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

Stem definition	Drug id	CAS RN
quaternary ammonium compounds	2776	10405-02-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: trospium trospium chloride relaspium	Molecular weight: 392.52 Formula: C25H30NO3 CLOGP: -1.16 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 46.53 ALOGS: -6.81 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

trospium
trospium chloride
relaspium

Molecular weight: 392.52
Formula: C25H30NO3
CLOGP: -1.16
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 46.53
ALOGS: -6.81
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	500 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	6 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.46 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	10 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	5.10 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	13.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.33 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
May 28, 2004	FDA	ALLERGAN

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
Pancreatic steatosis	114.04	19.70	25	6015	991	63481991
Lymphatic fistula	103.17	19.70	22	6018	764	63482218
Femoral hernia incarcerated	101.69	19.70	22	6018	819	63482163
Aortic valve stenosis	98.13	19.70	28	6012	3271	63479711
Arterial haemorrhage	95.97	19.70	24	6016	1693	63481289
Wound infection pseudomonas	91.68	19.70	22	6018	1306	63481676
Seroma	81.35	19.70	22	6018	2109	63480873
Tachyarrhythmia	77.43	19.70	25	6015	4425	63478557
Haemarthrosis	77.10	19.70	23	6017	3138	63479844
Fall	74.09	19.70	133	5907	392201	63090781
Faecaloma	73.97	19.70	28	6012	7913	63475069
Wound dehiscence	71.09	19.70	24	6016	4879	63478103
Urinary tract infection	70.64	19.70	105	5935	264579	63218403
Diverticulum intestinal	67.37	19.70	25	6015	6688	63476294
Hepatic cyst	66.04	19.70	23	6017	5131	63477851
Inflammatory marker increased	63.29	19.70	24	6016	6815	63476167
Eructation	62.12	19.70	25	6015	8308	63474674
Aortic arteriosclerosis	58.21	19.70	22	6018	6187	63476795
Coronary artery disease	58.16	19.70	37	6003	32340	63450642
Anuria	55.35	19.70	26	6014	12525	63470457
General physical health deterioration	55.25	19.70	81	5959	201321	63281661
Lactic acidosis	54.85	19.70	38	6002	38249	63444733
Hyponatraemia	54.60	19.70	60	5980	111840	63371142
Cardiovascular disorder	53.73	19.70	25	6015	11787	63471195
Urinary retention	52.86	19.70	34	6006	30267	63452715
Mitral valve incompetence	52.52	19.70	29	6011	19565	63463417
Aplastic anaemia	52.23	19.70	23	6017	9546	63473436
Labelled drug-drug interaction medication error	50.73	19.70	25	6015	13374	63469608
Escherichia infection	48.89	19.70	24	6016	12730	63470252
Groin pain	47.67	19.70	22	6018	10181	63472801
Left ventricular dysfunction	47.27	19.70	23	6017	11965	63471017
Postoperative wound infection	46.23	19.70	22	6018	10903	63472079
Hyperkalaemia	45.16	19.70	39	6001	54164	63428818
Pulmonary hypertension	44.35	19.70	33	6007	37090	63445892
Tricuspid valve incompetence	42.96	19.70	23	6017	14598	63468384
Myelodysplastic syndrome	42.72	19.70	24	6016	16730	63466252
Acute kidney injury	40.54	19.70	82	5958	263333	63219649
Hiatus hernia	39.57	19.70	25	6015	21569	63461413
Joint dislocation	37.57	19.70	23	6017	18777	63464205
Haematemesis	36.25	19.70	27	6013	30385	63452597
Cardiogenic shock	35.99	19.70	22	6018	17910	63465072
Bladder trabeculation	35.75	19.70	6	6034	54	63482928
Product monitoring error	35.22	19.70	14	6026	4502	63478480
Haematuria	35.00	19.70	26	6014	29131	63453851
Fracture	34.21	19.70	22	6018	19562	63463420
Osteopenia	34.01	19.70	22	6018	19763	63463219
Therapeutic drug monitoring analysis not performed	33.67	19.70	10	6030	1342	63481640
Multiple sclerosis relapse	27.16	19.70	28	6012	48450	63434532
Dry mouth	26.82	19.70	35	6005	77828	63405154
Oedema peripheral	26.77	19.70	57	5983	189454	63293528
Face oedema	26.47	19.70	19	6021	20193	63462789
Portal fibrosis	26.26	19.70	6	6034	287	63482695
Drug ineffective	25.17	19.70	38	6002	1044727	62438255
Distal intestinal obstruction syndrome	24.14	19.70	6	6034	412	63482570
Spinal pain	23.54	19.70	15	6025	13124	63469858
Gait disturbance	23.48	19.70	53	5987	183125	63299857
Postmortem blood drug level increased	21.95	19.70	6	6034	598	63482384
Upper airway obstruction	21.05	19.70	6	6034	697	63482285
Dementia	20.87	19.70	16	6024	18778	63464204
Product prescribing error	20.05	19.70	18	6022	26271	63456711
Left ventricular failure	19.72	19.70	10	6030	5677	63477305

