Identification

Name
Trospium
Accession Number
DB00209  (APRD00393)
Type
Small Molecule
Groups
Approved
Description

Trospium is a urinary antispasmodic. It is sold under the brand name Sanctura in the US, and as Trosec in Canada. [Wikipedia]

Structure
Thumb
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Trospium chloride1E6682427E10405-02-4RVCSYOQWLPPAOA-QKYUOBHYSA-M
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Sanctura XRCapsule, extended release60 mgOralAllergan2010-01-202016-04-13Canada
TrosecTablet20 mgOralSunovion2006-04-04Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Trospium ChlorideTablet, film coated20 mg/1OralExelan Pharmaceuticals, Inc.2017-07-11Not applicableUs
Trospium ChlorideCapsule, extended release60 mg/1OralActavis Pharma Company2012-10-12Not applicableUs00591 3636 30 nlmimage10 9241c94e
Trospium ChlorideTablet, film coated20 mg/1OralGlenmark Pharmaceuticals Inc.,Usa2010-08-13Not applicableUs68462 0461 60 nlmimage10 b73d5b9a
Trospium ChlorideTablet, film coated20 mg/1OralPaddock Laboratories, Inc.2010-11-17Not applicableUs
Trospium ChlorideTablet20 mg/1OralAv Kare, Inc.2016-10-06Not applicableUs
Trospium ChlorideTablet20 mg/1OralGolden State Medical Supply2013-02-08Not applicableUs60505 3454 06 nlmimage10 714338c9
Trospium ChlorideTablet20 mg/1OralApotex Corporation2012-10-15Not applicableUs
Trospium ChlorideTablet20 mg/1OralBiomes Pharmaceuticals2010-08-13Not applicableUs
Trospium ChlorideTablet20 mg/1OralAmerincan Health Packaging2014-12-152015-12-29Us
Trospium ChlorideTablet, film coated20 mg/1OralCipla Limited2016-09-23Not applicableUs
International/Other Brands
Flotros / Regurin / Spasmex / Spasmolyt / Spasmoplex / Tropez OD
Categories
UNII
T4Y8ORK057
CAS number
47608-32-2
Weight
Average: 392.518
Monoisotopic: 392.22202025
Chemical Formula
C25H30NO3
InChI Key
OYYDSUSKLWTMMQ-JKHIJQBDSA-N
InChI
InChI=1S/C25H30NO3/c27-24(25(28,19-9-3-1-4-10-19)20-11-5-2-6-12-20)29-23-17-21-13-14-22(18-23)26(21)15-7-8-16-26/h1-6,9-12,21-23,28H,7-8,13-18H2/q+1/t21-,22+,23+
IUPAC Name
(1S,3R,5R)-3-[(2-hydroxy-2,2-diphenylacetyl)oxy]-8λ⁵-azaspiro[bicyclo[3.2.1]octane-8,1'-pyrrolidin]-8-ylium
SMILES
[H][[email protected]]12CC[[email protected]]([H])(C[[email protected]@H](C1)OC(=O)C(O)(C1=CC=CC=C1)C1=CC=CC=C1)[N+]21CCCC1

Pharmacology

Indication

For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency, detrusor instability and frequency of micturition.

Structured Indications
Pharmacodynamics

Trospium is an antispasmodic, antimuscarinic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Receptor assays showed that trospium has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses.

Mechanism of action

Trospium antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder.

TargetActionsOrganism
UMuscarinic acetylcholine receptor M1
antagonist
Human
Absorption

9.6%

Volume of distribution
  • 395 ± 140 L
Protein binding

50-85%

Metabolism

Not fully defined

Route of elimination

After administration of oral 14C-trospium chloride, the majority of the dose (85.2%) was recovered in feces and a smaller amount (5.8% of the dose) was recovered in urine; 60% of the radioactivity excreted in urine was unchanged trospium. The mean renal clearance for trospium (29.07 L/hour) is 4-fold higher than average glomerular filtration rate, indicating that active tubular secretion is a major route of elimination for trospium. SANCTURA ® is metabolized by ester hydrolysis and excreted by the kidneys by a combination of tubular secretion and glomerular filtration.

