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Loperamide

Generic Name
Loperamide
Brand Names
Diamode, Imodium, Imodium Multi-symptom Relief
Drug Type
Small Molecule
Chemical Formula
C29H33ClN2O2
CAS Number
53179-11-6
Unique Ingredient Identifier
6X9OC3H4II

Overview

Loperamide is an anti-diarrheal agent that is available as various over-the-counter products for treating diarrhea. The drug was first synthesized in 1969 and used medically in 1976. It is a highly lipophilic synthetic phenylpiperidine opioid that is structurally similar to opiate receptor agonists such as diphenoxylate and haloperidol. Due to pharmacological properties, loperamide has been misused and abused to self-manage opioid withdrawal symptoms and to induce euphoria. However, loperamide is associated with a risk for experiencing a range of adverse effects, often life-threatening, if taking for non-therapeutic reasons or at doses higher than the recommended dose.

Indication

Loperamide is indicated for the relief of diarrhea, including Travelers’ Diarrhea. As an off-label use, it is often used to manage chemotherapy-related diarrhea.

Associated Conditions

  • Diarrhea
  • Traveler's Diarrhea

Research Report

Published: Aug 7, 2025

Loperamide (DB00836): A Comprehensive Pharmacological and Clinical Monograph

Section 1: Drug Identification and Physicochemical Properties

This section establishes the fundamental identity of loperamide, providing the necessary chemical, physical, and historical context for the subsequent pharmacological and clinical analysis.

1.1 Nomenclature and Identifiers

Loperamide is a synthetic small molecule drug identified across global databases by a standardized set of names and codes.[1] Its formal chemical name, as designated by the International Union of Pure and Applied Chemistry (IUPAC), is 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide.[1] The primary identifier for this chemical entity in the Chemical Abstracts Service (CAS) registry is the number 53179-11-6, which refers to the loperamide base.[1] The hydrochloride salt, the form in which the drug is most commonly manufactured and administered, is identified by the related CAS number 34552-83-5.[1]

In major drug and chemical databases, loperamide is cataloged under the DrugBank accession number DB00836, the PubChem Compound ID (CID) 3955, the ChEMBL ID CHEMBL841, and the FDA's Unique Ingredient Identifier (UNII) 6X9OC3H4II.[1] Its widespread use is reflected in a variety of synonyms and international nonproprietary names, including Loperamida (Spanish) and Lopéramide (French).[1] Commercially, it is best known by the brand name Imodium® but is marketed globally under numerous other trade names, such as Imodium A-D®, Kaopectate II®, and Pepto® Diarrhea Control, underscoring its status as a ubiquitous over-the-counter (OTC) medication.[1]

Table 1: Loperamide Chemical and Database Identifiers

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2024/05/22
Not Applicable
Recruiting
2023/01/10
Phase 4
Recruiting
Henry M. Jackson Foundation for the Advancement of Military Medicine
2022/09/06
Phase 1
Recruiting
2022/08/30
Phase 2
Active, not recruiting
MedSIR
2022/02/23
Phase 1
Completed
2022/02/23
Phase 2
Active, not recruiting
2021/03/30
Phase 1
Completed
Centre de recherche du Centre hospitalier universitaire de Sherbrooke
2021/02/03
Phase 2
UNKNOWN
2020/04/29
Phase 2
Completed
2020/03/19
Phase 1
Completed

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Wal-Mart Stores Inc
49035-695
ORAL
1 mg in 7.5 mL
6/19/2025
American Health Packaging
60687-229
ORAL
2 mg in 1 1
2/16/2024
Bryant Ranch Prepack
71335-2061
ORAL
2 mg in 1 1
5/24/2023
Physicians Total Care, Inc.
54868-2118
ORAL
2 mg in 1 1
9/18/2012
Amerisource Bergen
46122-620
ORAL
2 mg in 1 1
4/8/2025
REMEDYREPACK INC.
70518-3413
ORAL
2 mg in 1 1
1/10/2024
allphamed Pharbil Arzneimittel GmbH
60468-005
ORAL
2 mg in 1 1
2/22/2023
A-S Medication Solutions
50090-6208
ORAL
2 mg in 1 1
10/7/2021
NuCare Pharmaceuticals,Inc.
68071-2257
ORAL
2 mg in 1 1
1/20/2022
STAT Rx USA LLC
16590-423
ORAL
2 mg in 1 1
10/12/2012

