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meptazinol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1706 | 54340-58-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.20 | g | O |
| 1.20 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 63.53 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 9 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 28 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.73 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.70 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ZAP70 | 42 | |||
| kinase-selectivity-class | AXL,EIF2AK3,EPHB4,GRK2,PDK4 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1983 | YEAR INTRODUCED |
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)
| 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 |
|---|---|---|---|---|---|---|
| Bradycardia neonatal | 9.88 | 9.75 | 3 | 3 | 1066 | 112881 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02AX05 | NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000701 | Analgesics, Opioid |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009292 | Narcotic Antagonists |
| MeSH PA | D009294 | Narcotics |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35480 | analgesic |
Related Drugs by ATC class:
N02AX Other opioids 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Moderate pain | indication | 50415004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.58 | acidic |
| pKa2 | 8.96 | 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 | 8.06 | WOMBAT-PK | SCIENTIFIC LITERATURE | |||
| Solute carrier family 22 member 1 | Transporter | IC50 | 4.72 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | IC50 | 4.39 | CHEMBL | |||||
| Cholinesterase | Enzyme | IC50 | 4.82 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D04924 | KEGG_DRUG |
| 59263-76-2 | SECONDARY_CAS_RN |
| C0025387 | UMLSCUI |
| CHEBI:748375 | CHEBI |
| CHEMBL314437 | ChEMBL_ID |
| DB13478 | DRUGBANK_ID |
| CHEMBL1477274 | ChEMBL_ID |
| D008621 | MESH_DESCRIPTOR_UI |
| 41049 | PUBCHEM_CID |
| 9083 | IUPHAR_LIGAND_ID |
| 3605 | INN_ID |
| 18Y7S5JKZD | UNII |
| 11347 | RXNORM |
| 004001 | NDDF |
| 004002 | NDDF |
| 354055003 | SNOMEDCT_US |
| 395783008 | SNOMEDCT_US |
| 768496009 | SNOMEDCT_US |
| 18Y7S5JKZD | INXIGHT DRUGS |
Pharmaceutical products:
None