LOPERAMIDE HYDROCHLORIDE

First approved in 1976

Details

Stereochemistry	ACHIRAL
Molecular Formula	C29H33ClN2O2.ClH
Molecular Weight	513.498
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CN(C)C(=O)C(CCN1CCC(O)(CC1)C2=CC=C(Cl)C=C2)(C3=CC=CC=C3)C4=CC=CC=C4

InChI

InChIKey=PGYPOBZJRVSMDS-UHFFFAOYSA-N

InChI=1S/C29H33ClN2O2.ClH/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;1H

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C29H33ClN2O2
Molecular Weight	477.038
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.fda.gov/Drugs/DrugSafety/ucm504673.htm | https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/22671931

Loperamide is a commonly used over-the-counter (OTC) and prescription medicine that is approved to help control symptoms of diarrhea, including Travelers’ Diarrhea. The maximum approved daily dose for adults is 8 mg per day for OTC use and 16 mg per day for prescription use. It is sold under the OTC brand name Imodium A-D, as store brands, and as generics. In vitro and animal studies show that IMODIUM® (loperamide hydrochloride) acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing propulsive peristalsis, and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter, thereby reducing incontinence and urgency. 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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mu opioid receptor 221 Target ID: CHEMBL233 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/15454210 \| https://www.ncbi.nlm.nih.gov/pubmed/10087042	Agonist 2662		0.53 nM [Ki]
Delta opioid receptor 78 Target ID: CHEMBL236 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/15456245	Agonist 2662		156.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Diarrhea 35 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf	Primary		Approved 8360	IMODIUM A-D Approved Use Use controls symptoms of diarrhea, including Travelers'Diarrhea Launch Date 2.20579201E11

C_max

Value	Dose	Co-administered	Analyte	Population
2.24 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/438356	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:		LOPERAMIDE blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
26.1 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/438356	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:		LOPERAMIDE blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
11.2 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/438356	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:		LOPERAMIDE blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf052lbl.pdf	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:		LOPERAMIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
5% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf052lbl.pdf	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:		LOPERAMIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
400 mg 2 times / day multiple, oral Overdose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25935922	unhealthy, 26 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 26 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25935922	Disc. AE: Cardiac arrest... AEs leading to discontinuation/dose reduction: Cardiac arrest (grade 5) Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25935922
792 mg 1 times / day multiple, oral (total daily dose) Overdose Dose: 792 mg, 1 times / day Route: oral Route: multiple Dose: 792 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954	unhealthy, 28 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 28 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954	Disc. AE: Syncope, Tachycardia... AEs leading to discontinuation/dose reduction: Syncope Tachycardia Electrocardiogram QTc interval prolonged Cardiac arrest Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954
400 mg 1 times / day multiple, oral Overdose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442	unhealthy, 30 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 30 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442	Disc. AE: Syncope, Cardiac arrest... AEs leading to discontinuation/dose reduction: Syncope Cardiac arrest Torsades de pointes Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442
16 mg 8 times / day multiple, oral (total daily dose) Recommended Dose: 16 mg, 8 times / day Route: oral Route: multiple Dose: 16 mg, 8 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3	unhealthy Health Status: unhealthy Condition: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3	Disc. AE: Torsades de pointes, Cardiac arrest... AEs leading to discontinuation/dose reduction: Torsades de pointes Cardiac arrest Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3
16 mg 8 times / day multiple, oral (total daily dose) Recommended Dose: 16 mg, 8 times / day Route: oral Route: multiple Dose: 16 mg, 8 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3	unhealthy Health Status: unhealthy Condition: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3	Disc. AE: Ventricular tachycardia, Syncope... AEs leading to discontinuation/dose reduction: Ventricular tachycardia Syncope Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3

