dezocine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 847 | 53648-55-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
potent analgesic; RN given refers to ((5R-(5alpha,11alpha,13S*)))-isomer (dezocin); structure
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 20 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.68 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 5.60 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 27.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.08 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.90 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | ASTRAZENECA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02AX03 | NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000701 | Analgesics, Opioid |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009294 | Narcotics |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35482 | narcotic analgesic |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pain | indication | 22253000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.25 | acidic |
| pKa2 | 9.39 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | PARTIAL AGONIST | EC50 | 7.42 | CHEMBL | CHEMBL | |||
| Kappa-type opioid receptor | GPCR | ANTAGONIST | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019515 | VUID |
| N0000147635 | NUI |
| D00838 | KEGG_DRUG |
| 216364 | RXNORM |
| 4019515 | VANDF |
| C0057626 | UMLSCUI |
| CHEBI:4474 | CHEBI |
| CHEMBL1685 | ChEMBL_ID |
| DB01209 | DRUGBANK_ID |
| C010827 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3033053 | PUBCHEM_CID |
| 3906 | INN_ID |
| VHX8K5SV4X | UNII |
| 4570 | MMSL |
| 534 | MMSL |
| d00837 | MMSL |
| 003545 | NDDF |
| 108377005 | SNOMEDCT_US |
| 370233009 | SNOMEDCT_US |
Pharmaceutical products:
None