英文药名: Vantas(Histrelin Acetate)

中文药名: 醋酸组氨瑞林植入剂

药品介绍

组氨瑞林是一种促黄体激素释放激素（LHRH）激动剂，美国学者萧尔（Shore）等报告，对于晚期前列腺癌患者，每年一次给予组氨瑞林长效埋植剂皮下埋植，能长期稳定地抑制睾酮，使其保持去势水平（＜50 ng/dl）。

[别名]：LHRH-Hydrogel implant，RL 0903
[商品名]：Vantas
[作用机制]：促性腺激素释放激素类似物，前列腺癌治疗药物。
[开发公司]：Endo制药；西尔制药公司/Hydro Med Sciences公司（美国）（原开发公司）
[给药方式]：皮下植入

VANTAS®（histrelin醋酸）皮下埋植

最初美国批准：2004年8月
 
适应症
VANTAS是促性腺激素释放激素（GnRH）激动剂表示为晚期前列腺癌的姑息治疗。
 
剂量和用法
推荐剂量的VANTAS是一个植入12个月。每个植入含有50的毫克histrelin醋酸交付（毫克histrelin 41号）。插入皮下植入上臂的内在方面。
 
剂型和优势
皮下埋植：50的毫克histrelin醋酸。
 
禁忌
已知过敏的激素或GnRH类似物。
怀孕：VANTAS在怀孕期间使用时可导致胎儿造成伤害。
 
注意事项：
在治疗的第一周检测血清睾酮的瞬态增加：可能导致肿瘤的症​​状恶化。
脊髓压迫和尿路梗阻：可能会导致瘫痪或肾功能损害。在治疗过程中密切监察高危病人。
定位或移除植入的困难：遗失或无法找到或删除插入植入物已报告。建议谨慎。
已接受GnRH类似物的男性高血糖和糖尿病：高血糖患糖尿病的风险增加。监测血糖水平，根据目前的临床实践和管理。
心血管疾病：心肌梗死，心源性猝死和中风的风险增加了男性。为心血管疾病的监测和管理，根据目前的临床实践。
 
不良反应
> 5％的男性观察：潮热，疲劳，植入部位的反应，睾丸萎缩最常见的不良反应。

更新日期：03/2011

Vantas
Generic Name: histrelin (implant) (his TREL in)
Brand Names: Vantas

VANTAS® (histrelin acetate) implant is a drug-delivery system that contains the medicine histrelin and is placed under the skin. After it is placed under the skin, VANTAS delivers histrelin to your body continuously for 12 months. VANTAS may help relieve the symptoms of prostate cancer. VANTAS is not a cure for prostate cancer.
Important Safety Information
Do not use VANTAS if you are allergic to the medicine histrelin or other medicines called gonadotropin releasing hormone (GnRH) agonists, are a woman or are a child under 18 years of age.
Before using VANTAS, tell your doctor about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements.
VANTAS is placed under the skin of your upper arm. Your doctor will numb your arm, make a small cut (incision), and place VANTAS under the skin. The cut will be closed with stitches and special surgical tape and covered with a bandage. Keep your arm clean and dry for 24 hours. Your doctor will give you complete instructions. You may have some pain, bruising, and redness at the insertion site during and after VANTAS is inserted and removed. These usually go away without treatment within 2 weeks.
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Histrelin Acetate Implant
What is this medicine?
HISTRELIN (his TREL in) is used to treat the symptoms of advanced prostate cancer. The implant contains a drug that is like a natural hormone in the body called gonadotropin-releasing hormone (GnRH). It is placed under the skin and releases the drug over 12 months.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•diabetes
•female (this implant is not for use in women)
•heart disease or previous heart attack
•high blood pressure
•high cholesterol
•pain or trouble passing urine
•spinal cord metastasis
•stroke
•tobacco smoker
•an unusual or allergic reaction to histrelin, other medicines, foods, dyes, or preservatives
How should I use this medicine?
This medicine is placed under the skin of your arm by a health care professional in a clinic or office. After the implant is placed, keep the insertion site clean and dry for 24 hours. Avoid heavy lifting and strenuous exercise for 7 days after implant insertion. The surgical strips over the site should be allowed to fall off on their own over several days. The implant must be removed after 12 months. At this time, a new implant may be inserted to continue therapy.
Talk to your pediatrician regarding the use of this medicine in children. This medicine is not approved for use in children.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•female hormones, like estrogens or progestins and birth control pills, patches, rings, or injections
•herbal or dietary supplements, like black cohosh or DHEA
•male hormones, like testosterone
•medicines for depression, anxiety, or psychotic disturbances
•prasterone
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. During the first week, your symptoms may get worse but then will start to get better as you continue your treatment. You may get hot flashes, increased bone pain, increased difficulty passing urine, or an aggravation of nerve symptoms. Discuss these effects with your doctor or health care professional. Some of these may get better with continued use of this medicine.
Rarely, the implant can be expelled from the body through the original incision site. It is possible that you may see the implant being expelled, or rarely, the implant may be expelled without you noticing it. If you believe the implant has been expelled from your body, call your doctor.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•blood in your urine
•changes in vision
•loss of bladder or bowel control
•new or worse bone pain
•pain at the insertion site
•severe headache
•trouble passing urine or change in the amount of urine
•vomiting
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•breast enlargement
•change in sex drive or performance
•constipation
•hot flashes (sudden feelings of warmth or sweating)
•redness or irritation at the insertion site
•testicles become smaller
•trouble sleeping
•weight gain
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

晚期前列腺癌患者接受组氨瑞林皮下植入的有效性和安全性国纽约康奈尔大学Weill医学院的Schlegel PN博士及其同事评估了晚期前列腺癌患者接受50mg促性腺激素释放激素促效剂醋酸组氨瑞林皮下植入的有效性和安全性。在局麻下通过手术将3 cm×3.5
mm的组氨瑞林植入剂放入适宜患者非优势上臂的内侧。在植入后最初2周内每周对患者进行一次评估，此后改为每月评估一次。在52周时将植入剂取出，大多数患者再次放入新的植入剂。观察患者接受治疗的安全性和有效性，持续至60周。通过观察第4周至第52周内达到化学去势（血清睾酮低于50ng/dl）的患者比例来确定有效性。
结果显示，134名于第4周检测睾酮水平的患者全部都获得化学去势效果。超过99%的患者在植入后52周内睾酮水平都持续受到抑制。同时还观察到了明显的LH和PSA抑制效果。在16周前，PSA与基础值（83.6ng/ml）相比已平均降低了90%（p=0.0001）。到60周前，79%的患者出现PSA完全应答（p<0.0175）。再次植入并未导致睾酮或LH波动。此外，植入剂安全性高，且耐受良好。Schlegel博士等总结认为，通过植入剂输送装置使用促性腺激素释放激素促效剂醋酸组氨瑞林可有效治疗晚期前列腺癌患者，在4周时即可抑制睾酮和LH达到去势水平，并可将这一水平维持至52周。有效性的次级终末指标PSA也被明显抑制。
Indevus制药公司宣布FDA批准Supprelin—LA（醋酸组氨瑞林皮下植入剂）50mg在美国上市，用于治疗儿童性早熟（CPP）。Supprelin-LA是一种一年期的皮下植入剂，12个月每天持续释放65μg促性腺激素释放激素类似物组氨瑞林，从而可以有效的阻碍垂体腺产生促性腺激素。