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
Thumb
Synonyms
  • Loperamid
  • Loperamida
  • Lopéramide
  • Loperamidum
External IDs
PJ 185 / R 18553
Product Ingredients
IngredientUNIICASInChI Key
Loperamide hydrochloride77TI35393C34552-83-5PGYPOBZJRVSMDS-UHFFFAOYSA-N
Loperamide oxideNG66S4H2RL106900-12-3KXVSBTJVTUVNPM-UHFFFAOYSA-N
Product Images
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Loperamide HydrochlorideCapsule2 mg/1OralMylan Institutional1997-03-10Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-10-12Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralContract Pharmacy Services Pa2017-09-20Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralCardinal Health1991-09-182015-12-29Us
Loperamide HydrochlorideCapsule2 mg/1OralAidarex Pharmaceuticals LLC1993-05-01Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralRemedy Repack2016-12-12Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralDirectrx2014-01-01Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralNucare Pharmaceuticals, Inc.1993-05-01Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralPhysicians Total Care, Inc.1996-06-20Not applicableUs
Loperamide HydrochlorideCapsule2 mg/1OralNu Care Pharmceuticals,inc.1993-05-01Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
7 Select Anti DiarrhealTablet, film coated2 mg/1Oral7 Eleven2014-08-05Not applicableUs
A DTablet, film coated2 mg/1OralWestern Family Foods2003-04-102017-12-01Us
A DTablet, film coated2 mg/1OralWestern Family Foods2003-02-252017-12-01Us
Alti-loperamide - 2mg CapletTablet2 mgOralAltimed Pharma Inc.1995-12-311997-08-14Canada
Anti DiarrhealSolution1 mg/5mLOralRite Aid1992-07-132017-11-14Us
Anti DiarrhealTablet, film coated2 mg/1OralPublix Supermarkets, Inc.2003-03-19Not applicableUs
Anti DiarrhealTablet2 mg/1OralSam's West, Inc2005-05-032018-07-02Us
Anti DiarrhealCapsule2 mg/1OralNash Finch2005-05-032018-04-02Us
Anti DiarrhealTablet, film coated2 mg/1OralMeijer Distribution2003-03-05Not applicableUs
Anti DiarrhealTablet2 mg/1OralArmy + Air Force Exchange Service2005-05-03Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Doc in the Box All Day SupplyLoperamide hydrochloride + Acetaminophen + Calcium Carbonate + Dextromethorphan hydrobromide + Guaifenesin + Ibuprofen + Phenylephrine hydrochlorideKitOralDoc In The Box Llc2018-05-14Not applicableUs
Imodium Complete CapletsLoperamide hydrochloride (2 mg) + Simethicone (125 mg)TabletOralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc2002-06-20Not applicableCanada
Imodium Complete Chewable TabletsLoperamide hydrochloride (2 mg) + Simethicone (125 mg)Tablet, chewableOralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1998-05-12Not applicableCanada
IMODIUM Multi-Symptom ReliefLoperamide hydrochloride (2 mg/1) + Dimethicone (125 mg/1)TabletOralJohnson & Johnson Consumer Inc., Mc Neil Consumer Healthcare Division2008-07-01Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Gadavyt Loperamide HClLoperamide hydrochloride (1 mg/5mL)LiquidOralGadal Laboratories, Inc.2013-05-01Not applicableUs
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 )
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.

Associated Conditions
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.

TargetActionsOrganism
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 3Not AvailableHuman
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
DrugInteractionDrug group
AbafunginThe therapeutic efficacy of Abafungin can be increased when used in combination with Loperamide.Investigational
AbemaciclibThe serum concentration of Loperamide can be increased when it is combined with Abemaciclib.Approved, Investigational
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Loperamide.Approved, Investigational
AcepromazineThe risk or severity of hypotension can be increased when Acepromazine is combined with Loperamide.Approved, Vet Approved
AcetaminophenThe serum concentration of Loperamide can be increased when it is combined with Acetaminophen.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Loperamide.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Loperamide.Approved
AlbaconazoleThe therapeutic efficacy of Albaconazole can be increased when used in combination with Loperamide.Investigational
AlbendazoleThe serum concentration of Loperamide can be increased when it is combined with Albendazole.Approved, Vet Approved
AlcuroniumLoperamide may increase the neuromuscular blocking activities of Alcuronium.Experimental
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Loperamide.Experimental, Investigational
AlectinibThe serum concentration of Loperamide can be increased when it is combined with Alectinib.Approved, Investigational
AlfuzosinThe risk or severity of hypotension can be increased when Alfuzosin is combined with Loperamide.Approved, Investigational
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Loperamide.Approved, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Loperamide.Approved, Investigational
AmiodaroneThe serum concentration of Loperamide can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe risk or severity of hypotension can be increased when Amitriptyline is combined with Loperamide.Approved
AmlodipineThe serum concentration of Loperamide can be increased when it is combined with Amlodipine.Approved
AmobarbitalThe metabolism of Loperamide can be increased when combined with Amobarbital.Approved, Illicit
AmodiaquineThe serum concentration of Loperamide can be increased when it is combined with Amodiaquine.Approved, Investigational
AmoxapineThe risk or severity of hypotension can be increased when Amoxapine is combined with Loperamide.Approved
Amphotericin BLoperamide may decrease the nephrotoxic activities of Amphotericin B.Approved, Investigational
AmprenavirThe serum concentration of Amprenavir can be increased when it is combined with Loperamide.Approved, Investigational
AmsacrineThe serum concentration of Loperamide can be increased when it is combined with Amsacrine.Approved, Investigational
AnnamycinThe serum concentration of Loperamide can be increased when it is combined with Annamycin.Investigational
ApalutamideThe serum concentration of Loperamide can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Loperamide.Approved
AprepitantThe serum concentration of Loperamide can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of hypotension can be increased when Aripiprazole is combined with Loperamide.Approved, Investigational
Aripiprazole lauroxilThe risk or severity of hypotension can be increased when Aripiprazole lauroxil is combined with Loperamide.Approved, Investigational
ArotinololThe risk or severity of hypotension can be increased when Arotinolol is combined with Loperamide.Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Loperamide.Approved, Investigational
Ascorbic acidThe serum concentration of Ascorbic acid can be increased when it is combined with Loperamide.Approved, Nutraceutical
AsenapineThe risk or severity of hypotension can be increased when Asenapine is combined with Loperamide.Approved
AstemizoleThe serum concentration of Loperamide can be increased when it is combined with Astemizole.Approved, Withdrawn
AsunaprevirThe serum concentration of Asunaprevir can be increased when it is combined with Loperamide.Approved, Investigational, Withdrawn
AtazanavirThe metabolism of Loperamide can be decreased when combined with Atazanavir.Approved, Investigational
AtorvastatinThe serum concentration of Loperamide can be increased when it is combined with Atorvastatin.Approved
AtracuriumLoperamide may increase the neuromuscular blocking activities of Atracurium.Approved, Experimental, Investigational
Atracurium besylateLoperamide may increase the neuromuscular blocking activities of Atracurium besylate.Approved
AvatrombopagThe serum concentration of Avatrombopag can be increased when it is combined with Loperamide.Approved, Investigational
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Loperamide.Approved, Investigational
AzelastineThe serum concentration of Loperamide can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Loperamide can be increased when it is combined with Azithromycin.Approved
Bafilomycin A1The serum concentration of Loperamide can be increased when it is combined with Bafilomycin A1.Experimental
Bafilomycin B1The serum concentration of Loperamide can be increased when it is combined with Bafilomycin B1.Experimental
BarbexacloneThe metabolism of Loperamide can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Loperamide can be increased when combined with Barbital.Illicit
