Jump to section
IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- 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
Structure for DB00836 (Loperamide)
- Synonyms
- Loperamid
- Loperamida
- Lopéramide
- Loperamidum
- External IDs
- PJ 185 / R 18553
- Product Ingredients
Ingredient UNII CAS InChI Key Loperamide hydrochloride 77TI35393C 34552-83-5 PGYPOBZJRVSMDS-UHFFFAOYSA-N Loperamide oxide NG66S4H2RL 106900-12-3 KXVSBTJVTUVNPM-UHFFFAOYSA-N - Product Images
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Loperamide Hydrochloride Capsule 2 mg/1 Oral Mylan Institutional 1997-03-10 Not applicable US 
Loperamide Hydrochloride Capsule 2 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 2012-10-12 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Contract Pharmacy Services Pa 2017-09-20 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Cardinal Health 1991-09-18 2015-12-29 US Loperamide Hydrochloride Capsule 2 mg/1 Oral Aidarex Pharmaceuticals LLC 1993-05-01 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Remedy Repack 2016-12-12 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Directrx 2014-01-01 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Nucare Pharmaceuticals, Inc. 1993-05-01 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Physicians Total Care, Inc. 1996-06-20 Not applicable US Loperamide Hydrochloride Capsule 2 mg/1 Oral Nu Care Pharmceuticals,inc. 1993-05-01 Not applicable US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End 7 Select Anti Diarrheal Tablet, film coated 2 mg/1 Oral 7 Eleven 2014-08-05 Not applicable US A D Tablet, film coated 2 mg/1 Oral Western Family Foods 2003-04-10 2017-12-01 US A D Tablet, film coated 2 mg/1 Oral Western Family Foods 2003-02-25 2017-12-01 US Alti-loperamide - 2mg Caplet Tablet 2 mg Oral Altimed Pharma Inc. 1995-12-31 1997-08-14 Canada 
Anti Diarrheal Solution 1 mg/5mL Oral Rite Aid 1992-07-13 2017-11-14 US Anti Diarrheal Tablet, film coated 2 mg/1 Oral Publix Supermarkets, Inc. 2003-03-19 Not applicable US Anti Diarrheal Tablet 2 mg/1 Oral Sam's West, Inc 2005-05-03 2018-07-02 US Anti Diarrheal Capsule 2 mg/1 Oral Nash Finch 2005-05-03 2018-04-02 US Anti Diarrheal Tablet, film coated 2 mg/1 Oral Meijer Distribution 2003-03-05 Not applicable US Anti Diarrheal Tablet 2 mg/1 Oral Army + Air Force Exchange Service 2005-05-03 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Doc in the Box All Day Supply Loperamide hydrochloride + Acetaminophen + Calcium Carbonate + Dextromethorphan hydrobromide + Guaifenesin + Ibuprofen + Phenylephrine hydrochloride Kit Oral Doc In The Box Llc 2018-05-14 Not applicable US Imodium Complete Caplets Loperamide hydrochloride (2 mg) + Simethicone (125 mg) Tablet Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc 2002-06-20 Not applicable Canada Imodium Complete Chewable Tablets Loperamide hydrochloride (2 mg) + Simethicone (125 mg) Tablet, chewable Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc 1998-05-12 Not applicable Canada IMODIUM Multi-Symptom Relief Loperamide hydrochloride (2 mg/1) + Dimethicone (125 mg/1) Tablet Oral Johnson & Johnson Consumer Inc., Mc Neil Consumer Healthcare Division 2008-07-01 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Gadavyt Loperamide HCl Loperamide hydrochloride (1 mg/5mL) Liquid Oral Gadal Laboratories, Inc. 2013-05-01 Not applicable US - 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
- Alimentary Tract and Metabolism
- Antiarrhythmic agents
- Antidiarrheals
- Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
- Antipropulsives
- Calcium Channel Blockers
- Calcium Channel Blockers, Dihydropyridine and Nondihydropyridine
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Gastrointestinal Agents
- Opioid Agonist
- P-glycoprotein/ABCB1 Inhibitors
- P-glycoprotein/ABCB1 Substrates
- Piperidines
- 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.
Target Actions Organism AMu-type opioid receptor agonistHuman ADelta-type opioid receptor agonistHuman AKappa-type opioid receptor agonistHuman UVoltage-dependent P/Q-type calcium channel subunit alpha-1A inhibitorHuman UPro-opiomelanocortin modulatorHuman UCalmodulin inhibitorHuman UNuclear receptor subfamily 1 group I member 3 Not Available Human - Absorption
Not significantly absorbed from the gut
- Volume of distribution
- Not Available
- Protein binding
97%
- Metabolism
Hepatic
- Route of elimination
Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.
- Half life
9.1 to 14.4 hours (average 10.8 hours)
- Clearance
- Not Available
- Toxicity
Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group Abafungin The therapeutic efficacy of Abafungin can be increased when used in combination with Loperamide. Investigational Abemaciclib The serum concentration of Loperamide can be increased when it is combined with Abemaciclib. Approved, Investigational Acebutolol The serum concentration of Acebutolol can be increased when it is combined with Loperamide. Approved, Investigational Acepromazine The risk or severity of hypotension can be increased when Acepromazine is combined with Loperamide. Approved, Vet Approved Acetaminophen The serum concentration of Loperamide can be increased when it is combined with Acetaminophen. Approved Acetylsalicylic acid The serum concentration of Acetylsalicylic acid can be increased when it is combined with Loperamide. Approved, Vet Approved Afatinib The serum concentration of Afatinib can be increased when it is combined with Loperamide. Approved Albaconazole The therapeutic efficacy of Albaconazole can be increased when used in combination with Loperamide. Investigational Albendazole The serum concentration of Loperamide can be increased when it is combined with Albendazole. Approved, Vet Approved Alcuronium Loperamide may increase the neuromuscular blocking activities of Alcuronium. Experimental Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Loperamide. Experimental, Investigational Alectinib The serum concentration of Loperamide can be increased when it is combined with Alectinib. Approved, Investigational Alfuzosin The risk or severity of hypotension can be increased when Alfuzosin is combined with Loperamide. Approved, Investigational Alitretinoin The serum concentration of Alitretinoin can be increased when it is combined with Loperamide. Approved, Investigational Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Loperamide. Approved, Investigational Amiodarone The serum concentration of Loperamide can be increased when it is combined with Amiodarone. Approved, Investigational Amitriptyline The risk or severity of hypotension can be increased when Amitriptyline is combined with Loperamide. Approved Amlodipine The serum concentration of Loperamide can be increased when it is combined with Amlodipine. Approved Amobarbital The metabolism of Loperamide can be increased when combined with Amobarbital. Approved, Illicit Amodiaquine The serum concentration of Loperamide can be increased when it is combined with Amodiaquine. Approved, Investigational Amoxapine The risk or severity of hypotension can be increased when Amoxapine is combined with Loperamide. Approved Amphotericin B Loperamide may decrease the nephrotoxic activities of Amphotericin B. Approved, Investigational Amprenavir The serum concentration of Amprenavir can be increased when it is combined with Loperamide. Approved, Investigational Amsacrine The serum concentration of Loperamide can be increased when it is combined with Amsacrine. Approved, Investigational Annamycin The serum concentration of Loperamide can be increased when it is combined with Annamycin. Investigational Apalutamide The serum concentration of Loperamide can be decreased when it is combined with Apalutamide. Approved, Investigational Apixaban The serum concentration of Apixaban can be increased when it is combined with Loperamide. Approved Aprepitant The serum concentration of Loperamide can be increased when it is combined with Aprepitant. Approved, Investigational Aripiprazole The risk or severity of hypotension can be increased when Aripiprazole is combined with Loperamide. Approved, Investigational Aripiprazole lauroxil The risk or severity of hypotension can be increased when Aripiprazole lauroxil is combined with Loperamide. Approved, Investigational Arotinolol The risk or severity of hypotension can be increased when Arotinolol is combined with Loperamide. Investigational Arsenic trioxide The serum concentration of Arsenic trioxide can be increased when it is combined with Loperamide. Approved, Investigational Ascorbic acid The serum concentration of Ascorbic acid can be increased when it is combined with Loperamide. Approved, Nutraceutical Asenapine The risk or severity of hypotension can be increased when Asenapine is combined with Loperamide. Approved Astemizole The serum concentration of Loperamide can be increased when it is combined with Astemizole. Approved, Withdrawn Asunaprevir The serum concentration of Asunaprevir can be increased when it is combined with Loperamide. Approved, Investigational, Withdrawn Atazanavir The metabolism of Loperamide can be decreased when combined with Atazanavir. Approved, Investigational Atorvastatin The serum concentration of Loperamide can be increased when it is combined with Atorvastatin. Approved Atracurium Loperamide may increase the neuromuscular blocking activities of Atracurium. Approved, Experimental, Investigational Atracurium besylate Loperamide may increase the neuromuscular blocking activities of Atracurium besylate. Approved Avatrombopag The serum concentration of Avatrombopag can be increased when it is combined with Loperamide. Approved, Investigational Axitinib The serum concentration of Axitinib can be increased when it is combined with Loperamide. Approved, Investigational Azelastine The serum concentration of Loperamide can be increased when it is combined with Azelastine. Approved Azithromycin The serum concentration of Loperamide can