AEs

AE	Significance	Dose	Population
Cardiac arrest	grade 5 Disc. AE	400 mg 2 times / day multiple, oral Overdose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25935922	unhealthy, 26 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 26 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25935922
Cardiac arrest	Disc. AE	792 mg 1 times / day multiple, oral (total daily dose) Overdose Dose: 792 mg, 1 times / day Route: oral Route: multiple Dose: 792 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954	unhealthy, 28 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 28 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954
Electrocardiogram QTc interval prolonged	Disc. AE	792 mg 1 times / day multiple, oral (total daily dose) Overdose Dose: 792 mg, 1 times / day Route: oral Route: multiple Dose: 792 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954	unhealthy, 28 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 28 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954
Syncope	Disc. AE	792 mg 1 times / day multiple, oral (total daily dose) Overdose Dose: 792 mg, 1 times / day Route: oral Route: multiple Dose: 792 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954	unhealthy, 28 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 28 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954
Tachycardia	Disc. AE	792 mg 1 times / day multiple, oral (total daily dose) Overdose Dose: 792 mg, 1 times / day Route: oral Route: multiple Dose: 792 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954	unhealthy, 28 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 28 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/25345436 Page: p.954
Cardiac arrest	Disc. AE	400 mg 1 times / day multiple, oral Overdose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442	unhealthy, 30 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 30 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442
Syncope	Disc. AE	400 mg 1 times / day multiple, oral Overdose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442	unhealthy, 30 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 30 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442
Torsades de pointes	Disc. AE	400 mg 1 times / day multiple, oral Overdose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442	unhealthy, 30 n = 1 Health Status: unhealthy Condition: Opiate abuse Age Group: 30 Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28506439 https://pubmed.ncbi.nlm.nih.gov/25817442
Cardiac arrest	Disc. AE	16 mg 8 times / day multiple, oral (total daily dose) Recommended Dose: 16 mg, 8 times / day Route: oral Route: multiple Dose: 16 mg, 8 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3	unhealthy Health Status: unhealthy Condition: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3
Torsades de pointes	Disc. AE	16 mg 8 times / day multiple, oral (total daily dose) Recommended Dose: 16 mg, 8 times / day Route: oral Route: multiple Dose: 16 mg, 8 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3	unhealthy Health Status: unhealthy Condition: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.1, 3
Syncope	Disc. AE	16 mg 8 times / day multiple, oral (total daily dose) Recommended Dose: 16 mg, 8 times / day Route: oral Route: multiple Dose: 16 mg, 8 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3	unhealthy Health Status: unhealthy Condition: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3
Ventricular tachycardia	Disc. AE	16 mg 8 times / day multiple, oral (total daily dose) Recommended Dose: 16 mg, 8 times / day Route: oral Route: multiple Dose: 16 mg, 8 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3	unhealthy Health Status: unhealthy Condition: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017690s005lbl.pdf Page: p.3

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709 inhibitor 1579		substrate 1193	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	CYP2C8 688 CYP2B6 660 P-gp 1527

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1909	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/16415122/ Page: 1.0	strong [IC50 0.05 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2B6 660	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf#page=2 Page: 2.0	minor
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf#page=2 Page: 2.0	minor
P-gp 1527	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/17962372/	yes
CYP2C8 688	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf#page=2 Page: 2.0	yes	yes (co-administration study) Comment: single 4-mg dose of loperamide hydrochloride was co-administered with 600 mg gemfibrozil, a strong inhibitor of CYP2C8, on day 3 of a 5-day treatment with gemfibrozil twice daily, the mean peak plasma concentration and the systemic exposure to loperamide was increased by 1.6-fold and 2.2-fold, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf#page=2 Page: 2.0
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf#page=2 Page: 2.0	yes	yes (co-administration study) Comment: Concomitant administration of multiple doses of 100 mg itraconazole twice daily, an inhibitor of both CYP3A4, with a single 4-mg dose of loperamide hydrochloride increased the peak plasma concentration and the systemic exposure to loperamide by 2.9-fold and 3.8-fold, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017694s052lbl.pdf#page=2 Page: 2.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.sciencedirect.com/science/article/pii/S2405500X16302614

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:6532	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:6532
ChemicalBook	CB7402928	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7402928
ZINC	ZINC000000537928	http://zinc15.docking.org/substances/ZINC000000537928
eMolecules	902064	https://www.emolecules.com/cgi-bin/more?vid=902064