BaricitinibThe serum concentration of Baricitinib can be increased when it is combined with Loperamide.Approved, Investigational
BelinostatThe serum concentration of Belinostat can be increased when it is combined with Loperamide.Approved, Investigational
BenzquinamideThe serum concentration of Loperamide can be increased when it is combined with Benzquinamide.Withdrawn
Benzyl alcoholThe serum concentration of Loperamide can be increased when it is combined with Benzyl alcohol.Approved
BepridilThe serum concentration of Loperamide can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Loperamide.Approved, Vet Approved
BevantololThe risk or severity of hypotension can be increased when Bevantolol is combined with Loperamide.Approved
BicalutamideThe serum concentration of Loperamide can be increased when it is combined with Bicalutamide.Approved
BifonazoleThe therapeutic efficacy of Bifonazole can be increased when used in combination with Loperamide.Approved, Investigational
Biricodar dicitrateThe serum concentration of Loperamide can be increased when it is combined with Biricodar dicitrate.Investigational
BisacodylThe therapeutic efficacy of Bisacodyl can be decreased when used in combination with Loperamide.Approved
BisoxatinThe therapeutic efficacy of Bisoxatin can be decreased when used in combination with Loperamide.Approved
BoceprevirThe metabolism of Loperamide can be decreased when combined with Boceprevir.Approved, Withdrawn
BosentanThe serum concentration of Loperamide can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Loperamide.Approved
Brefeldin AThe serum concentration of Loperamide can be increased when it is combined with Brefeldin A.Experimental
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Loperamide.Approved, Investigational
BrexpiprazoleThe risk or severity of hypotension can be increased when Brexpiprazole is combined with Loperamide.Approved, Investigational
BromocriptineThe risk or severity of hypotension can be increased when Bromocriptine is combined with Loperamide.Approved, Investigational
BromperidolThe serum concentration of Bromperidol can be increased when it is combined with Loperamide.Approved, Investigational
BucindololThe risk or severity of hypotension can be increased when Bucindolol is combined with Loperamide.Investigational
BunazosinThe risk or severity of hypotension can be increased when Bunazosin is combined with Loperamide.Investigational
BuprenorphineThe serum concentration of Loperamide can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Loperamide can be increased when it is combined with Buspirone.Approved, Investigational
ButoconazoleThe therapeutic efficacy of Butoconazole can be increased when used in combination with Loperamide.Approved
CabazitaxelThe serum concentration of Loperamide can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Loperamide can be increased when it is combined with Caffeine.Approved
Calcium AcetateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Acetate.Approved, Investigational
Calcium CarbonateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Carbonate.Approved, Investigational
Calcium ChlorideThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Chloride.Approved
Calcium CitrateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Citrate.Approved
Calcium glubionateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
Calcium lactateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium lactate.Approved, Investigational, Vet Approved
Calcium lactate gluconateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium lactate gluconate.Experimental
Calcium levulinateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium levulinate.Approved, Experimental
Calcium pangamateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium pangamate.Experimental
Calcium PhosphateThe therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Phosphate.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Loperamide.Experimental
CanagliflozinThe serum concentration of Loperamide can be increased when it is combined with Canagliflozin.Approved
CaptoprilThe serum concentration of Loperamide can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Loperamide can be increased when combined with Carbamazepine.Approved, Investigational
CarboxymethylcelluloseThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Loperamide.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Loperamide.Approved, Investigational
CarvedilolThe risk or severity of hypotension can be increased when Carvedilol is combined with Loperamide.Approved, Investigational
Castor oilThe therapeutic efficacy of Castor oil can be decreased when used in combination with Loperamide.Approved, Investigational, Nutraceutical, Vet Approved
CefoperazoneThe serum concentration of Loperamide can be increased when it is combined with Cefoperazone.Approved, Investigational
CeftriaxoneThe serum concentration of Loperamide can be increased when it is combined with Ceftriaxone.Approved
CeliprololThe serum concentration of Celiprolol can be increased when it is combined with Loperamide.Approved, Investigational
CeritinibThe serum concentration of Loperamide can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Loperamide.Approved, Withdrawn
Cerliponase alfaThe serum concentration of Cerliponase alfa can be increased when it is combined with Loperamide.Approved, Investigational
ChlorambucilThe serum concentration of Chlorambucil can be increased when it is combined with Loperamide.Approved
ChloroformThe serum concentration of Loperamide can be increased when it is combined with Chloroform.Vet Approved
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
ChlorpromazineThe risk or severity of hypotension can be increased when Chlorpromazine is combined with Loperamide.Approved, Investigational, Vet Approved
ChlorprothixeneThe serum concentration of Loperamide can be increased when it is combined with Chlorprothixene.Approved, Investigational, Withdrawn
CimetidineThe serum concentration of Loperamide can be increased when it is combined with Cimetidine.Approved, Investigational
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Loperamide.Approved, Investigational
CisatracuriumLoperamide may increase the neuromuscular blocking activities of Cisatracurium.Approved
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Loperamide.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Loperamide.Approved
ClarithromycinThe metabolism of Loperamide can be decreased when combined with Clarithromycin.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Loperamide.Approved, Illicit
ClofazimineThe serum concentration of Loperamide can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Loperamide can be increased when it is combined with Clomipramine.Approved, Investigational, Vet Approved
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Loperamide.Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Loperamide.Approved
ClotrimazoleThe metabolism of Loperamide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of hypotension can be increased when Clozapine is combined with Loperamide.Approved
CobicistatThe metabolism of Loperamide can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Loperamide.Approved, Investigational
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Loperamide.Approved
Concanamycin AThe serum concentration of Loperamide can be increased when it is combined with Concanamycin A.Experimental
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Loperamide.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated estrogens can be increased when it is combined with Loperamide.Approved
CopanlisibThe serum concentration of Copanlisib can be increased when it is combined with Loperamide.Approved, Investigational
CrizotinibThe serum concentration of Loperamide can be increased when it is combined with Crizotinib.Approved
CurcuminThe metabolism of Loperamide can be decreased when combined with Curcumin.Approved, Investigational
CyclosporineThe serum concentration of Loperamide can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CytarabineThe serum concentration of Cytarabine can be increased when it is combined with Loperamide.Approved, Investigational
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Loperamide.Approved
DabrafenibThe serum concentration of Loperamide can be decreased when it is combined with Dabrafenib.Approved, Investigational
DaclatasvirThe serum concentration of Loperamide can be increased when it is combined with Daclatasvir.Approved, Investigational
DactinomycinThe serum concentration of Loperamide can be increased when it is combined with Dactinomycin.Approved, Investigational
