奥昔布宁

奥昔布宁(Oxybutynin),商品名DitropanLyrinel XLLenditro (ZA)Driptane (RU)Uripan (Middle East)[1],为一种抗胆碱剂,可以缓解膀胱排尿困难,包含频尿及尿失禁等症状,可以降低膀胱肌肉痉挛[2]。本品也可用于帮助缓解与肾结石相关的症状。

奥昔布宁
临床资料
商品名英语Drug nomenclatureDitropan
AHFS/Drugs.comMonograph
MedlinePlusa682141
核准状况
怀孕分级
给药途径口服给药transdermal英语transdermal gel、transdermal patch英语transdermal patch
ATC码
法律规范状态
法律规范
药物动力学数据
血浆蛋白结合率91–93%
生物半衰期12.4–13.2 hours
识别信息
  • 4-Diethylaminobut-2-ynyl 2-cyclohexyl-2-hydroxy-2-phenylethanoate
CAS号5633-20-5  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.158.590 编辑维基数据链接
化学信息
化学式C22H31NO3
摩尔质量357.486 g/mol
3D模型(JSmol英语JSmol
  • O=C(OCC#CCN(CC)CC)C(O)(c1ccccc1)C2CCCCC2
  • InChI=1S/C22H31NO3/c1-3-23(4-2)17-11-12-18-26-21(24)22(25,19-13-7-5-8-14-19)20-15-9-6-10-16-20/h5,7-8,13-14,20,25H,3-4,6,9-10,15-18H2,1-2H3 checkY
  • Key:XIQVNETUBQGFHX-UHFFFAOYSA-N checkY

本品可竞争性拮抗M1英语Muscarinic acetylcholine receptor M1M2英语Muscarinic acetylcholine receptor M2,及M3英语Muscarinic acetylcholine receptor M3蕈毒碱型乙酰胆碱受体

本品可能也可用于治疗多汗症[3][4][5]

立体化学

奥昔布宁含有一个立体中心,由两种对映体组成。这是外消旋体,即1:(R)的1:1混合物 - 和(S)形式:[6][7]

奥昔布宁的对映体
 
CAS-Nummer: 119618-21-2
 
CAS-Nummer: 119618-22-3

参考文献

  1. ^ Uripan Tablets. Adwia Pharmaceuticals. [22 November 2015]. (原始内容存档于2020-10-26). 
  2. ^ Chapple CR. "Muscarinic receptor antagonists in the treatment of overactive bladder". Urology (55)5, Supp. 1:33-46, 2000.
  3. ^ Tupker RA, Harmsze AM, Deneer VH. Oxybutynin therapy for generalized hyperhidrosis.. Arch Dermatol. 2006, 142 (8): 1065–6. PMID 16924061. doi:10.1001/archderm.142.8.1065. 
  4. ^ Mijnhout GS, Kloosterman H, Simsek S, Strack van Schijndel RJ, Netelenbos JC. Oxybutynin: dry days for patients with hyperhidrosis.. Neth J Med. 2006, 64 (9): 326–8. PMID 17057269. 
  5. ^ Schollhammer M, Misery L. Treatment of hyperhidrosis with oxybutynin.. Arch Dermatol. 2007, 143 (4): 544–5. PMID 17438194. doi:10.1001/archderm.143.4.544. 
  6. ^ Kachur JF, et al. R and S enantiomers of oxybutynin: pharmacological effects in guinea pig bladder and intestine, Journal of Pharmacology and Experimental Therapeutics, 247, S. 867–872, 1988; PMID 2849672.
  7. ^ Noronha-Blob L, Kachur JF. Enantiomers of oxybutynin: in vitro pharmacological characterization at M1, M2 and M3 muscarinic receptors and in vivo effects on urinary bladder contraction, mydriasis and salivary secretion in guinea pigs, Journal of Pharmacology and Experimental Therapeutics, 256, S. 562–567, 1991; PMID 1993995.

外部链接

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