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

Stem definition	Drug id	CAS RN
	1825	71320-77-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: moclobamide moclobemide auromid aurorix moclaime	A reversible inhibitor of monoamine oxidase type A (RIMA) that has antidepressive properties. Molecular weight: 268.74 Formula: C13H17ClN2O2 CLOGP: 1.97 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 41.57 ALOGS: -2.38 ROTB: 4

Molecule

Description

Molfile Inchi Smiles

Synonyms:

moclobamide
moclobemide
auromid
aurorix
moclaime

A reversible inhibitor of monoamine oxidase type A (RIMA) that has antidepressive properties.

Molecular weight: 268.74
Formula: C13H17ClN2O2
CLOGP: 1.97
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 41.57
ALOGS: -2.38
ROTB: 4

Drug dosage:

Dose	Unit	Route
0.30	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	75 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	4 mg/mL	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	10 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.50 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.10 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.77 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1990	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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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	110.74	52.22	33	933	28649	63459407
Drug interaction	61.79	52.22	40	926	229091	63258965
Apallic syndrome	58.21	52.22	10	956	711	63487345

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FDA Adverse Event Reporting System (Male)

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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	172.79	55.15	50	1005	19883	34935993
Intentional overdose	126.93	55.15	48	1007	43626	34912250
Physical deconditioning	104.02	55.15	20	1035	1339	34954537
Major depression	65.11	55.15	17	1038	4555	34951321
Suicide attempt	62.18	55.15	28	1027	39088	34916788
Dissociative disorder	55.67	55.15	10	1045	459	34955417

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FDA Adverse Event Reporting System (Geriatric)

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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	189.61	41.04	59	1539	44968	79697822
Drug interaction	86.46	41.04	69	1529	415114	79327676
Intentional overdose	74.14	41.04	38	1560	105922	79636868
Dissociative disorder	54.15	41.04	10	1588	811	79741979
Apallic syndrome	52.50	41.04	10	1588	958	79741832
Depressed mood	47.75	41.04	22	1576	48458	79694332
Toxicity to various agents	46.11	41.04	49	1549	421491	79321299
Electrocardiogram QT prolonged	45.26	41.04	26	1572	90360	79652430
Arrhythmia	42.85	41.04	22	1576	61250	79681540
Serum serotonin increased	41.77	41.04	7	1591	323	79742467

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06AG02	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Monoamine oxidase A inhibitors
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:78298	environmental contaminants
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D008996	Monoamine Oxidase Inhibitors
MeSH PA	D011619	Psychotropic Drugs

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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	13.45	acidic
pKa2	6.83	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Amine oxidase [flavin-containing] A	Enzyme	P21397	AOFA_HUMAN	INHIBITOR	Ki	8.30	CHEMBL	IUPHAR
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Kd	5.30	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme	P27338	AOFB_HUMAN		Ki	5.97	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.10	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme		AOFB_RAT		Ki	5.97	CHEMBL
Amine oxidase [flavin-containing] A	Enzyme		AOFA_RAT		Ki	8.30	CHEMBL
Amine oxidase [flavin-containing] A	Enzyme		AOFA_BOVIN		Ki	4.94	CHEMBL

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External reference:

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ID	Source
004179	NDDF
30121	RXNORM
321911007	SNOMEDCT_US
395800003	SNOMEDCT_US
4235	PUBCHEM_CID
4914	INN_ID
7428	IUPHAR_LIGAND_ID
C0066673	UMLSCUI
CHEBI:83531	CHEBI
CHEMBL86304	ChEMBL_ID

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Pharmaceutical products:

None