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dyclonine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 974 | 586-60-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
minor descriptor (66-83); on-line & Index Medicus search PROPIOPHENONES (66-83); RN given refers to parent cpd; structure
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.888 | Moderate | 0.70 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.325 | Moderate | 0.70 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 31.405 | 10^-6 cm/s | Moderate | 0.70 |
| dh-clint | Dog hepatocyte intrinsic clearance | 86.696 | uL/min/10^6 cells | Moderate | 0.70 |
| dppb | Dog plasma protein binding (% unbound) | 12.030 | % | Moderate | 0.70 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 27.410 | % | Moderate | 0.70 |
| herg | hERG pIC50 | 5.906 | pIC50 | Moderate | 0.70 |
| hh-clint | Human hepatocyte intrinsic clearance | 20.989 | uL/min/10^6 cells | Moderate | 0.70 |
| hlm-clint | Human liver microsomal intrinsic clearance | 26.303 | uL/min/mg protein | Moderate | 0.70 |
| hppb | Human plasma protein binding (% unbound) | 16.250 | % | Moderate | 0.70 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 55 | |||
| kinase-selectivity-class | GRK2,PDK4 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.110 | Moderate | 0.70 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 166.341 | Moderate | 0.70 | |
| mppb | Mouse plasma protein binding (% unbound) | 18.740 | Moderate | 0.70 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.398 | Moderate | 0.70 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 20 | % | Moderate | 0.70 |
| rh-clint | Rat hepatocyte intrinsic clearance | 272.270 | uL/min/10^6 cells | Moderate | 0.70 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 41.060 | % | Moderate | 0.70 |
| rppb | Rat plasma protein binding (% unbound) | 15.190 | % | Moderate | 0.70 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 609.537 | uM | Moderate | 0.70 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA |
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 |
|---|---|---|---|---|---|---|
| Heart rate abnormal | 165.42 | 48.49 | 34 | 1451 | 5937 | 90621025 |
| Blood magnesium decreased | 132.72 | 48.49 | 34 | 1451 | 15659 | 90611303 |
| Muscle twitching | 118.12 | 48.49 | 34 | 1451 | 24168 | 90602794 |
| Lymphadenitis | 111.26 | 48.49 | 23 | 1462 | 4114 | 90622848 |
| Clostridium difficile infection | 104.59 | 48.49 | 34 | 1451 | 36211 | 90590751 |
| Soft tissue disorder | 98.91 | 48.49 | 21 | 1464 | 4269 | 90622693 |
| Infection | 97.73 | 48.49 | 65 | 1420 | 362029 | 90264933 |
| Productive cough | 96.53 | 48.49 | 39 | 1446 | 77024 | 90549938 |
| Thrombosis | 81.26 | 48.49 | 34 | 1451 | 73217 | 90553745 |
| Pneumonia viral | 73.96 | 48.49 | 19 | 1466 | 8804 | 90618158 |
| White blood cell count decreased | 70.47 | 48.49 | 40 | 1445 | 167069 | 90459893 |
| Platelet count decreased | 66.54 | 48.49 | 36 | 1449 | 136933 | 90490029 |
| Liver function test abnormal | 64.51 | 48.49 | 26 | 1459 | 50819 | 90576143 |
| Lymphadenopathy | 60.11 | 48.49 | 24 | 1461 | 45751 | 90581211 |
| Febrile neutropenia | 56.41 | 48.49 | 34 | 1451 | 158315 | 90468647 |
| Herpes zoster | 51.91 | 48.49 | 27 | 1458 | 94617 | 90532345 |
| Soft tissue swelling | 50.99 | 48.49 | 10 | 1475 | 1368 | 90625594 |
| Leukopenia | 50.33 | 48.49 | 27 | 1458 | 100683 | 90526279 |
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 |
|---|---|---|---|---|---|---|
| Heart rate abnormal | 169.76 | 55.06 | 34 | 1283 | 7204 | 110580778 |
| Blood magnesium decreased | 135.36 | 55.06 | 34 | 1283 | 19962 | 110568020 |
| Muscle twitching | 121.76 | 55.06 | 34 | 1283 | 29901 | 110558081 |
| Lymphadenitis | 112.10 | 55.06 | 23 | 1294 | 5470 | 110582512 |
| Clostridium difficile infection | 103.15 | 55.06 | 34 | 1283 | 52095 | 110535887 |
| Productive cough | 97.15 | 55.06 | 40 | 1277 | 114265 | 110473717 |
| Infection | 87.74 | 55.06 | 54 | 1263 | 362146 | 110225836 |
| Thrombosis | 78.84 | 55.06 | 34 | 1283 | 108628 | 110479354 |
| White blood cell count decreased | 73.35 | 55.06 | 41 | 1276 | 229349 | 110358633 |
| Platelet count decreased | 62.45 | 55.06 | 37 | 1280 | 230406 | 110357576 |
| Lymphadenopathy | 59.82 | 55.06 | 24 | 1293 | 63811 | 110524171 |
| Pneumonia viral | 56.11 | 55.06 | 15 | 1302 | 11142 | 110576840 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N01BX02 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Other local anesthetics |
| ATC | R02AD04 | RESPIRATORY SYSTEM THROAT PREPARATIONS THROAT PREPARATIONS Anesthetics, local |
| 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 |
| CHEBI has role | CHEBI:48425 | topical anaesthetic |
Related Drugs by ATC class:
N01BX Other local anesthetics 3 drugs
