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Identification
NameLoperamide
Accession NumberDB00836  (APRD00275)
TypeSmall Molecule
GroupsApproved
Description

One of the long-acting synthetic antidiarrheals; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally. [PubChem]

Structure
Thumb
Synonyms
Loperamid
Loperamida
Lopéramide
Loperamidum
External Identifiers
  • PJ 185
  • R 18553
Approved Prescription ProductsNot Available
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Loperamide Hydrochloridecapsule2 mg/1oralNorthwind Pharmaceuticals, LLC2014-10-22Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralA S Medication Solutions1993-05-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralTeva Pharmaceuticals USA Inc1993-05-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralREMEDYREPACK INC.2013-03-18Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralDIRECT RX2014-01-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralMylan Institutional Inc.1997-10-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralCardinal Health1991-09-182015-12-29Us
Loperamide Hydrochloridecapsule2 mg/1oralREMEDYREPACK INC.2011-11-16Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralClinical Solutions Wholesale1993-05-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralMc Kesson Contract Packaging2012-01-26Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralUnit Dose Services2012-10-12Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralRebel Distributors Corp1992-04-30Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralPd Rx Pharmaceuticals, Inc.2011-09-23Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralPreferred Pharmaceuticals, Inc.2011-01-28Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-10-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralCardinal Health2011-07-27Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralSTAT Rx USA LLC1993-05-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-10-12Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralPd Rx Pharmaceuticals, Inc.2012-10-12Not applicableUs
Loperamide Hydrochloridesolution2 mg/10mLoralCardinal Health1992-04-30Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-10-12Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralDispensing Solutions, Inc.2011-09-23Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralPd Rx Pharmaceuticals, Inc.2011-09-23Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralREMEDYREPACK INC.2013-02-11Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralPhysicians Total Care, Inc.1996-06-20Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralMylan Pharmaceuticals Inc.1991-09-18Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralbryant ranch prepack1993-05-01Not applicableUs
Loperamide Hydrochloridecapsule2 mg/1oralAidarex Pharmaceuticals LLC1993-05-01Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
7 Select Anti Diarrhealtablet, film coated2 mg/1oral7 Eleven2014-08-05Not applicableUs
A Dtablet, film coated2 mg/1oralWestern Family Foods Inc2003-04-10Not applicableUs
A Dtablet, film coated2 mg/1oralWestern Family Foods Inc2003-02-25Not applicableUs
Alti-loperamide - 2mg Caplettablet2 mgoralAltimed Pharma Inc.1995-12-311997-08-14Canada
Anti Diarrhealtablet, film coated2 mg/1oralH E B2014-05-01Not applicableUs
Anti Diarrhealtablet2 mg/1oralArmy and Air Force Exchange Service2005-05-03Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralPreferred Pharmaceuticals Inc.2015-11-20Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralPublix Super Markets Inc2003-03-19Not applicableUs
Anti Diarrhealsolution1 mg/5mLoralRite Aid Corporation1992-07-13Not applicableUs
Anti Diarrhealsolution1 mg/5mLoralRebel Distributors Corp1992-07-13Not applicableUs
Anti Diarrhealcapsule2 mg/1oralWal Mart Stores Inc2005-05-032015-12-29Us
