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

Stem definitionDrug idCAS RN
local anaesthetics 859 85-79-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cinchocaine
  • dermacaine
  • dibucaine
  • nupercaine
  • percamine
  • dibucaine hydrochloride
  • dibucaine HCl
A local anesthetic of the amide type now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1006)
  • Molecular weight: 343.47
  • Formula: C20H29N3O2
  • CLOGP: 5.42
  • LIPINSKI: 1
  • HAC: 5
  • HDO: 1
  • TPSA: 54.46
  • ALOGS: -3.95
  • ROTB: 10
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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
Heart sounds 63.13 58.51 10 546 956 79742876
Prolonged expiration 60.39 58.51 10 546 1261 79742571

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C05AD04 CARDIOVASCULAR SYSTEM
VASOPROTECTIVES
AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
Local anesthetics
ATC D04AB02 DERMATOLOGICALS
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Anesthetics for topical use
ATC N01BB06 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Amides
ATC S01HA06 SENSORY ORGANS
OPHTHALMOLOGICALS
LOCAL ANESTHETICS
Local anesthetics
ATC S02DA04 SENSORY ORGANS
OTOLOGICALS
OTHER OTOLOGICALS
Analgesics and anesthetics
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

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

DiseaseRelationSNOMED_IDDOID
Skin irritation indication 367466007
Itching of skin indication 418363000
Minor Skin Wound Pain indication
Conduction disorder of the heart contraindication 44808001
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Bleeding hemorrhoids contraindication 51551000
Decreased respiratory function contraindication 80954004
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Disorder of mucous membrane contraindication 95351003
Open wound contraindication 125643001
Seizure disorder contraindication 128613002
Disease of liver contraindication 235856003 DOID:409
Deficiency of cholinesterase contraindication 360607009
Denuded skin contraindication 418242004




🐶 Veterinary Drug Use

SpeciesUseRelation
Dogs Euthanasia Indication

🐶 Veterinary products

ProductApplicantIngredients
Repose Euthanasia Solution Zoetis Inc. 2

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.24 acidic
pKa2 9.02 Basic
pKa3 3.84 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 5 subunit alpha Ion channel BLOCKER DRUGBANK CHEMBL
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER DRUGBANK CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.85 CHEMBL

External reference:

IDSource
4018897 VUID
N0000147191 NUI
D00733 KEGG_DRUG
235402 RXNORM
4018897 VANDF
C0012050 UMLSCUI
CHEBI:247956 CHEBI
CHEMBL1086 ChEMBL_ID
CHEMBL1200612 ChEMBL_ID
DB00527 DRUGBANK_ID
7159 IUPHAR_LIGAND_ID
61-12-1 SECONDARY_CAS_RN
3025 PUBCHEM_CID
14979 MMSL
4577 MMSL
5847 MMSL
73107 MMSL
001371 NDDF
001372 NDDF
349831001 SNOMEDCT_US
395953008 SNOMEDCT_US
39808001 SNOMEDCT_US
D003992 MESH_DESCRIPTOR_UI
108 INN_ID
L6JW2TJG99 UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DIBUCAINE HUMAN OTC DRUG LABEL 1 0168-0046 OINTMENT 1 g TOPICAL OTC monograph final 9 sections
Dibucaine Topical Anesthetic 1% Hemorrhoidal HUMAN OTC DRUG LABEL 1 0536-1211 OINTMENT 10 mg TOPICAL OTC monograph final 14 sections
Precaine HUMAN PRESCRIPTION DRUG LABEL 2 10866-0062 GEL 8 mg BUCCAL Export only 6 sections
Precaine HUMAN PRESCRIPTION DRUG LABEL 2 10866-0062 GEL 8 mg BUCCAL Export only 6 sections
Precaine HUMAN PRESCRIPTION DRUG LABEL 2 10866-0062 GEL 8 mg BUCCAL Export only 6 sections
dibucaine HUMAN OTC DRUG LABEL 1 45802-050 OINTMENT 1 g TOPICAL OTC monograph final 14 sections
Dibucaine HUMAN OTC DRUG LABEL 1 54162-011 OINTMENT 0.28 g TOPICAL OTC monograph final 9 sections
Nupercainal HUMAN OTC DRUG LABEL 1 55741-402 OINTMENT 1 g TOPICAL OTC monograph final 15 sections
Dibucaine HUMAN OTC DRUG LABEL 1 57896-131 OINTMENT 1 g TOPICAL OTC monograph final 14 sections
DIBUCAINE HUMAN OTC DRUG LABEL 1 59779-398 CREAM 10 mg TOPICAL OTC monograph final 7 sections
CVS Hemorrhoidal Topical Analgesic HUMAN OTC DRUG LABEL 1 59779-997 OINTMENT 10 mg TOPICAL OTC monograph final 13 sections
Dibucaine HUMAN OTC DRUG LABEL 1 63868-911 OINTMENT 1 g TOPICAL OTC monograph final 15 sections
Dibucaine HUMAN OTC DRUG LABEL 1 63868-911 OINTMENT 1 g TOPICAL OTC monograph final 15 sections
Dibucaine HUMAN OTC DRUG LABEL 1 69396-023 OINTMENT 1 g TOPICAL OTC monograph final 15 sections
Dibucaine HUMAN OTC DRUG LABEL 1 71399-2829 OINTMENT 0.28 g TOPICAL OTC monograph final 9 sections
Dibucaine HUMAN OTC DRUG LABEL 1 71399-2829 OINTMENT 0.28 g TOPICAL OTC monograph final 9 sections
DIBUCAINE HCL 0.5% / LIDOCAINE 15% / PHENYLEPHRINE HCL 1% / PRILOCAINE 5% HUMAN PRESCRIPTION DRUG LABEL 4 72934-5071 OINTMENT 0.50 g TOPICAL unapproved drug other 4 sections
DIBUCAINE HUMAN OTC DRUG LABEL 1 81266-920 OINTMENT 0.01 g TOPICAL OTC monograph final 15 sections