Estradurin(Estracyt)治疗确诊前列腺癌或已有骨、淋巴等远处转移3例患者的观察和疗效分析,证实该药对前列腺癌有抗肿瘤作用,对已有远处转移患者能稳定病情,延长寿命,且毒、副作用不大。雌醇部分作为一个携带体使氮芥集中于前列腺内分泌受体细胞内以达到最大杀死癌细胞作用。

【药物名称】雌二醇氮芥 Estramustine 　　
【药物别名】癌腺治，依立适 Estracyt 　　
【制剂规格】胶囊：每粒150mg。粉针剂：每支150mg；300mg。 　　
【药理毒理】雌二醇氮芥是依据“受体学说”设计的药物，是以雌二醇磷酸酯为载体的氮芥类化合物，具有烷化剂和雌二醇的双重作用。根据“受体学说”、不同的专一性，甾体类激素对不同的靶器官具有不同的专一性。甾体类激素与烷化剂的结合物有可能选择性地进入激素依赖性的瘤组织中，从而减轻了烷化剂对全身的作用。这不仅发挥了甾体类激素的作用，而且也加强了烷化剂的抗癌效应，同时相应降低了烷化剂的毒副反应。 　　
【适 应 证】前列腺癌、乳腺癌、胰腺癌，对其它晚期恶性肿瘤也有疗效。

【不良反应】
（1）轻度胃肠道反应，如恶心、呕吐等：
（2）静脉给药可有暂时性骨髓抑制及血栓性静脉炎；
（3）偶有肝功能异常；
（4）罕见有乳腺肿胀、男性女性化。 　　
【相互作用】 奶类制品会影响雌二醇氮芥的吸收。 　　
【用法用量】静注：每日300～500mg溶于溶剂中静注，连用3周，然后改为每周2次；或改为口服；每日600～900mg，分2次。静脉或口服一般3～4周为1疗程，无效停用。 　　
【注意事项】附带的粉针溶剂需小心缓慢地加入雌二醇氮芥的安瓶中，并避免震动，以防止起泡沫。等渗盐水不能作为溶剂使用。

Key: Chemotherapy, Cholesterol, Degenerative diseases, Malignant, Metastatic.

Definition

Estramustine is a combination of two drugs, estradiol and mechlorethamine, that is used to slow the growth of and kill malignant cells in prostate cancer. It is also known by the brand names Emcyt and Estracyte.

Purpose

Estramustine is used in the palliative treatment of metastatic or progressive cancer of the prostate. Palliative treatment helps to relieve symptoms, but does not cure the cancer.

In the early 2000s, estramustine is also being investigated in several clinical trials evaluating its usefulness in managing asymptomatic prostate cancer patients; its effectiveness in combination with docetaxel as an alternative to radical prostatectomy; and its usefulness in increasing the effectiveness of a microtubule drug in treating prostate cancer. These studies suggest that estramustine may have beneficial applications outside the field of palliative care.

Description

Estramustine is classified as an antineoplastic drug. Estramustine is a combination of two drugs: estradiol, a potent female hormone (estrogen), and mechlorethamine, a nitrogen mustard. Its action is to decrease testosterone, increase estrogen level, and suppress cell growth. Estramustine is approved by the United States Food and Drug Administration (FDA) for the palliative treatment of metastatic or progressive cancer of the prostate.

Recommended Dosage

As with many cancer-fighting drugs, the dose of estramustine a patient receives is individualized and depends on the patient's body weight and general health, as well as what other chemotherapy drugs are being used. A standard dose of estramustine is 14 mg per kg of body weight per day, divided into three or four doses. This is equivalent to one 140 mg capsule for each 22 lbs (10 kg) of body weight. It takes one to three months for estramustine to start to work. The therapy is continued as long as the patient has a favorable response. Some patients have successfully taken this drug for as long as three years.

Precautions

Estramustine should not be used by men who have a history of problems with blood clots, a blood clotting disorder, or allergic reactions to estrogen or nitrogen mustard.

Estramustine must be taken more than one hour before or more than two hours after meals. It should not be taken with dairy products, calcium supplements, of any food that is high in calcium.

Patients taking estramustine should avoid having any vaccinations while taking the drug, and should consult their doctor immediately if exposed to chicken pox or measles, as this drug may make them more susceptible to these diseases.

Side Effects

Nausea and vomiting can occur within 2 hours of taking estramustine. This side effect is mild and patients will respond to antiemetics to control the nausea and vomiting. Diarrhea and flatulence can occur while taking this drug. Patients taking estramustine also have an increased risk of developing blood clots, congestive heart failure, and heart attacks, although these side effects are rare. Therefore, men with a history of blood clots and heart disease require frequent monitoring while receiving this drug. Estramustine also decreases the glucose (sugar) tolerance in people with diabetes, and frequent blood sugar monitoring is recommended in this patient population. Blood pressure may also be increased with estramustine, and monitoring of blood pressure is recommended, especially in patients with a history of high blood pressure. Men receiving estramustine may also experience enlargement of their breasts due to the estrogen component in the drug combination. Patients may also experience decreased sexual drive, although this side effect is reversible. If sexually active, the patient should use a contraceptive method (even if he is impotent) prior to initiating therapy, because estramustine may reverse impotency while on the drug. Estramustine may also cause genetic mutations. Therefore, use of contraceptive measures is advisable. Other side effects include lethargy, rash, itching, dry skin, easy bruising, flushing, and thinning hair. If any of the above side effects occur, patients should alert their physician to these side effects immdediately.

Serious side effects that require immediate medical attention include:

sudden or severe headaches
sudden shortness of breath or difficulty breathing
increased weight gain or swelling of the feet or legs
pain in the chest
sudden pain or cramping in the legs or calves
weakness or numbness in the legs or arms
Interactions

Dairy products and other foods containing calcium interfere with the absorption of estramustine. Prior to treatment, patients should notify their physician about any medications they are taking and of any known allergies.

Patients taking estramustine should not use tobacco products, as smoking causes the blood vessels to narrow and may increase the risk of circulation problems during treatment with estramustine..

Estramustine intensifies the effects of vinblastine, another anticancer drug.