DanazolThe metabolism of Loperamide can be decreased when combined with Danazol.Approved
DanthronThe therapeutic efficacy of Danthron can be decreased when used in combination with Loperamide.Approved, Investigational, Withdrawn
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Loperamide.Approved
DapiprazoleThe risk or severity of hypotension can be increased when Dapiprazole is combined with Loperamide.Approved
DarunavirThe metabolism of Loperamide can be decreased when combined with Darunavir.Approved
DasabuvirThe serum concentration of Dasabuvir can be increased when it is combined with Loperamide.Approved
DaunorubicinThe serum concentration of Loperamide can be increased when it is combined with Daunorubicin.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Loperamide.Approved, Investigational
DeferasiroxThe serum concentration of Loperamide can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Loperamide can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Loperamide can be increased when it is combined with Desipramine.Approved, Investigational
DesmethylsertralineThe serum concentration of Loperamide can be increased when it is combined with Desmethylsertraline.Experimental
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
DexniguldipineThe serum concentration of Loperamide can be increased when it is combined with Dexniguldipine.Experimental
DexverapamilThe serum concentration of Loperamide can be increased when it is combined with Dexverapamil.Experimental
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Loperamide.Approved, Illicit, Investigational, Vet Approved
Diethyl etherThe serum concentration of Loperamide can be increased when it is combined with Diethyl ether.Experimental
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Loperamide.Approved, Investigational
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Loperamide.Approved, Investigational
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Loperamide.Approved
DihydroergotamineThe risk or severity of hypotension can be increased when Dihydroergotamine is combined with Loperamide.Approved, Investigational
DiltiazemThe metabolism of Loperamide can be decreased when combined with Diltiazem.Approved, Investigational
DipyridamoleThe serum concentration of Loperamide can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Loperamide.Approved, Investigational
DocusateThe therapeutic efficacy of Docusate can be decreased when used in combination with Loperamide.Approved
DofequidarThe serum concentration of Loperamide can be increased when it is combined with Dofequidar.Experimental, Investigational
DolutegravirThe serum concentration of Dolutegravir can be increased when it is combined with Loperamide.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
DovitinibThe serum concentration of Loperamide can be increased when it is combined with Dovitinib.Investigational
DoxacuriumLoperamide may increase the neuromuscular blocking activities of Doxacurium.Approved
DoxazosinThe risk or severity of hypotension can be increased when Doxazosin is combined with Loperamide.Approved
DoxepinThe risk or severity of hypotension can be increased when Doxepin is combined with Loperamide.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Loperamide.Approved, Investigational
DoxycyclineThe metabolism of Loperamide can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Loperamide can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe risk or severity of hypotension can be increased when Dronedarone is combined with Loperamide.Approved
DroperidolThe risk or severity of hypotension can be increased when Droperidol is combined with Loperamide.Approved, Vet Approved
DuloxetineThe serum concentration of Loperamide can be increased when it is combined with Duloxetine.Approved
EconazoleThe serum concentration of Loperamide can be increased when it is combined with Econazole.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Loperamide.Approved
EfavirenzThe serum concentration of Loperamide can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe therapeutic efficacy of Efinaconazole can be increased when used in combination with Loperamide.Approved
ElacridarThe serum concentration of Loperamide can be increased when it is combined with Elacridar.Investigational
ElagolixThe serum concentration of Elagolix can be increased when it is combined with Loperamide.Approved, Investigational
ElbasvirThe serum concentration of Elbasvir can be increased when it is combined with Loperamide.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Loperamide.Approved, Investigational
EmopamilThe serum concentration of Loperamide can be increased when it is combined with Emopamil.Experimental
EnasidenibThe serum concentration of Loperamide can be increased when it is combined with Enasidenib.Approved, Investigational
EnzalutamideThe serum concentration of Loperamide can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Loperamide.Approved, Investigational
ErgonovineThe serum concentration of Loperamide can be increased when it is combined with Ergonovine.Approved
ErgotamineThe risk or severity of hypotension can be increased when Ergotamine is combined with Loperamide.Approved
ErlotinibThe serum concentration of Loperamide can be increased when it is combined with Erlotinib.Approved, Investigational
ErtugliflozinThe serum concentration of Ertugliflozin can be increased when it is combined with Loperamide.Approved, Investigational
ErythromycinThe serum concentration of Loperamide can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EsomeprazoleThe serum concentration of Loperamide can be increased when it is combined with Esomeprazole.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
Estradiol acetateThe serum concentration of Estradiol acetate can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
Estradiol benzoateThe serum concentration of Estradiol benzoate can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
Estradiol cypionateThe serum concentration of Estradiol cypionate can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
Estradiol dienanthateThe serum concentration of Estradiol dienanthate can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
Estradiol valerateThe serum concentration of Estradiol valerate can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Loperamide can be increased when it is combined with Estramustine.Approved, Investigational
EstriolThe serum concentration of Estriol can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Loperamide.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Loperamide.Approved
EtoposideThe serum concentration of Loperamide can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Loperamide can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Loperamide.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Loperamide.Approved
FelodipineThe serum concentration of Loperamide can be increased when it is combined with Felodipine.Approved, Investigational
FenofibrateThe serum concentration of Loperamide can be increased when it is combined with Fenofibrate.Approved
FentanylThe serum concentration of Loperamide can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenticonazoleThe therapeutic efficacy of Fenticonazole can be increased when used in combination with Loperamide.Experimental
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Loperamide.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Loperamide.Approved, Investigational
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Loperamide.Approved
Fluciclovine (18F)The serum concentration of Fluciclovine (18F) can be increased when it is combined with Loperamide.Approved
FluconazoleThe serum concentration of Loperamide can be increased when it is combined with Fluconazole.Approved, Investigational
FluoxetineThe serum concentration of Loperamide can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of hypotension can be increased when Flupentixol is combined with Loperamide.Approved, Investigational, Withdrawn
FluphenazineThe serum concentration of Loperamide can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Loperamide can be increased when it is combined with Flurazepam.Approved, Illicit, Investigational
FluticasoneThe serum concentration of Fluticasone can be increased when it is combined with Loperamide.Approved, Experimental, Investigational
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Loperamide.Approved
Fluticasone propionateThe serum concentration of Fluticasone propionate can be increased when it is combined with Loperamide.Approved
FlutrimazoleThe therapeutic efficacy of Flutrimazole can be increased when used in combination with Loperamide.Experimental
