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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 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 Contract Pharmacy Services Pa 2017-09-20 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 Remedy Repack 2017-12-12 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 - 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 2003-02-25 2017-12-01 US A D Tablet, film coated 2 mg/1 Oral Western Family Foods 2003-04-10 2017-12-01 US Alti-loperamide - 2mg Caplet Tablet 2 mg Oral Altimed Pharma Inc. 1995-12-31 1997-08-14 Canada 
Anti Diarrheal Tablet, film coated 2 mg/1 Oral Remedy Repack 2017-10-11 Not applicable 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 Preferreed Pharmaceuticals Inc. 2015-11-20 Not applicable US Anti Diarrheal Tablet 2 mg/1 Oral Army + Air Force Exchange Service 2005-05-03 Not applicable US Anti Diarrheal Tablet, film coated 2 mg/1 Oral CVS Health 2003-02-24 Not applicable US Anti Diarrheal Tablet, film coated 2 mg/1 Oral Publix Supermarkets, Inc. 2003-03-19 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Imodium Complete Caplets Loperamide hydrochloride (2 mg) + Simethicone (125 mg) Tablet Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc 2002-06-20 Not applicable 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
- Antidiarrhea Agents
- Antidiarrheals
- Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
- Antipropulsives
- Calcium Channel Blockers
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A4 Substrates
- 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.
- Structured Indications
- Pharmacodynamics
Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Loperamide is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids. It works specifically by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.
- Mechanism of action
In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-selective calcium channel blocker and binds to opioid mu-receptors. Evidence also suggests that at higher concentrations it binds to calmodulin.
Target Actions Organism AMu-type opioid receptor 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 2-HYDROXY-1,4-NAPHTHOQUINONE The therapeutic efficacy of 2-HYDROXY-1,4-NAPHTHOQUINONE can be increased when used in combination with Loperamide. Experimental 2-mercaptobenzothiazole The therapeutic efficacy of 2-mercaptobenzothiazole can be increased when used in combination with Loperamide. Vet Approved Abiraterone The serum concentration of Loperamide can be increased when it is combined with Abiraterone. Approved Afatinib The serum concentration of Afatinib can be increased when it is combined with Loperamide. Approved Alfuzosin The risk or severity of hypotension can be increased when Alfuzosin is combined with Loperamide. Approved, Investigational Amiodarone The metabolism of Loperamide can be decreased when combined with Amiodarone. Approved, Investigational Amobarbital The metabolism of Loperamide can be increased when combined with Amobarbital. Approved, Illicit Amorolfine The therapeutic efficacy of Amorolfine can be increased when used in combination with Loperamide. Approved, Investigational Amphotericin B The therapeutic efficacy of Amphotericin B can be increased when used in combination with Loperamide. Approved, Investigational Anidulafungin The therapeutic efficacy of Anidulafungin can be increased when used in combination with Loperamide. Approved, Investigational Apalutamide The serum concentration of Loperamide can be decreased when it is combined with Apalutamide. Approved, Investigational Aprepitant The serum concentration of Loperamide can be increased when it is combined with Aprepitant. Approved, Investigational Arotinolol The risk or severity of hypotension, conduction block, and bradycardia can be increased when Arotinolol is combined with Loperamide. Investigational Artemether The metabolism of Loperamide can be decreased when combined with Artemether. Approved Atazanavir The metabolism of Loperamide can be decreased when combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Loperamide can be decreased when combined with Atomoxetine. Approved Bafilomycin A1 The therapeutic efficacy of Bafilomycin A1 can be increased when used in combination with Loperamide. 