Stem definition | Drug id | CAS RN |
---|---|---|
2705 | 124937-51-5 |
Dose | Unit | Route |
---|---|---|
4 | mg | O |
Property | Value | Reference |
---|---|---|
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
March 25, 1998 | FDA | PHARMACIA AND UPJOHN |
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 |
---|---|---|---|---|---|---|
Sensitivity to weather change | 92.75 | 11.33 | 47 | 21441 | 5469 | 46659105 |
Urinary tract infection | 92.60 | 11.33 | 266 | 21222 | 220000 | 46444574 |
Urinary incontinence | 83.28 | 11.33 | 83 | 21405 | 28447 | 46636127 |
Dry mouth | 83.17 | 11.33 | 114 | 21374 | 54812 | 46609762 |
Multiple sclerosis relapse | 70.77 | 11.33 | 92 | 21396 | 42033 | 46622541 |
Pollakiuria | 67.91 | 11.33 | 69 | 21419 | 24192 | 46640382 |
Multiple sclerosis | 66.66 | 11.33 | 69 | 21419 | 24722 | 46639852 |
Hypertonic bladder | 57.63 | 11.33 | 28 | 21460 | 2976 | 46661598 |
Fall | 54.95 | 11.33 | 297 | 21191 | 328800 | 46335774 |
Bladder disorder | 49.02 | 11.33 | 34 | 21454 | 7044 | 46657530 |
Antinuclear antibody negative | 44.37 | 11.33 | 12 | 21476 | 228 | 46664346 |
Coombs positive haemolytic anaemia | 42.86 | 11.33 | 13 | 21475 | 377 | 46664197 |
Nocturia | 41.91 | 11.33 | 31 | 21457 | 7101 | 46657473 |
Herpes simplex reactivation | 39.56 | 11.33 | 12 | 21476 | 348 | 46664226 |
Maternal exposure during pregnancy | 33.37 | 11.33 | 4 | 21484 | 102545 | 46562029 |
Exposure during pregnancy | 33.36 | 11.33 | 5 | 21483 | 108207 | 46556367 |
Micturition urgency | 31.03 | 11.33 | 27 | 21461 | 7790 | 46656784 |
Stress urinary incontinence | 29.76 | 11.33 | 16 | 21472 | 2100 | 46662474 |
Urinary retention | 29.21 | 11.33 | 47 | 21441 | 26014 | 46638560 |
Bladder spasm | 29.02 | 11.33 | 14 | 21474 | 1465 | 46663109 |
Gastritis haemorrhagic | 27.38 | 11.33 | 13 | 21475 | 1313 | 46663261 |
Balance disorder | 27.07 | 11.33 | 78 | 21410 | 64443 | 46600131 |
Gastrooesophageal reflux disease | 25.71 | 11.33 | 84 | 21404 | 74260 | 46590314 |
Completed suicide | 25.52 | 11.33 | 18 | 21470 | 145902 | 46518672 |
Cerebrovascular accident | 24.69 | 11.33 | 102 | 21386 | 100937 | 46563637 |
Off label use | 24.58 | 11.33 | 91 | 21397 | 379750 | 46284824 |
Antiphospholipid syndrome | 24.23 | 11.33 | 13 | 21475 | 1699 | 46662875 |
Treatment failure | 23.19 | 11.33 | 7 | 21481 | 93080 | 46571494 |
Hyperlipidaemia | 22.95 | 11.33 | 35 | 21453 | 18504 | 46646070 |
Transient ischaemic attack | 22.86 | 11.33 | 50 | 21438 | 34853 | 46629721 |
Complex regional pain syndrome | 21.95 | 11.33 | 13 | 21475 | 2053 | 46662521 |
Toxicity to various agents | 21.92 | 11.33 | 40 | 21448 | 211726 | 46452848 |
Hypothyroidism | 21.80 | 11.33 | 46 | 21442 | 31292 | 46633282 |
Oesophagitis | 20.14 | 11.33 | 28 | 21460 | 13623 | 46650951 |
Confusional state | 19.98 | 11.33 | 134 | 21354 | 159758 | 46504816 |
Contraindicated product administered | 19.94 | 11.33 | 6 | 21482 | 79941 | 46584633 |
Coronary artery disease | 19.49 | 11.33 | 46 | 21442 | 33706 | 46630868 |
Drug abuse | 19.38 | 11.33 | 3 | 21485 | 63405 | 46601169 |
Incontinence | 18.87 | 11.33 | 23 | 21465 | 9839 | 46654735 |
Dizziness | 18.33 | 11.33 | 238 | 21250 | 340176 | 46324398 |
Depression | 18.03 | 11.33 | 137 | 21351 | 169967 | 46494607 |
Anxiety disorder | 17.85 | 11.33 | 14 | 21474 | 3497 | 46661077 |
Therapy non-responder | 17.50 | 11.33 | 50 | 21438 | 41102 | 46623472 |
