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Economics

Properties

Spectra

Taxonomy

Loperamide

Targets (7)Enzymes (4)Transporters (1)Biointeractions (12)

Identification

Name

Loperamide

Accession Number

DB00836 (APRD00275)

Type

Small Molecule

Groups

Approved

Description

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. [PubChem]

Structure

Similar Structures

Synonyms

Loperamid
Loperamida
Lopéramide
Loperamidum

External IDs

PJ 185 / R 18553

Product Ingredients

Ingredient	UNII	CAS	InChI Key
Loperamide hydrochloride	77TI35393C	34552-83-5	PGYPOBZJRVSMDS-UHFFFAOYSA-N
Loperamide oxide	NG66S4H2RL	106900-12-3	KXVSBTJVTUVNPM-UHFFFAOYSA-N

Product Images

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Loperamide Hydrochloride	Solution	2 mg/10mL	Oral	Cardinal Health	1992-04-30	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Pd Rx Pharmaceuticals, Inc.	1991-09-18	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Dispensing Solutions, Inc.	2011-09-23	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Red Pharm Drug, Inc.	2016-04-13	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Remedy Repack	2013-03-18	2016-12-14
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Stat Rx USA	1993-05-01	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Mylan Institutional	1997-03-10	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Nucare Pharmaceuticals, Inc.	1993-05-01	Not applicable
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Lake Erie Medical Dba Quality Care Produts Llc	2010-10-01	2017-02-11
Loperamide Hydrochloride	Capsule	2 mg/1	Oral	Cardinal Health	2011-07-27	Not applicable

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
7 Select Anti Diarrheal	Tablet, film coated	2 mg/1	Oral	7 Eleven	2014-08-05	Not applicable
A D	Tablet, film coated	2 mg/1	Oral	Western Family Foods	2003-04-10	Not applicable
A D	Tablet, film coated	2 mg/1	Oral	Western Family Foods	2003-02-25	Not applicable
Alti-loperamide - 2mg Caplet	Tablet	2 mg	Oral	Altimed Pharma Inc.	1995-12-31	1997-08-14
Anti Diarrheal	Tablet, film coated	2 mg/1	Oral	Cvs Health	2003-02-24	Not applicable
Anti Diarrheal	Tablet, film coated	2 mg/1	Oral	Hyvee	2003-03-21	Not applicable
Anti Diarrheal	Tablet	2 mg/1	Oral	Sam's West, Inc	2005-05-03	Not applicable
Anti Diarrheal	Tablet, film coated	2 mg/1	Oral	Kroger	2003-03-31	Not applicable
Anti Diarrheal	Tablet	2 mg/1	Oral	Lnk International, Inc.	2005-05-03	Not applicable
Anti Diarrheal	Tablet	2 mg/1	Oral	Harmon Store Inc.	2005-05-03	Not applicable

Unapproved/Other Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Gadavyt Loperamide HCl	Liquid	1 mg/5mL	Oral	Gadal Laboratories, Inc.	2013-05-01	Not applicable

International/Other Brands

Dimor (Nordic Drugs) / Fortasec (Esteve) / Imodium (Johnson & Johnson) / Kaopectate II (Chattem, Inc.) / Lopedium (Sandoz) / Lopedium express (Sandoz) / Lopex (Orion) / Maalox Anti-Diarrheal (Novartis International AG) / Pepto Diarrhea Control (Procter & Gamble )

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Imodium Complete Caplets	Loperamide hydrochloride (2 mg) + Simethicone (125 mg)	Tablet	Oral	Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc	2002-06-20	Not applicable
Imodium Complete Chewable Tablets	Loperamide hydrochloride (2 mg) + Simethicone (125 mg)	Tablet, chewable	Oral	Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc	1998-05-12	Not applicable

Categories

UNII

6X9OC3H4II

CAS number

53179-11-6

Weight

Average: 477.038
Monoisotopic: 476.223056017

Chemical Formula

C₂₉H₃₃ClN₂O₂

InChI Key

RDOIQAHITMMDAJ-UHFFFAOYSA-N

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

IUPAC Name

4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide

SMILES

CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1

Pharmacology

Indication

For the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease or gastroenteritis. Also used for reducing the volume of discharge from ileostomies.

Structured Indications

Pharmacodynamics

Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Loperamide is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids. It works specifically by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.

Mechanism of action

In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-selective calcium channel blocker and binds to opioid mu-receptors. Evidence also suggests that at higher concentrations it binds to calmodulin.

Target	Actions	Organism
AMu-type opioid receptor	agonist	Human
ADelta-type opioid receptor	agonist	Human
AKappa-type opioid receptor	agonist	Human
UVoltage-dependent P/Q-type calcium channel subunit alpha-1A	inhibitor	Human
UPro-opiomelanocortin	modulator	Human
UCalmodulin	inhibitor	Human
UNuclear receptor subfamily 1 group I member 3	Not Available	Human

Absorption

Not significantly absorbed from the gut

Volume of distribution

Not Available

Protein binding

97%

Metabolism

Hepatic

Route of elimination

Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.

Half life

9.1 to 14.4 hours (average 10.8 hours)