be increased when it is combined with Azithromycin. Approved Bafilomycin A1 The serum concentration of Loperamide can be increased when it is combined with Bafilomycin A1. Experimental Bafilomycin B1 The serum concentration of Loperamide can be increased when it is combined with Bafilomycin B1. Experimental Barbexaclone The metabolism of Loperamide can be increased when combined with Barbexaclone. Experimental Barbital The metabolism of Loperamide can be increased when combined with Barbital. Illicit Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Loperamide. Approved, Investigational Belinostat The serum concentration of Belinostat can be increased when it is combined with Loperamide. Approved, Investigational Benzquinamide The serum concentration of Loperamide can be increased when it is combined with Benzquinamide. Withdrawn Benzyl alcohol The serum concentration of Loperamide can be increased when it is combined with Benzyl alcohol. Approved Bepridil The serum concentration of Loperamide can be increased when it is combined with Bepridil. Approved, Withdrawn Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Loperamide. Approved, Vet Approved Bevantolol The risk or severity of hypotension can be increased when Bevantolol is combined with Loperamide. Approved Bicalutamide The serum concentration of Loperamide can be increased when it is combined with Bicalutamide. Approved Bifonazole The therapeutic efficacy of Bifonazole can be increased when used in combination with Loperamide. Approved, Investigational Biricodar dicitrate The serum concentration of Loperamide can be increased when it is combined with Biricodar dicitrate. Investigational Bisacodyl The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Loperamide. Approved Bisoxatin The therapeutic efficacy of Bisoxatin can be decreased when used in combination with Loperamide. Approved Boceprevir The metabolism of Loperamide can be decreased when combined with Boceprevir. Approved, Withdrawn Bosentan The serum concentration of Loperamide can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Loperamide. Approved Brefeldin A The serum concentration of Loperamide can be increased when it is combined with Brefeldin A. Experimental Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Loperamide. Approved, Investigational Brexpiprazole The risk or severity of hypotension can be increased when Brexpiprazole is combined with Loperamide. Approved, Investigational Bromocriptine The risk or severity of hypotension can be increased when Bromocriptine is combined with Loperamide. Approved, Investigational Bromperidol The serum concentration of Bromperidol can be increased when it is combined with Loperamide. Approved, Investigational Bucindolol The risk or severity of hypotension can be increased when Bucindolol is combined with Loperamide. Investigational Bunazosin The risk or severity of hypotension can be increased when Bunazosin is combined with Loperamide. Investigational Buprenorphine The serum concentration of Loperamide can be increased when it is combined with Buprenorphine. Approved, Illicit, Investigational, Vet Approved Buspirone The serum concentration of Loperamide can be increased when it is combined with Buspirone. Approved, Investigational Butoconazole The therapeutic efficacy of Butoconazole can be increased when used in combination with Loperamide. Approved Cabazitaxel The serum concentration of Loperamide can be increased when it is combined with Cabazitaxel. Approved Caffeine The serum concentration of Loperamide can be increased when it is combined with Caffeine. Approved Calcium Acetate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Acetate. Approved, Investigational Calcium Carbonate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Carbonate. Approved, Investigational Calcium Chloride The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Chloride. Approved Calcium Citrate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Citrate. Approved Calcium glubionate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium glubionate. Approved Calcium Gluceptate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Gluceptate. Approved Calcium gluconate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium gluconate. Approved, Vet Approved Calcium lactate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium lactate. Approved, Investigational, Vet Approved Calcium lactate gluconate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium lactate gluconate. Experimental Calcium levulinate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium levulinate. Approved, Experimental Calcium pangamate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium pangamate. Experimental Calcium Phosphate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Phosphate. Approved Camptothecin The serum concentration of Camptothecin can be increased when it is combined with Loperamide. Experimental Canagliflozin The serum concentration of Loperamide can be increased when it is combined with Canagliflozin. Approved Captopril The serum concentration of Loperamide can be increased when it is combined with Captopril. Approved Carbamazepine The metabolism of Loperamide can be increased when combined with Carbamazepine. Approved, Investigational Carboxymethylcellulose The therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Loperamide. Approved, Investigational Carfilzomib The serum concentration of Carfilzomib can be increased when it is combined with Loperamide. Approved, Investigational Carvedilol The risk or severity of hypotension can be increased when Carvedilol is combined with Loperamide. Approved, Investigational Castor oil The therapeutic efficacy of Castor oil can be decreased when used in combination with Loperamide. Approved, Investigational, Nutraceutical, Vet Approved Cefoperazone The serum concentration of Loperamide can be increased when it is combined with Cefoperazone. Approved, Investigational Ceftriaxone The serum concentration of Loperamide can be increased when it is combined with Ceftriaxone. Approved Celiprolol The serum concentration of Celiprolol can be increased when it is combined with Loperamide. Approved, Investigational Ceritinib The serum concentration of Loperamide can be increased when it is combined with Ceritinib. Approved Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Loperamide. Approved, Withdrawn Cerliponase alfa The serum concentration of Cerliponase alfa can be increased when it is combined with Loperamide. Approved, Investigational Chlorambucil The serum concentration of Chlorambucil can be increased when it is combined with Loperamide. Approved Chloroform The serum concentration of Loperamide can be increased when it is combined with Chloroform. Vet Approved Chloroquine The serum concentration of Chloroquine can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Chlorpromazine The risk or severity of hypotension can be increased when Chlorpromazine is combined with Loperamide. Approved, Investigational, Vet Approved Chlorprothixene The serum concentration of Loperamide can be increased when it is combined with Chlorprothixene. Approved, Investigational, Withdrawn Cimetidine The serum concentration of Loperamide can be increased when it is combined with Cimetidine. Approved, Investigational Ciprofloxacin The serum concentration of Ciprofloxacin can be increased when it is combined with Loperamide. Approved, Investigational Cisatracurium Loperamide may increase the neuromuscular blocking activities of Cisatracurium. Approved Cisplatin The serum concentration of Cisplatin can be increased when it is combined with Loperamide. Approved Citalopram The serum concentration of Citalopram can be increased when it is combined with Loperamide. Approved Clarithromycin The metabolism of Loperamide can be decreased when combined with Clarithromycin. Approved Clobazam The serum concentration of Clobazam can be increased when it is combined with Loperamide. Approved, Illicit Clofazimine The serum concentration of Loperamide can be increased when it is combined with Clofazimine. Approved, Investigational Clomipramine The serum concentration of Loperamide can be increased when it is combined with Clomipramine. Approved, Investigational, Vet Approved Clonidine The serum concentration of Clonidine can be increased when it is combined with Loperamide. Approved Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Loperamide. Approved Clotrimazole The metabolism of Loperamide can be decreased when combined with Clotrimazole. Approved, Vet Approved Clozapine The risk or severity of hypotension can be increased when Clozapine is combined with Loperamide. Approved Cobicistat The metabolism of Loperamide can be decreased when combined with Cobicistat. Approved Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Loperamide. Approved, Investigational Colchicine The serum concentration of Colchicine can be increased when it is combined with Loperamide. Approved Concanamycin A The serum concentration of Loperamide can be increased when it is combined with Concanamycin A. Experimental Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Loperamide. Approved, Investigational Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Loperamide. Approved Copanlisib The serum concentration of Copanlisib can be increased when it is combined with Loperamide. Approved, Investigational Crizotinib The serum concentration of Loperamide can be increased when it is combined with Crizotinib. Approved Curcumin The metabolism of Loperamide can be decreased when combined with Curcumin. Approved, Investigational Cyclosporine The serum concentration of Loperamide can be increased when it is combined with Cyclosporine. Approved, Investigational, Vet Approved Cytarabine The serum concentration of Cytarabine can be increased when it is combined with Loperamide. Approved, Investigational Dabigatran etexilate The serum concentration of Dabigatran etexilate