英文药名: Suprecur（buserelin acetate nasal solution 0.15％）

中文药名: 布舍瑞林醋酸点鼻液0.15％

生产厂家: 持田药业
薬效分类名
促性腺激素释放激素诱导体制剤
欧文商標名
Suprecur nasal solution 0.15％
一般名
ブセレリン酢酸塩（buserelin acetate）
化学名
5‐Oxo‐L‐prolyl‐L‐histidyl‐L‐ ryptophyl‐L‐seryl‐L‐ yrosyl‐O‐ ert‐utyl‐D‐seryl‐L‐leucyl‐L‐arginyl‐N‐ethyl‐L‐prolinamide monoacetate
分子式
C60H86N16O13・C2H4O2
分子量
1299.48
構造式
H‐5‐oxo‐Pro‐His‐Trp‐Ser‐Tyr‐D‐Ser(t‐C4H9)‐Leu‐Arg‐Pro‐NHC2H5・CH3COOH
性　状
本产品为粉末或一团白色至浅黄色的白色。该产品是微溶于水，稍微溶于甲醇或乙醇（95），并在乙醚中几乎不溶。本产品是吸湿。
药效药理
1.动物试验
（1） 子宫内膜异位症
垂体 - 性腺系统功能的抑制作用
与雌性大鼠或雌性豚鼠，抑制垂体功能（在垂体GnRH受体含量，减少的LH金额等）和抑制的LH受体量（卵巢功能的卵巢的实验中，FSH受体量，观察到雌激素量，降低血液中的雌激素数量和孕激素量，抑制妊娠）。
由于使用雌性猴由子宫内膜萎缩和生长暂停图像表示卵巢功能，抑制增加孕酮量和FSH量，抑制排卵，闭经，正常性周期在实验血液雌二醇量抑制了观察。
影响实验子宫内膜异位症
通过实验，植入子宫条实验子宫内膜异位症的大鼠形成的囊肿的体积和重量减少，子宫内膜异位症的观察到的治疗效果。
（2）子宫肌瘤
垂体 - 性腺系统功能的抑制作用
与雌性大鼠或雌性豚鼠，抑制垂体功能（在垂体GnRH受体含量，减少的LH金额等）和抑制的LH受体量（卵巢功能的卵巢的实验中，FSH受体量，观察到雌激素量，降低血液中的雌激素数量和孕激素量，抑制妊娠）。
由于使用雌性猴由子宫内膜萎缩和生长暂停图像表示卵巢功能，抑制增加孕酮量和FSH量，抑制排卵，闭经，正常性周期在实验血液雌二醇量抑制了观察。
（3）中枢性性早熟
垂体 - 性腺系统功能的抑制作用
LH量和使用未成熟的雄性大鼠的实验垂体FSH含量，垂体功能抑制垂体反应性代表出席损失和血LH量GnRH激发试验，LH受体在睾丸的时间减少体重，血液睾丸酮量，睾丸重量，前列腺重量，抑制由在精囊重量的损失和睾丸分泌睾酮容量的降低表示睾丸功能进行观察。
此外，垂体功能的抑制通过还原垂体的GnRH受体量在使用的未成熟雌性大鼠观察抑制由子宫重量的减少表明卵巢功能实验的代表。
2.临床药理学研究
（1）子宫内膜异位症
垂体促性腺激素的分泌量的抑制作用
在正常的月经周期的妇女，LH时从21天卵泡早期连续给药，FSH分泌效果最大反应的第一天观察到的，此后，它逐渐减小，LH，FSH的分泌能力观察到，被抑制这是。
此外LH，当用此药24周子宫内膜异位症患者被显着抑制通过促性腺激素释放激素试验证实治疗FSH的分泌量
卵巢功能抑制动作
血雌二醇浓度升高，这种药物管理初始过渡，随后下降，直到绝经期的水平，停止排卵，月经，被认为是子宫内膜萎缩，卵巢功能受到抑制。
（2）子宫肌瘤
垂体促性腺激素的分泌量的抑制作用
在正常的月经周期的妇女，LH时从21天卵泡早期连续给药，FSH分泌效果最大反应的第一天观察到的，此后，它逐渐减小，LH，FSH的分泌能力观察到，被抑制这是。
影响子宫肌瘤组织
当给予这种药物16个星期到子宫肌瘤患者，玻璃样变性的程度高，观察子宫肌瘤组织在显微镜下观察
适应症
子宫内膜异位症
减少和子宫以下症状改善肌瘤子宫肌瘤
月经过多，下腹痛，腰痛，贫血
用法用量
1.子宫内膜异位症和子宫肌瘤
通常，一个由每一个喷入鼻腔的左，右每一个天（300微克如布舍瑞林）三次，给药从1〜2第二次月经周期至成人的空腔。此外，将根据症状调整
2.中枢性性早熟
每一个是（如布舍瑞林300微克）喷雾施用单剂量到左和鼻腔的权，给予正常之一天3-6次的。当效果不足切换到皮下注射方法。
这种药物的作用，故在降低的确定，并在血液LH的反应性血液中性类固醇的降低，GnRH的试验在给药两周后的FSH相比，这种药物的预施用。
包装规格
10毫升1瓶（附：点鼻用医薬品注入器）

生产商
持田药业有限公司
附件：
1.药如何使用：http://www.mochida.co.jp/naimakusho/drug/02_02.html
2.完整处方资料：http://www.kegg.jp/medicus-bin/japic_med?japic_code=00051523

Suprecur nasal solution 0.15％（buserelin acetate）
Therapeutic category name
GnRH derivative formulation
Brand Name
Supurekyua nasal solution 0.15%
Composition
This drug is a Nasal solutions containing buserelin acetate 15.75mg (15mg as buserelin) in one bottle 10mL. (With drugs injector point the nose)
Sodium citrate hydrate as an additive, sodium chloride, benzalkonium chloride, I contain a pH adjusting agent.