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 Benzoic Acid The therapeutic efficacy of Benzoic Acid can be increased when used in combination with Loperamide. Approved, Investigational Betaxolol The metabolism of Loperamide can be decreased when combined with Betaxolol. Approved, Investigational Bifonazole The therapeutic efficacy of Bifonazole can be increased when used in combination with Loperamide. Approved, Investigational Boceprevir The metabolism of Loperamide can be decreased when combined with Boceprevir. Approved, Withdrawn Bortezomib The metabolism of Loperamide can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Loperamide can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Loperamide. Approved Brefeldin A The therapeutic efficacy of Brefeldin A can be increased when used in combination with Loperamide. Experimental Brentuximab vedotin The serum concentration of Brentuximab vedotin 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 Bupropion The metabolism of Loperamide can be decreased when combined with Bupropion. Approved Butenafine The therapeutic efficacy of Butenafine can be increased when used in combination with Loperamide. Approved Butoconazole The therapeutic efficacy of Butoconazole can be increased when used in combination with Loperamide. Approved Calcium Acetate The therapeutic efficacy of Loperamide can be decreased when used in combination with Calcium Acetate. 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, Experimental, 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 Candicidin The therapeutic efficacy of Candicidin can be increased when used in combination with Loperamide. Withdrawn Capric acid The therapeutic efficacy of Capric acid can be increased when used in combination with Loperamide. Experimental Carbamazepine The metabolism of Loperamide can be increased when combined with Carbamazepine. Approved, Investigational Carvedilol The risk or severity of hypotension can be increased when Carvedilol is combined with Loperamide. Approved, Investigational Casein The therapeutic efficacy of Loperamide can be decreased when used in combination with Casein. Approved Caspofungin The therapeutic efficacy of Caspofungin can be increased when used in combination with Loperamide. Approved Celecoxib The metabolism of Loperamide can be decreased when combined with Celecoxib. Approved, Investigational Ceritinib The serum concentration of Loperamide can be increased when it is combined with Ceritinib. Approved Cerulenin The therapeutic efficacy of Cerulenin can be increased when used in combination with Loperamide. Approved Chloroquine The metabolism of Loperamide can be decreased when combined with Chloroquine. Approved, Investigational, Vet Approved Chloroxine The therapeutic efficacy of Chloroxine can be increased when used in combination with Loperamide. Approved Chlorpromazine The metabolism of Loperamide can be decreased when combined with Chlorpromazine. Approved, Investigational, Vet Approved Cholecalciferol The metabolism of Loperamide can be decreased when combined with Cholecalciferol. Approved, Nutraceutical Ciclopirox The therapeutic efficacy of Ciclopirox can be increased when used in combination with Loperamide. Approved, Investigational Cimetidine The serum concentration of Loperamide can be increased when it is combined with Cimetidine. Approved, Investigational Cinacalcet The metabolism of Loperamide can be decreased when combined with Cinacalcet. Approved Citalopram The metabolism of Loperamide can be decreased when combined with Citalopram. Approved Clarithromycin The metabolism of Loperamide can be decreased when combined with Clarithromycin. Approved Clemastine The metabolism of Loperamide can be decreased when combined with Clemastine. Approved, Investigational Clobazam The metabolism of Loperamide can be decreased when combined with Clobazam. Approved, Illicit Clomipramine The metabolism of Loperamide can be decreased when combined with Clomipramine. Approved, Investigational, Vet 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 metabolism of Loperamide can be decreased when combined with Clozapine. Approved Cobicistat The serum concentration of Loperamide can be increased when it is combined with Cobicistat. Approved Cocaine The metabolism of Loperamide can be decreased when combined with Cocaine. Approved, Illicit Colchicine The serum concentration of Colchicine can be increased when it is combined with Loperamide. Approved Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Loperamide. Approved, Investigational Cordycepin The therapeutic efficacy of Cordycepin can be increased when used in combination with Loperamide. Investigational Crisaborole The metabolism of Loperamide can be decreased when combined with Crisaborole. Approved, Investigational Crizotinib The metabolism of Loperamide can be decreased when combined with Crizotinib. Approved Cyclosporine The metabolism of Loperamide can be decreased when combined with Cyclosporine. Approved, Investigational, Vet Approved Dabigatran etexilate The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Loperamide. Approved Dabrafenib The serum concentration of Loperamide can be decreased when it is combined with Dabrafenib. Approved, Investigational Darifenacin The metabolism of Loperamide can be decreased when combined with Darifenacin. Approved, Investigational Darunavir The serum concentration of Loperamide can be increased when it is combined with Darunavir. Approved Dasatinib The serum concentration of Loperamide can be increased when it is combined with Dasatinib. Approved, Investigational 