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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:

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

Approvals:

Date	Agency	Company	Orphan
None	FDA	LILLY

FDA Adverse Event Reporting System (Female)

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
Haematochezia	84.01	30.18	49	4106	53495	63431372
Syncope	77.62	30.18	63	4092	117322	63367545
Systemic infection	68.23	30.18	21	4134	4639	63480228
Dyspnoea	62.89	30.18	135	4020	661178	62823689
Toxic epidermal necrolysis	58.62	30.18	30	4125	25304	63459563
Cardiac failure	57.10	30.18	47	4108	89095	63395772
Dizziness	55.58	30.18	100	4055	429825	63055042
Drug ineffective	50.79	30.18	5	4150	1044760	62440107
Stevens-Johnson syndrome	50.46	30.18	27	4128	24923	63459944
Cerebrospinal fluid retention	49.55	30.18	8	4147	84	63484783
Fracture	44.75	30.18	23	4132	19561	63465306
Cerebral ventricular rupture	42.73	30.18	8	4147	208	63484659
Labelled drug-drug interaction medication error	40.36	30.18	19	4136	13380	63471487
Spontaneous haemorrhage	39.98	30.18	9	4146	590	63484277
Gastric pH increased	39.09	30.18	6	4149	44	63484823
Therapeutic drug monitoring analysis incorrectly performed	39.02	30.18	8	4147	336	63484531
Cerebellar infarction	37.79	30.18	11	4144	2008	63482859
Dehydration	37.19	30.18	51	4104	173303	63311564
Pulmonary vein occlusion	34.31	30.18	6	4149	105	63484762
Reflexes abnormal	33.57	30.18	8	4147	673	63484194
Atrial flutter	32.99	30.18	15	4140	9757	63475110
Wound	31.99	30.18	46	4109	163217	63321650
Diverticulum intestinal haemorrhagic	31.42	30.18	9	4146	1552	63483315
Restlessness	31.13	30.18	21	4134	29432	63455435
Lip erosion	30.58	30.18	8	4147	985	63483882
Pallor	30.42	30.18	21	4134	30547	63454320

FDA Adverse Event Reporting System (Male)

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
Abdominal wall haemorrhage	76.48	33.74	17	4975	473	34951466
Atrial fibrillation	75.51	33.74	90	4902	122303	34829636
Carotid arteriosclerosis	75.51	33.74	22	4970	1836	34950103
Delayed graft function	71.63	33.74	22	4970	2199	34949740
Dyspnoea	69.32	33.74	160	4832	376622	34575317
Vascular anastomotic haemorrhage	67.73	33.74	14	4978	273	34951666
Bradycardia	66.56	33.74	67	4925	75351	34876588
Mean cell volume increased	63.95	33.74	22	4970	3147	34948792
Systemic infection	63.66	33.74	25	4967	5187	34946752
Spinal stenosis	63.39	33.74	25	4967	5244	34946695
Aortic dilatation	63.22	33.74	18	4974	1383	34950556
Perineal cyst	62.63	33.74	13	4979	259	34951680
Diverticulum intestinal	62.50	33.74	23	4969	3998	34947941
Hyperparathyroidism secondary	61.22	33.74	18	4974	1550	34950389
Aortic arteriosclerosis	59.31	33.74	23	4969	4613	34947326
Renal artery stenosis	58.78	33.74	19	4973	2242	34949697
Vascular compression	58.43	33.74	13	4979	363	34951576
Hepatosplenomegaly	58.05	33.74	22	4970	4147	34947792
Spinal osteoarthritis	57.46	33.74	26	4966	7657	34944282
Actinic keratosis	56.10	33.74	22	4970	4545	34947394
Intervertebral disc space narrowing	49.62	33.74	14	4978	1041	34950898
Labelled drug-drug interaction medication error	46.29	33.74	28	4964	14911	34937028
Blood 25-hydroxycholecalciferol decreased	45.67	33.74	10	4982	259	34951680
Swelling of eyelid	44.45	33.74	13	4979	1098	34950841
Left ventricular hypertrophy	43.92	33.74	22	4970	8108	34943831
Restless legs syndrome	43.36	33.74	22	4970	8332	34943607
Therapeutic drug monitoring analysis not performed	43.16	33.74	11	4981	554	34951385
Activated partial thromboplastin time prolonged	42.53	33.74	22	4970	8673	34943266
Electrocardiogram abnormal	41.25	33.74	22	4970	9225	34942714
Vitamin D decreased	40.09	33.74	16	4976	3460	34948479
Glycosylated haemoglobin increased	39.66	33.74	23	4969	11337	34940602
Therapeutic drug monitoring analysis incorrectly performed	38.38	33.74	9	4983	319	34951620
Squamous cell carcinoma of skin	37.90	33.74	22	4970	10859	34941080
Benign prostatic hyperplasia	36.93	33.74	24	4968	14471	34937468
C-reactive protein increased	35.27	33.74	41	4951	54057	34897882
Vertigo	34.84	33.74	29	4963	25507	34926432
Wound	33.97	33.74	23	4969	14841	34937098

FDA Adverse Event Reporting System (Geriatric)

