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propiverine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| spasmolytics with a papaverine-like action | 2300 | 60569-19-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
anticholinergic used for overactive bladder syndrome
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 2.73 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.94 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.10 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 15.20 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 1.10 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 39 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.269 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.614 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 30.061 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 45.082 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 5.860 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.260 | % | High | 1 |
| herg | hERG pIC50 | 5.659 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 23.714 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 134.276 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 6.160 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIM2,PRKDC,SIK2,SIK3,TEK,TGFBR1 | 38 | |||
| kinase-selectivity-class | AXL,GRK2,PDK4,SIK2,SIK3,TEK | 6 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.097 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 164.816 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.570 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 12.078 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 15.370 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 205.116 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 19.560 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 7.580 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 279.898 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Craniofacial fracture | 84.05 | 44.79 | 12 | 756 | 465 | 90627214 |
| Dyslalia | 64.12 | 44.79 | 10 | 758 | 708 | 90626971 |
| Fear of falling | 57.42 | 44.79 | 9 | 759 | 658 | 90627021 |
| Fall | 49.35 | 44.79 | 37 | 731 | 481773 | 90145906 |
| Electrocardiogram ST-T segment abnormal | 45.78 | 44.79 | 7 | 761 | 434 | 90627245 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Craniofacial fracture | 72.13 | 30.03 | 12 | 1324 | 889 | 110587074 |
| Fear of falling | 51.38 | 30.03 | 9 | 1327 | 904 | 110587059 |
| Dyslalia | 47.56 | 30.03 | 9 | 1327 | 1388 | 110586575 |
| Fall | 41.08 | 30.03 | 43 | 1293 | 603439 | 109984524 |
| Immobile | 32.27 | 30.03 | 9 | 1327 | 7693 | 110580270 |
| Medication error | 31.06 | 30.03 | 18 | 1318 | 105348 | 110482615 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G04BD06 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs for urinary frequency and incontinence |
| MeSH PA | D010276 | Parasympatholytics |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D018727 | Muscarinic Antagonists |
| MeSH PA | D064804 | Urological Agents |
| CHEBI has role | CHEBI:35846 | renal agent |
Related Drugs by ATC class:
G04BD Drugs for urinary frequency and incontinence 13 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.97 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D01007 | KEGG_DRUG |
| 54556-98-8 | SECONDARY_CAS_RN |
| C0138666 | UMLSCUI |
| CHEBI:8493 | CHEBI |
| CHEMBL1078261 | ChEMBL_ID |
| DB12278 | DRUGBANK_ID |
| C015586 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4942 | PUBCHEM_CID |
| 5020 | INN_ID |
| 468GE2241L | UNII |
| 55175 | RXNORM |
| 007118 | NDDF |
| 007119 | NDDF |
| 395848002 | SNOMEDCT_US |
| 395997007 | SNOMEDCT_US |
| 421592007 | SNOMEDCT_US |
Pharmaceutical products:
None