Anti Diarrhealtablet, film coated2 mg/1oralKroger Company2003-02-21Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralHy Vee Inc2003-03-21Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralShopko Stores Operating Co., LLC2003-03-07Not applicableUs
Anti Diarrhealsolution1 mg/5mLoralMeijer Distribution Inc1992-04-17Not applicableUs
Anti Diarrhealtablet2 mg/1oralBedrock Brands, Llc2005-05-03Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralCVS Pharmacy2003-04-21Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralKroger Company2003-03-31Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralMeijer Distribution Inc2003-03-05Not applicableUs
Anti Diarrhealcapsule2 mg/1oralNash Finch Company2005-05-03Not applicableUs
Anti Diarrhealtablet2 mg/1oralHarmon Store Inc.2005-05-03Not applicableUs
Anti Diarrhealtablet2 mg/1oralSam's West Inc2005-05-03Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralMajor Pharmaceuticals2003-02-24Not applicableUs
Anti Diarrhealtablet2 mg/1oralL.N.K. International, Inc.2005-05-03Not applicableUs
Anti Diarrhealtablet, film coated2 mg/1oralCVS Pharmacy2003-02-24Not applicableUs
Anti-diarrhealtablet2 mg/1oralGreenbrier International, Inc.2005-05-03Not applicableUs
Anti-diarrhealtablet2 mg/1oralL.N.K. International, Inc.2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralDolgencorp, Inc. (DOLLAR GENERAL & REXALL)2011-11-10Not applicableUs
Anti-diarrhealtablet2 mg/1oralGREAT LAKES WHOLESALE, MARKETING, & SALES, INC.2005-05-03Not applicableUs
Anti-diarrhealtablet2 mg/1oralBetter Living Brands, Llc2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralGeiss, Destin & Dunn, Inc (Goodsense)2010-07-15Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralFreds Inc2010-07-08Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralCVS Pharmacy2010-07-08Not applicableUs
Anti-diarrhealtablet2 mg/1oralH E B2005-05-03Not applicableUs
Anti-diarrhealtablet2 mg/1oralSam's West Inc2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralWalgreens2012-05-30Not applicableUs
Anti-diarrhealtablet2 mg/1oralWOONSOCKET PRESCRIPTION CENTER,INCORPORATED2005-05-03Not applicableUs
Anti-diarrhealtablet2 mg/1oralChain Drug Consortium2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralBest Choice (Valu Merchandisers Company)2010-08-30Not applicableUs
Anti-diarrhealtablet2 mg/1oralWALGREEN CO.2005-05-03Not applicableUs
Anti-diarrhealtablet2 mg/1oralL&R Distributors, Inc.2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralCare One (American Sales Company)2010-08-05Not applicableUs
Anti-diarrhealtablet2 mg/1oralFamily Dollar2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralASSURED / DOLLAR TREE (Greenbrier International, Inc.)2013-11-20Not applicableUs
Anti-diarrhealtablet2 mg/1oralRite Aid2005-05-03Not applicableUs
Anti-diarrhealtablet2 mg/1oralSUPERVALU INC.2005-05-03Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralAmerisource Bergen (Good Neighbor Pharmacy) 461222013-06-07Not applicableUs
Anti-diarrhealtablet2 mg/1oralGeri Care Pharmaceutical Corp2006-01-01Not applicableUs
Anti-diarrhealcapsule, liquid filled2 mg/1oralQUALITY CHOICE (Chain Drug Marketing Association)2013-05-31Not applicableUs
Anti-diarrheal Caplets - 2mgtablet2 mgoralStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1995-12-312007-08-01Canada
Anti-diarrheal Loperamide HClcapsule, liquid filled2 mg/1oralWestern Family Foods, Inc.2010-07-05Not applicableUs
Anti-diarrheal Loperamide HClcapsule, liquid filled2 mg/1oralEQUATE (Walmart Stores, Inc.)2013-01-15Not applicableUs
Anti-diarrheal Loperamide HClcapsule, liquid filled2 mg/1oralMcKesson (Sunmark)2010-07-09Not applicableUs
Anti-diarrheal Loperamide HClcapsule, liquid filled2 mg/1oralTOP CARE (Topco Associates LLC)2010-07-16Not applicableUs
Antidiarrheal Relieftablet2 mg/1oralNorth Safety Products LLC2013-04-29Not applicableUs
