Stem definition | Drug id | CAS RN |
---|---|---|
monoamine oxydase (MAO)-inhibitors type B | 3521 | 136236-51-6 |
Dose | Unit | Route |
---|---|---|
1 | mg | O |
Property | Value | Reference |
---|---|---|
BA (Bioavailability) | 36 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
May 16, 2006 | FDA | TEVA | |
March 23, 2018 | PMDA | Takeda Pharmaceutical Company Limited |
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 |
---|---|---|---|---|---|---|
Hallucination | 214.83 | 23.18 | 101 | 4542 | 53737 | 53290686 |
Dyskinesia | 192.46 | 23.18 | 80 | 4563 | 31753 | 53312670 |
Hallucination, visual | 176.30 | 23.18 | 65 | 4578 | 18767 | 53325656 |
Serotonin syndrome | 125.43 | 23.18 | 56 | 4587 | 26350 | 53318073 |
Fall | 113.54 | 23.18 | 147 | 4496 | 358293 | 52986130 |
Delusion | 71.85 | 23.18 | 30 | 4613 | 11979 | 53332444 |
Pleurothotonus | 67.36 | 23.18 | 17 | 4626 | 1362 | 53343061 |
On and off phenomenon | 65.60 | 23.18 | 19 | 4624 | 2559 | 53341864 |
Drug interaction | 60.01 | 23.18 | 84 | 4559 | 219245 | 53125178 |
Tremor | 53.30 | 23.18 | 60 | 4583 | 125676 | 53218747 |
Confusional state | 52.52 | 23.18 | 74 | 4569 | 194147 | 53150276 |
Orthostatic hypotension | 51.14 | 23.18 | 32 | 4611 | 29721 | 53314702 |
Bradykinesia | 48.07 | 23.18 | 17 | 4626 | 4336 | 53340087 |
Gambling disorder | 47.85 | 23.18 | 13 | 4630 | 1387 | 53343036 |
Freezing phenomenon | 45.60 | 23.18 | 13 | 4630 | 1654 | 53342769 |
Compulsive shopping | 44.42 | 23.18 | 11 | 4632 | 815 | 53343608 |
Sudden onset of sleep | 41.47 | 23.18 | 10 | 4633 | 663 | 53343760 |
Impulse-control disorder | 39.45 | 23.18 | 10 | 4633 | 815 | 53343608 |
Hypersexuality | 38.83 | 23.18 | 9 | 4634 | 503 | 53343920 |
Muscle rigidity | 36.05 | 23.18 | 18 | 4625 | 10823 | 53333600 |
Coronary artery dissection | 34.68 | 23.18 | 9 | 4634 | 805 | 53343618 |
Labelled drug-drug interaction medication error | 33.04 | 23.18 | 17 | 4626 | 10882 | 53333541 |
Altered state of consciousness | 31.25 | 23.18 | 22 | 4621 | 24814 | 53319609 |
Choking | 29.66 | 23.18 | 15 | 4628 | 9261 | 53335162 |
Stoma site extravasation | 29.65 | 23.18 | 7 | 4636 | 424 | 53343999 |
Serum serotonin increased | 28.99 | 23.18 | 6 | 4637 | 197 | 53344226 |
Gait disturbance | 28.25 | 23.18 | 50 | 4593 | 158792 | 53185631 |
Compulsive hoarding | 27.65 | 23.18 | 5 | 4638 | 79 | 53344344 |
Psychotic symptom | 27.63 | 23.18 | 8 | 4635 | 1075 | 53343348 |
Fracture | 25.11 | 23.18 | 17 | 4626 | 18002 | 53326421 |
Dystonia | 24.90 | 23.18 | 15 | 4628 | 13006 | 53331417 |
Dementia | 23.81 | 23.18 | 16 | 4627 | 16734 | 53327689 |
Parkinsonian gait | 23.65 | 23.18 | 6 | 4637 | 490 | 53343933 |
Sleep talking | 23.56 | 23.18 | 7 | 4636 | 1029 | 53343394 |
Nocturia | 23.38 | 23.18 | 12 | 4631 | 7638 | 53336785 |
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 |
---|---|---|---|---|---|---|
Hallucination | 456.21 | 24.50 | 228 | 7265 | 52391 | 32453642 |
