Stem definition | Drug id | CAS RN |
---|---|---|
1272 | 357-70-0 |
Dose | Unit | Route |
---|---|---|
16 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 10 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 20 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.45 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 99 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 2.30 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 5.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.83 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 5.30 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 28, 2001 | FDA | JANSSEN PHARMS |
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 |
---|---|---|---|---|---|---|
Orthostatic hypotension | 1217.80 | 40.90 | 359 | 7446 | 32840 | 56251422 |
Sedation complication | 1211.23 | 40.90 | 288 | 7517 | 11384 | 56272878 |
Creatinine renal clearance decreased | 1178.01 | 40.90 | 294 | 7511 | 14265 | 56269997 |
Sedation | 1139.88 | 40.90 | 345 | 7460 | 34509 | 56249753 |
Cognitive disorder | 1099.26 | 40.90 | 364 | 7441 | 48769 | 56235493 |
Blood calcium decreased | 1026.08 | 40.90 | 292 | 7513 | 23477 | 56260785 |
Balance disorder | 927.32 | 40.90 | 360 | 7445 | 76160 | 56208102 |
Depressed level of consciousness | 833.20 | 40.90 | 307 | 7498 | 56126 | 56228136 |
Mobility decreased | 619.55 | 40.90 | 292 | 7513 | 98699 | 56185563 |
Constipation | 599.80 | 40.90 | 362 | 7443 | 201581 | 56082681 |
Fall | 598.22 | 40.90 | 448 | 7357 | 357062 | 55927200 |
Hypotension | 547.42 | 40.90 | 370 | 7435 | 250138 | 56034124 |
Toxicity to various agents | 433.98 | 40.90 | 308 | 7497 | 224256 | 56060006 |
Pain | 144.73 | 40.90 | 296 | 7509 | 662888 | 55621374 |
Drug ineffective | 95.48 | 40.90 | 9 | 7796 | 918980 | 55365282 |
Fatigue | 63.15 | 40.90 | 16 | 7789 | 788536 | 55495726 |
Product dispensing error | 53.53 | 40.90 | 26 | 7779 | 9238 | 56275024 |
Pleurothotonus | 51.28 | 40.90 | 15 | 7790 | 1306 | 56282956 |
Marasmus | 45.21 | 40.90 | 11 | 7794 | 471 | 56283791 |
Multiple drug therapy | 43.95 | 40.90 | 16 | 7789 | 2776 | 56281486 |
Hallucination | 41.28 | 40.90 | 42 | 7763 | 49107 | 56235155 |
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 |
---|---|---|---|---|---|---|
Fall | 60.72 | 24.58 | 82 | 2998 | 186007 | 31508257 |
Dysphagia | 36.71 | 24.58 | 36 | 3044 | 57640 | 31636624 |
Post-traumatic stress disorder | 35.31 | 24.58 | 11 | 3069 | 1698 | 31692566 |
Aggression | 35.04 | 24.58 | 29 | 3051 | 37262 | 31657002 |
Dementia | 34.72 | 24.58 | 19 | 3061 | 12341 | 31681923 |
Compartment syndrome | 34.29 | 24.58 | 12 | 3068 | 2659 | 31691605 |
Fracture | 33.67 | 24.58 | 15 | 3065 | 6265 | 31687999 |
Hallucination | 33.39 | 24.58 | 31 | 3049 | 46379 | 31647885 |
Agitation | 31.14 | 24.58 | 32 | 3048 | 54137 | 31640127 |
Increased bronchial secretion | 26.68 | 24.58 | 9 | 3071 | 1785 | 31692479 |
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 |
---|---|---|---|---|---|---|
Sedation complication | 1269.57 | 30.49 | 309 | 9784 | 13101 | 70905250 |
Creatinine renal clearance decreased | 1193.18 | 30.49 | 309 | 9784 | 16891 | 70901460 |
Orthostatic hypotension | 1097.22 | 30.49 | 371 | 9722 | 51372 | 70866979 |
Sedation | 1081.81 | 30.49 | 358 | 9735 | 46373 | 70871978 |
Cognitive disorder | 1075.76 | 30.49 | 381 | 9712 | 60575 | 70857776 |
Blood calcium decreased | 1026.31 | 30.49 | 307 | 9786 | 28539 | 70889812 |
Balance disorder | 900.01 | 30.49 | 372 | 9721 | 89756 | 70828595 |
Depressed level of consciousness | 792.51 | 30.49 | 337 | 9756 | 87094 | 70831257 |
Mobility decreased | 651.97 | 30.49 | 309 | 9784 | 102690 | 70815661 |
Fall | 632.55 | 30.49 | 512 | 9581 | 443584 | 70474767 |
Constipation | 548.68 | 30.49 | 376 | 9717 | 252062 | 70666289 |
Hypotension | 446.94 | 30.49 | 404 | 9689 | 403977 | 70514374 |
Toxicity to various agents | 332.40 | 30.49 | 335 | 9758 | 381837 | 70536514 |
Pain | 177.35 | 30.49 | 318 | 9775 | 628498 | 70289853 |
Drug ineffective | 74.48 | 30.49 | 21 | 10072 | 939731 | 69978620 |
Dementia | 49.77 | 30.49 | 34 | 10059 | 22331 | 70896020 |
Marasmus | 46.80 | 30.49 | 13 | 10080 | 915 | 70917436 |
Pleurothotonus | 42.30 | 30.49 | 15 | 10078 | 2351 | 70916000 |
Multiple drug therapy | 41.46 | 30.49 | 16 | 10077 | 3176 | 70915175 |
Fatigue | 39.11 | 30.49 | 36 | 10057 | 824283 | 70094068 |
Arthralgia | 36.62 | 30.49 | 13 | 10080 | 503377 | 70414974 |
Headache | 34.42 | 30.49 | 20 | 10073 | 580385 | 70337966 |
Hallucination | 34.29 | 30.49 | 48 | 10045 | 76212 | 70842139 |
Bradycardia | 32.19 | 30.49 | 61 | 10032 | 124554 | 70793797 |
Poriomania | 31.23 | 30.49 | 7 | 10086 | 203 | 70918148 |
None
Source | Code | Description |
---|---|---|
ATC | N06DA04 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTI-DEMENTIA DRUGS Anticholinesterases |
FDA MoA | N0000000177 | Cholinesterase Inhibitors |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D018678 | Cholinergic Agents |
MeSH PA | D002800 | Cholinesterase Inhibitors |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D018697 | Nootropic Agents |
MeSH PA | D010277 | Parasympathomimetics |
MeSH PA | D018373 | Peripheral Nervous System Agents |
FDA EPC | N0000175723 | Cholinesterase Inhibitor |
CHEBI has role | CHEBI:37733 | EC 3.1.1.8 inhibitor |
CHEBI has role | CHEBI:38323 | cholinergic drugs |
CHEBI has role | CHEBI:38462 | acetylcholinesterase inhibitors |
CHEBI has role | CHEBI:74530 | curare poisoning antidote |
