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chloroprocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 605 | 133-16-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Chloroprocaine, like other local anesthetics, blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone.
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 |
|---|---|---|---|---|---|
| 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,JAK3,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 57 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK4,DDR1,DYRK1B,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK7,MARK4,PDK4,PRKCD,SIK2,SIK3,STK33,TEK,TTK,ULK1 | 19 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 11, 1955 | FDA | FRESENIUS KABI USA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N01BA04 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Esters of aminobenzoic acid |
| ATC | S01HA08 | SENSORY ORGANS OPHTHALMOLOGICALS LOCAL ANESTHETICS Local anesthetics |
| FDA CS | M0007766 | Esters |
| 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:35480 | analgesic |
| 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:66981 | ophthalmology drug |
| CHEBI has role | CHEBI:38867 | anaesthetic |
| FDA EPC | N0000175683 | Ester Local Anesthetic |
| FDA PE | N0000175976 | Local Anesthesia |
Related Drugs by ATC class:
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 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Deficiency of cholinesterase | contraindication | 360607009 |
🐶 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 | 2.01 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 50MG/5ML (10MG/ML) | CLOROTEKAL | B BRAUN MEDICAL | N208791 | Sept. 26, 2017 | DISCN | SOLUTION | INTRATHECAL | 8969412 | Sept. 5, 2026 | A METHOD FOR INDUCING A REGIONAL ANAESTHESIA VIA INTRATHECAL ADMINISTRATION OF A PATENTED PRESERVATIVE FREE SOLUTION FOR INJECTION (WITH A SPECIFIC COMPOSITION, PH, OSMOLALITY AND DENSITY) CONTAINING 9-11 MG/ML CHLOROPROCAINE HCL |
| 3% | IHEEZO | HARROW EYE | N216227 | Sept. 27, 2022 | RX | GEL | OPHTHALMIC | 10792271 | Sept. 15, 2038 | METHOD OF INDUCING OCULAR ANESTHESIA |
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 |
External reference:
| ID | Source |
|---|---|
| 4019674 | VUID |
| N0000179078 | NUI |
| D00732 | KEGG_DRUG |
| 3858-89-7 | SECONDARY_CAS_RN |
| 20859 | RXNORM |
| C0055443 | UMLSCUI |
| CHEBI:3636 | CHEBI |
| CHEMBL1179047 | ChEMBL_ID |
| DB01161 | DRUGBANK_ID |
| CHEMBL944 | ChEMBL_ID |
| C004616 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8612 | PUBCHEM_CID |
| 7145 | IUPHAR_LIGAND_ID |
| 487 | INN_ID |
| 5YVB0POT2H | UNII |
| 4416 | MMSL |
| 4737 | MMSL |
| d01395 | MMSL |
| 001349 | NDDF |
| 004566 | NDDF |
| 19421007 | SNOMEDCT_US |
| 370295004 | SNOMEDCT_US |
| 71668006 | SNOMEDCT_US |
| 4018722 | VANDF |
| 4019674 | VANDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Chloroprocaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9209 | INJECTION, SOLUTION | 20 mg | EPIDURAL | ANDA | 21 sections |
| Chloroprocaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9210 | INJECTION, SOLUTION | 30 mg | EPIDURAL | ANDA | 21 sections |
| Clorotekal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0264-7055 | INJECTION, SOLUTION | 10 mg | INTRATHECAL | NDA | 26 sections |
| NESACAINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9927 | INJECTION, SOLUTION | 20 mg | INFILTRATION | NDA | 11 sections |
| CHLOROPROCAINE HCI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1401 | INJECTION, SOLUTION | 20 mg | INFILTRATION | NDA | 13 sections |
| (CHLOROPROCAINE HCI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1407 | INJECTION, SOLUTION | 10 mg | INFILTRATION | NDA | 13 sections |
| CHLOROPROCAINE HCI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1408 | INJECTION, SOLUTION | 20 mg | INFILTRATION | NDA | 13 sections |
| Nesacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-475 | INJECTION, SOLUTION | 10 mg | INFILTRATION | NDA | 13 sections |
| Nesacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-476 | INJECTION, SOLUTION | 20 mg | INFILTRATION | NDA | 13 sections |
| Nesacaine MPF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-477 | INJECTION, SOLUTION | 20 mg | INFILTRATION | NDA | 13 sections |
| Nesacaine MPF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-478 | INJECTION, SOLUTION | 30 mg | INFILTRATION | NDA | 13 sections |
| IHEEZO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82667-300 | GEL | 24 mg | OPHTHALMIC | NDA | 15 sections |
| IHEEZO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82667-300 | GEL | 24 mg | OPHTHALMIC | NDA | 15 sections |
| Chloroprocaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 84549-209 | INJECTION, SOLUTION | 20 mg | EPIDURAL | ANDA | 21 sections |