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
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
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. |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
PERA SYRUP 2MG/5ML | N/A | N/A | N/A | 4/3/1995 | |
SANPO CAP 2MG | N/A | N/A | N/A | 4/17/2002 | |
TEDIUM CAP 2MG | N/A | N/A | N/A | 3/15/2008 | |
HAWKPERMIDE TAB 2MG | N/A | N/A | N/A | 10/14/2007 | |
WILLIPO LOPERAMIDE HYDROCHLORIDE TABLETS 2MG | N/A | N/A | N/A | 2/7/2022 | |
VACONTIL TAB 2MG | N/A | N/A | N/A | 3/20/1998 | |
LIDERIUM CAP 2MG | N/A | N/A | N/A | 11/12/1982 |
TGA Drug Approvals
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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