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聚磷酸雌二醇 - 维基百科，自由的百科全书 跳とべ转到内容ないよう

聚磷酸さん雌めす二に醇あつし

编辑链接
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聚磷酸さん雌めす二に醇あつし
上うえ圖ず：聚磷酸さん雌めす二に醇あつし的てき键线式しき，下圖したず：雌めす二醇磷酸酯（英えい语：estradiol phosphate）（聚磷酸さん雌めす二に醇あつし的てき单体）的てき球たま棒ぼう模型もけい
臨床りんしょう資料しりょう
商品しょうひん名めい（英えい语：Drug nomenclature）Estradurin, Estradurine
其他名稱めいしょうPEP; Estradiol phosphate polymer; Estradiol 17βべーた-phosphate polymer; Estradiol polymer with phosphoric acid; Leo-114
AHFS/Drugs.com国くに际药品ひん名称めいしょう
懷ふところ孕分級きゅう
  • 禁忌きんき[1]
给药途と径みち肌はだ肉にく注射ちゅうしゃ[1][2]
藥物やくぶつ類別るいべつ（英えい语：Drug class）雌めす激げき素もと藥物やくぶつ、雌めす激げき素もと酯（英えい语：Estrogen ester）
ATC碼
法律ほうりつ規範きはん狀態じょうたい
法律ほうりつ規範きはん
  • 处方药（℞-only）
藥物やくぶつ動力どうりょく學がく數かず據よりどころ
生物せいぶつ利用りよう度ど肌はだ肉にく注射ちゅうしゃ: 高こう
血漿けっしょう蛋白たんぱく結合けつごう率りつ雌めす二に醇あつし：~98%（和わalbumin及SHBG）[3][4][1]
药物代だい谢主要しゅよう是ぜ靠もたれ肝臟かんぞう，少しょう部ぶ份會透過とうか腎じん、生殖せいしょく腺せん及肌はだ肉にく（透過とうか磷酸酶）[1]
代謝たいしゃ產物さんぶつ雌めす激げき素もと藥物やくぶつ、磷酸及雌激げき素的すてき代謝たいしゃ產物さんぶつ[5][6]
生物せいぶつ半はん衰おとろえ期きPEP: 70 days (10 weeks)[7]
Estradiol: 1–2 hours[8]
排泄はいせつ途と徑みち尿にょう）（依よ生物せいぶつ轉化てんか作用さよう）[1]
识别信しん息いき
  • Estra-1,3,5(10)-triene-3,17βべーた-diol, polymer with phosphoric acid
CAS号ごう28014-46-2  checkY
PubChem SID
DrugBank
ChemSpider
  • None
UNII
KEGG
ChEMBL
化学かがく信しん息いき
化学かがく式しき(C18H23O4P)n
(n = variable; n = 13)
摩ま尔质量りょう聚合物ぶつ: 不ふ固定こてい
重じゅう覆くつがえ單元たんげん（英えい语：Repeat unit）: 334.347 g/mol
熔点195至いたり202 °C（383至いたり396 °F）

聚磷酸さん雌めす二に醇あつし（Polyestradiol phosphate），簡稱PEP，藥品やくひん名稱めいしょうEstradurin，是ぜ用よう來らい治療ちりょう男性だんせい前列ぜんれつ腺せん癌がん的てき雌めす激げき素もと（英えい语：Estrogen (medication)）藥品やくひん[1][9][2][10]。也可以用來らい作為さくい治療ちりょう女性じょせい的てき乳癌にゅうがん、是ぜ治療ちりょう低てい雌めす激げき素もと症しょう（英えい语：hypoestrogenism）及更年期こうねんき症狀しょうじょう的てき激げき素もと替がえ代だい療法りょうほう藥物やくぶつ之の一いち，也是給きゅう跨またが性別せいべつ女性じょせい的てき女性じょせい化か賀が爾しか蒙こうむ治療ちりょう[1][11]，以每4個こ星ほし期き一次肌肉注射的方式給藥[1][2][12]。

参考さんこう文献ぶんけん[编辑]

