【药品名称】：诺雷得 Zoladex
【药物别名】：戈舍瑞林；goserelin
【药物类别】：抗肿瘤激素类
诺雷德是一种可在体内逐渐进行生物降解的多聚缓释植入剂。无菌、白色或乳白色柱形，含醋酸戈舍瑞林（相当于3.6毫克戈舍瑞林），置于一注射器中，单剂量给药。
【药效学】：
作用方式：诺雷得(D-Ser (But)6 Azgly10 LHRH) 是促黄体生成素释放激素的一种类似物，长期使用诺雷得抑制脑垂体促黄体生成素的合成，从而引起 男性血清睾丸酮和女性血清雌二醇的下降，停药后这一作用可逆，初期用药时诺雷得同其它LHRH激动剂一样，可暂时增加男性血清睾丸酮和女性血清雌二醇的浓度。在接受诺雷得治疗的早期阶段，一些女性可出现不同程度的阴道出血，持续时间和出血量各有不同。这种现象为雌激素水平下降所导致并可自动停止。
男性病人在第一次注射此药后21天左右血清睾丸酮浓度下降至去势水平，并在以后的治疗中维持此浓度，这可使大多数病人的前列腺肿瘤消退，症状有所改善。
女性患者在初次给药后21天左右血清中雌二醇浓度受到抑制，并在以后每28天的治疗中维持在绝经后水平。这种抑制与激素依赖性的乳腺癌、子宫肌瘤和子宫内膜异位症相关。可导致子宫内膜变薄及多数病人闭经。
诺雷得和铁剂伍用可使贫血的子宫肌瘤患者产生闭经并改善血红蛋白浓度及相关的血液学参数。诺雷德和铁制剂伍用与单独铁剂疗法相比较，前者血红蛋白浓度的增高较后者多1g/dl。
在用LHRH类似物治疗期间产生停经且停止治疗后未恢复月经的患者很少见。
【药动学】：
诺雷得具有几乎完全的生物利用度，每四周用药一次，在无组织蓄积的情况下保持有效的血药浓度，诺雷德与血浆蛋白的结合能力较弱，在肾功能正常情况下血浆清除半衰期为2－4小时，对肾功能不全的病人其半衰期将会增加，此改变在每月一次的治疗中影响很小，故不需要调整剂量，在肝功能不全的病人中其药代动力学无明显变化。
【适应证】：
前列腺癌：
1.诺雷得适用于可用激素治疗的前列腺癌。
2.乳腺癌：适用于可用激素治疗的绝经前期及绝经期妇女的乳腺癌。
3.子宫内膜异位症：缓解症状包括减轻疼痛并减少子宫内膜损伤的大小和数目。
4.使子宫内膜变薄：在刮宫术或内膜切除术之前，用诺雷德使子宫内膜 变薄。
5.子宫肌瘤：术前与补铁药伍用可使患有贫血的肌瘤病人的贫血状况得到改善。
【用法与用量】
成人：
-- 在腹部皮下注射诺雷得3.6mg一支，每28天一次。
-- 肾功能不全者不需调整剂量。
-- 肝功能不全者不需调整剂量。
-- 老年病人不需调整剂量。
-- 子宫内膜异位症的治疗不应超过六个月，因为目前尚没有长期治疗的临床数据，考虑到有关骨质丢失的问题，应避免重复疗程。
-- 用于使子宫内膜变薄：每隔四周注射一支诺雷德共注射两次。手术在第二次注射后两周内进行。
-- 对由于子宫肌瘤导致贫血的妇女，手术前三月之内给予诺雷德3.6mg及补铁治疗。
