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

Stem definition	Drug id	CAS RN
	881	71-63-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: digitoxin digitoxoside cardidigin cardigin carditoxin coramedan cristapurat crystodigin digicor digipural digisidin digitophyllin digitoxigenin tridigitoxoside myodigin purpurid tradigal unidigin	A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665) Molecular weight: 764.95 Formula: C41H64O13 CLOGP: 2.85 LIPINSKI: 2 HAC: 13 HDO: 5 TPSA: 182.83 ALOGS: -4.42 ROTB: 7 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

digitoxin
digitoxoside
cardidigin
cardigin
carditoxin
coramedan
cristapurat
crystodigin
digicor
digipural
digisidin
digitophyllin
digitoxigenin tridigitoxoside
myodigin
purpurid
tradigal
unidigin

A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665)

Molecular weight: 764.95
Formula: C41H64O13
CLOGP: 2.85
LIPINSKI: 2
HAC: 13
HDO: 5
TPSA: 182.83
ALOGS: -4.42
ROTB: 7

Status: OFM

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

Drug dosage:

Dose	Unit	Route
0.10	mg	O
0.10	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	95 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	30 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	180 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.44 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.07 %	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.04 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
None	FDA	LILLY

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
General physical health deterioration	220.44	30.18	146	4009	201256	63283611
Atrial fibrillation	216.99	30.18	119	4036	116517	63368350
Product prescribing error	162.40	30.18	62	4093	26227	63458640
Arrhythmia	153.13	30.18	66	4089	38074	63446793
Product monitoring error	151.89	30.18	39	4116	4477	63480390
Bradycardia	136.68	30.18	75	4080	73152	63411715
Fall	124.73	30.18	140	4015	392194	63092673
Tachycardia	103.68	30.18	75	4080	118081	63366786
Anaemia	95.21	30.18	106	4049	293324	63191543
Therapeutic drug monitoring analysis not performed	88.55	30.18	20	4135	1332	63483535

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
General physical health deterioration	215.96	33.74	164	4828	128105	34823834
Rectal prolapse	104.54	33.74	22	4970	470	34951469
Renal cyst haemorrhage	104.33	33.74	23	4969	616	34951323
Product prescribing error	100.89	33.74	54	4938	22873	34929066
Product monitoring error	98.59	33.74	33	4959	4348	34947591
Haematochezia	92.52	33.74	66	4926	46468	34905471
Intraductal papillary mucinous neoplasm	91.47	33.74	20	4972	515	34951424
Oedema peripheral	83.85	33.74	94	4898	119718	34832221
SARS-CoV-2 antibody test positive	78.93	33.74	17	4975	407	34951532
Vena cava injury	76.84	33.74	16	4976	324	34951615

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
General physical health deterioration	413.65	30.31	295	8389	274943	79460761
Atrial fibrillation	262.27	30.31	197	8487	197689	79538015
Product prescribing error	257.13	30.31	116	8568	44697	79691007
Product monitoring error	239.39	30.31	72	8612	8834	79726870
Bradycardia	190.61	30.31	140	8544	135417	79600287
Haematochezia	171.49	30.31	111	8573	87534	79648170
Systemic infection	128.53	30.31	46	8638	9706	79725998
Arrhythmia	125.71	30.31	80	8604	61192	79674512
Dyspnoea	125.25	30.31	282	8402	856743	78878961
Therapeutic drug monitoring analysis not performed	123.98	30.31	31	8653	1905	79733799

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01AA04	CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC GLYCOSIDES Digitalis glycosides
CHEBI has role	CHEBI:63510	sodium-potassium adenosine triphosphatase inhibitors
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D002316	Cardiotonic Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D020011	Protective Agents

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

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🐶 Veterinary Drug Use

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🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium/potassium-transporting ATPase subunit alpha-1	Transporter	P05023	AT1A1_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.86	WOMBAT-PK
Signal transducer and activator of transcription 3	Transcription factor	P40763	STAT3_HUMAN		IC50	6.15	CHEMBL
Sodium/potassium-transporting ATPase	Transporter	P05023 P05026 P13637 P14415 P50993 P54709 P54710 Q13733	AT1A1_HUMAN AT1B1_HUMAN AT1A3_HUMAN AT1B2_HUMAN AT1A2_HUMAN AT1B3_HUMAN ATNG_HUMAN AT1A4_HUMAN		IC50	8.10	CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-2	Ion channel		AT1A2_PIG		IC50	6.65	DRUG MATRIX
Sodium/potassium-transporting ATPase subunit alpha-1	Transporter		AT1A1_CANFA		IC50	8.10	CHEMBL

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External reference:

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ID	Source
F9R	PDB_CHEM_ID
000592	NDDF
1547	INN_ID
195	MMSL
216288	RXNORM
373534001	SNOMEDCT_US
4017429	VUID
4017429	VANDF
441207	PUBCHEM_CID
4596	MMSL

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Pharmaceutical products:

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