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伯氨喹

伯氨喹
临床资料
其他名称primaquine phosphate
AHFS/Drugs.comMonograph
MedlinePlusa607037
核准状况
给药途径By mouth
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度96%[1]
药物代谢Liver
生物半衰期6 hours
识别信息
  • (RS)-N-(6-methoxyquinolin-8-yl)pentane-1,4-diamine
CAS号90-34-6  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.001.807 编辑维基数据链接
化学信息
化学式C15H21N3O
摩尔质量259.347
3D模型(JSmol英语JSmol
手性Racemic mixture
  • O(c1cc(NC(C)CCCN)c2ncccc2c1)C
  • InChI=1S/C15H21N3O/c1-11(5-3-7-16)18-14-10-13(19-2)9-12-6-4-8-17-15(12)14/h4,6,8-11,18H,3,5,7,16H2,1-2H3 checkY
  • Key:INDBQLZJXZLFIT-UHFFFAOYSA-N checkY

伯氨喹(英语:Primaquine),是一种药物,用于治疗和预防疟疾及治疗肺囊虫肺炎[2],尤其是当其他药物都不能使用时,可用于预防与治疗间日疟原虫卵形疟原虫引起的疟疾[2];此品可与克林霉素并用作为治疗肺囊虫肺炎的替代处方[2][3]。给药途径为口服[2]

常见副作用为恶心、呕吐及腹绞痛[2][4],因为溶血反应的风险很高[4],伯氨喹不能用于蚕豆症患者;也不建议用于怀孕患者[5][6]。如果确认婴儿并非蚕豆症患者,母乳哺育的母亲是可以使用的[6]。本品的作用机转尚不明朗,但据信对疟疾寄生虫的DNA有其作用[2]

1946 年,伯氨喹问世[3];名列世界卫生组织基本药物标准清单,认可为医疗系统中最安全有效的药品[7],市面上可取得其学名药[2]。在发展中国家的批发价为单日 0.04 美元到 0.11 美元[8],在美国,整套疗程的药费为 50 美元到 100 美元[5]

附注

  1. ^ Mihaly GW, Ward SA, Edwards G, et al. Pharmacokinetics of primaquine in man. I. Studies of the absolute bioavailability and effects of dose size. Br J Clin Pharmacol. 1985, 19 (6): 745–50. PMC 1463857可免费查阅. PMID 4027117. doi:10.1111/j.1365-2125.1985.tb02709.x. 
  2. ^ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 Primaquine Phosphate. The American Society of Health-System Pharmacists. [2 December 2016]. (原始内容存档于20 December 2016). 
  3. ^ 3.0 3.1 Vale, Nuno; Moreira, Rui; Gomes, Paula. Primaquine revisited six decades after its discovery. European Journal of Medicinal Chemistry. March 2009, 44 (3): 937–953. PMID 18930565. doi:10.1016/j.ejmech.2008.08.011. 
  4. ^ 4.0 4.1 Arguin, Paul M.; Tan, Kathrine R. Malaria - Chapter 3. Brunette, Gary W. (编). CDC Health Information for International Travel 2016 (Yellow Book). CDC and Oxford University Press. 2016. ISBN 978-0-19-937915-6. (原始内容存档于2016-01-14). 
  5. ^ 5.0 5.1 Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 57. ISBN 9781284057560. 
  6. ^ 6.0 6.1 Hill, D. R.; Baird, J. K.; Parise, M. E.; Lewis, L. S.; Ryan, E. T.; Magill, A. J. Primaquine: Report from CDC expert meeting on malaria chemoprophylaxis I. The American Journal of Tropical Medicine and Hygiene. 2006, 75 (3): 402–15. PMID 16968913. doi:10.4269/ajtmh.2006.75.402. (原始内容存档于2014-01-23). 
  7. ^ WHO Model List of Essential Medicines (19th List) (PDF). World Health Organization. April 2015 [8 December 2016]. (原始内容 (PDF)存档于13 December 2016). 
  8. ^ Primaquine. International Drug Price Indicator Guide. [3 December 2016]. (原始内容存档于2018-10-08). 
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伯氨喹
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