Details of the Drug

General Information of Drug (ID: DMOJZQ9)

• Drug Name: Loperamide
• Synonyms: Ioperamide; Loperacap; Loperamida; Loperamidum; Kaopectate II; Loperamide Monohydrochloride; Pepto Diarrhea Control; Apo-Loperamide; Diamide (TN); Diarr-Eze; Dimor (TN); Imodium (TN); Imodium A-D Caplets; Loperamida [INN-Spanish]; Loperamide (INN); Loperamide [INN:BAN]; Loperamidum [INN-Latin]; Lopex (TN); Maalox Anti-Diarrheal; Nu-Loperamide; PMS-Loperamide; Pepto (TN); R-18553; Rho-Loperamide

Indication

Disease Entry	ICD 11	Status	REF
Diarrhea	ME05.1	Approved	[1]
Traveler's diarrhea	ME05.1	Approved	[2]
Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[3]
Severe acute respiratory syndrome (SARS)	1D65	Preclinical	[3]

• Therapeutic Class: Antidiarrheals
• Affected Organisms: Humans and other mammals
• ATC Code:
  A07DA03: Loperamide
  A07DA: Antipropulsives
  A07D: ANTIPROPULSIVES
  A07: ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
  A: ALIMENTARY TRACT AND METABOLISM
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 477
  Logarithm of the Partition Coefficient (xlogp); 5
  Rotatable Bond Count (rotbonds); 7
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 3
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
  Elimination: 0.5% of drug is excreted from urine in the unchanged form [4]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.4791 micromolar/kg/day [5]
  Water Solubility: The ability of drug to dissolve in water is measured as 1.4 mg/mL [4]
• Chemical Identifiers:
  Formula: C29H33ClN2O2
  IUPAC Name: 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide
  Canonical SMILES: CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4
  InChI: InChI=1S/C29H33ClN2O2/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23/h3-16,34H,17-22H2,1-2H3
  InChIKey: RDOIQAHITMMDAJ-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 3955
  ChEBI ID: CHEBI:6532
  CAS Number: 53179-11-6
  UNII: 6X9OC3H4II
  DrugBank ID: DB00836
  TTD ID: D0CS2F
  VARIDT ID: DR00171
  INTEDE ID: DR0974
  ACDINA ID: D00373
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Opioid receptor delta (OPRD1)	TT27RFC	OPRD_HUMAN	Binder	[6]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[7]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[8]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Substrate	[9]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Substrate	[9]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Substrate	[9]
Oxygen-insensitive NADPH nitroreductase A (nfsA)	DEDPI65	NFSA_ECOLI	Substrate	[10]

Molecular Expression Atlas of This Drug

• The Studied Disease: Diarrhea
• ICD Disease Classification: ME05.1

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Opioid receptor delta (OPRD1)	DTT	OPRD1	5.52E-01	0.03	0.23
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.83E-01	4.69E-02	1.89E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	3.17E-01	-6.95E-02	-2.88E-01
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	5.79E-01	-1.30E-02	-9.78E-02
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	5.64E-01	2.36E-02	1.75E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	6.06E-01	-2.42E-02	-1.64E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Loperamide (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Ivosidenib.	Acute myeloid leukaemia [2A60]	[11]
Midostaurin	DMI6E0R	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Midostaurin.	Acute myeloid leukaemia [2A60]	[11]
Idarubicin	DMM0XGL	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Idarubicin.	Acute myeloid leukaemia [2A60]	[11]
Gilteritinib	DMTI0ZO	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Gilteritinib.	Acute myeloid leukaemia [2A60]	[11]
Oliceridine	DM6MDCF	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Oliceridine.	Acute pain [MG31]	[11]
Mepyramine	DMB4SFH	Moderate	Additive antimotility effects by the combination of Loperamide and Mepyramine.	Allergic/hypersensitivity disorder [4A80-4A8Z]	[12]
Phenyltoloxamine	DMKAEQW	Moderate	Additive antimotility effects by the combination of Loperamide and Phenyltoloxamine.	Allergic/hypersensitivity disorder [4A80-4A8Z]	[12]
Rivastigmine	DMG629M	Moderate	Antagonize the effect of Loperamide when combined with Rivastigmine.	Alzheimer disease [8A20]	[13]
Donepezil	DMIYG7Z	Moderate	Antagonize the effect of Loperamide when combined with Donepezil.	Alzheimer disease [8A20]	[13]
Metronidazole	DMTIVEN	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Metronidazole.	Amoebiasis [1A36]	[11]