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
Anaemia	112.37	30.31	185	8499	444830	79290874
Renal cyst haemorrhage	108.69	30.31	23	8661	669	79735035
Intraductal papillary mucinous neoplasm	88.88	30.31	20	8664	778	79734926
SARS-CoV-2 antibody test positive	82.92	30.31	17	8667	422	79735282
Labelled drug-drug interaction medication error	82.53	30.31	46	8638	27604	79708100
Oedema peripheral	81.93	30.31	118	8566	252170	79483534
Vena cava injury	80.60	30.31	16	8668	336	79735368
Fall	79.37	30.31	168	8516	487461	79248243
Toxic epidermal necrolysis	78.68	30.31	53	8631	44528	79691176
Rectal prolapse	77.92	30.31	22	8662	2156	79733548
Abdominal wall haemorrhage	75.16	30.31	17	8667	677	79735027
Therapeutic drug monitoring analysis incorrectly performed	74.63	30.31	17	8667	699	79735005
Carotid arteriosclerosis	73.61	30.31	22	8662	2634	79733070
Syncope	71.94	30.31	93	8591	179356	79556348
Vascular anastomotic haemorrhage	71.51	30.31	14	8670	273	79735431
Aortic dilatation	68.00	30.31	19	8665	1793	79733911
Delayed graft function	67.59	30.31	22	8662	3485	79732219
Spontaneous haemorrhage	67.18	30.31	16	8668	801	79734903
Perineal cyst	66.28	30.31	13	8671	256	79735448
Cardiac failure	61.65	30.31	80	8604	154762	79580942
Drug ineffective	57.68	30.31	23	8661	1080890	78654814
Wound	57.51	30.31	67	8617	116112	79619592
Hyperparathyroidism secondary	56.64	30.31	18	8666	2642	79733062
Vascular compression	56.46	30.31	13	8671	561	79735143
Tachycardia	55.96	30.31	82	8602	177686	79558018
Actinic keratosis	55.90	30.31	22	8662	6020	79729684
Hepatosplenomegaly	55.80	30.31	22	8662	6047	79729657
Renal artery stenosis	55.77	30.31	19	8665	3463	79732241
Mean cell volume increased	55.16	30.31	22	8662	6231	79729473
Dizziness	55.05	30.31	153	8531	526288	79209416
Restlessness	54.13	30.31	43	8641	46449	79689255
Aortic arteriosclerosis	53.98	30.31	24	8660	8894	79726810
Stevens-Johnson syndrome	53.88	30.31	40	8644	39126	79696578
Diverticulum intestinal	51.58	30.31	23	8661	8582	79727122
Electrocardiogram abnormal	50.36	30.31	28	8656	16709	79718995
Activated partial thromboplastin time prolonged	48.91	30.31	26	8658	14202	79721502
Pallor	47.25	30.31	41	8643	50021	79685683
Intervertebral disc space narrowing	46.48	30.31	14	8670	1721	79733983
Benign prostatic hyperplasia	45.01	30.31	23	8661	11589	79724115
Blood 25-hydroxycholecalciferol decreased	44.69	30.31	10	8674	379	79735325
Spinal osteoarthritis	44.69	30.31	26	8658	16901	79718803
Cerebrospinal fluid retention	44.50	30.31	8	8676	96	79735608
Spinal stenosis	43.67	30.31	25	8659	15766	79719938
Left ventricular hypertrophy	42.90	30.31	22	8662	11169	79724535
Squamous cell carcinoma of skin	38.23	30.31	22	8662	14011	79721693
Dehydration	36.21	30.31	82	8602	248105	79487599
Gastric pH increased	35.15	30.31	6	8678	52	79735652
Off label use	34.53	30.31	29	8655	907186	78828518
Renal impairment	33.58	30.31	61	8623	157722	79577982
Restless legs syndrome	33.32	30.31	23	8661	20069	79715635
Personality change	33.31	30.31	18	8666	10152	79725552
Cerebral ventricular rupture	32.64	30.31	8	8676	452	79735252
Thoracic haemorrhage	32.58	30.31	7	8677	219	79735485
Malaise	32.25	30.31	7	8677	489862	79245842
Swelling of eyelid	32.20	30.31	13	8671	3798	79731906
Glycosylated haemoglobin increased	31.83	30.31	22	8662	19238	79716466
Fracture	31.63	30.31	23	8661	21778	79713926

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C01AA04	CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC GLYCOSIDES Digitalis glycosides
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
CHEBI has role	CHEBI:63510	sodium-potassium adenosine triphosphatase inhibitors

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

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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])	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

External reference:

ID	Source
4017429	VUID
N0000145817	NUI
D00297	KEGG_DRUG
216288	RXNORM
4017429	VANDF
C0012258	UMLSCUI
CHEBI:28544	CHEBI
F9R	PDB_CHEM_ID
CHEMBL254219	ChEMBL_ID
D004074	MESH_DESCRIPTOR_UI
DB01396	DRUGBANK_ID
6782	IUPHAR_LIGAND_ID
1547	INN_ID
E90NZP2L9U	UNII
441207	PUBCHEM_CID
195	MMSL
4596	MMSL
d00209	MMSL
000592	NDDF
373534001	SNOMEDCT_US
81728006	SNOMEDCT_US

Pharmaceutical products:

None