can be increased when it is combined with Loperamide. Approved Dabrafenib The serum concentration of Loperamide can be decreased when it is combined with Dabrafenib. Approved, Investigational Daclatasvir The serum concentration of Loperamide can be increased when it is combined with Daclatasvir. Approved, Investigational Dactinomycin The serum concentration of Loperamide can be increased when it is combined with Dactinomycin. Approved, Investigational Danazol The metabolism of Loperamide can be decreased when combined with Danazol. Approved Danthron The therapeutic efficacy of Danthron can be decreased when used in combination with Loperamide. Approved, Investigational, Withdrawn Dapagliflozin The serum concentration of Dapagliflozin can be increased when it is combined with Loperamide. Approved Dapiprazole The risk or severity of hypotension can be increased when Dapiprazole is combined with Loperamide. Approved Darunavir The metabolism of Loperamide can be decreased when combined with Darunavir. Approved Dasabuvir The serum concentration of Dasabuvir can be increased when it is combined with Loperamide. Approved Daunorubicin The serum concentration of Loperamide can be increased when it is combined with Daunorubicin. Approved Debrisoquin The serum concentration of Debrisoquin can be increased when it is combined with Loperamide. Approved, Investigational Deferasirox The serum concentration of Loperamide can be decreased when it is combined with Deferasirox. Approved, Investigational Delavirdine The metabolism of Loperamide can be decreased when combined with Delavirdine. Approved Desipramine The serum concentration of Loperamide can be increased when it is combined with Desipramine. Approved, Investigational Desmethylsertraline The serum concentration of Loperamide can be increased when it is combined with Desmethylsertraline. Experimental Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Dexniguldipine The serum concentration of Loperamide can be increased when it is combined with Dexniguldipine. Experimental Dexverapamil The serum concentration of Loperamide can be increased when it is combined with Dexverapamil. Experimental Diazepam The serum concentration of Diazepam can be increased when it is combined with Loperamide. Approved, Illicit, Investigational, Vet Approved Diethyl ether The serum concentration of Loperamide can be increased when it is combined with Diethyl ether. Experimental Diethylstilbestrol The serum concentration of Diethylstilbestrol can be increased when it is combined with Loperamide. Approved, Investigational Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Loperamide. Approved, Investigational Digoxin The serum concentration of Digoxin can be increased when it is combined with Loperamide. Approved Dihydroergotamine The risk or severity of hypotension can be increased when Dihydroergotamine is combined with Loperamide. Approved, Investigational Diltiazem The metabolism of Loperamide can be decreased when combined with Diltiazem. Approved, Investigational Dipyridamole The serum concentration of Loperamide can be increased when it is combined with Dipyridamole. Approved Docetaxel The serum concentration of Docetaxel can be increased when it is combined with Loperamide. Approved, Investigational Docusate The therapeutic efficacy of Docusate can be decreased when used in combination with Loperamide. Approved Dofequidar The serum concentration of Loperamide can be increased when it is combined with Dofequidar. Experimental, Investigational Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Loperamide. Approved Domperidone The serum concentration of Domperidone can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Dovitinib The serum concentration of Loperamide can be increased when it is combined with Dovitinib. Investigational Doxacurium Loperamide may increase the neuromuscular blocking activities of Doxacurium. Approved Doxazosin The risk or severity of hypotension can be increased when Doxazosin is combined with Loperamide. Approved Doxepin The risk or severity of hypotension can be increased when Doxepin is combined with Loperamide. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Loperamide. Approved, Investigational Doxycycline The metabolism of Loperamide can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronabinol The serum concentration of Loperamide can be increased when it is combined with Dronabinol. Approved, Illicit Dronedarone The risk or severity of hypotension can be increased when Dronedarone is combined with Loperamide. Approved Droperidol The risk or severity of hypotension can be increased when Droperidol is combined with Loperamide. Approved, Vet Approved Duloxetine The serum concentration of Loperamide can be increased when it is combined with Duloxetine. Approved Econazole The serum concentration of Loperamide can be increased when it is combined with Econazole. Approved Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Loperamide. Approved Efavirenz The serum concentration of Loperamide can be decreased when it is combined with Efavirenz. Approved, Investigational Efinaconazole The therapeutic efficacy of Efinaconazole can be increased when used in combination with Loperamide. Approved Elacridar The serum concentration of Loperamide can be increased when it is combined with Elacridar. Investigational Elagolix The serum concentration of Elagolix can be increased when it is combined with Loperamide. Approved, Investigational Elbasvir The serum concentration of Elbasvir can be increased when it is combined with Loperamide. Approved Eletriptan The serum concentration of Eletriptan can be increased when it is combined with Loperamide. Approved, Investigational Emopamil The serum concentration of Loperamide can be increased when it is combined with Emopamil. Experimental Enasidenib The serum concentration of Loperamide can be increased when it is combined with Enasidenib. Approved, Investigational Enzalutamide The serum concentration of Loperamide can be decreased when it is combined with Enzalutamide. Approved Epinastine The serum concentration of Epinastine can be increased when it is combined with Loperamide. Approved, Investigational Ergonovine The serum concentration of Loperamide can be increased when it is combined with Ergonovine. Approved Ergotamine The risk or severity of hypotension can be increased when Ergotamine is combined with Loperamide. Approved Erlotinib The serum concentration of Loperamide can be increased when it is combined with Erlotinib. Approved, Investigational Ertugliflozin The serum concentration of Ertugliflozin can be increased when it is combined with Loperamide. Approved, Investigational Erythromycin The serum concentration of Loperamide can be increased when it is combined with Erythromycin. Approved, Investigational, Vet Approved Esomeprazole The serum concentration of Loperamide can be increased when it is combined with Esomeprazole. Approved, Investigational Estradiol The serum concentration of Estradiol can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estradiol acetate The serum concentration of Estradiol acetate can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estradiol benzoate The serum concentration of Estradiol benzoate can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estradiol cypionate The serum concentration of Estradiol cypionate can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estradiol dienanthate The serum concentration of Estradiol dienanthate can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estradiol valerate The serum concentration of Estradiol valerate can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estramustine The serum concentration of Loperamide can be increased when it is combined with Estramustine. Approved, Investigational Estriol The serum concentration of Estriol can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Estrone The serum concentration of Estrone can be increased when it is combined with Loperamide. Approved Ethinyl Estradiol The serum concentration of Ethinyl Estradiol can be increased when it is combined with Loperamide. Approved Etoposide The serum concentration of Loperamide can be increased when it is combined with Etoposide. Approved Etravirine The serum concentration of Loperamide can be decreased when it is combined with Etravirine. Approved Everolimus The serum concentration of Everolimus can be increased when it is combined with Loperamide. Approved Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Loperamide. Approved Felodipine The serum concentration of Loperamide can be increased when it is combined with Felodipine. Approved, Investigational Fenofibrate The serum concentration of Loperamide can be increased when it is combined with Fenofibrate. Approved Fentanyl The serum concentration of Loperamide can be increased when it is combined with Fentanyl. Approved, Illicit, Investigational, Vet Approved Fenticonazole The therapeutic efficacy of Fenticonazole can be increased when used in combination with Loperamide. Experimental Fesoterodine The serum concentration of Fesoterodine can be increased when it is combined with Loperamide. Approved Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Loperamide. Approved, Investigational Fidaxomicin The 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 Fluconazole The serum concentration of Loperamide can be increased when it is combined with Fluconazole. Approved, Investigational Fluoxetine The serum concentration of Loperamide can be increased when it is combined with Fluoxetine. Approved, Vet Approved Flupentixol The risk or severity of hypotension can be increased when Flupentixol is combined with Loperamide. Approved, Investigational, Withdrawn Fluphenazine The serum concentration of Loperamide can be increased when it is combined with Fluphenazine. Approved Flurazepam The serum concentration of Loperamide can be increased when it is combined with