Apo-loperamide - Tab 2mgtablet2 mgoralApotex Inc1996-12-31Not applicableCanada
Berkley and Jensen Anti Diarrhealtablet, film coated2 mg/1oralBJWC2003-04-19Not applicableUs
Care One Anti Diarrhealtablet, film coated2 mg/1oralAmerican Sales Company2004-01-23Not applicableUs
Care One Anti Diarrheal Loperamide Hydrochloridetablet, film coated2 mg/1oralAmerican Sales Company2004-01-23Not applicableUs
Careone Loperamide Hydrochloridesuspension1 mg/7.5mLoralAmerican Sales Company2014-05-10Not applicableUs
Careone Loperamide Hydrochloridesuspension1 mg/7.5mLoralAmerican Sales Company2012-05-21Not applicableUs
Circle K Anti-diarrhealtablet2 mg/1oralLil' Drug Store Products, Inc2014-11-01Not applicableUs
Dg Health Anti Diarrhealsuspension1 mg/7.5mLoralDolgencorp, LLC2015-11-19Not applicableUs
Dg Health Anti Diarrhealtablet, film coated2 mg/1oralDolgencorp, LLC2009-12-28Not applicableUs
Dg Health Loperamide Hydrochlorideliquid1 mg/7.5mLoralDolgencorp Inc2012-07-26Not applicableUs
Diahalt Caplets - 2mgtablet2 mgoralWampole Brands, A Division Of Pangeo Pharma (Canada) Inc.1997-04-112006-08-25Canada
Diarr-ezetablet2 mgoralPharmascience Inc1997-02-18Not applicableCanada
Diarr-eze - Liq Orl 0.2mg/mlsolution.2 mgoralPharmascience Inc1997-02-25Not applicableCanada
Diarrhea Relieftablet2 mgoralPharmascience Inc2004-06-11Not applicableCanada
Diarrhea Relieftablet2 mgoralTeva Canada Limited2014-01-24Not applicableCanada
Diarrhea Relieftablet2 mgoralLaboratoire Riva IncNot applicableNot applicableCanada
Diarrhea Relieftablet2 mgoralVita Health Products Inc2004-12-19Not applicableCanada
Diarrhea Relief - Caplets 2mgtablet2 mgoralStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1995-12-312002-07-31Canada
Diarrhea Relief Liquid Gelscapsule2 mgoralPharmascience IncNot applicableNot applicableCanada
Dom-loperamide Caplets 2mgtablet2 mgoralDominion Pharmacal2001-06-20Not applicableCanada
Dom-loperamide Hydrochloride Solution-orlsolution.2 mgoralDominion Pharmacal1995-12-31Not applicableCanada
Equaline Anti Diarrhealtablet, film coated2 mg/1oralSupervalu Inc2004-09-03Not applicableUs
Equaline Loperamide Hydrochloridesuspension1 mg/7.5mLoralSupervalu Inc2012-02-06Not applicableUs
Equate Anti Diarrhealtablet, film coated2 mg/1oralWal Mart Stores Inc2003-02-14Not applicableUs
Equate Loperamide Hydrochloridesuspension1 mg/7.5mLoralWal Mart Stores Inc2011-10-07Not applicableUs
Fad First Aid Direct Anti-diarrhealtablet, film coated2 mg/1oralFirst Aid Direct2014-10-15Not applicableUs
Family Wellness Anti Diarrhealtablet, film coated2 mg/1oralFamily Dollar Services Inc2003-02-26Not applicableUs
Good Neighbor Pharmacy Anti Diarrhealtablet, film coated2 mg/1oralAmerisource Bergen2003-05-12Not applicableUs
Good Neighbor Pharmacy Anti Diarrhealtablet, film coated2 mg/1oralAmerisource Bergen2008-06-26Not applicableUs
Good Neighbor Pharmacy Anti Diarrhealsolution1 mg/5mLoralAmerisource Bergen2003-09-19Not applicableUs
Good Neighbor Pharmacy Loperamide Hydrochloridesuspension1 mg/7.5mLoralAmerisource Bergen2014-01-31Not applicableUs
Good Neighbor Pharmacy Loperamide Hydrochlorideliquid1 mg/7.5mLoralAmerisource Bergen2012-02-17Not applicableUs
Good Sense Anti Diarrhealtablet, film coated2 mg/1oralL Perrigo Company2003-02-25Not applicableUs
Good Sense Anti Diarrhealsolution1 mg/5mLoralL. Perrigo Company1992-03-30Not applicableUs
Good Sense Loperamide Hydrochloridesuspension1 mg/7.5mLoralL Perrigo Company2012-01-31Not applicableUs
Harmon Face Values Anti Diarrhealtablet, film coated2 mg/1oralHarmon Stores Inc.2011-12-18Not applicableUs
Harris Teeter Anti Diarrhealtablet, film coated2 mg/1oralHarris Teeter, LLC2015-03-30Not applicableUs
Harris Teeter Loperamide Hydrochloridesuspension1 mg/7.5mLoralHarris Teeter, LLC2015-03-30Not applicableUs
Health Mart Anti Diarrhealtablet, film coated2 mg/1oralMc Kesson2012-03-20Not applicableUs