  1. ^ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 Archived copy. [2018-01-01]. （原始げんし内容ないよう存そん档于2018-01-02）. 
  2. ^ 2.0 2.1 2.2 Mikkola A, Ruutu M, Aro J, Rannikko S, Salo J. The role of parenteral polyestradiol phosphate in the treatment of advanced prostatic cancer on the threshold of the new millennium. Ann Chir Gynaecol. 1999, 88 (1): 18–21. ISSN 0355-9521. PMID 10230677. Orchiectomy and estrogens have been used for over 50 years in the treatment of advanced prostatic cancer. Although orchiectomy is a simple procedure, it may cause psychological stress. Oral estrogen therapy is as effective as orchiectomy in terms of cancer inhibitory effect, but its acceptance as primary hormonal treatment is overshadowed by an increased risk of cardiovascular complications. Parenteral estrogen, polyestradiol phosphate (PEP), is effective, but also associated with cardiovascular complications, although to a lesser extent. During the last 20 years, well tolerated luteinizing hormone releasing hormone (LHRH) analogues have been replacing orchiectomy and estrogens. Efforts have been made to increase the efficacy of the treatment by adding antiandrogens to LHRH analogues and also to orchiectomy (combined androgen blockade, CAB). However, the efficacy of LHRH analogues and CAB has not proved to be superior to that of simple orchiectomy and, moreover, they are expensive treatment modalities. Orchiectomy and LHRH analogues are associated with negative effects on bone mass and may cause osteoporosis, whereas PEP treatment has an opposite effect. Parenteral polyestradiol phosphate is still a cheap potential treatment for advanced prostatic cancer, but further studies should be conducted to establish its future role, e.g. combining acetylsalicylic acid to prevent cardiovascular complications. 
  3. ^ Stanczyk, Frank Z.; Archer, David F.; Bhavnani, Bhagu R. Ethinyl estradiol and 17βべーた-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception. 2013, 87 (6): 706–727. ISSN 0010-7824. PMID 23375353. doi:10.1016/j.contraception.2012.12.011. 
  4. ^ Tommaso Falcone; William W. Hurd. Clinical Reproductive Medicine and Surgery. Elsevier Health Sciences. 2007: 22,362,388 [2021-01-26]. ISBN 978-0-323-03309-1. （原始げんし内容ないよう存そん档于2021-04-15）. 
  5. ^ Michael Oettel; Ekkehard Schillinger. Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. 6 December 2012: 261,544 [2021-01-26]. ISBN 978-3-642-60107-1. （原始げんし内容ないよう存そん档于2021-03-07）. Natural estrogens considered here include: [...] Esters of 17βべーた-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17βべーた-estradiol is released; therefore, the esters are considered as natural estrogens. 
  6. ^ Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration (PDF). Climacteric. 2005,. 8 Suppl 1: 3–63 [2021-01-26]. PMID 16112947. S2CID 24616324. doi:10.1080/13697130500148875. （原始げんし内容ないよう (PDF)存そん档于2016-08-22）. 
  7. ^ Stege R, Gunnarsson PO, Johansson CJ, Olsson P, Pousette A, Carlström K. Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin) in prostatic cancer patients. Prostate. May 1996, 28 (5): 307–10. PMID 8610057. doi:10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8. 
  8. ^ Düsterberg B, Nishino Y. Pharmacokinetic and pharmacological features of oestradiol valerate. Maturitas. 1982, 4 (4): 315–24. PMID 7169965. doi:10.1016/0378-5122(82)90064-0. 
  9. ^ Stege R, Carlström K, Hedlund PO, Pousette A, von Schoultz B, Henriksson P. Intramuskuläres Depotöstrogen (Estradurin) in der Behandlung von Patienten mit Prostatakarzinom. Historische Aspekte, Wirkungsmechanismus, Resultate und aktueller klinischer Stand [Intramuscular depot estrogens (Estradurin) in treatment of patients with prostate carcinoma. Historical aspects, mechanism of action, results and current clinical status]. Urologe A. September 1995, 34 (5): 398–403. ISSN 0340-2592. PMID 7483157 （德とく语）. More than 50 years ago, orally given estrogen was already used in the treatment of prostate cancer. Due to cardiovascular side-effects with a high morbidity of 25%, this treatment has not become standard. Recent investigations show that parenteral application reduces the risk of cardiovascular side-effects, because it avoids the first passage through the liver with high concentrations of estrogen which normally occur after oral application. Therefore, an increased synthesis of so-called "steroid-sensitive" liver proteins, such as coagulation factors (especially factor VII) can be avoided. This newer parenteral estrogen application shows encouraging results of a cheap and effective hormonal therapy with a low rate of side-effects in patients with prostate cancer. 
  10. ^ Mikkola, A; Aro, J; Rannikko, S; Ruutu, M; Finnprostate, Group. Ten-year survival and cardiovascular mortality in patients with advanced prostate cancer primarily treated by intramuscular polyestradiol phosphate or orchiectomy. Prostate. March 2007, 67 (4): 447–55. PMID 17219379. S2CID 20549248. doi:10.1002/pros.20547. 
  11. ^ Urdl, W. Behandlungsgrundsätze bei Transsexualität [Therapeutic principles in transsexualism]. Gynäkologische Endokrinologie. 2009, 7 (3): 153–160. ISSN 1610-2894. S2CID 8001811. doi:10.1007/s10304-009-0314-9 （德とく语）. 
  12. ^ Steinbach T, Wurm FR. Poly(phosphoester)s: A New Platform for Degradable Polymers. Angew. Chem. Int. Ed. Engl. 2015, 54 (21): 6098–108. PMID 25951459. doi:10.1002/anie.201500147. 
主題しゅだい
雌めす激げき素もと酯（英えい语：Estrogen ester）
相關そうかん激げき素もと
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