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

Stem definition	Drug id	CAS RN
	1599	53179-11-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: loperamide loperamide hydrochloride imodium loperamide HCl	One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally. Molecular weight: 477.05 Formula: C29H33ClN2O2 CLOGP: 4.66 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 43.78 ALOGS: -5.74 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

loperamide
loperamide hydrochloride
imodium
loperamide HCl

One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.

Molecular weight: 477.05
Formula: C29H33ClN2O2
CLOGP: 4.66
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 43.78
ALOGS: -5.74
ROTB: 7

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.48 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1976	FDA	MCNEIL CONS

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
Diarrhoea	1016.61	10.86	2785	89437	712581	62684219
Dehydration	328.32	10.86	756	91466	172598	63224202
Maternal exposure during pregnancy	239.26	10.86	22	92200	220040	63176760
Systemic lupus erythematosus	237.92	10.86	17	92205	208901	63187899
Hand deformity	211.67	10.86	4	92218	159453	63237347
Vomiting	179.18	10.86	1406	90816	558211	62838589
Pneumonia viral	175.26	10.86	121	92101	7801	63388999
Hypomania	174.74	10.86	111	92111	6219	63390581
Colitis	174.18	10.86	278	91944	48250	63348550
Hypokalaemia	172.88	10.86	431	91791	103373	63293427

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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
Diarrhoea	628.41	11.21	1685	53984	388227	34513035
Torsade de pointes	281.14	11.21	163	55506	7046	34894216
Electrocardiogram QT prolonged	220.48	11.21	298	55371	40654	34860608
Electrocardiogram QRS complex prolonged	207.84	11.21	117	55552	4777	34896485
Drug abuse	200.52	11.21	469	55200	98627	34802635
Dehydration	190.67	11.21	545	55124	129424	34771838
Intentional overdose	160.72	11.21	266	55403	43408	34857854
Colitis	154.04	11.21	241	55428	37509	34863753
Ventricular tachycardia	146.95	11.21	196	55473	26383	34874879
Abdominal pain	113.32	11.21	538	55131	163080	34738182

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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
Diarrhoea	1109.12	10.32	3455	121777	877034	78742122
Dehydration	407.29	10.32	1075	124157	247112	79372044
Torsade de pointes	381.87	10.32	284	124948	19028	79600128
Colitis	319.56	10.32	479	124753	72828	79546328
Electrocardiogram QT prolonged	317.42	10.32	535	124697	89851	79529305
Ventricular tachycardia	290.86	10.32	344	124888	41591	79577565
Drug abuse	255.76	10.32	694	124538	161997	79457159
Electrocardiogram QRS complex prolonged	193.59	10.32	150	125082	10683	79608473
Vomiting	191.64	10.32	1736	123496	664092	78955064
Abdominal pain	187.49	10.32	1148	124084	388421	79230735

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A07DA03	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS ANTIPROPULSIVES Antipropulsives
ATC	A07DA53	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS ANTIPROPULSIVES Antipropulsives
CHEBI has role	CHEBI:55322	mu-opioid agonists
CHEBI has role	CHEBI:55323	antidiarrheal drug
CHEBI has role	CHEBI:149553	anticoronaviral drug
FDA EPC	N0000175690	Opioid Agonist
FDA MoA	N0000000174	Opioid Agonists
MeSH PA	D000930	Antidiarrheals
MeSH PA	D005765	Gastrointestinal Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Traveler's diarrhea	indication	11840006
Diarrhea	indication	62315008
Diarrhea Secondary to Inflammatory Bowel Disease	indication
Chemotherapy-Induced Diarrhea	off-label use
Infectious diarrheal disease	contraindication	19213003	DOID:13250
Paralytic ileus	contraindication	55525008	DOID:8442
Hemorrhagic diarrhea	contraindication	95545007
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.78	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
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	Ki	8.82	WOMBAT-PK	CHEMBL
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN		IC50	6.62	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.24	CHEMBL
Glutamate receptor ionotropic, NMDA 2A	Ion channel	Q12879	NMDE1_HUMAN				WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.58	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.93	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.58	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.34	DRUG MATRIX
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		IC50	5.70	WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.52	DRUG MATRIX

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External reference:

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ID	Source
001154	NDDF
004545	NDDF
116726003	SNOMEDCT_US
151889	RXNORM
2069	MMSL
2336	MMSL
3098	INN_ID
34552-83-5	SECONDARY_CAS_RN
387040009	SNOMEDCT_US
3955	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
anti diarrheal	HUMAN OTC DRUG LABEL	1	0113-2224	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
anti diarrheal	HUMAN OTC DRUG LABEL	1	0363-1010	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
anti diarrheal	HUMAN OTC DRUG LABEL	1	0363-1010	TABLET, FILM COATED	2 mg	ORAL	ANDA	16 sections
Anti Diarrheal	HUMAN OTC DRUG LABEL	1	0363-2022	SOLUTION	1 mg	ORAL	ANDA	16 sections
anti diarrheal and anti gas	HUMAN OTC DRUG LABEL	2	0363-1830	TABLET	2 mg	ORAL	ANDA	16 sections
anti diarrheal and anti gas	HUMAN OTC DRUG LABEL	2	0363-1830	TABLET	2 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	0363-0375	TABLET	2 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	0363-0375	TABLET	2 mg	ORAL	ANDA	16 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	0363-1176	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	17 sections
Anti-Diarrheal	HUMAN OTC DRUG LABEL	1	0363-1176	CAPSULE, LIQUID FILLED	2 mg	ORAL	NDA	17 sections

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