Clearance

Not Available

Toxicity

Oral, mouse: LD₅₀ = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction	Drug group
Abiraterone	The serum concentration of Loperamide can be increased when it is combined with Abiraterone.	Approved
Acebutolol	The serum concentration of Acebutolol can be increased when it is combined with Loperamide.	Approved
Acetaminophen	The serum concentration of Loperamide can be increased when it is combined with Acetaminophen.	Approved
Acetylsalicylic acid	The serum concentration of Acetylsalicylic acid can be increased when it is combined with Loperamide.	Approved, Vet Approved
Afatinib	The serum concentration of Afatinib can be increased when it is combined with Loperamide.	Approved
Albendazole	The serum concentration of Loperamide can be increased when it is combined with Albendazole.	Approved, Vet Approved
Aldosterone	The serum concentration of Loperamide can be decreased when it is combined with Aldosterone.	Experimental
Alectinib	The serum concentration of Loperamide can be increased when it is combined with Alectinib.	Approved
Alfentanil	The serum concentration of Loperamide can be increased when it is combined with Alfentanil.	Approved, Illicit
Alitretinoin	The serum concentration of Alitretinoin can be increased when it is combined with Loperamide.	Approved, Investigational
Amantadine	The serum concentration of Loperamide can be increased when it is combined with Amantadine.	Approved
Ambrisentan	The serum concentration of Ambrisentan can be increased when it is combined with Loperamide.	Approved, Investigational
Aminohippuric acid	The serum concentration of Loperamide can be increased when it is combined with Aminohippuric acid.	Approved
Amiodarone	The metabolism of Loperamide can be decreased when combined with Amiodarone.	Approved, Investigational
Amitriptyline	The serum concentration of Amitriptyline can be increased when it is combined with Loperamide.	Approved
Amlodipine	The serum concentration of Loperamide can be increased when it is combined with Amlodipine.	Approved
Amprenavir	The serum concentration of Loperamide can be decreased when it is combined with Amprenavir.	Approved
Amsacrine	The serum concentration of Loperamide can be increased when it is combined with Amsacrine.	Approved
Apixaban	The serum concentration of Apixaban can be increased when it is combined with Loperamide.	Approved
Aprepitant	The serum concentration of Loperamide can be increased when it is combined with Aprepitant.	Approved, Investigational
Arsenic trioxide	The serum concentration of Arsenic trioxide can be increased when it is combined with Loperamide.	Approved, Investigational
Artemether	The metabolism of Loperamide can be decreased when combined with Artemether.	Approved
Astemizole	The serum concentration of Loperamide can be increased when it is combined with Astemizole.	Approved, Withdrawn
Atazanavir	The metabolism of Loperamide can be decreased when combined with Atazanavir.	Approved, Investigational
Atenolol	The serum concentration of Loperamide can be increased when it is combined with Atenolol.	Approved
Atomoxetine	The metabolism of Loperamide can be decreased when combined with Atomoxetine.	Approved
Atorvastatin	The serum concentration of Loperamide can be increased when it is combined with Atorvastatin.	Approved
Axitinib	The serum concentration of Axitinib can be increased when it is combined with Loperamide.	Approved, Investigational
Azelastine	The serum concentration of Loperamide can be increased when it is combined with Azelastine.	Approved
Azithromycin	The serum concentration of Loperamide can be increased when it is combined with Azithromycin.	Approved
Belinostat	The serum concentration of Belinostat can be increased when it is combined with Loperamide.	Approved, Investigational
Benzocaine	The serum concentration of Loperamide can be increased when it is combined with Benzocaine.	Approved
Bepridil	The serum concentration of Loperamide can be increased when it is combined with Bepridil.	Approved, Withdrawn
Betamethasone	The serum concentration of Betamethasone can be increased when it is combined with Loperamide.	Approved, Vet Approved
Betaxolol	The metabolism of Loperamide can be decreased when combined with Betaxolol.	Approved
Biperiden	The serum concentration of Loperamide can be increased when it is combined with Biperiden.	Approved
Boceprevir	The metabolism of Loperamide can be decreased when combined with Boceprevir.	Withdrawn
Bortezomib	The metabolism of Loperamide can be decreased when combined with Bortezomib.	Approved, Investigational
Bosentan	The serum concentration of Loperamide can be decreased when it is combined with Bosentan.	Approved, Investigational
Bosutinib	The serum concentration of Bosutinib can be increased when it is combined with Loperamide.	Approved
Brentuximab vedotin	The serum concentration of Brentuximab vedotin can be increased when it is combined with Loperamide.	Approved
Bromocriptine	The serum concentration of Loperamide can be increased when it is combined with Bromocriptine.	Approved, Investigational
Buprenorphine	The serum concentration of Loperamide can be increased when it is combined with Buprenorphine.	Approved, Illicit, Investigational, Vet Approved
Bupropion	The metabolism of Loperamide can be decreased when combined with Bupropion.	Approved
Buspirone	The serum concentration of Loperamide can be increased when it is combined with Buspirone.	Approved, Investigational
Cabazitaxel	The serum concentration of Cabazitaxel can be increased when it is combined with Loperamide.	Approved
Caffeine	The serum concentration of Caffeine can be increased when it is combined with Loperamide.	Approved
Camptothecin	The serum concentration of Camptothecin can be increased when it is combined with Loperamide.	Experimental
Canagliflozin	The serum concentration of Canagliflozin can be increased when it is combined with Loperamide.	Approved
Candesartan	The serum concentration of Loperamide can be increased when it is combined with Candesartan.	Approved
Captopril	The serum concentration of Loperamide can be increased when it is combined with Captopril.	Approved
Carbamazepine	The metabolism of Loperamide can be increased when combined with Carbamazepine.	Approved, Investigational
Carfilzomib	The serum concentration of Carfilzomib can be increased when it is combined with Loperamide.	Approved
Carvedilol	The serum concentration of Loperamide can be increased when it is combined with Carvedilol.	Approved, Investigational
Caspofungin	The serum concentration of Loperamide can be increased when it is combined with Caspofungin.	Approved
Celecoxib	The metabolism of Loperamide can be decreased when combined with Celecoxib.	Approved, Investigational
Ceritinib	The serum concentration of Loperamide can be increased when it is combined with Ceritinib.	Approved
Cerivastatin	The serum concentration of Cerivastatin can be increased when it is combined with Loperamide.	Withdrawn
Chloroquine	The serum concentration of Loperamide can be increased when it is combined with Chloroquine.	Approved, Vet Approved
Chlorpromazine	The serum concentration of Loperamide can be increased when it is combined with Chlorpromazine.	Approved, Vet Approved
Chlorpropamide	The serum concentration of Loperamide can be increased when it is combined with Chlorpropamide.	Approved
Chlorprothixene	The serum concentration of Loperamide can be increased when it is combined with Chlorprothixene.	Approved, Withdrawn
Cholecalciferol	The metabolism of Loperamide can be decreased when combined with Cholecalciferol.	Approved, Nutraceutical
Cholesterol	The serum concentration of Loperamide can be increased when it is combined with Cholesterol.	Experimental
Cholic Acid	The serum concentration of Loperamide can be decreased when it is combined with Cholic Acid.	Approved
Cilazapril	The serum concentration of Loperamide can be increased when it is combined with Cilazapril.	Approved
Cimetidine	The serum concentration of Loperamide can be decreased when it is combined with Cimetidine.	Approved
Cinacalcet	The metabolism of Loperamide can be decreased when combined with Cinacalcet.	Approved
Ciprofloxacin	The serum concentration of Loperamide can be increased when it is combined with Ciprofloxacin.	Approved, Investigational
Cisplatin	The serum concentration of Cisplatin can be increased when it is combined with Loperamide.	Approved
Citalopram	The serum concentration of Citalopram can be increased when it is combined with Loperamide.	Approved
Clarithromycin	The metabolism of Loperamide can be decreased when combined with Clarithromycin.	Approved
Clemastine	The metabolism of Loperamide can be decreased when combined with Clemastine.	Approved
Clobazam	The serum concentration of Clobazam can be increased when it is combined with Loperamide.	Approved, Illicit
Clofazimine	The serum concentration of Loperamide can be increased when it is combined with Clofazimine.	Approved, Investigational
Clomifene	The serum concentration of Clomifene can be increased when it is combined with Loperamide.	Approved, Investigational
Clomipramine	The serum concentration of Loperamide can be increased when it is combined with Clomipramine.	Approved, Vet Approved
Clonidine	The serum concentration of Clonidine can be increased when it is combined with Loperamide.	Approved
Clopidogrel	The serum concentration of Clopidogrel can be increased when it is combined with Loperamide.	Approved, Nutraceutical
Clotrimazole	The metabolism of Loperamide can be decreased when combined with Clotrimazole.	Approved, Vet Approved
Clozapine	The serum concentration of Clozapine can be increased when it is combined with Loperamide.	Approved
Cobicistat	The serum concentration of Loperamide can be increased when it is combined with Cobicistat.	Approved
Cobimetinib	The serum concentration of Cobimetinib can be increased when it is combined with Loperamide.	Approved
Cocaine	The metabolism of Loperamide can be decreased when combined with Cocaine.	Approved, Illicit
Colchicine	The serum concentration of Colchicine can be increased when it is combined with Loperamide.	Approved
Colforsin	The serum concentration of Loperamide can be increased when it is combined with Colforsin.	Experimental
Conivaptan	The serum concentration of Loperamide can be increased when it is combined with Conivaptan.	Approved, Investigational
Conjugated estrogens	The serum concentration of Conjugated estrogens can be increased when it is combined with Loperamide.	Approved
Copanlisib	The serum concentration of Copanlisib can be increased when it is combined with Loperamide.	Approved
Crisaborole	The metabolism of Loperamide can be decreased when combined with Crisaborole.	Approved
Crizotinib	The metabolism of Loperamide can be decreased when combined with Crizotinib.	Approved
Cyclophosphamide	The serum concentration of Loperamide can be increased when it is combined with Cyclophosphamide.	Approved, Investigational
Cyclosporine	The metabolism of Loperamide can be decreased when combined with Cyclosporine.	Approved, Investigational, Vet Approved
Dabigatran etexilate	The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Loperamide.	Approved
Dabrafenib	The serum concentration of Loperamide can be decreased when it is combined with Dabrafenib.	Approved
Daclatasvir	The serum concentration of Loperamide can be increased when it is combined with Daclatasvir.	Approved
Dactinomycin	The serum concentration of Loperamide can be increased when it is combined with Dactinomycin.	Approved
Dapagliflozin	The serum concentration of Dapagliflozin can be increased when it is combined with Loperamide.	Approved
Darifenacin	The metabolism of Loperamide can be decreased when combined with Darifenacin.	Approved, Investigational
Darunavir	The serum concentration of Loperamide can be increased when it is combined with Darunavir.	Approved
Dasatinib	The serum concentration of Loperamide can be increased when it is combined with Dasatinib.	Approved, Investigational