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	74.17	25.39	71	2870	128198	34825792
Product prescribing error	65.67	25.39	34	2907	22893	34931097
Anticholinergic syndrome	49.56	25.39	13	2928	1256	34952734
Hyperkinesia	45.29	25.39	13	2928	1755	34952235
Arteriosclerotic gangrene	41.73	25.39	7	2934	72	34953918
Bladder spasm	38.79	25.39	10	2931	902	34953088
Freezing phenomenon	38.03	25.39	11	2930	1525	34952465
Mucosal haemorrhage	37.42	25.39	11	2930	1614	34952376
Fall	35.39	25.39	62	2879	202823	34751167
Skin swelling	34.80	25.39	10	2931	1355	34952635
Labelled drug-drug interaction medication error	33.91	25.39	19	2922	14920	34939070
Therapeutic product effect variable	32.95	25.39	11	2930	2445	34951545
Atrioventricular block second degree	31.88	25.39	12	2929	3776	34950214
Confusional state	29.00	25.39	47	2894	144113	34809877
Disorientation	28.36	25.39	23	2918	33165	34920825
Pallor	26.86	25.39	20	2921	25460	34928530
Thrombophlebitis	26.37	25.39	10	2931	3212	34950778

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	120.73	18.49	144	7963	275094	79461187
Pancreatic steatosis	104.04	18.49	24	8083	1121	79735160
Lymphatic fistula	101.24	18.49	22	8085	781	79735500
Femoral hernia incarcerated	100.20	18.49	22	8085	820	79735461
Wound infection pseudomonas	85.86	18.49	22	8085	1599	79734682
Fall	85.04	18.49	166	7941	487463	79248818
Arterial haemorrhage	84.87	18.49	24	8083	2537	79733744
Aortic valve stenosis	83.23	18.49	28	8079	5266	79731015
Labelled drug-drug interaction medication error	79.95	18.49	44	8063	27606	79708675
Seroma	78.24	18.49	22	8085	2278	79734003
Faecaloma	74.96	18.49	32	8075	11532	79724749
Product prescribing error	74.47	18.49	50	8057	44763	79691518
Wound dehiscence	69.82	18.49	26	8081	6569	79729712
Urinary tract infection	66.46	18.49	108	7999	274404	79461877
Urinary retention	66.13	18.49	51	8056	56579	79679702
Tachyarrhythmia	64.86	18.49	25	8082	6937	79729344
Haemarthrosis	61.84	18.49	23	8084	5789	79730492
Diverticulum intestinal	59.73	18.49	25	8082	8580	79727701
Hepatic cyst	57.20	18.49	22	8085	6067	79730214
Hyponatraemia	55.81	18.49	79	8028	177769	79558512
Inflammatory marker increased	54.40	18.49	25	8082	10715	79725566
Eructation	54.03	18.49	25	8082	10884	79725397
Escherichia infection	52.98	18.49	29	8078	17988	79718293
Groin pain	49.71	18.49	25	8082	13055	79723226
Aortic arteriosclerosis	49.09	18.49	22	8085	8896	79727385
Cardiovascular disorder	44.83	18.49	26	8081	17999	79718282
Distal intestinal obstruction syndrome	43.25	18.49	11	8096	776	79735505
Product monitoring error	42.83	18.49	20	8087	8886	79727395
Postoperative wound infection	41.28	18.49	22	8085	12939	79723342
Anuria	41.20	18.49	26	8081	20937	79715344
Hyperkinesia	41.19	18.49	14	8093	2715	79733566
Mitral valve incompetence	40.68	18.49	29	8078	28536	79707745
Arteriosclerotic gangrene	40.23	18.49	7	8100	74	79736207
Dementia	39.72	18.49	27	8080	24632	79711649
Lactic acidosis	39.58	18.49	42	8065	70317	79665964
Gait disturbance	38.89	18.49	73	8034	207433	79528848
Joint dislocation	38.37	18.49	23	8084	16916	79719365