Health Mart Loperamide Hydrochloridesuspension1 mg/7.5mLoralMc Kesson2014-06-11Not applicableUs
Health Mart Loperamide Hydrochlorideliquid1 mg/7.5mLoralMc Kesson2012-03-20Not applicableUs
Healthy Accents Anti Diarrhealtablet, film coated2 mg/1oralDZA Brands LLC2008-02-04Not applicableUs
Imodium - Caplet 2mgtablet2 mgoralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1996-09-09Not applicableCanada
Imodium A-Dtablet, film coated2 mg/1oralREMEDYREPACK INC.2015-10-20Not applicableUs
Imodium A-Dtablet, film coated2 mg/1oralJohnson & Johnson Consumer Inc., Mc Neil Consumer Healthcare Division2015-07-13Not applicableUs
Imodium A-Dsolution1 mg/7.5mLoralJohnson & Johnson Consumer Inc., Mc Neil Consumer Healthcare Division2005-01-01Not applicableUs
Imodium Adtablet, coated2 mg/1oralLil' Drug Store Products, Inc.2010-05-10Not applicableUs
Imodium Calming Liquidsolution2 mgoralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc2007-07-11Not applicableCanada
Imodium Cap 2mgcapsule2 mgoralJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1983-12-311997-07-03Canada
Imodium Caplets 2mgtablet2 mgoralJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1990-12-311999-06-16Canada
Imodium Liqui-gelscapsule2 mgoralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc2013-07-02Not applicableCanada
Imodium Oral Sol 0.2mg/mlliquid.2 mgoralJanssen Pharmaceutica, Division Of Janssen Ortho Inc.1984-12-311996-09-10Canada
Imodium Quick Dissolvetablet2 mgoralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1997-09-24Not applicableCanada
Kirkland Signature Anti Diarrhealtablet, film coated2 mg/1oralCostco Wholesale Company2003-02-26Not applicableUs
Leader Anti Diarrhealsolution1 mg/5mLoralCardinal Health1997-10-28Not applicableUs
Leader Anti Diarrhealtablet, film coated2 mg/1oralCardinal Health2003-04-02Not applicableUs
Leader Anti-diarrhealtablet, film coated2 mg/1oralCardinal Health2014-09-25Not applicableUs
Leader Loperamidesuspension1 mg/7.5mLoralCardinal Health2014-05-30Not applicableUs
Leader Loperamide Hydrochlorideliquid1 mg/7.5mLoralCardinal Health2012-03-28Not applicableUs
Leader Loperamide Hydrochloridesuspension1 mg/7.5mLoralCardinal Health2014-04-23Not applicableUs
Lil Drug Store Anti-diarrhealtablet2 mg/1oralLil' Drug Store Products, Inc.2012-09-012015-12-30Us
Loperacaptablet2 mgoralValeant Canada Lp Valeant Canada S.E.C.1996-09-24Not applicableCanada
Loperamidetablet2 mgoralLaboratoires Trianon Inc2005-07-15Not applicableCanada
Loperamidetablet2 mgoralApotex IncNot applicableNot applicableCanada
Loperamidetablet2 mgoralD.C. Labs Limited2001-07-062005-07-19Canada
Loperamide HClcapsule, liquid filled2 mg/1oralTarget Corporation2011-10-01Not applicableUs
Loperamide HClcapsule, liquid filled2 mg/1oralMc Kesson2012-06-25Not applicableUs
Loperamide HClcapsule, liquid filled2 mg/1oralChain Drug Consortium, LLC2012-12-04Not applicableUs
Loperamide HCl Anti-diarrhealcapsule, liquid filled2 mg/1oralP And L Development Of New York Corporation (Ready In Case)2011-08-30Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralHy Vee Inc2012-04-30Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralZee Medical Inc2014-01-16Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralAmerisource Bergen1993-02-01Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralWin Co Foods, Llc1993-02-01Not applicableUs
Loperamide Hydrochloridesolution1 mg/5mLoralPreferred Pharmaceuticals, Inc.2012-07-27Not applicableUs
Loperamide Hydrochloridetablet2 mgoralVita Health Products Inc2000-06-012007-07-30Canada
