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

Stem definition	Drug id	CAS RN
atropine derivatives	2677	186691-13-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tiotropium bromide hydrate tiotropium respimat tiotropium bromide tiotropium bromide monohydrate spiriva tiotropiumbromide	A scopolamine derivative and CHOLINERGIC ANTAGONIST that functions as a BRONCHODILATOR AGENT. It is used in the treatment of CHRONIC OBSTRUCTIVE PULMONARY DISEASE. Molecular weight: 392.51 Formula: C19H22NO4S2 CLOGP: -1.91 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 59.06 ALOGS: -4.44 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tiotropium bromide hydrate
tiotropium
respimat
tiotropium bromide
tiotropium bromide monohydrate
spiriva
tiotropiumbromide

A scopolamine derivative and CHOLINERGIC ANTAGONIST that functions as a BRONCHODILATOR AGENT. It is used in the treatment of CHRONIC OBSTRUCTIVE PULMONARY DISEASE.

Molecular weight: 392.51
Formula: C19H22NO4S2
CLOGP: -1.91
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 59.06
ALOGS: -4.44
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mcg	Inhal.powder
5	mcg	Inhal.solution

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	74 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	32 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	2.50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	12.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.28 %	Lombardo F, Berellini G, Obach RS
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
Jan. 30, 2004	FDA	BOEHRINGER INGELHEIM

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
Incorrect route of product administration	6957.90	11.69	2455	124239	24997	63337331
Asthma	3325.81	11.69	2430	124264	125131	63237197
Dyspnoea	1950.79	11.69	4145	122549	657168	62705160
Wheezing	1880.59	11.69	1543	125151	94052	63268276
Obstructive airways disorder	1540.63	11.69	775	125919	19924	63342404
Chronic obstructive pulmonary disease	1234.03	11.69	1013	125681	61673	63300655
Sleep disorder due to a general medical condition	979.69	11.69	481	126213	11707	63350621
Full blood count abnormal	935.65	11.69	653	126041	31064	63331264
Productive cough	915.27	11.69	858	125836	62350	63299978
Cough	891.79	11.69	1866	124828	290877	63071451

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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
Incorrect route of product administration	2981.69	11.25	1193	86964	13652	34855122
Asthma	2661.74	11.25	1534	86623	41122	34827652
Wheezing	1794.87	11.25	1181	86976	40221	34828553
Dyspnoea	1522.15	11.25	3083	85074	373699	34495075
Obstructive airways disorder	1165.41	11.25	631	87526	14863	34853911
Chronic obstructive pulmonary disease	1077.74	11.25	931	87226	47987	34820787
Full blood count abnormal	955.53	11.25	592	87565	18076	34850698
Sleep disorder due to a general medical condition	766.20	11.25	336	87821	4885	34863889
Productive cough	706.25	11.25	656	87501	37157	34831617
Therapeutic product effect incomplete	705.32	11.25	748	87409	49793	34818981

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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
Asthma	4621.32	10.88	3163	173275	131932	79436018
Wheezing	2884.70	10.88	2247	174191	114417	79453533
Dyspnoea	2514.81	10.88	5703	170735	851322	78716628
Obstructive airways disorder	2329.97	10.88	1214	175224	30245	79537705
Incorrect route of product administration	2202.29	10.88	1211	175227	33718	79534232
Chronic obstructive pulmonary disease	1749.38	10.88	1475	174963	83944	79484006
Full blood count abnormal	1649.24	10.88	1059	175379	39415	79528535
Productive cough	1458.27	10.88	1350	175088	86981	79480969
Cough	1319.12	10.88	2660	173778	364129	79203821
Sleep disorder due to a general medical condition	1154.97	10.88	585	175853	13692	79554258

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R03AL06	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03AL10	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03BB04	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Anticholinergics
ATC	R03BB54	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Anticholinergics
CHEBI has role	CHEBI:35523	bronchodilator
CHEBI has role	CHEBI:48876	muscarinic antagonists
FDA EPC	N0000175574	Anticholinergic
FDA MoA	N0000175370	Cholinergic Antagonists
MeSH PA	D018927	Anti-Asthmatic Agents
MeSH PA	D001993	Bronchodilator Agents

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

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Disease	Relation	SNOMED_ID	DOID
Chronic bronchitis	indication	63480004	DOID:6132
Pulmonary emphysema	indication	87433001
Asthma	indication	195967001	DOID:2841
Bronchospasm Prevention with COPD	indication
Chronic Obstructive Pulmonary Disease with Bronchospasms	indication
Impaired renal function disorder	contraindication	197663003
Bladder outflow obstruction	contraindication	236645006
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Angle-closure glaucoma	contraindication	392291006	DOID:13550

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.97	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.0025MG BASE/INH;EQ 0.0025MG BASE/INH	STIOLTO RESPIMAT	BOEHRINGER INGELHEIM	N206756	May 21, 2015	RX	SPRAY, METERED	INHALATION	8044046	Nov. 10, 2023	TREATMENT OF COPD
EQ 0.0025MG BASE/INH;EQ 0.0025MG BASE/INH	STIOLTO RESPIMAT	BOEHRINGER INGELHEIM	N206756	May 21, 2015	RX	SPRAY, METERED	INHALATION	7220742	May 12, 2025	TREATMENT OF RESPIRATORY COMPLAINTS
EQ 0.0025MG BASE/INH;EQ 0.0025MG BASE/INH	STIOLTO RESPIMAT	BOEHRINGER INGELHEIM	N206756	May 21, 2015	RX	SPRAY, METERED	INHALATION	8034809	May 12, 2025	TREATMENT OF COPD
EQ 0.018MG BASE/INH	SPIRIVA	BOEHRINGER INGELHEIM	N021395	Jan. 30, 2004	RX	POWDER	INHALATION	8022082	Jan. 19, 2026	ADMINISTRATION OF AN INHALABLE POWDER COMPRISING TIOTROPIUM VIA DEVICE

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	ANTAGONIST	Ki	11.10	WOMBAT-PK	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	11	WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	11	WOMBAT-PK
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	11	WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	11	WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR		ACM2_RAT		Ki	9.82	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR		ACM1_RAT		Ki	9.80	CHEMBL
Muscarinic acetylcholine receptor M3	GPCR		ACM3_RAT		Ki	9.52	CHEMBL

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External reference:

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ID	Source
0HK	PDB_CHEM_ID
009712	NDDF
009713	NDDF
0EB439235F	UNII
1298831	RXNORM
17045	MMSL
31060	MMSL
367	IUPHAR_LIGAND_ID
4021416	VUID
4021416	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Spiriva	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4414	CAPSULE	18 ug	ORAL	NDA	29 sections
Spiriva	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5109	CAPSULE	18 ug	ORAL	NDA	29 sections
Spiriva HandiHaler	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0075	CAPSULE	18 ug	ORAL	NDA	30 sections
Spiriva HandiHaler	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4248	CAPSULE	18 ug	ORAL	NDA	29 sections
Spiriva HandiHaler	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4248	CAPSULE	18 ug	ORAL	NDA	29 sections
Stiolto Respimat	HUMAN PRESCRIPTION DRUG LABEL	2	0597-0155	SPRAY, METERED	3.12 ug	RESPIRATORY (INHALATION)	NDA	31 sections
Stiolto Respimat	HUMAN PRESCRIPTION DRUG LABEL	2	0597-0155	SPRAY, METERED	3.12 ug	RESPIRATORY (INHALATION)	NDA	31 sections
Tiotropium Bromide	HUMAN PRESCRIPTION DRUG LABEL	1	68180-964	CAPSULE	18 ug	ORAL	ANDA	24 sections

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