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

Stem definitionDrug idCAS RN
2705 124937-51-5

Description:

MoleculeDescription

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:

DoseUnitRoute
4 mg O

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
March 25, 1998 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug ineffective 374.64 28.68 156 826 101468 2255635
Dry mouth 365.61 28.68 86 896 8167 2348936
Drug hypersensitivity 319.01 28.68 113 869 46530 2310573
Urinary incontinence 149.88 28.68 37 945 4196 2352907
Urinary retention 144.80 28.68 35 947 3632 2353471
Pollakiuria 143.97 28.68 35 947 3721 2353382
Constipation 111.56 28.68 43 939 21586 2335517
Nocturia 99.65 28.68 20 962 870 2356233
Urinary tract infection 91.56 28.68 41 941 29901 2327202
Fall 90.92 28.68 47 935 47052 2310051
Hypertonic bladder 82.59 28.68 15 967 379 2356724
Drug interaction 73.64 28.68 35 947 29128 2327975
Condition aggravated 67.60 28.68 34 948 31945 2325158
Dizziness 65.56 28.68 41 941 58624 2298479
Hallucination, auditory 61.78 28.68 16 966 2176 2354927
Confusional state 60.73 28.68 29 953 24315 2332788
Oesophagitis 58.27 28.68 15 967 1991 2355112
Paranoia 57.54 28.68 15 967 2092 2355011
Dry eye 52.43 28.68 16 966 3940 2353163
Blood cholesterol increased 52.02 28.68 17 965 5224 2351879
Haemoglobin abnormal 50.91 28.68 11 971 684 2356419
Neutrophil count abnormal 49.73 28.68 10 972 437 2356666
Hypertension 48.84 28.68 26 956 27335 2329768
Incontinence 47.77 28.68 12 970 1442 2355661
Bladder disorder 45.68 28.68 11 971 1110 2355993
White blood cell count abnormal 45.05 28.68 10 972 705 2356398
Vision blurred 44.38 28.68 20 962 14648 2342455
Pain in extremity 43.07 28.68 28 954 42512 2314591
Therapeutic product effect decreased 40.06 28.68 17 965 10772 2346331
Macular degeneration 39.71 28.68 10 972 1213 2355890
Depressed level of consciousness 38.60 28.68 15 967 7589 2349514
Arthritis 37.98 28.68 16 966 9952 2347151
Abdominal pain upper 36.60 28.68 20 962 22080 2335023
Gastrooesophageal reflux disease 36.00 28.68 15 967 9080 2348023
Micturition urgency 34.55 28.68 9 973 1247 2355856
Dysphagia 34.14 28.68 16 966 12789 2344314
Psychotic disorder 33.93 28.68 12 970 4667 2352436
Insomnia 33.72 28.68 20 962 25767 2331336
Vulvovaginal dryness 32.47 28.68 7 975 430 2356673
Headache 31.17 28.68 30 952 80149 2276954
Weight decreased 29.46 28.68 19 963 28352 2328751

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug ineffective 106.48 35.81 48 300 63753 1682680
Urinary retention 104.24 35.81 26 322 5369 1741064
Dry mouth 101.91 35.81 24 324 3889 1742544
Nocturia 56.98 35.81 12 336 1149 1745284
Pollakiuria 55.69 35.81 14 334 2932 1743501
Urinary incontinence 41.88 35.81 11 337 2725 1743708
Dysuria 38.68 35.81 11 337 3661 1742772

Pharmacologic Action:

SourceCodeDescription
ATC G04BD07 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist
FDA MoA N0000000125 Cholinergic Muscarinic Antagonists
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:53784 antispasmodic drug
CHEBI has role CHEBI:51371 muscle relaxant
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D064804 Urological Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
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
Bladder outflow obstruction contraindication 236645006
Pyloric obstruction contraindication 244815007
Retention of urine contraindication 267064002
Gastric retention contraindication 307227006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Gastrointestinal hypomotility contraindication 421807004
Poor metabolizer due to cytochrome p450 CYP2D6 variant contraindication 423629005
Congenital long QT syndrome contraindication 442917000
Aggravated Glaucoma contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 8.49 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST Ki 8.57 CHEMBL CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7.77 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 8.51 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 8.66 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8.85 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 8.15 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 8.16 CHEMBL

External reference:

IDSource
D000068737 MESH_DESCRIPTOR_UI
4024113 VUID
N0000022118 NUI
C0388753 UMLSCUI
D00646 KEGG_DRUG
5T619TQR3R UNII
124937-52-6 SECONDARY_CAS_RN
109113000 SNOMEDCT_US
4024113 VANDF
007444 NDDF
d04294 MMSL
119565 RXNORM
372570008 SNOMEDCT_US
CHEMBL1382 ChEMBL_ID
DB01036 DRUGBANK_ID
CHEBI:9622 CHEBI
6768 INN_ID
443879 PUBCHEM_CID
CHEMBL1722209 ChEMBL_ID
360 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Detrol HUMAN PRESCRIPTION DRUG LABEL 1 0009-4541 TABLET, FILM COATED 1 mg ORAL NDA 14 sections
Detrol HUMAN PRESCRIPTION DRUG LABEL 1 0009-4544 TABLET, FILM COATED 2 mg ORAL NDA 14 sections
Detrol LA HUMAN PRESCRIPTION DRUG LABEL 1 0009-5190 CAPSULE, EXTENDED RELEASE 2 mg ORAL NDA 18 sections
Detrol LA HUMAN PRESCRIPTION DRUG LABEL 1 0009-5191 CAPSULE, EXTENDED RELEASE 4 mg ORAL NDA 18 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-0010 TABLET, FILM COATED 1 mg ORAL ANDA 13 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-0018 TABLET, FILM COATED 2 mg ORAL ANDA 13 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7163 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7164 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-3402 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-3404 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 17 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6592 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 16 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6593 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 16 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-189 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 16 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-190 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 16 sections
DETROL HUMAN PRESCRIPTION DRUG LABEL 1 16590-959 TABLET, FILM COATED 2 mg ORAL NDA 13 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 31722-607 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 31722-608 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 17 sections
Tolterodine tartrate HUMAN PRESCRIPTION DRUG LABEL 1 33342-097 TABLET, FILM COATED 1 mg ORAL ANDA 13 sections
Tolterodine tartrate HUMAN PRESCRIPTION DRUG LABEL 1 33342-098 TABLET, FILM COATED 2 mg ORAL ANDA 13 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 43353-346 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 19 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 43975-322 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 43975-323 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-3475 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 17 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 51079-197 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 18 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 51079-198 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 18 sections
Detrol LA HUMAN PRESCRIPTION DRUG LABEL 1 54868-4514 CAPSULE, EXTENDED RELEASE 4 mg ORAL NDA 17 sections
Detrol LA HUMAN PRESCRIPTION DRUG LABEL 1 54868-5126 CAPSULE, EXTENDED RELEASE 2 mg ORAL NDA 17 sections
Detrol LA HUMAN PRESCRIPTION DRUG LABEL 1 55289-132 CAPSULE, EXTENDED RELEASE 4 mg ORAL NDA 18 sections
Tolterodine Tartrate Extended Release HUMAN PRESCRIPTION DRUG LABEL 1 59762-0047 CAPSULE, EXTENDED RELEASE 2 mg ORAL NDA 18 sections
Tolterodine Tartrate Extended Release HUMAN PRESCRIPTION DRUG LABEL 1 59762-0048 CAPSULE, EXTENDED RELEASE 4 mg ORAL NDA 18 sections