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tianeptine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2650 | 72797-41-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 37.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 99 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.05 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.40 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK14,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 | 42 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,MAP2K6,MAPK7,PDK4,STK33,TEK | 8 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
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 |
|---|---|---|---|---|---|---|
| Persistent genital arousal disorder | 162.65 | 42.46 | 24 | 1291 | 676 | 90626456 |
| Overdose | 77.28 | 42.46 | 40 | 1275 | 157669 | 90469463 |
| Drug interaction | 75.90 | 42.46 | 48 | 1267 | 276405 | 90350727 |
| Intentional overdose | 61.36 | 42.46 | 29 | 1286 | 93805 | 90533327 |
| Disturbance in sexual arousal | 59.99 | 42.46 | 9 | 1306 | 283 | 90626849 |
| Suicide attempt | 54.54 | 42.46 | 25 | 1290 | 75374 | 90551758 |
| Perineal pain | 53.77 | 42.46 | 9 | 1306 | 574 | 90626558 |
| Female reproductive tract disorder | 52.98 | 42.46 | 9 | 1306 | 627 | 90626505 |
| Genital pain | 51.41 | 42.46 | 9 | 1306 | 749 | 90626383 |
| Crush syndrome | 44.50 | 42.46 | 7 | 1308 | 302 | 90626830 |
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 |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 93.06 | 48.46 | 28 | 606 | 25817 | 42594884 |
| Stress cardiomyopathy | 73.60 | 48.46 | 15 | 619 | 2770 | 42617931 |
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 |
|---|---|---|---|---|---|---|
| Persistent genital arousal disorder | 144.74 | 36.16 | 22 | 1829 | 654 | 110586794 |
| Serotonin syndrome | 109.36 | 36.16 | 40 | 1811 | 59113 | 110528335 |
| Overdose | 61.99 | 36.16 | 42 | 1809 | 233752 | 110353696 |
| Drug interaction | 48.20 | 36.16 | 50 | 1801 | 500133 | 110087315 |
| Stress cardiomyopathy | 45.89 | 36.16 | 15 | 1836 | 15791 | 110571657 |
| Crush syndrome | 41.77 | 36.16 | 7 | 1844 | 388 | 110587060 |
| Disturbance in sexual arousal | 41.58 | 36.16 | 7 | 1844 | 399 | 110587049 |
| Female reproductive tract disorder | 40.10 | 36.16 | 7 | 1844 | 495 | 110586953 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AX14 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D000929 | Antidepressive Agents, Tricyclic |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:55322 | μ-opioid receptor agonist |
| CHEBI has role | CHEBI:65191 | second generation antipsychotic |
Related Drugs by ATC class:
N06AX Other antidepressants 28 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.76 | acidic |
| pKa2 | 6.85 | 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 | Ki | 6.42 | PDSP |
External reference:
| ID | Source |
|---|---|
| D02575 | KEGG_DRUG |
| 30123-17-2 | SECONDARY_CAS_RN |
| C0076652 | UMLSCUI |
| CHEBI:91749 | CHEBI |
| CHEMBL1289110 | ChEMBL_ID |
| DB09289 | DRUGBANK_ID |
| C050504 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7558 | IUPHAR_LIGAND_ID |
| 4906 | INN_ID |
| 0T493YFU8O | UNII |
| 68870 | PUBCHEM_CID |
| 38252 | RXNORM |
| 005515 | NDDF |
| 005516 | NDDF |
| 1172815007 | SNOMEDCT_US |
| 703713005 | SNOMEDCT_US |
| 703714004 | SNOMEDCT_US |
Pharmaceutical products:
None