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lofepramine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| substances of the imipramine group | 1592 | 23047-25-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.11 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | 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) | 7.16 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 6 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 54 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,PDK4,STK33,TTK | 6 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1977 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Restless legs syndrome | 62.21 | 57.32 | 14 | 266 | 24612 | 110564407 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AA07 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D000929 | Antidepressive Agents, Tricyclic |
| MeSH PA | D011619 | Psychotropic Drugs |
| CHEBI has role | CHEBI:35469 | antidepressant |
Related Drugs by ATC class:
N06AA Non-selective monoamine reuptake inhibitors 20 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Depressive disorder | indication | 35489007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.05 | Basic |
| pKa2 | 5.01 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Ki | 8.27 | WOMBAT-PK | IUPHAR | |||
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 7.16 | WOMBAT-PK | IUPHAR | |||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.70 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 6.44 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.17 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.48 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.89 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.47 | WOMBAT-PK | |||||
| D(2) dopamine receptor | GPCR | Ki | 5.70 | PDSP | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.34 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.34 | PDSP |
External reference:
| ID | Source |
|---|---|
| N0000167255 | NUI |
| D01285 | KEGG_DRUG |
| C0023961 | UMLSCUI |
| CHEBI:47782 | CHEBI |
| CHEMBL87708 | ChEMBL_ID |
| CHEMBL2106638 | ChEMBL_ID |
| D008127 | MESH_DESCRIPTOR_UI |
| DB13411 | DRUGBANK_ID |
| 3947 | PUBCHEM_CID |
| 7551 | IUPHAR_LIGAND_ID |
| 2909 | INN_ID |
| 26786-32-3 | SECONDARY_CAS_RN |
| OCA4JT7PAW | UNII |
| 6294 | RXNORM |
| 004095 | NDDF |
| 004096 | NDDF |
| 321831005 | SNOMEDCT_US |
| 395772004 | SNOMEDCT_US |
| 441539007 | SNOMEDCT_US |
| OCA4JT7PAW | INXIGHT DRUGS |
Pharmaceutical products:
None