benzocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
local anaesthetics 323 94-09-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • benzocaine
  • norcaine
  • 4-Carbethoxyaniline
  • benzocaine hydrobromide
  • benzocaine hydrochloride
  • benzocaine HCl
  • benzocaine methanesulfonate
  • ethyl aminobenzoate
  • parathesin
  • americaine
  • benzocaine formate
A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.
  • Molecular weight: 165.19
  • Formula: C9H11NO2
  • CLOGP: 1.92
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 52.32
  • ALOGS: -1.76
  • ROTB: 3

Drug dosage:

None

ADMET properties:

None

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
Methaemoglobinaemia 258.36 25.04 58 6145 1984 50596937
Irritable bowel syndrome 183.39 25.04 100 6103 51341 50547580
Helicobacter infection 140.35 25.04 83 6120 49619 50549302
Ill-defined disorder 130.55 25.04 82 6121 54572 50544349
Pericarditis 130.24 25.04 94 6109 78595 50520326
Muscle injury 118.08 25.04 67 6136 37044 50561877
Folliculitis 117.28 25.04 68 6135 39157 50559764
Blister 116.77 25.04 91 6112 85327 50513594
Contusion 108.79 25.04 98 6105 112085 50486836
Duodenal ulcer perforation 95.44 25.04 63 6140 45548 50553373
Arthropathy 89.11 25.04 103 6100 157803 50441118
Discomfort 84.60 25.04 84 6119 108296 50490625
Impaired healing 83.90 25.04 69 6134 69717 50529204
Hepatic enzyme increased 73.11 25.04 87 6116 137293 50461628
Completed suicide 70.96 25.04 84 6119 131805 50467116
Drug abuse 69.47 25.04 58 6145 59788 50539133
Stomatitis 69 25.04 73 6130 101271 50497650
Anti-cyclic citrullinated peptide antibody positive 67.01 25.04 61 6142 70526 50528395
Sleep disorder due to general medical condition, insomnia type 64.69 25.04 43 6160 31404 50567517
Lower respiratory tract infection 63.78 25.04 68 6135 95133 50503788
Gastrointestinal disorder 62.45 25.04 67 6136 94389 50504532
Hypersensitivity 61.44 25.04 101 6102 215060 50383861
Synovitis 55.51 25.04 72 6131 123793 50475128
Rheumatoid factor positive 53.09 25.04 46 6157 49813 50549108
Systemic lupus erythematosus 52.79 25.04 75 6128 140547 50458374
Hand deformity 49.24 25.04 61 6142 100138 50498783
Toxicity to various agents 46.73 25.04 89 6114 212410 50386511
Swelling 45.23 25.04 85 6118 200787 50398134
Glossodynia 43.88 25.04 62 6141 115507 50483414
Pemphigus 42.02 25.04 62 6141 120104 50478817
Confusional state 41.01 25.04 78 6125 185850 50413071
Wound 40.52 25.04 57 6146 105737 50493184
Infection 39.93 25.04 74 6129 172880 50426041
Respiratory arrest 38.82 25.04 31 6172 29978 50568943
Abdominal discomfort 37.97 25.04 86 6117 231555 50367366
Alopecia 35.82 25.04 87 6116 244960 50353961
Pruritus 35.57 25.04 95 6108 283473 50315448
Nasopharyngitis 33.13 25.04 73 6130 192854 50406067
Cyanosis 29.38 25.04 20 6183 15164 50583757
Nausea 28.33 25.04 27 6176 705371 49893550
Infusion related reaction 26.69 25.04 62 6141 169495 50429426

FDA Adverse Event Reporting System (Male)