Daunorubicin	The serum concentration of Loperamide can be decreased when it is combined with Daunorubicin.	Approved
Debrisoquin	The serum concentration of Debrisoquin can be increased when it is combined with Loperamide.	Approved
Deferasirox	The serum concentration of Loperamide can be decreased when it is combined with Deferasirox.	Approved, Investigational
Delavirdine	The metabolism of Loperamide can be decreased when combined with Delavirdine.	Approved
Desipramine	The serum concentration of Loperamide can be increased when it is combined with Desipramine.	Approved
Desloratadine	The serum concentration of Loperamide can be increased when it is combined with Desloratadine.	Approved, Investigational
Dexamethasone	The serum concentration of Loperamide can be decreased when it is combined with Dexamethasone.	Approved, Investigational, Vet Approved
Dextromethorphan	The serum concentration of Loperamide can be increased when it is combined with Dextromethorphan.	Approved
Diazepam	The serum concentration of Diazepam can be increased when it is combined with Loperamide.	Approved, Illicit, Vet Approved
Diclofenac	The serum concentration of Loperamide can be increased when it is combined with Diclofenac.	Approved, Vet Approved
Diethylstilbestrol	The serum concentration of Diethylstilbestrol can be increased when it is combined with Loperamide.	Approved
Digitoxin	The serum concentration of Digitoxin can be increased when it is combined with Loperamide.	Approved
Digoxin	The serum concentration of Loperamide can be decreased when it is combined with Digoxin.	Approved
Dihydroergotamine	The metabolism of Loperamide can be decreased when combined with Dihydroergotamine.	Approved
Dihydrotestosterone	The serum concentration of Dihydrotestosterone can be increased when it is combined with Loperamide.	Illicit
Diltiazem	The metabolism of Loperamide can be decreased when combined with Diltiazem.	Approved
Diphenhydramine	The metabolism of Loperamide can be decreased when combined with Diphenhydramine.	Approved
Dipyridamole	The serum concentration of Loperamide can be increased when it is combined with Dipyridamole.	Approved
Docetaxel	The serum concentration of Docetaxel can be increased when it is combined with Loperamide.	Approved, Investigational
Domperidone	The serum concentration of Domperidone can be increased when it is combined with Loperamide.	Approved, Investigational, Vet Approved
Dosulepin	The metabolism of Loperamide can be decreased when combined with Dosulepin.	Approved
Doxazosin	The serum concentration of Loperamide can be increased when it is combined with Doxazosin.	Approved
Doxepin	The serum concentration of Loperamide can be increased when it is combined with Doxepin.	Approved
Doxorubicin	The serum concentration of Doxorubicin can be increased when it is combined with Loperamide.	Approved, Investigational
Doxorubicin	The serum concentration of Loperamide can be decreased when it is combined with Doxorubicin.	Approved, Investigational
Doxycycline	The metabolism of Loperamide can be decreased when combined with Doxycycline.	Approved, Investigational, Vet Approved
Dronabinol	The serum concentration of Loperamide can be increased when it is combined with Dronabinol.	Approved, Illicit
Dronedarone	The metabolism of Loperamide can be decreased when combined with Dronedarone.	Approved
Duloxetine	The metabolism of Loperamide can be decreased when combined with Duloxetine.	Approved
Edoxaban	The serum concentration of Edoxaban can be increased when it is combined with Loperamide.	Approved
Efavirenz	The metabolism of Loperamide can be decreased when combined with Efavirenz.	Approved, Investigational
Elbasvir	The serum concentration of Elbasvir can be increased when it is combined with Loperamide.	Approved
Eletriptan	The serum concentration of Eletriptan can be increased when it is combined with Loperamide.	Approved, Investigational
Eliglustat	The metabolism of Loperamide can be decreased when combined with Eliglustat.	Approved
Enalapril	The serum concentration of Loperamide can be increased when it is combined with Enalapril.	Approved, Vet Approved
Enasidenib	The serum concentration of Enasidenib can be increased when it is combined with Loperamide.	Approved
Enzalutamide	The serum concentration of Loperamide can be decreased when it is combined with Enzalutamide.	Approved
Epinastine	The serum concentration of Epinastine can be increased when it is combined with Loperamide.	Approved, Investigational
Ergonovine	The serum concentration of Loperamide can be increased when it is combined with Ergonovine.	Approved
Ergotamine	The serum concentration of Loperamide can be increased when it is combined with Ergotamine.	Approved
Erlotinib	The serum concentration of Erlotinib can be increased when it is combined with Loperamide.	Approved, Investigational
Erythromycin	The metabolism of Loperamide can be decreased when combined with Erythromycin.	Approved, Vet Approved
Estradiol	The serum concentration of Estradiol can be increased when it is combined with Loperamide.	Approved, Investigational, Vet Approved
Estramustine	The serum concentration of Loperamide can be increased when it is combined with Estramustine.	Approved
Estriol	The serum concentration of Loperamide can be decreased when it is combined with Estriol.	Approved, Vet Approved
Estrone	The serum concentration of Loperamide can be decreased when it is combined with Estrone.	Approved
Ethinyl Estradiol	The serum concentration of Ethinyl Estradiol can be increased when it is combined with Loperamide.	Approved
Etoposide	The serum concentration of Loperamide can be increased when it is combined with Etoposide.	Approved
Etravirine	The serum concentration of Loperamide can be increased when it is combined with Etravirine.	Approved
Everolimus	The serum concentration of Everolimus can be increased when it is combined with Loperamide.	Approved
Ezetimibe	The serum concentration of Ezetimibe can be increased when it is combined with Loperamide.	Approved
Felodipine	The serum concentration of Loperamide can be increased when it is combined with Felodipine.	Approved, Investigational
Fentanyl	The serum concentration of Loperamide can be increased when it is combined with Fentanyl.	Approved, Illicit, Investigational, Vet Approved
Fesoterodine	The serum concentration of Fesoterodine can be increased when it is combined with Loperamide.	Approved
Fexofenadine	The serum concentration of Fexofenadine can be increased when it is combined with Loperamide.	Approved
Fidaxomicin	The serum concentration of Fidaxomicin can be increased when it is combined with Loperamide.	Approved
Fluconazole	The metabolism of Loperamide can be decreased when combined with Fluconazole.	Approved
Fluoxetine	The metabolism of Loperamide can be decreased when combined with Fluoxetine.	Approved, Vet Approved
Flupentixol	The serum concentration of Loperamide can be increased when it is combined with Flupentixol.	Approved, Withdrawn
Fluphenazine	The serum concentration of Loperamide can be increased when it is combined with Fluphenazine.	Approved
Flurazepam	The serum concentration of Loperamide can be increased when it is combined with Flurazepam.	Approved, Illicit
Fluticasone furoate	The serum concentration of Fluticasone furoate can be increased when it is combined with Loperamide.	Approved
Fluvoxamine	The metabolism of Loperamide can be decreased when combined with Fluvoxamine.	Approved, Investigational
Fosamprenavir	The metabolism of Loperamide can be decreased when combined with Fosamprenavir.	Approved
Fosaprepitant	The serum concentration of Loperamide can be increased when it is combined with Fosaprepitant.	Approved
Fosphenytoin	The metabolism of Loperamide can be increased when combined with Fosphenytoin.	Approved
Fusidic Acid	The serum concentration of Loperamide can be increased when it is combined with Fusidic Acid.	Approved
Gefitinib	The serum concentration of Gefitinib can be increased when it is combined with Loperamide.	Approved, Investigational
Gemcitabine	The serum concentration of Gemcitabine can be increased when it is combined with Loperamide.	Approved
Genistein	The serum concentration of Loperamide can be increased when it is combined with Genistein.	Investigational
Glecaprevir	The serum concentration of Glecaprevir can be increased when it is combined with Loperamide.	Approved
Glyburide	The serum concentration of Loperamide can be increased when it is combined with Glyburide.	Approved
Glycerin	The serum concentration of Loperamide can be increased when it is combined with Glycerin.	Approved, Investigational
Gramicidin D	The serum concentration of Loperamide can be increased when it is combined with Gramicidin D.	Approved
Grazoprevir	The serum concentration of Grazoprevir can be increased when it is combined with Loperamide.	Approved
Grepafloxacin	The serum concentration of Grepafloxacin can be increased when it is combined with Loperamide.	Withdrawn
Haloperidol	The serum concentration of Haloperidol can be increased when it is combined with Loperamide.	Approved
Hydrocortisone	The serum concentration of Hydrocortisone can be increased when it is combined with Loperamide.	Approved, Vet Approved
Ibuprofen	The serum concentration of Ibuprofen can be increased when it is combined with Loperamide.	Approved
Idelalisib	The serum concentration of Loperamide can be increased when it is combined with Idelalisib.	Approved
Imatinib	The metabolism of Loperamide can be decreased when combined with Imatinib.	Approved
Imipramine	The serum concentration of Imipramine can be increased when it is combined with Loperamide.	Approved
Indacaterol	The serum concentration of Indacaterol can be increased when it is combined with Loperamide.	Approved
Indinavir	The metabolism of Loperamide can be decreased when combined with Indinavir.	Approved
Indomethacin	The serum concentration of Loperamide can be increased when it is combined with Indomethacin.	Approved, Investigational
Inotuzumab ozogamicin	The serum concentration of Inotuzumab ozogamicin can be increased when it is combined with Loperamide.	Approved
Irbesartan	The metabolism of Loperamide can be decreased when combined with Irbesartan.	Approved, Investigational
Irinotecan	The serum concentration of Irinotecan can be increased when it is combined with Loperamide.	Approved, Investigational
Isavuconazonium	The metabolism of Loperamide can be decreased when combined with Isavuconazonium.	Approved, Investigational
Isoniazid	The metabolism of Loperamide can be decreased when combined with Isoniazid.	Approved
Isradipine	The metabolism of Loperamide can be decreased when combined with Isradipine.	Approved
Itraconazole	The metabolism of Loperamide can be decreased when combined with Itraconazole.	Approved, Investigational
Ivacaftor	The serum concentration of Loperamide can be increased when it is combined with Ivacaftor.	Approved
Ivermectin	The serum concentration of Ivermectin can be increased when it is combined with Loperamide.	Approved, Vet Approved
Ketamine	The serum concentration of Loperamide can be increased when it is combined with Ketamine.	Approved, Vet Approved
Ketazolam	The serum concentration of Ketazolam can be increased when it is combined with Loperamide.	Approved
Ketoconazole	The metabolism of Loperamide can be decreased when combined with Ketoconazole.	Approved, Investigational
Lamivudine	The serum concentration of Lamivudine can be increased when it is combined with Loperamide.	Approved, Investigational
Lamotrigine	The serum concentration of Lamotrigine can be increased when it is combined with Loperamide.	Approved, Investigational
Lansoprazole	The serum concentration of Loperamide can be increased when it is combined with Lansoprazole.	Approved, Investigational
Lapatinib	The serum concentration of Loperamide can be increased when it is combined with Lapatinib.	Approved, Investigational
Ledipasvir	The serum concentration of Ledipasvir can be increased when it is combined with Loperamide.	Approved