Impulse-control disorder | 279.15 | 24.50 | 66 | 7427 | 1483 | 32504550 |
Dyskinesia | 239.08 | 24.50 | 114 | 7379 | 23489 | 32482544 |
Hypersexuality | 213.96 | 24.50 | 54 | 7439 | 1603 | 32504430 |
Hallucination, visual | 177.09 | 24.50 | 84 | 7409 | 17075 | 32488958 |
Gambling disorder | 155.50 | 24.50 | 43 | 7450 | 1826 | 32504207 |
Fall | 151.81 | 24.50 | 205 | 7288 | 195996 | 32310037 |
On and off phenomenon | 117.05 | 24.50 | 40 | 7453 | 3461 | 32502572 |
Orthostatic hypotension | 116.71 | 24.50 | 73 | 7420 | 25577 | 32480456 |
Confusional state | 114.18 | 24.50 | 152 | 7341 | 142963 | 32363070 |
Dopamine dysregulation syndrome | 113.01 | 24.50 | 26 | 7467 | 515 | 32505518 |
Freezing phenomenon | 94.90 | 24.50 | 31 | 7462 | 2332 | 32503701 |
Delusion | 90.69 | 24.50 | 49 | 7444 | 13059 | 32492974 |
Serotonin syndrome | 73.58 | 24.50 | 49 | 7444 | 19068 | 32486965 |
Abnormal behaviour | 72.21 | 24.50 | 55 | 7438 | 26411 | 32479622 |
Resting tremor | 68.10 | 24.50 | 18 | 7475 | 642 | 32505391 |
Somnolence | 64.49 | 24.50 | 98 | 7395 | 103699 | 32402334 |
Dystonia | 60.62 | 24.50 | 35 | 7458 | 10588 | 32495445 |
Compulsive shopping | 54.34 | 24.50 | 14 | 7479 | 451 | 32505582 |
Cogwheel rigidity | 51.34 | 24.50 | 17 | 7476 | 1333 | 32504700 |
Bradykinesia | 50.42 | 24.50 | 23 | 7470 | 4263 | 32501770 |
Tremor | 49.39 | 24.50 | 76 | 7417 | 81201 | 32424832 |
Stereotypy | 48.47 | 24.50 | 14 | 7479 | 696 | 32505337 |
Muscle rigidity | 46.26 | 24.50 | 30 | 7463 | 11156 | 32494877 |
Balance disorder | 44.43 | 24.50 | 50 | 7443 | 39409 | 32466624 |
Cognitive disorder | 44.07 | 24.50 | 41 | 7452 | 25853 | 32480180 |
Sudden onset of sleep | 44.04 | 24.50 | 12 | 7481 | 481 | 32505552 |
Supine hypertension | 42.52 | 24.50 | 11 | 7482 | 360 | 32505673 |
Psychomotor hyperactivity | 41.75 | 24.50 | 26 | 7467 | 9013 | 32497020 |
Marasmus | 40.96 | 24.50 | 12 | 7481 | 627 | 32505406 |
Jealous delusion | 40.68 | 24.50 | 10 | 7483 | 265 | 32505768 |
Akinesia | 40.28 | 24.50 | 17 | 7476 | 2616 | 32503417 |
Stoma site discharge | 38.27 | 24.50 | 15 | 7478 | 1910 | 32504123 |
Oesophageal achalasia | 37.42 | 24.50 | 10 | 7483 | 372 | 32505661 |
Anticholinergic syndrome | 36.91 | 24.50 | 12 | 7481 | 888 | 32505145 |
Obsessive-compulsive personality disorder | 34.01 | 24.50 | 8 | 7485 | 175 | 32505858 |
Sleep disorder | 33.75 | 24.50 | 36 | 7457 | 26716 | 32479317 |
Paraphilia | 33.25 | 24.50 | 7 | 7486 | 90 | 32505943 |
Gait disturbance | 32.76 | 24.50 | 63 | 7430 | 80345 | 32425688 |
Parkinson's disease | 32.74 | 24.50 | 13 | 7480 | 1713 | 32504320 |
Dementia | 32.54 | 24.50 | 26 | 7467 | 13360 | 32492673 |
Agitation | 31.26 | 24.50 | 51 | 7442 | 57185 | 32448848 |
Mesenteric artery thrombosis | 31.10 | 24.50 | 9 | 7484 | 450 | 32505583 |
Autonomic nervous system imbalance | 30.94 | 24.50 | 14 | 7479 | 2546 | 32503487 |
Psychotic disorder | 30.86 | 24.50 | 32 | 7461 | 22988 | 32483045 |
Hyperkinesia | 29.24 | 24.50 | 13 | 7480 | 2269 | 32503764 |