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
Drug abuse 273.11 21.94 136 2548 79747 29492096
Methaemoglobinaemia 175.07 21.94 42 2642 2629 29569214
Intentional product misuse 151.16 21.94 70 2614 34591 29537252
Toxicity to various agents 125.15 21.94 112 2572 173549 29398294
Serotonin syndrome 84.46 21.94 38 2646 17474 29554369
Completed suicide 82.66 21.94 67 2617 90179 29481664
Respiratory arrest 67.65 21.94 37 2647 25796 29546047
Hangover 42.14 21.94 11 2673 966 29570877
Intentional overdose 35.97 21.94 29 2655 38499 29533344
Mydriasis 35.12 21.94 15 2669 6070 29565773
Cardiac arrest 31.88 21.94 39 2645 85552 29486291
Cardio-respiratory arrest 31.02 21.94 30 2654 50571 29521272
Overdose 25.95 21.94 34 2650 79785 29492058
Paranoia 22.69 21.94 13 2671 9864 29561979
Rebound effect 22.36 21.94 8 2676 2023 29569820

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
Methaemoglobinaemia 400.94 21.18 93 6797 4255 64487587
Drug abuse 333.21 21.18 195 6695 132179 64359663
Toxicity to various agents 157.05 21.18 193 6697 363320 64128522
Intentional product misuse 144.18 21.18 92 6798 72203 64419639
Completed suicide 142.84 21.18 146 6744 224268 64267574
Irritable bowel syndrome 112.30 21.18 62 6828 37307 64454535
Respiratory arrest 107.00 21.18 68 6822 52917 64438925
Helicobacter infection 84.38 21.18 52 6838 38310 64453532
Pericarditis 80.83 21.18 61 6829 62455 64429387
Systemic lupus erythematosus 69.23 21.18 61 6829 77551 64414291
Sleep disorder due to general medical condition, insomnia type 69.19 21.18 40 6850 26230 64465612
Stomatitis 63.57 21.18 68 6822 109537 64382305
Arthropathy 61.43 21.18 70 6820 120897 64370945
Contusion 59.65 21.18 67 6823 113898 64377944
Ill-defined disorder 59.18 21.18 44 6846 44008 64447834
Discomfort 57.47 21.18 56 6834 80822 64411020
Blister 57.41 21.18 56 6834 80911 64410931
Synovitis 56.61 21.18 61 6829 99029 64392813
Serotonin syndrome 52.23 21.18 39 6851 39243 64452599
Cardiac arrest 50.95 21.18 72 6818 153992 64337850
Cyanosis 46.09 21.18 29 6861 22126 64469716
Cardio-respiratory arrest 45.02 21.18 54 6836 98339 64393503
Rheumatoid factor positive 44.92 21.18 34 6856 34904 64456938
Muscle injury 43.77 21.18 30 6860 26407 64465435
Folliculitis 42.54 21.18 31 6859 30046 64461796
Swelling 41.73 21.18 67 6823 160151 64331691
Intentional overdose 40.55 21.18 49 6841 89895 64401947
Sleep disorder 39.90 21.18 40 6850 59669 64432173
Duodenal ulcer perforation 38.66 21.18 31 6859 34594 64457248
Wound 38.35 21.18 44 6846 76433 64415409
Sudden infant death syndrome 34.66 21.18 7 6883 164 64491678
Hepatic enzyme increased 33.36 21.18 54 6836 129889 64361953
Hangover 33.13 21.18 11 6879 1890 64489952
Hypersensitivity 31.92 21.18 67 6823 196385 64295457
Overdose 28.97 21.18 57 6833 159509 64332333
Medication error 27.18 21.18 30 6860 49936 64441906
Impaired healing 25.71 21.18 32 6858 60441 64431401
Anti-cyclic citrullinated peptide antibody positive 25.65 21.18 29 6861 49533 64442309
Injection site ulcer 25.19 21.18 7 6883 660 64491182
Mydriasis 24.45 21.18 17 6873 15295 64476547
Alopecia 24.03 21.18 54 6836 165636 64326206
Abdominal discomfort 23.79 21.18 57 6833 182265 64309577
Glossodynia 22.48 21.18 31 6859 64665 64427177
Pemphigus 22.48 21.18 30 6860 60671 64431171
Accidental overdose 21.53 21.18 22 6868 33535 64458307

