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

Stem definition	Drug id	CAS RN
class III antiarrhythmics	1412	122647-31-8

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

U82209E
U-82209E
U 82209E
ibutilide
ibutilide fumarate

Molecular weight: 384.58
Formula: C20H36N2O3S
CLOGP: 3.78
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 69.64
ALOGS: -4.91
ROTB: 13

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	100 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	7 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.34 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	8 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	12 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	26 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)	7 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1995	FDA	PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C01BD05	CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class III
FDA EPC	N0000175426	Antiarrhythmic
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D002317	Cardiovascular Agents

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

Disease	Relation	SNOMED_ID	DOID
Cardioversion of Atrial Flutter	indication
Cardioversion of Atrial Fibrillation	indication
Torsades de pointes	contraindication	31722008
Hypokalemia	contraindication	43339004
Bradycardia	contraindication	48867003
Prolonged QT interval	contraindication	111975006
Hypomagnesemia	contraindication	190855004
Heart block	contraindication	233916004
Congenital long QT syndrome	contraindication	442917000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.03	acidic
pKa2	9.4	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN	BLOCKER	IC50	8		CHEMBL

External reference:

ID	Source
4024018	VUID
N0000022023	NUI
D00648	KEGG_DRUG
122647-32-9	SECONDARY_CAS_RN
4020956	VANDF
4024018	VANDF
C0082966	UMLSCUI
CHEBI:5856	CHEBI
CHEMBL533	ChEMBL_ID
DB00308	DRUGBANK_ID
CHEMBL2355456	ChEMBL_ID
C067192	MESH_SUPPLEMENTAL_RECORD_UI
60753	PUBCHEM_CID
7200	IUPHAR_LIGAND_ID
6642	INN_ID
2436VX1U9B	UNII
41289	RXNORM
169546	MMSL
4863	MMSL
d03871	MMSL
005740	NDDF
005741	NDDF
108491000	SNOMEDCT_US
108492007	SNOMEDCT_US
372500009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Corvert	HUMAN PRESCRIPTION DRUG LABEL	1	0009-3794	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	25 sections
Corvert	HUMAN PRESCRIPTION DRUG LABEL	1	0009-3794	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	25 sections
Ibutilide Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	67457-366	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	25 sections