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butacaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 3050 | 149-16-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
was MH 1965-92; BUTAPROBENZ & BUTOCAIN were see BUTACAINE 1978-92; use 4-AMINOBENZOIC ACID to search BUTACAINE 1966-92
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.120 | Moderate | 0.66 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.264 | Moderate | 0.66 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 36.141 | 10^-6 cm/s | Moderate | 0.66 |
| dh-clint | Dog hepatocyte intrinsic clearance | 243.781 | uL/min/10^6 cells | Moderate | 0.66 |
| dppb | Dog plasma protein binding (% unbound) | 25.790 | % | Moderate | 0.66 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 40.060 | % | Moderate | 0.66 |
| herg | hERG pIC50 | 6.313 | pIC50 | Moderate | 0.66 |
| hh-clint | Human hepatocyte intrinsic clearance | 89.125 | uL/min/10^6 cells | Moderate | 0.66 |
| hlm-clint | Human liver microsomal intrinsic clearance | 176.604 | uL/min/mg protein | Moderate | 0.66 |
| hppb | Human plasma protein binding (% unbound) | 28.850 | % | Moderate | 0.66 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2 | 69 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK4,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,MAP2K6,MAP3K7,MAPK12,MAPK7,MARK4,MTOR,NUAK1,PDK4,PRKCD,SIK2,SIK3,STK33,TEK,TTK,ULK1 | 24 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.902 | Moderate | 0.66 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 452.898 | Moderate | 0.66 | |
| mppb | Mouse plasma protein binding (% unbound) | 49.020 | Moderate | 0.66 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.213 | Moderate | 0.66 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 64.170 | % | Moderate | 0.66 |
| rh-clint | Rat hepatocyte intrinsic clearance | 272.898 | uL/min/10^6 cells | Moderate | 0.66 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 77.330 | % | Moderate | 0.66 |
| rppb | Rat plasma protein binding (% unbound) | 37.650 | % | Moderate | 0.66 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 578.096 | uM | Moderate | 0.66 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D000779 | Anesthetics, Local |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Urgent desire to urinate | indication | 75088002 | |
| Urge incontinence of urine | indication | 87557004 | |
| Bladder muscle dysfunction - overactive | indication | 236633002 | |
| Neurogenic bladder | indication | 398064005 | |
| Increased Urinary Frequency | indication | ||
| Sinus tachycardia | contraindication | 11092001 | |
| Severe chronic ulcerative colitis | contraindication | 14311001 | |
| Toxic megacolon | contraindication | 28536002 | DOID:1770 |
| Atony of colon | contraindication | 29479008 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Gastroesophageal reflux disease | contraindication | 235595009 | DOID:8534 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Drowsy | contraindication | 271782001 | |
| Gastric retention | contraindication | 307227006 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Disorder of coronary artery | contraindication | 414024009 | |
| Gastrointestinal hypomotility | contraindication | 421807004 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cats | Surface bacterial infections of ears | Indication |
| Cats | Surface bacterial infections of wounds | Indication |
| Cats | Surface bacterial infections of burns | Indication |
| Cats | Surface bacterial infections of cutaneous ulcers | Indication |
| Dogs | Surface bacterial infections of ears | Indication |
| Dogs | Surface bacterial infections of wounds | Indication |
| Dogs | Surface bacterial infections of burns | Indication |
| Dogs | Surface bacterial infections of cutaneous ulcers | Indication |
| Horses | Surface bacterial infections of ears | Indication |
| Horses | Surface bacterial infections of wounds | Indication |
| Horses | Surface bacterial infections of burns | Indication |
| Horses | Surface bacterial infections of cutaneous ulcers | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Nitrofurazone Anesthetic Dress. | Med-Pharmex Inc. | 2 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.16 | Basic |
| pKa2 | 2.5 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 5.57 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019434 | VUID |
| N0000147564 | NUI |
| 4019434 | VANDF |
| C0006466 | UMLSCUI |
| CHEBI:94820 | CHEBI |
| CHEMBL129529 | ChEMBL_ID |
| DB11502 | DRUGBANK_ID |
| C073325 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2480 | PUBCHEM_CID |
| 381 | INN_ID |
| Z84S23CGJJ | UNII |
| 133044 | RXNORM |
| 001373 | NDDF |
| 004575 | NDDF |
| 373532002 | SNOMEDCT_US |
| 8028001 | SNOMEDCT_US |
| 96272007 | SNOMEDCT_US |
| CHEMBL3142544 | ChEMBL_ID |
| 149-15-5 | SECONDARY_CAS_RN |
Pharmaceutical products:
None