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 metabolism of Loperamide can be decreased when combined with Desipramine. Approved, Investigational Dichlorophene The therapeutic efficacy of Dichlorophene can be increased when used in combination with Loperamide. Vet Approved Dihydroergotamine The metabolism of Loperamide can be decreased when combined with Dihydroergotamine. Approved, Investigational Diltiazem The metabolism of Loperamide can be decreased when combined with Diltiazem. Approved, Investigational Diphenhydramine The metabolism of Loperamide can be decreased when combined with Diphenhydramine. Approved, Investigational Dosulepin The metabolism of Loperamide can be decreased when combined with Dosulepin. Approved Doxazosin The risk or severity of hypotension can be increased when Doxazosin is combined with Loperamide. Approved Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Loperamide. Approved, Investigational Doxorubicin The metabolism of Loperamide can be decreased when combined with Doxorubicin. Approved, Investigational Doxycycline The metabolism of Loperamide can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronedarone The metabolism of Loperamide can be decreased when combined with Dronedarone. Approved Duloxetine The metabolism of Loperamide can be decreased when combined with Duloxetine. Approved Econazole The therapeutic efficacy of Econazole can be increased when used in combination with Loperamide. 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 Eliglustat The metabolism of Loperamide can be decreased when combined with Eliglustat. Approved Enzalutamide The serum concentration of Loperamide can be decreased when it is combined with Enzalutamide. Approved Erythromycin The metabolism of Loperamide can be decreased when combined with Erythromycin. Approved, Investigational, Vet Approved Everolimus The serum concentration of Everolimus can be increased when it is combined with Loperamide. Approved Felodipine The metabolism of Loperamide can be decreased when combined with Felodipine. Approved, Investigational Fenticonazole The therapeutic efficacy of Fenticonazole can be increased when used in combination with Loperamide. Experimental Fluconazole The metabolism of Loperamide can be decreased when combined with Fluconazole. Approved, Investigational Flucytosine The therapeutic efficacy of Flucytosine can be increased when used in combination with Loperamide. Approved, Investigational Fluoxetine The metabolism of Loperamide can be decreased when combined with Fluoxetine. Approved, Vet Approved Flutrimazole The therapeutic efficacy of Flutrimazole can be increased when used in combination with Loperamide. Experimental Fluvoxamine The metabolism of Loperamide can be decreased when combined with Fluvoxamine. Approved, Investigational Fosamprenavir The metabolism of Loperamide can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Loperamide can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The metabolism of Loperamide can be increased when combined with Fosphenytoin. Approved, Investigational Fusidic Acid The serum concentration of Loperamide can be increased when it is combined with Fusidic Acid. Approved, Investigational Glyphosate The therapeutic efficacy of Glyphosate can be increased when used in combination with Loperamide. Experimental Griseofulvin The therapeutic efficacy of Griseofulvin can be increased when used in combination with Loperamide. Approved, Investigational, Vet Approved Hachimycin The therapeutic efficacy of Hachimycin can be increased when used in combination with Loperamide. Experimental Haloperidol The metabolism of Loperamide can be decreased when combined with Haloperidol. Approved Haloprogin The therapeutic efficacy of Haloprogin can be increased when used in combination with Loperamide. Approved, Withdrawn Hexetidine The therapeutic efficacy of Hexetidine can be increased when used in combination with Loperamide. Approved, Investigational Hexobarbital The metabolism of Loperamide can be increased when combined with Hexobarbital. Approved Idelalisib The metabolism of Loperamide can be decreased when combined with Idelalisib. Approved Imatinib The metabolism of Loperamide can be decreased when combined with Imatinib. Approved Imipramine The metabolism of Loperamide can be decreased when combined with Imipramine. Approved Indinavir The metabolism of Loperamide can be decreased when combined with Indinavir. Approved Indoramin The risk or severity of hypotension can be increased when Indoramin is combined with Loperamide. Withdrawn Irbesartan The metabolism of Loperamide can be decreased when combined with Irbesartan. Approved, Investigational Isavuconazole The serum concentration of Loperamide can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The metabolism of Loperamide can be decreased when 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 metabolism of Loperamide can be decreased when combined with Isradipine. Approved, Investigational Itraconazole The metabolism of Loperamide can be decreased when combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Loperamide can be increased when it is combined with Ivacaftor. Approved 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 Lapatinib The metabolism of Loperamide can be decreased when combined with Lapatinib. