apraclonidine indications/contra

Stem definitionDrug idCAS RN
antihypertensives, clonidine derivatives 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

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 31, 1987 FDA ALCON

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC S01EA03 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Sympathomimetics in glaucoma therapy1)
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
CHEBI has role CHEBI:66981 ophthalmology drug
CHEBI has role CHEBI:35522 beta-adrenergic agonist
CHEBI has role CHEBI:33295 diagnostic agent
CHEBI has role CHEBI:35569 alpha-adrenergic agonist
CHEBI has role CHEBI:39456 antiglaucoma drug
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Open-angle glaucoma indication 84494001 DOID:1067
Percutaneous coronary intervention indication 415070008
Subacute Stent Thrombosis Prevention indication
Cerebrovascular Occlusion indication
Increased Intraocular Pressure after Ocular Procedure indication
Prevention of Cerebral Thrombosis indication
Obstruction of bile duct contraindication 30144000 DOID:13580
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 DOID:13724
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Congenital hypoplastic anemia contraindication 88854002 DOID:1342
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
Ocular hypertension off-label use 4210003 DOID:9282

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2B adrenergic receptor GPCR AGONIST Ki 7.94 PDSP CHEMBL
Alpha-2C adrenergic receptor GPCR AGONIST Ki 7.52 CHEMBL CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST Ki 8.54 CHEMBL CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 6.74 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 8.32 CHEMBL

External reference:

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IDSource
4021073 VUID
N0000148534 NUI
C0048038 UMLSCUI
7117 IUPHAR_LIGAND_ID
D01008 KEGG_DRUG
CHEMBL647 ChEMBL_ID
DB00964 DRUGBANK_ID
2216 PUBCHEM_CID
391786008 SNOMEDCT_US
N0000006575 NDFRT
N0000148534 NDFRT
14845 RXNORM
330870004 SNOMEDCT_US
4021073 VANDF
000651 NDDF
843CEN85DI UNII
6263 INN_ID
CHEBI:2788 CHEBI
CHEMBL1200379 ChEMBL_ID
73218-79-8 SECONDARY_CAS_RN
C016986 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
IOPIDINE HUMAN PRESCRIPTION DRUG LABEL 1 0065-0660 SOLUTION/ DROPS 10 mg OPHTHALMIC NDA 14 sections
Iopidine HUMAN PRESCRIPTION DRUG LABEL 1 0065-0665 SOLUTION 5 mg OPHTHALMIC NDA 18 sections
Apraclonidine Ophthalmic HUMAN PRESCRIPTION DRUG LABEL 1 17478-716 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 sections
Apraclonidine HUMAN PRESCRIPTION DRUG LABEL 1 61314-665 SOLUTION 5.75 mg OPHTHALMIC NDA authorized generic 12 sections