Flurazepam. Approved, Illicit, Investigational Fluticasone The serum concentration of Fluticasone can be increased when it is combined with Loperamide. Approved, Experimental, Investigational Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Loperamide. Approved Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Loperamide. Approved Flutrimazole The therapeutic efficacy of Flutrimazole can be increased when used in combination with Loperamide. Experimental Fluvoxamine The serum concentration of Loperamide can be increased when it is combined with Fluvoxamine. Approved, Investigational Fosamprenavir The metabolism of Loperamide can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Loperamide can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Loperamide. Approved, Investigational Fusidic Acid The serum concentration of Loperamide can be increased when it is combined with Fusidic Acid. Approved, Investigational Gallamine Loperamide may increase the neuromuscular blocking activities of Gallamine. Experimental Gallamine Triethiodide Loperamide may increase the neuromuscular blocking activities of Gallamine Triethiodide. Approved Gallopamil The serum concentration of Loperamide can be increased when it is combined with Gallopamil. Investigational Gefitinib The serum concentration of Loperamide can be increased when it is combined with Gefitinib. Approved, Investigational Genistein The serum concentration of Loperamide can be increased when it is combined with Genistein. Investigational Glecaprevir The serum concentration of Loperamide can be increased when it is combined with Glecaprevir. Approved, Investigational Glyburide The serum concentration of Loperamide can be increased when it is combined with Glyburide. Approved Glycerin The serum concentration of Loperamide can be increased when it is combined with Glycerin. Approved, Investigational Gramicidin D The serum concentration of Loperamide can be increased when it is combined with Gramicidin D. Approved Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Loperamide. Approved Grepafloxacin The serum concentration of Grepafloxacin can be increased when it is combined with Loperamide. Approved, Investigational, Withdrawn Hexobarbital The metabolism of Loperamide can be increased when combined with Hexobarbital. Approved HM-30181 The serum concentration of Loperamide can be increased when it is combined with HM-30181. Experimental Hycanthone The serum concentration of Loperamide can be increased when it is combined with Hycanthone. Approved, Investigational Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Loperamide. Approved, Vet Approved Hydroxychloroquine The serum concentration of Loperamide can be increased when it is combined with Hydroxychloroquine. Approved Hydroxyurea The serum concentration of Hydroxyurea can be increased when it is combined with Loperamide. Approved Ibuprofen The serum concentration of Loperamide can be increased when it is combined with Ibuprofen. Approved Idelalisib The metabolism of Loperamide can be decreased when combined with Idelalisib. Approved Iloperidone The risk or severity of hypotension can be increased when Iloperidone is combined with Loperamide. Approved Imatinib The serum concentration of Loperamide can be increased when it is combined with Imatinib. Approved Imipramine The risk or severity of hypotension can be increased when Imipramine is combined with Loperamide. Approved Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Loperamide. Approved Indinavir The metabolism of Loperamide can be decreased when combined with Indinavir. Approved Indomethacin The serum concentration of Loperamide can be increased when it is combined with Indomethacin. Approved, Investigational Indoramin The risk or severity of hypotension can be increased when Indoramin is combined with Loperamide. Withdrawn Inotuzumab ozogamicin The serum concentration of Inotuzumab ozogamicin can be increased when it is combined with Loperamide. Approved, Investigational Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Loperamide. Approved, Investigational Isavuconazole The serum concentration of Loperamide can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The serum concentration of Loperamide can be increased when it is combined with Isavuconazonium. Approved, Investigational Isoconazole The therapeutic efficacy of Isoconazole can be increased when used in combination with Loperamide. Approved Isoniazid The metabolism of Loperamide can be decreased when combined with Isoniazid. Approved, Investigational Isradipine The serum concentration of Loperamide can be increased when it is combined with Isradipine. Approved, Investigational Itraconazole The metabolism of Loperamide can be decreased when combined with Itraconazole. Approved, Investigational Ivermectin The serum concentration of Loperamide can be increased when it is combined with Ivermectin. Approved, Investigational, Vet Approved Ivosidenib The serum concentration of Ivosidenib can be increased when it is combined with Loperamide. Approved, Investigational Ketazolam The serum concentration of Ketazolam can be increased when it is combined with Loperamide. Approved Ketoconazole The metabolism of Loperamide can be decreased when combined with Ketoconazole. Approved, Investigational Labetalol The risk or severity of hypotension can be increased when Labetalol is combined with Loperamide. Approved Lactitol The therapeutic efficacy of Lactitol can be decreased when used in combination with Loperamide. Investigational Lactulose The therapeutic efficacy of Lactulose can be decreased when used in combination with Loperamide. Approved Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Loperamide. Approved, Investigational Lamotrigine The serum concentration of Lamotrigine can be increased when it is combined with Loperamide. Approved, Investigational Laniquidar The serum concentration of Loperamide can be increased when it is combined with Laniquidar. Investigational Lansoprazole The serum concentration of Loperamide can be increased when it is combined with Lansoprazole. Approved, Investigational Lapatinib The serum concentration of Loperamide can be increased when it is combined with Lapatinib. Approved, Investigational Lenalidomide The serum concentration of Lenalidomide can be increased when it is combined with Loperamide. Approved Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Loperamide. Approved, Investigational Letermovir The serum concentration of Loperamide can be increased when it is combined with Letermovir. Approved, Investigational Levetiracetam The serum concentration of Levetiracetam can be increased when it is combined with Loperamide. Approved, Investigational Levofloxacin The serum concentration of Loperamide can be increased when it is combined with Levofloxacin. Approved, Investigational Levomilnacipran The serum concentration of Levomilnacipran can be increased when it is combined with Loperamide. Approved, Investigational Lidocaine The serum concentration of Loperamide can be increased when it is combined with Lidocaine. Approved, Vet Approved Linaclotide The therapeutic efficacy of Linaclotide can be decreased when used in combination with Loperamide. Approved Linagliptin The serum concentration of Loperamide can be increased when it is combined with Linagliptin. Approved Lomerizine The serum concentration of Loperamide can be increased when it is combined with Lomerizine. Experimental Lomitapide The serum concentration of Loperamide can be increased when it is combined with Lomitapide. Approved, Investigational Lonafarnib The serum concentration of Loperamide can be increased when it is combined with Lonafarnib. Investigational Lopinavir The metabolism of Loperamide can be decreased when combined with Lopinavir. Approved Loratadine The serum concentration of Loperamide can be increased when it is combined with Loratadine. Approved, Investigational Lorpiprazole The serum concentration of Loperamide can be increased when it is combined with Lorpiprazole. Approved Losartan The serum concentration of Loperamide can be increased when it is combined with Losartan. Approved Lovastatin The serum concentration of Loperamide can be increased when it is combined with Lovastatin. Approved, Investigational Loxapine The serum concentration of Loperamide can be increased when it is combined with Loxapine. Approved Lubiprostone The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Loperamide. Approved, Investigational Luliconazole The serum concentration of Loperamide can be increased when it is combined with Luliconazole. Approved Lumacaftor The serum concentration of Loperamide can be decreased when it is combined with Lumacaftor. Approved Lusutrombopag The serum concentration of Lusutrombopag can be increased when it is combined with Loperamide. Approved, Investigational Magnesium carbonate The therapeutic efficacy of Magnesium carbonate can be decreased when used in combination with Loperamide. Approved, Investigational Magnesium citrate The therapeutic efficacy of Magnesium citrate can be decreased when used in combination with Loperamide. Approved Magnesium hydroxide The risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium hydroxide. Approved, Investigational Magnesium oxide The risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium oxide. Approved Magnesium peroxide The therapeutic efficacy of Magnesium peroxide can be decreased when used in combination with Loperamide. Experimental Magnesium salicylate The risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium salicylate. Approved Magnesium sulfate The risk or severity of hypotension and neuromuscular blockade can be increased when Loperamide is combined with Magnesium sulfate. Approved, Investigational, Vet Approved Mannitol The therapeutic efficacy of Mannitol can be decreased when used in combination with Loperamide. Approved, Investigational Mefloquine The serum concentration of