用户名： 密   码：
注册 | 忘记密码？
药品详细

Oxybutynin(奥昔布宁)

化学结构式图
中文名
奥昔布宁
英文名
Oxybutynin
分子式
C22H31NO3
化学名
4-(diethylamino)but-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate
分子量
Average: 357.4864
Monoisotopic: 357.230393863
CAS号
5633-20-5
ATC分类
G04B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination, by decreasing muscle spasms of the bladder. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor.

生产厂家
  • Impax pharmaceuticals
  • Janssen Pharmaceuticals, Inc
  • Mikart inc
  • Mylan pharmaceuticals inc
  • Novex pharma
  • Ortho mcneil janssen pharmaceuticals inc
  • Osmotica pharmaceutical corp
  • Pharmaceutical assoc inc div beach products
  • Pliva inc
  • Quantum pharmics ltd
  • Silarx pharmaceuticals inc
  • Usl pharma inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • Wockhardt eu operations (swiss) ag
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Tupker RA, Harmsze AM, Deneer VH: Oxybutynin therapy for generalized hyperhidrosis. Arch Dermatol. 2006 Aug;142(8):1065-6. Pubmed
  2. Mijnhout GS, Kloosterman H, Simsek S, Strack van Schijndel RJ, Netelenbos JC: Oxybutynin: dry days for patients with hyperhidrosis. Neth J Med. 2006 Oct;64(9):326-8. Pubmed
  3. Schollhammer M, Misery L: Treatment of hyperhidrosis with oxybutynin. Arch Dermatol. 2007 Apr;143(4):544-5. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenylacetates
Substructures
  • Carboxylic Acids and Derivatives
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Acetates
  • Alkynes
  • Phenylacetates
  • Short-chain Hydroxy Acids
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Alcohols and Polyols
  • Aromatic compounds
适应症
药理
Indication For the treatment of overactive bladder.
Pharmacodynamics Oxybutynin is an antispasmodic, anticholinergic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Oxybutynin relaxes bladder smooth muscle. Oxybutynin exhibits only one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. Antimuscarinic activity resides predominantly in the R-isomer.
Mechanism of action Oxybutynin exerts a direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects). By inhibiting particularily the M1 and M2 receptors of the bladder, detrusor activity is markedly decreased.
Absorption Rapidly absorbed from gastrointestinal tract.
Volume of distribution
  • 193 L
Protein binding 91%-93%
Metabolism
Hepatic, primarily by CYP3A4

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Oxybutynin
N-desethyloxybutynin Details
Route of elimination Oxybutynin is metabolized primarily by the cytochrome P450 enzyme systems, particularly CYP3A4, found mostly in the liver and gut wall. Oxybutynin is extensively metabolized by the liver, with less than 0.1% of the administered dose excreted unchanged in the urine. Also, less than 0.1% of the administered dose is excreted as the metabolite N-desethyloxybutynin.
Half life 12.4-13.2 hours
Clearance Not Available
Toxicity LD50=1220 mg/kg (Orally in rats, Goldenthal)
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 129-130 °C Not Available
logP 4.3 Not Available
Predicted Properties
Property Value Source
water solubility 1.00e-02 g/l ALOGPS
logP 4.36 ALOGPS
logP 4.44 ChemAxon
logS -4.5 ALOGPS
pKa (strongest acidic) 11.53 ChemAxon
pKa (strongest basic) 8.77 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 49.77 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 105.26 ChemAxon
polarizability 41.25 ChemAxon
药物相互作用
Drug Interaction
Carbamazepine Oxybutynin may cause carbamazepine toxicity
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Rivastigmine Possible antagonism of action
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Oxybutynin, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Trimethobenzamide Trimethobenzamide and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trospium Trospium and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
食物相互作用
  • Avoid alcohol.
  • Take with food.

返回 | 收藏