儿童：
-- 诺雷德不推荐用于儿童。
【禁忌证】：
已知对诺雷得或LHRH类似物过敏的病人不可使用诺雷得。
妊娠期及哺乳期妇女不可使用诺雷德。
【注意事项】：
由于诺雷得的安全性及有效性在儿童中尚未论证，故儿童病人不推荐使用诺雷德。
男性：
对有发展为尿道阻塞或脊髓压迫危险的男性病人 诺雷得应慎用，而且在 治疗的第一个月期间应密切监护病人，如果因尿道梗阻而引起脊髓压迫或肾脏损伤并恶化，则应给予适当治疗。
女性：
妇女使用LHRH激动剂可能引起骨密度丢失，从目前所得到的诺雷得研究数据表明六个月疗程结束时椎骨矿物质密度平均下降4.6％，再经六个月后逐渐恢复到只比基值低2.6％。
对已知有骨代谢异常的妇女使用 诺雷德时应注意。 诺雷德可引起子宫颈阻抗增加，因而可导致扩宫困难。
目前尚无用诺雷德治疗子宫内膜异位症超过六个月的临床数据。
【妊娠和哺乳】
虽然动物生殖毒理研究没有提供致畸的证据，但如果在妊娠期间使用LHRH激动剂理论上有流产或致畸的危险性，因而在妊娠期间不要使用。对于可能妊娠的妇女在使用本药前应先仔细检验以排除妊娠可能，在治疗中应使用非激素的避孕方法，直到治疗后月经恢复为止。
哺乳期间不推荐使用诺雷得。
对驾驶和机械操作者的影响
无证据表明诺雷德对上述能力有损害。
【不良反应】：
一般的：
过敏反应发生率很低，一些过敏现象已见报道。关节痛已见报道。有报道出现皮疹，多为轻度，不需中断治疗即可恢复。
血压的变化，服用诺雷得的病人，发生低血压或高血压反应的病例已偶见报道。这种变化通常很短暂，继续治疗或停止治疗后均可恢复，很少需要停药及其它药物治疗。
偶然出现的局部反应包括在注射位置上有轻度瘀血。
男性：
男性病人副作用包括潮红和性欲下降，少有必需中断治疗，偶见乳房肿胀和触痛，给药初期前列腺癌症病人可能有骨骼疼痛暂时性加重，应对症处理。尿道梗阻和脊髓压缩的个别病例也曾有报道。
女性：
女性病人副作用有潮红，多汗及性欲下降，无需中止治疗；也曾观察到头痛，情绪变化如抑郁，阴道干燥及乳房大小的变化。治疗初期乳腺癌的病人会有症状的加剧，应按症状进行处理。子宫肌瘤患者可见肌瘤退行性变性。在治疗初期，有骨转移的乳腺癌患者很少发展为高钙血征。
【药物过量】
人体尚无超剂量用药的试验。动物试验表明使用超剂量的诺雷得时除对性激素浓度和生殖道的预想的作用外无其它影响，如发生超量使用的情况，应对症处理。
与处方有关的临床前安全资料
长期重复注射诺雷得之后曾在雄性鼠中观察到良性脑垂体肿瘤发病率上升的现象，这一发现与对雄鼠阉割后所得结果相似，尚未发现与人体使用的经验有任何关联。 在小鼠体内，长期重复使用几倍人用的剂量下在消化道内产生了组织结构的变化，这可由胃部幽门区域良性增生和胰岛细胞增殖来证明。这些事实与临床的关系尚不清楚。
【储藏】：储存在25℃以下。
【生产单位】：阿斯利康

