Stem definition | Drug id | CAS RN |
---|---|---|
diazepam derivatives | 1056 | 29975-16-4 |
Dose | Unit | Route |
---|---|---|
3 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 0.00 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 4 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.10 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 93 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 26, 1990 | FDA | ABBOTT |
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 |
---|---|---|---|---|---|---|
Serotonin syndrome | 54.58 | 24.29 | 25 | 2203 | 24688 | 50578208 |
Electrocardiogram QT prolonged | 47.14 | 24.29 | 29 | 2199 | 51857 | 50551039 |
Intentional overdose | 39.85 | 24.29 | 28 | 2200 | 62476 | 50540420 |
Disseminated intravascular coagulation | 36.77 | 24.29 | 17 | 2211 | 17118 | 50585778 |
Drug interaction | 35.94 | 24.29 | 44 | 2184 | 199577 | 50403319 |
Ventricular arrhythmia | 32.46 | 24.29 | 10 | 2218 | 3299 | 50599597 |
Electrocardiogram QRS complex prolonged | 31.56 | 24.29 | 11 | 2217 | 5333 | 50597563 |
Bradycardia | 30.19 | 24.29 | 24 | 2204 | 64402 | 50538494 |
Suicide attempt | 28.01 | 24.29 | 21 | 2207 | 51711 | 50551185 |
Rhabdomyolysis | 26.06 | 24.29 | 18 | 2210 | 39009 | 50563887 |
Poverty of speech | 24.36 | 24.29 | 5 | 2223 | 316 | 50602580 |
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 |
---|---|---|---|---|---|---|
Hyperammonaemia | 30.79 | 23.02 | 11 | 1310 | 5652 | 29567554 |
Inappropriate antidiuretic hormone secretion | 30.21 | 23.02 | 13 | 1308 | 10919 | 29562287 |
Altered state of consciousness | 28.36 | 23.02 | 15 | 1306 | 19874 | 29553332 |
Delirium | 28.08 | 23.02 | 19 | 1302 | 39378 | 29533828 |
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 |
---|---|---|---|---|---|---|
Delirium | 45.68 | 20.75 | 35 | 3619 | 69159 | 64425919 |
Drug interaction | 40.56 | 20.75 | 73 | 3581 | 362010 | 64133068 |
Electrocardiogram QT prolonged | 37.36 | 20.75 | 33 | 3621 | 79415 | 64415663 |
Altered state of consciousness | 36.15 | 20.75 | 24 | 3630 | 37878 | 64457200 |
Intentional overdose | 35.74 | 20.75 | 34 | 3620 | 89910 | 64405168 |
Persecutory delusion | 31.53 | 20.75 | 11 | 3643 | 4147 | 64490931 |
Serotonin syndrome | 30.68 | 20.75 | 22 | 3632 | 39260 | 64455818 |
Rhabdomyolysis | 29.65 | 20.75 | 31 | 3623 | 91695 | 64403383 |
Inappropriate antidiuretic hormone secretion | 28.50 | 20.75 | 17 | 3637 | 22272 | 64472806 |
Suicide attempt | 26.61 | 20.75 | 26 | 3628 | 70981 | 64424097 |
Disseminated intravascular coagulation | 24.99 | 20.75 | 18 | 3636 | 32330 | 64462748 |
Hepatic function abnormal | 23.07 | 20.75 | 23 | 3631 | 64290 | 64430788 |
Electrocardiogram QRS complex prolonged | 23.03 | 20.75 | 11 | 3643 | 9233 | 64485845 |
Hyperammonaemia | 22.31 | 20.75 | 11 | 3643 | 9893 | 64485185 |
Ventricular arrhythmia | 22.13 | 20.75 | 10 | 3644 | 7405 | 64487673 |
Neuroleptic malignant syndrome | 21.84 | 20.75 | 15 | 3639 | 24981 | 64470097 |
None
Source | Code | Description |
---|---|---|
ATC | N05CD04 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives |
FDA CS | M0002356 | Benzodiazepines |
CHEBI has role | CHEBI:35474 | anti-anxiety agents |
CHEBI has role | CHEBI:35623 | anticonvulsants |
CHEBI has role | CHEBI:50268 | GABA modulators |
MeSH PA | D014151 | Anti-Anxiety Agents |
MeSH PA | D000927 | Anticonvulsants |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D018682 | GABA Agents |
MeSH PA | D018757 | GABA Modulators |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D011619 | Psychotropic Drugs |
MeSH PA | D014149 | Tranquilizing Agents |
FDA EPC | N0000175694 | Benzodiazepine |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Severe Insomnia | indication | ||
Alcohol intoxication | contraindication | 25702006 | |
Depressive disorder | contraindication | 35489007 | |
Substance abuse | contraindication | 66214007 | |
Psychotic disorder | contraindication | 69322001 | |
Sleep apnea | contraindication | 73430006 | DOID:0050847 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Myasthenia gravis | contraindication | 91637004 | DOID:437 |
Disease of liver | contraindication | 235856003 | DOID:409 |
Pregnancy, function | contraindication | 289908002 | |
Severe chronic obstructive pulmonary disease | contraindication | 313299006 | |
Breastfeeding (mother) | contraindication | 413712001 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 5.82 | Basic |
pKa2 | 4.83 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL | |||||
GABA-A receptor alpha-2/beta-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL | |||||
GABA-A receptor alpha-3/beta-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL | |||||
GABA-A receptor alpha-5/beta-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL |
ID | Source |
---|---|
4019566 | VUID |
N0000147666 | NUI |
D00311 | KEGG_DRUG |
4019566 | VANDF |
C0014892 | UMLSCUI |
CHEBI:4858 | CHEBI |
CHEMBL285674 | ChEMBL_ID |
DB01215 | DRUGBANK_ID |
D004949 | MESH_DESCRIPTOR_UI |
3261 | PUBCHEM_CID |
7550 | IUPHAR_LIGAND_ID |
3611 | INN_ID |
36S3EQV54C | UNII |
4077 | RXNORM |
10202 | MMSL |
4682 | MMSL |
d00915 | MMSL |
003566 | NDDF |
371364001 | SNOMEDCT_US |
96235001 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0744 | TABLET | 1 mg | ORAL | ANDA | 16 sections |
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0745 | TABLET | 2 mg | ORAL | ANDA | 16 sections |
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-220 | TABLET | 2 mg | ORAL | ANDA | 29 sections |
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-069 | TABLET | 1 mg | ORAL | ANDA | 33 sections |
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-070 | TABLET | 2 mg | ORAL | ANDA | 33 sections |
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-073 | TABLET | 1 mg | ORAL | ANDA | 33 sections |
Estazolam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-074 | TABLET | 2 mg | ORAL | ANDA | 33 sections |
Estazolam | Human Prescription Drug Label | 1 | 70954-480 | TABLET | 1 mg | ORAL | ANDA | 27 sections |
Estazolam | Human Prescription Drug Label | 1 | 70954-481 | TABLET | 2 mg | ORAL | ANDA | 27 sections |