pinacidil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasodilators 2173 60560-33-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • (R,S)-Pinacidil
  • pinacidil monohydrate
  • pinacidil
  • pindac
  • (+/-)-Pinacidil
  • pinacidil hydrate
A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)
  • Molecular weight: 245.33
  • Formula: C13H19N5
  • CLOGP: 1.91
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 73.10
  • ALOGS: -3.29
  • ROTB: 3

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 2.91 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 57 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.68 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.60 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
None FDA LEO PHARM

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C02DG01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON
Guanidine derivatives
ATC C02LX01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
Other antihypertensives and diuretics
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.09 Basic
pKa2 0.0 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
Sulfonylurea receptor 2, Kir6.2 Ion channel OPENER Ki 6.49 CHEMBL CHEMBL
ATP-binding cassette sub-family C member 9 Ion channel EC50 5.45 CHEMBL
Calcium-activated potassium channel subunit alpha-1 Ion channel WOMBAT-PK

External reference:

IDSource
4025256 VUID
N0000171786 NUI
D05482 KEGG_DRUG
85371-64-8 SECONDARY_CAS_RN
4025256 VANDF
C0071074 UMLSCUI
CHEBI:91706 CHEBI
4826 PUBCHEM_CID
CHEMBL1159 ChEMBL_ID
CHEMBL398879 ChEMBL_ID
CHEMBL251647 ChEMBL_ID
CHEMBL1200338 ChEMBL_ID
D020110 MESH_DESCRIPTOR_UI
DB06762 DRUGBANK_ID
2412 IUPHAR_LIGAND_ID
7B0ZZH8P2W UNII
33717 RXNORM
003753 NDDF
003777 NDDF

Pharmaceutical products:

None