英文药名: Suprecur MP S.C.Inj.（buserelin acetate）

中文药名: 布舍瑞林醋酸注射器

生产厂家: 持田药业
治疗类别名称
促性腺激素释放激素衍生物制剂
一般名ブセレリン酢酸塩（buserelin acetate）
欧文商標名
Suprecur MP 1.8 for S.C.Inj.
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.作用机序
布舍瑞林乙酸具有促性腺激素释放激素样作用，但施用初始增强垂体的促性腺激素分泌能力，通过重复给药（下调），垂体的GnRH反应引起的垂体GnRH受体量减少减少并最终从卵巢抑制性激素分泌。垂体 - 性腺系统功能通过抑制作用，施加于子宫肌瘤和子宫内膜异位的治疗效果是性激素依赖性疾病。
2.动物试验
1）垂体 - 性腺系统功能的抑制作用
与雌性大鼠的研究中，垂体功能通过在垂体GnRH受体量的减少和垂体的GnRH反应性的降低所表示的抑制，卵巢功能的抑制指示的子宫重量的减少进行了观察。
2）对实验性子宫内膜异位症
在实验大鼠子宫内膜异位症研究中，通过植入子宫条形成囊肿体积减小观察，子宫内膜异位症的观察治疗效果。
3.临床药理学研究
1）垂体促性腺激素的分泌量的抑制作用
当在第一次剂量的时间皮下给药，每4周为1.8mg如布舍瑞林醋酸子宫肌瘤16例的子宫内膜异位症的患者子宫，血清LH和FSH值表示在第一天的最高值，之后逐渐减小这是。
此外，当肌瘤患者服用单一的皮下作为为1.8mg醋酸布舍瑞林6起案件见于GnRH的负载测试的垂体功能的反应是在抑制状态，在4周给药后，在给药后的恢复8周承认。
2）卵巢功能抑制作用
当它是4-6次皮下注射，4周的间隔为子宫肌瘤和子宫内膜异位症的患者，给予上涨初始瞬时后雌激素水平，减少更年期的水平，一般排卵受到抑制，月经停止。
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
一般，1管每四周成人一次（如为1.8mg布舍瑞林乙酸酯）I被皮下给药。应当指出的是，第一剂余做1至5天的月经周期。
包装规格
MP皮下注射1.8*1支
生产商:
持田药业有限公司

Suprecur MP 1.8 for  S.C.Inj.（buserelin acetate）
Therapeutic category name
GnRH derivative formulation
Brand Name
Supurekyua MP subcutaneous injection for the 1.8
Composition
This drug, glass container partitioned into two chambers with a rubber stopper (double chamber syringe: DCS) containing the following ingredients in a 1-cylinder.
DCS front chamber (needle side)
Buserelin acetate 1.80mg
DCS front chamber (needle side): additive
Lactic acid-glycolic acid copolymer (1: 1) 28.20mg
DCS front chamber (needle side): additive
Dextran 40 75.00mg
DCS front chamber (needle side): additive
Polysorbate 40 3.75mg
DCS front chamber (needle side): additive
Sodium chloride 6.75mg
DCS rear chamber (plunger side): suspending liquid
Water for injection 0.75mL
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
Usually, 1 tube once every four weeks in adults (1.8mg as buserelin acetate) it is administered subcutaneously. It should be noted that the first dose I do 1 to 5 day menstrual cycle.
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.
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 Note 1)
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 Note 1)
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 removal Note 1)
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 Note 1)
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 Note 1)
Thrombocytopenia, because it may leukopenia appears, carefully observed, administration should be discontinued if any abnormality is observed, to take appropriate measures.
Fraud bleeding Note 1)
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 Note 1)
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 Note 1)
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.
The onset of diabetes or exacerbation Note 1)
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
Mechanism of action 8)
Buserelin acetate has a GnRH-like action, but the administration initial enhances the gonadotropin secretion ability of the pituitary gland, causing a decrease in the pituitary GnRH receptor amount by repeated administration (down-regulation), GnRH reactivity of the pituitary reduce and eventually suppress sex hormone secretion from the ovaries. The pituitary - gonadal system function by inhibiting action, to exert a therapeutic effect on uterine fibroids and endometriosis is a sex hormone-dependent diseases.
Animal testing
Pituitary - gonadal system function inhibitory effect 9, 10)
In studies with female rats, the inhibition of pituitary function represented by the decrease in the reduction and pituitary GnRH reactivity of the pituitary GnRH receptor amount, the suppression of ovarian function indicated by the decrease in uterine weight was observed.
Effect on experimental endometriosis 11)
In studies with experimental endometriosis rats, a decrease in cyst volume formed by implantation uterine strips are observed, the observed therapeutic effect of endometriosis.
Clinical pharmacology studies
Pituitary gonadotropin secretion capacity inhibiting action 1,7)
When administered subcutaneously every 4 weeks 1.8mg as buserelin acetate to uterine fibroids and 16 cases of endometriosis patients uterus, serum LH and FSH value at the time of first dose represents the highest value on the first day, thereafter gradually decreases did.
Also when administered single subcutaneous the 1.8mg as buserelin acetate in fibroid patients six cases, the reactivity of the pituitary function seen in GnRH load test is in the suppression state in the 4 weeks after the administration, the recovery in 8 weeks after the administration Admitted.
Ovarian function suppression action 1-4)
When it is 4-6 times subcutaneously at 4 week intervals for uterine fibroids and endometriosis patients, serum estradiol levels after rising administration initial transient and reduced to menopause levels, usually ovulation is inhibited, menstruation was stopped.
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 a mass of white to pale 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.
http://www.kegg.jp/medicus-bin/japic_med?japic_code=00052362