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dosulepin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tricyclic compounds | 951 | 113-53-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A tricyclic antidepressant with some tranquilizing action.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.15 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 500 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 5 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 6.46 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 30 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PDPK1,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 37 | |||
| kinase-selectivity-class | AXL,BRAF,PDK4,TTK | 4 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.566 | Moderate | 0.67 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.67 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.904 | % | Moderate | 0.67 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1962 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Acute kidney injury | 54.47 | 31.94 | 46 | 1639 | 320341 | 90306421 |
| Toxicity to various agents | 44.15 | 31.94 | 39 | 1646 | 287807 | 90338955 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Head discomfort | 343.48 | 70.13 | 61 | 633 | 5116 | 42615525 |
| Migraine | 246.73 | 70.13 | 61 | 633 | 25353 | 42595288 |
| Neck pain | 231.74 | 70.13 | 60 | 634 | 29954 | 42590687 |
| Back pain | 143.60 | 70.13 | 61 | 633 | 141715 | 42478926 |
| Headache | 115.96 | 70.13 | 62 | 632 | 239307 | 42381334 |
| Pain | 111.81 | 70.13 | 61 | 633 | 244787 | 42375854 |
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 |
|---|---|---|---|---|---|---|
| Head discomfort | 240.00 | 30.36 | 60 | 2339 | 18940 | 110567960 |
| Neck pain | 126.95 | 30.36 | 59 | 2340 | 123071 | 110463829 |
| Migraine | 113.98 | 30.36 | 61 | 2338 | 171591 | 110415309 |
| Back pain | 90.27 | 30.36 | 70 | 2329 | 370926 | 110215974 |
| Headache | 55.80 | 30.36 | 81 | 2318 | 882296 | 109704604 |
| Pain | 35.23 | 30.36 | 69 | 2330 | 954886 | 109632014 |
| Toxicity to various agents | 32.98 | 30.36 | 46 | 2353 | 480509 | 110106391 |
| Anticholinergic syndrome | 32.28 | 30.36 | 9 | 2390 | 4271 | 110582629 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AA16 | 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 |
| MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018759 | Adrenergic Uptake Inhibitors |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:149553 | anticoronaviral agent |
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 |
|---|---|---|---|
| Major depressive disorder | indication | 370143000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.66 | 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 | Kd | 7.34 | WOMBAT-PK | IUPHAR | |||
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Kd | 8.07 | WOMBAT-PK | IUPHAR | |||
| Alpha-1A adrenergic receptor | GPCR | Ki | 6.38 | WOMBAT-PK | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 7.92 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 8.70 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.74 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.96 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7.42 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 7.22 | WOMBAT-PK | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.28 | PDSP | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 7.04 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.59 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000167275 | NUI |
| D01546 | KEGG_DRUG |
| C0013065 | UMLSCUI |
| CHEBI:36798 | CHEBI |
| CHEMBL1492500 | ChEMBL_ID |
| DB09167 | DRUGBANK_ID |
| CHEMBL1711280 | ChEMBL_ID |
| 5284550 | PUBCHEM_CID |
| 7549 | IUPHAR_LIGAND_ID |
| 897-15-4 | SECONDARY_CAS_RN |
| 142133 | RXNORM |
| 003960 | NDDF |
| 003961 | NDDF |
| 349856007 | SNOMEDCT_US |
| 396037001 | SNOMEDCT_US |
| 414047005 | SNOMEDCT_US |
| D004308 | MESH_DESCRIPTOR_UI |
| 1790 | INN_ID |
| W13O82Z7HL | UNII |
| W13O82Z7HL | INXIGHT DRUGS |
Pharmaceutical products:
None