Bepridil	DM0RKS4	Major	Decreased clearance of Loperamide due to the transporter inhibition by Bepridil.	Angina pectoris [BA40]	[14]
Bedaquiline	DM3906J	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[11]
Cilostazol	DMZMSCT	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Cilostazol.	Arterial occlusive disease [BD40]	[11]
Posaconazole	DMUL5EW	Major	Decreased clearance of Loperamide due to the transporter inhibition by Posaconazole.	Aspergillosis [1F20]	[11]
Terbutaline	DMD4381	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Terbutaline.	Asthma [CA23]	[11]
Lisdexamfetamine	DM6W8V5	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Lisdexamfetamine.	Attention deficit hyperactivity disorder [6A05]	[11]
Ofloxacin	DM0VQN3	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Ofloxacin.	Bacterial infection [1A00-1C4Z]	[11]
Clarithromycin	DM4M1SG	Major	Decreased metabolism of Loperamide caused by Clarithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Sparfloxacin	DMB4HCT	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Sparfloxacin.	Bacterial infection [1A00-1C4Z]	[11]
Gemifloxacin	DMHT34O	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Gemifloxacin.	Bacterial infection [1A00-1C4Z]	[11]
Norfloxacin	DMIZ6W2	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Norfloxacin.	Bacterial infection [1A00-1C4Z]	[11]
Levofloxacin	DMS60RB	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Levofloxacin.	Bacterial infection [1A00-1C4Z]	[11]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Loperamide caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Lomefloxacin	DMVRH9C	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Lomefloxacin.	Bacterial infection [1A00-1C4Z]	[11]
Telithromycin	DMZ4P3A	Major	Decreased metabolism of Loperamide caused by Telithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Retigabine	DMGNYIH	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Retigabine.	Behcet disease [4A62]	[11]
Erdafitinib	DMI782S	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Erdafitinib.	Bladder cancer [2C94]	[15]
Eribulin	DM1DX4Q	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Eribulin.	Breast cancer [2C60-2C6Y]	[11]
Lapatinib	DM3BH1Y	Major	Decreased clearance of Loperamide due to the transporter inhibition by Lapatinib.	Breast cancer [2C60-2C6Y]	[14]
Tucatinib	DMBESUA	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Tucatinib.	Breast cancer [2C60-2C6Y]	[16]
Olodaterol	DM62B78	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Olodaterol.	Chronic obstructive pulmonary disease [CA22]	[11]
Dihydrocodeine	DMB0FWL	Moderate	Additive CNS depression effects by the combination of Loperamide and Dihydrocodeine.	Chronic pain [MG30]	[17]
Halothane	DM80OZ5	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Halothane.	Corneal disease [9A76-9A78]	[11]
Sevoflurane	DMC9O43	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Sevoflurane.	Corneal disease [9A76-9A78]	[11]
Probucol	DMVZQ2M	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Probucol.	Coronary atherosclerosis [BA80]	[11]
Clofazimine	DMEBOFW	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Clofazimine.	Crohn disease [DD70]	[11]
Pasireotide	DMHM7JS	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Pasireotide.	Cushing syndrome [5A70]	[11]
Osilodrostat	DMIJC9X	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Osilodrostat.	Cushing syndrome [5A70]	[11]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Loperamide caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[18]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Loperamide and Ethanol.	Cystitis [GC00]	[19]
Sertraline	DM0FB1J	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Sertraline.	Depression [6A70-6A7Z]	[11]
Cyclobenzaprine	DM1YBRM	Moderate	Additive antimotility effects by the combination of Loperamide and Cyclobenzaprine.	Depression [6A70-6A7Z]	[12]
Nefazodone	DM4ZS8M	Major	Decreased metabolism of Loperamide caused by Nefazodone mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[11]
Escitalopram	DMFK9HG	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Escitalopram.	Depression [6A70-6A7Z]	[11]
OPC-34712	DMHG57U	Moderate	Additive antimotility effects by the combination of Loperamide and OPC-34712.	Depression [6A70-6A7Z]	[12]
Clomipramine	DMINRKW	Moderate	Additive antimotility effects by the combination of Loperamide and Clomipramine.	Depression [6A70-6A7Z]	[12]
Doxepin	DMPI98T	Moderate	Additive antimotility effects by the combination of Loperamide and Doxepin.	Depression [6A70-6A7Z]	[12]