Loperamide can be increased when it is combined with Mefloquine. Approved, Investigational Megestrol acetate The serum concentration of Loperamide can be increased when it is combined with Megestrol acetate. Approved, Investigational, Vet Approved Melphalan The serum concentration of Melphalan can be increased when it is combined with Loperamide. Approved Methadone The serum concentration of Loperamide can be increased when it is combined with Methadone. Approved Methohexital The metabolism of Loperamide can be increased when combined with Methohexital. Approved Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Loperamide. Approved Methotrimeprazine The risk or severity of hypotension can be increased when Methotrimeprazine is combined with Loperamide. Approved, Investigational Methyl cellulose The therapeutic efficacy of Methyl cellulose can be decreased when used in combination with Loperamide. Approved Methylphenobarbital The metabolism of Loperamide can be increased when combined with Methylphenobarbital. Approved Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Loperamide. Approved, Vet Approved Metocurine Loperamide may increase the neuromuscular blocking activities of Metocurine. Approved Metocurine Iodide Loperamide may increase the neuromuscular blocking activities of Metocurine Iodide. Approved, Withdrawn Metronidazole The serum concentration of Loperamide can be increased when it is combined with Metronidazole. Approved Mibefradil The metabolism of Loperamide can be decreased when combined with Mibefradil. Investigational, Withdrawn Miconazole The serum concentration of Loperamide can be increased when it is combined with Miconazole. Approved, Investigational, Vet Approved Midazolam The serum concentration of Loperamide can be increased when it is combined with Midazolam. Approved, Illicit Mifepristone The serum concentration of Loperamide can be increased when it is combined with Mifepristone. Approved, Investigational Mineral oil The therapeutic efficacy of Mineral oil can be decreased when used in combination with Loperamide. Approved, Vet Approved Mirabegron The serum concentration of Mirabegron can be increased when it is combined with Loperamide. Approved Mitomycin The serum concentration of Mitomycin can be increased when it is combined with Loperamide. Approved Mitotane The serum concentration of Loperamide can be decreased when it is combined with Mitotane. Approved Mitoxantrone The serum concentration of Loperamide can be increased when it is combined with Mitoxantrone. Approved, Investigational Mivacurium Loperamide may increase the neuromuscular blocking activities of Mivacurium. Approved Modafinil The serum concentration of Loperamide can be decreased when it is combined with Modafinil. Approved, Investigational Monensin The serum concentration of Loperamide can be increased when it is combined with Monensin. Vet Approved Morphine The serum concentration of Morphine can be increased when it is combined with Loperamide. Approved, Investigational Moxidectin The serum concentration of Moxidectin can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Loperamide. Approved, Investigational Nadolol The serum concentration of Nadolol can be increased when it is combined with Loperamide. Approved Nafcillin The therapeutic efficacy of Loperamide can be decreased when used in combination with Nafcillin. Approved, Investigational Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Loperamide. Approved Naloxone The metabolism of Loperamide can be decreased when combined with Naloxone. Approved, Vet Approved Nefazodone The risk or severity of hypotension can be increased when Nefazodone is combined with Loperamide. Approved, Withdrawn Nelfinavir The metabolism of Loperamide can be decreased when combined with Nelfinavir. Approved Neostigmine The serum concentration of Neostigmine can be increased when it is combined with Loperamide. Approved, Vet Approved Neratinib The serum concentration of Loperamide can be increased when it is combined with Neratinib. Approved, Investigational Netupitant The serum concentration of Loperamide can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The metabolism of Loperamide can be increased when combined with Nevirapine. Approved Nicardipine The risk or severity of hypotension can be increased when Nicardipine is combined with Loperamide. Approved, Investigational Nicergoline The risk or severity of hypotension can be increased when Nicergoline is combined with Loperamide. Approved, Investigational Nifedipine The serum concentration of Nifedipine can be increased when it is combined with Loperamide. Approved Nigericin The serum concentration of Loperamide can be increased when it is combined with Nigericin. Experimental Niguldipine The risk or severity of hypotension can be increased when Niguldipine is combined with Loperamide. Experimental Nilotinib The metabolism of Loperamide can be decreased when combined with Nilotinib. Approved, Investigational Nimodipine The serum concentration of Loperamide can be increased when it is combined with Nimodipine. Approved, Investigational Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Loperamide. Approved Nisoldipine The serum concentration of Loperamide can be increased when it is combined with Nisoldipine. Approved Nitrendipine The serum concentration of Loperamide can be increased when it is combined with Nitrendipine. Approved, Investigational Nitroprusside Loperamide may increase the hypotensive activities of Nitroprusside. Approved, Investigational Nizatidine The serum concentration of Nizatidine can be increased when it is combined with Loperamide. Approved Nortriptyline The risk or severity of hypotension can be increased when Nortriptyline is combined with Loperamide. Approved Octreotide The serum concentration of Octreotide can be increased when it is combined with Loperamide. Approved, Investigational Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Loperamide. Investigational Olanzapine The risk or severity of hypotension can be increased when Olanzapine is combined with Loperamide. Approved, Investigational Olaparib The metabolism of Loperamide can be decreased when combined with Olaparib. Approved Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Loperamide. Approved, Investigational Omeprazole The serum concentration of Loperamide can be increased when it is combined with Omeprazole. Approved, Investigational, Vet Approved Omoconazole The therapeutic efficacy of Omoconazole can be increased when used in combination with Loperamide. Experimental Ondansetron The serum concentration of Ondansetron can be increased when it is combined with Loperamide. Approved ONT-093 The serum concentration of Loperamide can be increased when it is combined with ONT-093. Investigational Oxiconazole The therapeutic efficacy of Oxiconazole can be increased when used in combination with Loperamide. Approved Oxyphenisatin The therapeutic efficacy of Oxyphenisatin can be decreased when used in combination with Loperamide. Investigational, Withdrawn Paclitaxel The serum concentration of Loperamide can be increased when it is combined with Paclitaxel. Approved, Vet Approved Palbociclib The serum concentration of Loperamide can be increased when it is combined with Palbociclib. Approved, Investigational Paliperidone The risk or severity of hypotension can be increased when Paliperidone is combined with Loperamide. Approved Pancuronium Loperamide may increase the neuromuscular blocking activities of Pancuronium. Approved Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Loperamide. Approved, Investigational Pantoprazole The serum concentration of Loperamide can be increased when it is combined with Pantoprazole. Approved Paritaprevir The serum concentration of Loperamide can be increased when it is combined with Paritaprevir. Approved, Investigational Paroxetine The serum concentration of Loperamide can be increased when it is combined with Paroxetine. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Loperamide. Approved Pentaerithrityl The therapeutic efficacy of Pentaerithrityl can be decreased when used in combination with Loperamide. Experimental Pentazocine The serum concentration of Loperamide can be increased when it is combined with Pentazocine. Approved, Vet Approved Pentobarbital The metabolism of Loperamide can be increased when combined with Pentobarbital. Approved, Investigational, Vet Approved Pethidine The serum concentration of Loperamide can be increased when it is combined with Pethidine. Approved Phenobarbital The metabolism of Loperamide can be increased when combined with Phenobarbital. Approved, Investigational Phenolphthalein The therapeutic efficacy of Phenolphthalein can be decreased when used in combination with Loperamide. Approved, Withdrawn Phenothiazine The serum concentration of Phenothiazine can be increased when it is combined with Loperamide. Vet Approved Phenoxybenzamine The risk or severity of hypotension can be increased when Phenoxybenzamine is combined with Loperamide. Approved Phentolamine The risk or severity of hypotension can be increased when Phentolamine is combined with Loperamide. Approved Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Loperamide. Approved, Vet Approved Pibrentasvir The serum concentration of Loperamide can be increased when it is combined with Pibrentasvir. Approved, Investigational Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Loperamide. Approved Pimozide The serum concentration of Loperamide can be increased when it is combined with Pimozide. Approved Pipecuronium Loperamide may increase the neuromuscular blocking activities of Pipecuronium. Approved Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Loperamide. Approved Pitolisant The serum concentration of Loperamide can be decreased when it is combined with Pitolisant. Approved, Investigational Pizotifen The risk or severity of hypotension can be increased when Pizotifen