Restlessness | 28.80 | 24.50 | 32 | 7461 | 24849 | 32481184 |
Hyperthermia | 28.59 | 24.50 | 22 | 7471 | 10706 | 32495327 |
Stoma site erythema | 28.15 | 24.50 | 11 | 7482 | 1389 | 32504644 |
Blood lactic acid | 27.84 | 24.50 | 8 | 7485 | 390 | 32505643 |
Thunderclap headache | 27.70 | 24.50 | 6 | 7487 | 89 | 32505944 |
Dysphagia | 27.31 | 24.50 | 50 | 7443 | 61426 | 32444607 |
Binge eating | 27.22 | 24.50 | 6 | 7487 | 97 | 32505936 |
Therapeutic product effect variable | 27.04 | 24.50 | 12 | 7481 | 2084 | 32503949 |
Prescribed underdose | 25.83 | 24.50 | 19 | 7474 | 8640 | 32497393 |
Aggression | 25.54 | 24.50 | 38 | 7455 | 39351 | 32466682 |
Fracture | 25.39 | 24.50 | 17 | 7476 | 6662 | 32499371 |
Disturbance in attention | 24.86 | 24.50 | 29 | 7464 | 23724 | 32482309 |
Obsessive-compulsive disorder | 24.84 | 24.50 | 15 | 7478 | 4919 | 32501114 |
Nocturia | 24.63 | 24.50 | 19 | 7474 | 9275 | 32496758 |
Source | Code | Description |
---|---|---|
ATC | N04BD02 | NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Monoamine oxidase B inhibitors |
FDA MoA | N0000000184 | Monoamine Oxidase Inhibitors |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D008996 | Monoamine Oxidase Inhibitors |
MeSH PA | D018696 | Neuroprotective Agents |
MeSH PA | D020011 | Protective Agents |
FDA EPC | N0000175744 | Monoamine Oxidase Inhibitor |
CHEBI has role | CHEBI:38623 | monoamine oxidase inhibitors |
CHEBI has role | CHEBI:63726 | neuroprotective agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Parkinson's disease | indication | 49049000 | DOID:14330 |
Dyskinesia | contraindication | 9748009 | |
Bipolar disorder | contraindication | 13746004 | DOID:3312 |
Orthostatic hypotension | contraindication | 28651003 | |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Epilepsy | contraindication | 84757009 | DOID:1826 |
Disease of liver | contraindication | 235856003 | DOID:409 |
Pheochromocytoma | contraindication | 302835009 | |
Malignant melanoma | contraindication | 372244006 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 7.54 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 0.5MG BASE | AZILECT | TEVA | N021641 | May 16, 2006 | RX | TABLET | ORAL | 7815942 | Aug. 27, 2027 | TREATMENT OF PARKINSONS DISEASE |
EQ 1MG BASE | AZILECT | TEVA | N021641 | May 16, 2006 | RX | TABLET | ORAL | 7815942 | Aug. 27, 2027 | TREATMENT OF PARKINSONS DISEASE |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Amine oxidase [flavin-containing] B | Enzyme | INHIBITOR | Ki | 6.15 | CHEMBL | CHEMBL | |||
Acetylcholinesterase | Enzyme | IC50 | 7.72 | CHEMBL | |||||
Cholinesterase | Enzyme | IC50 | 5.32 | CHEMBL | |||||
Amine oxidase [flavin-containing] A | Enzyme | Ki | 5.01 | CHEMBL | |||||
Amine oxidase [flavin-containing] B | Enzyme | IC50 | 8.36 | CHEMBL | |||||
Amine oxidase [flavin-containing] A | Enzyme | IC50 | 6.39 | CHEMBL |
ID | Source |
---|---|
4025261 | VUID |
N0000179514 | NUI |
D02562 | KEGG_DRUG |
