tetracaine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
local anaesthetics 2610 94-24-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tetracaine monohydrochloride
  • pontocaine
  • tetracaine
  • amethocaine
  • laudocaine
  • tetracaine hydrochloride
  • tetracaine HCl
Local ester anesthetic that blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.
  • Molecular weight: 264.37
  • Formula: C15H24N2O2
  • CLOGP: 3.83
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 41.57
  • ALOGS: -2.68
  • ROTB: 9

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 23, 2005 FDA GALEN SPECIALTY

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
Toxic anterior segment syndrome 70.41 38.86 14 731 2123 46683194
Endophthalmitis 70.08 38.86 15 730 3263 46682054
Visual acuity reduced 45.55 38.86 16 729 22097 46663220

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
Toxic anterior segment syndrome 97.32 46.82 17 394 1504 29950563
Corneal epithelium defect 59.32 46.82 9 402 326 29951741
Endophthalmitis 49.03 46.82 11 400 3469 29948598

Pharmacologic Action:

SourceCodeDescription
ATC C05AD02 CARDIOVASCULAR SYSTEM
VASOPROTECTIVES
AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
Local anesthetics
ATC D04AB06 DERMATOLOGICALS
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Anesthetics for topical use
ATC N01BA03 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Esters of aminobenzoic acid
ATC S01HA03 SENSORY ORGANS
OPHTHALMOLOGICALS
LOCAL ANESTHETICS
Local anesthetics
ATC N01BA53 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Esters of aminobenzoic acid
FDA CS M0007766 Esters
FDA EPC N0000175683 Ester Local Anesthetic
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
CHEBI has role CHEBI:36333 local anesthetics
FDA PE N0000175976 Local Anesthesia

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Local anesthetic intrathecal block indication 231249005
Skin irritation indication 367466007
Local anesthesia indication 386761002
Itching of skin indication 418363000
Minor Skin Wound Pain indication
Local Anesthesia for Ophthalmologic Procedure indication
Administration of Corneal Anesthesia indication
Hyperthyroidism contraindication 34486009 DOID:7998
Conduction disorder of the heart contraindication 44808001
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Heart disease contraindication 56265001 DOID:114
Decreased respiratory function contraindication 80954004
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Magnetic resonance imaging contraindication 113091000
Open wound contraindication 125643001
Eye infection contraindication 128351009
Uveitis contraindication 128473001 DOID:13141
Seizure disorder contraindication 128613002
Disease of liver contraindication 235856003 DOID:409
Deficiency of cholinesterase contraindication 360607009
Denuded skin contraindication 418242004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.51 Basic
pKa2 2.67 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 9 subunit alpha Ion channel BLOCKER Ki 6.30 CHEMBL CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel BLOCKER IC50 5.47 CHEMBL CHEMBL
Sodium channel protein type 2 subunit alpha Ion channel BLOCKER IC50 5.96 CHEMBL CHEMBL
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER IC50 6.28 CHEMBL CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.15 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.01 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 5.77 DRUG MATRIX
Amine oxidase [flavin-containing] A Enzyme IC50 6.50 DRUG MATRIX
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.22 CHEMBL
cGMP-gated cation channel alpha-1 Ion channel Kd 5.17 CHEMBL

External reference:

