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articaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 3070 | 23964-58-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A thiophene-containing local anesthetic pharmacologically similar to MEPIVACAINE.
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 48 | |||
| kinase-selectivity-class | AXL,BRAF,DDR1,GRK2,MAP2K6,MAPK7,STK33,TEK,TTK | 9 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
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 |
|---|---|---|---|---|---|---|
| Sinobronchitis | 107.44 | 97.03 | 14 | 542 | 468 | 110588275 |
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 | D002492 | Central Nervous System Depressants |
| MeSH PA | D018689 | Sensory System Agents |
| FDA EPC | N0000175682 | Amide Local Anesthetic |
| FDA PE | N0000175976 | Local Anesthesia |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
Related Drugs by ATC class:
N01BB Amides 10 drugs
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 8% BASE | CYKLX | THEA PHARMA | N218643 | Aug. 15, 2025 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 11096922 | March 27, 2039 | METHOD OF ANESTHETIZING AN OCULAR SURFACE VIA TOPICAL ADMINISTRATION PRIOR TO OCULAR PROCEDURES AND/OR INTRAOCULAR INJECTIONS |
| EQ 8% BASE | CYKLX | THEA PHARMA | N218643 | Aug. 15, 2025 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 11826347 | March 27, 2039 | METHOD OF ANESTHETIZING AN OCULAR SURFACE VIA TOPICAL ADMINISTRATION PRIOR TO OCULAR PROCEDURES AND/OR INTRAOCULAR INJECTIONS |
| EQ 8% BASE | CYKLX | THEA PHARMA | N218643 | Aug. 15, 2025 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 12403126 | March 27, 2039 | METHOD OF ANESTHETIZING AN OCULAR SURFACE PRIOR TO OCULAR PROCEDURES AND/OR INTRAOCULAR INJECTIONS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 8% BASE | CYKLX | THEA PHARMA | N218643 | Aug. 15, 2025 | DISCN | SOLUTION/DROPS | OPHTHALMIC | Aug. 15, 2028 | NEW PRODUCT |
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 | 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:748399 | 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 | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Septocaine and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0362-9048 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA | 29 sections |
| Septocaine and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0362-9049 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA | 29 sections |
| Articaine Hydrochloride and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0404-6620 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine Hydrochloride and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0404-6625 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43128-101 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43128-102 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine Hydrochloride and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43498-816 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine Hydrochloride and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43498-993 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 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 | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50227-1050 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-0102 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-1010 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-1040 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-4175 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-4185 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine Hydrochloride and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-6620 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine Hydrochloride and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 51004-6625 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 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 | SUBMUCOSAL | NDA authorized generic | 30 sections |
| Articadent | HUMAN PRESCRIPTION DRUG LABEL | 2 | 66312-602 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 30 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 66975-417 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| ARTICAINE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 66975-418 | INJECTION, SOLUTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine HCl and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 67239-0209 | INJECTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |
| Articaine HCl and Epinephrine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 67239-0210 | INJECTION | 40 mg | SUBMUCOSAL | NDA authorized generic | 29 sections |