136236-50-5 | SECONDARY_CAS_RN |
4025261 | VANDF |
4025262 | VANDF |
C0525678 | UMLSCUI |
CHEBI:63620 | CHEBI |
RAU | PDB_CHEM_ID |
CHEMBL887 | ChEMBL_ID |
DB01367 | DRUGBANK_ID |
CHEMBL1201142 | ChEMBL_ID |
CHEMBL1235738 | ChEMBL_ID |
3052776 | PUBCHEM_CID |
7151 | INN_ID |
C031967 | MESH_SUPPLEMENTAL_RECORD_UI |
6641 | IUPHAR_LIGAND_ID |
003N66TS6T | UNII |
134748 | RXNORM |
162358 | MMSL |
20417 | MMSL |
70623 | MMSL |
d05612 | MMSL |
010775 | NDDF |
010776 | NDDF |
418734001 | SNOMEDCT_US |
419010007 | SNOMEDCT_US |
734664007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Rasagiline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3060 | TABLET | 0.50 mg | ORAL | NDA authorized generic | 29 sections |
Rasagiline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3061 | TABLET | 1 mg | ORAL | NDA authorized generic | 29 sections |
Rasagiline Mesylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-1270 | TABLET | 0.50 mg | ORAL | ANDA | 30 sections |
Rasagiline Mesylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-1271 | TABLET | 1 mg | ORAL | ANDA | 30 sections |
Rasagiline | Human Prescription Drug Label | 1 | 16714-770 | TABLET | 0.50 mg | ORAL | ANDA | 29 sections |
Rasagiline | Human Prescription Drug Label | 1 | 16714-771 | TABLET | 1 mg | ORAL | ANDA | 29 sections |
Rasagiline Mesylate | Human Prescription Drug Label | 1 | 23155-746 | TABLET | 0.50 mg | ORAL | ANDA | 29 sections |
Rasagiline Mesylate | Human Prescription Drug Label | 1 | 23155-747 | TABLET | 1 mg | ORAL | ANDA | 29 sections |
Rasagiline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-779 | TABLET | 0.50 mg | ORAL | NDA authorized generic | 29 sections |
Rasagiline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-780 | TABLET | 1 mg | ORAL | NDA authorized generic | 29 sections |
RASAGILINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42571-220 | TABLET | 0.50 mg | ORAL | ANDA | 29 sections |
RASAGILINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42571-221 | TABLET | 1 mg | ORAL | ANDA | 29 sections |
Azilect | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43353-015 | TABLET | 1 mg | ORAL | NDA | 30 sections |
Rasagiline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-683 | TABLET | 0.50 mg | ORAL | ANDA | 27 sections |
Rasagiline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-690 | TABLET | 1 mg | ORAL | ANDA | 27 sections |
Azilect | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6206 | TABLET | 1 mg | ORAL | NDA | 30 sections |
Rasagiline | Human Prescription Drug Label | 1 | 67877-259 | TABLET | 0.50 mg | ORAL | ANDA | 29 sections |
Rasagiline | Human Prescription Drug Label | 1 | 67877-260 | TABLET | 1 mg | ORAL | ANDA | 29 sections |
Azilect | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68546-142 | TABLET | 0.50 mg | ORAL | NDA | 30 sections |
Azilect | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68546-229 | TABLET | 1 mg | ORAL | NDA | 30 sections |