tianeptine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2650	72797-41-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tianeptine monosodium
tianeptine sodium
stablon
tianeptine
coaxil

Molecular weight: 436.95
Formula: C21H25ClN2O4S
CLOGP: 1.52
LIPINSKI: 0
HAC: 6
HDO: 2
TPSA: 86.71
ALOGS: -5.03
ROTB: 8

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

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
Overdose	68.21	40.42	34	960	115044	63372984
Intentional overdose	62.65	40.42	28	966	74124	63413904
Suicide attempt	54.63	40.42	24	970	60894	63427134
Drug interaction	48.82	40.42	35	959	229096	63258932

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	101.62	54.40	28	470	19905	34936528
Stress cardiomyopathy	78.81	54.40	15	483	2044	34954389

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
Serotonin syndrome	117.94	33.85	40	1373	44987	79697988
Overdose	51.66	33.85	35	1378	184171	79558804
Stress cardiomyopathy	50.20	33.85	15	1398	11151	79731824

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:35474	anti-anxiety agents
CHEBI has role	CHEBI:55322	mu-opioid agonists
CHEBI has role	CHEBI:65191	atypical antipsychotic agent

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	P35372	OPRM_HUMAN		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