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

Stem definition	Drug id	CAS RN
local anaesthetics	3070	23964-58-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: articaine carticaine articaine hydrochloride articaine HCl	A thiophene-containing local anesthetic pharmacologically similar to MEPIVACAINE. Molecular weight: 284.37 Formula: C13H20N2O3S CLOGP: 1.98 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 67.43 ALOGS: -4 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

articaine
carticaine
articaine hydrochloride
articaine HCl

A thiophene-containing local anesthetic pharmacologically similar to MEPIVACAINE.

Molecular weight: 284.37
Formula: C13H20N2O3S
CLOGP: 1.98
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 67.43
ALOGS: -4
ROTB: 7

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	7.70 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	126.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.46 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.98 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
April 3, 2000	FDA

FDA Adverse Event Reporting System (Female)

None

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
Electrocardiogram ST segment elevation	79.29	75.07	14	163	8383	79735828

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N01BB08	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides
ATC	N01BB58	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides
FDA CS	M0000897	Amides
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 EPC	N0000175682	Amide Local Anesthetic
FDA PE	N0000175976	Local Anesthesia

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

Disease	Relation	SNOMED_ID	DOID
Local anesthesia, by infiltration	indication	44596000
Administration of Local Anesthetic Nerve Block	indication
Sinus tachycardia	contraindication	11092001
Myocardial infarction	contraindication	22298006	DOID:5844
Parkinsonism	contraindication	32798002
Hyperthyroidism	contraindication	34486009	DOID:7998
Hypertensive disorder	contraindication	38341003	DOID:10763
Conduction disorder of the heart	contraindication	44808001
Disorder of cardiovascular system	contraindication	49601007	DOID:1287
Cerebral arteriosclerosis	contraindication	65312002
Diabetes mellitus	contraindication	73211009	DOID:9351
Cardiogenic shock	contraindication	89138009
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Bleeding	contraindication	131148009
Angina pectoris	contraindication	194828000
Primary dilated cardiomyopathy	contraindication	195021004
Disease of liver	contraindication	235856003	DOID:409
Deficiency of cholinesterase	contraindication	360607009
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Disorder of coronary artery	contraindication	414024009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.35	acidic
pKa2	7.9	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 alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN	BLOCKER	IC50	4.29		CHEMBL	CHEMBL

External reference:

ID	Source
4021368	VUID
N0000148787	NUI
D02991	KEGG_DRUG
23964-57-0	SECONDARY_CAS_RN
4021368	VANDF
C1608295	UMLSCUI
CHEBI:91834	CHEBI
CHEMBL1093	ChEMBL_ID
CHEMBL1200819	ChEMBL_ID
DB09009	DRUGBANK_ID
3193	INN_ID
D3SQ406G9X	UNII
32170	PUBCHEM_CID
2117	RXNORM
14782	MMSL
d04536	MMSL
003780	NDDF
003799	NDDF
005096	NDDF
410851000	SNOMEDCT_US
703107005	SNOMEDCT_US
D002355	MESH_DESCRIPTOR_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zorcaine	HUMAN PRESCRIPTION DRUG LABEL	2	0362-0830	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Zorcaine	HUMAN PRESCRIPTION DRUG LABEL	2	0362-0830	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Septocaine and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	0362-9048	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Septocaine and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	0362-9049	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Articaine Hydrochloride and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	0404-6620	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Articaine Hydrochloride and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	0404-6620	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Articaine Hydrochloride and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	0404-6625	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Articaine Hydrochloride and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	0404-6625	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Zorcaine	HUMAN PRESCRIPTION DRUG LABEL	2	31382-830	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	28 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	43128-101	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	43128-101	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	43128-102	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	43128-102	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Orabloc	HUMAN PRESCRIPTION DRUG LABEL	2	45146-110	INJECTION	40 mg	SUBMUCOSAL	NDA	29 sections
Orabloc	HUMAN PRESCRIPTION DRUG LABEL	2	45146-120	INJECTION	40 mg	SUBMUCOSAL	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	50227-1040	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	50227-1040	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	50227-1050	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	50227-1050	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Ultacan Forte	HUMAN PRESCRIPTION DRUG LABEL	2	52120-100	INJECTION, SOLUTION	40 mg	SUBMUCOSAL	ANDA	26 sections
Ultacan	HUMAN PRESCRIPTION DRUG LABEL	2	52120-200	INJECTION, SOLUTION	40 mg	SUBMUCOSAL	ANDA	26 sections
Articadent	HUMAN PRESCRIPTION DRUG LABEL	2	66312-601	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	30 sections
Articadent	HUMAN PRESCRIPTION DRUG LABEL	2	66312-601	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	30 sections
Articadent	HUMAN PRESCRIPTION DRUG LABEL	2	66312-602	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	30 sections
Articadent	HUMAN PRESCRIPTION DRUG LABEL	2	66312-602	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	30 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	66975-417	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	66975-417	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	66975-418	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
ARTICAINE	HUMAN PRESCRIPTION DRUG LABEL	2	66975-418	INJECTION, SOLUTION	40 mg	SUBCUTANEOUS	NDA	29 sections
Articaine HCl and Epinephrine	HUMAN PRESCRIPTION DRUG LABEL	2	67239-0209	INJECTION	40 mg	SUBMUCOSAL	NDA	29 sections