is combined with Loperamide. Approved Plantago seed The therapeutic efficacy of Plantago seed can be decreased when used in combination with Loperamide. Approved, Investigational Plecanatide The therapeutic efficacy of Plecanatide can be decreased when used in combination with Loperamide. Approved, Investigational Polycarbophil The therapeutic efficacy of Polycarbophil can be decreased when used in combination with Loperamide. Approved Polyethylene glycol The therapeutic efficacy of Polyethylene glycol can be decreased when used in combination with Loperamide. Approved, Vet Approved Pomalidomide The serum concentration of Pomalidomide can be increased when it is combined with Loperamide. Approved Ponatinib The serum concentration of Loperamide can be increased when it is combined with Ponatinib. Approved, Investigational Posaconazole The metabolism of Loperamide can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Potassium acetate The therapeutic efficacy of Potassium acetate can be decreased when used in combination with Loperamide. Approved, Investigational Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Loperamide. Approved Prazosin The risk or severity of hypotension can be increased when Prazosin is combined with Loperamide. Approved Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Loperamide. Approved, Vet Approved Prednisone The serum concentration of Loperamide can be increased when it is combined with Prednisone. Approved, Vet Approved Primaquine The serum concentration of Loperamide can be increased when it is combined with Primaquine. Approved Primidone The metabolism of Loperamide can be increased when combined with Primidone. Approved, Vet Approved Progesterone The serum concentration of Loperamide can be increased when it is combined with Progesterone. Approved, Vet Approved Promazine The risk or severity of hypotension can be increased when Promazine is combined with Loperamide. Approved, Vet Approved Promethazine The serum concentration of Loperamide can be increased when it is combined with Promethazine. Approved, Investigational Propafenone The serum concentration of Loperamide can be increased when it is combined with Propafenone. Approved Propericiazine The risk or severity of hypotension can be increased when Propericiazine is combined with Loperamide. Approved, Investigational Propiomazine The risk or severity of hypotension can be increased when Propiomazine is combined with Loperamide. Approved Propiverine The risk or severity of hypotension can be increased when Propiverine is combined with Loperamide. Approved, Investigational Propofol The serum concentration of Loperamide can be increased when it is combined with Propofol. Approved, Investigational, Vet Approved Propranolol The serum concentration of Propranolol can be increased when it is combined with Loperamide. Approved, Investigational Protriptyline The serum concentration of Loperamide can be increased when it is combined with Protriptyline. Approved Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Loperamide. Approved Quercetin The serum concentration of Loperamide can be increased when it is combined with Quercetin. Experimental, Investigational Quetiapine The risk or severity of hypotension can be increased when Quetiapine is combined with Loperamide. Approved Quinacrine The serum concentration of Loperamide can be increased when it is combined with Quinacrine. Approved, Investigational Quinidine The risk or severity of hypotension can be increased when Quinidine is combined with Loperamide. Approved, Investigational Quinine The metabolism of Loperamide can be increased when combined with Quinine. Approved Ranitidine The serum concentration of Loperamide can be increased when it is combined with Ranitidine. Approved Rapacuronium Loperamide may increase the neuromuscular blocking activities of Rapacuronium. Withdrawn Ravuconazole The therapeutic efficacy of Ravuconazole can be increased when used in combination with Loperamide. Investigational Reboxetine The serum concentration of Loperamide can be increased when it is combined with Reboxetine. Approved, Investigational Regorafenib The serum concentration of Regorafenib can be increased when it is combined with Loperamide. Approved Reserpine The serum concentration of Loperamide can be increased when it is combined with Reserpine. Approved, Investigational Reversin 121 The serum concentration of Loperamide can be increased when it is combined with Reversin 121. Experimental Rhodamine 6G The serum concentration of Rhodamine 6G can be increased when it is combined with Loperamide. Experimental Rifampicin The metabolism of Loperamide can be increased when combined with Rifampicin. Approved Rifamycin The metabolism of Loperamide can be increased when combined with Rifamycin. Investigational Rifapentine The metabolism of Loperamide can be increased when combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Loperamide. Approved, Investigational Rilpivirine The serum concentration of Loperamide can be increased when it is combined with Rilpivirine. Approved Rimexolone The metabolism of Loperamide can be increased when combined with Rimexolone. Approved Risperidone The risk or severity of hypotension can be increased when Risperidone is combined with Loperamide. Approved, Investigational Ritonavir The metabolism of Loperamide can be decreased when combined with Ritonavir. Approved, Investigational Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Loperamide. Approved Rocuronium Loperamide may increase the neuromuscular blocking activities of Rocuronium. Approved Rolapitant The serum concentration of Loperamide can be increased when it is combined with Rolapitant. Approved, Investigational Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Loperamide. Approved, Investigational Rucaparib The serum concentration of Loperamide can be increased when it is combined with Rucaparib. Approved, Investigational Salinomycin The serum concentration of Loperamide can be increased when it is combined with Salinomycin. Vet Approved Saquinavir The metabolism of Loperamide can be decreased when combined with Saquinavir. Approved, Investigational Sarilumab The therapeutic efficacy of Loperamide can be decreased when used in combination with Sarilumab. Approved, Investigational Secobarbital The metabolism of Loperamide can be increased when combined with Secobarbital. Approved, Vet Approved Selexipag The serum concentration of Selexipag can be increased when it is combined with Loperamide. Approved Sennosides The therapeutic efficacy of Sennosides can be decreased when used in combination with Loperamide. Approved Sertaconazole The therapeutic efficacy of Sertaconazole can be increased when used in combination with Loperamide. Approved, Investigational Sertraline The serum concentration of Loperamide can be increased when it is combined with Sertraline. Approved Silodosin The serum concentration of Silodosin can be increased when it is combined with Loperamide. Approved Siltuximab The serum concentration of Loperamide can be decreased when it is combined with Siltuximab. Approved, Investigational Simeprevir The serum concentration of Loperamide can be increased when it is combined with Simeprevir. Approved Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Loperamide. Approved Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Loperamide. Approved, Investigational Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Loperamide. Approved, Investigational Sodium phosphate, monobasic The therapeutic efficacy of Sodium phosphate, monobasic can be decreased when used in combination with Loperamide. Approved Sodium sulfate The therapeutic efficacy of Sodium sulfate can be decreased when used in combination with Loperamide. Approved, Vet Approved Sodium tartrate The therapeutic efficacy of Sodium tartrate can be decreased when used in combination with Loperamide. Approved Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Loperamide. Approved Somatostatin The serum concentration of Somatostatin can be increased when it is combined with Loperamide. Approved, Investigational Sorafenib The serum concentration of Loperamide can be increased when it is combined with Sorafenib. Approved, Investigational Sorbitol The therapeutic efficacy of Sorbitol can be decreased when used in combination with Loperamide. Approved Sparfloxacin The serum concentration of Sparfloxacin can be increased when it is combined with Loperamide. Approved, Investigational Sphingosine The serum concentration of Sphingosine can be increased when it is combined with Loperamide. Experimental St. John's Wort The serum concentration of Loperamide can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stanolone The serum concentration of Stanolone can be increased when it is combined with Loperamide. Illicit, Investigational Stanolone acetate The serum concentration of Stanolone acetate can be increased when it is combined with Loperamide. Experimental Staurosporine The serum concentration of Loperamide can be increased when it is combined with Staurosporine. Experimental Stiripentol The serum concentration of Loperamide can be increased when it is combined with Stiripentol. Approved Sulconazole The therapeutic efficacy of Sulconazole can be increased when used in combination with Loperamide. Approved Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Loperamide. Approved, Investigational Sunitinib The serum concentration of Loperamide can be increased when it is combined with Sunitinib. Approved, Investigational Suvorexant The serum concentration of Loperamide can be increased when it is combined with Suvorexant. Approved, Investigational Tacrine The serum concentration of Tacrine can be increased when it is combined with Loperamide. Investigational, Withdrawn Tacrolimus The serum concentration of Loperamide can be increased when it is combined with Tacrolimus. Approved, Investigational Talinolol The serum