procaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 |
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 | 348.45 | 44.71 | 102 | 205 | 310585 | 63178130 |
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 | 256.47 | 38.86 | 90 | 477 | 298826 | 79444995 |
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 | 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:35488 | central nervous system depressants |
| CHEBI has role | CHEBI:36333 | local anesthetics |
| CHEBI has role | CHEBI:49110 | peripheral nervous system drugs |
| CHEBI has role | CHEBI:88188 | allergenic drug |
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 |
| 51-05-8 | SECONDARY_CAS_RN |
| 4018250 | VANDF |
| 4019905 | VANDF |
| C0033218 | UMLSCUI |
| CHEBI:8430 | CHEBI |
| CHEMBL569 | ChEMBL_ID |
| DB00721 | DRUGBANK_ID |
| CHEMBL1985617 | ChEMBL_ID |
| D011343 | MESH_DESCRIPTOR_UI |
| 4914 | PUBCHEM_CID |
| 4291 | IUPHAR_LIGAND_ID |
| 975 | INN_ID |
| 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 |
| CHEMBL1200841 | ChEMBL_ID |
Pharmaceutical products:
None