FluvoxamineThe serum concentration of Loperamide can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Loperamide can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Loperamide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Loperamide.Approved, Investigational
Fusidic AcidThe serum concentration of Loperamide can be increased when it is combined with Fusidic Acid.Approved, Investigational
GallamineLoperamide may increase the neuromuscular blocking activities of Gallamine.Experimental
Gallamine TriethiodideLoperamide may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
GallopamilThe serum concentration of Loperamide can be increased when it is combined with Gallopamil.Investigational
GefitinibThe serum concentration of Loperamide can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Loperamide can be increased when it is combined with Genistein.Investigational
GlecaprevirThe serum concentration of Loperamide can be increased when it is combined with Glecaprevir.Approved, Investigational
GlyburideThe serum concentration of Loperamide can be increased when it is combined with Glyburide.Approved
GlycerinThe serum concentration of Loperamide can be increased when it is combined with Glycerin.Approved, Investigational
Gramicidin DThe serum concentration of Loperamide can be increased when it is combined with Gramicidin D.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Loperamide.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Loperamide.Approved, Investigational, Withdrawn
HexobarbitalThe metabolism of Loperamide can be increased when combined with Hexobarbital.Approved
HM-30181The serum concentration of Loperamide can be increased when it is combined with HM-30181.Experimental
HycanthoneThe serum concentration of Loperamide can be increased when it is combined with Hycanthone.Approved, Investigational
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Loperamide.Approved, Vet Approved
HydroxychloroquineThe serum concentration of Loperamide can be increased when it is combined with Hydroxychloroquine.Approved
HydroxyureaThe serum concentration of Hydroxyurea can be increased when it is combined with Loperamide.Approved
IbuprofenThe serum concentration of Loperamide can be increased when it is combined with Ibuprofen.Approved
IdelalisibThe metabolism of Loperamide can be decreased when combined with Idelalisib.Approved
IloperidoneThe risk or severity of hypotension can be increased when Iloperidone is combined with Loperamide.Approved
ImatinibThe serum concentration of Loperamide can be increased when it is combined with Imatinib.Approved
ImipramineThe risk or severity of hypotension can be increased when Imipramine is combined with Loperamide.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Loperamide.Approved
IndinavirThe metabolism of Loperamide can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Loperamide can be increased when it is combined with Indomethacin.Approved, Investigational
IndoraminThe risk or severity of hypotension can be increased when Indoramin is combined with Loperamide.Withdrawn
Inotuzumab ozogamicinThe serum concentration of Inotuzumab ozogamicin can be increased when it is combined with Loperamide.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Loperamide.Approved, Investigational
IsavuconazoleThe serum concentration of Loperamide can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe serum concentration of Loperamide can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoconazoleThe therapeutic efficacy of Isoconazole can be increased when used in combination with Loperamide.Approved
IsoniazidThe metabolism of Loperamide can be decreased when combined with Isoniazid.Approved, Investigational
IsradipineThe serum concentration of Loperamide can be increased when it is combined with Isradipine.Approved, Investigational
ItraconazoleThe metabolism of Loperamide can be decreased when combined with Itraconazole.Approved, Investigational
IvermectinThe serum concentration of Loperamide can be increased when it is combined with Ivermectin.Approved, Investigational, Vet Approved
IvosidenibThe serum concentration of Ivosidenib can be increased when it is combined with Loperamide.Approved, Investigational
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Loperamide.Approved
KetoconazoleThe metabolism of Loperamide can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe risk or severity of hypotension can be increased when Labetalol is combined with Loperamide.Approved
LactitolThe therapeutic efficacy of Lactitol can be decreased when used in combination with Loperamide.Investigational
LactuloseThe therapeutic efficacy of Lactulose can be decreased when used in combination with Loperamide.Approved
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Loperamide.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Loperamide.Approved, Investigational
LaniquidarThe serum concentration of Loperamide can be increased when it is combined with Laniquidar.Investigational
LansoprazoleThe serum concentration of Loperamide can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Loperamide can be increased when it is combined with Lapatinib.Approved, Investigational
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Loperamide.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Loperamide.Approved, Investigational
LetermovirThe serum concentration of Loperamide can be increased when it is combined with Letermovir.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Loperamide.Approved, Investigational
LevofloxacinThe serum concentration of Loperamide can be increased when it is combined with Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Loperamide.Approved, Investigational
LidocaineThe serum concentration of Loperamide can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinaclotideThe therapeutic efficacy of Linaclotide can be decreased when used in combination with Loperamide.Approved
LinagliptinThe serum concentration of Loperamide can be increased when it is combined with Linagliptin.Approved
LomerizineThe serum concentration of Loperamide can be increased when it is combined with Lomerizine.Experimental
LomitapideThe serum concentration of Loperamide can be increased when it is combined with Lomitapide.Approved, Investigational
LonafarnibThe serum concentration of Loperamide can be increased when it is combined with Lonafarnib.Investigational
LopinavirThe metabolism of Loperamide can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Loperamide can be increased when it is combined with Loratadine.Approved, Investigational
LorpiprazoleThe serum concentration of Loperamide can be increased when it is combined with Lorpiprazole.Approved
LosartanThe serum concentration of Loperamide can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Loperamide can be increased when it is combined with Lovastatin.Approved, Investigational
LoxapineThe serum concentration of Loperamide can be increased when it is combined with Loxapine.Approved
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Loperamide.Approved, Investigational
LuliconazoleThe serum concentration of Loperamide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Loperamide can be decreased when it is combined with Lumacaftor.Approved
LusutrombopagThe serum concentration of Lusutrombopag can be increased when it is combined with Loperamide.Approved, Investigational
Magnesium carbonateThe therapeutic efficacy of Magnesium carbonate can be decreased when used in combination with Loperamide.Approved, Investigational
Magnesium citrateThe therapeutic efficacy of Magnesium citrate can be decreased when used in combination with Loperamide.Approved
Magnesium hydroxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium hydroxide.Approved, Investigational
Magnesium oxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium oxide.Approved
Magnesium peroxideThe therapeutic efficacy of Magnesium peroxide can be decreased when used in combination with Loperamide.Experimental
Magnesium salicylateThe risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium salicylate.Approved
Magnesium sulfateThe risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium sulfate.Approved, Investigational, Vet Approved
MannitolThe therapeutic efficacy of Mannitol can be decreased when used in combination with Loperamide.Approved, Investigational
MefloquineThe serum concentration of Loperamide can be increased when it is combined with Mefloquine.Approved, Investigational
Megestrol acetateThe serum concentration of Loperamide can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