CHEBI has role | CHEBI:76924 | plant metabolites |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Alzheimer's disease | indication | 26929004 | DOID:10652 |
Diffuse Lewy body disease | off-label use | 80098002 | |
Moderate to Severe Alzheimer's Type Dementia | off-label use | ||
Peptic ulcer | contraindication | 13200003 | DOID:750 |
Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
Gastrointestinal ulcer | contraindication | 40845000 | |
Bradycardia | contraindication | 48867003 | |
Duodenal ulcer disease | contraindication | 51868009 | DOID:1724 |
Acute nephropathy | contraindication | 58574008 | |
Hepatic failure | contraindication | 59927004 | |
Epilepsy | contraindication | 84757009 | DOID:1826 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Asthma | contraindication | 195967001 | DOID:2841 |
Atrioventricular block | contraindication | 233917008 | DOID:0050820 |
Disease of liver | contraindication | 235856003 | DOID:409 |
Bladder outflow obstruction | contraindication | 236645006 | |
Congenital long QT syndrome | contraindication | 442917000 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.14 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Acetylcholinesterase | Enzyme | INHIBITOR | Ki | 7.21 | CHEMBL | CHEMBL | |||
Cholinesterase | Enzyme | Ki | 6.72 | CHEMBL | |||||
Acetylcholinesterase | Enzyme | IC50 | 6.44 | CHEMBL | |||||
Acetylcholinesterase | Enzyme | IC50 | 5.60 | CHEMBL | |||||
Butyrylcholinesterase; Protein Bche | Enzyme | IC50 | 5.23 | CHEMBL | |||||
Acetylcholinesterase | Enzyme | IC50 | 6.27 | CHEMBL | |||||
Acetylcholinesterase | Enzyme | Ki | 6.37 | CHEMBL | |||||
Acetylcholinesterase | Enzyme | IC50 | 5.06 | CHEMBL | |||||
Butyrylcholinesterase | Enzyme | Ki | 5.10 | CHEMBL | |||||
Cholinesterase | Enzyme | Ki | 5.03 | CHEMBL |
ID | Source |
---|---|
4021250 | VUID |
N0000148691 | NUI |
D02173 | KEGG_DRUG |
1953-04-4 | SECONDARY_CAS_RN |
4021250 | VANDF |
4021251 | VANDF |
C0016967 | UMLSCUI |
CHEBI:42944 | CHEBI |
GNT | PDB_CHEM_ID |
CHEMBL659 | ChEMBL_ID |
DB00674 | DRUGBANK_ID |
CHEMBL1555 | ChEMBL_ID |
D005702 | MESH_DESCRIPTOR_UI |
9651 | PUBCHEM_CID |
6693 | IUPHAR_LIGAND_ID |
1392 | INN_ID |
0D3Q044KCA | UNII |
4637 | RXNORM |
147848 | MMSL |
15913 | MMSL |
d04750 | MMSL |
007026 | NDDF |
007027 | NDDF |
129482002 | SNOMEDCT_US |
323377002 | SNOMEDCT_US |
395727007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Galantamine Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0137 | SOLUTION | 4 mg | ORAL | ANDA | 24 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3496 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | ANDA | 25 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3496 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | ANDA | 25 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3497 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | ANDA | 25 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3497 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | ANDA | 25 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3498 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | ANDA | 25 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3498 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | ANDA | 25 sections |
Galantamine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7104 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 26 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0881 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0881 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0882 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0882 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0883 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0883 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0891 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0891 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0892 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0892 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0893 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | NDA | 28 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0893 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | NDA | 28 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-184 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 20 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-591 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 20 sections |
Galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43353-984 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | ANDA | 20 sections |
Galantamine Hydrobromide | Human Prescription Drug Label | 1 | 47335-835 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | ANDA | 25 sections |
Galantamine Hydrobromide | Human Prescription Drug Label | 1 | 47335-835 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | ANDA | 25 sections |
Galantamine Hydrobromide | Human Prescription Drug Label | 1 | 47335-836 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | ANDA | 25 sections |
Galantamine Hydrobromide | Human Prescription Drug Label | 1 | 47335-836 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | ANDA | 25 sections |
Galantamine Hydrobromide | Human Prescription Drug Label | 1 | 47335-837 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | ANDA | 25 sections |
Galantamine Hydrobromide | Human Prescription Drug Label | 1 | 47335-837 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | ANDA | 25 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-387 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | NDA | 27 sections |