Anticholinergic syndrome	37.36	18.49	14	8093	3597	79732684
Aplastic anaemia	37.19	18.49	23	8084	17882	79718399
Haematuria	36.80	18.49	40	8067	68796	79667485
Hiatus hernia	36.30	18.49	25	8082	23287	79712994
Bladder spasm	35.28	18.49	12	8095	2331	79733950
Tricuspid valve incompetence	35.16	18.49	23	8084	19689	79716592
Bladder trabeculation	34.97	18.49	6	8101	58	79736223
Haematemesis	34.47	18.49	34	8073	52230	79684051
Disorientation	34.47	18.49	37	8070	62739	79673542
Osteopenia	34.16	18.49	22	8085	18342	79717939
Mucosal haemorrhage	34.12	18.49	12	8095	2574	79733707
Freezing phenomenon	33.59	18.49	11	8096	1903	79734378
Left ventricular dysfunction	33.10	18.49	22	8085	19339	79716942
Therapeutic product effect variable	33.06	18.49	11	8096	1998	79734283
Dizziness	32.34	18.49	122	7985	526319	79209962
Coronary artery disease	31.48	18.49	36	8071	65438	79670843
Pallor	30.14	18.49	31	8076	50031	79686250
Therapeutic drug monitoring analysis not performed	29.48	18.49	10	8097	1926	79734355
Confusional state	28.70	18.49	84	8023	317913	79418368
Fracture	28.46	18.49	21	8086	21780	79714501
Myelodysplastic syndrome	28.38	18.49	24	8083	30277	79706004
Atrioventricular block second degree	27.85	18.49	14	8093	7298	79728983
Urogenital haemorrhage	27.21	18.49	8	8099	969	79735312
Dysuria	26.17	18.49	29	8078	50922	79685359
Urinary incontinence	25.84	18.49	26	8081	40883	79695398
Orthostatic intolerance	25.66	18.49	9	8098	1915	79734366
Pyelonephritis	25.19	18.49	19	8088	20369	79715912
Subileus	25.05	18.49	12	8095	5642	79730639
Syncope	24.02	18.49	55	8052	179394	79556887
Hydronephrosis	23.20	18.49	17	8090	17437	79718844
Skin swelling	22.40	18.49	10	8097	4004	79732277
Face oedema	21.77	18.49	20	8087	28116	79708165
Portal fibrosis	21.39	18.49	6	8101	615	79735666
Disturbance in attention	21.22	18.49	26	8081	50775	79685506
Asthenia	20.94	18.49	105	8002	511584	79224697
Pulmonary hypertension	20.72	18.49	25	8082	48055	79688226
Drug ineffective	19.96	18.49	51	8056	1080862	78655419
Postmortem blood drug level increased	19.82	18.49	6	8101	803	79735478
Nocturia	19.73	18.49	14	8093	13667	79722614
Fractured sacrum	19.32	18.49	7	8100	1636	79734645
Pulmonary haematoma	18.77	18.49	4	8103	129	79736152
Pollakiuria	18.75	18.49	21	8086	37296	79698985
Hyperkalaemia	18.67	18.49	38	8069	114360	79621921

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A03DA06	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS ANTISPASMODICS IN COMBINATION WITH ANALGESICS Synthetic anticholinergic agents in combination with analgesics
ATC	G04BD09	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs for urinary frequency and incontinence
FDA MoA	N0000000125	Cholinergic Muscarinic Antagonists
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D018680	Cholinergic Antagonists
MeSH PA	D018727	Muscarinic Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D010276	Parasympatholytics
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D064804	Urological Agents
FDA EPC	N0000175700	Cholinergic Muscarinic Antagonist
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:53784	antispasmodics