MelphalanThe serum concentration of Melphalan can be increased when it is combined with Loperamide.Approved
MethadoneThe serum concentration of Loperamide can be increased when it is combined with Methadone.Approved
MethohexitalThe metabolism of Loperamide can be increased when combined with Methohexital.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Loperamide.Approved
MethotrimeprazineThe risk or severity of hypotension can be increased when Methotrimeprazine is combined with Loperamide.Approved, Investigational
Methyl celluloseThe therapeutic efficacy of Methyl cellulose can be decreased when used in combination with Loperamide.Approved
MethylphenobarbitalThe metabolism of Loperamide can be increased when combined with Methylphenobarbital.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Loperamide.Approved, Vet Approved
MetocurineLoperamide may increase the neuromuscular blocking activities of Metocurine.Approved
Metocurine IodideLoperamide may increase the neuromuscular blocking activities of Metocurine Iodide.Approved, Withdrawn
MetronidazoleThe serum concentration of Loperamide can be increased when it is combined with Metronidazole.Approved
MibefradilThe metabolism of Loperamide can be decreased when combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Loperamide can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Loperamide can be increased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Loperamide can be increased when it is combined with Mifepristone.Approved, Investigational
Mineral oilThe therapeutic efficacy of Mineral oil can be decreased when used in combination with Loperamide.Approved, Vet Approved
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Loperamide.Approved
MitomycinThe serum concentration of Mitomycin can be increased when it is combined with Loperamide.Approved
MitotaneThe serum concentration of Loperamide can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Loperamide can be increased when it is combined with Mitoxantrone.Approved, Investigational
MivacuriumLoperamide may increase the neuromuscular blocking activities of Mivacurium.Approved
ModafinilThe serum concentration of Loperamide can be decreased when it is combined with Modafinil.Approved, Investigational
MonensinThe serum concentration of Loperamide can be increased when it is combined with Monensin.Vet Approved
MorphineThe serum concentration of Morphine can be increased when it is combined with Loperamide.Approved, Investigational
MoxidectinThe serum concentration of Moxidectin can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Loperamide.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Loperamide.Approved
NafcillinThe therapeutic efficacy of Loperamide can be decreased when used in combination with Nafcillin.Approved, Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Loperamide.Approved
NaloxoneThe metabolism of Loperamide can be decreased when combined with Naloxone.Approved, Vet Approved
NefazodoneThe risk or severity of hypotension can be increased when Nefazodone is combined with Loperamide.Approved, Withdrawn
NelfinavirThe metabolism of Loperamide can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Neostigmine can be increased when it is combined with Loperamide.Approved, Vet Approved
NeratinibThe serum concentration of Loperamide can be increased when it is combined with Neratinib.Approved, Investigational
NetupitantThe serum concentration of Loperamide can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Loperamide can be increased when combined with Nevirapine.Approved
NicardipineThe risk or severity of hypotension can be increased when Nicardipine is combined with Loperamide.Approved, Investigational
NicergolineThe risk or severity of hypotension can be increased when Nicergoline is combined with Loperamide.Approved, Investigational
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Loperamide.Approved
NigericinThe serum concentration of Loperamide can be increased when it is combined with Nigericin.Experimental
NiguldipineThe risk or severity of hypotension can be increased when Niguldipine is combined with Loperamide.Experimental
NilotinibThe metabolism of Loperamide can be decreased when combined with Nilotinib.Approved, Investigational
NimodipineThe serum concentration of Loperamide can be increased when it is combined with Nimodipine.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Loperamide.Approved
NisoldipineThe serum concentration of Loperamide can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Loperamide can be increased when it is combined with Nitrendipine.Approved, Investigational
NitroprussideLoperamide may increase the hypotensive activities of Nitroprusside.Approved, Investigational
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Loperamide.Approved
NortriptylineThe risk or severity of hypotension can be increased when Nortriptyline is combined with Loperamide.Approved
OctreotideThe serum concentration of Octreotide can be increased when it is combined with Loperamide.Approved, Investigational
OdanacatibThe serum concentration of Odanacatib can be increased when it is combined with Loperamide.Investigational
OlanzapineThe risk or severity of hypotension can be increased when Olanzapine is combined with Loperamide.Approved, Investigational
OlaparibThe metabolism of Loperamide can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Loperamide.Approved, Investigational
OmeprazoleThe serum concentration of Loperamide can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OmoconazoleThe therapeutic efficacy of Omoconazole can be increased when used in combination with Loperamide.Experimental
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Loperamide.Approved
ONT-093The serum concentration of Loperamide can be increased when it is combined with ONT-093.Investigational
OxiconazoleThe therapeutic efficacy of Oxiconazole can be increased when used in combination with Loperamide.Approved
OxyphenisatinThe therapeutic efficacy of Oxyphenisatin can be decreased when used in combination with Loperamide.Investigational, Withdrawn
PaclitaxelThe serum concentration of Loperamide can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Loperamide can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneThe risk or severity of hypotension can be increased when Paliperidone is combined with Loperamide.Approved
PancuroniumLoperamide may increase the neuromuscular blocking activities of Pancuronium.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Loperamide.Approved, Investigational
PantoprazoleThe serum concentration of Loperamide can be increased when it is combined with Pantoprazole.Approved
ParitaprevirThe serum concentration of Loperamide can be increased when it is combined with Paritaprevir.Approved, Investigational
ParoxetineThe serum concentration of Loperamide can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Loperamide.Approved
PentaerithritylThe therapeutic efficacy of Pentaerithrityl can be decreased when used in combination with Loperamide.Experimental
PentazocineThe serum concentration of Loperamide can be increased when it is combined with Pentazocine.Approved, Vet Approved
PentobarbitalThe metabolism of Loperamide can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PethidineThe serum concentration of Loperamide can be increased when it is combined with Pethidine.Approved
PhenobarbitalThe metabolism of Loperamide can be increased when combined with Phenobarbital.Approved, Investigational
PhenolphthaleinThe therapeutic efficacy of Phenolphthalein can be decreased when used in combination with Loperamide.Approved, Withdrawn
PhenothiazineThe serum concentration of Phenothiazine can be increased when it is combined with Loperamide.Vet Approved
PhenoxybenzamineThe risk or severity of hypotension can be increased when Phenoxybenzamine is combined with Loperamide.Approved
PhentolamineThe risk or severity of hypotension can be increased when Phentolamine is combined with Loperamide.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Loperamide.Approved, Vet Approved
PibrentasvirThe serum concentration of Loperamide can be increased when it is combined with Pibrentasvir.Approved, Investigational
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Loperamide.Approved
PimozideThe serum concentration of Loperamide can be increased when it is combined with Pimozide.Approved
PipecuroniumLoperamide may increase the neuromuscular blocking activities of Pipecuronium.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Loperamide.Approved
PitolisantThe serum concentration of Loperamide can be decreased when it is combined with Pitolisant.Approved, Investigational
