格拉司琼

格拉司琼
临床资料
商品名（英语：Drug nomenclature）	Kytril、Sancuso及其他
AHFS/Drugs.com	Monograph
MedlinePlus	a601211
核准状况	欧 EMA: yes;
怀孕分级	澳: B1 ; ;
给药途径	口服给药, 静脉注射, 微针贴片（经皮）
ATC码	A04AA02 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 欧：Rx-only; 英：处方药（℞-only） (POM); 美：处方药（℞-only）;
药物动力学数据
生物利用度	60%
血浆蛋白结合率	65%
药物代谢	肝脏
生物半衰期	3–14小时
排泄途径	尿液11–12%, 粪便38%
识别信息
	IUPAC命名法 1-Methyl-N-((1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1H-indazole-3-carboxamide; ;
CAS号	109889-09-0
PubChem CID	3510;
IUPHAR/BPS	2300; [3H]granisetron: 2292;
DrugBank	DB00889 ;
ChemSpider	10482033 ;
UNII	WZG3J2MCOL;
KEGG	D04370 ;
ChEBI	CHEBI:5537 ;
ChEMBL	ChEMBL519643 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID0023111 ;
ECHA InfoCard	100.212.327
化学信息
化学式	C18H24N4O
摩尔质量	312.42 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CN4[C@@H]1CCC[C@H]4C[C@H](C1)NC(=O)c3nn(C)c2ccccc23;
	InChI InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12-,13+,14- ; Key:MFWNKCLOYSRHCJ-BTTYYORXSA-N ;

格拉司琼（INN:granisetron）是一种血清素5-HT3受体拮抗剂（英语：5-HT3 antagonist），作止吐剂使用，以治疗化学疗法和放射治疗后出现的恶心和呕吐。^[2]它的主要作用是降低迷走神经的活性，迷走神经是一种激活延脑呕吐中枢的神经。它对晕动病引起的呕吐没有太大作用。^[3]这种药物对多巴胺受体或毒蕈碱型乙酰胆碱受体没有任何作用。^[3]

格拉司琼是由在英国制药公司Beecham集团（英语：Beechham Group）服务的化学家于大约1985年开发成功，并取得专利，于1991年获得英国批准用于医疗用途。^[4]并于1994年获得美国食品药物管理局（FDA）核准用于医疗用途。此药物已列入世界卫生组织基本药物标准清单内。^[5]

由罗氏制药生产的格拉司琼，以商品名称Kytril贩售。有一种名为Sancuso的格拉司琼制剂，于2008年9月12日获得FDA批准。^[6]Sancuso由3M公司旗下的3M Drug Delivery Systems为协和麒麟制药公司生产。市面上有此药物的通用名药物（学名药）贩售。^[7]

医疗用途

化学疗法

此药物可用于治疗化学疗法引起的恶心和呕吐，且效力似乎与另一名列世界卫生组织基本药物标准清单中的昂丹司琼大致相同。^[8]昂丹司琼于2022年是美国排名第61的最常使用处方药，开立的处方笺数量有1千万张。^[9]^[10]

手术后

包括格拉司琼在内的许多药物似乎都能有效控制术后恶心和呕吐（英语：Postoperative nausea and vomiting）（PONV）。^[11]目前尚不清楚它是否比其他药物（如多潘立酮、甲氧氯普胺或昂丹司琼）更有效或是更无效。^[12]

胃轻瘫

格拉司琼贴片（Sancuso）已被研究用于治疗胃轻瘫，^[13]但尚未获得FDA批准用于此适应症。^[14]

其他

可能是治疗急性或慢性疾病或急性肠胃炎引起的恶心和呕吐的疗法。^[15]
治疗周期性呕吐症候群（英语：Cyclic vomiting syndrome），但尚无正式试验证实其疗效。

不良反应

格拉司琼是一种耐受性良好的药物。^[16]副作用很少，仅为头痛、头晕和便秘。^[17]尚未报导使用该药物时会出现显著的药物交互作用。^[18]它在人体内由肝脏的细胞色素P450系统分解，^[19]对经此肝酶系统进行代谢的其他药物影响很小。

特定群体

怀孕

在动物实验中，无论是静脉注射或口服给药，均未发现对于胎儿有致畸性的证据。然而，针对人类的怀孕个体对照试验数据仍付之阙如。但仅在个体明确需要且效益大于风险时，才建议使用。^[20]

母乳哺育

对于母乳哺育的婴儿以及乳汁分泌的影响，目前仍属未知。应权衡药物对母亲的必要性，做出停止哺乳或停止用药的决定。^[20]