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Loperamide. Approved Lopinavir The metabolism of Loperamide can be decreased when combined with Lopinavir. Approved Lorcaserin The metabolism of Loperamide can be decreased when combined with Lorcaserin. Approved Lorpiprazole The serum concentration of Loperamide can be increased when it is combined with Lorpiprazole. Approved Losartan The metabolism of Loperamide can be decreased when combined with Losartan. Approved Lovastatin The metabolism of Loperamide can be decreased when combined with Lovastatin. Approved, Investigational Luliconazole The serum concentration of Loperamide can be increased when it is combined with Luliconazole. Approved Lumacaftor The serum concentration of Loperamide can be increased when it is combined with Lumacaftor. Approved Lumefantrine The metabolism of Loperamide can be decreased when combined with Lumefantrine. Approved 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 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 Manidipine The metabolism of Loperamide can be decreased when combined with Manidipine. Approved, Investigational Mepartricin The therapeutic efficacy of Mepartricin can be increased when used in combination with Loperamide. Experimental Methadone The metabolism of Loperamide can be decreased when combined with Methadone. Approved Methohexital The metabolism of Loperamide can be increased when combined with Methohexital. Approved Methotrimeprazine The metabolism of Loperamide can be decreased when combined with Methotrimeprazine. Approved, Investigational Methylphenobarbital The metabolism of Loperamide can be increased when combined with Methylphenobarbital. Approved Metoprolol The metabolism of Loperamide can be decreased when combined with Metoprolol. Approved, Investigational Mevastatin The therapeutic efficacy of Mevastatin can be increased when used in combination with Loperamide. Experimental Micafungin The therapeutic efficacy of Micafungin can be increased when used in combination with Loperamide. Approved, Investigational Miconazole The therapeutic efficacy of Miconazole can be increased when used in combination with Loperamide. Approved, Investigational, Vet Approved Midostaurin The metabolism of Loperamide can be decreased when combined with Midostaurin. Approved, Investigational Mifepristone The serum concentration of Loperamide can be increased when it is combined with Mifepristone. Approved, Investigational Miltefosine The therapeutic efficacy of Miltefosine can be increased when used in combination with Loperamide. Approved, Investigational Mirabegron The metabolism of Loperamide can be decreased when combined with Mirabegron. Approved Mitotane The serum concentration of Loperamide can be decreased when it is combined with Mitotane. Approved Monensin The therapeutic efficacy of Monensin can be increased when used in combination with Loperamide. Vet Approved Myxothiazol The therapeutic efficacy of Myxothiazol can be increased when used in combination with Loperamide. Experimental Nafcillin The therapeutic efficacy of Loperamide can be decreased when used in combination with Nafcillin. Approved, Investigational Naftifine The therapeutic efficacy of Naftifine can be increased when used in combination with Loperamide. Approved Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Loperamide. Approved Natamycin The therapeutic efficacy of Natamycin can be increased when used in combination with Loperamide. Approved Nefazodone The metabolism of Loperamide can be decreased when combined with Nefazodone. Approved, Withdrawn Nelfinavir The metabolism of Loperamide can be decreased when combined with Nelfinavir. Approved 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 metabolism of Loperamide can be decreased when combined with Nicardipine. Approved, Investigational Nifuratel The therapeutic efficacy of Nifuratel can be increased when used in combination with Loperamide. Experimental Nikkomycin Z The therapeutic efficacy of Nikkomycin Z can be increased when used in combination with Loperamide. Investigational Nilotinib The metabolism of Loperamide can be decreased when combined with Nilotinib. Approved, Investigational Nitroprusside Loperamide may increase the hypotensive activities of Nitroprusside. Approved, Investigational Nitroxoline The therapeutic efficacy of Nitroxoline can be increased when used in combination with Loperamide. Approved Nystatin The therapeutic efficacy of Nystatin can be increased when used in combination with Loperamide. Approved, Vet Approved Olaparib The metabolism of Loperamide can be decreased when