奧昔布寧(Oxybutynin),商品名DitropanLyrinel XLLenditro (ZA)Driptane (RU)Uripan (Middle East)[1],為一種抗膽鹼劑,可以緩解膀胱排尿困難,包含頻尿及尿失禁等症狀,可以降低膀胱肌肉痙攣[2]。本品也可用於幫助緩解與腎結石相關的症狀。

奧昔布寧
臨床資料
商品名英語Drug nomenclatureDitropan
AHFS/Drugs.comMonograph
MedlinePlusa682141
核准狀況
懷孕分級
給藥途徑口服給藥transdermal英語transdermal gel、transdermal patch英語transdermal patch
ATC碼
法律規範狀態
法律規範
藥物動力學數據
血漿蛋白結合率91–93%
生物半衰期12.4–13.2 hours
識別資訊
  • 4-Diethylaminobut-2-ynyl 2-cyclohexyl-2-hydroxy-2-phenylethanoate
CAS號5633-20-5  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.158.590 編輯維基數據鏈接
化學資訊
化學式C22H31NO3
摩爾質量357.486 g/mol
3D模型(JSmol英語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

本品可競爭性拮抗M1英語Muscarinic acetylcholine receptor M1M2英語Muscarinic acetylcholine receptor M2,及M3英語Muscarinic acetylcholine receptor M3蕈毒鹼型乙醯膽鹼受體

本品可能也可用於治療多汗症[3][4][5]

立體化學

編輯

奧昔布寧含有一個立體中心,由兩種對映體組成。這是外消旋體,即1:(R)的1:1混合物 - 和(S)形式:[6][7]

奧昔布寧的對映體
 
CAS-Nummer: 119618-21-2
 
CAS-Nummer: 119618-22-3

參考文獻

編輯
  1. ^ Uripan Tablets. Adwia Pharmaceuticals. [22 November 2015]. (原始內容存檔於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.

外部連結

編輯

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