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

Stem definitionDrug idCAS RN
potassium channel blockers 4365 794466-70-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • RSD1235
  • vernakalant
  • vernakalant hydrochloride
  • brinavess
  • vernakalant HCl
Vernakalant is an antiarrhythmic medicine that acts preferentially in the atria to prolong atrial refractoriness and to rate-dependently slow impulse conduction. These anti-fibrillatory actions on refractoriness and conduction are thought to suppress re-entry, and are potentiated in the atria during atrial fibrillation. The relative selectivity of vernakalant on atrial versus ventricular refractoriness is postulated to result from the block of currents that are expressed in the atria, but not in the ventricles, as well as the unique electrophysiologic condition of the fibrillating atria. However, blockade of cationic currents, including hERG channels and cardiac voltage-dependent sodium channels, which are present in the ventricles has been documented.
  • Molecular weight: 349.47
  • Formula: C20H31NO4
  • CLOGP: 2.53
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 51.16
  • ALOGS: -3.35
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.20 g P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.80 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.29 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.13 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 1, 2010 EMA Cardiome UK Limited

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
Sinus arrest 25.57 22.19 3 3 1737 34955188

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
Sinus arrest 25.84 23.22 3 3 3619 79740763

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01BG11 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Other antiarrhythmics, class I and III

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

DiseaseRelationSNOMED_IDDOID
Atrial fibrillation indication 49436004 DOID:0060224




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.61 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
Potassium voltage-gated channel subfamily A member 5 Ion channel BLOCKER IC50 4.88 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium channel protein type 5 subunit alpha Ion channel IC50 4.73 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.16 CHEMBL
Potassium voltage-gated channel subfamily D member 2 Ion channel IC50 4.30 CHEMBL

External reference:

IDSource
D06665 KEGG_DRUG
748810-28-8 SECONDARY_CAS_RN
C2001572 UMLSCUI
CHEBI:135956 CHEBI
CHEMBL2111112 ChEMBL_ID
CHEMBL2107383 ChEMBL_ID
DB06217 DRUGBANK_ID
C524581 MESH_SUPPLEMENTAL_RECORD_UI
8733 INN_ID
9G468C8B13 UNII
9930049 PUBCHEM_CID
014756 NDDF
014757 NDDF
698874004 SNOMEDCT_US

Pharmaceutical products:

None