Lenalidomide	The serum concentration of Lenalidomide can be increased when it is combined with Loperamide.	Approved
Lenvatinib	The serum concentration of Lenvatinib can be increased when it is combined with Loperamide.	Approved
Levetiracetam	The serum concentration of Levetiracetam can be increased when it is combined with Loperamide.	Approved, Investigational
Levofloxacin	The serum concentration of Levofloxacin can be increased when it is combined with Loperamide.	Approved, Investigational
Levomilnacipran	The serum concentration of Levomilnacipran can be increased when it is combined with Loperamide.	Approved
Levothyroxine	The serum concentration of Loperamide can be decreased when it is combined with Levothyroxine.	Approved
Lidocaine	The serum concentration of Loperamide can be increased when it is combined with Lidocaine.	Approved, Vet Approved
Linagliptin	The serum concentration of Linagliptin can be increased when it is combined with Loperamide.	Approved
Liothyronine	The serum concentration of Loperamide can be decreased when it is combined with Liothyronine.	Approved, Vet Approved
Liotrix	The serum concentration of Loperamide can be decreased when it is combined with Liotrix.	Approved
Lisinopril	The serum concentration of Loperamide can be increased when it is combined with Lisinopril.	Approved, Investigational
Lomitapide	The serum concentration of Loperamide can be increased when it is combined with Lomitapide.	Approved
Lopinavir	The metabolism of Loperamide can be decreased when combined with Lopinavir.	Approved
Loratadine	The serum concentration of Loperamide can be increased when it is combined with Loratadine.	Approved
Lorcaserin	The metabolism of Loperamide can be decreased when combined with Lorcaserin.	Approved
Losartan	The serum concentration of Loperamide can be increased when it is combined with Losartan.	Approved
Lovastatin	The metabolism of Loperamide can be decreased when combined with Lovastatin.	Approved, Investigational
Luliconazole	The serum concentration of Loperamide can be increased when it is combined with Luliconazole.	Approved
Lumacaftor	The serum concentration of Loperamide can be increased when it is combined with Lumacaftor.	Approved
Lumefantrine	The metabolism of Loperamide can be decreased when combined with Lumefantrine.	Approved
Manidipine	The metabolism of Loperamide can be decreased when combined with Manidipine.	Approved
Mannitol	The serum concentration of Mannitol can be increased when it is combined with Loperamide.	Approved, Investigational
Maprotiline	The serum concentration of Loperamide can be increased when it is combined with Maprotiline.	Approved
Mebendazole	The serum concentration of Loperamide can be increased when it is combined with Mebendazole.	Approved, Vet Approved
Mefloquine	The serum concentration of Loperamide can be increased when it is combined with Mefloquine.	Approved
Megestrol acetate	The serum concentration of Loperamide can be increased when it is combined with Megestrol acetate.	Approved, Vet Approved
Meprobamate	The serum concentration of Loperamide can be increased when it is combined with Meprobamate.	Approved, Illicit
Methadone	The serum concentration of Loperamide can be increased when it is combined with Methadone.	Approved
Methotrexate	The serum concentration of Methotrexate can be increased when it is combined with Loperamide.	Approved
Methotrimeprazine	The metabolism of Loperamide can be decreased when combined with Methotrimeprazine.	Approved
Methylprednisolone	The serum concentration of Methylprednisolone can be increased when it is combined with Loperamide.	Approved, Vet Approved
Metoprolol	The serum concentration of Loperamide can be increased when it is combined with Metoprolol.	Approved, Investigational
Mibefradil	The serum concentration of Loperamide can be increased when it is combined with Mibefradil.	Withdrawn
Miconazole	The serum concentration of Loperamide can be increased when it is combined with Miconazole.	Approved, Investigational, Vet Approved
Midazolam	The serum concentration of Loperamide can be decreased when it is combined with Midazolam.	Approved, Illicit
Midostaurin	The metabolism of Loperamide can be decreased when combined with Midostaurin.	Approved
Mifepristone	The serum concentration of Loperamide can be increased when it is combined with Mifepristone.	Approved, Investigational
Mirabegron	The serum concentration of Mirabegron can be increased when it is combined with Loperamide.	Approved
Mitomycin	The serum concentration of Loperamide can be increased when it is combined with Mitomycin.	Approved
Mitotane	The serum concentration of Loperamide can be decreased when it is combined with Mitotane.	Approved
Mitoxantrone	The serum concentration of Loperamide can be decreased when it is combined with Mitoxantrone.	Approved, Investigational
Morphine	The serum concentration of Morphine can be increased when it is combined with Loperamide.	Approved, Investigational
Mycophenolate mofetil	The serum concentration of Mycophenolate mofetil can be increased when it is combined with Loperamide.	Approved, Investigational
Nadolol	The serum concentration of Nadolol can be increased when it is combined with Loperamide.	Approved
Naloxegol	The serum concentration of Naloxegol can be increased when it is combined with Loperamide.	Approved
Naloxone	The serum concentration of Naloxone can be increased when it is combined with Loperamide.	Approved, Vet Approved
Naltrexone	The serum concentration of Loperamide can be increased when it is combined with Naltrexone.	Approved, Investigational, Vet Approved
Naringenin	The serum concentration of Loperamide can be increased when it is combined with Naringenin.	Experimental
Nefazodone	The metabolism of Loperamide can be decreased when combined with Nefazodone.	Approved, Withdrawn
Nelfinavir	The metabolism of Loperamide can be decreased when combined with Nelfinavir.	Approved
Neostigmine	The serum concentration of Loperamide can be increased when it is combined with Neostigmine.	Approved, Vet Approved
Netupitant	The serum concentration of Loperamide can be increased when it is combined with Netupitant.	Approved
Nevirapine	The metabolism of Loperamide can be increased when combined with Nevirapine.	Approved
Nicardipine	The serum concentration of Loperamide can be increased when it is combined with Nicardipine.	Approved
Nifedipine	The serum concentration of Loperamide can be decreased when it is combined with Nifedipine.	Approved
Nilotinib	The metabolism of Loperamide can be decreased when combined with Nilotinib.	Approved, Investigational
Nintedanib	The serum concentration of Nintedanib can be increased when it is combined with Loperamide.	Approved
Nisoldipine	The serum concentration of Loperamide can be increased when it is combined with Nisoldipine.	Approved
Nitrazepam	The serum concentration of Loperamide can be increased when it is combined with Nitrazepam.	Approved
Nitrendipine	The serum concentration of Loperamide can be increased when it is combined with Nitrendipine.	Approved
Nizatidine	The serum concentration of Nizatidine can be increased when it is combined with Loperamide.	Approved
Norethisterone	The serum concentration of Loperamide can be decreased when it is combined with Norethisterone.	Approved
Odanacatib	The serum concentration of Odanacatib can be increased when it is combined with Loperamide.	Investigational
Olanzapine	The serum concentration of Olanzapine can be increased when it is combined with Loperamide.	Approved, Investigational
Olaparib	The metabolism of Loperamide can be decreased when combined with Olaparib.	Approved
Ombitasvir	The serum concentration of Ombitasvir can be increased when it is combined with Loperamide.	Approved
Omeprazole	The serum concentration of Loperamide can be increased when it is combined with Omeprazole.	Approved, Investigational, Vet Approved
Osimertinib	The serum concentration of Loperamide can be increased when it is combined with Osimertinib.	Approved
P-Nitrophenol	The serum concentration of Loperamide can be increased when it is combined with P-Nitrophenol.	Experimental
Paclitaxel	The serum concentration of Loperamide can be increased when it is combined with Paclitaxel.	Approved, Vet Approved
Palbociclib	The serum concentration of Loperamide can be increased when it is combined with Palbociclib.	Approved
Palmitic Acid	The serum concentration of Loperamide can be increased when it is combined with Palmitic Acid.	Experimental
Panobinostat	The serum concentration of Loperamide can be increased when it is combined with Panobinostat.	Approved, Investigational
Pantoprazole	The serum concentration of Loperamide can be increased when it is combined with Pantoprazole.	Approved
Paroxetine	The metabolism of Loperamide can be decreased when combined with Paroxetine.	Approved, Investigational
Pazopanib	The serum concentration of Pazopanib can be increased when it is combined with Loperamide.	Approved
Peginterferon alfa-2b	The serum concentration of Loperamide can be decreased when it is combined with Peginterferon alfa-2b.	Approved
Pentobarbital	The metabolism of Loperamide can be increased when combined with Pentobarbital.	Approved, Vet Approved
Perindopril	The serum concentration of Loperamide can be increased when it is combined with Perindopril.	Approved
Phenobarbital	The metabolism of Loperamide can be increased when combined with Phenobarbital.	Approved
Phenytoin	The metabolism of Loperamide can be increased when combined with Phenytoin.	Approved, Vet Approved
Pibrentasvir	The serum concentration of Pibrentasvir can be increased when it is combined with Loperamide.	Approved
Pimozide	The serum concentration of Loperamide can be increased when it is combined with Pimozide.	Approved
Pioglitazone	The metabolism of Loperamide can be decreased when combined with Pioglitazone.	Approved, Investigational
Pitavastatin	The serum concentration of Pitavastatin can be increased when it is combined with Loperamide.	Approved
Platelet Activating Factor	The serum concentration of Loperamide can be decreased when it is combined with Platelet Activating Factor.	Experimental
Pomalidomide	The serum concentration of Pomalidomide can be increased when it is combined with Loperamide.	Approved
Ponatinib	The serum concentration of Ponatinib can be increased when it is combined with Loperamide.	Approved
Posaconazole	The metabolism of Loperamide can be decreased when combined with Posaconazole.	Approved, Investigational, Vet Approved
Pravastatin	The serum concentration of Pravastatin can be increased when it is combined with Loperamide.	Approved
Prazosin	The serum concentration of Loperamide can be increased when it is combined with Prazosin.	Approved
Prednisolone	The serum concentration of Prednisolone can be increased when it is combined with Loperamide.	Approved, Vet Approved
Prednisone	The serum concentration of Prednisone can be increased when it is combined with Loperamide.	Approved, Vet Approved
Primidone	The metabolism of Loperamide can be increased when combined with Primidone.	Approved, Vet Approved
Probenecid	The serum concentration of Loperamide can be increased when it is combined with Probenecid.	Approved
Progesterone	The serum concentration of Loperamide can be decreased when it is combined with Progesterone.	Approved, Vet Approved
Promazine	The metabolism of Loperamide can be decreased when combined with Promazine.	Approved, Vet Approved
Promethazine	The serum concentration of Loperamide can be increased when it is combined with Promethazine.	Approved
Propafenone	The serum concentration of Loperamide can be increased when it is combined with Propafenone.	Approved
Propranolol	The serum concentration of Propranolol can be increased when it is combined with Loperamide.	Approved, Investigational
Protriptyline	The serum concentration of Loperamide can be increased when it is combined with Protriptyline.	Approved
Prucalopride	The serum concentration of Prucalopride can be increased when it is combined with Loperamide.	Approved
