risk, however you should consult your doctor immediately if you experience any of the following symptoms during treatment: stabbing pains and/or unusual swelling in one leg, pain on breathing or coughing, sudden breathlessness or sudden severe chest pain. Consult your doctor for further information.

* Your doctor may want you to stop taking this medicine prior to any planned surgery or period of prolonged immobility. Discuss this with your doctor.

Use with caution in
* Breast cancer patients with a personal or family history of abnormal blood clots in the veins
* Breast cancer patients who are also receiving chemotherapy (see below for more information)
* Severe obesity
* Smokers
* Life long inherited blood diseases which can cause a variety of symptoms, including mental health problems (porphyrias)

Not to be used in
* Infertility patients with a personal or family history, or genetic risk, of abnormal blood clots in the veins with no known cause
* Pregnancy
* Breastfeeding

This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.

If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.

Pregnancy and Breastfeeding
Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.

* This medicine must not be used during pregnancy as it may potentially cause harm to a developing baby. Pre-menopausal women should use a non-hormonal method of contraception to prevent pregnancy both during, and for two months following, treatment with this medicine.

* As there is no safety information available, the manufacturer does not recommend the use of this medicine when breastfeeding. Alternatively, if this medicine must be used, the mother should not breastfeed. Seek medical advice from your doctor.

Side effects
Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect.

* Hot flushes
* Vaginal bleeding or discharge
* Itching of the external female genitalia (pruritus vulva)
* Suppression of menstrual periods in pre-menopausal women receiving tamoxifen for breast cancer
* Stimulation of tumour growth
* Headache
* Light-headedness
* Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain
* Fluid retention
* Hair loss (alopecia)
* Blood disorders
* Visual disturbances
* Liver disorders
* Increased risk of abnormal blood clots within the blood vessels (thromboembolic disorders)
* The presence of tissue similar to the lining of the uterus at other sites in the pelvis (endometriosis)
* Cancerous changes in the endometrium (lining of the womb)
* Fibroids in the womb (uterus)
* Severe blistering skin reaction affecting the tissues of the eyes, mouth, throat and genitals (Stevens-Johnson Syndrome)
* Severe swelling of lips, face or tongue (angioedema)

The side effects listed above may not include all of the side effects reported by the drug's manufacturer.

For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.

How can this medicine affect other medicines?
You should tell your doctor or pharmacist what medicines you are using, particularly those listed below, before you start treatment with this medicine. This includes those bought without a prescription and herbal medicines. Likewise, check with your doctor or pharmacist before starting any new medicines while you are taking this medicine, so they can check that the combination is safe.

Medicines that contain oestrogens, for example oral contraceptives or HRT, should not be used in combination with this medicine, as they will oppose its action.

There may be an increased risk of abnormal blood clots in the veins (thromboembolism) if tamoxifen is used in combination with cytotoxic chemotherapy medicines. Your doctor may prescribe you a medicine to prevent blood clots if you are having chemotherapy with tamoxifen.

Tamoxifen decreases the removal of the anticoagulant medicines nicoumalone and warfarin from the body and hence increases their anti-blood-clotting effect. Women taking anticoagulants in combination with tamoxifen should have their blood-clotting times regularly monitored, and your doctor may need to reduce the dose of your anticoagulant.