tolterodine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/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
BA (Bioavailability) 42 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.029 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.786 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 24.717 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 46.774 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 9.700 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 35.940 % High 1
herg hERG pIC50 6.591 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 42.855 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 130.918 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 13.410 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 50
kinase-selectivity-class AKT3,AXL,BRAF,EIF2AK3,EPHB4,GRK2,PDK4 7
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.635 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.159 High 1
mh-clint Mouse hepatocyte intrinsic clearance 218.273 High 1
mppb Mouse plasma protein binding (% unbound) 33.640 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.762 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 38.200 % High 1
rat-kpuu-brain Rat brain Kpuu 0.489 % High 1
rh-clint Rat hepatocyte intrinsic clearance 311.889 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 63.150 % High 1
rppb Rat plasma protein binding (% unbound) 34.890 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 937.562 uM High 1

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
Urinary tract infection 162.20 11.69 301 25294 305331 90297521
Fall 119.55 11.69 352 25243 481458 90121394
Sensitivity to weather change 105.00 11.69 51 25544 8863 90593989
Multiple sclerosis 104.37 11.69 76 25519 27764 90575088
Multiple sclerosis relapse 104.25 11.69 99 25496 52206 90550646
Urinary incontinence 96.40 11.69 82 25513 37484 90565368
Systemic lupus erythematosus 82.30 11.69 5 25590 361891 90240961
Maternal exposure during pregnancy 78.89 11.69 6 25589 360057 90242795
Synovitis 73.66 11.69 5 25590 329747 90273105
Hand deformity 70.84 11.69 3 25592 296359 90306493
Antinuclear antibody negative 68.71 11.69 16 25579 270 90602582
Coombs positive haemolytic anaemia 64.93 11.69 17 25578 473 90602379
Contraindicated product administered 63.15 11.69 8 25587 320131 90282721
Pollakiuria 62.97 11.69 61 25534 32944 90569908
Off label use 59.20 11.69 141 25454 1102111 89500741
Treatment failure 58.97 11.69 8 25587 303920 90298932
Glossodynia 58.94 11.69 10 25585 321769 90281083
Helicobacter infection 51.96 11.69 3 25592 226847 90376005
Bladder disorder 51.13 11.69 34 25561 10738 90592114
Infusion related reaction 51.11 11.69 27 25568 416753 90186099
Cerebrovascular accident 50.17 11.69 109 25486 123424 90479428
Balance disorder 46.88 11.69 92 25503 96988 90505864
Wound 46.32 11.69 14 25581 302966 90299886
Hypertonic bladder 45.63 11.69 23 25572 4325 90598527
Nocturia 45.40 11.69 31 25564 10224 90592628
Herpes simplex reactivation 44.60 11.69 15 25580 1004 90601848
Exposure during pregnancy 44.56 11.69 7 25588 238403 90364449
Drug intolerance 44.11 11.69 37 25558 447554 90155298
Pericarditis 44.08 11.69 11 25584 270140 90332712
Gastritis haemorrhagic 43.18 11.69 17 25578 1783 90601069
Paranoia 41.17 11.69 32 25563 12876 90589976
Polyp 40.87 11.69 26 25569 7618 90595234
Hepatic enzyme increased 40.48 11.69 26 25569 360710 90242142
Hyperlipidaemia 39.35 11.69 40 25555 22876 90579976
