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

Stem definition	Drug id	CAS RN
tricyclic compounds	951	113-53-1

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

dosulepin
dosulepine
dothiepin
prothiaden
prothiadene
dosulepin hydrochloride
dothiepin hydrochloride
dosulepin HCl
dothiepin HCl

A tricyclic antidepressant with some tranquilizing action.

Molecular weight: 295.44
Formula: C19H21NS
CLOGP: 4.53
LIPINSKI: 0
HAC: 1
HDO: 0
TPSA: 3.24
ALOGS: -5.71
ROTB: 3

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

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	49.02	30.93	44	1446	263371	63224161

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	239.20	73.40	43	495	4073	34952320
Migraine	177.21	73.40	43	495	17435	34938958
Neck pain	161.33	73.40	43	495	25306	34931087
Back pain	95.21	73.40	43	495	121746	34834647
Headache	74.87	73.40	43	495	200592	34755801
Pain	74.07	73.40	43	495	204632	34751761

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	156.88	30.24	42	2025	14460	79727861
Neck pain	89.18	30.24	42	2025	75375	79666946
Migraine	80.32	30.24	41	2026	87452	79654869
Back pain	54.45	30.24	52	2015	304128	79438193
Headache	33.26	30.24	60	2007	653712	79088609
Anticholinergic syndrome	32.21	30.24	9	2058	3602	79738719

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	D018663	Adrenergic Agents
MeSH PA	D018759	Adrenergic Uptake Inhibitors
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D000929	Antidepressive Agents, Tricyclic
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D014179	Neurotransmitter Uptake Inhibitors
MeSH PA	D011619	Psychotropic Drugs
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:149553	anticoronaviral drug

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 serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Kd	8.07		WOMBAT-PK	IUPHAR
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Kd	7.34		WOMBAT-PK	IUPHAR
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.59		WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	6.38		WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.92		WOMBAT-PK
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	8.70		WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	7.74		WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.96		WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	7.42		WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	7.22		WOMBAT-PK
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	7.04		WOMBAT-PK
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	5.28		PDSP

External reference:

ID	Source
N0000167275	NUI
D01546	KEGG_DRUG
C0013065	UMLSCUI
CHEBI:36798	CHEBI
CHEMBL1492500	ChEMBL_ID
DB09167	DRUGBANK_ID
CHEMBL108947	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
CHEMBL1711280	ChEMBL_ID
1790	INN_ID
W13O82Z7HL	UNII

Pharmaceutical products:

None