Drug nameFlavoxate
DescriptionA 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]
DrugBankPrimary Accession Number: DB01148
DIN02245480
TypeApproved, Small Molecule
IndicationFor symptomatic relief of dysuria, urgency, nocturia, suprapubic pain, frequency and incontinence as may occur in cystitis, prostatitis, urethritis, urethrocystitis/urethrotrigonitis.
Mechanism of ActionFlavoxate 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.
AbsorptionWell absorbed from gastrointestinal tract.
ToxicityThe 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.
Protein BindingNot available
Interactions
RXListhttp://www.rxlist.com/cgi/generic3/flavoxate.htm
KEGGdrug: Not available / compound: C07809
PubChemcompound: 3354 / substance: 10011
PharmGKBPA164781386
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Target
NameGeneEntrezIDSwissprotSNP
Muscarinic acetylcholine receptor M1CHRM11128ACM1_HUMANrs2067477 rs2067478 rs2067480 rs2067479 rs1065435 rs1065431 rs1065429 rs1065428
Muscarinic acetylcholine receptor M2CHRM21129ACM2_HUMANrs61540534 rs60372903 rs36044268 rs34586275 rs11773032 s2278098 rs12721506
FilesDB01148.mol | DB01148_136.pdf | pdb_9250976724834-0.pdb | sdf_3796793014996-0.sdf |
Smilesisomeric:
CC1=C(OC2=C(C=CC=C2C(=O)OCCN2CCCCC2)C1=O)C1=CC=CC=C1
canonical:
CC1=C(OC2=C(C=CC=C2C(=O)OCCN2CCCCC2)C1=O)C1=CC=CC=C1

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