Tìm theo
Oxybutynin
Các tên gọi khác (9 ) :
  • 4-(Diethylamino)-2-butynyl alpha-phenylcyclohexaneglycolic acid ester
  • 4-Diethylamino-2-butinyl alpha-cyclohexylmandelat
  • 4-Diethylamino-2-butynyl alpha-phenylcyclohexaneglycolate
  • Benzeneacetic acid, alpha-cyclohexyl-alpha-hydroxy-, 4-(diethylamino)-2-butynyl ester
  • Cyclohexaneglycolic acid, alpha-phenyl-, 4-(diethylamino)-2-butynyl ester
  • Oxibutinina
  • Oxybutynin
  • Oxybutynine
  • Oxybutyninum
muscarinic antagonists, parasympatholytics, cholinergic antagonists, antispasmodics, muscle relaxants ge
Thuốc Gốc
Small Molecule
CAS: 5633-20-5
ATC: G04BD04
ĐG : Alza Corp.
CTHH: C22H31NO3
PTK: 357.4864
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H31NO3
Phân tử khối
357.4864
Monoisotopic mass
357.230393863
InChI
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
InChI Key
InChIKey=XIQVNETUBQGFHX-UHFFFAOYSA-N
IUPAC Name
4-(diethylamino)but-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate
Traditional IUPAC Name
oxybutynin
SMILES
CCN(CC)CC#CCOC(=O)C(O)(C1CCCCC1)C1=CC=CC=C1
Độ tan chảy
129-130 °C
Độ hòa tan
1.00e-02 g/l
logP
4.3
logS
-4.5
pKa (strongest acidic)
11.53
pKa (Strongest Basic)
8.77
PSA
49.77 Å2
Refractivity
105.26 m3·mol-1
Polarizability
41.25 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from gastrointestinal tract.
▧ Volume of Distribution :
* 193 L
▧ Protein binding :
91%-93%
▧ Metabolism :
Hepatic, primarily by CYP3A4
▧ 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
Độc Tính : LD50=1220 mg/kg (Orally in rats, Goldenthal)
Chỉ Định : For the treatment of overactive bladder.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Patch - Transdermal
Syrup - Oral
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Ditropan
  • Công ty :
    Sản phẩm biệt dược : Gelnique
  • Công ty :
    Sản phẩm biệt dược : Lenditro
  • Công ty :
    Sản phẩm biệt dược : Lyrinel XL
  • Công ty :
    Sản phẩm biệt dược : Oxytrol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01062
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4634
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508005
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07360
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00465
ChemSpider
http://www.chemspider.com/Chemical-Structure.4473.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/52544-920-08
PharmGKB
http://www.pharmgkb.org/drug/PA164746030
Wikipedia
http://en.wikipedia.org/wiki/Oxybutynin
RxList
http://www.rxlist.com/cgi/generic/ditropan.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dit1143.shtml
Drugs.com
http://www.drugs.com/oxybutynin.html
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