benzocaine indications/contra

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

Approvals:

DateAgencyCompanyOrphan
None FDA

FDA Adverse Event Reporting System

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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 509.47 42.72 70 711 472 3384606
Drug abuse 429.64 42.72 103 678 18227 3366851
Intentional product misuse 352.18 42.72 82 699 12619 3372459
Completed suicide 301.69 42.72 87 694 31027 3354051
Toxicity to various agents 282.70 42.72 91 690 46963 3338115
Cardio-respiratory arrest 161.15 42.72 46 735 15394 3369684
Respiratory arrest 123.50 42.72 35 746 11333 3373745
Cardiac arrest 108.22 42.72 39 742 27280 3357798
Serotonin syndrome 108.00 42.72 27 754 5396 3379682
Overdose 107.10 42.72 41 740 33937 3351141
Cyanosis 100.14 42.72 25 756 4961 3380117
Intentional overdose 80.45 42.72 27 754 15198 3369880
Accidental overdose 55.53 42.72 17 764 7101 3377977
Oxygen saturation decreased 53.64 42.72 18 763 10073 3375005
Sudden infant death syndrome 48.33 42.72 8 773 197 3384881
Death 43.26 42.72 38 743 152286 3232792
Drug hypersensitivity 43.02 42.72 22 759 35658 3349420

Pharmacologic Action:

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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
CHEBI has role CHEBI:59683 antipruritic drug
CHEBI has role CHEBI:48425 topical anaesthetic
FDA EPC N0000185508 Standardized Chemical Allergen
FDA PE N0000175629 Increased Histamine Release
FDA PE N0000184306 Cell-mediated Immunity
FDA Chemical/Ingredient N0000171131 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

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Tinea pedis indication 6020002 DOID:12403
Cough indication 49727002
Tinea corporis indication 84849002 DOID:12179
Sore throat symptom indication 267102003
Skin irritation indication 367466007
Local anesthesia indication 386761002
Itching of skin indication 418363000
Minor Skin Wound Pain indication
Mouth Irritation indication
Tinea Infections indication
Suppression of the Gag Reflex indication
Prevent Minor Bacterial Skin Infection indication
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:13404
Dehydration contraindication 34095006
Depressive disorder contraindication 35489007 DOID:2848
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:0050848
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:2527
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 DOID:1826
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 DOID:13268
Fever greater than 100.4 Fahrenheit contraindication 426000000
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 DOID:2321
Renal Osteodystrophy with Hyperphosphatemia off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER ED50 3.49 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
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 7 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 10 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 11 subunit alpha Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

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IDSource
CHEBI:116735 CHEBI
4018117 VUID
N0000146455 NUI
C0005059 UMLSCUI
D00552 KEGG_DRUG
CHEMBL278172 ChEMBL_ID
DB01086 DRUGBANK_ID
d03987 MMSL
4018117 VANDF
N0000005906 NDFRT
N0000146455 NDFRT
001366 NDDF
199 MMSL
1399 RXNORM
387357002 SNOMEDCT_US
65020006 SNOMEDCT_US
4256 MMSL
OG625Z9LEO UNII
23239-88-5 SECONDARY_CAS_RN
3953 INN_ID
D001566 MESH_DESCRIPTOR_UI
2337 PUBCHEM_CID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Major Oral Pain Relief HUMAN OTC DRUG LABEL 1 00904-5899 LIQUID 200 mg ORAL OTC monograph final 10 sections
Colgate HUMAN OTC DRUG LABEL 1 0126-0065 PASTE, DENTIFRICE 200 mg TOPICAL OTC monograph not final 10 sections
Orabase Benzocaine HUMAN OTC DRUG LABEL 1 0126-0082 PASTE, DENTIFRICE 19.80 mg DENTAL UNAPPROVED DRUG OTHER 10 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0293 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine 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 183 mg DENTAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0679 SPRAY 200 mg ORAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0871 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0886 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0914 SPRAY 200 mg ORAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-0998 GEL 200 mg DENTAL OTC monograph not final 13 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-1016 GEL 200 mg ORAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-1116 LIQUID 200 mg DENTAL OTC monograph not final 12 sections
HurriCaine HUMAN OTC DRUG LABEL 1 0283-1886 LIQUID 200 mg DENTAL OTC monograph not final 12 sections
Projel-20 HUMAN OTC DRUG LABEL 1 0362-0122 GEL 20 1 TOPICAL OTC monograph final 8 sections
Projel-20 HUMAN OTC DRUG LABEL 1 0362-0123 GEL 20 g TOPICAL OTC monograph final 8 sections
Projel-20 HUMAN OTC DRUG LABEL 1 0362-0124 GEL 20 g TOPICAL OTC monograph final 8 sections
Projel-20 HUMAN OTC DRUG LABEL 1 0362-0125 GEL 20 g TOPICAL OTC monograph final 8 sections
Anti Itch HUMAN OTC DRUG LABEL 2 0363-0673 CREAM 5 g TOPICAL OTC monograph not final 9 sections
Well at Walgreens Anti-Itch HUMAN OTC DRUG LABEL 2 0363-0674 CREAM 20 g TOPICAL OTC monograph final 8 sections
Walgreens HUMAN OTC DRUG LABEL 1 0363-0835 PASTE, DENTIFRICE 20 g TOPICAL OTC monograph final 8 sections
Severe Oral Pain Reliever HUMAN OTC DRUG LABEL 1 0363-0838 LIQUID 20 g ORAL OTC monograph final 7 sections
Cherry Sore Throat Lozenge HUMAN OTC DRUG LABEL 2 0363-1079 LOZENGE 15 mg ORAL OTC monograph not final 12 sections
Mixed Berry Sore Throat and Cough Lozenge HUMAN OTC DRUG LABEL 2 0363-1080 LOZENGE 7.50 mg ORAL OTC monograph not final 14 sections
Honey Lemon Throat Drops HUMAN OTC DRUG LABEL 2 0363-1088 LOZENGE 15 mg ORAL OTC monograph not final 12 sections
Bite and Sting Relief HUMAN OTC DRUG LABEL 1 0363-3190 SPRAY 5 g TOPICAL OTC monograph not final 9 sections
Walgreens Cold Sore Treatment HUMAN OTC DRUG LABEL 1 0363-3191 OINTMENT 5 mg TOPICAL OTC monograph not final 8 sections
Walgreens HUMAN OTC DRUG LABEL 1 0363-5335 LIQUID 20 g ORAL OTC monograph final 8 sections
Walgreens HUMAN OTC DRUG LABEL 1 0363-5336 PASTE, DENTIFRICE 20 g TOPICAL OTC monograph final 8 sections
Walgreens HUMAN OTC DRUG LABEL 1 0363-5337 PASTE, DENTIFRICE 20 g TOPICAL OTC monograph final 8 sections