英文药名：GANIRELIX ACETATE(FORMERLY ANTAGON)
中文药名：醋酸加尼瑞克注射剂
分类名称
一级分类：内分泌系统药物 二级分类：性腺疾病用药 三级分类：
药品英文名
Ganirelix
药品别名
Antagon
药物剂型
注射剂：250μg。
药理作用
醋酸加尼瑞克是一合成的与内源性促性腺素释放素（GnRH）（又称促黄体生成素释放素，LHRH）类似的十肽化合物，是GnRH的拮抗剂。
本品竞争性拮抗促性腺的GnRH受休，从而变异途径，引起快速、可逆性地抑制促性腺激素（黄体生成素LH和促卵泡激素FSH）分泌。其抑制垂体分泌LH比抑制分泌FSH更显著，从而降低性激素的产生。通过抑制中周期GnRH对LH诱导波动，本品能够抑制排卵、卵母细胞成熟分裂和黄体化。
对患卵巢过度刺激症妇女，本品能够预防LH波动及相关刺激，并提高植入和妊娠比率。本品从大鼠垂体LHRH受体处取代放射性125I标记过的亮丙瑞林的pKi值为10.78，因此与受体结合力是LHRH的2倍。在培养大鼠垂体细胞中，本品竞争性抑制亮丙瑞林诱导LH释放的pA2值为11.37。在实验中，1μg本品能抑制90%大鼠排卵，2μg则100%抑制。而0.5μg本品抑制50%排卵。本品在发情完盛期雌性大鼠中的半数有效剂量ED50值为1.4μg/kg。本品在培养大鼠乳腺细胞诱导组胺释放的半数有效浓度EC50值为5.3～11μg/ml，而亮丙瑞林的对应值为1.8μg/ml，说明本品作为组胺释放诱导剂其能力弱6倍。更重要的是，在麻醉的雄性大鼠，通过低血压效应评价体内过敏性样能力跟早期LHRH拮抗剂值（20～40μg/kgiv）相比，本品非常小（ED50=0.9mg/kgiv），具有非常良好的抗促性腺激素与过敏性样能力。
本品作为一个LHRH拮抗剂被当作FSH在试管受精（IVF）或胞质内精子注射前来控制卵巢刺激，对卵母细胞形态学和质量影响进行了评价。在卵巢刺激病人，用本品或LHRH拮抗剂亮丙瑞林的对应值为1.8μg/ml，说明本品作为组胺释放诱导剂其能力弱6倍。更重要的是，在麻醉的雄性大鼠，通过低血压效应评价体内过敏性样能力跟早期LHRH拮抗剂值（20～40μg/kgiv）相比，本品非常小（ED50=0.9mg/kgiv），具有非常良好的抗促性腺激素与过敏性样能力。
本品作为一个LHRH拮抗剂被当作FSH在试管受精（IVF）或胞质内精子注射前来控制卵巢刺激，对卵母细胞形态学和质量影响进行了评价。在卵巢刺激病人，用本品或LHRH拮抗剂亮丙瑞林治疗发现在核酸成熟、卵质形态学、卵膜弹性、受精及分裂率两者没有差别，并且具有足够质量适合转移的胚胎数量也是相同的。
适应证：
治疗妇女不孕症（人工取卵、受精、植入）。
禁忌证
1.对本品过敏者、哺乳者、期望受孕者禁用。
2.儿童、＞65岁老人不宜使用。
注意事项
1.使用本品前，必须先做妊娠试验，以免发生流产或其他意外。
2.临床试验表明，用本品治疗不育症(女性)是有效的。
3.本品一定要由富有治疗不育症经验的医生指导使用，这是治疗有效的保证。
4.贮于2～8℃条件下。
不良反应
1.中性粒细胞数≥8.3/mm3。
2.妇科腹痛，胎儿死亡。
3.头痛、卵巢过度刺激综合征，阴道出血。
4.注射部位反应、恶心和胃肠不适。
用法用量
本品一般须合用促卵泡激素(FSH，如促卵泡素α或β)，以控制卵巢过度刺激综合征。使用的方法是，在月经周期第2天或第3天早晨开始给予FSH治疗(参见促卵泡激素)，接着在月经周期第7天或第8天早晨皮下注射本品250μg，1次/d，直至出现充分的卵泡反应为止，此时，再给予人绒促性素，并停用本品和FSH治疗。然后进行卵细胞检索(为体外受精或向胞质内注射精液)，接着就期盼着植入和怀孕。
药物相应作用
尚缺资料
About Ganirelix Acetate Injection 250 mcg
Ganirelix Acetate Injection is a gonadotropin-releasing hormone (GnRH) antagonist that can help patients in suppressing premature luteinizing hormone (LH) surges in women while they are going through assisted reproductive technology (ART) treatment. The usage of Ganirelix Acetate Injection prevents premature release of eggs. Make sure that you use Ganirelix Acetate Injection after telling your doctor about all the medication that you are taking and your medical history for any allergies or adverse reactions to any medications.
Ganirelix Acetate Injection can also be used by women who are using an injectable gonadotropin, such as Follistim® AQ Cartridge (follitropin beta injection). The injectable gonadotropin present in Ganirelix Acetate Injection stimulates the growth of multiple follicles, which can cause an early rise in LH.