缓释剂型

有种格拉司琼的缓释注射剂型，商品名称为Sustol，自2016年起在美国上市。^[21]这种长效剂型用于治疗中度致吐化疗，以及蒽环类药物和/或环磷酰胺（anthrocycline and/or cyclophosphamide，简称AC）高度致吐方案，所引起的急性和延迟性恶心和呕吐（Chemotherapy-Induced Nausea and Vomiting，简称CINV）。FDA在审查Sustol的申请后，认为该药物的主要应用范围集中于AC方案（只要在乳癌），且相关数据不足，FDA未认可该药物可广泛应用于高度致吐性化疗（Highly Emetogenic Chemotherapy，简称HEC）。^[22]

参考文献

^ Sancuso EPAR. European Medicines Agency (EMA). 2012-04-20 [2024-12-03]. （原始内容存档于2021-01-08）.
^ Stevens, Jonathan R.; Coffey, M. Justin. The Use of Transdermal Therapeutic Systems in Psychiatric Care: A Primer on Patches. Psychosomatics. September–October 2015, 56 (5): 423–444 [2025-03-04]. doi:10.1016/j.psym.2015.03.007.
^ ^3.0 ^3.1 Jacoby, Henry I. Gastric Emptying. Reference Module in Biomedical Sciences 2017. 2017 [2025-03-04]. doi:10.1016/B978-0-12-801238-3.64921-8.
^ Fischer J, Ganellin CR. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 448. ISBN 9783527607495 （英语）.
^ World Health Organization. World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. hdl:10665/345533 . WHO/MHP/HPS/EML/2021.02.
^ FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy. PRNewswire. September 12, 2008 [2025-03-26]. （原始内容存档于2021-04-10）.
^ Granisetron. RxList. [2025--03-04].
^ Giglio, A del; Soares, H P. Granisetron is equivalent to ondansetron for prophylaxis of chemotherapy-induced nausea and vomiting: results of a meta-analysis of randomized controlled trials. Cancer. 2000-12-01, 89 (11): 2301–8 [2025-03-04]. doi:10.1002/1097-0142(20001201)89:11<2301::aid-cncr19>3.0.co;2-6.
^ The Top 300 of 2022. ClinCalc. [2024-08-30]. （原始内容存档于2024-08-30）.
^ Ondansetron Drug Usage Statistics, United States, 2013 - 2022. ClinCalc. [2024-08-30]. （原始内容存档于2020-07-08）.
^ Ngo AL, Orhurhu V, Urits I, Delfin EO, Sharma M, Jones MR, Viswanath O, Urman RD. Extended release granisetron: Review of pharmacologic considerations and clinical role in the perioperative setting. Saudi Journal of Anaesthesia. July 2019, 13 (3): 231–236. PMC 6625288 . PMID 31333369. doi:10.4103/sja.SJA_817_18 .
^ Carlisle JB, Stevenson CA. Carlisle J , 编. Drugs for preventing postoperative nausea and vomiting. The Cochrane Database of Systematic Reviews. July 2006, 2006 (3): CD004125. PMC 6463839 . PMID 16856030. doi:10.1002/14651858.CD004125.pub2. （已撤稿，见doi:10.1002/14651858.CD004125.pub3, PMID 28715610)
^ Midani D, Parkman HP. Granisetron Transdermal System for Treatment of Symptoms of Gastroparesis: A Prescription Registry Study. Journal of Neurogastroenterology and Motility. October 2016, 22 (4): 650–655. PMC 5056574 . PMID 27400689. doi:10.5056/jnm15203.
^ Sancuso Full Prescribing Information (PDF). U.S. Food and Drug Administration. September 2015 [2019-11-29]. （原始内容存档 (PDF)于2021-04-15）.
^ Granisetron HCl Injection. Advacare Pharma. [2025-03-03].
^ Plosker, G L; Goa, K L. Granisetron. A review of its pharmacological properties and therapeutic use as an antiemetic. Drugs. November 1991, 4 (25): 805–24 [2025-03-04]. doi:10.2165/00003495-199142050-00007.
^ Granisetron. Drugs.com. [2025-03-04].
^ Granisetron (PDF). FDA. [2025-03-04].
^ Bloomer, J C; Baldwin, S J. Characterisation of the cytochrome P450 enzymes involved in the in vitro metabolism of granisetron. British Journal of Clinical Pharmacology. December 1994, 3 (86): 557–66 [2025-03-04]. doi:10.1111/j.1365-2125.1994.tb04397.x. 请检查|doi=值 (帮助).
^ ^20.0 ^20.1 RGranisetron Pregnancy and Breastfeeding Warnings. Drug.com. [2025-03-04]. （原始内容存档于2021-01-25）.
^ Drugs.com Heron Therapeutics Announces FDA Approval of Sustol (granisetron) Extended-Release Injection for the Prevention of Chemotherapy-Induced Nausea and Vomiting （页面存档备份，存于互联网档案馆）
^ FDA.gov Sustol Prescribing Information （页面存档备份，存于互联网档案馆）.

