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

Stem definition	Drug id	CAS RN
acetylcholinesterase inhibitors	927	17299-00-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: BC-51 hexamarium distigmine distigmine bromide ubretid	Molecular weight: 416.52 Formula: C22H32N4O4 CLOGP: -7.11 LIPINSKI: 0 HAC: 8 HDO: 0 TPSA: 66.84 ALOGS: -6.02 ROTB: 11

Molecule

Description

Molfile Inchi Smiles

Synonyms:

BC-51
hexamarium
distigmine
distigmine bromide
ubretid

Molecular weight: 416.52
Formula: C22H32N4O4
CLOGP: -7.11
LIPINSKI: 0
HAC: 8
HDO: 0
TPSA: 66.84
ALOGS: -6.02
ROTB: 11

Drug dosage:

Dose	Unit	Route
5	mg	O
0.25	mg	P

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	8 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	59.80 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 5, 1967	PMDA	Torii Pharmaceuticals

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
Cholinergic syndrome	58.23	39.49	8	245	510	63488259

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
Appendicolith	497.25	87.30	123	3187	8478	34945143
Appendicitis	431.00	87.30	123	3187	14684	34938937
Cardiogenic shock	363.87	87.30	124	3186	26494	34927127
Stress	351.76	87.30	125	3185	30222	34923399
Ventricular fibrillation	305.94	87.30	105	3205	22849	34930772
Ascites	296.32	87.30	124	3186	46447	34907174
Blood phosphorus increased	273.87	87.30	75	3235	7646	34945975
Abdominal distension	272.30	87.30	125	3185	58367	34895254
Hyponatraemia	242.52	87.30	129	3181	82562	34871059
Multiple organ dysfunction syndrome	237.41	87.30	124	3186	76442	34877179
Constipation	198.89	87.30	136	3174	136846	34816775
General physical health deterioration	182.89	87.30	126	3184	128143	34825478
Sepsis	161.99	87.30	130	3180	166431	34787190
Dry mouth	160.70	87.30	71	3239	30094	34923527
Abdominal pain	151.21	87.30	124	3186	163494	34790127
Myasthenia gravis	121.13	87.30	39	3271	6901	34946720
Blood uric acid increased	116.22	87.30	41	3269	9583	34944038
Vomiting	109.23	87.30	125	3185	247496	34706125

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
Appendicolith	580.53	56.35	122	3541	8429	79732296
Appendicitis	472.67	56.35	122	3541	20672	79720053
Cardiogenic shock	392.27	56.35	123	3540	41791	79698934
Ventricular fibrillation	342.11	56.35	104	3559	31822	79708903
Ascites	321.28	56.35	123	3540	75439	79665286
Stress	318.59	56.35	124	3539	79488	79661237
Blood phosphorus increased	305.84	56.35	75	3588	10272	79730453
Abdominal distension	269.85	56.35	124	3539	119526	79621199
Multiple organ dysfunction syndrome	269.26	56.35	124	3539	120122	79620603
Hyponatraemia	237.16	56.35	129	3534	177719	79563006
Constipation	205.55	56.35	139	3524	282911	79457814
Sepsis	192.41	56.35	131	3532	269297	79471428
General physical health deterioration	180.45	56.35	127	3536	275111	79465614
Dry mouth	137.12	56.35	71	3592	87948	79652777
Abdominal pain	135.49	56.35	124	3539	389445	79351280
Myasthenia gravis	133.37	56.35	39	3624	10360	79730365
Blood uric acid increased	132.11	56.35	41	3622	13319	79727406
Vomiting	88.60	56.35	129	3534	665699	79075026
Drug therapy	74.81	56.35	16	3647	1185	79739540
Somnolence	73.02	56.35	71	3592	238910	79501815
Analgesic therapy	71.77	56.35	15	3648	994	79739731
Sleep disorder therapy	65.82	56.35	14	3649	1010	79739715
Incorrect route of product administration	65.51	56.35	32	3631	34897	79705828
Nausea	61.57	56.35	135	3528	957061	78783664
Hyperphosphataemia	60.62	56.35	19	3644	6357	79734368
Cholinergic syndrome	59.38	56.35	13	3650	1074	79739651
Iron deficiency	58.49	56.35	21	3642	10633	79730092
Blood cholesterol increased	57.70	56.35	40	3623	83680	79657045

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N07AA03	NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D002800	Cholinesterase Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D018377	Neurotransmitter Agents
CHEBI has role	CHEBI:37733	EC 3.1.1.8 inhibitor
CHEBI has role	CHEBI:38325	muscarinic agonists

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

Disease	Relation	SNOMED_ID	DOID
Acute cystitis	indication	68226007	DOID:13148
Myasthenia gravis	indication	91637004	DOID:437
Difficulty passing urine	indication	102835006

🐶 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])	Mechanism action	Bioact source	MoA source
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN	INHIBITOR				KEGG DRUG	KEGG DRUG

External reference:

ID	Source
D01228	KEGG_DRUG
154982	RXNORM
C0012757	UMLSCUI
CHEBI:31512	CHEBI
CHEMBL1199307	ChEMBL_ID
CHEMBL1098285	ChEMBL_ID
DB13694	DRUGBANK_ID
C084645	MESH_SUPPLEMENTAL_RECORD_UI
3116	PUBCHEM_CID
15876-67-2	SECONDARY_CAS_RN
T940307O7B	UNII
003959	NDDF
349943004	SNOMEDCT_US
395966008	SNOMEDCT_US
396033002	SNOMEDCT_US
764	INN_ID

Pharmaceutical products:

None