Tìm theo
Flavoxate
Các tên gọi khác (8 ) :
  • 2-(1-Piperidinyl)ethyl 3-methyl-4-oxo-2-phenyl-4H-chromene-8-carboxylate
  • 2-Piperidinoethyl 3-methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylate
  • 2-Piperidinoethyl 3-methylflavone-8-carboxylate
  • beta-Piperidinoethyl 3-methylflavone-8-carboxylate
  • Flavoxate
  • Flavoxate HCI
  • Flavoxato
  • Flavoxatum
parasympatholytics
Thuốc Gốc
Small Molecule
CAS: 15301-69-6
ATC: G04BD02
ĐG : Alza Corp.
CTHH: C24H25NO4
PTK: 391.4596
A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H25NO4
Phân tử khối
391.4596
Monoisotopic mass
391.178358293
InChI
InChI=1S/C24H25NO4/c1-17-21(26)19-11-8-12-20(23(19)29-22(17)18-9-4-2-5-10-18)24(27)28-16-15-25-13-6-3-7-14-25/h2,4-5,8-12H,3,6-7,13-16H2,1H3
InChI Key
InChIKey=SPIUTQOUKAMGCX-UHFFFAOYSA-N
IUPAC Name
2-(piperidin-1-yl)ethyl 3-methyl-4-oxo-2-phenyl-4H-chromene-8-carboxylate
Traditional IUPAC Name
flavoxate
SMILES
CC1=C(OC2=C(C=CC=C2C(=O)OCCN2CCCCC2)C1=O)C1=CC=CC=C1
Độ tan chảy
232-234
Độ hòa tan
10 mg/L (at 37 °C)
logP
4.4
logS
-4.4
pKa (Strongest Basic)
7.29
PSA
55.84 Å2
Refractivity
113.51 m3·mol-1
Polarizability
43.39 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
pKa
7.3
Dược Lực Học : Flavoxate is a spasmolytic flavone derivative that acts by relaxing the smooth muscle in the urinary tract. Flavoxate is a competitive muscarinic receptor antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Muscarinic receptors play an important role in several major cholin-ergically mediated functions, including contractions of urinary bladder smooth muscle and stimulation of salivary secretion.
Cơ Chế Tác Dụng : A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist. [PubChem] Flavoxate acts as a direct antagonist at muscarinic acetylcholine receptors in cholinergically innervated organs. Its anticholinergic-parasympatholytic action reduces the tonus of smooth muscle in the bladder, effectively reducing the number of required voids, urge incontinence episodes, urge severity and improving retention, facilitating increased volume per void.
Dược Động Học :
▧ Absorption :
Well absorbed from gastrointestinal tract.
▧ Route of Elimination :
57% of the flavoxate HCl was excreted in the urine within 24 hours.
Độc Tính : The oral LD50 for flavoxate HCl in rats is 4273 mg/kg. The oral LD50 for flavoxate HCl in mice is 1837 mg/kg. Symptoms of overdose include convulsions, decreased ability to sweat, (warm, red skin, dry mouth, and increased body temperature), hallucinations, increased heart rate and blood pressure, and mental confusion.
Chỉ Định : For symptomatic relief of dysuria, urgency, nocturia, suprapubic pain, frequency and incontinence as may occur in cystitis, prostatitis, urethritis, urethrocystitis/urethrotrigonitis.
Tương Tác Thuốc :
  • 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, Flavoxate, 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 Flavoxate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Flavoxate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Flavoxate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Sanofi
    Sản phẩm biệt dược : Bladuril
  • Công ty : Daito
    Sản phẩm biệt dược : Flavosert
  • Công ty : Sanwa Kagaku
    Sản phẩm biệt dược : Progut
  • Công ty : Sawai Seiyaku
    Sản phẩm biệt dược : Sawadaron
  • Công ty : Johnson
    Sản phẩm biệt dược : Uridron
  • Công ty : Farmindustria
    Sản phẩm biệt dược : Uripax
  • Sản phẩm biệt dược : Urispas
  • Công ty : Sandoz
    Sản phẩm biệt dược : Uroxal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01148
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3354
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505138
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07809
ChemSpider
http://www.chemspider.com/Chemical-Structure.3237.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0574-0115-01
PharmGKB
http://www.pharmgkb.org/drug/PA164781386
Wikipedia
http://en.wikipedia.org/wiki/Flavoxate
RxList
http://www.rxlist.com/cgi/generic3/flavoxate.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/uri1471.shtml
Drugs.com
http://www.drugs.com/cdi/flavoxate.html
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