Maprotiline	DMPWB7T	Moderate	Additive antimotility effects by the combination of Loperamide and Maprotiline.	Depression [6A70-6A7Z]	[12]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Loperamide and Esketamine.	Depression [6A70-6A7Z]	[20]
Mepenzolate	DM8YU2F	Moderate	Additive antimotility effects by the combination of Loperamide and Mepenzolate.	Digestive system disease [DE2Z]	[12]
Oxybutynine	DMJPBAX	Moderate	Additive antimotility effects by the combination of Loperamide and Oxybutynine.	Discovery agent [N.A.]	[12]
Tetrabenazine	DMYWQ0O	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Tetrabenazine.	Dissociative neurological symptom disorder [6B60]	[11]
Deutetrabenazine	DMUPFLI	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Deutetrabenazine.	Dystonic disorder [8A02]	[11]
Ingrezza	DMVPLNC	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Ingrezza.	Dystonic disorder [8A02]	[11]
Solifenacin	DMG592Q	Moderate	Additive antimotility effects by the combination of Loperamide and Solifenacin.	Functional bladder disorder [GC50]	[12]
Tolterodine	DMSHPW8	Moderate	Additive antimotility effects by the combination of Loperamide and Tolterodine.	Functional bladder disorder [GC50]	[12]
Itraconazole	DMCR1MV	Major	Decreased metabolism of Loperamide caused by Itraconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[11]
Ketoconazole	DMPZI3Q	Major	Decreased metabolism of Loperamide caused by Ketoconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[11]
Sunitinib	DMCBJSR	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Sunitinib.	Gastrointestinal stromal tumour [2B5B]	[11]
Boceprevir	DMBSHMF	Major	Decreased clearance of Loperamide due to the transporter inhibition by Boceprevir.	Hepatitis virus infection [1E50-1E51]	[11]
Telaprevir	DMMRV29	Major	Decreased metabolism of Loperamide caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[11]
GS-5885	DMSL3DX	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by GS-5885.	Hepatitis virus infection [1E50-1E51]	[21]
Fostemsavir	DM50ILT	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Saquinavir	DMG814N	Moderate	Altered absorption of Loperamide due to GI dynamics variation caused by Saquinavir.	Human immunodeficiency virus disease [1C60-1C62]	[22]
Rilpivirine	DMJ0QOW	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Rilpivirine.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Atazanavir	DMSYRBX	Major	Decreased clearance of Loperamide due to the transporter inhibition by Atazanavir.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Gemfibrozil	DMD8Q3J	Major	Decreased metabolism of Loperamide caused by Gemfibrozil mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[11]
BMS-201038	DMQTAGO	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by BMS-201038.	Hyper-lipoproteinaemia [5C80]	[23]
Conivaptan	DM1V329	Major	Decreased clearance of Loperamide due to the transporter inhibition by Conivaptan.	Hypo-osmolality/hyponatraemia [5C72]	[11]
Tolvaptan	DMIWFRL	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Tolvaptan.	Hypo-osmolality/hyponatraemia [5C72]	[20]
Belladonna	DM2RBWK	Moderate	Additive antimotility effects by the combination of Loperamide and Belladonna.	Infectious gastroenteritis/colitis [1A40]	[12]
Physostigmine	DM2N0TO	Moderate	Antagonize the effect of Loperamide when combined with Physostigmine.	Lips/oral mucosa miscellaneous disorder [DA02]	[13]
Crizotinib	DM4F29C	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Crizotinib.	Lung cancer [2C25]	[11]
Ceritinib	DMB920Z	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Ceritinib.	Lung cancer [2C25]	[11]
Osimertinib	DMRJLAT	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Osimertinib.	Lung cancer [2C25]	[11]
Capmatinib	DMYCXKL	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Capmatinib.	Lung cancer [2C25]	[24]
Selpercatinib	DMZR15V	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Selpercatinib.	Lung cancer [2C25]	[11]
Lumefantrine	DM29GAD	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Lumefantrine.	Malaria [1F40-1F45]	[11]
Halofantrine	DMOMK1V	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Halofantrine.	Malaria [1F40-1F45]	[11]
Hydroxychloroquine	DMSIVND	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Hydroxychloroquine.	Malaria [1F40-1F45]	[11]
Primaquine	DMWQ16I	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Primaquine.	Malaria [1F40-1F45]	[11]