Half life

20 hours

Clearance
  • Renal cl=29.07 L/hour
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Trospium can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AclidiniumAclidinium may increase the anticholinergic activities of Trospium.Approved
AlcuroniumThe risk or severity of adverse effects can be increased when Trospium is combined with Alcuronium.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Trospium is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Trospium is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Trospium is combined with Alphaprodine.Illicit
AmbenoniumThe therapeutic efficacy of Trospium can be decreased when used in combination with Ambenonium.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Trospium is combined with Anisotropine Methylbromide.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Trospium is combined with Atracurium.Experimental, Investigational
Atracurium besylateThe risk or severity of adverse effects can be increased when Trospium is combined with Atracurium besylate.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Trospium.Approved, Vet Approved
BenactyzineThe risk or severity of adverse effects can be increased when Trospium is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Trospium.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Trospium.Approved
BezitramideThe risk or severity of adverse effects can be increased when Trospium is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Trospium.Approved, Investigational
BornaprineThe risk or severity of adverse effects can be increased when Bornaprine is combined with Trospium.Experimental
Botulinum Toxin Type ATrospium may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BTrospium may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Trospium is combined with Butorphanol.Approved, Illicit, Vet Approved
CarfentanilThe risk or severity of adverse effects can be increased when Trospium is combined with Carfentanil.Illicit, Investigational, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Trospium.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Trospium is combined with Chlorphenoxamine.Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Trospium.Approved
CimetropiumTrospium may increase the anticholinergic activities of Cimetropium.Experimental, Investigational
CodeineThe risk or severity of adverse effects can be increased when Trospium is combined with Codeine.Approved, Illicit
CoumaphosThe therapeutic efficacy of Trospium can be decreased when used in combination with Coumaphos.Vet Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Trospium.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Trospium.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Trospium is combined with Darifenacin.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Trospium can be decreased when used in combination with Decamethonium.Approved
DemecariumThe therapeutic efficacy of Trospium can be decreased when used in combination with Demecarium.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Trospium is combined with Desloratadine.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Trospium.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Trospium is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Trospium is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Trospium is combined with Dezocine.Approved, Investigational
DichlorvosThe therapeutic efficacy of Trospium can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Trospium.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Trospium is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Dihydromorphine.Experimental, Illicit
DiphenoxylateThe risk or severity of adverse effects can be increased when Trospium is combined with Diphenoxylate.Approved, Illicit
DistigmineThe therapeutic efficacy of Trospium can be decreased when used in combination with Distigmine.Experimental
DonepezilThe therapeutic efficacy of Trospium can be decreased when used in combination with Donepezil.Approved
DPDPEThe risk or severity of adverse effects can be increased when Trospium is combined with DPDPE.Investigational
DronabinolTrospium may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Trospium can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Trospium can be decreased when used in combination with Edrophonium.Approved
EluxadolineTrospium may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Trospium is combined with Emepronium.Experimental
EtanautineThe risk or severity of adverse effects can be increased when Trospium is combined with Etanautine.Experimental
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Trospium.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Trospium.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Etorphine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Trospium is combined with Etybenzatropine.Experimental
FentanylThe risk or severity of adverse effects can be increased when Trospium is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Trospium can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Trospium.Approved
GalantamineThe therapeutic efficacy of Trospium can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Trospium is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Trospium is combined with Gallamine Triethiodide.Approved
Glucagon recombinantThe risk or severity of adverse effects can be increased when Trospium is combined with Glucagon recombinant.Approved
GlycopyrroniumTrospium may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Trospium is combined with Heroin.Approved, Illicit, Investigational
HexamethoniumThe risk or severity of adverse effects can be increased when Trospium is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Trospium is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Trospium can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Trospium.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Trospium is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Trospium.Approved, Investigational
HydromorphoneThe risk or severity of adverse effects can be increased when Trospium is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Trospium is combined with Hyoscyamine.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Trospium.Approved
IpidacrineThe therapeutic efficacy of Trospium can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Trospium.Approved
IsoflurophateThe therapeutic efficacy of Trospium can be decreased when used in combination with Isoflurophate.Approved, Investigational, Withdrawn
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Trospium.Investigational
KetobemidoneThe risk or severity of adverse effects can be increased when Trospium is combined with Ketobemidone.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Trospium is combined with Levomethadyl Acetate.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Trospium is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Trospium is combined with Lofentanil.Illicit
MalathionThe therapeutic efficacy of Trospium can be decreased when used in combination with Malathion.Approved, Investigational
MazaticolThe risk or severity of adverse effects can be increased when Trospium is combined with Mazaticol.Experimental