Loperamide Hydrochlorideliquid1 mg/7.5mLoralShopko Stores Operating Co., LLC2013-08-08Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralMeijer Distribution Inc2012-05-11Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralCVS Pharmacy2012-02-28Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralChain Drug Marketing Association Inc.1993-02-01Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralPrecision Dose Inc.2014-02-26Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralPhysicians Total Care, Inc.2011-09-24Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralWalgreen Company2012-05-18Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralProficient Rx LP1993-02-01Not applicableUs
Loperamide Hydrochloridesolution1 mg/5mLoralPrecision Dose Inc.2009-09-012016-01-30Us
Loperamide Hydrochloridetablet2 mg/1oralMedline Industries, Inc.1993-02-01Not applicableUs
Loperamide Hydrochloridesolution1 mg/5mLoralAtlantic Biologicals Corps1995-11-17Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralShopko Stores Operating Co., LLC1993-02-01Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralFred's Inc.1993-02-01Not applicableUs
Loperamide Hydrochloridetablet, film coated2 mg/1oralCVS Pharmacy2015-12-04Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralKroger Company2013-08-06Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralFamily Dollar Services, Inc.1993-02-01Not applicableUs
Loperamide Hydrochloridetablet, film coated2 mg/1oralCVS Pharmacy2015-10-06Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralValu Merchandisers Company1993-02-01Not applicableUs
Loperamide Hydrochloridetablet, film coated2 mg/1oralCentral Texas Community Health Centers2003-06-27Not applicableUs
Loperamide Hydrochloridesolution1 mg/5mLoralHi Tech Pharmacal Co., Inc.1995-11-17Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralWestern Family Foods Inc2014-05-21Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralAurohealth LLC2015-12-15Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralChain Drug Consortium, LLC1993-02-01Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralSelect Brand1993-02-01Not applicableUs
Loperamide Hydrochlorideliquid1 mg/7.5mLoralMajor Pharmaceuticals2012-03-14Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralOhm Laboratories Inc.1993-02-01Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralCVS Pharmacy2014-02-04Not applicableUs
Loperamide Hydrochloridesolution2 mg/10mLoralPrecision Dose Inc.2009-08-182016-01-30Us
Loperamide Hydrochloridetablet2 mg/1oralREMEDYREPACK INC.2016-04-05Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralH E B2012-03-05Not applicableUs
Loperamide Hydrochlorideliquid1 mg/7.5mLoralPreferred Pharmaceuticals, Inc.2013-03-08Not applicableUs
Loperamide Hydrochlorideliquid1 mg/7.5mLoralWestern Family Foods Inc2012-05-19Not applicableUs
Loperamide Hydrochloridetablet2 mg/1oralWin Co Foods, Llc1993-02-01Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralRite Aid Corporation2012-05-23Not applicableUs
Loperamide Hydrochloridesuspension1 mg/7.5mLoralPrecision Dose Inc.2014-02-26Not applicableUs
Loperamide-2tablet2 mgoralPro Doc Limitee1997-11-05Not applicableCanada
Medex Anti-diarrheal Relieftablet2 mg/1oralMedex Merchandising, Llc2015-10-20Not applicableUs
Medique Diamodetablet2 mg/1oralUnifirst First Aid Corporation2008-12-30Not applicableUs
Novo-loperamide Tablets-2mgtablet2 mgoralTeva Canada Limited1995-12-31Not applicableCanada
PHL-loperamidetablet2 mgoralPharmel Inc2007-08-13Not applicableCanada
PMS-loperamide - Caplet 2mgtablet2 mgoralPharmascience Inc1996-09-12Not applicableCanada
PMS-loperamide Hydrochloride Solution.2mg/mlsolution0.2 mgoralPharmascience Inc1993-12-31Not applicableCanada
Preferred Plus Loperamidesuspension1 mg/7.5mLoralKinray2014-05-27Not applicableUs
Preferred Plus Loperamide Hydrochloridesuspension1 mg/7.5mLoralKinray2014-06-09Not applicableUs
Preferred Plus Loperamide Hydrochloridetablet, film coated2 mg/1oralKinray2014-05-27Not applicableUs
Rexall Anti Diarrhealsolution1 mg/5mLoralDolgencorp, LLC2010-08-09Not applicableUs
