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apraclonidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| alpha-2 adrenoreceptor agonists | 229 | 66711-21-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
relieves postoperative intraocular pressure following trabeculoplasty; RN given refers to parent cpd
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,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K1,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 58 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,MAPK7,PDK4,STK33,TEK | 7 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 31, 1987 | FDA | ALCON |
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 | S01EA03 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Sympathomimetics in glaucoma therapy |
| FDA MoA | N0000000209 | Adrenergic alpha-Agonists |
| FDA EPC | N0000175552 | alpha-Adrenergic Agonist |
| CHEBI has role | CHEBI:33295 | diagnostic agent |
| CHEBI has role | CHEBI:35522 | β-adrenergic agonist |
| CHEBI has role | CHEBI:35569 | α-adrenergic agonist |
| CHEBI has role | CHEBI:39456 | antiglaucoma drug |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
| MeSH PA | D000316 | Adrenergic alpha-Agonists |
| MeSH PA | D000322 | Adrenergic Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D058647 | Adrenergic alpha-2 Receptor Agonists |
Related Drugs by ATC class:
S01EA Sympathomimetics in glaucoma therapy 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Percutaneous coronary intervention | indication | 415070008 | |
| Increased Intraocular Pressure after Ocular Procedure | indication | ||
| Prevention of Cerebral Thrombosis | indication | ||
| Subacute Stent Thrombosis Prevention | indication | ||
| Cerebrovascular Occlusion | indication | ||
| Ocular hypertension | off-label use | 4210003 | DOID:9282 |
| Obstruction of bile duct | contraindication | 30144000 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Hyperlipidemia | contraindication | 55822004 | DOID:1168 |
| Acute nephropathy | contraindication | 58574008 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Ascorbic acid deficiency | contraindication | 76169001 | |
| Thrombotic thrombocytopenic purpura | contraindication | 78129009 | DOID:10772 |
| Congenital hypoplastic anemia | contraindication | 88854002 | DOID:1339 |
| Leukemia, disease | contraindication | 93143009 | DOID:1240 |
| Procedure on central nervous system | contraindication | 118679007 | |
| Bleeding | contraindication | 131148009 | |
| Arterial aneurysm | contraindication | 233981004 | |
| Syncope | contraindication | 271594007 | |
| Cerebral hemorrhage | contraindication | 274100004 | |
| Lumbar puncture | contraindication | 277762005 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Surgical procedure | contraindication | 387713003 | |
| Severe Cardiopulmonary Disease | contraindication | ||
| Vagal Reflex Bradycardia | 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 | 8.5 | Basic |
| pKa2 | 2.53 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | AGONIST | Ki | 8.54 | CHEMBL | CHEMBL | |||
| Alpha-2B adrenergic receptor | GPCR | AGONIST | Ki | 7.94 | PDSP | CHEMBL | |||
| Alpha-2C adrenergic receptor | GPCR | AGONIST | Ki | 7.52 | CHEMBL | CHEMBL | |||
| Adrenergic receptor alpha-1 | GPCR | Ki | 6.74 | CHEMBL | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 8.32 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021073 | VUID |
| N0000148534 | NUI |
| D01008 | KEGG_DRUG |
| 73218-79-8 | SECONDARY_CAS_RN |
| 14845 | RXNORM |
| C0048038 | UMLSCUI |
| CHEBI:2788 | CHEBI |
| CHEMBL647 | ChEMBL_ID |
| DB00964 | DRUGBANK_ID |
| CHEMBL1200379 | ChEMBL_ID |
| C016986 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2216 | PUBCHEM_CID |
| 7117 | IUPHAR_LIGAND_ID |
| 6263 | INN_ID |
| 843CEN85DI | UNII |
| 167318 | MMSL |
| 4214 | MMSL |
| 4020012 | VANDF |
| 4021073 | VANDF |
| 000651 | NDDF |
| 000652 | NDDF |
| 17244004 | SNOMEDCT_US |
| 330870004 | SNOMEDCT_US |
| 391786008 | SNOMEDCT_US |
| 843CEN85DI | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| IOPIDINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0065-0660 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | NDA | 19 sections |
| Apraclonidine Ophthalmic | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-716 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 20 sections |
| Apraclonidine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-665 | SOLUTION | 5.75 mg | OPHTHALMIC | NDA authorized generic | 20 sections |
| IOPIDINE 1% | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82667-200 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | NDA | 19 sections |
| IOPIDINE 1% | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82667-200 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | NDA | 19 sections |