Quazepam	The serum concentration of Loperamide can be increased when it is combined with Quazepam.	Approved, Illicit
Quercetin	The serum concentration of Loperamide can be increased when it is combined with Quercetin.	Experimental
Quetiapine	The serum concentration of Quetiapine can be increased when it is combined with Loperamide.	Approved
Quinacrine	The serum concentration of Loperamide can be increased when it is combined with Quinacrine.	Approved
Quinidine	The metabolism of Loperamide can be decreased when combined with Quinidine.	Approved
Quinine	The serum concentration of Loperamide can be increased when it is combined with Quinine.	Approved
Rabeprazole	The metabolism of Loperamide can be decreased when combined with Rabeprazole.	Approved, Investigational
Ramosetron	Loperamide may increase the constipating activities of Ramosetron.	Approved
Ranitidine	The serum concentration of Loperamide can be increased when it is combined with Ranitidine.	Approved
Ranolazine	The serum concentration of Ranolazine can be increased when it is combined with Loperamide.	Approved, Investigational
Reboxetine	The serum concentration of Loperamide can be increased when it is combined with Reboxetine.	Approved, Investigational
Regorafenib	The serum concentration of Loperamide can be increased when it is combined with Regorafenib.	Approved
Reserpine	The serum concentration of Loperamide can be decreased when it is combined with Reserpine.	Approved
Rifabutin	The metabolism of Loperamide can be increased when combined with Rifabutin.	Approved
Rifampicin	The metabolism of Loperamide can be increased when combined with Rifampicin.	Approved
Rifapentine	The metabolism of Loperamide can be increased when combined with Rifapentine.	Approved
Rifaximin	The serum concentration of Rifaximin can be increased when it is combined with Loperamide.	Approved, Investigational
Rilpivirine	The serum concentration of Loperamide can be increased when it is combined with Rilpivirine.	Approved
Risperidone	The serum concentration of Risperidone can be increased when it is combined with Loperamide.	Approved, Investigational
Ritonavir	The metabolism of Loperamide can be decreased when combined with Ritonavir.	Approved, Investigational
Rivaroxaban	The serum concentration of Rivaroxaban can be increased when it is combined with Loperamide.	Approved
Rolapitant	The serum concentration of Loperamide can be increased when it is combined with Rolapitant.	Approved
Romidepsin	The serum concentration of Romidepsin can be increased when it is combined with Loperamide.	Approved, Investigational
Ropinirole	The metabolism of Loperamide can be decreased when combined with Ropinirole.	Approved, Investigational
Rosiglitazone	The metabolism of Loperamide can be decreased when combined with Rosiglitazone.	Approved, Investigational
Salicylic acid	The serum concentration of Salicylic acid can be increased when it is combined with Loperamide.	Approved, Vet Approved
Saquinavir	The metabolism of Loperamide can be decreased when combined with Saquinavir.	Approved, Investigational
Scopolamine	The serum concentration of Loperamide can be increased when it is combined with Scopolamine.	Approved
Secobarbital	The metabolism of Loperamide can be increased when combined with Secobarbital.	Approved, Vet Approved
Selegiline	The serum concentration of Loperamide can be increased when it is combined with Selegiline.	Approved, Investigational, Vet Approved
Selexipag	The serum concentration of Selexipag can be increased when it is combined with Loperamide.	Approved
Sertraline	The serum concentration of Loperamide can be increased when it is combined with Sertraline.	Approved
Sildenafil	The metabolism of Loperamide can be decreased when combined with Sildenafil.	Approved, Investigational
Silodosin	The serum concentration of Silodosin can be increased when it is combined with Loperamide.	Approved
Siltuximab	The serum concentration of Loperamide can be decreased when it is combined with Siltuximab.	Approved
Simeprevir	The serum concentration of Loperamide can be increased when it is combined with Simeprevir.	Approved
Simvastatin	The serum concentration of Loperamide can be increased when it is combined with Simvastatin.	Approved
Sirolimus	The serum concentration of Loperamide can be decreased when it is combined with Sirolimus.	Approved, Investigational
Sitagliptin	The serum concentration of Sitagliptin can be increased when it is combined with Loperamide.	Approved, Investigational
Sofosbuvir	The serum concentration of Sofosbuvir can be increased when it is combined with Loperamide.	Approved
Sorafenib	The serum concentration of Sorafenib can be increased when it is combined with Loperamide.	Approved, Investigational
Sparfloxacin	The serum concentration of Sparfloxacin can be increased when it is combined with Loperamide.	Approved
Sphingosine	The serum concentration of Sphingosine can be increased when it is combined with Loperamide.	Experimental
Spironolactone	The serum concentration of Loperamide can be increased when it is combined with Spironolactone.	Approved
St. John's Wort	The serum concentration of Loperamide can be decreased when it is combined with St. John's Wort.	Nutraceutical
Staurosporine	The serum concentration of Loperamide can be increased when it is combined with Staurosporine.	Experimental
Stiripentol	The serum concentration of Loperamide can be increased when it is combined with Stiripentol.	Approved
Streptozocin	The serum concentration of Loperamide can be decreased when it is combined with Streptozocin.	Approved
Sulfamethoxazole	The metabolism of Loperamide can be decreased when combined with Sulfamethoxazole.	Approved
Sulfinpyrazone	The serum concentration of Loperamide can be increased when it is combined with Sulfinpyrazone.	Approved
Sulfisoxazole	The metabolism of Loperamide can be decreased when combined with Sulfisoxazole.	Approved, Vet Approved
Sumatriptan	The serum concentration of Loperamide can be increased when it is combined with Sumatriptan.	Approved, Investigational
Sunitinib	The serum concentration of Loperamide can be increased when it is combined with Sunitinib.	Approved, Investigational
Tacrine	The serum concentration of Loperamide can be increased when it is combined with Tacrine.	Withdrawn
Tacrolimus	The serum concentration of Loperamide can be decreased when it is combined with Tacrolimus.	Approved, Investigational
Tamoxifen	The serum concentration of Loperamide can be decreased when it is combined with Tamoxifen.	Approved
Taurocholic Acid	The serum concentration of Taurocholic Acid can be increased when it is combined with Loperamide.	Experimental
Technetium Tc-99m sestamibi	The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Loperamide.	Approved
Telaprevir	The metabolism of Loperamide can be decreased when combined with Telaprevir.	Withdrawn
Telithromycin	The metabolism of Loperamide can be decreased when combined with Telithromycin.	Approved
Telmisartan	The serum concentration of Loperamide can be increased when it is combined with Telmisartan.	Approved, Investigational
Temsirolimus	The serum concentration of Temsirolimus can be increased when it is combined with Loperamide.	Approved
Terazosin	The serum concentration of Loperamide can be increased when it is combined with Terazosin.	Approved
Terbinafine	The metabolism of Loperamide can be decreased when combined with Terbinafine.	Approved, Investigational, Vet Approved
Terfenadine	The serum concentration of Loperamide can be increased when it is combined with Terfenadine.	Withdrawn
Teriflunomide	The metabolism of Loperamide can be decreased when combined with Teriflunomide.	Approved
Tesmilifene	The serum concentration of Loperamide can be decreased when it is combined with Tesmilifene.	Investigational
Testosterone	The serum concentration of Loperamide can be increased when it is combined with Testosterone.	Approved, Investigational
Thioridazine	The metabolism of Loperamide can be decreased when combined with Thioridazine.	Withdrawn
Thiotepa	The metabolism of Loperamide can be decreased when combined with Thiotepa.	Approved
Ticagrelor	The serum concentration of Ticagrelor can be increased when it is combined with Loperamide.	Approved
Ticlopidine	The metabolism of Loperamide can be decreased when combined with Ticlopidine.	Approved
Timolol	The serum concentration of Timolol can be increased when it is combined with Loperamide.	Approved
Tipranavir	The metabolism of Loperamide can be decreased when combined with Tipranavir.	Approved, Investigational
Tocilizumab	The serum concentration of Loperamide can be decreased when it is combined with Tocilizumab.	Approved
Tolvaptan	The serum concentration of Tolvaptan can be increased when it is combined with Loperamide.	Approved
Topiroxostat	The metabolism of Loperamide can be decreased when combined with Topiroxostat.	Approved
Topotecan	The serum concentration of Topotecan can be increased when it is combined with Loperamide.	Approved, Investigational
Toremifene	The serum concentration of Toremifene can be increased when it is combined with Loperamide.	Approved, Investigational
Tranylcypromine	The metabolism of Loperamide can be decreased when combined with Tranylcypromine.	Approved
Trastuzumab emtansine	The serum concentration of Trastuzumab emtansine can be increased when it is combined with Loperamide.	Approved
Trazodone	The serum concentration of Loperamide can be decreased when it is combined with Trazodone.	Approved, Investigational
Trifluoperazine	The serum concentration of Loperamide can be increased when it is combined with Trifluoperazine.	Approved
Triflupromazine	The serum concentration of Loperamide can be increased when it is combined with Triflupromazine.	Approved, Vet Approved
Trimethoprim	The serum concentration of Loperamide can be decreased when it is combined with Trimethoprim.	Approved, Vet Approved
Trimipramine	The serum concentration of Loperamide can be increased when it is combined with Trimipramine.	Approved
Troleandomycin	The serum concentration of Loperamide can be increased when it is combined with Troleandomycin.	Approved
Ulipristal	The serum concentration of Ulipristal can be increased when it is combined with Loperamide.	Approved
Umeclidinium	The serum concentration of Umeclidinium can be increased when it is combined with Loperamide.	Approved
Vecuronium	The serum concentration of Vecuronium can be increased when it is combined with Loperamide.	Approved
Velpatasvir	The serum concentration of Velpatasvir can be increased when it is combined with Loperamide.	Approved
Venetoclax	The serum concentration of Venetoclax can be increased when it is combined with Loperamide.	Approved
Venlafaxine	The metabolism of Loperamide can be decreased when combined with Venlafaxine.	Approved
Verapamil	The metabolism of Loperamide can be decreased when combined with Verapamil.	Approved
Vinblastine	The serum concentration of Loperamide can be decreased when it is combined with Vinblastine.	Approved
Vincristine	The serum concentration of Vincristine can be increased when it is combined with Loperamide.	Approved, Investigational
Vincristine	The serum concentration of Loperamide can be decreased when it is combined with Vincristine.	Approved, Investigational
Vinorelbine	The serum concentration of Loperamide can be increased when it is combined with Vinorelbine.	Approved, Investigational
Vismodegib	The serum concentration of Vismodegib can be increased when it is combined with Loperamide.	Approved
Voriconazole	The metabolism of Loperamide can be decreased when combined with Voriconazole.	Approved, Investigational
Voxilaprevir	The serum concentration of Voxilaprevir can be increased when it is combined with Loperamide.	Approved
Zidovudine	The serum concentration of Zidovudine can be increased when it is combined with Loperamide.	Approved
Zimelidine	The serum concentration of Loperamide can be increased when it is combined with Zimelidine.	Withdrawn
Ziprasidone	The metabolism of Loperamide can be decreased when combined with Ziprasidone.	Approved

