部份中文醋酸亮丙瑞林处方资料（仅供参考）
商品名：LEUPLIN PRO FOR INJECTION KIT
英文名：Leuprorelin Acetate
中文名：醋酸亮丙瑞林
生产商：武田薬品
リュープリンPRO注射用キット22.5mg
藥用類別名稱
lh-rh 注 1)
注 1) lh-rh: 黃體釋放激素微膠囊型緩釋製劑
批准日期：2015年11月
商標名
LEUPLIN PRO FOR INJECTION KIT 22.5mg.
化学構造式
一般名
リュープロレリン酢酸塩（Leuprorelin Acetate）〔JAN〕
化学名
5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate
分子式
C59H84N16O12・C2H4O2
分子量
1269.45
性状：
醋酸利普林是一種白色帶淡黃色白色粉末。 很易溶于水或醋酸 (100), 易溶于甲醇, 微溶于乙醇 (99.5)。它是吸濕的。
批准條件
制定藥品風險管理計劃並加以實施。
藥用藥理學
1. 作用機制
當反復給藥lh-h或高活性lh-r衍生物的賴普拉乙酸鹽, 第一次給藥後的短暫垂體後, 促性腺激素刺激作用 (急性作用) 觀察到, 在腦垂體刺激生產和釋放促性腺激素降低。 此外, 睾丸和卵巢促性腺激素反應性降低, 睾酮和雌二醇的產生能力降低 (慢性作用)。利普林醋酸鹽的lh釋放活性約為lh-rh的100倍, 其垂體性腺功能抑制效果強于lh-rh。醋酸盧普羅林是一種活性很強的lh-rh 衍生物, 垂體腺體的抑制作用強, 乙酸利普蘭酯與lh-rh相比對蛋白水解酶具有很高的抵抗力, 由於lh-rh受體的高親和力。此外, 由於目前的製劑是一種緩釋製劑, 它通過在血液中釋放利普倫林醋酸酯, 在任何時候都表現出性腺功能的抑制作用, 從而導致有效睾丸和卵巢的反應性減少。
2. 促性腺激素濃度的抑制作用
(1) 前列腺癌患者經皮下注射24週一次血清睾酮濃度降低到以下持續去勢, 觀察藥物去勢。
(2) 絕經前乳腺癌患者經皮下給藥一次, 24週一次, 一般降低到低於更年期水準, 認識到卵巢功能的抑制作用, 通常排卵抑制, 月經停止。
适应症
0 前列腺癌
0 絕經期前乳腺癌
用法与用量
通常情況下, 成人在24周內作為醋酸溶苯硫醚, 在皮下給藥一次, 為22.5毫克。
在給藥過程中, 通過將柱塞杆按在針頭上, 懸浮液總量被轉移到粉末部分, 同時注意不要抽打, 使用充分懸浮。
臨床結果
前列腺癌
對於前列腺癌治療患者 (抗腫瘤作用的患者通過使用11.25毫克的雷普林sr注射試劑盒是穩定的), (共4次)11.25毫克在24周皮下注射一次 (共兩次) 或作為磷酸酯的利帕拉乙酸鹽。作為一個主要的評價專案, 患者在開始給藥後48周內保持血清睾酮濃度的比例(100ng/dl或以下)是100%在22.5毫克給藥組(81/81例), 11.25毫克管理組98.7%(78/ 79), 兩組[95%置信區間]之間的差異為1.3%[-3.4%, 6.8%], 並且滿足預先設定的非隱性標準(95%置信區間的下限超過10%)。
絕經前乳腺癌
對於絕經後乳腺癌術後患者, 皮下給予1次(共2次)或11.25毫克(共4次) (與每組他莫西芬20mg day聯合使用), 作為每24週一次22.5毫克的lprorylacetic醋酸鹽。是一個主要的評價專案, 患者在絕經水準48周後服用後抑制血清雌二醇濃度的比例 (30pgsm或以下), 在22.5mg管理組 (81/83 例), 11.25毫克給藥組(81。 /84), 兩組[95%置信區間] 之間的差異為 1.2%[-5.2%, 7.8%], 滿足預先設定的非隱性標準 (95% 置信區間的下限大於10%)。
包装
1套件
製造商
武田薬品
注：以上中文不够完整，使用者以原处方资料为准。
完整说明附件：http://www.info.pmda.go.jp/go/pack/2499407G4029_1_06/
For manufacturing and marketing approval prostate cancer and premenopausal breast cancer therapeutic agent of the "Leuplin ®PRO injection kit 22.5mg" in Japan
On September 28, 2015, the Company announced today its "Leuplin® PR Injection Kit 22.5 mg" (hereinafter referred to as "Injection Kit"), asustained 24-week product of "Leuprin®" (generic name: leuprorelin acetate, for the "24-week sustained formulation"), let you know that it has acquired a manufacturing and marketing approval from the Ministry of Health, Labor and welfare as prostate cancer and premenopausal breast cancer therapeutic agent.
Leuplin is an LH-RH agonist (luteinizing hormone releasing hormone derivative) injectable formulation created by the Company, which acts continuously on the pituitary gland and decreases the reactivity of the pituitary gland, thereby producing sex hormone Suppress. This drug is, as a therapeutic agent for hormone-dependent diseases such as prostate cancer and premenopausal breast cancer, the United States, Europe, has been used in Asia and the like.
We repeated innovation of pharmaceutical technology and developed this drug which was administered once daily at the time of first approval in the United States (1985) as a sustained release formulation by original microcapsule formulation technology, and 1 It has made it possible to maintain a stable blood concentration over a long period of time by administration. Currently, sales in Japan are 4 weeks sustained preparation of this drug and 12 weeks sustained preparation.
The approval acquisition of the 24-week sustained preparation in Japan this time, our company examined the efficacy, safety, pharmacokinetics and hormonal dynamics etc. of this drug for prostate cancer and premenopausal breast cancer in Japan, 2 It is based on the results of one multicenter, randomized, open-label clinical phase III trial. As the premenopausal breast cancer therapeutic agent, it will be approved as the world's first 24-week sustained-release preparation.
We expect that we can respond to the needs of prostate cancer · premenopausal breast cancer patients and medical personnel by delivering this drug.
Outline of sustained preparation for 24 weeks
product name
Leuplin® PRO injection kit 22.5 mg
common name
Leuprorelin acetate
Indication
○ Prostate cancer
○ premenopausal breast cancer
Dosage regimen
Usually, adults receive 22.5 mg subcutaneously as leuprorelin acetate once every 24 weeks.
Upon administration, the plunger rod is pushed with the injection needle facing upward, and the total amount of the suspension liquid
Move it to the powder part, use it while sufficiently suspending it, taking care not to foam.