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

Stem definition	Drug id	CAS RN
	2705	124937-51-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tolterodine tolterodine tartrate (+)-Tolterodine (R)-Tolterodine	An ANTIMUSCARINIC AGENT selective for the MUSCARINIC RECEPTORS of the BLADDER that is used in the treatment of URINARY INCONTINENCE and URINARY URGE INCONTINENCE. Molecular weight: 325.50 Formula: C22H31NO CLOGP: 5.24 LIPINSKI: 1 HAC: 2 HDO: 1 TPSA: 23.47 ALOGS: -4.78 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tolterodine
tolterodine tartrate
(+)-Tolterodine
(R)-Tolterodine

An ANTIMUSCARINIC AGENT selective for the MUSCARINIC RECEPTORS of the BLADDER that is used in the treatment of URINARY INCONTINENCE and URINARY URGE INCONTINENCE.

Molecular weight: 325.50
Formula: C22H31NO
CLOGP: 5.24
LIPINSKI: 1
HAC: 2
HDO: 1
TPSA: 23.47
ALOGS: -4.78
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
4	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	24.58 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	2.40 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	12 mg/mL	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.50 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.04 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
March 25, 1998	FDA	PHARMACIA AND UPJOHN

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
Urinary tract infection	116.47	12.17	287	23681	264397	63200657
Sensitivity to weather change	101.05	12.17	51	23917	7186	63457868
Multiple sclerosis	91.66	12.17	75	23893	24297	63440757
Fall	87.26	12.17	335	23633	391999	63073055
Multiple sclerosis relapse	84.88	12.17	98	23870	48380	63416674
Urinary incontinence	83.38	12.17	80	23888	31934	63433120
Dry mouth	72.79	12.17	116	23852	77747	63387307
Systemic lupus erythematosus	66.18	12.17	3	23965	208915	63256139
Maternal exposure during pregnancy	64.15	12.17	5	23963	220057	63244997
Contraindicated product administered	60.59	12.17	6	23962	217642	63247412

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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
Seronegative arthritis	66.27	15.11	19	7262	1020	34948630
Lipoma	56.77	15.11	19	7262	1707	34947943
Fall	55.51	15.11	127	7154	202758	34746892
Dry mouth	48.02	15.11	44	7237	30121	34919529
Urinary incontinence	45.52	15.11	35	7246	18839	34930811
Prostatic specific antigen increased	43.92	15.11	31	7250	14649	34935001
Urinary retention	41.16	15.11	44	7237	36244	34913406
Balance disorder	38.73	15.11	45	7236	40609	34909041
Pollakiuria	37.92	15.11	32	7249	19642	34930008
Inflammatory marker increased	37.14	15.11	19	7262	5009	34944641

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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
Multiple sclerosis	108.17	11.73	73	23896	22209	79698210
Urinary tract infection	104.71	11.73	245	23724	274267	79446152
Fall	100.34	11.73	348	23621	487281	79233138
Sensitivity to weather change	91.95	11.73	46	23923	8001	79712418
Urinary incontinence	80.34	11.73	79	23890	40830	79679589
Multiple sclerosis relapse	73.59	11.73	80	23889	46453	79673966
Pollakiuria	55.28	11.73	62	23907	37255	79683164
Cerebrovascular accident	51.01	11.73	131	23838	155161	79565258
Lipoma	48.78	11.73	22	23947	3037	79717382
Off label use	46.81	11.73	130	23839	907085	78813334

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G04BD07	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs for urinary frequency and incontinence
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:51371	muscle relaxants
CHEBI has role	CHEBI:53784	antispasmodics
FDA EPC	N0000175700	Cholinergic Muscarinic Antagonist
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

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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
Urgent desire to urinate	indication	75088002
Urge incontinence of urine	indication	87557004
Bladder muscle dysfunction - overactive	indication	236633002
Increased Urinary Frequency	indication
Torsades de pointes	contraindication	31722008
Dementia	contraindication	52448006
Acute nephropathy	contraindication	58574008
Hepatic failure	contraindication	59927004
Myasthenia gravis	contraindication	91637004	DOID:437
Prolonged QT interval	contraindication	111975006

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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	9.83	acidic
pKa2	9.14	Basic

Orange Book patent data (new drug applications)

None

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	8.49	CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	ANTAGONIST	Ki	8.57	CHEMBL	CHEMBL
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	8.51	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	8.66	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	7.77	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	8.85	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR		ACM2_RAT		Ki	8.16	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR		ACM1_RAT		Ki	8.85	CHEMBL
Muscarinic acetylcholine receptor M3	GPCR		ACM3_RAT		Ki	8.15	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR		ACM5_RAT		Ki	8.66	CHEMBL

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External reference:

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ID	Source
007444	NDDF
007445	NDDF
109113000	SNOMEDCT_US
119565	RXNORM
124937-52-6	SECONDARY_CAS_RN
191519	MMSL
360	IUPHAR_LIGAND_ID
372570008	SNOMEDCT_US
386971005	SNOMEDCT_US
4021103	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Detrol	HUMAN PRESCRIPTION DRUG LABEL	1	0009-4541	TABLET, FILM COATED	1 mg	ORAL	NDA	25 sections
Detrol	HUMAN PRESCRIPTION DRUG LABEL	1	0009-4544	TABLET, FILM COATED	2 mg	ORAL	NDA	25 sections
Detrol LA	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5190	CAPSULE, EXTENDED RELEASE	2 mg	ORAL	NDA	29 sections
Detrol LA	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5190	CAPSULE, EXTENDED RELEASE	2 mg	ORAL	NDA	29 sections
Detrol LA	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5191	CAPSULE, EXTENDED RELEASE	4 mg	ORAL	NDA	29 sections
Detrol LA	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5191	CAPSULE, EXTENDED RELEASE	4 mg	ORAL	NDA	29 sections
Tolterodine Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0010	TABLET, FILM COATED	1 mg	ORAL	ANDA	25 sections
Tolterodine Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0010	TABLET, FILM COATED	1 mg	ORAL	ANDA	25 sections
Tolterodine Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0018	TABLET, FILM COATED	2 mg	ORAL	ANDA	25 sections
Tolterodine Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0018	TABLET, FILM COATED	2 mg	ORAL	ANDA	25 sections

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