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procaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 2271 | 59-46-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 60.45 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.149 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.259 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 31.046 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 66.834 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 88.310 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 79.550 | % | High | 1 |
| herg | hERG pIC50 | 5.095 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 10.116 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.920 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 87.770 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 58 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK4,DDR1,DYRK1B,EPHB4,GRK2,MAP2K6,MAPK7,MARK4,NUAK1,PDK4,PRKCD,SIK2,SIK3,STK33,TEK,TTK,ULK1 | 19 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.516 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 294.442 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 93.100 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.608 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 87.990 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 248.313 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 95.730 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 83.080 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 914.113 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 1, 1954 | FDA | LEDERLE |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 333.88 | 40.19 | 104 | 255 | 463505 | 90164583 |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 248.50 | 35.22 | 92 | 521 | 453998 | 110134688 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C05AD05 | CARDIOVASCULAR SYSTEM VASOPROTECTIVES AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Local anesthetics |
| ATC | N01BA02 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Esters of aminobenzoic acid |
| ATC | N01BA52 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Esters of aminobenzoic acid |
| ATC | S01HA05 | SENSORY ORGANS OPHTHALMOLOGICALS LOCAL ANESTHETICS Local anesthetics |
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D000779 | Anesthetics, Local |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35488 | central nervous system depressant |
| CHEBI has role | CHEBI:36333 | local anaesthetic |
| CHEBI has role | CHEBI:49110 | peripheral nervous system drug |
| CHEBI has role | CHEBI:88188 | drug allergen |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
Related Drugs by ATC class:
C05AD Local anesthetics 6 drugs
N01BA Esters of aminobenzoic acid 4 drugs
S01HA Local anesthetics 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Local anesthesia | indication | 386761002 | |
| Life-Threatening Ventricular Tachycardia | indication | ||
| Bundle branch block | contraindication | 6374002 | |
| Poisoning by digitalis glycoside | contraindication | 12876009 | |
| Hyperkalemia | contraindication | 14140009 | |
| Agranulocytosis | contraindication | 17182001 | DOID:12987 |
| Complete atrioventricular block | contraindication | 27885002 | |
| Torsades de pointes | contraindication | 31722008 | |
| Hypokalemia | contraindication | 43339004 | |
| Low blood pressure | contraindication | 45007003 | |
| Chronic heart failure | contraindication | 48447003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Bleeding hemorrhoids | contraindication | 51551000 | |
| Systemic lupus erythematosus | contraindication | 55464009 | DOID:9074 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Disorder of mucous membrane | contraindication | 95351003 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Second degree atrioventricular block | contraindication | 195042002 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Infectious mononucleosis | contraindication | 271558008 | DOID:8568 |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Deficiency of cholinesterase | contraindication | 360607009 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Myocardial infarction in recovery phase | contraindication | 418044006 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Procainamide Toxicity | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.8 | Basic |
| pKa2 | 2.5 | 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 10 subunit alpha | Ion channel | BLOCKER | DRUGBANK | CHEMBL | |||||
| 5-hydroxytryptamine receptor 3A | Ion channel | IC50 | 5.57 | WOMBAT-PK | |||||
| Glutamate receptor ionotropic, NMDA 3A | Ion channel | IC50 | 3.53 | WOMBAT-PK | |||||
| Ryanodine receptor 1 | Ion channel | IC50 | 2.22 | WOMBAT-PK | |||||
| Acetylcholine receptor | Ion channel | IC50 | 4.34 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019905 | VUID |
| N0000147990 | NUI |
| D00740 | KEGG_DRUG |
| 4018250 | VANDF |
| 4019905 | VANDF |
| C0033218 | UMLSCUI |
| CHEBI:8430 | CHEBI |
| CHEMBL569 | ChEMBL_ID |
| DB00721 | DRUGBANK_ID |
| CHEMBL1985617 | ChEMBL_ID |
| CHEMBL1200841 | ChEMBL_ID |
| D011343 | MESH_DESCRIPTOR_UI |
| 4914 | PUBCHEM_CID |
| 4291 | IUPHAR_LIGAND_ID |
| 975 | INN_ID |
| 51-05-8 | SECONDARY_CAS_RN |
| 4Z8Y51M438 | UNII |
| 106558 | RXNORM |
| 12417 | MMSL |
| 2045 | MMSL |
| 5359 | MMSL |
| 7218 | MMSL |
| d01394 | MMSL |
| 001348 | NDDF |
| 004565 | NDDF |
| 387238009 | SNOMEDCT_US |
| 42514000 | SNOMEDCT_US |
| 73444000 | SNOMEDCT_US |
| D008619 | MESH_DESCRIPTOR_UI |
| 4Z8Y51M438 | INXIGHT DRUGS |
Pharmaceutical products:
None