combined with Olaparib. Approved Omoconazole The therapeutic efficacy of Omoconazole can be increased when used in combination with Loperamide. Experimental Osimertinib The serum concentration of Loperamide can be increased when it is combined with Osimertinib. Approved Oxiconazole The therapeutic efficacy of Oxiconazole can be increased when used in combination with Loperamide. Approved Pafuramidine The therapeutic efficacy of Pafuramidine can be increased when used in combination with Loperamide. Investigational Palbociclib The serum concentration of Loperamide can be increased when it is combined with Palbociclib. Approved, Investigational Panobinostat The serum concentration of Loperamide can be increased when it is combined with Panobinostat. Approved, Investigational Paroxetine The metabolism of Loperamide can be decreased when combined with Paroxetine. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Loperamide. Approved Peginterferon alfa-2b The serum concentration of Loperamide can be decreased when it is combined with Peginterferon alfa-2b. Approved Pentamidine The therapeutic efficacy of Pentamidine can be increased when used in combination with Loperamide. Approved, Investigational Pentobarbital The metabolism of Loperamide can be increased when combined with Pentobarbital. Approved, Investigational, Vet Approved Phenobarbital The metabolism of Loperamide can be increased when combined with Phenobarbital. Approved, Investigational Phenytoin The metabolism of Loperamide can be increased when combined with Phenytoin. Approved, Vet Approved Pioglitazone The metabolism of Loperamide can be decreased when combined with Pioglitazone. Approved, Investigational Pitolisant The serum concentration of Loperamide can be decreased when it is combined with Pitolisant. Approved, Investigational Posaconazole The metabolism of Loperamide can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Prazosin The risk or severity of hypotension can be increased when Prazosin is combined with Loperamide. Approved Primidone The metabolism of Loperamide can be increased when combined with Primidone. Approved, Vet Approved Promazine The metabolism of Loperamide can be decreased when combined with Promazine. Approved, Vet Approved Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Loperamide. Approved Pyrrolnitrin The therapeutic efficacy of Pyrrolnitrin can be increased when used in combination with Loperamide. Experimental Quazepam The serum concentration of Loperamide can be increased when it is combined with Quazepam. Approved, Illicit Quinidine The metabolism of Loperamide can be decreased when combined with Quinidine. Approved, Investigational Quinine The metabolism of Loperamide can be decreased when combined with Quinine. Approved Rabeprazole The metabolism of Loperamide can be decreased when combined with Rabeprazole. Approved, Investigational Radicicol The therapeutic efficacy of Radicicol can be increased when used in combination with Loperamide. Experimental Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Loperamide. Approved, Investigational Rifabutin The metabolism of Loperamide can be increased when combined with Rifabutin. Approved, Investigational Rifampicin The metabolism of Loperamide can be increased when combined with Rifampicin. Approved Rifapentine The metabolism of Loperamide can be increased when combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Loperamide. Approved, Investigational Ritonavir The metabolism of Loperamide can be decreased when combined with Ritonavir. Approved, Investigational Rolapitant The metabolism of Loperamide can be decreased when combined with Rolapitant. Approved, Investigational Ropinirole The metabolism of Loperamide can be decreased when combined with Ropinirole. Approved, Investigational Rosiglitazone The metabolism of Loperamide can be decreased when combined with Rosiglitazone. Approved, Investigational Rucaparib The metabolism of Loperamide can be decreased when combined with Rucaparib. Approved, Investigational Salicylhydroxamic Acid The therapeutic efficacy of Salicylhydroxamic Acid can be increased when used in combination with Loperamide. Experimental Salicylic acid The therapeutic efficacy of Salicylic acid can be increased when used in combination with Loperamide. Approved, Investigational, 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 Sertaconazole The therapeutic efficacy of Sertaconazole can be increased when used in combination with Loperamide. Approved, Investigational Sertraline The metabolism of Loperamide can be decreased when combined with Sertraline. Approved Sildenafil The metabolism of Loperamide can be decreased when combined with Sildenafil. Approved, Investigational Silodosin The serum concentration of Silodosin can be increased when it is combined with Loperamide. Approved Siltuximab The serum concentration of Loperamide can be decreased when it is combined with Siltuximab. Approved, Investigational