Antiphospholipid syndrome 39.34 11.69 17 25578 2257 90600595
Irritable bowel syndrome 38.97 11.69 6 25589 207442 90395410
Hallucination, auditory 37.19 11.69 33 25562 15942 90586910
Complex regional pain syndrome 36.79 11.69 17 25578 2642 90600210
Psoriatic arthropathy 35.91 11.69 10 25585 228325 90374527
Stress urinary incontinence 34.94 11.69 16 25579 2436 90600416
Coronary artery disease 34.53 11.69 45 25550 33578 90569274
Transient ischaemic attack 34.20 11.69 51 25544 43125 90559727
Abdominal discomfort 33.41 11.69 52 25543 477276 90125576
Haemorrhoids 32.65 11.69 39 25556 26663 90576189
Gastrooesophageal reflux disease 32.37 11.69 112 25483 166225 90436627
Dizziness 32.35 11.69 280 25315 589004 90013848
Anxiety disorder 32.08 11.69 19 25576 4903 90597949
Urinary retention 31.95 11.69 46 25549 37698 90565154
Liver injury 31.88 11.69 5 25590 170562 90432290
Micturition urgency 31.88 11.69 26 25569 11207 90591645
Bladder spasm 31.31 11.69 14 25581 2016 90600836
Dry mouth 30.80 11.69 118 25477 183941 90418911
Stomatitis 30.53 11.69 20 25575 274678 90328174
Cardiac failure congestive 29.16 11.69 77 25518 98617 90504235
Swelling 28.98 11.69 46 25549 419012 90183840
Myocardial infarction 28.64 11.69 80 25515 105892 90496960
Osteonecrosis 28.33 11.69 36 25559 26205 90576647
Secondary progressive multiple sclerosis 27.96 11.69 12 25583 1567 90601285
Depression 27.69 11.69 162 25433 300439 90302413
Dysphagia 27.67 11.69 82 25513 112196 90490656
Hypothyroidism 27.66 11.69 52 25543 53075 90549777
Oesophagitis 27.62 11.69 29 25566 17220 90585632
Mental status changes 27.45 11.69 47 25548 44632 90558220
Peritonitis 26.12 11.69 30 25565 19675 90583177
Inflammation 25.96 11.69 9 25586 178583 90424269
Atrial fibrillation 24.30 11.69 88 25507 133523 90469329
Blister 23.98 11.69 22 25573 254976 90347876
Vision blurred 23.88 11.69 77 25518 110216 90492636
Joint range of motion decreased 23.15 11.69 5 25590 135638 90467214
Tremor 23.05 11.69 95 25500 153078 90449774
Infection 22.96 11.69 42 25553 362052 90240800
Arthropathy 22.76 11.69 43 25552 366199 90236653
Constipation 22.60 11.69 146 25449 280249 90322603
Lower respiratory tract infection 21.98 11.69 23 25572 250636 90352216
Ill-defined disorder 21.17 11.69 13 25582 184878 90417974
Discomfort 21.03 11.69 28 25567 274307 90328545
Back pain 20.77 11.69 157 25438 317018 90285834
Gait disturbance 20.60 11.69 135 25460 260361 90342491
White blood cell count abnormal 20.52 11.69 17 25578 7487 90595365
Incontinence 20.47 11.69 22 25573 13413 90589439
Asthenia 19.78 11.69 234 25361 533517 90069335
Barrett's oesophagus 19.65 11.69 7 25588 556 90602296
Cystitis 19.65 11.69 52 25543 66666 90536186
Skin disorder 19.20 11.69 36 25559 36670 90566182
Biopsy muscle abnormal 18.93 11.69 4 25591 42 90602810
Product complaint 18.65 11.69 21 25574 13479 90589373
Colitis ischaemic 18.43 11.69 20 25575 12326 90590526
Palpitations 18.41 11.69 82 25513 136646 90466206
Somnolence 18.16 11.69 111 25484 208973 90393879
Facet joint syndrome 18.12 11.69 3 25592 98386 90504466
Patient elopement 18.11 11.69 5 25590 171 90602681
Body temperature fluctuation 18.09 11.69 10 25585 2265 90600587
Wound infection 18.00 11.69 4 25591 106398 90496454
Liver iron concentration abnormal 17.74 11.69 4 25591 58 90602794
Urge incontinence 17.51 11.69 8 25587 1211 90601641
Intervertebral disc compression 17.35 11.69 8 25587 1237 90601615
Chronic obstructive pulmonary disease 17.32 11.69 53 25542 73776 90529076