R02AD Anesthetics, local 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Skin irritation | indication | 367466007 | |
| Local anesthesia | indication | 386761002 | |
| Itching of skin | indication | 418363000 | |
| Suppression of the Gag Reflex | indication | ||
| Prevent Minor Bacterial Skin Infection | indication | ||
| Minor Skin Wound Pain | indication | ||
| Mouth Irritation | indication | ||
| Conduction disorder of the heart | contraindication | 44808001 | |
| Bleeding hemorrhoids | contraindication | 51551000 | |
| Decreased respiratory function | contraindication | 80954004 | |
| Disorder of mucous membrane | contraindication | 95351003 | |
| Open wound | contraindication | 125643001 | |
| Seizure disorder | contraindication | 128613002 | |
| Denuded skin | contraindication | 418242004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.79 | 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 protein type 10 subunit alpha | Ion channel | BLOCKER | DRUGBANK | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 6.74 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019739 | VUID |
| N0000147831 | NUI |
| D00735 | KEGG_DRUG |
| 536-43-6 | SECONDARY_CAS_RN |
| 4018913 | VANDF |
| 4019739 | VANDF |
| C0058831 | UMLSCUI |
| CHEBI:4724 | CHEBI |
| N8R | PDB_CHEM_ID |
| CHEMBL1201217 | ChEMBL_ID |
| CHEMBL1200478 | ChEMBL_ID |
| DB00645 | DRUGBANK_ID |
| C100063 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3180 | PUBCHEM_CID |
| 7173 | IUPHAR_LIGAND_ID |
| 640 | INN_ID |
| 078A24Q30O | UNII |
| 23744 | RXNORM |
| 4647 | MMSL |
| 72161 | MMSL |
| 001336 | NDDF |
| 005055 | NDDF |
| 23564005 | SNOMEDCT_US |
| 370307004 | SNOMEDCT_US |
| 57164003 | SNOMEDCT_US |
| 078A24Q30O | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| DycloPro | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0362-3971 | SOLUTION | 5 mg | TOPICAL | ANDA | 18 sections |
| Benzethonium chloride and Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 0363-0210 | LIQUID | 0.23 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride and Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 0363-0210 | LIQUID | 0.23 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Ambix First Aid | HUMAN OTC DRUG LABEL | 2 | 10038-250 | CREAM | 0.01 g | TOPICAL | OTC monograph not final | 11 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 11822-0128 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 30142-150 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 30142-150 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 36800-382 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 36800-382 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 37808-512 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 37808-512 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 41250-132 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 41520-089 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 41520-089 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 46122-525 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 46122-525 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Premier Solutions Liquid Bandage | HUMAN OTC DRUG LABEL | 2 | 56104-246 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Premier Solutions Liquid Bandage | HUMAN OTC DRUG LABEL | 2 | 56104-246 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Liquid Bandage | HUMAN OTC DRUG LABEL | 2 | 56104-502 | LIQUID | 7.50 mg | TOPICAL | OTC Monograph Drug | 14 sections |
| Liquid Bandage | HUMAN OTC DRUG LABEL | 2 | 56104-502 | LIQUID | 7.50 mg | TOPICAL | OTC Monograph Drug | 14 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 59779-385 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 59779-385 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Skin Shield | HUMAN OTC DRUG LABEL | 2 | 63736-293 | LIQUID | 0.10 mL | TOPICAL | OTC monograph not final | 14 sections |
| Sucrets Sore Throat Wild Cherry | HUMAN OTC DRUG LABEL | 1 | 63736-560 | LOZENGE | 2 mg | ORAL | OTC Monograph Drug | 12 sections |
| Sucrets | HUMAN OTC DRUG LABEL | 3 | 63736-567 | LOZENGE | 2 mg | ORAL | OTC Monograph Drug | 13 sections |
| Sucrets CompleteVapor Cherry | HUMAN OTC DRUG LABEL | 2 | 63736-920 | LOZENGE | 3 mg | ORAL | OTC monograph not final | 14 sections |
| SUCRETS VAPOR CHERRY | HUMAN OTC DRUG LABEL | 2 | 63736-925 | LOZENGE | 3 mg | ORAL | OTC Monograph Drug | 11 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 63868-045 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 63941-546 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |
| Benzethonium chloride Plus Dyclonine hydrochloride | HUMAN OTC DRUG LABEL | 2 | 63941-546 | LIQUID | 0.75 mg | TOPICAL | OTC Monograph Drug | 15 sections |