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
IMODIUM CAPSULE 2 mg
SIN06212P
CAPSULE
2 mg
5/8/1991
COLODIUM CAPSULE 2 mg
SIN08031P
CAPSULE
2.00MG
2/23/1995
DIATROL SYRUP 1 mg/5 ml
SIN05600P
SYRUP
1 mg/5 ml
3/27/1991
ABYDIUM CAPSULES 2MG
SIN16450P
CAPSULE
2.00 mg
3/24/2022
DIATROL CAPSULE 2 mg
SIN07107P
CAPSULE
2 mg
7/10/1992
LORAMIDE CAPSULE 2 mg
SIN09217P
CAPSULE
2 mg
2/20/1997
LOPERAX CAPSULE 2 mg
SIN05595P
CAPSULE
2 mg
3/27/1991
LOPERAMIL TABLET 2 mg
SIN07812P
TABLET, FILM COATED
2 mg
8/1/1994
LORPA SYRUP 1mg/5ml
SIN06525P
SYRUP
1.05 mg/5 ml
8/29/1991
ELDOPER CAPSULE 2 mg
SIN09601P
CAPSULE
2 mg
1/6/1998

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

Health Canada Drug Approvals

Approved Product
Company
DIN
Dosage Form
Strength
Market Date
DOM-LOPERAMIDE HYDROCHLORIDE SOLUTION-ORL
dominion pharmacal
02138301
Solution - Oral
.2 MG / ML
12/31/1995
RHOXAL-LOPERAMIDE
rhoxalpharma inc
02233998
Tablet - Oral
2 MG / TAB
12/2/1997
LOPERAMIDE-2
PRO DOC LIMITEE
02225182
Tablet - Oral
2 MG
11/5/1997
JAMP LOPERAMIDE
02544989
Capsule - Oral
2 MG
3/14/2025
DIARR-EZE
02229552
Tablet - Oral
2 MG
2/18/1997
PMS-LOPERAMIDE HYDROCHLORIDE SOLUTION.2MG/ML
02016095
Solution - Oral
0.2 MG / ML
12/31/1993
IMODIUM COMPLETE
mcneil consumer healthcare division of johnson & johnson inc
02245185
Tablet - Oral
2 MG
6/20/2002
LOPERAMIDE
d.c. labs limited
02244262
Tablet - Oral
2 MG
7/6/2001
DIAHALT CAPLETS - 2MG
wampole brands, a division of pangeo pharma (canada) inc.
02219484
Tablet - Oral
2 MG
4/11/1997
PHL-LOPERAMIDE
pharmel inc
02298198
Tablet - Oral
2 MG
8/13/2007

CIMA AEMPS Drug Approvals

Approved Product
Company
Registration Number
Pharmaceutical Form
Prescription Type
Status
FORTASEC FLAS 2 mg LIOFILIZADO ORAL
Jntl Consumer Health (Spain) S.L.
65349
LIOFILIZADO ORAL
Sin Receta
Commercialized
FORTASEC FLAS 2 MG LIOFILIZADO ORAL
Mcneil Healthcare (Ireland) Limited
9091
LIOFILIZADO ORAL
Sin Receta
Not Commercialized

Philippines FDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product
Company
Registration Number
Dosage Form
Strength
Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name
MA Holder
MA Number
Pharmaceutical Form
Active Ingredient
Authorization Date
No UK EMC drug information found for this drug.

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