Contraindication
Patients with used without the diagnostic abnormal genital bleeding [there is a risk of similar diseases (such as malignant tumor). ]
There may not be a continuation of the patient [pregnancy that may be pregnant or pregnant. Refer to the section "5. pregnant women, maternal, administration to lactating women, etc."]
The transition to breast milk in lactating patients [animal experiments have been observed. Refer to the section "5. pregnant women, maternal, administration to lactating women, etc."]
Patients with a history of hypersensitivity to ingredients or other GnRH derivative of this drug
Efficacy or effect
Endometriosis
Improvement of the following symptoms based on the reduction and uterine fibroids uterine fibroids
Excessive menstruation, lower abdominal pain, low back pain, anemia
Endometriosis and uterine fibroids
Normally, one by each one sprayed into the nasal cavity of the left and right per three times a day (300μg as buserelin), administered from menstrual cycle 1? Second day to adult. In addition, it will be adjusted according to the symptoms.
Since there is a decrease in bone mineral density is observed by long-term administration of this drug and other GnRH derivatives formulations, continuous administration is not performed in principle more than 6 months of GnRH derivative formulations.
Central precocious puberty
Central precocious puberty
Was with the administration once (300μg as buserelin) each 1 spray administered to the left and right nasal cavity, is administered usually three daily? 6 times. When the effect insufficient switched to subcutaneous injection method.
The effect of this drug, it is determined at a reduced and a decrease in blood neutral steroid of the reactivity of blood LH, FSH of GnRH test in administration two weeks later as compared to pre-administration of this drug.
Careful administration
Patients with liver failure [liver function is likely to be worse. ]
There is a possibility that appears patient and depressive symptoms of the patient [menopause-like with their history of depression or depressive state. ]
Patients with submucosal fibroids [bleeding symptoms of exacerbation, or there is a risk of massive bleeding. ]
Noting the patient's blood pressure there is a risk of increasing the patient 'blood pressure hypertension. ]
Attention should be paid to the patient's blood glucose level because the patient [impaired glucose tolerance of diabetes is likely to be worse. ]
Cerebrovascular disease, coronary artery disease or the patient [vascular lesions that its history is progress, there is that these diseases are exacerbated. ]
Clinically significant adverse reactions
Shock, anaphylactoid symptoms
Shock, anaphylactoid symptoms (difficulty breathing, feeling of heat, systemic flushing, decreased blood pressure, etc.) because it may cause, carefully observed, administration should be discontinued if any abnormality is observed, to take appropriate measures thing.
Depressive symptoms
Because may cause depressive symptoms of menopause like has been reported, that to fully observe the condition of the patient is in use of this drug.
Hair loss
Because there is a report of hair loss, it should be discontinued administration should be aware of the patient's condition, symptoms appear.
Angina pectoris, myocardial infarction, cerebral infarction
Angina pectoris, myocardial infarction, and because there is a report of cerebral infarction, and in use of this drug and note the condition of the patient, should be discontinued the administration if any abnormality is observed.
Thrombocytopenia, leukopenia
Thrombocytopenia, because it may leukopenia appears, carefully observed, administration should be discontinued if any abnormality is observed, to take appropriate measures.
Fraud bleeding
Since there is a large amount of illegal bleeding appears, it is carefully monitored, and if any abnormalities are observed, and that it take appropriate measures.
