Stem definition | Drug id | CAS RN |
---|---|---|
opioid receptor antagonists/agonists, morphinan derivates | 454 | 42408-82-2 |
Dose | Unit | Route |
---|---|---|
12 | mg | P |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 2 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 2 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.82 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 17 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 12 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 41 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.17 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 4.80 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 22, 1978 | FDA |
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 |
---|---|---|---|---|---|---|
Drug hypersensitivity | 289.92 | 36.82 | 103 | 393 | 243722 | 46441844 |
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 |
---|
Source | Code | Description |
---|---|---|
ATC | N02AF01 | NERVOUS SYSTEM ANALGESICS OPIOIDS Morphinan derivatives |
FDA MoA | N0000175685 | Partial Opioid Agonists |
FDA MoA | N0000175686 | Competitive Opioid Antagonists |
FDA EPC | N0000175692 | Opioid Agonist/Antagonist |
CHEBI has role | CHEBI:35482 | narcotic analgesics |
CHEBI has role | CHEBI:51177 | cough suppressant |
CHEBI has role | CHEBI:55322 | mu opioid agonist |
CHEBI has role | CHEBI:59282 | kappa-opioid receptor agonists |
MeSH PA | D000700 | Analgesics |
MeSH PA | D000701 | Analgesics, Opioid |
MeSH PA | D000996 | Antitussive Agents |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D009292 | Narcotic Antagonists |
MeSH PA | D009294 | Narcotics |
MeSH PA | D018373 | Peripheral Nervous System Agents |
MeSH PA | D019141 | Respiratory System Agents |
MeSH PA | D018689 | Sensory System Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Pain | indication | 22253000 | |
General anesthesia | indication | 50697003 | |
Labor pain | indication | 247412007 | |
Sedation as Adjunct to Anesthesia | indication | ||
Migraine | off-label use | 37796009 | DOID:6364 |
Chronic disease of respiratory system | contraindication | 17097001 | |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Chronic heart failure | contraindication | 48447003 | |
Substance abuse | contraindication | 66214007 | |
Benign intracranial hypertension | contraindication | 68267002 | DOID:11459 |
Opioid dependence | contraindication | 75544000 | DOID:2559 |
Decreased respiratory function | contraindication | 80954004 | |
Injury of head | contraindication | 82271004 | |
Impaired renal function disorder | contraindication | 197663003 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Disorder of coronary artery | contraindication | 414024009 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.7 | acidic |
pKa2 | 8.56 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Kappa-type opioid receptor | GPCR | PARTIAL AGONIST | Ki | 9.92 | CHEMBL | CHEMBL | |||
Mu-type opioid receptor | GPCR | PARTIAL AGONIST | Ki | 9.92 | CHEMBL | CHEMBL | |||
Delta-type opioid receptor | GPCR | Ki | 7.92 | CHEMBL |
ID | Source |
---|---|
4019650 | VUID |
N0000147743 | NUI |
D00837 | KEGG_DRUG |
58786-99-5 | SECONDARY_CAS_RN |
4018146 | VANDF |
4019650 | VANDF |
C0006491 | UMLSCUI |
CHEBI:3242 | CHEBI |
5361092 | PUBCHEM_CID |
CHEMBL33986 | ChEMBL_ID |
CHEMBL299400 | ChEMBL_ID |
DB00611 | DRUGBANK_ID |
D002077 | MESH_DESCRIPTOR_UI |
3620 | INN_ID |
7591 | IUPHAR_LIGAND_ID |
QV897JC36D | UNII |
1841 | RXNORM |
11596 | MMSL |
4315 | MMSL |
d00838 | MMSL |
001580 | NDDF |
004635 | NDDF |
13936006 | SNOMEDCT_US |
373467000 | SNOMEDCT_US |
69241001 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3090 | SPRAY, METERED | 10 mg | NULLSAL | ANDA | 29 sections |
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9864 | INJECTION, SOLUTION | 1 mg | INTRAMUSCULAR | ANDA | 28 sections |
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9867 | INJECTION, SOLUTION | 2 mg | INTRAMUSCULAR | ANDA | 28 sections |
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-9639 | SPRAY | 10 mg | NULLSAL | ANDA | 31 sections |
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1623 | INJECTION, SOLUTION | 1 mg | INTRAMUSCULAR | ANDA | 31 sections |
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1626 | INJECTION, SOLUTION | 2 mg | INTRAMUSCULAR | ANDA | 31 sections |
Butorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-0813 | SPRAY | 10 mg | NULLSAL | ANDA | 15 sections |