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cinchocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 859 | 85-79-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.594 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.693 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 30.339 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 32.211 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 13.460 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 22.300 | % | High | 1 |
| herg | hERG pIC50 | 5.863 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 11.695 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 28.774 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 17.350 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 32 | |||
| kinase-selectivity-class | AXL,BRAF | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.465 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 117.220 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 16.290 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.664 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.66 | |
| pppb | Pig plasma protein binding (% unbound) | 24.490 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 222.331 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 41.620 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 15.550 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 855.067 | uM | High | 1 |
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 |
|---|---|---|---|---|---|---|
| Heart sounds | 113.53 | 105.55 | 17 | 615 | 1127 | 90626688 |
| Prolonged expiration | 111.93 | 105.55 | 17 | 615 | 1240 | 90626575 |
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 |
|---|---|---|---|---|---|---|
| Heart sounds | 108.20 | 61.84 | 17 | 1034 | 1126 | 110587122 |
| Prolonged expiration | 103.00 | 61.84 | 17 | 1034 | 1535 | 110586713 |
| Depressive symptom | 74.33 | 61.84 | 17 | 1034 | 8397 | 110579851 |
| Appetite disorder | 71.80 | 61.84 | 17 | 1034 | 9752 | 110578496 |
| Respiration abnormal | 71.73 | 61.84 | 17 | 1034 | 9792 | 110578456 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | D002492 | Central Nervous System Depressants |
| 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 anaesthetic |
Related Drugs by ATC class:
C05AD Local anesthetics 6 drugs
D04AB Anesthetics for topical use 6 drugs
N01BB Amides 10 drugs
S01HA Local anesthetics 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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
| Species | Use | Relation |
|---|---|---|
| Dogs | Euthanasia | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Repose Euthanasia Solution | Zoetis Inc. | 2 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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 |
| 61-12-1 | SECONDARY_CAS_RN |
| 3025 | PUBCHEM_CID |
| 14979 | MMSL |
| 399945 | MMSL |
| 4577 | MMSL |
| 5847 | MMSL |
| 73107 | MMSL |
| 001371 | NDDF |
| 001372 | NDDF |
| 349831001 | SNOMEDCT_US |
| 395953008 | SNOMEDCT_US |
| 39808001 | SNOMEDCT_US |
| D003992 | MESH_DESCRIPTOR_UI |
| 7159 | IUPHAR_LIGAND_ID |
| 108 | INN_ID |
| L6JW2TJG99 | UNII |
| L6JW2TJG99 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 Drug | 14 sections |
| Precaine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 10866-0062 | GEL | 8 mg | TOPICAL | Export only | 6 sections |
| CVS Topical Analgesic Hemorrhoidal | HUMAN OTC DRUG LABEL | 1 | 51316-207 | OINTMENT | 10 mg | TOPICAL | OTC Monograph Drug | 13 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 Drug | 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 | 69396-023 | OINTMENT | 1 g | TOPICAL | OTC Monograph Drug | 15 sections |
| Dibucaine | HUMAN OTC DRUG LABEL | 1 | 71399-2829 | OINTMENT | 0.28 g | TOPICAL | OTC Monograph Drug | 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 |
| Gaayou Numbing | HUMAN OTC DRUG LABEL | 1 | 85248-150 | CREAM | 0.50 g | TOPICAL | OTC Monograph Drug | 13 sections |