Ovarian cyst rupture
Since there is that ovarian cysts rupture, carefully monitored, bloating, if the abnormalities were observed such as lower abdominal pain (tenderness, etc.) to discontinue administration, carrying out the appropriate action.
Liver dysfunction, jaundice
AST (GOT), liver dysfunction with elevated such as ALT (GPT), jaundice may occur, carefully observed, administration should be discontinued if any abnormality is observed, to take appropriate measures thing.
Onset or exacerbation of diabetes
Because it may appear onset or exacerbation of diabetes, carefully observed, administration should be discontinued if any abnormality is observed, that it take appropriate measures.
Pharmacology
Animal testing
Endometriosis
Pituitary Gonadal function inhibitory effect 12, 13)
In experiments with female rats or female guinea pigs, suppression of pituitary function (GnRH receptor content in the pituitary gland, reduction of LH amount, etc.) and LH receptor amount of suppression (in the ovaries of ovarian function, FSH receptor amount , estradiol amount, decrease in blood estradiol amount and progesterone amount, suppression of pregnancy) was observed.
Blood estradiol amount due to the normal sexual cycle in the experiment using a female monkey, suppression of an increase in progesterone amount and FSH amount, suppression of ovulation, amenorrhea, of ovarian function represented by the atrophy and growth pause image of the endometrium suppression was observed.
Effect 14 to the experimental endometriosis)
The volume and weight of the cysts formed by experiments with implantation uterine strips experimental endometriosis rats is reduced, the observed healing effect of endometriosis.
Uterine fibroid
Pituitary Gonadal function inhibitory effect 12, 13)
In experiments with female rats or female guinea pigs, suppression of pituitary function (GnRH receptor content in the pituitary gland, reduction of LH amount, etc.) and LH receptor amount of suppression (in the ovaries of ovarian function, FSH receptor amount , estradiol amount, decrease in blood estradiol amount and progesterone amount, suppression of pregnancy) was observed.
Blood estradiol amount due to the normal sexual cycle in the experiment using a female monkey, suppression of an increase in progesterone amount and FSH amount, suppression of ovulation, amenorrhea, of ovarian function represented by the atrophy and growth pause image of the endometrium suppression was observed.
Central precocious puberty
Pituitary? Gonadal function inhibitory effect 15, 16)
LH amount and FSH content in the pituitary gland in the experiments using immature male rats, and the suppression of pituitary function represented by the pituitary reactivity decreases at the time of loss and GnRH test of blood LH amount, LH receptors in the testes body weight, blood testosterone amount, testis weight, prostate weight, suppression of testicular function indicated by the decrease in the loss and testicular testosterone secretion capacity of the seminal vesicle weights were observed.
In addition, the suppression of pituitary function represented by reduction of the pituitary GnRH receptors amount in experiments using immature female rats was observed suppression of ovarian function indicated by the reduction in uterine weight.
Clinical pharmacology studies
Endometriosis
Pituitary gonadotropin secretion capacity inhibiting action 17, 18)
In the normal menstrual cycle women, LH when administered continuously from early follicular phase of 21 days, FSH secretion effect maximum reaction is observed on the first day, thereafter, it gradually decreased, LH, the FSH secretion capacity observed that is suppressed It was.
Also LH when this drug was administered 24 weeks endometriosis patients, FSH secretion capacity, be suppressed markedly by the GnRH test
confirmed.
Ovarian function suppression effect 2? 4, 18)
Blood estradiol concentration is elevated in this drug administration initial transient, decreased thereafter until menopause level, stop ovulation, menstruation, is seen atrophy of the endometrium, ovarian function was suppressed.
Uterine fibroid
Pituitary gonadotropin secretion capacity inhibiting action 17)
In the normal menstrual cycle women, LH when administered continuously from early follicular phase of 21 days, FSH secretion effect maximum reaction is observed on the first day, thereafter, it gradually decreased, LH, the FSH secretion capacity observed that is suppressed It was.
Effect 19 for uterine fibroids organization)
When administered this drug 16 weeks to uterine fibroids patients, a high degree of hyaline degeneration was observed in uterine fibroid tissue in the microscope observation.
The physicochemical knowledge of active ingredient
Generic name
Buserelin acetate (buserelin acetate)
Chemical name
5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate
Molecular formula
C60H86N16O13 · C2H4O2
Molecular weight
1299.48
Sex-like
This product is a powder or mass of white? Fine yellowish white. The product is slightly soluble in water, slightly slightly soluble in methanol or ethanol (95), and practically insoluble in diethyl ether. This product is hygroscopic.