Neutrophil count abnormal 17.15 11.69 12 25583 4116 90598736
Speech disorder 17.11 11.69 39 25556 45546 90557306
Psychotic disorder 16.80 11.69 31 25564 31199 90571653
Aphonia 16.74 11.69 19 25576 12300 90590552
Grip strength decreased 16.66 11.69 3 25592 92573 90510279
Varicose ulceration 16.40 11.69 6 25589 515 90602337
Iliac artery occlusion 16.16 11.69 5 25590 256 90602596
Pain 16.15 11.69 192 25403 996149 89606703
International normalised ratio increased 16.15 11.69 39 25556 47277 90555575
Neurogenic bladder 16 11.69 11 25584 3667 90599185
Erysipelas 15.90 11.69 16 25579 9036 90593816
Disorientation 15.75 11.69 37 25558 44077 90558775
Pleuritic pain 15.71 11.69 17 25578 10444 90592408
Urine albumin/creatinine ratio decreased 15.61 11.69 4 25591 102 90602750
C-reactive protein increased 15.50 11.69 17 25578 181372 90421480
Mixed incontinence 15.46 11.69 4 25591 106 90602746
Sepsis 15.32 11.69 95 25500 179719 90423133
Haematoma 15.32 11.69 34 25561 39014 90563838
Diverticulum 15.31 11.69 18 25577 12095 90590757
Haemoglobin abnormal 15.22 11.69 14 25581 7086 90595766
Blood triglycerides increased 15.04 11.69 19 25576 13742 90589110
Pathological fracture 15.04 11.69 16 25579 9644 90593208
Escherichia urinary tract infection 14.98 11.69 19 25576 13796 90589056
Pulmonary fibrosis 14.64 11.69 6 25589 107497 90495355
Musculoskeletal chest pain 14.61 11.69 25 25570 23725 90579127
Fibula fracture 14.60 11.69 11 25584 4226 90598626
Peripheral venous disease 14.51 11.69 3 25592 83918 90518934
Type 2 diabetes mellitus 14.33 11.69 22 25573 203222 90399630
Impaired healing 14.10 11.69 28 25567 234171 90368681
Increased appetite 14.08 11.69 17 25578 11748 90591104
Syncope 13.86 11.69 74 25521 132589 90470263
Cellulitis 13.22 11.69 56 25539 91281 90511571
Lip dry 13.17 11.69 6 25589 100949 90501903
Abscess jaw 13.14 11.69 7 25588 1474 90601378
Haemoglobin 13.10 11.69 4 25591 196 90602656
Abnormal dreams 13.04 11.69 16 25579 11241 90591611
Malignant neoplasm progression 12.96 11.69 7 25588 106863 90495989
Dysuria 12.94 11.69 32 25563 39369 90563483
Musculoskeletal stiffness 12.80 11.69 42 25553 296490 90306362
Therapeutic product effect incomplete 12.72 11.69 22 25573 193874 90408978
Dysarthria 12.67 11.69 39 25556 54443 90548409
Dementia Alzheimer's type 12.61 11.69 6 25589 995 90601857
Musculoskeletal pain 12.59 11.69 18 25577 171233 90431619
Antineutrophil cytoplasmic antibody increased 12.46 11.69 4 25591 231 90602621
Pulmonary granuloma 12.42 11.69 7 25588 1646 90601206
Red blood cell sedimentation rate increased 12.28 11.69 4 25591 82591 90520261
Drug abuse 12.22 11.69 4 25591 82343 90520509
Fibromyalgia 12.13 11.69 25 25570 206244 90396608
Weight decreased 12.10 11.69 162 25433 379748 90223104
Seizure 11.99 11.69 79 25516 152550 90450302
Dementia 11.98 11.69 23 25572 23838 90579014
Lethargy 11.82 11.69 42 25553 63097 90539755
Drug hypersensitivity 11.75 11.69 190 25405 463419 90139433

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
Seronegative arthritis 107.56 14.81 28 7745 1196 42612366
Lipoma 96.41 14.81 29 7744 2109 42611453
Fall 71.81 14.81 142 7631 234378 42379184
Prostatic specific antigen increased 65.65 14.81 40 7733 16885 42596677
Inflammatory marker increased 60.74 14.81 28 7745 6728 42606834
Musculoskeletal discomfort 54.56 14.81 29 7744 9447 42604115
Urinary incontinence 49.78 14.81 37 7736 21631 42591931
Dry mouth 44.38 14.81 45 7728 39834 42573728