PubMed

Title	Date	PubMed
Herbal medicines as a factor in delirium.	1999 Jul	10402626
Effect of the 5-hydroxytryptamine3 (5-HT3)-receptor antagonist KB-R6933 on experimental diarrhea models.	1999 May	10446763
Acute abstinence syndrome following abrupt cessation of long-term use of tramadol (Ultram): a case study.	2000	10985875
Interactions between herbal medicines and prescribed drugs: a systematic review.	2001	11772128
Therapeutic response to octreotide in patients with refractory CPT-11 induced diarrhea.	2001	11561696
Effects of brewer's yeast cell wall on constipation and defecation in experimentally constipated rats.	2001 Apr	11388452
Recent concepts in fecal incontinence.	2001 Aug	12112954
Increase of opioid mu-receptor gene expression in streptozotocin-induced diabetic rats.	2001 Aug	11544560
Effects of loperamide and other opioid-related substances on the transcriptional regulation of the rat pro-opiomelanocortin gene in AtT20 cells.	2001 Aug	11474216
Effects of yogurt supplemented with brewer's yeast cell wall on constipation and intestinal microflora in rats.	2001 Dec	11922109
Peripheral and preemptive opioid antinociception in a mouse visceral pain model.	2001 Jan	11166478
Oral glutamine in the prevention of fluorouracil induced intestinal toxicity: a double blind, placebo controlled, randomised trial.	2001 Jan	11115819
Sulfated polysaccharides, but not cellulose, increase colonic mucus in rats with loperamide-induced constipation.	2001 Jul	11478500
A scintigraphic study to investigate the potential for altered gut distribution of loperamide from a loperamide-simethicone formulation in man.	2001 Jul	11408151
Optimal dosing of ofloxacin with loperamide in the treatment of non-dysenteric travelers' diarrhea.	2001 Jul-Aug	11703897
[Travelers' diarrhea].	2001 Jun	11441697
Control of irinotecan-induced diarrhea by octreotide after loperamide failure.	2001 Jun	11430421
Guidelines for adults on self-medication for the treatment of acute diarrhoea.	2001 Jun	11380315
Ritonavir increases loperamide plasma concentrations without evidence for P-glycoprotein involvement.	2001 Nov	11719726
Traveler's diarrhea.	2001 Sep	11586551
Clinical evaluation and management of acute infectious diarrhea in adults.	2001 Sep	11586547
Loperamide-induced enhancement of moxidectin availability in cattle.	2002 Apr	12000531
Urinary retention with loperamide.	2002 Apr	11987317
Irinotecan in relapsed or refractory non-Hodgkin's lymphomas. Indications of activity in a phase II trial.	2002 Aug	12199630
Determination of the active ingredient loperamide hydrochloride in pharmaceutical caplets by high performance thin layer chromatography with ultraviolet absorption densitometry of fluorescence quenched zones.	2002 Jan-Feb	12026106
Irritable bowel syndrome: update on pathogenesis and management.	2002 Jan-Mar	12116690
Irritable bowel syndrome neuropharmacology. A review of approved and investigational compounds.	2002 Jul	12184141
Acute gastroenteritis in children.	2002 Jun	12230646
A multinational comparison of racecadotril and loperamide in the treatment of acute watery diarrhoea in adults.	2002 Jun	12126242
Laxative and anti-diarrheal activity of polycarbophil in mice and rats.	2002 Jun	12120755
Fumagillin treatment of intestinal microsporidiosis.	2002 Jun 20	12075057
Spreading depression: imaging and blockade in the rat neocortical brain slice.	2002 Nov	12424306
Phase I study of docetaxel in combination with cyclophosphamide as first-line chemotherapy for metastatic breast cancer.	2002 Nov 4	12402144
Efficacy of prophylactic anti-diarrhoeal treatment in patients receiving Campto for advanced colorectal cancer.	2002 Nov-Dec	12552984
Antipruritic and antihyperalgesic actions of loperamide and analogs.	2002 Oct 25	12383884
Irinotecan, cisplatin and mitomycin in inoperable gastro-oesophageal and pancreatic cancers - a new active regimen.	2002 Oct 7	12373598
[Taking charge of adult's anal incontinence].	2002 Sep	12422473
[Travellers' acute diarrhea].	2002 Sep	12422471
Antidiarrhoeal activity of seed extract of Albizzia lebbeck Benth.	2002 Sep	12237809
Effect of loperamide on gastro-oesophageal reflux.	2003 Apr	12739704
Antidiarrhoeal activity of hot water extract of black tea (Camellia sinensis).	2003 Apr	12722145
Cost of illness in the 1993 waterborne Cryptosporidium outbreak, Milwaukee, Wisconsin.	2003 Apr	12702221
Irinotecan plus raltitrexed vs raltitrexed alone in patients with gemcitabine-pretreated advanced pancreatic adenocarcinoma.	2003 Apr 22	12698181
[Ileus after the use of loperamide in a child with acute diarrhea].	2003 Apr 5	12712653
Racecadotril versus loperamide: antidiarrheal research revisited.	2003 Feb	12643598
Lack of opioid or dopaminergic effects on unconditioned sexual incentive motivation in male rats.	2003 Feb	12619908
Travellers' diarrhoea.	2003 Feb	12615374
Evaluation of different calorimetric methods to determine the glass transition temperature and molecular mobility below T(g) for amorphous drugs.	2003 Jun 18	12787632
EORTC Early Clinical Studies Group early phase II trial of S-1 in patients with advanced or metastatic colorectal cancer.	2003 Mar 10	12659110
Suspicion of microscopic colitis raised by sonographic examination.	2003 May	12692829