Like a GnRH agonist, Ganirelix Acetate Injection (a GnRH antagonist) is effective in preventing LH surges. Unlike a GnRH agonist, Ganirelix rapidly acts to prevent the LH surge after its initial injection. The gonadotropin-releasing hormone (GnRH) antagonist Ganirelix Acetate Injection contains the active ingredient Ganirelix acetate. The average cycle of Ganirelix Acetate Injection is based on five days mid-cycle gonadotropin stimulation. This leads to several benefits for the patients:
• Shorter treatment days.
• Lesser total medication is used.
• Fewer injections are needed.
Ganirelix Acetate Injection is the only GnRH antagonist in a ready-to-use pre-filled syringe and it is really easy to administer because mixing isn't required. One pre-filled syringe of Ganirelix Acetate Injection contains 250 micrograms of ganirelix acetate. Ganirelix Acetate Injection can be stored at room temperature..
----------------------------------------------------
What is Ganirelix Acetate (ganirelix)?
Ganirelix is a man-made form of a protein that reduces the amount of certain hormones in the body, including estrogen.
Ganirelix is used along with other medications to regulate hormones during treatment for infertility in women.
Ganirelix may also be used for other purposes not listed in this medication guide.
What is the most important information I should know about Ganirelix Acetate (ganirelix)?You should not use this medication if you are allergic to ganirelix or similar medications such as leuprolide (Lupron, Eligard), goserelin (Zoladex), or nafarelin (Synarel).
Before using ganirelix, tell your doctor if you are allergic to latex rubber.
Do not use ganirelix if you are already pregnant. Your doctor may give you a pregnancy test to make sure you are not pregnant before you receive ganirelix. Do not use this medication without telling your doctor if you are breast-feeding a baby. During your treatment with ganirelix, your blood may need to be tested often. Do not miss any follow-up visits to your doctor. You must remain under the care of your doctor while using ganirelix. Some women using this medicine have developed a condition called ovarian hyperstimulation syndrome (OHSS), especially after the first treatment cycle. OHSS can be a life-threatening condition. Call your doctor right away if you have any of the following symptoms of OHSS: severe pelvic or stomach pain, swelling or rapid weight gain, shortness of breath, diarrhea, nausea, vomiting, or urinating less than usual.What should I discuss with my healthcare provider before using Ganirelix Acetate (ganirelix)?You should not use this medication if you are allergic to ganirelix or similar medications such as leuprolide (Lupron, Eligard), goserelin (Zoladex), or nafarelin (Synarel).
Before using ganirelix, tell your doctor if you are allergic to latex rubber.
FDA pregnancy category X. This medication can harm an unborn baby or cause birth defects. Do not use ganirelix if you are already pregnant. Your doctor may give you a pregnancy test to make sure you are not pregnant before you receive ganirelix. Tell your doctor right away if you become pregnant during treatment. It is not known whether ganirelix passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.
How should I use Ganirelix Acetate (ganirelix)?
Ganirelix is given as an injection under the skin. Your doctor, nurse, or other healthcare provider will give you this injection. You may be shown how to inject your medicine at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.
Ganirelix is usually given once daily for several days in a row during certain phases of your fertility treatment cycle. Follow your doctor's instructions and try not to miss any doses.
Each single-use prefilled syringe of this medicine is for one use only. Throw away the vial after one use, even if there is still some medicine left in it after injecting your dose.
Use each disposable needle only one time. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.
During your treatment with ganirelix, your blood may need to be tested often. Do not miss any follow-up visits to your doctor. You must remain under the care of your doctor while using ganirelix. Store the ganirelix prefilled syringe at room temperature, away from heat, moisture and light.
What happens if I miss a dose?
Call your doctor for instructions if you miss a dose.
What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine.
Symptoms of a ganirelix overdose are not known.
What should I avoid while using Ganirelix Acetate (ganirelix)?
Follow your doctor's instructions about any restrictions on food, beverages, or activity.
Ganirelix Acetate (ganirelix) side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Some women using this medicine have developed a condition called ovarian hyperstimulation syndrome (OHSS), especially after the first treatment cycle. OHSS can be a life-threatening condition. Call your doctor right away if you have any of the following symptoms of OHSS:
severe pelvic pain;
swelling of the hands or legs;
stomach pain and swelling;
shortness of breath;
weight gain;
diarrhea;
nausea or vomiting; or
urinating less than normal.
Less serious side effects may include:
pelvic pain (similar to menstrual cramps);
mild nausea or stomach pain;
headache;
vaginal bleeding; or
pain, redness, or irritation at the injection site.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What other drugs will affect Ganirelix Acetate (ganirelix)?
There may be other drugs that can interact with ganirelix. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.
附件:
---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
GANIRELIX ACETATE (FORMERLY ANTAGON) 250MCG/0.5ML/DISP SYRINGE/BOX
原产地英文药品名:
GANIRELIX ACETATE
中文参考商品译名:
醋酸加尼瑞克(以前名称为ANTAGON) 250微克/0.5毫升/注射器/盒
中文参考药品译名:
醋酸加尼瑞克
生产厂家中文参考译名:
ORGANON USA INC
生产厂家英文名:
ORGANON USA INC