Rexall Anti Diarrhealtablet, film coated2 mg/1oralDolgencorp, LLC2010-08-15Not applicableUs
Rhoxal-loperamidetablet2 mgoralRhoxalpharma Inc1997-12-022009-11-24Canada
Riva-loperamidetablet2 mgoralLaboratoire Riva Inc1998-08-27Not applicableCanada
Rx Act Anti Diarrhealsolution1 mg/5mLoralH E B1992-05-14Not applicableUs
Rx Act Anti Diarrhealtablet, film coated2 mg/1oralH E B2003-03-24Not applicableUs
Sandoz Loperamidetablet2 mgoralSandoz Canada Incorporated2004-11-10Not applicableCanada
Shoprite Anti Diarrhealtablet, film coated2 mg/1oralWakefern Food Corporation2013-09-17Not applicableUs
Simply Right Anti Diarrhealtablet, film coated2 mg/1oralSam's West Inc2003-04-29Not applicableUs
Smart Sense Anti Diarrhealtablet, film coated2 mg/1oralKmart Corporation2011-01-09Not applicableUs
Smart Sense Anti Diarrhealsolution1 mg/5mLoralKmart Corporation2011-02-03Not applicableUs
Smart Sense Anti Diarrhealsuspension1 mg/7.5mLoralKmart Corporation2016-01-26Not applicableUs
Smart Sense Loperamide Hydrochloridesuspension1 mg/7.5mLoralKmart Corporation2012-05-14Not applicableUs
Stomach Relief Anti Diarrhealtablet2 mg/1oralSelect Corporation2012-10-15Not applicableUs
Sunmark Anti Diarrhealtablet, film coated2 mg/1oralMc Kesson2003-06-27Not applicableUs
Sunmark Anti Diarrhealsolution1 mg/5mLoralMc Kesson2003-09-19Not applicableUs
Sunmark Loperamide Hydrochloridesuspension1 mg/7.5mLoralMc Kesson2014-02-18Not applicableUs
Topcare Anti Diarrhealtablet, film coated2 mg/1oralTopco Associates LLC2003-02-26Not applicableUs
Topcare Loperamide Hydrochloridesuspension1 mg/7.5mLoralTopco Associates LLC2012-06-05Not applicableUs
Up and Up Anti Diarrhealsolution1 mg/5mLoralTarget Corporation2009-07-31Not applicableUs
Up and Up Anti Diarrhealsuspension1 mg/7.5mLoralTarget Corporation2016-02-26Not applicableUs
Up and Up Anti Diarrhealtablet2 mg/1oralTarget Corporation2009-07-20Not applicableUs
Vaprino A-Dtablet2 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2013-09-02Not applicableUs
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gadavyt Loperamide HClliquid1 mg/5mLoralGadal Laboratories Inc2013-05-01Not applicableUs
International Brands
NameCompany
DimorNordic Drugs
FortasecEsteve
ImodiumJohnson & Johnson
Kaopectate IIChattem, Inc.
LopediumSandoz
Lopedium expressSandoz
LopexOrion
Maalox Anti-DiarrhealNovartis International AG
Pepto Diarrhea ControlProcter & Gamble
Brand mixtures
NameLabellerIngredients
Imodium Complete CapletsMcneil Consumer Healthcare Division Of Johnson & Johnson Inc
Imodium Complete Chewable TabletsMcneil Consumer Healthcare Division Of Johnson & Johnson Inc
Salts
Name/CASStructureProperties
Loperamide hydrochloride
Thumb
  • InChI Key: PGYPOBZJRVSMDS-UHFFFAOYSA-N
  • Monoisotopic Mass: 512.199733756
  • Average Mass: 513.498
DBSALT000709
Loperamide oxide
106900-12-3
Thumb
  • InChI Key: KXVSBTJVTUVNPM-UHFFFAOYSA-N
  • Monoisotopic Mass: 492.2179706
  • Average Mass: 493.04
DBSALT001714
Categories
UNII6X9OC3H4II
CAS number53179-11-6
WeightAverage: 477.038
Monoisotopic: 476.223056017
Chemical FormulaC29H33ClN2O2
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylpiperidine
  • Phenylacetamide
  • Phenylpropylamine
  • Aralkylamine
  • Halobenzene
  • Chlorobenzene
  • Piperidine
  • N-acyl-amine
  • Aryl halide
  • Aryl chloride
  • Tertiary carboxylic acid amide
  • Tertiary alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor 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.
PharmacodynamicsLoperamide 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 actionIn 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.
Related Articles
AbsorptionNot significantly absorbed from the gut
Volume of distributionNot Available
Protein binding97%
Metabolism

Hepatic

Route of eliminationExcretion of the unchanged loperamide and its metabolites mainly occurs through the feces.
