亮丙瑞林

亮丙瑞林
临床资料
商品名（英语：Drug nomenclature）	Lupron, Eligard, Lucrin, Lupaneta, others
其他名称	leuprolide, leuprolidine, A-43818, Abbott-43818, DC-2-269, TAP-144
AHFS/Drugs.com	Monograph
MedlinePlus	a685040
核准状况	美 DailyMed: Leuprolide;
怀孕分级	澳: D ; ;
给药途径	植入物、皮下注射、肌肉注射
药物类别（英语：Drug class）	促性腺素释素相似剂（英语：GnRH analogue）; 促性腺素释素刺激剂（英语：GnRH agonist）; 抗促性腺素（英语：Antigonadotropin）
ATC码	L02AE02 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 加：处方药（℞-only）; 欧：Rx-only; 美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
生物半衰期	3小时
排泄途径	肾
识别信息
	IUPAC命名法 N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(diaminomethylideneamino)-1-; [2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxo-pentan-2-; yl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl-; butyl]carbamoyl]-2-(4-hydroxyphenyl)ethyl]; carbamoyl]-2-hydroxy-ethyl]carbamoyl]-2-(1H-indol-3-; yl)ethyl]carbamoyl]-2-(3H-imidazol-4-yl)ethyl]-5-oxo-; pyrrolidine-2-carboxamide; ;
CAS号	53714-56-0（; 74381-53-6 (乙酸盐)）
PubChem CID	657181;
IUPHAR/BPS	1175;
DrugBank	DB00007 ;
ChemSpider	571356 ;
UNII	EFY6W0M8TG;
KEGG	D08113 ;
ChEMBL	ChEMBL1201199 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID50872411 ;
ECHA InfoCard	100.161.466
化学信息
化学式	C59H84N16O12
摩尔质量	1,209.42 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc3c[nH]c4c3cccc4)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@@H]6CCC(=O)N6;
	InChI InChI=1S/C59H84N16O12/c1-6-63-57(86)48-14-10-22-75(48)58(87)41(13-9-21-64-59(60)61)68-51(80)42(23-32(2)3)69-52(81)43(24-33(4)5)70-53(82)44(25-34-15-17-37(77)18-16-34)71-56(85)47(30-76)74-54(83)45(26-35-28-65-39-12-8-7-11-38(35)39)72-55(84)46(27-36-29-62-31-66-36)73-50(79)40-19-20-49(78)67-40/h7-8,11-12,15-18,28-29,31-33,40-48,65,76-77H,6,9-10,13-14,19-27,30H2,1-5H3,(H,62,66)(H,63,86)(H,67,78)(H,68,80)(H,69,81)(H,70,82)(H,71,85)(H,72,84)(H,73,79)(H,74,83)(H4,60,61,64)/t40-,41-,42-,43+,44-,45-,46-,47-,48-/m0/s1 ; Key:GFIJNRVAKGFPGQ-LIJARHBVSA-N ;

亮丙瑞林（Leuprorelin、leuprolide），商品名柳菩林（Lupron），^[10]是一种人工合成的激素，用于治疗前列腺癌、乳癌、子宫内膜异位症、子宫肌瘤和性早熟（英语：Precocious puberty）^[10] ^[11]。可以肌肉或皮下注射^[10]。

常见副作用包括潮热、情绪不稳定、失眠、头痛和注射部位疼痛^[10]。其他副作用包括可能高血糖、过敏和脑下垂体中风（英语：Pituitary apoplexy）^[10]。怀孕期使用可能会伤害婴儿^[10]。它属于促性腺素释素调节剂（英语：Gonadotropin-releasing hormone modulator）家族， ^[10]可降低促性腺激素，而降低睾酮和雌二醇^[10]。