【原产地英文商品名】ZOLADEX IMPLANT-10.8mg/Implant Syrn
【原产地英文药品名】GOSERELIN ACETATE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·诺雷德-10.8毫克/支
·诺雷德-3.6毫克/支
【中文参考药品译名】戈舍瑞林
【生产厂家中文参考译名】阿斯利康
【生产厂家英文名】AstraZeneca

Brand Name Zoladex Options - Manufacturer: AstraZeneca

Zoladex Description

Goserelin is used in men to treat prostate cancer. It is used in women to treat certain breast cancers or a certain uterus disorder (endometriosis). It is also used in women to thin the lining of the uterus (endometrium) in preparation for a procedure to treat abnormal uterine bleeding. Talk to your doctor about the risks and benefits of treatment.

Zoladex Directions

Read the Patient Information Leaflet if available from your pharmacist before you start using goserelin and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
This medication is an implant that slowly releases hormone into your body. It is placed by a health care professional by injection under the skin of the lower abdomen below the navel. The implant itself will be completely absorbed into the body over weeks or months.
Dosage is based on your medical condition and response to therapy.
Receive this medication as directed by your doctor. The 3.6-milligram syringe is usually injected every 4 weeks. The 10.8-milligram syringe is usually injected every 12 weeks. Follow the dosing schedule carefully to get the most benefit from the drug. To help you remember, mark your calendar to keep track of when to receive the next dose. Do not stop this medication without your doctor's approval.
During the first few weeks of treatment, your hormone levels will actually increase before they decrease. This is a normal response by your body to this drug. This effect may result in new symptoms or worsening of symptoms (e.g., pain, tumor size) for the first few weeks.
In women, it is expected that menstrual periods will stop when this medication is used regularly. Tell your doctor promptly if regular periods continue after 2 months of treatment with goserelin.
Usually, this medication will not need to be removed because the implant will be slowly and completely absorbed by your body. However, in the unlikely event that you have serious side effects or other problems, your doctor may remove this medication.
Tell your doctor if your condition persists or worsens.

Zoladex Cautions

Before using goserelin, tell your doctor or pharmacist if you are allergic to it; or to LHRH or LHRH-like hormones (e.g., triptorelin); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: unexplained abnormal vaginal bleeding, diabetes, long-term alcohol use, smoking, personal or family history of bone loss (osteoporosis), high cholesterol/triglyceride levels, stroke, urinary blockage problem (in men), spinal cord problem (in men).
If you have diabetes, this drug may make it harder to control your blood sugar levels. Monitor your blood sugar levels regularly and tell your doctor of the results. Your doctor may need to adjust your diabetes medication, exercise program, or diet.
Goserelin may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away. The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may affect the heart rhythm. Before using goserelin, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).
Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using goserelin safely.
This medication is not recommended for use during pregnancy. It may harm an unborn baby. Women of child-bearing age must make sure they are not pregnant before starting this medication. If you become pregnant or think you may be pregnant, tell your doctor immediately. Consult your doctor for more details and to discuss reliable forms of birth control. For women, this medication should stop the release of an egg (ovulation) and your periods, but this should not be used as a reliable method of birth control. It is recommended that men and women using this medication use 2 effective forms of nonhormonal birth control (e.g., condoms and diaphragm with spermicide) while taking this medication. Continue using effective birth control until the return of the woman's period or for at least 12 weeks after stopping this medication.
It is not known whether this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this medication is not recommended. Consult your doctor before breast-feeding.

Zoladex Side Effects

Hot flashes (flushing), dizziness, headache, increased sweating, decreased sexual interest/ability, trouble sleeping, nausea, change in breast size, hair loss, or mental/mood changes (such as depression, mood swings, hallucinations) may occur. Pain, bruising, bleeding, redness, or swelling at the injection site may also occur. In women, vaginal dryness may also occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor immediately if any of these unlikely but serious side effects occur: vaginal burning/pain (in women), pain during sex (in women), breast pain/tenderness, new/worsening bone pain, new broken bone, burning feeling in feet/toes, swelling of the ankles/feet, unusual tiredness, change in the amount of urine.
This drug may infrequently make your blood sugar level rise, which can cause or worsen diabetes. High blood sugar can rarely cause serious conditions such as diabetic coma. Tell your doctor immediately if you develop symptoms of high blood sugar, such as unusual increased thirst and urination. If you already have diabetes, be sure to check your blood sugars regularly.
Get medical help right away if any of these rare but serious side effects occur: fast/irregular heartbeat, severe dizziness, fainting.
Seek immediate medical attention if any of these rare but very serious side effects occur: chest/jaw/left arm pain, trouble breathing, confusion, vision changes, slurred speech, weakness on one side of the body.
Rarely, a very serious problem with your pituitary gland (pituitary apoplexy) may occur, usually in the first hour to 2 weeks after your first dose of this medication. Seek immediate medical attention if any of these very serious side effects occur: sudden severe headache, mental/mood changes (e.g., confusion), vision changes, vomiting.
In men using this medication for prostate cancer, a rare but very serious urinary blockage problem or spinal cord problem (compression) can occur, especially during the first month of treatment. Tell your doctor immediately if you experience any of the following serious side effects: severe back pain, numbness/tingling/weakness of the arms/legs, inability to move, painful/difficult urination, blood in the urine.
A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.