flavoxate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
1175 15301-69-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • urispas
  • flavoxate
  • flavoxate hydrochloride
  • flavoxate HCl
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.
  • Molecular weight: 391.47
  • Formula: C24H25NO4
  • CLOGP: 4.97
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 55.84
  • ALOGS: -4.41
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ
S (Water solubility) 6.60 mg/mL Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 100 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.626 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.558 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 25.882 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 72.778 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 3.330 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 8.390 % High 1
herg hERG pIC50 5.886 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 73.114 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 235.505 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 2.730 % High 1
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,KIT,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2 61
kinase-selectivity-class ACVR2A,ACVR2B,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK9,DDR1,DYRK1B,EPHB4,ERBB2,FLT3,GRK2,MAP2K3,MAP3K21,MAP4K1,MAPK12,MAPK7,MARK4,MTOR,PDK4,PIK3CD,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,TYRO3,ULK1 33
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.471 High 1
mh-clint Mouse hepatocyte intrinsic clearance 366.438 High 1
mppb Mouse plasma protein binding (% unbound) 4.930 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.622 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 8.790 % High 1
rh-clint Rat hepatocyte intrinsic clearance 314.051 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 22.870 % High 1
rppb Rat plasma protein binding (% unbound) 2.780 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 16.520 uM High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 15, 1970 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Soft tissue disorder 433.72 56.54 77 2106 4213 90622051
Pneumonia viral 285.30 56.54 61 2122 8762 90617502
Liver function test abnormal 273.98 56.54 84 2099 50761 90575503
Herpes zoster 226.45 56.54 85 2098 94559 90531705
Leukopenia 221.31 56.54 85 2098 100625 90525639
Arthritis 173.56 56.54 83 2100 167232 90459032
Blood cholesterol increased 159.28 56.54 84 2099 207928 90418336
Fibromyalgia 157.09 56.54 83 2100 206186 90420078
Peripheral swelling 137.92 56.54 98 2085 413008 90213256
Synovitis 121.02 56.54 83 2100 329669 90296595
Anaemia 120.60 56.54 85 2098 352717 90273547
Oral pain 118.27 56.54 40 2143 32643 90593621
Infection 116.30 56.54 84 2099 362010 90264254
Arteriovenous fistula occlusion 89.05 56.54 14 2169 357 90625907
Joint swelling 86.07 56.54 81 2102 503219 90123045
Blue toe syndrome 85.27 56.54 14 2169 472 90625792
Therapeutic product effect incomplete 76.09 56.54 51 2132 193845 90432419
Tenderness 70.82 56.54 26 2157 26842 90599422

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Soft tissue disorder 239.05 41.51 43 1893 3481 110583882
Pneumonia viral 217.00 41.51 48 1888 11109 110576254
Liver function test abnormal 134.28 41.51 49 1887 68901 110518462
Herpes zoster 119.39 41.51 51 1885 108328 110479035
Leukopenia 100.92 41.51 50 1886 148741 110438622
Arthritis 89.62 41.51 48 1888 167538 110419825
Fibromyalgia 88.73 41.51 48 1888 170861 110416502
Arteriovenous fistula occlusion 88.04 41.51 14 1922 535 110586828
Blood cholesterol increased 85.22 41.51 48 1888 184737 110402626
Blue toe syndrome 84.88 41.51 14 1922 674 110586689
Peripheral swelling 82.66 41.51 63 1873 403971 110183392
Oral pain 77.98 41.51 28 1908 37416 110549947
Therapeutic product effect incomplete 74.18 41.51 47 1889 223758 110363605
Synovitis 67.83 41.51 48 1888 274044 110313319
Tenderness 65.01 41.51 23 1913 29414 110557949
Infection 58.01 41.51 49 1887 362151 110225212
Renal pain 52.27 41.51 15 1921 9802 110577561
Joint swelling 47.69 41.51 48 1888 442797 110144566
Muscle strain 46 41.51 14 1922 11188 110576175
Anaemia 44.32 41.51 51 1885 547035 110040328
Soft tissue swelling 42.20 41.51 9 1927 1740 110585623

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G04BD02 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
FDA MoA N0000000125 Cholinergic Muscarinic Antagonists
MeSH PA D010276 Parasympatholytics
MeSH PA D064804 Urological Agents
CHEBI has role CHEBI:35846 renal agent
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:50370 parasympatholytic
CHEBI has role CHEBI:53784 antispasmodic drug
CHEBI has role CHEBI:35441 antiinfective agent
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist

Related Drugs by ATC class:

G04BD Drugs for urinary frequency and incontinence 13 drugs
darifenacinemeproniumfesoterodineimidafenacinmeladrazinemirabegronoxybutyninpropiverinesolifenacinterodilinetolterodinetrospium show all 13 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Dysuria indication 49650001
Urgent desire to urinate indication 75088002
Nocturia indication 139394000
Suprapubic pain indication 162053006
Urinary incontinence indication 165232002
Urinary Tract Irritation indication
Increased Urinary Frequency indication
Urinary tract obstruction contraindication 7163005 DOID:5200
Paralytic ileus contraindication 55525008 DOID:8442
Gastrointestinal hemorrhage contraindication 74474003
Gastrointestinal obstruction contraindication 126765001
Pyloric obstruction contraindication 244815007
Angle-closure glaucoma contraindication 392291006 DOID:13550




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.69 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phosphodiesterase 4 Enzyme INHIBITOR CHEMBL CHEMBL
Phosphodiesterase 7 Enzyme INHIBITOR CHEMBL CHEMBL
Phosphodiesterase 8 Enzyme INHIBITOR CHEMBL CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel Ki 4.70 DRUG MATRIX

External reference:

IDSource
4019756 VUID
N0000147847 NUI
D00718 KEGG_DRUG
3717-88-2 SECONDARY_CAS_RN
4018018 VANDF
4019756 VANDF
C0016225 UMLSCUI
CHEBI:5088 CHEBI
HWL PDB_CHEM_ID
CHEMBL1493 ChEMBL_ID
CHEMBL1200875 ChEMBL_ID
DB01148 DRUGBANK_ID
D005422 MESH_DESCRIPTOR_UI
3354 PUBCHEM_CID
7187 IUPHAR_LIGAND_ID
1929 INN_ID
3E74Y80MEY UNII
11048 RXNORM
4272 MMSL
4729 MMSL
47596 MMSL
d01425 MMSL
001767 NDDF
004714 NDDF
372768002 SNOMEDCT_US
53641000 SNOMEDCT_US
87090006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FLAVOXATE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0574-0115 TABLET, FILM COATED 100 mg ORAL ANDA 17 sections
FLAVOXATE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0574-0115 TABLET, FILM COATED 100 mg ORAL ANDA 17 sections
Flavoxate Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24658-720 TABLET 100 mg ORAL ANDA 17 sections
Flavoxate Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-058 TABLET 100 mg ORAL ANDA 17 sections
Flavoxate Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-6326 TABLET, FILM COATED 100 mg ORAL ANDA 19 sections
FLAVOXATE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 68151-3826 TABLET, FILM COATED 100 mg ORAL ANDA 19 sections