亮丙瑞林于 1973 年获得专利，于 1985 年取得美国的医疗使用许可^[10] ^[12]。名列世界卫生组织基本药物清单^[13]。

参考文献

^ ELIGARD (Mundipharma Pty Ltd) Department of Health and Aged Care. Retrieved 30 March 2023
^ Product monograph brand safety updates. Health Canada. February 2024 [24 March 2024].
^ Regulatory Decision Summary for Eligard. Drug and Health Products Portal. 21 September 2023 [2 April 2024].
^ Lupron- leuprolide acetate lupron- leuprolide acetate injection, solution. DailyMed. [27 May 2021]. （原始内容存档于27 May 2021）.
^ Eligard- leuprolide acetate kit. DailyMed. 26 March 2020 [20 August 2020]. （原始内容存档于10 August 2020）.
^ Fensolvi- leuprolide acetate kit. DailyMed. 3 June 2020 [20 August 2020]. （原始内容存档于26 October 2020）.
^ Viadur- leuprolide acetate. DailyMed. [26 May 2021]. （原始内容存档于27 May 2021）.
^ Lupron Depot- leuprolide acetate kit. DailyMed. [27 May 2021]. （原始内容存档于27 May 2021）.
^ Camcevi EPAR. European Medicines Agency (EMA). 22 March 2022 [21 June 2022].
^ ^10.0 ^10.1 ^10.2 ^10.3 ^10.4 ^10.5 ^10.6 ^10.7 ^10.8 Leuprolide Acetate. The American Society of Health-System Pharmacists. [8 December 2016]. （原始内容存档于23 December 2016）. "Leuprolide Acetate". The American Society of Health-System Pharmacists. Archived from the original on 23 December 2016. Retrieved 8 December 2016.
^ 19th WHO Model List of Essential Medicines (April 2015) (PDF). WHO. April 2015 [May 10, 2015]. （原始内容存档 (PDF)于May 13, 2015）.
^ Fischer, Jnos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 514 [2019-03-02]. ISBN 9783527607495. （原始内容存档于2019-03-06）（英语）.
^ World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.

延伸阅读

Shajnfeld A, Krueger RB. Reforming (Purportedly) Non-Punitive Responses to Sexual Offending. Developments in Mental Health Law. July 2006, 25: 81. SSRN 1077282 .

[1] ELIGARD (Mundipharma Pty Ltd) Department of Health and Aged Care. Retrieved 30 March 2023

[2] Product monograph brand safety updates. Health Canada. February 2024 [24 March 2024].

[3] Regulatory Decision Summary for Eligard. Drug and Health Products Portal. 21 September 2023 [2 April 2024].

[Lupron_FDA_label-4] Lupron- leuprolide acetate lupron- leuprolide acetate injection, solution. DailyMed. [27 May 2021]. （原始内容存档于27 May 2021）.

[Eligard_FDA_label-5] Eligard- leuprolide acetate kit. DailyMed. 26 March 2020 [20 August 2020]. （原始内容存档于10 August 2020）.

[Fensolvi_FDA_label-6] Fensolvi- leuprolide acetate kit. DailyMed. 3 June 2020 [20 August 2020]. （原始内容存档于26 October 2020）.

[Viadur_FDA_label-7] Viadur- leuprolide acetate. DailyMed. [26 May 2021]. （原始内容存档于27 May 2021）.

[Lupron_Depot_FDA_label-8] Lupron Depot- leuprolide acetate kit. DailyMed. [27 May 2021]. （原始内容存档于27 May 2021）.

[Camcevi_EPAR-9] Camcevi EPAR. European Medicines Agency (EMA). 22 March 2022 [21 June 2022].

[AHFS2016-11] 10.0 ^10.1 ^10.2 ^10.3 ^10.4 ^10.5 ^10.6 ^10.7 ^10.8 Leuprolide Acetate. The American Society of Health-System Pharmacists. [8 December 2016]. （原始内容存档于23 December 2016）. "Leuprolide Acetate". The American Society of Health-System Pharmacists. Archived from the original on 23 December 2016. Retrieved 8 December 2016.

[WHO2015E-12] 19th WHO Model List of Essential Medicines (April 2015) (PDF). WHO. April 2015 [May 10, 2015]. （原始内容存档 (PDF)于May 13, 2015）.

[Fis2006-13] Fischer, Jnos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 514 [2019-03-02]. ISBN 9783527607495. （原始内容存档于2019-03-06）（英语）.

[WHO21st-14] World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.

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