Urinary retention 44.02 14.81 46 7727 42168 42571394
Balance disorder 39.44 14.81 46 7727 47599 42565963
Confusional state 37.99 14.81 90 7683 167507 42446055
Pollakiuria 37.87 14.81 32 7741 22473 42591089
Urinary tract infection 32.54 14.81 62 7711 99222 42514340
Multiple sclerosis 29.56 14.81 18 7755 7580 42605982
Blood pressure systolic increased 28.30 14.81 30 7743 27938 42585624
Micturition urgency 24.41 14.81 19 7754 11879 42601683
Head injury 22.47 14.81 23 7750 20559 42593003
Oesophageal obstruction 22.20 14.81 7 7766 595 42612967
Dizziness 22.15 14.81 97 7676 249157 42364405
Asthenia 21.79 14.81 105 7668 280688 42332874
Cerebrovascular accident 21.78 14.81 52 7721 97108 42516454
Failure to thrive 21.43 14.81 16 7757 9406 42604156
Off label use 20.42 14.81 55 7718 638280 41975282
Cerebral haemorrhage 18.92 14.81 29 7744 38937 42574625
Gait inability 18.80 14.81 22 7751 22811 42590751
Muscular weakness 17.97 14.81 44 7729 83454 42530108
Toxicity to various agents 17.55 14.81 10 7763 229126 42384436
Faecaloma 17.36 14.81 12 7761 6258 42607304
Subarachnoid haemorrhage 17.32 14.81 17 7756 14455 42599107
Incontinence 16.44 14.81 12 7761 6818 42606744
Speech disorder 16.04 14.81 23 7750 29098 42584464
Nocturia 15.95 14.81 15 7758 12097 42601465
Joint swelling 15.88 14.81 37 7736 67985 42545577
Multiple sclerosis relapse 15.68 14.81 16 7757 14248 42599314
Anticholinergic syndrome 15.58 14.81 7 7766 1582 42611980
Psoriasis 15.47 14.81 30 7743 48574 42564988
Orthostatic hypotension 15.19 14.81 23 7750 30547 42583015
Prothrombin time prolonged 14.98 14.81 13 7760 9456 42604106

FDA Adverse Event Reporting System (Geriatric)

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
Urinary tract infection 145.35 11.77 269 25810 326013 110237207
Fall 138.61 11.77 382 25697 603100 109960120
Multiple sclerosis 114.82 11.77 73 26006 25625 110537595
Urinary incontinence 94.90 11.77 84 25995 48503 110514717
Sensitivity to weather change 92.93 11.77 46 26033 9982 110553238
Multiple sclerosis relapse 88.58 11.77 82 25997 50158 110513062
Lipoma 82.09 11.77 32 26047 3923 110559297
Off label use 70.80 11.77 156 25923 1500029 109063191
Cerebrovascular accident 62.00 11.77 134 25945 181150 110382070
Pollakiuria 59.03 11.77 62 26017 44133 110519087
Prostatic specific antigen increased 54.54 11.77 35 26044 12476 110550744
Balance disorder 54.17 11.77 98 25981 116462 110446758
Synovitis 46.91 11.77 5 26074 274087 110289133
Systemic lupus erythematosus 45.21 11.77 4 26075 254334 110308886
Musculoskeletal discomfort 44.57 11.77 40 26039 23498 110539722
Bladder disorder 43.29 11.77 29 26050 11108 110552112
Maternal exposure during pregnancy 42.73 11.77 5 26074 254878 110308342
Urinary retention 42.25 11.77 66 26013 69617 110493603
Dizziness 40.84 11.77 293 25786 697900 109865320
Hand deformity 37.35 11.77 4 26075 218502 110344718
Seronegative arthritis 36.68 11.77 28 26051 13149 110550071
Treatment failure 36.66 11.77 10 26069 277224 110285996
Inflammatory marker increased 36.48 11.77 29 26050 14440 110548780
Contraindicated product administered 34.67 11.77 8 26071 248259 110314961
Micturition urgency 33.01 11.77 31 26048 19289 110543931
Helicobacter infection 31.94 11.77 3 26076 181874 110381346
Hallucination, auditory 31.68 11.77 35 26044 26362 110536858
Haemorrhoids 30.80 11.77 40 26039 35632 110527588
Secondary progressive multiple sclerosis 30.12 11.77 12 26067 1557 110561663
Antinuclear antibody negative 29.91 11.77 7 26072 146 110563074
