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

Stem definition	Drug id	CAS RN
local anaesthetics	323	94-09-7

Description:

Molecule	Description
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

Molecule

Description

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:

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
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 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
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 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
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:

Source	Code	Description
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 | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	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])	Bioact source	MoA source
Sodium channel protein type 1 subunit alpha	Ion channel	P35498	SCN1A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 2 subunit alpha	Ion channel	Q99250	SCN2A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 3 subunit alpha	Ion channel	Q9NY46	SCN3A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 4 subunit alpha	Ion channel	P35499	SCN4A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 8 subunit alpha	Ion channel	Q9UQD0	SCN8A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 9 subunit alpha	Ion channel	Q15858	SCN9A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 11 subunit alpha	Ion channel	Q9UI33	SCNBA_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 10 subunit alpha	Ion channel	Q9Y5Y9	SCNAA_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 7 subunit alpha	Ion channel	Q01118	SCN7A_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	ED50	3.50	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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