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

Stem definitionDrug idCAS RN
local anaesthetics 974 586-60-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dyclonine
  • dyclonine hydrochloride
  • dyclocaine
  • dyclonin
  • dyclonine HCl
minor descriptor (66-83); on-line & Index Medicus search PROPIOPHENONES (66-83); RN given refers to parent cpd; structure
  • Molecular weight: 289.42
  • Formula: C18H27NO2
  • CLOGP: 4.83
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 29.54
  • ALOGS: -3.80
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
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:

DateAgencyCompanyOrphan
None 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
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 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
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:

SourceCodeDescription
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
capsaicinethyl chloridephenol
R02AD Anesthetics, local 4 drugs
ambroxolbenzocainecocainelidocaine

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 8.79 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
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER DRUGBANK CHEMBL
Acetylcholinesterase Enzyme IC50 6.74 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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