Asthenia 29.83 11.77 270 25809 688729 109874491
Polyp 29.53 11.77 22 26057 9958 110553262
Incontinence 29.02 11.77 27 26052 16608 110546612
Drug intolerance 28.83 11.77 32 26047 406480 110156740
Vision blurred 28.79 11.77 81 25998 128941 110434279
Confusional state 28.70 11.77 199 25880 468481 110094739
Infusion related reaction 28.15 11.77 29 26050 381133 110182087
Head injury 27.84 11.77 42 26037 42975 110520245
Stress urinary incontinence 27.71 11.77 12 26067 1921 110561299
Back pain 26.65 11.77 164 25915 370832 110192388
Gastrooesophageal reflux disease 26.51 11.77 98 25981 179878 110383342
Dysphagia 26.39 11.77 88 25991 153512 110409708
Exposure during pregnancy 26.35 11.77 4 26075 167420 110395800
Bladder spasm 26.26 11.77 13 26066 2819 110560401
Drug abuse 26.24 11.77 5 26074 177406 110385814
Febrile neutropenia 25.86 11.77 22 26057 316745 110246475
Stomatitis 25.66 11.77 16 26063 270226 110292994
Inflammation 25.48 11.77 7 26072 193231 110369989
Speech disorder 25.14 11.77 49 26030 61520 110501700
Wound 24.99 11.77 12 26067 234425 110328795
Glossodynia 24.22 11.77 11 26068 221993 110341227
Paranoia 24.02 11.77 28 26051 22346 110540874
Blood pressure systolic increased 23.53 11.77 57 26022 82934 110480286
Hypertonic bladder 23.52 11.77 15 26064 5287 110557933
Toxicity to various agents 23.32 11.77 49 26030 480506 110082714
Muscle injury 23.01 11.77 3 26076 140804 110422416
Psoriatic arthropathy 22.67 11.77 9 26070 196752 110366468
Tremor 22.54 11.77 101 25978 202131 110361089
Mental status changes 22.36 11.77 53 26026 76069 110487151
Coronary artery disease 22.24 11.77 51 26028 71639 110491581
Pericarditis 22.18 11.77 12 26067 219102 110344118
Palpitations 22.04 11.77 85 25994 159127 110404093
Swelling 20.42 11.77 32 26047 351009 110212211
Orthostatic hypotension 20.41 11.77 47 26032 66202 110497018
Transient ischaemic attack 20.38 11.77 46 26033 63936 110499284
Body temperature fluctuation 20.11 11.77 12 26067 3761 110559459
Irritable bowel syndrome 19.77 11.77 7 26072 164208 110399012
Nocturia 19.48 11.77 22 26057 16968 110546252
Myocardial infarction 19.24 11.77 93 25986 191990 110371230
Biopsy muscle abnormal 19.01 11.77 4 26075 50 110563170
Dysarthria 18.94 11.77 53 26026 84068 110479152
Hepatic enzyme increased 18.90 11.77 29 26050 320863 110242357
International normalised ratio increased 18.89 11.77 54 26025 86718 110476502
Dysuria 18.85 11.77 43 26036 60188 110503032
Liver iron concentration abnormal 18.46 11.77 4 26075 58 110563162
Disorientation 18.41 11.77 47 26032 70624 110492596
Cystitis 18.34 11.77 45 26034 65991 110497229
Dry mouth 18.05 11.77 94 25985 199854 110363366
Psychotic disorder 17.79 11.77 38 26041 50899 110512321
Hyperlipidaemia 17.75 11.77 31 26048 35817 110527403
Product complaint 17.59 11.77 19 26060 13953 110549267
Syncope 17.45 11.77 94 25985 202442 110360778
Aphonia 17.09 11.77 18 26061 12842 110550378
Colitis ischaemic 17.06 11.77 21 26058 17729 110545491
Ill-defined disorder 16.76 11.77 8 26071 156845 110406375
Barrett's oesophagus 15.83 11.77 6 26073 682 110562538
Musculoskeletal chest pain 15.67 11.77 26 26053 28821 110534399
Patient elopement 15.58 11.77 5 26074 347 110562873
Escherichia urinary tract infection 15.34 11.77 19 26060 16143 110547077
Urine albumin/creatinine ratio decreased 15.14 11.77 4 26075 139 110563081
Intervertebral disc protrusion 15.09 11.77 25 26054 27673 110535547
Depression 15.06 11.77 127 25952 317208 110246012