Inotuzumab ozogamicin	DMAC130	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Inotuzumab ozogamicin.	Malignant haematopoietic neoplasm [2B33]	[11]
Idelalisib	DM602WT	Major	Decreased metabolism of Loperamide caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[11]
Arsenic trioxide	DM61TA4	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Arsenic trioxide.	Mature B-cell lymphoma [2A85]	[11]
Ibrutinib	DMHZCPO	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Ibrutinib.	Mature B-cell lymphoma [2A85]	[17]
LGX818	DMNQXV8	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and LGX818.	Melanoma [2C30]	[11]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Loperamide and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[25]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[26]
Flibanserin	DM70DTN	Major	Decreased clearance of Loperamide due to the transporter inhibition by Flibanserin.	Mood disorder [6A60-6E23]	[14]
Panobinostat	DM58WKG	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Panobinostat.	Multiple myeloma [2A83]	[11]
Siponimod	DM2R86O	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Siponimod.	Multiple sclerosis [8A40]	[11]
Fingolimod	DM5JVAN	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Fingolimod.	Multiple sclerosis [8A40]	[11]
Ozanimod	DMT6AM2	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Ozanimod.	Multiple sclerosis [8A40]	[11]
Romidepsin	DMT5GNL	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Romidepsin.	Mycosis fungoides [2B01]	[11]
Dasatinib	DMJV2EK	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Dasatinib.	Myeloproliferative neoplasm [2A20]	[11]
Phenindamine	DMDTC7R	Moderate	Additive antimotility effects by the combination of Loperamide and Phenindamine.	Nasopharyngitis [CA00]	[12]
Dimenhydrinate	DM264B3	Moderate	Additive antimotility effects by the combination of Loperamide and Dimenhydrinate.	Nausea/vomiting [MD90]	[12]
Promethazine	DM6I5GR	Moderate	Additive antimotility effects by the combination of Loperamide and Promethazine.	Nausea/vomiting [MD90]	[12]
Rolapitant	DM8XP26	Moderate	Decreased clearance of Loperamide due to the transporter inhibition by Rolapitant.	Nausea/vomiting [MD90]	[27]
Cyclizine	DM9G7BS	Moderate	Additive antimotility effects by the combination of Loperamide and Cyclizine.	Nausea/vomiting [MD90]	[12]
Granisetron	DMIUW25	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Granisetron.	Nausea/vomiting [MD90]	[11]
Ondansetron	DMOTQ1I	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Ondansetron.	Nausea/vomiting [MD90]	[11]
Entrectinib	DMMPTLH	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Entrectinib.	Non-small cell lung cancer [2C25]	[11]
Levomethadyl Acetate	DM06HG5	Moderate	Additive antimotility effects by the combination of Loperamide and Levomethadyl Acetate.	Opioid use disorder [6C43]	[17]
Lofexidine	DM1WXA6	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Lofexidine.	Opioid use disorder [6C43]	[11]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Loperamide and Apraclonidine.	Optic nerve disorder [9C40]	[28]
Rucaparib	DM9PVX8	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Rucaparib.	Ovarian cancer [2C73]	[11]
Flavoxate	DMKV4NL	Moderate	Additive antimotility effects by the combination of Loperamide and Flavoxate.	Pain [MG30-MG3Z]	[12]
Nalbuphine	DMOSQGU	Moderate	Additive CNS depression effects by the combination of Loperamide and Nalbuphine.	Pain [MG30-MG3Z]	[17]
Buprenorphine	DMPRI8G	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Buprenorphine.	Pain [MG30-MG3Z]	[11]
Hydrocodone	DMQ2JO5	Moderate	Additive CNS depression effects by the combination of Loperamide and Hydrocodone.	Pain [MG30-MG3Z]	[17]
Triclabendazole	DMPWGBR	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Triclabendazole.	Parasitic worm infestation [1F90]	[11]
Pimavanserin	DMR7IVC	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Pimavanserin.	Parkinsonism [8A00]	[11]
Orphenadrine	DMW542E	Moderate	Additive antimotility effects by the combination of Loperamide and Orphenadrine.	Parkinsonism [8A00]	[12]
Ranitidine	DM0GUSX	Major	Decreased clearance of Loperamide due to the transporter inhibition by Ranitidine.	Peptic ulcer [DA61]	[11]
Methylscopolamine	DM5VWOB	Moderate	Additive antimotility effects by the combination of Loperamide and Methylscopolamine.	Peptic ulcer [DA61]	[12]
Macimorelin	DMQYJIR	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Macimorelin.	Pituitary gland disorder [5A60-5A61]	[11]
Lefamulin	DME6G97	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Lefamulin.	Pneumonia [CA40]	[11]