Half life9.1 to 14.4 hours (average 10.8 hours)
ClearanceNot Available
ToxicityOral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9878
Blood Brain Barrier+0.7709
Caco-2 permeable+0.5875
P-glycoprotein substrateSubstrate0.7476
P-glycoprotein inhibitor IInhibitor0.8277
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterInhibitor0.5059
CYP450 2C9 substrateNon-substrate0.8057
CYP450 2D6 substrateNon-substrate0.5315
CYP450 3A4 substrateSubstrate0.7918
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9154
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9207
Ames testNon AMES toxic0.768
CarcinogenicityNon-carcinogens0.8564
BiodegradationNot ready biodegradable0.9953
Rat acute toxicity3.6560 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9461
hERG inhibition (predictor II)Inhibitor0.7639
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Mcneil consumer healthcare
  • Mcneil pediatrics
  • Janssen pharmaceutica products lp
Packagers
Dosage forms
FormRouteStrength
Capsule, liquid filledoral2 mg/1
Tabletoral2 mg/1
Solutionoral.2 mg
Liquidoral1 mg/5mL
Solutionoral1 mg/5mL
Tablet, film coatedoral2 mg/1
Suspensionoral1 mg/7.5mL
Solutionoral1 mg/7.5mL
Tablet, coatedoral2 mg/1
Solutionoral2 mg
Tabletoral
Tablet (chewable)oral
Capsuleoral2 mg
Liquidoral.2 mg
Capsuleoral2 mg/1
Liquidoral1 mg/7.5mL
Solutionoral2 mg/10mL
Tabletoral2 mg
Solutionoral0.2 mg
Prices
Unit descriptionCostUnit
Loperamide hcl powder26.01USD g
Loperamide HCl 2 mg capsule0.64USD capsule
Imodium a-d 2 mg caplet0.49USD caplet
Imodium advanced caplet0.46USD caplet
Imodium ms relief caplet0.46USD caplet
Kaopectate 262 mg caplet0.37USD caplet
Loperamide 2 mg caplet0.37USD caplet
Qc anti-diarrheal adv caplet0.3USD caplet
Diamode 2 mg tablet0.28USD tablet
Kaopectate 240 mg softgel0.25USD softgel capsule
Anti-diarrheal 2 mg caplet0.18USD caplet
CVS Pharmacy anti-diarrheal 2 mg caplet0.14USD caplet
Kaopectate children's suspension0.02USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2134611 No2002-12-242014-10-28Canada
US6103260 No1997-07-172017-07-17Us
US6814978 No2001-08-262021-08-26Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point222.1U.S. Patent 3,714,159; 3,884,916.
water solubilitySlightNot Available
logP5.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00086 mg/mLALOGPS
logP4.44ALOGPS
logP4.77ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)13.96ChemAxon
pKa (Strongest Basic)9.41ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area43.78 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity139.32 m3·mol-1ChemAxon
Polarizability52.67 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)splash10-004i-0000900000-673950710672b433271cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)splash10-014i-0090000000-4b7b347a8b8e9dca406cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)splash10-02t9-0090000000-31f15df976e23e73330aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Positivesplash10-004i-0000900000-d91d13c4e4665bd5fb5aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Positivesplash10-004i-0020900000-f1be3181a6918c985ffdView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Positivesplash10-014i-0090000000-e5e41346303f41f65688View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Positivesplash10-014i-0090000000-acd8b87c1338e5d0fe25View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Positivesplash10-014i-0090000000-81b85f788d14641430fdView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-014i-0090000000-3ce1a89454d777268799View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-03di-0090000000-f101d63ad0bf8e5d2178View in MoNA
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

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

US20110159058
General ReferencesNot Available
External Links
ATC CodesA07DA03A07DA05A07DA53
AHFS Codes
  • 56:08.00
PDB EntriesNot Available
FDA labelDownload (55.5 KB)
MSDSDownload (73.8 KB)
Interactions
Drug Interactions
Drug
LumacaftorThe serum concentration of Loperamide can be decreased when it is combined with Lumacaftor.
RamosetronLoperamide may increase the activities of Ramosetron.
RanolazineThe serum concentration of Loperamide can be increased when it is combined with Ranolazine.
SaquinavirThe serum concentration of Loperamide can be increased when it is combined with Saquinavir.
TesmilifeneThe serum concentration of Loperamide can be decreased when it is combined with Tesmilifene.
VerapamilThe serum concentration of Loperamide can be increased when it is combined with Verapamil.
Food Interactions
  • Take without regard to meals. Increase liquid intake.

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. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed:10087042 ]
  2. Tan-No K, Niijima F, Nakagawasai O, Sato T, Satoh S, Tadano T: Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. Eur J Pharm Sci. 2003 Nov;20(3):357-63. [PubMed:14592702 ]
  3. Roge J, Baumer P, Berard H, Schwartz JC, Lecomte JM: The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide. Scand J Gastroenterol. 1993 Apr;28(4):352-4. [PubMed:8488368 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  5. Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E: Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. [PubMed:6319884 ]
  6. di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O: Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors. Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12. [PubMed:18284554 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40368.235 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Giagnoni G, Casiraghi L, Senini R, Revel L, Parolaro D, Sala M, Gori E: Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. [PubMed:6319884 ]
  3. di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O: Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors. Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12. [PubMed:18284554 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 Da
References
  1. DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed:10087042 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1A gives rise to P and/or Q-type calcium currents. P/Q-type calcium channels belong to...