Joint range of motion decreased 15.00 11.77 5 26074 121827 110441393
Iliac artery occlusion 14.97 11.77 5 26074 393 110562827
Bladder adenocarcinoma stage unspecified 14.87 11.77 3 26076 30 110563190
Intervertebral disc compression 14.72 11.77 7 26072 1390 110561830
Urge incontinence 14.64 11.77 7 26072 1408 110561812
C-reactive protein increased 14.53 11.77 18 26061 217901 110345319
Urosepsis 14.50 11.77 26 26053 30649 110532571
Neutropenia 14.42 11.77 43 26036 374577 110188643
Skin lesion 14.14 11.77 35 26044 51596 110511624
Liver injury 14.14 11.77 9 26070 150404 110412816
Coombs positive haemolytic anaemia 13.92 11.77 7 26072 1570 110561650
Facet joint syndrome 13.75 11.77 3 26076 96825 110466395
Complex regional pain syndrome 13.74 11.77 8 26071 2397 110560823
Wound infection 13.68 11.77 3 26076 96462 110466758
Musculoskeletal pain 13.41 11.77 14 26065 183009 110380211
Internal hernia 13.40 11.77 3 26076 51 110563169
Antiphospholipid syndrome 13.39 11.77 8 26071 2515 110560705
Fibula fracture 13.30 11.77 10 26069 4588 110558632
Drug-induced liver injury 13.01 11.77 6 26073 120061 110443159
Perforation 13.01 11.77 7 26072 1803 110561417
Abscess jaw 12.99 11.77 7 26072 1807 110561413
Diverticulum 12.77 11.77 17 26062 15509 110547711
Abdominal discomfort 12.58 11.77 49 26030 393809 110169411
Anxiety disorder 12.49 11.77 10 26069 5030 110558190
Oesophageal stenosis 12.27 11.77 10 26069 5155 110558065
Mixed incontinence 12.23 11.77 3 26076 77 110563143
Antineutrophil cytoplasmic antibody increased 12.08 11.77 4 26075 306 110562914
Spinal osteoarthritis 12.07 11.77 19 26060 20164 110543056
Blister 12.04 11.77 22 26057 227354 110335866
Gastric ulcer 11.98 11.77 28 26051 39799 110523421
Gait disturbance 11.98 11.77 109 25970 278099 110285121
Emotional distress 11.86 11.77 30 26049 44817 110518403
Multiple organ dysfunction syndrome 11.82 11.77 11 26068 151699 110411521
Electrocardiogram Q waves 11.78 11.77 3 26076 90 110563130

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G04BD07 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
FDA MoA N0000000125 Cholinergic Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D064804 Urological Agents
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35846 renal agent
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:51371 muscle relaxant
CHEBI has role CHEBI:53784 antispasmodic drug

Related Drugs by ATC class:

G04BD Drugs for urinary frequency and incontinence 13 drugs
darifenacinemeproniumfesoterodineflavoxateimidafenacinmeladrazinemirabegronoxybutyninpropiverinesolifenacinterodilinetrospium show all 13 →

Drug Use | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 M2 GPCR ANTAGONIST Ki 8.57 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 8.49 CHEMBL CHEMBL
Histamine H1 receptor GPCR Ki 6.89 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8.85 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 8.51 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 8.66 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.67 CHEMBL
Transmembrane protein 97 Enzyme Ki 6.78 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7.77 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 8.16 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8.85 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 8.15 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 8.66 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 8.51 CHEMBL

