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distigmine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| acetylcholinesterase inhibitors | 927 | 17299-00-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mg | O |
| 0.25 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 8 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 59.80 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,MAP3K7,MAPK7,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 38 | |||
| kinase-selectivity-class | AXL,BRAF,EIF2AK3,EPHB4,ERBB2,GRK2,MAP2K6,MTOR,SIK2,STK33,TEK,TTK | 12 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 5, 1967 | PMDA | Torii Pharmaceuticals |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Cholinergic syndrome | 49.21 | 35.61 | 8 | 813 | 688 | 90626938 |
| Sleep disorder therapy | 37.33 | 35.61 | 6 | 815 | 480 | 90627146 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Appendicolith | 588.50 | 110.11 | 174 | 6888 | 13282 | 42600991 |
| Appendicitis | 527.34 | 110.11 | 177 | 6885 | 20436 | 42593837 |
| Cardiogenic shock | 409.02 | 110.11 | 170 | 6892 | 35470 | 42578803 |
| Ventricular fibrillation | 408.50 | 110.11 | 162 | 6900 | 29961 | 42584312 |
| Blood phosphorus increased | 382.21 | 110.11 | 123 | 6939 | 12402 | 42601871 |
| Stress | 373.77 | 110.11 | 170 | 6892 | 44042 | 42570231 |
| Ascites | 357.10 | 110.11 | 178 | 6884 | 56500 | 42557773 |
| Abdominal distension | 334.09 | 110.11 | 184 | 6878 | 71551 | 42542722 |
| Myasthenia gravis | 276.47 | 110.11 | 103 | 6959 | 16034 | 42598239 |
| Hyponatraemia | 263.09 | 110.11 | 179 | 6883 | 101283 | 42512990 |
| Multiple organ dysfunction syndrome | 263.08 | 110.11 | 176 | 6886 | 96859 | 42517414 |
| Blood uric acid increased | 243.69 | 110.11 | 93 | 6969 | 15454 | 42598819 |
| Dry mouth | 223.84 | 110.11 | 116 | 6946 | 39763 | 42574510 |
| Hyperphosphataemia | 222.67 | 110.11 | 83 | 6979 | 12921 | 42601352 |
| Blood cholesterol increased | 216.74 | 110.11 | 100 | 6962 | 26641 | 42587632 |
| Incorrect route of product administration | 206.73 | 110.11 | 94 | 6968 | 24211 | 42590062 |
| General physical health deterioration | 193.75 | 110.11 | 176 | 6886 | 151070 | 42463203 |
| Constipation | 188.86 | 110.11 | 179 | 6883 | 162112 | 42452161 |
| Hypophosphataemia | 184.41 | 110.11 | 83 | 6979 | 20862 | 42593411 |
| Neuralgia | 180.40 | 110.11 | 87 | 6975 | 25560 | 42588713 |
| Analgesic therapy | 178.30 | 110.11 | 59 | 7003 | 6465 | 42607808 |
| Bacterial infection | 176.46 | 110.11 | 88 | 6974 | 27791 | 42586482 |
| Sepsis | 166.70 | 110.11 | 184 | 6878 | 199150 | 42415123 |
| Iron deficiency | 165.51 | 110.11 | 64 | 6998 | 10997 | 42603276 |
| Sleep disorder therapy | 163.33 | 110.11 | 56 | 7006 | 6838 | 42607435 |
| Drug therapy | 155.73 | 110.11 | 53 | 7009 | 6327 | 42607946 |
| Abdominal pain | 152.62 | 110.11 | 172 | 6890 | 190299 | 42423974 |
| Diabetes mellitus | 134.32 | 110.11 | 97 | 6965 | 59990 | 42554283 |
| Swelling | 121.27 | 110.11 | 88 | 6974 | 54797 | 42559476 |
| Sleep disorder | 117.52 | 110.11 | 82 | 6980 | 48013 | 42566260 |
| Intentional product misuse | 116.18 | 110.11 | 90 | 6972 | 61810 | 42552463 |
| Activated partial thromboplastin time prolonged | 114.95 | 110.11 | 55 | 7007 | 15848 | 42598425 |
| Antacid therapy | 110.47 | 110.11 | 38 | 7024 | 4679 | 42609594 |
| Thrombosis | 110.22 | 110.11 | 91 | 6971 | 68420 | 42545853 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Appendicolith | 751.37 | 81.45 | 180 | 7859 | 14075 | 110567185 |
| Appendicitis | 641.39 | 81.45 | 183 | 7856 | 28281 | 110552979 |
| Ventricular fibrillation | 512.79 | 81.45 | 168 | 7871 | 41145 | 110540115 |
| Cardiogenic shock | 488.79 | 81.45 | 176 | 7863 | 57162 | 110524098 |
| Blood phosphorus increased | 482.63 | 81.45 | 130 | 7909 | 16210 | 110565050 |
| Ascites | 433.01 | 81.45 | 184 | 7855 | 92624 | 110488636 |
| Stress | 385.15 | 81.45 | 176 | 7863 | 105172 | 110476088 |
| Myasthenia gravis | 360.18 | 81.45 | 110 | 7929 | 21401 | 110559859 |
| Multiple organ dysfunction syndrome | 346.77 | 81.45 | 184 | 7855 | 151526 | 110429734 |