Patents

Sample Use Guides

In Vivo Use Guide

Usual Adult Dose for Diarrhea - Acute Tablets, capsules, and liquid: Initial: 4 mg orally after the first loose stool, then Maintenance: 2 mg after each loose stool, not to exceed 16 mg in any 24-hour period. Clinical improvement is usually observed within 48 hours. Chewable tablets: Initial: 4 mg after the first loose stool, then Maintenance: 2 mg after each subsequent loose stool, but not exceeding 8 mg in 24 hours. Usual Adult Dose for Diarrhea - Chronic Tablets, capsules, and liquid: Initial: 4 mg orally once followed by 2 mg orally after each loose stool, not to exceed 16 mg in any 24-hour period. Maintenance: The average daily maintenance dosage is 4 to 8 mg. Clinical improvement is usually observed within 10 days. If clinical improvement is not observed at a maximum dosage of 16 mg for duration of 10 days, symptoms are unlikely to be controlled by further administration.

Route of Administration: Oral

In Vitro Use Guide

Loperamide caused a concentration-dependent inhibition of the ascending contractile reflex response in the rat ileum with an IC(50) of 1.4x10(-7)M

Substance Class	Chemical Created by `admin` on `Wed Jul 05 23:04:18 UTC 2023` Edited by `admin` on `Wed Jul 05 23:04:18 UTC 2023`
Record UNII	77TI35393C
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LOPERAMIDE HYDROCHLORIDE

Official Name

English

LOPERAMIDE HYDROCHLORIDE [USP-RS]

Common Name

English

LOPERAMIDE HYDROCHLORIDE COMPONENT OF IMODIUM MULTI-SYMPTOM RELIEF

Common Name

English

R 18,553

Code

English

LOPERAMIDE HYDROCHLORIDE [USP MONOGRAPH]

Common Name

English

LOPERAMIDE HYDROCHLORIDE [EP MONOGRAPH]

Common Name

English

1-PIPERIDINEBUTANAMIDE, 4-(4-CHLOROPHENYL)-4-HYDROXY-N,N-DIMETHYL-.ALPHA.,.ALPHA.-DIPHENYL-, MONOHYDROCHLORIDE

Common Name

English

LOPERAMIDE HYDROCHLORIDE [MI]

Common Name

English

LOPERAMIDE HYDROCHLORIDE [VANDF]

Common Name

English

LOPERAMIDI HYDROCHLORIDUM [WHO-IP LATIN]

Common Name

English

R-18553

Code

English

LOPERAMIDE HYDROCHLORIDE [MART.]

Common Name

English

LOPERAMIDE HYDROCHLORIDE [WHO-IP]

Common Name

English

LOPERAMIDE HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

LOPERAMIDE HCL

Common Name

English

NSC-696356

Code

English

LOPERAMIDE HYDROCHLORIDE [USAN]

Common Name

English

Loperamide hydrochloride [WHO-DD]

Common Name

English

LOPERAMIDE HYDROCHLORIDE [EP IMPURITY]

Common Name

English

4-(P-CHLOROPHENYL)-4-HYDROXY-N,N-DIMETHYL-.ALPHA.,.ALPHA.-DIPHENYL-1-PIPERIDINEBUTYRAMIDE MONOHYDROCHLORIDE

Common Name

English

LOPERAMIDE HYDROCHLORIDE [JAN]

Common Name

English

IMODIUM

Brand Name

English

IMODIUM MULTI-SYMPTOM RELIEF COMPONENT LOPERAMIDE HYDROCHLORIDE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C266