PizotifenThe risk or severity of hypotension can be increased when Pizotifen is combined with Loperamide.Approved
Plantago seedThe therapeutic efficacy of Plantago seed can be decreased when used in combination with Loperamide.Approved, Investigational
PlecanatideThe therapeutic efficacy of Plecanatide can be decreased when used in combination with Loperamide.Approved, Investigational
PolycarbophilThe therapeutic efficacy of Polycarbophil can be decreased when used in combination with Loperamide.Approved
Polyethylene glycolThe therapeutic efficacy of Polyethylene glycol can be decreased when used in combination with Loperamide.Approved, Vet Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Loperamide.Approved
PonatinibThe serum concentration of Loperamide can be increased when it is combined with Ponatinib.Approved, Investigational
PosaconazoleThe metabolism of Loperamide can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium acetateThe therapeutic efficacy of Potassium acetate can be decreased when used in combination with Loperamide.Approved, Investigational
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Loperamide.Approved
PrazosinThe risk or severity of hypotension can be increased when Prazosin is combined with Loperamide.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Loperamide.Approved, Vet Approved
PrednisoneThe serum concentration of Loperamide can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimaquineThe serum concentration of Loperamide can be increased when it is combined with Primaquine.Approved
PrimidoneThe metabolism of Loperamide can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Loperamide can be increased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe risk or severity of hypotension can be increased when Promazine is combined with Loperamide.Approved, Vet Approved
PromethazineThe serum concentration of Loperamide can be increased when it is combined with Promethazine.Approved, Investigational
PropafenoneThe serum concentration of Loperamide can be increased when it is combined with Propafenone.Approved
PropericiazineThe risk or severity of hypotension can be increased when Propericiazine is combined with Loperamide.Approved, Investigational
PropiomazineThe risk or severity of hypotension can be increased when Propiomazine is combined with Loperamide.Approved
PropiverineThe risk or severity of hypotension can be increased when Propiverine is combined with Loperamide.Approved, Investigational
PropofolThe serum concentration of Loperamide can be increased when it is combined with Propofol.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Loperamide.Approved, Investigational
ProtriptylineThe serum concentration of Loperamide can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Loperamide.Approved
QuercetinThe serum concentration of Loperamide can be increased when it is combined with Quercetin.Experimental, Investigational
QuetiapineThe risk or severity of hypotension can be increased when Quetiapine is combined with Loperamide.Approved
QuinacrineThe serum concentration of Loperamide can be increased when it is combined with Quinacrine.Approved, Investigational
QuinidineThe risk or severity of hypotension can be increased when Quinidine is combined with Loperamide.Approved, Investigational
QuinineThe metabolism of Loperamide can be increased when combined with Quinine.Approved
RanitidineThe serum concentration of Loperamide can be increased when it is combined with Ranitidine.Approved
RapacuroniumLoperamide may increase the neuromuscular blocking activities of Rapacuronium.Withdrawn
RavuconazoleThe therapeutic efficacy of Ravuconazole can be increased when used in combination with Loperamide.Investigational
ReboxetineThe serum concentration of Loperamide can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Loperamide.Approved
ReserpineThe serum concentration of Loperamide can be increased when it is combined with Reserpine.Approved, Investigational
Reversin 121The serum concentration of Loperamide can be increased when it is combined with Reversin 121.Experimental
Rhodamine 6GThe serum concentration of Rhodamine 6G can be increased when it is combined with Loperamide.Experimental
RifampicinThe metabolism of Loperamide can be increased when combined with Rifampicin.Approved
RifamycinThe metabolism of Loperamide can be increased when combined with Rifamycin.Investigational
RifapentineThe metabolism of Loperamide can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Loperamide.Approved, Investigational
RilpivirineThe serum concentration of Loperamide can be increased when it is combined with Rilpivirine.Approved
RimexoloneThe metabolism of Loperamide can be increased when combined with Rimexolone.Approved
RisperidoneThe risk or severity of hypotension can be increased when Risperidone is combined with Loperamide.Approved, Investigational
RitonavirThe metabolism of Loperamide can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Loperamide.Approved
RocuroniumLoperamide may increase the neuromuscular blocking activities of Rocuronium.Approved
RolapitantThe serum concentration of Loperamide can be increased when it is combined with Rolapitant.Approved, Investigational
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Loperamide.Approved, Investigational
RucaparibThe serum concentration of Loperamide can be increased when it is combined with Rucaparib.Approved, Investigational
SalinomycinThe serum concentration of Loperamide can be increased when it is combined with Salinomycin.Vet Approved
SaquinavirThe metabolism of Loperamide can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Loperamide can be decreased when used in combination with Sarilumab.Approved, Investigational
SecobarbitalThe metabolism of Loperamide can be increased when combined with Secobarbital.Approved, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Loperamide.Approved
SennosidesThe therapeutic efficacy of Sennosides can be decreased when used in combination with Loperamide.Approved
SertaconazoleThe therapeutic efficacy of Sertaconazole can be increased when used in combination with Loperamide.Approved, Investigational
SertralineThe serum concentration of Loperamide can be increased when it is combined with Sertraline.Approved
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Loperamide.Approved
SiltuximabThe serum concentration of Loperamide can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Loperamide can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Loperamide.Approved
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Loperamide.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Loperamide.Approved, Investigational
Sodium phosphate, monobasicThe therapeutic efficacy of Sodium phosphate, monobasic can be decreased when used in combination with Loperamide.Approved
Sodium sulfateThe therapeutic efficacy of Sodium sulfate can be decreased when used in combination with Loperamide.Approved, Vet Approved
Sodium tartrateThe therapeutic efficacy of Sodium tartrate can be decreased when used in combination with Loperamide.Approved
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Loperamide.Approved
SomatostatinThe serum concentration of Somatostatin can be increased when it is combined with Loperamide.Approved, Investigational
SorafenibThe serum concentration of Loperamide can be increased when it is combined with Sorafenib.Approved, Investigational
SorbitolThe therapeutic efficacy of Sorbitol can be decreased when used in combination with Loperamide.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Loperamide.Approved, Investigational
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Loperamide.Experimental
St. John's WortThe serum concentration of Loperamide can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StanoloneThe serum concentration of Stanolone can be increased when it is combined with Loperamide.Illicit, Investigational
Stanolone acetateThe serum concentration of Stanolone acetate can be increased when it is combined with Loperamide.Experimental
StaurosporineThe serum concentration of Loperamide can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Loperamide can be increased when it is combined with Stiripentol.Approved
SulconazoleThe therapeutic efficacy of Sulconazole can be increased when used in combination with Loperamide.Approved
SumatriptanThe serum concentration of Sumatriptan can be increased when it is combined with Loperamide.Approved, Investigational
SunitinibThe serum concentration of Loperamide can be increased when it is combined with Sunitinib.Approved, Investigational