External reference:

IDSource
4024113 VUID
N0000022118 NUI
D00646 KEGG_DRUG
124937-52-6 SECONDARY_CAS_RN
4021103 VANDF
4024113 VANDF
C0388753 UMLSCUI
CHEBI:9622 CHEBI
CHEMBL1382 ChEMBL_ID
CHEMBL1722209 ChEMBL_ID
DB01036 DRUGBANK_ID
D000068737 MESH_DESCRIPTOR_UI
443879 PUBCHEM_CID
360 IUPHAR_LIGAND_ID
6768 INN_ID
WHE7A56U7K UNII
119565 RXNORM
191519 MMSL
5600 MMSL
d04294 MMSL
007444 NDDF
007445 NDDF
109113000 SNOMEDCT_US
372570008 SNOMEDCT_US
386971005 SNOMEDCT_US
WHE7A56U7K INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 0093-7163 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 26 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7164 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6592 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 21 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6593 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 21 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7574 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 26 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7575 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 10135-706 TABLET, EXTENDED RELEASE 1 mg ORAL ANDA 22 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 10135-707 TABLET, EXTENDED RELEASE 2 mg ORAL ANDA 22 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-189 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 21 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-189 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 21 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-190 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 21 sections
TOLTERODINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-190 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 21 sections
Tolterodine Tartrate Human Prescription Drug Label 1 16571-126 TABLET, FILM COATED 1 mg ORAL ANDA 21 sections
Tolterodine Tartrate Human Prescription Drug Label 1 16571-126 TABLET, FILM COATED 1 mg ORAL ANDA 21 sections
Tolterodine Tartrate Human Prescription Drug Label 1 16571-127 TABLET, FILM COATED 2 mg ORAL ANDA 21 sections
Tolterodine Tartrate Human Prescription Drug Label 1 16571-127 TABLET, FILM COATED 2 mg ORAL ANDA 21 sections
DETROL HUMAN PRESCRIPTION DRUG LABEL 1 16590-959 TABLET, FILM COATED 2 mg ORAL NDA 23 sections
Tolterodine tartrate Human Prescription Drug Label 1 27241-191 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 26 sections
Tolterodine tartrate Human Prescription Drug Label 1 27241-192 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 29300-239 TABLET 1 mg ORAL ANDA 20 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 29300-240 TABLET 2 mg ORAL ANDA 20 sections
Tolterodine tartrate HUMAN PRESCRIPTION DRUG LABEL 1 29300-306 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 17 sections
Tolterodine tartrate HUMAN PRESCRIPTION DRUG LABEL 1 29300-307 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 17 sections
Tolterodine Tartrate Human Prescription Drug Label 1 31722-607 CAPSULE, EXTENDED RELEASE 2 mg ORAL ANDA 26 sections
Tolterodine Tartrate Human Prescription Drug Label 1 31722-608 CAPSULE, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 31722-805 TABLET, FILM COATED 1 mg ORAL ANDA 22 sections
Tolterodine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 31722-806 TABLET, FILM COATED 2 mg ORAL ANDA 22 sections
Tolterodine tartrate Human Prescription Drug Label 1 33342-097 TABLET, FILM COATED 1 mg ORAL ANDA 22 sections