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

Stem definitionDrug idCAS RN
vasodilators 1873 57149-07-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • BM-15275
  • KT-611
  • naftopidil
  • avishot
  • flivas
  • naftopil
  • naftopidil hydrochloride
  • naftopidil dihydrochloride
  • naftopidil HCl
  • Molecular weight: 392.50
  • Formula: C24H28N2O3
  • CLOGP: 4.24
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 45.17
  • ALOGS: -3.75
  • ROTB: 7

Drug dosage:

None

ADMET properties:

PropertyValueReference
CL (Clearance) 11 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.30 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.11 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 0.18 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

DateAgencyCompanyOrphan
Dec. 25, 1998 PMDA Asahi Kasei

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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
Interstitial lung disease 56.34 30.33 33 1249 65249 34890400
Urinary retention 49.88 30.33 25 1257 36263 34919386
Cerebral infarction 40.93 30.33 20 1262 27435 34928214

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
Interstitial lung disease 68.95 33.95 34 1209 112566 79630579
Urinary retention 53.07 33.95 23 1220 56607 79686538
Cerebral infarction 47.57 33.95 20 1223 45656 79697489
Hepatic function abnormal 35.73 33.95 19 1224 73088 79670057

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D018663 Adrenergic Agents
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010975 Platelet Aggregation Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Benign prostatic hyperplasia indication 266569009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.57 Basic
pKa2 0.4 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-1A adrenergic receptor GPCR ANTAGONIST Ki 8.43 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.92 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 7.70 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor GPCR Ki 6 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 5.80 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 7.41 CHEMBL

External reference:

IDSource
D01674 KEGG_DRUG
C0083701 UMLSCUI
CHEBI:31891 CHEBI
CHEMBL142635 ChEMBL_ID
DB12092 DRUGBANK_ID
C064357 MESH_SUPPLEMENTAL_RECORD_UI
4418 PUBCHEM_CID
5589 INN_ID
57149-08-3 SECONDARY_CAS_RN
R9PHW59SFN UNII
CHEMBL1257069 ChEMBL_ID

Pharmaceutical products:

None