SuvorexantThe serum concentration of Loperamide can be increased when it is combined with Suvorexant.Approved, Investigational
TacrineThe serum concentration of Tacrine can be increased when it is combined with Loperamide.Investigational, Withdrawn
TacrolimusThe serum concentration of Loperamide can be increased when it is combined with Tacrolimus.Approved, Investigational
TalinololThe serum concentration of Talinolol can be increased when it is combined with Loperamide.Investigational
TamoxifenThe serum concentration of Loperamide can be increased when it is combined with Tamoxifen.Approved
TamsulosinThe risk or severity of hypotension can be increased when Tamsulosin is combined with Loperamide.Approved, Investigational
TariquidarThe serum concentration of Loperamide can be increased when it is combined with Tariquidar.Investigational
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Loperamide.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Loperamide.Approved, Investigational
TegaserodThe therapeutic efficacy of Tegaserod can be decreased when used in combination with Loperamide.Approved, Investigational, Withdrawn
TelaprevirThe metabolism of Loperamide can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Loperamide can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Loperamide can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Loperamide can be increased when it is combined with Temsirolimus.Approved
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Loperamide.Approved
TerazosinThe risk or severity of hypotension can be increased when Terazosin is combined with Loperamide.Approved
TerconazoleThe therapeutic efficacy of Terconazole can be increased when used in combination with Loperamide.Approved
TerfenadineThe serum concentration of Loperamide can be increased when it is combined with Terfenadine.Approved, Withdrawn
TesmilifeneThe serum concentration of Loperamide can be increased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Loperamide can be increased when it is combined with Testosterone.Approved, Investigational
Testosterone cypionateThe serum concentration of Loperamide can be increased when it is combined with Testosterone cypionate.Approved
Testosterone enanthateThe serum concentration of Loperamide can be increased when it is combined with Testosterone enanthate.Approved
Testosterone propionateThe serum concentration of Testosterone propionate can be increased when it is combined with Loperamide.Approved, Investigational, Vet Approved, Withdrawn
Testosterone undecanoateThe serum concentration of Loperamide can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
TetracyclineThe serum concentration of Tetracycline can be increased when it is combined with Loperamide.Approved, Vet Approved
TetrandrineThe serum concentration of Loperamide can be increased when it is combined with Tetrandrine.Experimental
ThiamylalThe metabolism of Loperamide can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Loperamide can be increased when combined with Thiopental.Approved, Vet Approved
ThioproperazineThe risk or severity of hypotension can be increased when Thioproperazine is combined with Loperamide.Approved
ThioridazineThe risk or severity of hypotension can be increased when Thioridazine is combined with Loperamide.Approved, Withdrawn
TicagrelorThe serum concentration of Loperamide can be increased when it is combined with Ticagrelor.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Loperamide.Approved
TioconazoleThe therapeutic efficacy of Tioconazole can be increased when used in combination with Loperamide.Approved
TipifarnibThe serum concentration of Loperamide can be increased when it is combined with Tipifarnib.Investigational
TipranavirThe metabolism of Loperamide can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Loperamide can be decreased when it is combined with Tocilizumab.Approved
TolazolineThe risk or severity of hypotension can be increased when Tolazoline is combined with Loperamide.Approved, Vet Approved
TolvaptanThe serum concentration of Loperamide can be increased when it is combined with Tolvaptan.Approved
TopiramateThe serum concentration of Topiramate can be increased when it is combined with Loperamide.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Loperamide.Approved, Investigational
ToremifeneThe serum concentration of Loperamide can be increased when it is combined with Toremifene.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Loperamide.Approved, Investigational
TrazodoneThe risk or severity of hypotension can be increased when Trazodone is combined with Loperamide.Approved, Investigational
TrifluoperazineThe risk or severity of hypotension can be increased when Trifluoperazine is combined with Loperamide.Approved, Investigational
TriflupromazineThe serum concentration of Loperamide can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimazosinThe risk or severity of hypotension can be increased when Trimazosin is combined with Loperamide.Experimental
TrimethoprimThe serum concentration of Loperamide can be increased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe risk or severity of hypotension can be increased when Trimipramine is combined with Loperamide.Approved
TroleandomycinThe metabolism of Loperamide can be decreased when combined with Troleandomycin.Approved
TubocurarineLoperamide may increase the neuromuscular blocking activities of Tubocurarine.Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Loperamide.Approved, Investigational, Nutraceutical
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Loperamide.Approved
UrapidilThe risk or severity of hypotension can be increased when Urapidil is combined with Loperamide.Investigational
ValinomycinThe serum concentration of Loperamide can be increased when it is combined with Valinomycin.Experimental
ValspodarThe serum concentration of Loperamide can be increased when it is combined with Valspodar.Investigational
VecuroniumLoperamide may increase the neuromuscular blocking activities of Vecuronium.Approved
VelpatasvirThe serum concentration of Loperamide can be increased when it is combined with Velpatasvir.Approved, Investigational
VemurafenibThe risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Loperamide.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Loperamide.Approved, Investigational
VenlafaxineThe serum concentration of Loperamide can be increased when it is combined with Venlafaxine.Approved
VerapamilThe risk or severity of hypotension can be increased when Verapamil is combined with Loperamide.Approved
VinblastineThe serum concentration of Loperamide can be increased when it is combined with Vinblastine.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Loperamide.Approved, Investigational
VinflunineThe serum concentration of Vinflunine can be increased when it is combined with Loperamide.Approved, Investigational
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Loperamide.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Loperamide.Approved, Investigational
VoacamineThe serum concentration of Loperamide can be increased when it is combined with Voacamine.Approved, Investigational
VorapaxarThe serum concentration of Loperamide can be increased when it is combined with Vorapaxar.Approved
VoriconazoleThe metabolism of Loperamide can be decreased when combined with Voriconazole.Approved, Investigational
VoxilaprevirThe serum concentration of Loperamide can be increased when it is combined with Voxilaprevir.Approved, Investigational
YohimbineThe serum concentration of Loperamide can be increased when it is combined with Yohimbine.Approved, Investigational, Vet Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Loperamide.Approved
ZiprasidoneThe risk or severity of hypotension can be increased when Ziprasidone is combined with Loperamide.Approved
ZomepiracThe serum concentration of Loperamide can be increased when it is combined with Zomepirac.Withdrawn
ZosuquidarThe serum concentration of Loperamide can be increased when it is combined with Zosuquidar.Investigational
ZuclopenthixolThe risk or severity of hypotension can be increased when Zuclopenthixol is combined with Loperamide.Approved, Investigational
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
HMDB0004999
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, combinationsA07DA03 — LoperamideA07DA05 — Loperamide oxide
AHFS Codes
  • 56:08.00 — Antidiarrhea Agents
FDA label
Download (55.5 KB)
MSDS
Download (73.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentPain1
1CompletedBasic ScienceDrug Interactions1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceIntestinal Obstruction2