concentration of Talinolol can be increased when it is combined with Loperamide. Investigational Tamoxifen The serum concentration of Loperamide can be increased when it is combined with Tamoxifen. Approved Tamsulosin The risk or severity of hypotension can be increased when Tamsulosin is combined with Loperamide. Approved, Investigational Tariquidar The serum concentration of Loperamide can be increased when it is combined with Tariquidar. Investigational Taurocholic Acid The serum concentration of Taurocholic Acid can be increased when it is combined with Loperamide. Experimental Technetium Tc-99m sestamibi The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Loperamide. Approved, Investigational Tegaserod The therapeutic efficacy of Tegaserod can be decreased when used in combination with Loperamide. Approved, Investigational, Withdrawn Telaprevir The metabolism of Loperamide can be decreased when combined with Telaprevir. Approved, Withdrawn Telithromycin The metabolism of Loperamide can be decreased when combined with Telithromycin. Approved Telmisartan The serum concentration of Loperamide can be increased when it is combined with Telmisartan. Approved, Investigational Temsirolimus The serum concentration of Loperamide can be increased when it is combined with Temsirolimus. Approved Teniposide The serum concentration of Teniposide can be increased when it is combined with Loperamide. Approved Terazosin The risk or severity of hypotension can be increased when Terazosin is combined with Loperamide. Approved Terconazole The therapeutic efficacy of Terconazole can be increased when used in combination with Loperamide. Approved Terfenadine The serum concentration of Loperamide can be increased when it is combined with Terfenadine. Approved, Withdrawn Tesmilifene The serum concentration of Loperamide can be increased when it is combined with Tesmilifene. Investigational Testosterone The serum concentration of Loperamide can be increased when it is combined with Testosterone. Approved, Investigational Testosterone cypionate The serum concentration of Loperamide can be increased when it is combined with Testosterone cypionate. Approved Testosterone enanthate The serum concentration of Loperamide can be increased when it is combined with Testosterone enanthate. Approved Testosterone propionate The serum concentration of Testosterone propionate can be increased when it is combined with Loperamide. Approved, Investigational, Vet Approved, Withdrawn Testosterone undecanoate The serum concentration of Loperamide can be increased when it is combined with Testosterone undecanoate. Approved, Investigational Tetracycline The serum concentration of Tetracycline can be increased when it is combined with Loperamide. Approved, Vet Approved Tetrandrine The serum concentration of Loperamide can be increased when it is combined with Tetrandrine. Experimental Thiamylal The metabolism of Loperamide can be increased when combined with Thiamylal. Approved, Vet Approved Thiopental The metabolism of Loperamide can be increased when combined with Thiopental. Approved, Vet Approved Thioproperazine The risk or severity of hypotension can be increased when Thioproperazine is combined with Loperamide. Approved Thioridazine The risk or severity of hypotension can be increased when Thioridazine is combined with Loperamide. Approved, Withdrawn Ticagrelor The serum concentration of Loperamide can be increased when it is combined with Ticagrelor. Approved Timolol The serum concentration of Timolol can be increased when it is combined with Loperamide. Approved Tioconazole The therapeutic efficacy of Tioconazole can be increased when used in combination with Loperamide. Approved Tipifarnib The serum concentration of Loperamide can be increased when it is combined with Tipifarnib. Investigational Tipranavir The metabolism of Loperamide can be decreased when combined with Tipranavir. Approved, Investigational Tocilizumab The serum concentration of Loperamide can be decreased when it is combined with Tocilizumab. Approved Tolazoline The risk or severity of hypotension can be increased when Tolazoline is combined with Loperamide. Approved, Vet Approved Tolvaptan The serum concentration of Loperamide can be increased when it is combined with Tolvaptan. Approved Topiramate The serum concentration of Topiramate can be increased when it is combined with Loperamide. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Loperamide. Approved, Investigational Toremifene The serum concentration of Loperamide can be increased when it is combined with Toremifene. Approved, Investigational Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Loperamide. Approved, Investigational Trazodone The risk or severity of hypotension can be increased when Trazodone is combined with Loperamide. Approved, Investigational Trifluoperazine The risk or severity of hypotension can be increased when Trifluoperazine is combined with Loperamide. Approved, Investigational Triflupromazine The serum concentration of Loperamide can be increased when it is combined with Triflupromazine. Approved, Vet Approved Trimazosin The risk or severity of hypotension can be increased when Trimazosin is combined with Loperamide. Experimental Trimethoprim The serum concentration of Loperamide can be increased when it is combined with Trimethoprim. Approved, Vet Approved Trimipramine The risk or severity of hypotension can be increased when Trimipramine is combined with Loperamide. Approved Troleandomycin The metabolism of Loperamide can be decreased when combined with Troleandomycin. Approved Tubocurarine Loperamide may increase the neuromuscular blocking activities of Tubocurarine. Approved Ubidecarenone The serum concentration of Ubidecarenone can be increased when it is combined with Loperamide. Approved, Investigational, Nutraceutical Umeclidinium The serum concentration of Umeclidinium can be increased when it is combined with Loperamide. Approved Urapidil The risk or severity of hypotension can be increased when Urapidil is combined with Loperamide. Investigational Valinomycin The serum concentration of Loperamide can be increased when it is combined with Valinomycin. Experimental Valspodar The serum concentration of Loperamide can be increased when it is combined with Valspodar. Investigational Vecuronium Loperamide may increase the neuromuscular blocking activities of Vecuronium. Approved Velpatasvir The serum concentration of Loperamide can be increased when it is combined with Velpatasvir. Approved, Investigational Vemurafenib The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Loperamide. Approved Venetoclax The serum concentration of Venetoclax can be increased when it is combined with Loperamide. Approved, Investigational Venlafaxine The serum concentration of Loperamide can be increased when it is combined with Venlafaxine. Approved Verapamil The risk or severity of hypotension can be increased when Verapamil is combined with Loperamide. Approved Vinblastine The serum concentration of Loperamide can be increased when it is combined with Vinblastine. Approved Vincristine The excretion of Vincristine can be decreased when combined with Loperamide. Approved, Investigational Vinflunine The serum concentration of Vinflunine can be increased when it is combined with Loperamide. Approved, Investigational Vinorelbine The serum concentration of Vinorelbine can be increased when it is combined with Loperamide. Approved, Investigational Vismodegib The serum concentration of Vismodegib can be increased when it is combined with Loperamide. Approved, Investigational Voacamine The serum concentration of Loperamide can be increased when it is combined with Voacamine. Approved, Investigational Vorapaxar The serum concentration of Loperamide can be increased when it is combined with Vorapaxar. Approved Voriconazole The metabolism of Loperamide can be decreased when combined with Voriconazole. Approved, Investigational Voxilaprevir The serum concentration of Loperamide can be increased when it is combined with Voxilaprevir. Approved, Investigational Yohimbine The serum concentration of Loperamide can be increased when it is combined with Yohimbine. Approved, Investigational, Vet Approved Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Loperamide. Approved Ziprasidone The risk or severity of hypotension can be increased when Ziprasidone is combined with Loperamide. Approved Zomepirac The serum concentration of Loperamide can be increased when it is combined with Zomepirac. Withdrawn Zosuquidar The serum concentration of Loperamide can be increased when it is combined with Zosuquidar. Investigational Zuclopenthixol The 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, combinations
- A07DA — Antipropulsives
- A07D — ANTIPROPULSIVES
- A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
- A — ALIMENTARY TRACT AND METABOLISM
- A07DA — Antipropulsives
- A07D — ANTIPROPULSIVES
- A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
- A — ALIMENTARY TRACT AND METABOLISM
- AHFS Codes
- 56:08.00 — Antidiarrhea Agents
- FDA label
- Download (55.5 KB)
- MSDS
- Download (73.8 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Mcneil consumer healthcare
- Mcneil pediatrics
- Janssen pharmaceutica products lp
- Packagers
- Advanced Pharmaceutical Services Inc.
- AQ Pharmaceuticals Inc.
- A-S Medication Solutions LLC
- Cardinal Health
- Chain Drug
- Chattem Chemicals Inc.
- Comprehensive Consultant Services Inc.
- CVS Pharmacy
- Dept Health Central Pharmacy
- DHHS Program Support Center Supply Service Center
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Heartland Repack Services LLC
- Janssen-Ortho Inc.
- Lake Chemicals Pvt Ltd.
- Lake Erie Medical and Surgical Supply
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- McNeil Laboratories
- Medique Products
- Medisca Inc.
- Mylan
- Novopharm Ltd.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Perrigo Co.
- Pharmacia Inc.