Lonafarnib	DMGM2Z6	Major	Decreased clearance of Loperamide due to the transporter inhibition by Lonafarnib.	Premature ageing appearance [LD2B]	[29]
Degarelix	DM3O8QY	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Degarelix.	Prostate cancer [2C82]	[11]
ABIRATERONE	DM8V75C	Major	Decreased metabolism of Loperamide caused by ABIRATERONE mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[11]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Loperamide caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[30]
Bicalutamide	DMZMSPF	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Bicalutamide.	Prostate cancer [2C82]	[11]
Levomepromazine	DMIKFEL	Moderate	Additive antimotility effects by the combination of Loperamide and Levomepromazine.	Psychotic disorder [6A20-6A25]	[12]
Gatifloxacin	DMSL679	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Gatifloxacin.	Respiratory infection [CA07-CA4Z]	[11]
Quetiapine	DM1N62C	Moderate	Additive antimotility effects by the combination of Loperamide and Quetiapine.	Schizophrenia [6A20]	[12]
Aripiprazole	DM3NUMH	Moderate	Additive antimotility effects by the combination of Loperamide and Aripiprazole.	Schizophrenia [6A20]	[12]
Iloperidone	DM6AUFY	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Iloperidone.	Schizophrenia [6A20]	[11]
Paliperidone	DM7NPJS	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Paliperidone.	Schizophrenia [6A20]	[11]
Perphenazine	DMA4MRX	Moderate	Additive antimotility effects by the combination of Loperamide and Perphenazine.	Schizophrenia [6A20]	[12]
Molindone	DMAH70G	Moderate	Additive antimotility effects by the combination of Loperamide and Molindone.	Schizophrenia [6A20]	[12]
Thiothixene	DMDINC4	Moderate	Additive antimotility effects by the combination of Loperamide and Thiothixene.	Schizophrenia [6A20]	[12]
Amisulpride	DMSJVAM	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Amisulpride.	Schizophrenia [6A20]	[11]
Asenapine	DMSQZE2	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Asenapine.	Schizophrenia [6A20]	[11]
Vardenafil	DMTBGW8	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Vardenafil.	Sexual dysfunction [HA00-HA01]	[11]
LEE011	DMMX75K	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and LEE011.	Solid tumour/cancer [2A00-2F9Z]	[11]
Vandetanib	DMRICNP	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Vandetanib.	Solid tumour/cancer [2A00-2F9Z]	[11]
Triptorelin	DMTK4LS	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Triptorelin.	Solid tumour/cancer [2A00-2F9Z]	[11]
Doxorubicin	DMVP5YE	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Doxorubicin.	Solid tumour/cancer [2A00-2F9Z]	[11]
Pitolisant	DM8RFNJ	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Pitolisant.	Somnolence [MG42]	[11]
Telavancin	DM58VQX	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Telavancin.	Staphylococcal/streptococcal disease [1B5Y]	[11]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Loperamide caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[31]
Lenvatinib	DMB1IU4	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Lenvatinib.	Thyroid cancer [2D10]	[11]
Papaverine	DMCA9QP	Major	Increased risk of prolong QT interval by the combination of Loperamide and Papaverine.	Tonus and reflex abnormality [MB47]	[32]
Tacrolimus	DMZ7XNQ	Major	Decreased clearance of Loperamide due to the transporter inhibition by Tacrolimus.	Transplant rejection [NE84]	[14]
Pramlintide	DM0EZ9Q	Moderate	Altered absorption of Loperamide due to GI dynamics variation caused by Pramlintide.	Type-1/2 diabete [5A10-5A11]	[33]
Chlorpheniramine	DM5URA2	Moderate	Additive antimotility effects by the combination of Loperamide and Chlorpheniramine.	Vasomotor/allergic rhinitis [CA08]	[12]
Methdilazine	DMAUHQX	Moderate	Additive antimotility effects by the combination of Loperamide and Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[12]
Trimeprazine	DMEMV9D	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[11]
Acrivastine	DMTIGA0	Moderate	Additive antimotility effects by the combination of Loperamide and Acrivastine.	Vasomotor/allergic rhinitis [CA08]	[12]
Procainamide	DMNMXR8	Moderate	Additive antimotility effects by the combination of Loperamide and Procainamide.	Ventricular tachyarrhythmia [BC71]	[12]
Propafenone	DMPIBJK	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Propafenone.	Ventricular tachyarrhythmia [BC71]	[11]
Flecainide	DMSQDLE	Moderate	Increased risk of prolong QT interval by the combination of Loperamide and Flecainide.	Ventricular tachyarrhythmia [BC71]	[11]