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C05AD03 CARDIOVASCULAR SYSTEM
VASOPROTECTIVES
AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
Local anesthetics
ATC D04AB04 DERMATOLOGICALS
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Anesthetics for topical use
ATC N01BA05 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Esters of aminobenzoic acid
ATC R02AD01 RESPIRATORY SYSTEM
THROAT PREPARATIONS
THROAT PREPARATIONS
Anesthetics, local
FDA CS M0000728 Allergens
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
FDA PE N0000175629 Increased Histamine Release
FDA PE N0000184306 Cell-mediated Immunity
FDA EPC N0000185508 Standardized Chemical Allergen
CHEBI has role CHEBI:48425 topical anesthetic
CHEBI has role CHEBI:50904 alergeno
CHEBI has role CHEBI:59683 antipruritic drugs
CHEBI has role CHEBI:139492 sensitizers

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Tinea pedis indication 6020002 DOID:12403
Cough indication 49727002
Tinea corporis indication 84849002
Sore throat symptom indication 267102003
Skin irritation indication 367466007
Local anesthesia indication 386761002
Itching of skin indication 418363000
Suppression of the Gag Reflex indication
Tinea Infections indication
Minor Skin Wound Pain indication
Mouth Irritation indication
Prevent Minor Bacterial Skin Infection indication
Hypocalcemia off-label use 5291005
Otalgia off-label use 16001004
Impacted cerumen off-label use 18070006
Osteoporosis off-label use 64859006 DOID:11476
Postmenopausal osteoporosis off-label use 102447009
Indigestion off-label use 162031009
Renal Osteodystrophy with Hyperphosphatemia off-label use
Gastritis contraindication 4556007 DOID:4029
Suicidal thoughts contraindication 6471006
Alcoholism contraindication 7200002
Hyperammonemia contraindication 9360008
Infectious gastroenteritis contraindication 12463005
Hepatic encephalopathy contraindication 13920009 DOID:13413
Constipation contraindication 14760008 DOID:2089
Hypocupremia contraindication 19577007
Herpes zoster auricularis contraindication 21954000 DOID:9210
Sarcoidosis contraindication 31541009 DOID:11335
Dehydration contraindication 34095006
Depressive disorder contraindication 35489007
Methemoglobinemia contraindication 38959009 DOID:10783
Gastrointestinal ulcer contraindication 40845000
Body fluid retention contraindication 43498006
Conduction disorder of the heart contraindication 44808001
Encephalitis contraindication 45170000 DOID:9588
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Bleeding hemorrhoids contraindication 51551000
Vitamin K deficiency contraindication 52675005 DOID:11249
Nasal polyp contraindication 52756005
Hepatic failure contraindication 59927004
Perforation of tympanic membrane contraindication 60442001
Diarrhea contraindication 62315008
Blood coagulation disorder contraindication 64779008 DOID:1247
Poisoning by phenobarbital contraindication 64921004
Substance abuse contraindication 66214007
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Incontinence of feces contraindication 72042002
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Sleep apnea contraindication 73430006 DOID:0050847
Factor II deficiency contraindication 73975000
Appendicitis contraindication 74400008 DOID:8337
Gastrointestinal hemorrhage contraindication 74474003
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Decreased respiratory function contraindication 80954004
Herpes simplex contraindication 88594005 DOID:8566
Kidney disease contraindication 90708001 DOID:557
Thyrotoxicosis contraindication 90739004 DOID:7997
Hemophilia contraindication 90935002
Diaper rash contraindication 91487003
Disorder of skin contraindication 95320005 DOID:37
Disorder of mucous membrane contraindication 95351003
Kidney stone contraindication 95570007
Anemia due to enzyme deficiency contraindication 111577008
Deficiency of glucose-6-phosphate dehydrogenase contraindication 124134002 DOID:2862
Deficiency of cytochrome-b>5< reductase contraindication 124184009
Open wound contraindication 125643001
Gastrointestinal obstruction contraindication 126765001
Seizure disorder contraindication 128613002
Tuberculosis of ear contraindication 186269001
Osteolysis contraindication 203522001
Gastroesophageal reflux disease contraindication 235595009 DOID:8534
Disease of liver contraindication 235856003 DOID:409
Disorder of electrolytes contraindication 237840007
Dyspnea contraindication 267036007
