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proparacaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 2294 | 499-67-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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,ACVRL1,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,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 62 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,PDK4,STK33 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 1, 1953 | 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 |
|---|---|---|---|---|---|---|
| Retinopathy of prematurity | 180.52 | 82.18 | 23 | 789 | 351 | 90627284 |
| Endophthalmitis | 97.45 | 82.18 | 19 | 793 | 4666 | 90622969 |
| Visual acuity reduced | 85.57 | 82.18 | 23 | 789 | 23387 | 90604248 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Conjunctival hyperaemia | 226.72 | 105.54 | 42 | 919 | 3134 | 42617240 |
| Hypopyon | 220.82 | 105.54 | 32 | 929 | 503 | 42619871 |
| Corneal epithelium defect | 212.17 | 105.54 | 30 | 931 | 392 | 42619982 |
| Corneal oedema | 193.71 | 105.54 | 33 | 928 | 1515 | 42618859 |
| Ulcerative keratitis | 190.45 | 105.54 | 34 | 927 | 2054 | 42618320 |
| Keratopathy | 159.61 | 105.54 | 25 | 936 | 673 | 42619701 |
| Eye pain | 156.48 | 105.54 | 42 | 919 | 16988 | 42603386 |
| Corneal infiltrates | 133.63 | 105.54 | 18 | 943 | 159 | 42620215 |
| Photophobia | 108.39 | 105.54 | 27 | 934 | 8092 | 42612282 |
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 |
|---|---|---|---|---|---|---|
| Corneal epithelium defect | 299.20 | 80.49 | 42 | 1489 | 870 | 110586898 |
| Conjunctival hyperaemia | 285.31 | 80.49 | 52 | 1479 | 5779 | 110581989 |
| Hypopyon | 264.71 | 80.49 | 40 | 1491 | 1400 | 110586368 |
| Corneal oedema | 253.77 | 80.49 | 43 | 1488 | 3130 | 110584638 |
| Keratopathy | 221.03 | 80.49 | 34 | 1497 | 1339 | 110586429 |
| Ulcerative keratitis | 210.46 | 80.49 | 39 | 1492 | 4727 | 110583041 |
| Eye pain | 169.71 | 80.49 | 51 | 1480 | 50048 | 110537720 |
| Corneal infiltrates | 145.75 | 80.49 | 20 | 1511 | 346 | 110587422 |
| Endophthalmitis | 143.38 | 80.49 | 31 | 1500 | 8156 | 110579612 |
| Visual acuity reduced | 127.41 | 80.49 | 37 | 1494 | 32136 | 110555632 |
| Persistent corneal epithelial defect | 113.71 | 80.49 | 14 | 1517 | 97 | 110587671 |
| Ciliary hyperaemia | 109.04 | 80.49 | 13 | 1518 | 66 | 110587702 |
| Photophobia | 103.60 | 80.49 | 30 | 1501 | 25741 | 110562027 |
| Corneal opacity | 100.23 | 80.49 | 17 | 1514 | 1234 | 110586534 |
| Toxic anterior segment syndrome | 94.88 | 80.49 | 19 | 1512 | 3435 | 110584333 |
| Drug abuse | 91.87 | 80.49 | 46 | 1485 | 177365 | 110410403 |
| Lacrimation increased | 89.71 | 80.49 | 28 | 1503 | 30922 | 110556846 |
| Off label use | 86.64 | 80.49 | 104 | 1427 | 1500081 | 109087687 |
| Retinal disorder | 83.15 | 80.49 | 16 | 1515 | 2354 | 110585414 |
| Vitreous floaters | 81.53 | 80.49 | 20 | 1511 | 9114 | 110578654 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | S01HA04 | SENSORY ORGANS OPHTHALMOLOGICALS LOCAL ANESTHETICS Local anesthetics |
| FDA EPC | N0000175539 | Local Anesthetic |
| 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 | N0000175976 | Local Anesthesia |
| CHEBI has role | CHEBI:35480 | analgesic |
Related Drugs by ATC class:
S01HA Local anesthetics 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Administration of Corneal Anesthesia | indication | ||
| Local Anesthesia for Ophthalmologic Procedure | indication | ||
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Eye infection | contraindication | 128351009 | |
| Uveitis | contraindication | 128473001 | DOID:13141 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Multiple Species | Ophthalmic anesthetic | Indication |
| Multiple Species | Anesthetic in cauterization of corneal ulcers, minor surgery, removal of sutures from the cornea, removal of foreign bodies cornea | Indication |
| Multiple Species | For examination and treatment of painful otitis, and prior to catheterization | Indication |
| Multiple Species | For removal of foreign bodies from eye, ear, and nose | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Ophthaine Solution | Zoetis Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.8 | Basic |
| pKa2 | 3.76 | 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 | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | BLOCKER | IC50 | 5.72 | CHEMBL | CHEMBL | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7 | DRUG MATRIX | |||||
| Amine oxidase [flavin-containing] A | Enzyme | IC50 | 5.75 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| 4019913 | VUID |
| N0000179224 | NUI |
| D02098 | KEGG_DRUG |
| 5875-06-9 | SECONDARY_CAS_RN |
| 4017727 | VANDF |
| 4019913 | VANDF |
| C0072510 | UMLSCUI |
| CHEBI:8485 | CHEBI |
| CHEMBL1196 | ChEMBL_ID |
| DB00807 | DRUGBANK_ID |
| CHEMBL1200464 | ChEMBL_ID |
| 4935 | PUBCHEM_CID |
| 7283 | IUPHAR_LIGAND_ID |
| C005717 | MESH_SUPPLEMENTAL_RECORD_UI |
| 540 | INN_ID |
| B4OB0JHI1X | UNII |
| 203759 | RXNORM |
| 3827 | MMSL |
| 39893 | MMSL |
| 5370 | MMSL |
| 7955 | MMSL |
| 001360 | NDDF |
| 004572 | NDDF |
| 30424002 | SNOMEDCT_US |
| 349837002 | SNOMEDCT_US |
| 373465008 | SNOMEDCT_US |
| B4OB0JHI1X | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Alcaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0998-0016 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 15 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13985-611 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 17 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-195 | SOLUTION | 5 mg | OPHTHALMIC | ANDA | 10 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-263 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 18 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-530 | SOLUTION | 5 mg | OPHTHALMIC | ANDA | 18 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-730 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Proparacaine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42571-497 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 17 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-0259 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 17 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1923 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1931 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52959-705 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Fluorescein Sodium and Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 59390-205 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | unapproved drug other | 10 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-016 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68071-4368 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| proparacaine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68071-5139 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 15 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70069-601 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 15 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-3408 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Proparacaine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70756-193 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 10 sections |
| Mydriatic-4 | HUMAN PRESCRIPTION DRUG LABEL | 4 | 71384-632 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | unapproved drug other | 2 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 85766-039 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 15 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 85766-056 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |
| Proparacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 85766-057 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 16 sections |