Food Interactions

Take without regard to meals. Increase liquid intake.

References

Synthesis Reference

Tsutomu Awamura, Hisanobu Nishikawa, Toshio Inagi, "FILM PREPARATION CONTAINING LOPERAMIDE HYDROCHLORIDE." U.S. Patent US20110159058, issued June 30, 2011.

US20110159058

General References

Not Available

External Links

Human Metabolome Database: HMDB04999
KEGG Drug: D08144
KEGG Compound: C07080
PubChem Compound: 3955
PubChem Substance: 46504591
ChemSpider: 3818
BindingDB: 50017698
ChEBI: 6532
ChEMBL: CHEMBL841
Therapeutic Targets Database: DAP000425
PharmGKB: PA450262
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
PDRhealth: PDRhealth Drug Page
Wikipedia: Loperamide

ATC Codes

A07DA53 — Loperamide, combinations

A07DA03 — Loperamide

A07DA05 — Loperamide oxide

AHFS Codes

56:08.00

PDB Entries

Not Available

FDA label

Download (55.5 KB)

MSDS

Download (73.8 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
0	Completed	Treatment	Pain	1
1	Completed	Basic Science	Drug Interactions	1
1	Completed	Basic Science	Healthy Volunteers	1
1	Completed	Basic Science	Intestinal Obstruction	2
1	Completed	Treatment	Healthy Volunteers	2
2	Completed	Treatment	Cancer, Breast / Early-Stage Breast Carcinoma / Hormone Receptor Positive Tumor	1
2	Recruiting	Treatment	Early Stage HER2+ Breast Cancer	1
2	Recruiting	Treatment	Her2-Positive Breast Cancer	1
2	Withdrawn	Treatment	Cancers	1
2, 3	Completed	Treatment	Diarrhea-predominant Irritable Bowel Syndrome / Functional Diarrhea	1
2, 3	Completed	Treatment	Female Genital Diseases	1
2, 3	Completed	Treatment	Incontinence, Fecal	1
2, 3	Not Yet Recruiting	Treatment	Clostridium Difficile Infection (CDI)	1
3	Completed	Supportive Care	Colorectal Cancers / Diarrhea	1
3	Completed	Treatment	Diarrhea	1
3	Completed	Treatment	Incontinence, Fecal	1
3	Completed	Treatment	Lung Cancer Non-Small Cell Cancer (NSCLC)	1
3	Recruiting	Prevention	Dehydration, Diverting Ileostomy, Loperamide	1
3	Recruiting	Treatment	High Output Stoma	1
3	Terminated	Prevention	Diarrhea	1
3	Terminated	Treatment	Rectal Carcinoma / Short Bowel Syndrome (SBS) / Ulcerative Colitis (UC)	1
4	Completed	Treatment	Diarrhea	3
4	Completed	Treatment	Travelers' Diarrhea	1
4	Recruiting	Treatment	Opiate withdrawal symptoms	1
4	Suspended	Treatment	Antibiotic Associated Diarrhea / Antibiotic-Associated Diarrhea / Clostridium Difficile	1
4	Terminated	Treatment	Relapsing Remitting Multiple Sclerosis (RRMS)	1
4	Withdrawn	Treatment	Incontinence, Fecal	1
Not Available	Completed	Not Available	Healthy Volunteers	1
Not Available	Completed	Treatment	Incontinence, Fecal	1
Not Available	Recruiting	Treatment	Incontinence, Fecal	1
Not Available	Terminated	Treatment	Incontinence, Fecal	1