Anemia contraindication 271737000 DOID:2355
Eruption of skin contraindication 271807003 DOID:0050486
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Viral ear infection contraindication 312137007
Fungal ear infection contraindication 312148000
Infective otitis media contraindication 312218008
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Denuded skin contraindication 418242004
Porphyria contraindication 418470004
Fever greater than 100.4 Fahrenheit contraindication 426000000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.5 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 1 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 2 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 3 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 4 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 8 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 9 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 11 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 7 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER ED50 3.50 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
4018117 VUID
N0000146455 NUI
D00552 KEGG_DRUG
1049105 RXNORM
C0005059 UMLSCUI
CHEBI:116735 CHEBI
CHEMBL278172 ChEMBL_ID
DB01086 DRUGBANK_ID
D001566 MESH_DESCRIPTOR_UI
2337 PUBCHEM_CID
3953 INN_ID
23239-88-5 SECONDARY_CAS_RN
U3RSY48JW5 UNII
199 MMSL
359 MMSL
4256 MMSL
001366 NDDF
4018117 VANDF
387357002 SNOMEDCT_US
65020006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
good sense vagicaineanti itch HUMAN OTC DRUG LABEL 2 0113-0142 CREAM 20 g TOPICAL OTC monograph not final 13 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0220 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Gel HUMAN OTC DRUG LABEL 1 0283-0293 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Gel HUMAN OTC DRUG LABEL 1 0283-0293 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Gel HUMAN OTC DRUG LABEL 1 0283-0293 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0520 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Liquid HUMAN OTC DRUG LABEL 1 0283-0569 LIQUID 200 mg DENTAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0610 SPRAY 200 mg DENTAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0679 SPRAY 200 mg ORAL OTC monograph not final 11 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0871 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0871 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0871 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Gel HUMAN OTC DRUG LABEL 1 0283-0886 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Gel HUMAN OTC DRUG LABEL 1 0283-0886 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0914 SPRAY 200 mg ORAL OTC monograph not final 11 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0920 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0998 GEL 200 mg DENTAL OTC monograph not final 13 sections
HurriCaineTopical Anesthetic HUMAN OTC DRUG LABEL 1 0283-0998 GEL 200 mg DENTAL OTC monograph not final 13 sections
HurriCaineTopical Anesthetic HUMAN OTC DRUG LABEL 1 0283-1016 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic HUMAN OTC DRUG LABEL 1 0283-1016 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Liquid HUMAN OTC DRUG LABEL 1 0283-1116 LIQUID 200 mg DENTAL OTC monograph not final 12 sections
HurriCaine Topical Anesthetic HUMAN OTC DRUG LABEL 1 0283-1820 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaineTopical Anesthetic Liquid HUMAN OTC DRUG LABEL 1 0283-1886 LIQUID 200 mg DENTAL OTC monograph not final 12 sections
4x Medicated Toothache and Gum Cream HUMAN OTC DRUG LABEL 4 0363-0607 CREAM 20 g ORAL OTC monograph not final 9 sections
Anti-Itch Regular Strength HUMAN OTC DRUG LABEL 2 0363-0621 CREAM 5 g TOPICAL OTC monograph final 11 sections
Well at Walgreens Anti-Itch Maximum Strength HUMAN OTC DRUG LABEL 2 0363-0674 CREAM 20 g TOPICAL OTC monograph final 11 sections
Cherry Sore Throat Lozenge HUMAN OTC DRUG LABEL 2 0363-1079 LOZENGE 15 mg ORAL OTC monograph not final 14 sections
Mixed Berry Sore Throat and Cough Lozenge HUMAN OTC DRUG LABEL 2 0363-1080 LOZENGE 7.50 mg ORAL OTC monograph not final 15 sections
Walgreens Mixed Berry Benz-Dex Lozenges HUMAN OTC DRUG LABEL 2 0363-1113 LOZENGE 7.50 mg ORAL OTC monograph not final 15 sections
3x Medicated Mouth Sore Gel HUMAN OTC DRUG LABEL 3 0363-1605 GEL 20 g ORAL OTC monograph not final 7 sections