延伸阅读

Aapro M. Granisetron: an update on its clinical use in the management of nausea and vomiting. The Oncologist. 2004, 9 (6): 673–86. PMID 15561811. doi:10.1634/theoncologist.9-6-673.

[1] Sancuso EPAR. European Medicines Agency (EMA). 2012-04-20 [2024-12-03]. （原始内容存档于2021-01-08）.

[2] Stevens, Jonathan R.; Coffey, M. Justin. The Use of Transdermal Therapeutic Systems in Psychiatric Care: A Primer on Patches. Psychosomatics. September–October 2015, 56 (5): 423–444 [2025-03-04]. doi:10.1016/j.psym.2015.03.007.

[aa-3] 3.0 ^3.1 Jacoby, Henry I. Gastric Emptying. Reference Module in Biomedical Sciences 2017. 2017 [2025-03-04]. doi:10.1016/B978-0-12-801238-3.64921-8.

[4] Fischer J, Ganellin CR. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 448. ISBN 9783527607495 （英语）.

[WHO22nd-5] World Health Organization. World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. hdl:10665/345533 . WHO/MHP/HPS/EML/2021.02.

[6] FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy. PRNewswire. September 12, 2008 [2025-03-26]. （原始内容存档于2021-04-10）.

[7] Granisetron. RxList. [2025--03-04].

[8] Giglio, A del; Soares, H P. Granisetron is equivalent to ondansetron for prophylaxis of chemotherapy-induced nausea and vomiting: results of a meta-analysis of randomized controlled trials. Cancer. 2000-12-01, 89 (11): 2301–8 [2025-03-04]. doi:10.1002/1097-0142(20001201)89:11<2301::aid-cncr19>3.0.co;2-6.

[9] The Top 300 of 2022. ClinCalc. [2024-08-30]. （原始内容存档于2024-08-30）.

[10] Ondansetron Drug Usage Statistics, United States, 2013 - 2022. ClinCalc. [2024-08-30]. （原始内容存档于2020-07-08）.

[Ngo2019-11] Ngo AL, Orhurhu V, Urits I, Delfin EO, Sharma M, Jones MR, Viswanath O, Urman RD. Extended release granisetron: Review of pharmacologic considerations and clinical role in the perioperative setting. Saudi Journal of Anaesthesia. July 2019, 13 (3): 231–236. PMC 6625288 . PMID 31333369. doi:10.4103/sja.SJA_817_18 .

[Carl2006-12] Carlisle JB, Stevenson CA. Carlisle J , 编. Drugs for preventing postoperative nausea and vomiting. The Cochrane Database of Systematic Reviews. July 2006, 2006 (3): CD004125. PMC 6463839 . PMID 16856030. doi:10.1002/14651858.CD004125.pub2. （已撤稿，见doi:10.1002/14651858.CD004125.pub3, PMID 28715610)

[:0-13] Midani D, Parkman HP. Granisetron Transdermal System for Treatment of Symptoms of Gastroparesis: A Prescription Registry Study. Journal of Neurogastroenterology and Motility. October 2016, 22 (4): 650–655. PMC 5056574 . PMID 27400689. doi:10.5056/jnm15203.

[14] Sancuso Full Prescribing Information (PDF). U.S. Food and Drug Administration. September 2015 [2019-11-29]. （原始内容存档 (PDF)于2021-04-15）.

[15] Granisetron HCl Injection. Advacare Pharma. [2025-03-03].

[16] Plosker, G L; Goa, K L. Granisetron. A review of its pharmacological properties and therapeutic use as an antiemetic. Drugs. November 1991, 4 (25): 805–24 [2025-03-04]. doi:10.2165/00003495-199142050-00007.

[17] Granisetron. Drugs.com. [2025-03-04].

[18] Granisetron (PDF). FDA. [2025-03-04].

[19] Bloomer, J C; Baldwin, S J. Characterisation of the cytochrome P450 enzymes involved in the in vitro metabolism of granisetron. British Journal of Clinical Pharmacology. December 1994, 3 (86): 557–66 [2025-03-04]. doi:10.1111/j.1365-2125.1994.tb04397.x. 请检查|doi=值 (帮助).

[Drugs.com-20] 20.0 ^20.1 RGranisetron Pregnancy and Breastfeeding Warnings. Drug.com. [2025-03-04]. （原始内容存档于2021-01-25）.

[21] Drugs.com Heron Therapeutics Announces FDA Approval of Sustol (granisetron) Extended-Release Injection for the Prevention of Chemotherapy-Induced Nausea and Vomiting （页面存档备份，存于互联网档案馆）

[22] FDA.gov Sustol Prescribing Information （页面存档备份，存于互联网档案馆）.

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