Urge incontinence | 17.42 | 11.33 | 8 | 21480 | 749 | 46663825 |
Hallucination, auditory | 17.29 | 11.33 | 23 | 21465 | 10733 | 46653841 |
White blood cell count abnormal | 16.98 | 11.33 | 16 | 21472 | 5116 | 46659458 |
Neutropenia | 16.72 | 11.33 | 25 | 21463 | 143179 | 46521395 |
Constipation | 16.68 | 11.33 | 137 | 21351 | 173960 | 46490614 |
Secondary progressive multiple sclerosis | 16.53 | 11.33 | 9 | 21479 | 1211 | 46663363 |
Iliac artery occlusion | 16.45 | 11.33 | 5 | 21483 | 146 | 46664428 |
Blood cholesterol increased | 16.42 | 11.33 | 48 | 21440 | 39965 | 46624609 |
Paranoia | 16.03 | 11.33 | 22 | 21466 | 10575 | 46653999 |
Mental status changes | 15.93 | 11.33 | 46 | 21442 | 38042 | 46626532 |
Perforation | 15.40 | 11.33 | 8 | 21480 | 979 | 46663595 |
Gait disturbance | 15.39 | 11.33 | 117 | 21371 | 145146 | 46519428 |
Neutrophil count abnormal | 15.19 | 11.33 | 11 | 21477 | 2439 | 46662135 |
Barrett's oesophagus | 15.09 | 11.33 | 7 | 21481 | 671 | 46663903 |
Death | 14.36 | 11.33 | 93 | 21395 | 335455 | 46329119 |
Aphonia | 14.35 | 11.33 | 18 | 21470 | 7927 | 46656647 |
Malignant neoplasm progression | 14.26 | 11.33 | 6 | 21482 | 64920 | 46599654 |
Drug hypersensitivity | 14.18 | 11.33 | 173 | 21315 | 243652 | 46420922 |
Febrile neutropenia | 13.69 | 11.33 | 14 | 21474 | 94613 | 46569961 |
Dysphagia | 13.66 | 11.33 | 71 | 21417 | 77241 | 46587333 |
Infusion related reaction | 13.51 | 11.33 | 16 | 21472 | 101192 | 46563382 |
Drug intolerance | 13.31 | 11.33 | 30 | 21458 | 147019 | 46517555 |
Haemoglobin abnormal | 13.29 | 11.33 | 13 | 21475 | 4350 | 46660224 |
Product complaint | 12.45 | 11.33 | 21 | 21467 | 12080 | 46652494 |
Cystitis | 12.22 | 11.33 | 45 | 21443 | 42196 | 46622378 |
Rheumatoid arthritis | 12.18 | 11.33 | 63 | 21425 | 240152 | 46424422 |
Increased appetite | 11.85 | 11.33 | 17 | 21471 | 8510 | 46656064 |
Dementia | 11.66 | 11.33 | 23 | 21465 | 14907 | 46649667 |
Osteonecrosis | 11.65 | 11.33 | 32 | 21456 | 25712 | 46638862 |
Neurogenic bladder | 11.45 | 11.33 | 10 | 21478 | 2900 | 46661674 |
Haemoglobin | 11.42 | 11.33 | 4 | 21484 | 184 | 46664390 |
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 | 55.96 | 14.78 | 16 | 6631 | 797 | 29945034 |
Dry mouth | 54.10 | 14.78 | 43 | 6604 | 22807 | 29923024 |
Pollakiuria | 53.82 | 14.78 | 38 | 6609 | 16868 | 29928963 |
Lipoma | 46.49 | 14.78 | 16 | 6631 | 1467 | 29944364 |
Urinary incontinence | 44.70 | 14.78 | 34 | 6613 | 16906 | 29928925 |
Fall | 42.04 | 14.78 | 111 | 6536 | 181761 | 29764070 |
Urinary retention | 38.86 | 14.78 | 42 | 6605 | 32875 | 29912956 |
Balance disorder | 38.67 | 14.78 | 44 | 6603 | 36449 | 29909382 |
Prostatic specific antigen increased | 35.94 | 14.78 | 26 | 6621 | 11978 | 29933853 |
Micturition urgency | 35.43 | 14.78 | 18 | 6629 | 4389 | 29941442 |
Inflammatory marker increased | 34.62 | 14.78 | 16 | 6631 | 3172 | 29942659 |
Musculoskeletal discomfort | 26.88 | 14.78 | 17 | 6630 | 6283 | 29939548 |
Multiple sclerosis | 22.34 | 14.78 | 16 | 6631 | 7251 | 29938580 |
Urinary tract infection | 22.33 | 14.78 | 50 | 6597 | 73609 | 29872222 |
Hypertonic bladder | 21.91 | 14.78 | 8 | 6639 | 871 | 29944960 |
Bladder disorder | 21.01 | 14.78 | 11 | 6636 | 2852 | 29942979 |
Nocturia | 20.43 | 14.78 | 16 | 6631 | 8296 | 29937535 |
Failure to thrive | 18.71 | 14.78 | 15 | 6632 | 8039 | 29937792 |