Amiodarone	DMUTEX3	Major	Decreased clearance of Loperamide due to the transporter inhibition by Amiodarone.	Ventricular tachyarrhythmia [BC71]	[14]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Acesulfame	E00341	36573	Flavoring agent
Allura red AC dye	E00338	33258	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sucralose	E00370	71485	Flavoring agent
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Brushite	E00392	104805	Diluent
Butylhydroxyanisole	E00308	24667	Antimicrobial preservative; Antioxidant
Calcium hydrogenphosphate	E00294	24441	Diluent
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Elemental iron	E00280	23925	Other agent
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Gelatin	E00630	Not Available	Other agent
Glycerin	E00026	753	Antimicrobial preservative; Emollient; Flavoring agent; Humectant; Lubricant; Plasticizing agent; Solvent; Suppository base; Tonicity agent; Viscosity-controlling agent
Glyceryl monocaprylate	E00458	3033877	Emollient; Emulsifying agent; Surfactant
Hydrogenated polyoxyl 40 castor oil	E00662	Not Available	Emulsifying agent; Solubilizing agent; Surfactant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Tristearin	E00207	11146	Emollient; Viscosity-controlling agent
Water	E00035	962	Solvent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Loperamide 2 mg tablet	2 mg	Chewable Tablet	Oral
Loperamide 2 mg tablet	2 mg	Oral Tablet	Oral
Loperamide 2 mg capsule	2 mg	Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] Loperamide FDA Label
• [3] Screening of an FDA-approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture Antimicrob Agents Chemother. 2014 Aug;58(8):4875-84.
• [4] BDDCS applied to over 900 drugs
• [5] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [6] Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8.
• [7] In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos. 2008 Feb;36(2):268-75.
• [8] Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8.
• [9] Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81.
• [10] Reduction of the prodrug loperamide oxide to its active drug loperamide in the gut of rats, dogs, and humans. Drug Metab Dispos. 1995 Mar;23(3):354-62.
• [11] Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747]
• [12] Eronen M, Putkonen H, Hallikainen T, Vartiainen H "Lethal gastroenteritis associated with clozapine and loperamide." Am J Psychiatry 160 (2003): 2242-2243. [PMID: 14638602]
• [13] Beers MH, Ouslander JG, Rollingher I, Reuben DB, Brooks J, Beck JC "Explicit criteria for determining inappropriate medication use in nursing home residents." Arch Intern Med 151 (1991): 1825-32. [PMID: 1888249]
• [14] Adachi Y, Suzuki H, Sugiyama Y "Quantitative evaluation of the function of small intestinal P-glycoprotein: comparative studies between in Situ and in Vivo." Pharm Res 20 (2003): 1163-9. [PMID: 12948013]
• [15] Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
• [16] Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
• [17] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [18] Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
• [19] Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
• [20] Cerner Multum, Inc. "Australian Product Information.".
• [21] Product Information. Harvoni (ledipasvir-sofosbuvir). Gilead Sciences, Foster City, CA.
• [22] John L, Marra F, Ensom MH "Role of therapeutic drug monitoring for protease inhibitors." Ann Pharmacother 35 (2001): 745-54. [PMID: 11408994]
• [23] Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
• [24] Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
• [25] Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
• [26] Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
• [27] Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
• [28] Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
• [29] Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
• [30] Benoist G, van Oort I, et al "Drug-drug interaction potential in men treated with enzalutamide: Mind the gap." Br J Clin Pharmacol 0 (2017): epub. [PMID: 28881501]
• [31] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
• [32] Goto M, Sato M, Kitzazawa H, et.al "Papaverine-induced QT interval prolongation and ventricular fibrillation in a patient with a history of drug-induced QT prolongation." Intern Med 53 (2014): 1629-31. [PMID: 25088875]
• [33] Product Information. Symlin (pramlintide). Amphastar Pharmaceuticals Inc, South El Monte, CA.