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

Disease	Relation	SNOMED_ID	DOID
Urgent desire to urinate	indication	75088002
Urge incontinence of urine	indication	87557004
Bladder muscle dysfunction - overactive	indication	236633002
Increased Urinary Frequency	indication
Constipation	contraindication	14760008	DOID:2089
Atony of colon	contraindication	29479008
Acute nephropathy	contraindication	58574008
Ulcerative colitis	contraindication	64766004	DOID:8577
Myasthenia gravis	contraindication	91637004	DOID:437
Gastrointestinal obstruction	contraindication	126765001
Disease of liver	contraindication	235856003	DOID:409
Bladder outflow obstruction	contraindication	236645006
Retention of urine	contraindication	267064002
Gastric retention	contraindication	307227006
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Gastrointestinal hypomotility	contraindication	421807004

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.67	acidic

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
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	ANTAGONIST	Ki	8.94	CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	ANTAGONIST	Ki	8.99	CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	8.46	CHEMBL
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	8.84	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	8.22	CHEMBL

External reference:

ID	Source
4021473	VUID
N0000148857	NUI
D01103	KEGG_DRUG
4021473	VANDF
C0772089	UMLSCUI
CHEBI:32270	CHEBI
CHEMBL1888176	ChEMBL_ID
DB00209	DRUGBANK_ID
CHEMBL3084748	ChEMBL_ID
C003330	MESH_SUPPLEMENTAL_RECORD_UI
5284632	PUBCHEM_CID
7480	IUPHAR_LIGAND_ID
T4Y8ORK057	UNII
236778	RXNORM
107689	MMSL
17758	MMSL
d04929	MMSL
006793	NDDF
006794	NDDF
326557004	SNOMEDCT_US
359380005	SNOMEDCT_US
412604005	SNOMEDCT_US
3001	INN_ID
47608-32-2	SECONDARY_CAS_RN

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Trospium ChlorideER	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0118	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	29 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0145	TABLET, FILM COATED	20 mg	ORAL	ANDA	30 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3636	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7059	TABLET, FILM COATED	20 mg	ORAL	ANDA	21 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	23155-530	TABLET, FILM COATED	20 mg	ORAL	ANDA	20 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	23155-530	TABLET, FILM COATED	20 mg	ORAL	ANDA	20 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	23155-530	TABLET, FILM COATED	20 mg	ORAL	ANDA	20 sections
TROSPIUM CHLORIDE ER	HUMAN PRESCRIPTION DRUG LABEL	1	35573-446	CAPSULE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE ER	HUMAN PRESCRIPTION DRUG LABEL	1	35573-446	CAPSULE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	50090-5994	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	22 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	60429-098	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	62135-742	TABLET, FILM COATED	20 mg	ORAL	ANDA	19 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8457	TABLET, FILM COATED	20 mg	ORAL	ANDA	29 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8457	TABLET, FILM COATED	20 mg	ORAL	ANDA	29 sections
Trospium ChlorideER	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8458	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	28 sections
Trospium ChlorideER	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8458	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	28 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	63629-9279	TABLET, FILM COATED	20 mg	ORAL	ANDA	29 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	68001-427	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	68462-461	TABLET, FILM COATED	20 mg	ORAL	ANDA	29 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	68462-461	TABLET, FILM COATED	20 mg	ORAL	ANDA	29 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	69097-912	TABLET, FILM COATED	20 mg	ORAL	ANDA	28 sections
Trospium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	69150-258	TABLET	20 mg	ORAL	ANDA	28 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	70010-027	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	70010-027	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	70436-174	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	22 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	70436-174	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	22 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	70436-174	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	22 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	71205-917	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	71205-917	CAPSULE, EXTENDED RELEASE	60 mg	ORAL	ANDA	26 sections
TROSPIUM CHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	72789-348	TABLET, FILM COATED	20 mg	ORAL	ANDA	30 sections