Cerebrovascular accident | 18.25 | 14.78 | 50 | 6597 | 83427 | 29862404 |
Rectal tenesmus | 17.53 | 14.78 | 6 | 6641 | 541 | 29945290 |
Confusional state | 16.23 | 14.78 | 66 | 6581 | 134768 | 29811063 |
Blood pressure systolic increased | 15.62 | 14.78 | 18 | 6629 | 15092 | 29930739 |
Muscular weakness | 14.78 | 14.78 | 39 | 6608 | 63606 | 29882225 |
Source | Code | Description |
---|---|---|
ATC | G04BD07 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs for urinary frequency and incontinence |
FDA MoA | N0000000125 | Cholinergic Muscarinic Antagonists |
FDA EPC | N0000175700 | Cholinergic Muscarinic Antagonist |
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 |
CHEBI has role | CHEBI:48876 | antimuskarinika |
CHEBI has role | CHEBI:51371 | muscle relaxants |
CHEBI has role | CHEBI:53784 | antispasmodics |
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 | |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.83 | acidic |
pKa2 | 9.14 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
4024113 | VUID |
N0000022118 | NUI |
D00646 | KEGG_DRUG |
124937-52-6 | SECONDARY_CAS_RN |
4021103 | VANDF |
4024113 | VANDF |
C0388753 | UMLSCUI |
CHEBI:9622 | CHEBI |
443879 | PUBCHEM_CID |
DB01036 | DRUGBANK_ID |
CHEMBL1382 | ChEMBL_ID |
CHEMBL1722209 | ChEMBL_ID |
D000068737 | MESH_DESCRIPTOR_UI |
6768 | INN_ID |
WHE7A56U7K | UNII |
360 | IUPHAR_LIGAND_ID |
119565 | RXNORM |
191519 | MMSL |
5600 | MMSL |
d04294 | MMSL |
007444 | NDDF |
007445 | NDDF |
109113000 | SNOMEDCT_US |
372570008 | SNOMEDCT_US |
386971005 | SNOMEDCT_US |
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 | 0009-5191 | 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 | 0093-0018 | 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 | 0378-3402 | CAPSULE, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 27 sections |
Tolterodine Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-3404 | CAPSULE, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 27 sections |
TOLTERODINE TARTRATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6592 | CAPSULE, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 20 sections |
TOLTERODINE TARTRATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6593 | CAPSULE, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 20 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 | 20 sections |
TOLTERODINE TARTRATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-190 | CAPSULE, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 20 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 |
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 | 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 | 33342-097 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 22 sections |
Tolterodine tartrate | Human Prescription Drug Label | 1 | 33342-098 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 22 sections |
Tolterodine Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43353-346 | CAPSULE, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 27 sections |
Tolterodine Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43975-322 | CAPSULE, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 25 sections |
Tolterodine Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43975-323 | CAPSULE, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 25 sections |