1CompletedTreatmentHealthy Volunteers2
1RecruitingTreatmentNeoplasms, Breast1
2CompletedTreatmentCancer, Breast / Early-Stage Breast Carcinoma / Hormone Receptor Positive Tumor1
2RecruitingTreatmentEarly Stage HER2+ Breast Cancer1
2RecruitingTreatmentHer2-Positive Breast Cancer1
2WithdrawnTreatmentCancers1
2, 3CompletedTreatmentDiarrhea-predominant Irritable Bowel Syndrome / Functional Diarrhea1
2, 3CompletedTreatmentFemale Genital Diseases1
2, 3CompletedTreatmentIncontinence, Fecal1
2, 3Not Yet RecruitingTreatmentClostridium Difficile Infection (CDI)1
3CompletedSupportive CareColorectal Cancers / Diarrhea1
3CompletedTreatmentDiarrhea1
3CompletedTreatmentIncontinence, Fecal1
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3TerminatedPreventionDehydration, Diverting Ileostomy, Loperamide1
3TerminatedPreventionDiarrhea1
3TerminatedTreatmentCancers / Diarrhea / Enteritis1
3TerminatedTreatmentHigh Output Stoma1
3TerminatedTreatmentRectal Carcinoma / Short Bowel Syndrome (SBS) / Ulcerative Colitis (UC)1
4CompletedTreatmentDiarrhea3
4CompletedTreatmentTravelers' Diarrhea1
4RecruitingTreatmentOpiate withdrawal symptoms1
4SuspendedTreatmentAntibiotic Associated Diarrhea / Antibiotic-Associated Diarrhea / Clostridium Difficile1
4TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4WithdrawnTreatmentIncontinence, Fecal1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedTreatmentIncontinence, Fecal1
Not AvailableNot Yet RecruitingBasic ScienceIntestinal Transit1
Not AvailableRecruitingTreatmentIncontinence, Fecal1
Not AvailableTerminatedTreatmentIncontinence, Fecal1

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
FormRouteStrength
SolutionOral1 mg/5mL
Capsule, liquid filledOral2 mg/1
KitOral
SolutionOral.2 mg
LiquidOral1 mg/5mL
Tablet, film coatedOral2 mg/1
SolutionOral1 mg/7.5mL
Tablet, coatedOral2 mg/1
SolutionOral2 mg
TabletOral
Tablet, chewableOral
CapsuleOral2 mg
LiquidOral.2 mg
CapsuleOral2 mg/1
LiquidOral1 mg/7.5mL
SolutionOral2 mg/10mL
SuspensionOral1 mg/7.5mL
TabletOral2 mg
SolutionOral0.2 mg
TabletOral2 mg/1
Prices
Unit descriptionCostUnit
Loperamide hcl powder26.01USD g
Loperamide HCl 2 mg capsule0.64USD capsule
Imodium a-d 2 mg caplet0.49USD caplet
Imodium advanced caplet0.46USD caplet
Imodium ms relief caplet0.46USD caplet
Kaopectate 262 mg caplet0.37USD caplet
Loperamide 2 mg caplet0.37USD caplet
Qc anti-diarrheal adv caplet0.3USD caplet
Diamode 2 mg tablet0.28USD tablet
Kaopectate 240 mg softgel0.25USD softgel capsule
Anti-diarrheal 2 mg caplet0.18USD caplet
CVS Pharmacy anti-diarrheal 2 mg caplet0.14USD caplet
Kaopectate children's suspension0.02USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2134611No2002-12-242014-10-28Canada
US6814978Yes2002-02-262022-02-26Us
US6103260No1997-07-172017-07-17Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)222.1U.S. Patent 3,714,159; 3,884,916.
water solubilitySlightNot Available
logP5.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00086 mg/mLALOGPS
logP4.44ALOGPS
logP4.77ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)13.96ChemAxon
pKa (Strongest Basic)9.41ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area43.78 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity139.32 m3·mol-1ChemAxon
Polarizability52.67 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9878
Blood Brain Barrier+0.7709
Caco-2 permeable+0.5875
P-glycoprotein substrateSubstrate0.7476
P-glycoprotein inhibitor IInhibitor0.8277
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterInhibitor0.5059
CYP450 2C9 substrateNon-substrate0.8057
CYP450 2D6 substrateNon-substrate0.5315
CYP450 3A4 substrateSubstrate0.7918
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9154
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9207
Ames testNon AMES toxic0.768
CarcinogenicityNon-carcinogens0.8564
BiodegradationNot ready biodegradable0.9953
Rat acute toxicity3.6560 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9461
hERG inhibition (predictor II)Inhibitor0.7639
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
MS/MS Spectrum - Quattro_QQQ 10V, PositiveLC-MS/MSsplash10-004i-0000900000-673950710672b433271c
MS/MS Spectrum - Quattro_QQQ 25V, PositiveLC-MS/MSsplash10-014i-0090000000-4b7b347a8b8e9dca406c
MS/MS Spectrum - Quattro_QQQ 40V, PositiveLC-MS/MSsplash10-02t9-0090000000-31f15df976e23e73330a
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, PositiveLC-MS/MSsplash10-004i-0000900000-d91d13c4e4665bd5fb5a
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, PositiveLC-MS/MSsplash10-004i-0020900000-f1be3181a6918c985ffd
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, PositiveLC-MS/MSsplash10-014i-0090000000-e5e41346303f41f65688
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, PositiveLC-MS/MSsplash10-014i-0090000000-acd8b87c1338e5d0fe25
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, PositiveLC-MS/MSsplash10-014i-0090000000-81b85f788d14641430fd
LC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , PositiveLC-MS/MSsplash10-014i-0090000000-3ce1a89454d777268799
LC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , PositiveLC-MS/MSsplash10-03di-0090000000-f101d63ad0bf8e5d2178
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004i-0000900000-d91d13c4e4665bd5fb5a
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004i-0020900000-f1be3181a6918c985ffd
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-0090000000-e5e41346303f41f65688
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-0090000000-acd8b87c1338e5d0fe25
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-0090000000-81b85f788d14641430fd
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-014i-0090000000-1a1a49f09397ad090e82
MS/MS Spectrum - , positiveLC-MS/MSsplash10-016r-0090600000-794ea6214c0cd97c73fa
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-016r-0090300000-e11942e343a28799a5ab
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot 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

Details
1. 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
  1. 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]
  2. 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]
  3. 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]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  5. 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]
  6. 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]
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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. 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]
  3. 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]
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
  1. 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]
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
  1. 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]
  2. 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]
  3. 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]
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
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
  1. Daly JW, Harper J: Loperamide: novel effects on capacitative calcium influx. Cell Mol Life Sci. 2000 Jan 20;57(1):149-57. [PubMed:10949586]
  2. 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]
  3. Mellstrand T: Loperamide--an opiate receptor agonist with gastrointestinal motility effects. Scand J Gastroenterol Suppl. 1987;130:65-6. [PubMed:2820051]
  4. 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]
  5. 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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Curator comments
Inverse agonist at the canonical form of the receptor. Likely an antagonist at isoform 3 of the receptor.
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
  1. 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

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
  1. Baker DE: Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8. [PubMed:18192961]
  2. 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]
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
  1. 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]
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
  1. 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]
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
  1. 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

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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
  1. 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]
  2. 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]
  3. 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 August 15, 2018 09:45