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Qualitest
- Redpharm Drug
- Remedy Repack
- Rugby Laboratories
- Sandhills Packaging Inc.
- Teva Pharmaceutical Industries Ltd.
- Tya Pharmaceuticals
- UDL Laboratories
- Vangard Labs Inc.
- Dosage forms
Form Route Strength Solution Oral 1 mg/5mL Capsule, liquid filled Oral 2 mg/1 Kit Oral Solution Oral .2 mg Liquid Oral 1 mg/5mL Tablet, film coated Oral 2 mg/1 Solution Oral 1 mg/7.5mL Tablet, coated Oral 2 mg/1 Solution Oral 2 mg Tablet Oral Tablet, chewable Oral Capsule Oral 2 mg Liquid Oral .2 mg Capsule Oral 2 mg/1 Liquid Oral 1 mg/7.5mL Solution Oral 2 mg/10mL Suspension Oral 1 mg/7.5mL Tablet Oral 2 mg Solution Oral 0.2 mg Tablet Oral 2 mg/1 - Prices
Unit description Cost Unit Loperamide hcl powder 26.01USD g Loperamide HCl 2 mg capsule 0.64USD capsule Imodium a-d 2 mg caplet 0.49USD caplet Imodium advanced caplet 0.46USD caplet Imodium ms relief caplet 0.46USD caplet Kaopectate 262 mg caplet 0.37USD caplet Loperamide 2 mg caplet 0.37USD caplet Qc anti-diarrheal adv caplet 0.3USD caplet Diamode 2 mg tablet 0.28USD tablet Kaopectate 240 mg softgel 0.25USD softgel capsule Anti-diarrheal 2 mg caplet 0.18USD caplet CVS Pharmacy anti-diarrheal 2 mg caplet 0.14USD caplet Kaopectate children's suspension 0.02USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) CA2134611 No 2002-12-24 2014-10-28 Canada US6814978 Yes 2002-02-26 2022-02-26 US US6103260 No 1997-07-17 2017-07-17 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 222.1 U.S. Patent 3,714,159; 3,884,916. water solubility Slight Not Available logP 5.5 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00086 mg/mL ALOGPS logP 4.44 ALOGPS logP 4.77 ChemAxon logS -5.7 ALOGPS pKa (Strongest Acidic) 13.96 ChemAxon pKa (Strongest Basic) 9.41 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 43.78 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 139.32 m3·mol-1 ChemAxon Polarizability 52.67 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9878 Blood Brain Barrier + 0.7709 Caco-2 permeable + 0.5875 P-glycoprotein substrate Substrate 0.7476 P-glycoprotein inhibitor I Inhibitor 0.8277 P-glycoprotein inhibitor II Inhibitor 0.8387 Renal organic cation transporter Inhibitor 0.5059 CYP450 2C9 substrate Non-substrate 0.8057 CYP450 2D6 substrate Non-substrate 0.5315 CYP450 3A4 substrate Substrate 0.7918 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9154 CYP450 2D6 inhibitor Inhibitor 0.8933 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9207 Ames test Non AMES toxic 0.768 Carcinogenicity Non-carcinogens 0.8564 Biodegradation Not ready biodegradable 0.9953 Rat acute toxicity 3.6560 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9461 hERG inhibition (predictor II) Inhibitor 0.7639
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
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
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed:10087042]
- Tan-No K, Niijima F, Nakagawasai O, Sato T, Satoh S, Tadano T: Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. Eur J Pharm Sci. 2003 Nov;20(3):357-63. [PubMed:14592702]
- Roge J, Baumer P, Berard H, Schwartz JC, Lecomte JM: The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide. Scand J Gastroenterol. 1993 Apr;28(4):352-4. [PubMed:8488368]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E: Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. [PubMed:6319884]
- di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O: Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors. Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12. [PubMed:18284554]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E: Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. [PubMed:6319884]
- di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O: Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors. Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12. [PubMed:18284554]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed:10087042]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1A
- Uniprot ID
- O00555
- Uniprot Name
- Voltage-dependent P/Q-type calcium channel subunit alpha-1A
- Molecular Weight
- 282362.39 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
- Church J, Fletcher EJ, Abdel-Hamid K, MacDonald JF: Loperamide blocks high-voltage-activated calcium channels and N-methyl-D-aspartate-evoked responses in rat and mouse cultured hippocampal pyramidal neurons. Mol Pharmacol. 1994 Apr;45(4):747-57. [PubMed:8183255]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Modulator
- General Function
- Type 4 melanocortin receptor binding
- Specific Function
- ACTH stimulates the adrenal glands to release cortisol.MSH (melanocyte-stimulating hormone) increases the pigmentation of skin by increasing melanin production in melanocytes.Beta-endorphin and Met...
- Gene Name
- POMC
- Uniprot ID
- P01189
- Uniprot Name
- Pro-opiomelanocortin
- Molecular Weight
- 29423.72 Da
References
- Nomura A, Iwasaki Y, Aoki Y, Yamamori E, Mutsuga N, Yoshida M, Asai M, Oiso Y, Saito H: Effects of loperamide and other opioid-related substances on the transcriptional regulation of the rat pro-opiomelanocortin gene in AtT20 cells. Neuroendocrinology. 2001 Aug;74(2):87-94. [PubMed:11474216]
- Auernhammer CJ, Stalla GK, Lange M, Pfeiffer A, Muller OA: Effects of loperamide on the human hypothalamo-pituitary-adrenal axis in vivo and in vitro. J Clin Endocrinol Metab. 1992 Aug;75(2):552-7. [PubMed:1322429]
- Ambrosi B, Bochicchio D, Ferrario R, Colombo P, Faglia G: Effects of the opiate agonist loperamide on pituitary-adrenal function in patients with suspected hypercortisolism. J Endocrinol Invest. 1989 Jan;12(1):31-5. [PubMed:2545766]
- Ambrosi B, Bochicchio D, Colombo P, Ferrario R, Faglia G: Loperamide modifies but does not block the corticotropin-releasing hormone-induced ACTH response in patients with Addison's disease. Horm Metab Res Suppl. 1987;16:74-5. [PubMed:2832297]
- Bochicchio D, Ambrosi B, Faglia G: Loperamide, an opiate analog, differently modifies the adrenocorticotropin responses to corticotropin-releasing hormone and lysine vasopressin in patients with Addison's disease. Neuroendocrinology. 1988 Dec;48(6):611-4. [PubMed:2855105]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Titin binding
- Specific Function
- Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
- Gene Name
- CALM1
- Uniprot ID
- P0DP23
- Uniprot Name
- Calmodulin
- Molecular Weight
- 16837.47 Da
References
- Daly JW, Harper J: Loperamide: novel effects on capacitative calcium influx. Cell Mol Life Sci. 2000 Jan 20;57(1):149-57. [PubMed:10949586]
- Suzuki T, Sakai H, Ikari A, Takeguchi N: Inhibition of thromboxane A(2)-induced Cl(-) secretion by antidiarrhea drug loperamide in isolated rat colon. J Pharmacol Exp Ther. 2000 Oct;295(1):233-8. [PubMed:10991984]
- Mellstrand T: Loperamide--an opiate receptor agonist with gastrointestinal motility effects. Scand J Gastroenterol Suppl. 1987;130:65-6. [PubMed:2820051]
- Stoll R, Ruppin H, Domschke W: Calmodulin-mediated effects of loperamide on chloride transport by brush border membrane vesicles from human ileum. Gastroenterology. 1988 Jul;95(1):69-76. [PubMed:2836258]
- Diener M, Knobloch SF, Rummel W: Action of loperamide on neuronally mediated and Ca2+- or cAMP-mediated secretion in rat colon. Eur J Pharmacol. 1988 Aug 2;152(3):217-25. [PubMed:2851449]
- 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
- 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
- Baker DE: Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8. [PubMed:18192961]
- Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656]
Transporters
- 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
- Wandel C, Kim R, Wood M, Wood A: Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. Anesthesiology. 2002 Apr;96(4):913-20. [PubMed:11964599]
- Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684]
- Schinkel AH, Wagenaar E, Mol CA, van Deemter L: P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest. 1996 Jun 1;97(11):2517-24. [PubMed:8647944]
Drug created on June 13, 2005 07:24 / Updated on August 15, 2018 09:45