| Abdominal distension | 338.30 | 81.45 | 190 | 7849 | 174913 | 110406347 |
| Blood uric acid increased | 317.90 | 81.45 | 100 | 7939 | 21429 | 110559831 |
| Hyperphosphataemia | 300.95 | 81.45 | 90 | 7949 | 16291 | 110564969 |
| Hyponatraemia | 290.01 | 81.45 | 186 | 7853 | 217467 | 110363793 |
| Analgesic therapy | 253.28 | 81.45 | 66 | 7973 | 7218 | 110574042 |
| Hypophosphataemia | 238.63 | 81.45 | 90 | 7949 | 33092 | 110548168 |
| Sleep disorder therapy | 237.27 | 81.45 | 63 | 7976 | 7408 | 110573852 |
| Sepsis | 236.58 | 81.45 | 193 | 7846 | 327153 | 110254107 |
| Bacterial infection | 226.74 | 81.45 | 95 | 7944 | 45941 | 110535319 |
| Drug therapy | 224.50 | 81.45 | 60 | 7979 | 7231 | 110574029 |
| Neuralgia | 222.00 | 81.45 | 95 | 7944 | 48383 | 110532877 |
| Constipation | 215.53 | 81.45 | 190 | 7849 | 357596 | 110223664 |
| Iron deficiency | 212.35 | 81.45 | 71 | 7968 | 18405 | 110562855 |
| Incorrect route of product administration | 211.91 | 81.45 | 100 | 7939 | 63961 | 110517299 |
| Diabetes mellitus | 183.86 | 81.45 | 105 | 7934 | 99276 | 110481984 |
| General physical health deterioration | 178.39 | 81.45 | 185 | 7854 | 425110 | 110156150 |
| Antacid therapy | 163.49 | 81.45 | 44 | 7995 | 5440 | 110575820 |
| Activated partial thromboplastin time prolonged | 161.96 | 81.45 | 61 | 7978 | 22307 | 110558953 |
| Thrombosis | 157.19 | 81.45 | 98 | 7941 | 108564 | 110472696 |
| Dry mouth | 154.96 | 81.45 | 123 | 7916 | 199825 | 110381435 |
| Anticoagulant therapy | 150.39 | 81.45 | 41 | 7998 | 5320 | 110575940 |
| Aortic stenosis | 141.40 | 81.45 | 48 | 7991 | 13011 | 110568249 |
| Abdominal pain | 140.34 | 81.45 | 179 | 7860 | 512810 | 110068450 |
| Chronic obstructive pulmonary disease | 139.37 | 81.45 | 91 | 7948 | 109067 | 110472193 |
| End stage renal disease | 139.09 | 81.45 | 54 | 7985 | 21419 | 110559841 |
| Intentional product misuse | 136.88 | 81.45 | 97 | 7942 | 132807 | 110448453 |
| Blood cholesterol increased | 129.02 | 81.45 | 107 | 7932 | 184678 | 110396582 |
| Somnolence | 123.75 | 81.45 | 129 | 7910 | 297320 | 110283940 |
| Bacteroides infection | 113.87 | 81.45 | 29 | 8010 | 2890 | 110578370 |
| Gout | 111.44 | 81.45 | 54 | 7985 | 36512 | 110544748 |
| Hyperlipidaemia | 103.43 | 81.45 | 51 | 7988 | 35797 | 110545463 |
| Ulcer | 103.01 | 81.45 | 54 | 7985 | 43062 | 110538198 |
| Troponin increased | 99.97 | 81.45 | 47 | 7992 | 29719 | 110551541 |
| Pulmonary embolism | 92.67 | 81.45 | 95 | 7944 | 214379 | 110366881 |
| Total lung capacity decreased | 92.39 | 81.45 | 30 | 8009 | 7084 | 110574176 |
| Sleep disorder | 89.48 | 81.45 | 90 | 7949 | 198554 | 110382706 |
| Congenital hiatus hernia | 87.85 | 81.45 | 28 | 8011 | 6231 | 110575029 |
| Blood calcium increased | 84.63 | 81.45 | 36 | 8003 | 18004 | 110563256 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07AA03 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Anticholinesterases |
| MeSH PA | D002800 | Cholinesterase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| CHEBI has role | CHEBI:37733 | EC 3.1.1.8 (cholinesterase) inhibitor |
| CHEBI has role | CHEBI:38325 | muscarinic agonist |
Related Drugs by ATC class:
N07AA Anticholinesterases 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute cystitis | indication | 68226007 | DOID:13148 |
| Myasthenia gravis | indication | 91637004 | DOID:437 |
| Difficulty passing urine | indication | 102835006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase | Enzyme | INHIBITOR | KEGG DRUG | KEGG DRUG |
External reference:
| ID | Source |
|---|---|
| D01228 | KEGG_DRUG |
| 154982 | RXNORM |
| C0012757 | UMLSCUI |
| CHEMBL1199307 | ChEMBL_ID |
| CHEMBL1098285 | ChEMBL_ID |
| DB13694 | DRUGBANK_ID |
| C084645 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3116 | PUBCHEM_CID |
| 15876-67-2 | SECONDARY_CAS_RN |
| T940307O7B | UNII |
| 003959 | NDDF |
| 349943004 | SNOMEDCT_US |
| 395966008 | SNOMEDCT_US |
| 396033002 | SNOMEDCT_US |
| CHEBI:31512 | CHEBI |
| 764 | INN_ID |
| T940307O7B | INXIGHT DRUGS |
Pharmaceutical products:
None