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 | 932.25 | 38.03 | 281 | 6376 | 29200 | 50569267 |
Sedation complication | 929.48 | 38.03 | 218 | 6439 | 8548 | 50589919 |
Creatinine renal clearance decreased | 913.54 | 38.03 | 228 | 6429 | 11653 | 50586814 |
Sedation | 874.90 | 38.03 | 270 | 6387 | 30340 | 50568127 |
Cognitive disorder | 836.51 | 38.03 | 285 | 6372 | 43838 | 50554629 |
Blood calcium decreased | 779.09 | 38.03 | 226 | 6431 | 20480 | 50577987 |
Balance disorder | 705.92 | 38.03 | 285 | 6372 | 70305 | 50528162 |
Depressed level of consciousness | 628.65 | 38.03 | 241 | 6416 | 51712 | 50546755 |
Mobility decreased | 481.31 | 38.03 | 226 | 6431 | 79722 | 50518745 |
Fall | 456.55 | 38.03 | 364 | 6293 | 334568 | 50263899 |
Constipation | 442.28 | 38.03 | 284 | 6373 | 185424 | 50413043 |
Hypotension | 403.88 | 38.03 | 294 | 6363 | 235175 | 50363292 |
Toxicity to various agents | 292.23 | 38.03 | 233 | 6424 | 212266 | 50386201 |
Pain | 96.60 | 38.03 | 225 | 6432 | 578678 | 50019789 |
Drug ineffective | 77.18 | 38.03 | 9 | 6648 | 819324 | 49779143 |
Product dispensing error | 55.85 | 38.03 | 26 | 6631 | 8865 | 50589602 |
Pleurothotonus | 52.29 | 38.03 | 15 | 6642 | 1286 | 50597181 |
Fatigue | 49.36 | 38.03 | 16 | 6641 | 707585 | 49890882 |
Marasmus | 46.79 | 38.03 | 11 | 6646 | 429 | 50598038 |
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 | 62.14 | 22.60 | 82 | 2872 | 177096 | 29394477 |
Dysphagia | 37.37 | 22.60 | 36 | 2918 | 54890 | 29516683 |
Post-traumatic stress disorder | 35.58 | 22.60 | 11 | 2943 | 1611 | 29569962 |
Compartment syndrome | 34.97 | 22.60 | 12 | 2942 | 2440 | 29569133 |
Fracture | 33.81 | 22.60 | 15 | 2939 | 6038 | 29565535 |
Agitation | 31.86 | 22.60 | 32 | 2922 | 51272 | 29520301 |
Hallucination | 27.96 | 22.60 | 28 | 2926 | 44684 | 29526889 |
Increased bronchial secretion | 27.56 | 22.60 | 9 | 2945 | 1572 | 29570001 |
Aggression | 25.49 | 22.60 | 24 | 2930 | 35517 | 29536056 |
Miosis | 24.07 | 22.60 | 13 | 2941 | 7996 | 29563577 |
Coombs negative haemolytic anaemia | 23.91 | 22.60 | 5 | 2949 | 150 | 29571423 |
Loss of consciousness | 23.86 | 22.60 | 33 | 2921 | 74023 | 29497550 |
Bradycardia | 23.82 | 22.60 | 31 | 2923 | 65598 | 29505975 |
Hallucination, visual | 23.41 | 22.60 | 16 | 2938 | 14999 | 29556574 |
Cholinergic syndrome | 22.96 | 22.60 | 6 | 2948 | 480 | 29571093 |
Pneumonia aspiration | 22.95 | 22.60 | 23 | 2931 | 36714 | 29534859 |
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 | 984.79 | 28.87 | 238 | 8636 | 10116 | 64479742 |
Creatinine renal clearance decreased | 925.77 | 28.87 | 242 | 8632 | 14179 | 64475679 |
Orthostatic hypotension | 844.83 | 28.87 | 295 | 8579 | 46443 | 64443415 |
Sedation | 839.85 | 28.87 | 285 | 8589 | 41177 | 64448681 |
Cognitive disorder | 830.85 | 28.87 | 304 | 8570 | 54783 | 64435075 |
Blood calcium decreased | 780.30 | 28.87 | 240 | 8634 | 25314 | 64464544 |
Balance disorder | 690.21 | 28.87 | 299 | 8575 | 83627 | 64406231 |
Depressed level of consciousness | 604.19 | 28.87 | 270 | 8604 | 81166 | 64408692 |
Mobility decreased | 503.66 | 28.87 | 242 | 8632 | 85598 | 64404260 |
Fall | 501.63 | 28.87 | 430 | 8444 | 416396 | 64073462 |
Constipation | 409.02 | 28.87 | 299 | 8575 | 229038 | 64260820 |
Hypotension | 326.53 | 28.87 | 326 | 8548 | 380648 | 64109210 |
Toxicity to various agents | 226.15 | 28.87 | 263 | 8611 | 363250 | 64126608 |
Pain | 119.07 | 28.87 | 245 | 8629 | 553266 | 63936592 |
Drug ineffective | 59.30 | 28.87 | 21 | 8853 | 840226 | 63649632 |
Marasmus | 48.10 | 28.87 | 13 | 8861 | 855 | 64489003 |
Pleurothotonus | 43.20 | 28.87 | 15 | 8859 | 2287 | 64487571 |
Bradycardia | 33.39 | 28.87 | 59 | 8815 | 118160 | 64371698 |
Poriomania | 31.70 | 28.87 | 7 | 8867 | 196 | 64489662 |
Agitation | 31.53 | 28.87 | 49 | 8825 | 88318 | 64401540 |
Fracture | 29.92 | 28.87 | 23 | 8851 | 18732 | 64471126 |
Loss of consciousness | 29.66 | 28.87 | 64 | 8810 | 148301 | 64341557 |
Fatigue | 29.42 | 28.87 | 36 | 8838 | 748694 | 63741164 |
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 | 27 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0882 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 27 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0883 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 27 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0891 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | NDA | 27 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0892 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | NDA | 27 sections |
galantamine hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10147-0893 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | NDA | 27 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 | 47335-836 | 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 |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-387 | CAPSULE, EXTENDED RELEASE | 8 mg | ORAL | NDA | 26 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-388 | CAPSULE, EXTENDED RELEASE | 16 mg | ORAL | NDA | 26 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-389 | CAPSULE, EXTENDED RELEASE | 24 mg | ORAL | NDA | 26 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-396 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 26 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-397 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 26 sections |
RAZADYNE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-398 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 26 sections |
Galantamine Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51990-111 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 26 sections |
Galantamine Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51990-112 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 26 sections |
Galantamine Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51990-113 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 26 sections |
Galantamine | Human Prescription Drug Label | 1 | 57237-049 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 25 sections |