IDSource
4019456 VUID
N0000147578 NUI
D00551 KEGG_DRUG
136-47-0 SECONDARY_CAS_RN
4018254 VANDF
4019456 VANDF
C0039629 UMLSCUI
CHEBI:9468 CHEBI
TE4 PDB_CHEM_ID
CHEMBL698 ChEMBL_ID
DB09085 DRUGBANK_ID
CHEMBL1255654 ChEMBL_ID
5411 PUBCHEM_CID
D013748 MESH_DESCRIPTOR_UI
431 INN_ID
0619F35CGV UNII
10391 RXNORM
177214 MMSL
5559 MMSL
5560 MMSL
59765 MMSL
5987 MMSL
80869 MMSL
d01217 MMSL
001361 NDDF
001362 NDDF
387309008 SNOMEDCT_US
51844001 SNOMEDCT_US
55556000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tetracaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0065-0741 SOLUTION 5 mg OPHTHALMIC NDA 23 sections
Tetracaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0187-0920 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 24 sections
Cetacaine Anesthetic HUMAN PRESCRIPTION DRUG LABEL 3 10223-0201 AEROSOL, SPRAY 0.00 g TOPICAL UNULLPPROVED DRUG OTHER 12 sections
Cetacaine Anesthetic HUMAN PRESCRIPTION DRUG LABEL 3 10223-0202 SOLUTION 0.00 g TOPICAL UNULLPPROVED DRUG OTHER 12 sections
Cetacaine Topical Anesthetic HUMAN PRESCRIPTION DRUG LABEL 3 10223-0217 GEL 0.00 g TOPICAL UNULLPPROVED DRUG OTHER 11 sections
Cetacaine Topical Anesthetic HUMAN PRESCRIPTION DRUG LABEL 3 10223-0221 GEL 0.00 g TOPICAL UNULLPPROVED DRUG OTHER 11 sections
Synera HUMAN PRESCRIPTION DRUG LABEL 2 10885-002 PATCH 70 mg CUTANEOUS NDA 26 sections
Tetracaine HUMAN PRESCRIPTION DRUG LABEL 1 17478-045 INJECTION 10 mg SUBARACHNOID unapproved drug other 19 sections
Burn Cream HUMAN OTC DRUG LABEL 1 37945-212 CREAM 10 mg TOPICAL OTC monograph not final 11 sections
Tetracaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42702-170 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 24 sections
Cutiecaine HUMAN OTC DRUG LABEL 2 50876-182 CREAM 20 mg TOPICAL OTC monograph not final 10 sections
PLIAGLIS HUMAN PRESCRIPTION DRUG LABEL 2 51672-5305 CREAM 70 mg TOPICAL NDA 28 sections
Tetracaine HCL HUMAN PRESCRIPTION DRUG LABEL 1 54288-127 INJECTION 10 mg SUBARACHNOID unapproved drug other 11 sections
NeuroMed Topical AnalgesicLA HUMAN OTC DRUG LABEL 1 54723-310 CREAM 20 mg TOPICAL OTC monograph not final 12 sections
Eclipse Topical AnalgesicLL HUMAN OTC DRUG LABEL 1 54723-669 CREAM 20 mg TOPICAL OTC monograph not final 11 sections
Eclipse Topical AnalgesicLL HUMAN OTC DRUG LABEL 1 54723-669 CREAM 20 mg TOPICAL OTC monograph not final 11 sections
Eclipse Topical AnalgesicLL HUMAN OTC DRUG LABEL 1 54723-669 CREAM 20 mg TOPICAL OTC monograph not final 11 sections
Comfortox Tetracaine HUMAN OTC DRUG LABEL 1 54723-997 CREAM 20 mg TOPICAL OTC monograph not final 11 sections
ONE TOUCH ADVANCED TOPICAL ANESTHETIC GELCOOL MINT HUMAN PRESCRIPTION DRUG LABEL 3 62565-901 GEL 4 mg TOPICAL unapproved drug other 11 sections
ONE TOUCH ADVANCED TOPICAL ANESTHETICSTRAWBERRY ICE HUMAN PRESCRIPTION DRUG LABEL 3 62565-902 GEL 4 mg TOPICAL unapproved drug other 11 sections
ONE TOUCH ADVANCED TOPICAL ANESTHETICBUBBLE GUM HUMAN PRESCRIPTION DRUG LABEL 3 62565-903 GEL 4 mg TOPICAL unapproved drug other 11 sections
ONE TOUCH ADVANCED TOPICAL ANESTHETICCHERRY HUMAN PRESCRIPTION DRUG LABEL 3 62565-904 GEL 4 mg TOPICAL unapproved drug other 11 sections
Denti-Care Denti-FreezeTopical Anesthetic Bubblegum HUMAN PRESCRIPTION DRUG LABEL 2 64778-0393 GEL 0.02 g DENTAL unapproved drug other 7 sections
Denti-Care Denti-FreezeTopical Anesthetic Cherry HUMAN PRESCRIPTION DRUG LABEL 2 64778-0394 GEL 0.02 g DENTAL unapproved drug other 7 sections
Denti-Care Denti-FreezeTopical Anesthetic Mint HUMAN PRESCRIPTION DRUG LABEL 2 64778-0396 GEL 0.02 g DENTAL unapproved drug other 7 sections
Denti-Care Denti-FreezeTopical Anesthetic Raspberry HUMAN PRESCRIPTION DRUG LABEL 2 64778-0398 GEL 0.02 g DENTAL unapproved drug other 7 sections
Denti-Care Denti-FreezeTopical Anesthetic Strawberry HUMAN PRESCRIPTION DRUG LABEL 2 64778-0399 GEL 0.02 g DENTAL unapproved drug other 7 sections
Numfast Tetracaine Green HUMAN OTC DRUG LABEL 1 67194-020 CREAM 20 mg TOPICAL OTC monograph not final 12 sections
Tetracaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-5079 SOLUTION 5 mg OPHTHALMIC NDA 23 sections
Tetracaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68682-920 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 24 sections