Pharmacoeconomics

Manufacturers

Mcneil consumer healthcare
Mcneil pediatrics
Janssen pharmaceutica products lp

Packagers

Advanced Pharmaceutical Services Inc.
AQ Pharmaceuticals Inc.
A-S Medication Solutions LLC
Cardinal Health
Chain Drug
Chattem Chemicals Inc.
Comprehensive Consultant Services Inc.
CVS Pharmacy
Dept Health Central Pharmacy
DHHS Program Support Center Supply Service Center
Direct Dispensing Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Heartland Repack Services LLC
Janssen-Ortho Inc.
Lake Chemicals Pvt Ltd.
Lake Erie Medical and Surgical Supply
Liberty Pharmaceuticals
Major Pharmaceuticals
McNeil Laboratories
Medique Products
Medisca Inc.
Mylan
Novopharm Ltd.
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
PCA LLC
PD-Rx Pharmaceuticals Inc.
Perrigo Co.
Pharmacia Inc.
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Qualitest
Redpharm Drug
Remedy Repack
Rugby Laboratories
Sandhills Packaging Inc.
Teva Pharmaceutical Industries Ltd.
Tya Pharmaceuticals
UDL Laboratories
Vangard Labs Inc.

Dosage forms

Form	Route	Strength
Capsule, liquid filled	Oral	2 mg/1
Tablet	Oral	2 mg/1
Solution	Oral	.2 mg
Liquid	Oral	1 mg/5mL
Solution	Oral	1 mg/5mL
Tablet, film coated	Oral	2 mg/1
Suspension	Oral	1 mg/7.5mL
Solution	Oral	1 mg/7.5mL
Tablet, coated	Oral	2 mg/1
Solution	Oral	2 mg
Tablet	Oral
Tablet, chewable	Oral
Capsule	Oral	2 mg
Liquid	Oral	.2 mg
Capsule	Oral	2 mg/1
Liquid	Oral	1 mg/7.5mL
Solution	Oral	2 mg/10mL
Tablet	Oral	2 mg
Solution	Oral	0.2 mg

Prices

Unit description	Cost	Unit
Loperamide hcl powder	26.01USD	g
Loperamide HCl 2 mg capsule	0.64USD	capsule
Imodium a-d 2 mg caplet	0.49USD	caplet
Imodium advanced caplet	0.46USD	caplet
Imodium ms relief caplet	0.46USD	caplet
Kaopectate 262 mg caplet	0.37USD	caplet
Loperamide 2 mg caplet	0.37USD	caplet
Qc anti-diarrheal adv caplet	0.3USD	caplet
Diamode 2 mg tablet	0.28USD	tablet
Kaopectate 240 mg softgel	0.25USD	softgel capsule
Anti-diarrheal 2 mg caplet	0.18USD	caplet
CVS Pharmacy anti-diarrheal 2 mg caplet	0.14USD	caplet
Kaopectate children's suspension	0.02USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
CA2134611	No	2002-12-24	2014-10-28
US6814978	Yes	2002-02-26	2022-02-26
US6103260	No	1997-07-17	2017-07-17

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	222.1	U.S. Patent 3,714,159; 3,884,916.
water solubility	Slight	Not Available
logP	5.5	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.00086 mg/mL	ALOGPS
logP	4.44	ALOGPS
logP	4.77	ChemAxon
logS	-5.7	ALOGPS
pKa (Strongest Acidic)	13.96	ChemAxon
pKa (Strongest Basic)	9.41	ChemAxon
Physiological Charge	1	ChemAxon
Hydrogen Acceptor Count	3	ChemAxon
Hydrogen Donor Count	1	ChemAxon
Polar Surface Area	43.78 Å²	ChemAxon
Rotatable Bond Count	7	ChemAxon
Refractivity	139.32 m³·mol^-1	ChemAxon
Polarizability	52.67 Å³	ChemAxon
Number of Rings	4	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	Yes	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9878
Blood Brain Barrier	+	0.7709
Caco-2 permeable	+	0.5875
P-glycoprotein substrate	Substrate	0.7476
P-glycoprotein inhibitor I	Inhibitor	0.8277
P-glycoprotein inhibitor II	Inhibitor	0.8387
Renal organic cation transporter	Inhibitor	0.5059
CYP450 2C9 substrate	Non-substrate	0.8057
CYP450 2D6 substrate	Non-substrate	0.5315
CYP450 3A4 substrate	Substrate	0.7918
CYP450 1A2 substrate	Non-inhibitor	0.9045
CYP450 2C9 inhibitor	Non-inhibitor	0.9154
CYP450 2D6 inhibitor	Inhibitor	0.8933
CYP450 2C19 inhibitor	Non-inhibitor	0.9026
CYP450 3A4 inhibitor	Non-inhibitor	0.8309
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.9207
Ames test	Non AMES toxic	0.768
Carcinogenicity	Non-carcinogens	0.8564
Biodegradation	Not ready biodegradable	0.9953
Rat acute toxicity	3.6560 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9461
hERG inhibition (predictor II)	Inhibitor	0.7639

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
MS/MS Spectrum - Quattro_QQQ 10V, Positive	LC-MS/MS	splash10-004i-0000900000-673950710672b433271c
MS/MS Spectrum - Quattro_QQQ 25V, Positive	LC-MS/MS	splash10-014i-0090000000-4b7b347a8b8e9dca406c
MS/MS Spectrum - Quattro_QQQ 40V, Positive	LC-MS/MS	splash10-02t9-0090000000-31f15df976e23e73330a
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Positive	LC-MS/MS	splash10-004i-0000900000-d91d13c4e4665bd5fb5a
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Positive	LC-MS/MS	splash10-004i-0020900000-f1be3181a6918c985ffd
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Positive	LC-MS/MS	splash10-014i-0090000000-e5e41346303f41f65688
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Positive	LC-MS/MS	splash10-014i-0090000000-acd8b87c1338e5d0fe25
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Positive	LC-MS/MS	splash10-014i-0090000000-81b85f788d14641430fd
LC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positive	LC-MS/MS	splash10-014i-0090000000-3ce1a89454d777268799
LC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positive	LC-MS/MS	splash10-03di-0090000000-f101d63ad0bf8e5d2178
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-004i-0000900000-d91d13c4e4665bd5fb5a
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-004i-0020900000-f1be3181a6918c985ffd
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-014i-0090000000-e5e41346303f41f65688
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-014i-0090000000-acd8b87c1338e5d0fe25
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-014i-0090000000-81b85f788d14641430fd
LC-MS/MS Spectrum - LC-ESI-IT , positive	LC-MS/MS	splash10-014i-0090000000-1a1a49f09397ad090e82
MS/MS Spectrum - , positive	LC-MS/MS	splash10-016r-0090600000-794ea6214c0cd97c73fa
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-016r-0090300000-e11942e343a28799a5ab
1H NMR Spectrum	1D NMR	Not Applicable
[1H,13C] 2D NMR Spectrum	2D NMR	Not Applicable

Taxonomy

Description: This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom: Organic compounds
Super Class: Benzenoids
Class: Benzene and substituted derivatives
Sub Class: Diphenylmethanes
Direct Parent: Diphenylmethanes
Alternative Parents: Phenylpiperidines / Phenylacetamides / Aralkylamines / Chlorobenzenes / Aryl chlorides / N-acyl amines / Tertiary carboxylic acid amides / Tertiary alcohols / Trialkylamines / Amino acids and derivatives
show 6 more
Substituents: Diphenylmethane / Phenylpiperidine / Phenylacetamide / Chlorobenzene / Aralkylamine / Halobenzene / Aryl chloride / Aryl halide / Piperidine / N-acyl-amine
show 22 more
Molecular Framework: Aromatic heteromonocyclic compounds
External Descriptors: piperidines, tertiary alcohol, monocarboxylic acid amide, monochlorobenzenes (CHEBI:6532)

