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

Stem definition	Drug id	CAS RN
substances of the imipramine group	1592	23047-25-8

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lofepramine
lopramine
lofepramine hydrochloride
lopramine hydrochloride
WHR-2908A
lofepramine HCl
lopramine HCl

A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.

Molecular weight: 418.97
Formula: C26H27ClN2O
CLOGP: 7.29
LIPINSKI: 1
HAC: 3
HDO: 0
TPSA: 23.55
ALOGS: -5.70
ROTB: 7

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

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	63.63	58.70	14	211	20078	79724085

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	D002491	Central Nervous System Agents
MeSH PA	D011619	Psychotropic Drugs
CHEBI has role	CHEBI:35469	antidepressants

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	P23975	SC6A2_HUMAN	INHIBITOR	Ki	8.27		WOMBAT-PK	IUPHAR
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Ki	7.16		WOMBAT-PK	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.70		WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7		WOMBAT-PK
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.44		WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	7.17		WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.48		WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.89		WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	6.47		WOMBAT-PK
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.70		PDSP
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.34		WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.34		PDSP

External reference:

ID	Source
N0000167255	NUI
D01285	KEGG_DRUG
C0023961	UMLSCUI
CHEBI:47782	CHEBI
CHEMBL87708	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
CHEMBL2106638	ChEMBL_ID

Pharmaceutical products:

None