MecamylamineThe risk or severity of adverse effects can be increased when Trospium is combined with Mecamylamine.Approved
MefloquineThe therapeutic efficacy of Trospium can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Trospium can be decreased when used in combination with Memantine.Approved, Investigational
MeptazinolThe risk or severity of adverse effects can be increased when Trospium is combined with Meptazinol.Experimental
MetforminThe serum concentration of Trospium can be decreased when it is combined with Metformin.Approved
MethadoneThe risk or severity of adverse effects can be increased when Trospium is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Trospium is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Trospium can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Trospium is combined with Methantheline.Approved, Investigational
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Trospium.Approved
Methylscopolamine bromideThe risk or severity of adverse effects can be increased when Trospium is combined with Methylscopolamine bromide.Approved
MetixeneThe risk or severity of adverse effects can be increased when Trospium is combined with Metixene.Approved
MetoclopramideThe therapeutic efficacy of Trospium can be decreased when used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Trospium.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Trospium.Approved, Investigational
MianserinMianserin may increase the anticholinergic activities of Trospium.Approved, Investigational
MinaprineThe therapeutic efficacy of Trospium can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Trospium is combined with Mirabegron.Approved
MorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Morphine.Approved, Investigational
NabiloneTrospium may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Trospium is combined with Nalbuphine.Approved
NeostigmineThe therapeutic efficacy of Trospium can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NicomorphineThe risk or severity of adverse effects can be increased when Trospium is combined with Nicomorphine.Experimental
NormethadoneThe risk or severity of adverse effects can be increased when Trospium is combined with Normethadone.Approved, Illicit
OpiumThe risk or severity of adverse effects can be increased when Trospium is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Trospium is combined with Orphenadrine.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Trospium is combined with Otilonium.Experimental, Investigational
OxitropiumThe risk or severity of adverse effects can be increased when Trospium is combined with Oxitropium.Investigational
OxybutyninThe risk or severity of adverse effects can be increased when Trospium is combined with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Trospium is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Trospium is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Trospium is combined with Oxyphenonium.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Trospium is combined with Pancuronium.Approved
ParaoxonThe therapeutic efficacy of Trospium can be decreased when used in combination with Paraoxon.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Trospium is combined with Pentazocine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Trospium is combined with Pentolinium.Approved
PethidineThe risk or severity of adverse effects can be increased when Trospium is combined with Pethidine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Trospium is combined with Phenazocine.Experimental
PhenglutarimideThe risk or severity of adverse effects can be increased when Phenglutarimide is combined with Trospium.Experimental
PhenoperidineThe risk or severity of adverse effects can be increased when Trospium is combined with Phenoperidine.Experimental
PhysostigmineThe therapeutic efficacy of Trospium can be decreased when used in combination with Physostigmine.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Trospium is combined with Pipecuronium.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Trospium is combined with Pirenzepine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Trospium is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Trospium.Approved
Potassium ChlorideTrospium may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Trospium.Approved, Investigational
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Trospium.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Trospium.Approved
PropiverineThe risk or severity of adverse effects can be increased when Trospium is combined with Propiverine.Approved, Investigational
PyridostigmineThe therapeutic efficacy of Trospium can be decreased when used in combination with Pyridostigmine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Trospium.Approved
QuinidineThe risk or severity of adverse effects can be increased when Trospium is combined with Quinidine.Approved
RamosetronTrospium may increase the constipating activities of Ramosetron.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Trospium is combined with Remifentanil.Approved
RivastigmineThe therapeutic efficacy of Trospium can be decreased when used in combination with Rivastigmine.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Trospium.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Trospium is combined with Scopolamine butylbromide.Approved, Vet Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Trospium.Approved, Investigational
SolifenacinThe risk or severity of adverse effects can be increased when Trospium is combined with Solifenacin.Approved
SufentanilThe risk or severity of adverse effects can be increased when Trospium is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Trospium.Approved, Investigational
TacrineThe therapeutic efficacy of Trospium can be decreased when used in combination with Tacrine.Investigational, Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Trospium is combined with Tapentadol.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Trospium.Approved, Withdrawn
TilidineThe risk or severity of adverse effects can be increased when Trospium is combined with Tilidine.Experimental
TiotropiumTrospium may increase the anticholinergic activities of Tiotropium.Approved
TolterodineThe risk or severity of adverse effects can be increased when Trospium is combined with Tolterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Trospium is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Trospium is combined with Tramadol.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Trospium can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Trospium.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Trospium.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trospium is combined with Trimethaphan.Approved, Investigational
TropatepineThe risk or severity of adverse effects can be increased when Trospium is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Trospium.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Trospium is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Trospium.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Trospium is combined with Vecuronium.Approved
Food Interactions
Not Available