Simeprevir The serum concentration of Loperamide can be increased when it is combined with Simeprevir. Approved Sinefungin The therapeutic efficacy of Sinefungin can be increased when used in combination with Loperamide. Experimental Sirolimus The therapeutic efficacy of Sirolimus can be increased when used in combination with Loperamide. Approved, Investigational Sorafenib The metabolism of Loperamide can be decreased when combined with Sorafenib. Approved, Investigational St. John's Wort The serum concentration of Loperamide can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical 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 Sulfamethoxazole The metabolism of Loperamide can be decreased when combined with Sulfamethoxazole. Approved Sulfisoxazole The metabolism of Loperamide can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Tamoxifen The metabolism of Loperamide can be decreased when combined with Tamoxifen. Approved Tamsulosin The risk or severity of hypotension can be increased when Tamsulosin is combined with Loperamide. Approved, Investigational Tavaborole The therapeutic efficacy of Tavaborole can be increased when used in combination with Loperamide. Approved, Investigational 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 Terazosin The risk or severity of hypotension can be increased when Terazosin is combined with Loperamide. Approved Terbinafine The metabolism of Loperamide can be decreased when combined with Terbinafine. Approved, Investigational, Vet Approved Terconazole The therapeutic efficacy of Terconazole can be increased when used in combination with Loperamide. Approved Teriflunomide The metabolism of Loperamide can be decreased when combined with Teriflunomide. Approved 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 Thioridazine The metabolism of Loperamide can be decreased when combined with Thioridazine. Approved, Withdrawn Thiotepa The metabolism of Loperamide can be decreased when combined with Thiotepa. Approved, Investigational Thymol The therapeutic efficacy of Thymol can be increased when used in combination with Loperamide. Approved Ticlopidine The metabolism of Loperamide can be decreased when combined with Ticlopidine. Approved Tioconazole The therapeutic efficacy of Tioconazole can be increased when used in combination with Loperamide. Approved Tipranavir The metabolism of Loperamide can be decreased when combined with Tipranavir. Approved, Investigational Tocilizumab The serum concentration of Loperamide can be decreased when it is combined with Tocilizumab. Approved Tolciclate The therapeutic efficacy of Tolciclate can be increased when used in combination with Loperamide. Experimental Tolnaftate The therapeutic efficacy of Tolnaftate can be increased when used in combination with Loperamide. Approved, Investigational, Vet Approved Topiroxostat The metabolism of Loperamide can be decreased when combined with Topiroxostat. Approved, Investigational Topotecan The serum concentration of Topotecan can be increased when it is combined with Loperamide. Approved, Investigational Tranylcypromine The metabolism of Loperamide can be decreased when combined with Tranylcypromine. Approved, Investigational Trimazosin The risk or severity of hypotension can be increased when Trimazosin is combined with Loperamide. Experimental Trimethoprim The metabolism of Loperamide can be decreased when combined with Trimethoprim. Approved, Vet Approved Trimetrexate The therapeutic efficacy of Trimetrexate can be increased when used in combination with Loperamide. Approved, Investigational Urapidil The risk or severity of hypotension can be increased when Urapidil is combined with Loperamide. Investigational Vemurafenib The serum concentration of Loperamide can be increased when it is combined with Vemurafenib. Approved Venlafaxine The metabolism of Loperamide can be decreased when combined with Venlafaxine. Approved Verapamil The metabolism of Loperamide can be decreased when combined with Verapamil. Approved Vincristine The excretion of Vincristine can be decreased when combined with Loperamide. Approved, Investigational Voriconazole The metabolism of Loperamide can be decreased when combined with Voriconazole. Approved, Investigational Ziprasidone The metabolism of Loperamide can be decreased when combined with Ziprasidone. Approved - Food Interactions
- Take without regard to meals. Increase liquid intake.
References
- Synthesis Reference
Tsutomu Awamura, Hisanobu Nishikawa, Toshio Inagi, "FILM PREPARATION CONTAINING LOPERAMIDE HYDROCHLORIDE." U.S. Patent US20110159058, issued June 30, 2011.
US20110159058- General References
- Not Available
- External Links
- Human Metabolome Database
- 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 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
- 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
- SubstrateInhibitor
- 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 April 22, 2018 23:40