Stem definition | Drug id | CAS RN |
---|---|---|
2298 | 362-29-8 |
Dose | Unit | Route |
---|---|---|
25 | mg | O |
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.45 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 33 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 5, 1960 | FDA | HIKMA MAPLE |
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 |
---|---|---|---|---|---|---|
Intentional self-injury | 4723.02 | 155.72 | 886 | 2901 | 24398 | 53320881 |
Intentional overdose | 4252.58 | 155.72 | 957 | 2830 | 66248 | 53279031 |
Depressed level of consciousness | 590.39 | 155.72 | 198 | 3589 | 54230 | 53291049 |
Tachycardia | 279.36 | 155.72 | 141 | 3646 | 108071 | 53237208 |
Fatigue | 242.44 | 155.72 | 275 | 3512 | 730231 | 52615048 |
Snoring | 175.68 | 155.72 | 43 | 3744 | 3749 | 53341530 |
Akathisia | 171.38 | 155.72 | 50 | 3737 | 8521 | 53336758 |
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 |
---|---|---|---|---|---|---|
Intentional self-injury | 1671.35 | 89.90 | 318 | 1274 | 13582 | 32498352 |
Intentional overdose | 1440.76 | 89.90 | 340 | 1252 | 41261 | 32470673 |
Depressed level of consciousness | 161.03 | 89.90 | 64 | 1528 | 40783 | 32471151 |
Tachycardia | 112.09 | 89.90 | 61 | 1531 | 79027 | 32432907 |
Source | Code | Description |
---|---|---|
ATC | N05CM06 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Other hypnotics and sedatives |
CHEBI has role | CHEBI:35717 | sedatives |
CHEBI has role | CHEBI:37930 | phenothiazine antipsychotics |
CHEBI has role | CHEBI:37956 | histamine receptor blocker |
CHEBI has role | CHEBI:48279 | 5-hydroxytryptamine antagonists |
CHEBI has role | CHEBI:48561 | dopamine blocker |
CHEBI has role | CHEBI:48876 | Antimuskarinika |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
General anesthesia | indication | 50697003 | |
Local anesthesia | indication | 386761002 | |
Alcoholism | contraindication | 7200002 | |
Organophosphate poisoning | contraindication | 8260003 | |
Weight gain finding | contraindication | 8943002 | |
Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
Senile dementia | contraindication | 15662003 | |
Chronic disease of respiratory system | contraindication | 17097001 | |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Glaucoma | contraindication | 23986001 | DOID:1686 |
Orthostatic hypotension | contraindication | 28651003 | |
Torsades de pointes | contraindication | 31722008 | |
Parkinsonism | contraindication | 32798002 | |
Conduction disorder of the heart | contraindication | 44808001 | |
Chronic heart failure | contraindication | 48447003 | |
Bradycardia | contraindication | 48867003 | |
Extrapyramidal disease | contraindication | 76349003 | |
Hyperglycemia | contraindication | 80394007 | DOID:4195 |
Epilepsy | contraindication | 84757009 | DOID:1826 |
Leukopenia | contraindication | 84828003 | DOID:615 |
Stupor | contraindication | 89458003 | |
Tardive dyskinesia | contraindication | 102449007 | |
Prolonged QT interval | contraindication | 111975006 | |
Acute disease of cardiovascular system | contraindication | 128487001 | |
Angina pectoris | contraindication | 194828000 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Metabolic syndrome X | contraindication | 237602007 | DOID:14221 |
Hyperprolactinemia | contraindication | 237662005 | DOID:12700 |
Benign prostatic hyperplasia | contraindication | 266569009 | |
Retention of urine | contraindication | 267064002 | |
Anemia | contraindication | 271737000 | DOID:2355 |
Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
Coma | contraindication | 371632003 | |
At risk for aspiration | contraindication | 371736008 | |
Visual impairment | contraindication | 397540003 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
Obesity | contraindication | 414916001 | DOID:9970 |
Congenital long QT syndrome | contraindication | 442917000 | |
Carcinoma of female breast | contraindication | 447782002 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.19 | Basic |
pKa2 | 1.58 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Histamine H1 receptor | GPCR | ANTAGONIST | WOMBAT-PK | CHEMBL | |||||
D(2) dopamine receptor | GPCR | WOMBAT-PK | |||||||
5-hydroxytryptamine receptor 2A | GPCR | WOMBAT-PK | |||||||
5-hydroxytryptamine receptor 2C | GPCR | WOMBAT-PK | |||||||
Muscarinic acetylcholine receptor M1 | GPCR | WOMBAT-PK | |||||||
Muscarinic acetylcholine receptor M2 | GPCR | WOMBAT-PK | |||||||
Muscarinic acetylcholine receptor M3 | GPCR | WOMBAT-PK | |||||||
Muscarinic acetylcholine receptor M4 | GPCR | WOMBAT-PK | |||||||
Muscarinic acetylcholine receptor M5 | GPCR | WOMBAT-PK | |||||||
D(4) dopamine receptor | GPCR | WOMBAT-PK | |||||||
D(1A) dopamine receptor | GPCR | WOMBAT-PK | |||||||
Alpha-1B adrenergic receptor | GPCR | WOMBAT-PK |
ID | Source |
---|---|
4019914 | VUID |
N0000147999 | NUI |
D02361 | KEGG_DRUG |
1240-15-9 | SECONDARY_CAS_RN |
4018031 | VANDF |
4019914 | VANDF |
C0033473 | UMLSCUI |
CHEBI:8491 | CHEBI |
CHEMBL252103 | ChEMBL_ID |
CHEMBL1201210 | ChEMBL_ID |
CHEMBL1201068 | ChEMBL_ID |
DB00777 | DRUGBANK_ID |
C084591 | MESH_SUPPLEMENTAL_RECORD_UI |
4940 | PUBCHEM_CID |
7284 | IUPHAR_LIGAND_ID |
735 | INN_ID |
242Z0PM79Y | UNII |
227589 | RXNORM |
1709 | MMSL |
5371 | MMSL |
d00914 | MMSL |
001488 | NDDF |
001489 | NDDF |
373493007 | SNOMEDCT_US |
41324009 | SNOMEDCT_US |
65868004 | SNOMEDCT_US |
None