References

General References
Not Available
External Links
KEGG Drug
D01103
PubChem Compound
5284632
PubChem Substance
46506398
ChemSpider
10482307
ChEBI
32270
ChEMBL
CHEMBL1888176
Therapeutic Targets Database
DAP000342
PharmGKB
PA164748976
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Trospium
ATC Codes
A03DA06 — Trospium and analgesicsG04BD09 — Trospium
AHFS Codes
  • 86:12.04 — Antimuscarinics
FDA label
Download (249 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentSchizophrenic Disorders1
3CompletedTreatmentOveractive Bladder / Urge Urinary Incontinence1
4CompletedBasic ScienceCognitive Function / Mental Competency / Urinary Bladder, Overactive1
4CompletedTreatmentBMI >30 kg/m2 / Incontinence / Overactive Bladder1
4CompletedTreatmentElderly / Overactive Bladder / Pharmacokinetics1
4CompletedTreatmentNeurogenic Detrusor Overactivity / Spinal Cord Injuries (SCI)1
4CompletedTreatmentOveractive Bladder2
Not AvailableCompletedNot AvailableOveractive Bladder / Urinary Bladder Diseases / Urinary Bladder Overactive / Urologic Diseases1
Not AvailableUnknown StatusNot AvailableOveractive Bladder1

Pharmacoeconomics

Manufacturers
  • Allergan inc
Packagers
Dosage forms
FormRouteStrength
Capsule, extended releaseOral60 mg
TabletOral20 mg
TabletOral20 mg/1
Tablet, film coatedOral20 mg/1
Capsule, extended releaseOral60 mg/1
Prices
Unit descriptionCostUnit
Sanctura XR 60 mg 24 Hour Capsule5.17USD capsule
Sanctura xr 60 mg capsule5.02USD capsule
Sanctura 20 mg tablet3.12USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2537103No2010-01-192024-11-04Canada
US7759359No2004-11-042024-11-04Us
US7763635No2004-11-042024-11-04Us
US7781448No2004-11-042024-11-04Us
US7781449No2004-11-042024-11-04Us
US7410978No2005-02-012025-02-01Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility6.68e-05 mg/mLALOGPS
logP2.86ALOGPS
logP-0.5ChemAxon
logS-6.8ALOGPS
pKa (Strongest Acidic)11.05ChemAxon
pKa (Strongest Basic)-4.5ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area46.53 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity124.04 m3·mol-1ChemAxon
Polarizability43.25 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9469
Blood Brain Barrier+0.9418
Caco-2 permeable+0.6042
P-glycoprotein substrateSubstrate0.6431
P-glycoprotein inhibitor INon-inhibitor0.7783
P-glycoprotein inhibitor IINon-inhibitor0.9759
Renal organic cation transporterInhibitor0.7234
CYP450 2C9 substrateNon-substrate0.818
CYP450 2D6 substrateNon-substrate0.774
CYP450 3A4 substrateSubstrate0.5716
CYP450 1A2 substrateNon-inhibitor0.9005
CYP450 2C9 inhibitorNon-inhibitor0.89
CYP450 2D6 inhibitorNon-inhibitor0.7317
CYP450 2C19 inhibitorNon-inhibitor0.9147
CYP450 3A4 inhibitorNon-inhibitor0.8121
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9567
Ames testNon AMES toxic0.8238
CarcinogenicityNon-carcinogens0.9458
BiodegradationNot ready biodegradable0.8128
Rat acute toxicity2.8407 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9135
hERG inhibition (predictor II)Non-inhibitor0.6933
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Piperidines / N-alkylpyrrolidines / Tetraalkylammonium salts / Tertiary alcohols / Carboxylic acid esters / Monocarboxylic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic salts / Organic oxides
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Substituents
Diphenylmethane / Piperidine / N-alkylpyrrolidine / Pyrrolidine / Quaternary ammonium salt / Tertiary alcohol / Tetraalkylammonium salt / Carboxylic acid ester / Organoheterocyclic compound / Azacycle
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34