Gene Name:
CACNA1A
Uniprot ID:
O00555
Molecular Weight:
282362.39 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Church J, Fletcher EJ, Abdel-Hamid K, MacDonald JF: Loperamide blocks high-voltage-activated calcium channels and N-methyl-D-aspartate-evoked responses in rat and mouse cultured hippocampal pyramidal neurons. Mol Pharmacol. 1994 Apr;45(4):747-57. [PubMed:8183255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
modulator
General Function:
Type 4 melanocortin receptor binding
Specific Function:
ACTH stimulates the adrenal glands to release cortisol.MSH (melanocyte-stimulating hormone) increases the pigmentation of skin by increasing melanin production in melanocytes.Beta-endorphin and Met-enkephalin are endogenous opiates.
Gene Name:
POMC
Uniprot ID:
P01189
Molecular Weight:
29423.72 Da
References
  1. Nomura A, Iwasaki Y, Aoki Y, Yamamori E, Mutsuga N, Yoshida M, Asai M, Oiso Y, Saito H: Effects of loperamide and other opioid-related substances on the transcriptional regulation of the rat pro-opiomelanocortin gene in AtT20 cells. Neuroendocrinology. 2001 Aug;74(2):87-94. [PubMed:11474216 ]
  2. Auernhammer CJ, Stalla GK, Lange M, Pfeiffer A, Muller OA: Effects of loperamide on the human hypothalamo-pituitary-adrenal axis in vivo and in vitro. J Clin Endocrinol Metab. 1992 Aug;75(2):552-7. [PubMed:1322429 ]
  3. Ambrosi B, Bochicchio D, Ferrario R, Colombo P, Faglia G: Effects of the opiate agonist loperamide on pituitary-adrenal function in patients with suspected hypercortisolism. J Endocrinol Invest. 1989 Jan;12(1):31-5. [PubMed:2545766 ]
  4. Ambrosi B, Bochicchio D, Colombo P, Ferrario R, Faglia G: Loperamide modifies but does not block the corticotropin-releasing hormone-induced ACTH response in patients with Addison's disease. Horm Metab Res Suppl. 1987;16:74-5. [PubMed:2832297 ]
  5. Bochicchio D, Ambrosi B, Faglia G: Loperamide, an opiate analog, differently modifies the adrenocorticotropin responses to corticotropin-releasing hormone and lysine vasopressin in patients with Addison's disease. Neuroendocrinology. 1988 Dec;48(6):611-4. [PubMed:2855105 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Titin binding
Specific Function:
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 Da
References
  1. Daly JW, Harper J: Loperamide: novel effects on capacitative calcium influx. Cell Mol Life Sci. 2000 Jan 20;57(1):149-57. [PubMed:10949586 ]
  2. Suzuki T, Sakai H, Ikari A, Takeguchi N: Inhibition of thromboxane A(2)-induced Cl(-) secretion by antidiarrhea drug loperamide in isolated rat colon. J Pharmacol Exp Ther. 2000 Oct;295(1):233-8. [PubMed:10991984 ]
  3. Mellstrand T: Loperamide--an opiate receptor agonist with gastrointestinal motility effects. Scand J Gastroenterol Suppl. 1987;130:65-6. [PubMed:2820051 ]
  4. Stoll R, Ruppin H, Domschke W: Calmodulin-mediated effects of loperamide on chloride transport by brush border membrane vesicles from human ileum. Gastroenterology. 1988 Jul;95(1):69-76. [PubMed:2836258 ]
  5. Diener M, Knobloch SF, Rummel W: Action of loperamide on neuronally mediated and Ca2+- or cAMP-mediated secretion in rat colon. Eur J Pharmacol. 1988 Aug 2;152(3):217-25. [PubMed:2851449 ]

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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Baker DE: Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8. [PubMed:18192961 ]
  2. Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Kim KA, Chung J, Jung DH, Park JY: Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81. Epub 2004 Sep 8. [PubMed:15365656 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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
Molecular Weight:
141477.255 Da
References
  1. Wandel C, Kim R, Wood M, Wood A: Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. Anesthesiology. 2002 Apr;96(4):913-20. [PubMed:11964599 ]
  2. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684 ]
  3. Schinkel AH, Wagenaar E, Mol CA, van Deemter L: P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest. 1996 Jun 1;97(11):2517-24. [PubMed:8647944 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on July 29, 2016 01:52