Targets

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	58	N/A	N/A	15456245
Ki (nM)	0.53	N/A	N/A	15454210

Details1. Mu-type opioid receptor

Kind: Protein
Organism: Human
Pharmacological action: Yes
Actions: Agonist

General Function: Voltage-gated calcium channel activity
Specific Function: Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name: OPRM1
Uniprot ID: P35372
Uniprot Name: Mu-type opioid receptor
Molecular Weight: 44778.855 Da

References

DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed:10087042]
Tan-No K, Niijima F, Nakagawasai O, Sato T, Satoh S, Tadano T: Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. Eur J Pharm Sci. 2003 Nov;20(3):357-63. [PubMed:14592702]
Roge J, Baumer P, Berard H, Schwartz JC, Lecomte JM: The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide. Scand J Gastroenterol. 1993 Apr;28(4):352-4. [PubMed:8488368]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E: Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. [PubMed:6319884]
di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O: Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors. Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12. [PubMed:18284554]

Details2. Delta-type opioid receptor

Kind: Protein
Organism: Human
Pharmacological action: Yes
Actions: Agonist

General Function: Opioid receptor activity
Specific Function: G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name: OPRD1
Uniprot ID: P41143
Uniprot Name: Delta-type opioid receptor
Molecular Weight: 40368.235 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E: Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. [PubMed:6319884]
di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O: Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors. Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12. [PubMed:18284554]

Details3. Kappa-type opioid receptor

Kind: Protein
Organism: Human
Pharmacological action: Yes
Actions: Agonist

General Function: Opioid receptor activity
Specific Function: G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name: OPRK1
Uniprot ID: P41145
Uniprot Name: Kappa-type opioid receptor
Molecular Weight: 42644.665 Da

References

DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed:10087042]

Details4. Voltage-dependent P/Q-type calcium channel subunit alpha-1A

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Voltage-gated calcium channel activity
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1A
Uniprot ID: O00555
Uniprot Name: Voltage-dependent P/Q-type calcium channel subunit alpha-1A
Molecular Weight: 282362.39 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Church J, Fletcher EJ, Abdel-Hamid K, MacDonald JF: Loperamide blocks high-voltage-activated calcium channels and N-methyl-D-aspartate-evoked responses in rat and mouse cultured hippocampal pyramidal neurons. Mol Pharmacol. 1994 Apr;45(4):747-57. [PubMed:8183255]

Details5. Pro-opiomelanocortin

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Modulator

General Function: Type 4 melanocortin receptor binding
Specific Function: ACTH stimulates the adrenal glands to release cortisol.MSH (melanocyte-stimulating hormone) increases the pigmentation of skin by increasing melanin production in melanocytes.Beta-endorphin and Met...
Gene Name: POMC
Uniprot ID: P01189
Uniprot Name: Pro-opiomelanocortin
Molecular Weight: 29423.72 Da

References

Nomura A, Iwasaki Y, Aoki Y, Yamamori E, Mutsuga N, Yoshida M, Asai M, Oiso Y, Saito H: Effects of loperamide and other opioid-related substances on the transcriptional regulation of the rat pro-opiomelanocortin gene in AtT20 cells. Neuroendocrinology. 2001 Aug;74(2):87-94. [PubMed:11474216]
Auernhammer CJ, Stalla GK, Lange M, Pfeiffer A, Muller OA: Effects of loperamide on the human hypothalamo-pituitary-adrenal axis in vivo and in vitro. J Clin Endocrinol Metab. 1992 Aug;75(2):552-7. [PubMed:1322429]
Ambrosi B, Bochicchio D, Ferrario R, Colombo P, Faglia G: Effects of the opiate agonist loperamide on pituitary-adrenal function in patients with suspected hypercortisolism. J Endocrinol Invest. 1989 Jan;12(1):31-5. [PubMed:2545766]
Ambrosi B, Bochicchio D, Colombo P, Ferrario R, Faglia G: Loperamide modifies but does not block the corticotropin-releasing hormone-induced ACTH response in patients with Addison's disease. Horm Metab Res Suppl. 1987;16:74-5. [PubMed:2832297]
Bochicchio D, Ambrosi B, Faglia G: Loperamide, an opiate analog, differently modifies the adrenocorticotropin responses to corticotropin-releasing hormone and lysine vasopressin in patients with Addison's disease. Neuroendocrinology. 1988 Dec;48(6):611-4. [PubMed:2855105]

Details6. Calmodulin

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Titin binding
Specific Function: Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
Gene Name: CALM1
Uniprot ID: P0DP23
Uniprot Name: Calmodulin
Molecular Weight: 16837.47 Da

References

Daly JW, Harper J: Loperamide: novel effects on capacitative calcium influx. Cell Mol Life Sci. 2000 Jan 20;57(1):149-57. [PubMed:10949586]
Suzuki T, Sakai H, Ikari A, Takeguchi N: Inhibition of thromboxane A(2)-induced Cl(-) secretion by antidiarrhea drug loperamide in isolated rat colon. J Pharmacol Exp Ther. 2000 Oct;295(1):233-8. [PubMed:10991984]
Mellstrand T: Loperamide--an opiate receptor agonist with gastrointestinal motility effects. Scand J Gastroenterol Suppl. 1987;130:65-6. [PubMed:2820051]
Stoll R, Ruppin H, Domschke W: Calmodulin-mediated effects of loperamide on chloride transport by brush border membrane vesicles from human ileum. Gastroenterology. 1988 Jul;95(1):69-76. [PubMed:2836258]
Diener M, Knobloch SF, Rummel W: Action of loperamide on neuronally mediated and Ca2+- or cAMP-mediated secretion in rat colon. Eur J Pharmacol. 1988 Aug 2;152(3):217-25. [PubMed:2851449]

Details7. Nuclear receptor subfamily 1 group I member 3

Kind: Protein
Organism: Human
Pharmacological action: Unknown

General Function: Zinc ion binding
Specific Function: Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes. Transactivates both the phenobarbital re...
Gene Name: NR1I3
Uniprot ID: Q14994
Uniprot Name: Nuclear receptor subfamily 1 group I member 3
Molecular Weight: 39942.145 Da

References

Dring AM, Anderson LE, Qamar S, Stoner MA: Rational quantitative structure-activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands. Chem Biol Interact. 2010 Dec 5;188(3):512-25. doi: 10.1016/j.cbi.2010.09.018. Epub 2010 Oct 20. [PubMed:20869355]

Enzymes

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Baker DE: Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8. [PubMed:18192961]
Kim KA, Chung J, Jung DH, Park JY: 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. Epub 2004 Sep 8. [PubMed:15365656]

Details2. Cytochrome P450 2C8

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP2C8
Uniprot ID: P10632
Uniprot Name: Cytochrome P450 2C8
Molecular Weight: 55824.275 Da

References

Kim KA, Chung J, Jung DH, Park JY: 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. Epub 2004 Sep 8. [PubMed:15365656]

Details3. Cytochrome P450 2B6

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP2B6
Uniprot ID: P20813
Uniprot Name: Cytochrome P450 2B6
Molecular Weight: 56277.81 Da

References

Kim KA, Chung J, Jung DH, Park JY: 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. Epub 2004 Sep 8. [PubMed:15365656]

Details4. Cytochrome P450 2D6

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name: CYP2D6
Uniprot ID: P10635
Uniprot Name: Cytochrome P450 2D6
Molecular Weight: 55768.94 Da

References

Kim KA, Chung J, Jung DH, Park JY: 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. Epub 2004 Sep 8. [PubMed:15365656]

Transporters

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	2500	N/A	N/A	11964599

Details1. Multidrug resistance protein 1

Kind: Protein
Organism: Human
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Xenobiotic-transporting atpase activity
Specific Function: Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: Multidrug resistance protein 1
Molecular Weight: 141477.255 Da

References

Wandel C, Kim R, Wood M, Wood A: Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. Anesthesiology. 2002 Apr;96(4):913-20. [PubMed:11964599]
Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684]
Schinkel AH, Wagenaar E, Mol CA, van Deemter L: P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest. 1996 Jun 1;97(11):2517-24. [PubMed:8647944]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:46

Loperamide

Identification

Structure for DB00836 (Loperamide)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

References

References

References

References

References

References

References

Enzymes

References

References

References

References

Transporters

References