apraclonidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
alpha-2 adrenoreceptor agonists 229 66711-21-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • apraclonidine
  • aplonidine
  • lopidine
  • apraclonidine hydrochloride
  • aminoclonidine monohydrochloride
  • apraclonidine HCl
relieves postoperative intraocular pressure following trabeculoplasty; RN given refers to parent cpd
  • Molecular weight: 245.11
  • Formula: C9H10Cl2N4
  • CLOGP: 0.61
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 3
  • TPSA: 62.44
  • ALOGS: -2.78
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Retinal detachment 88.15 82.83 19 575 9228 79734566

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 aid
CHEBI has role CHEBI:35522 beta-adrenergic agonists
CHEBI has role CHEBI:35569 alpha-adrenergic agonists
CHEBI has role CHEBI:39456 antiglaucoma agent
CHEBI has role CHEBI:66981 ophthalmology drugs
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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:

IDSource
4021073 VUID
N0000148534 NUI
D01008 KEGG_DRUG
73218-79-8 SECONDARY_CAS_RN
14845 RXNORM
C0048038 UMLSCUI
CHEBI:2789 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
17244004 SNOMEDCT_US
330870004 SNOMEDCT_US
391786008 SNOMEDCT_US
4020012 VANDF
4021073 VANDF
000651 NDDF
000652 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 Ophthalmic HUMAN PRESCRIPTION DRUG LABEL 1 17478-716 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 20 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