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Loperamide and simethicone: Drug information

Loperamide and simethicone: Drug information
(For additional information see "Loperamide and simethicone: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Imodium Multi-Symptom Relief [OTC]
Brand Names: Canada
  • Imodium Advanced Multi-Symptom
Pharmacologic Category
  • Antidiarrheal;
  • Antiflatulent
Dosing: Adult
Diarrhea, acute and gas

Diarrhea, acute and gas: Oral: Two tablets after first loose stool, followed by 1 tablet with each subsequent loose stool (maximum dose: 4 tablets/24 hours)

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric
Diarrhea, acute and gas

Diarrhea, acute and gas: Note: Weight-based dosing is preferred

Children 6 to 8 years (22 to 26 kg): Oral: One tablet after first loose stool, followed by one-half tablet with each subsequent loose stool (maximum dose: 2 tablets/24 hours)

Children 9 to 11 years (27 to 43 kg): Oral: One tablet after first loose stool, followed by one-half tablet with each subsequent loose stool (maximum dose: 3 tablets/24 hours)

Children ≥12 years and Adolescents: Refer to adult dosing.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling; see individual agents.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling; see individual agents.

Adverse Reactions

See individual agents.

Contraindications

OTC labeling: When used for self-medication, do not use if you have had a rash or allergic reaction to loperamide; bloody or black stool; difficulty swallowing (non-chewable tablets).

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

Other warnings/precautions:

• Self medication (OTC use): Consult health care provider prior to using, if taking antibiotics, if pregnant or breast-feeding, or in the presence of fever, mucus in stool, or a history of liver disease. Use should be stopped and healthcare provider consulted if symptoms get worse, diarrhea persists for >2 days, or abdominal swelling or bulging occurs. Tiredness, drowsiness, or dizziness may occur; serious heart problems may occur if taken more than directed.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Caplet:

Imodium Multi-Symptom Relief: Loperamide hydrochloride 2 mg and simethicone 125 mg [contains calcium 65 mg/caplet, sodium 4 mg/caplet]

Tablet:

Imodium Multi-Symptom Relief: Loperamide hydrochloride 2 mg and simethicone 125 mg

Tablet, chewable:

Imodium Multi-Symptom Relief: Loperamide hydrochloride 2 mg and simethicone 125 mg [DSC] [contains calcium 50 mg/tablet; mint flavor]

Generic Equivalent Available: US

No

Pricing: US

Tablets (Imodium Multi-Symptom Relief Oral)

2-125 mg (per each): $0.53

Tablets (Loperamide-Simethicone Oral)

2-125 mg (per each): $0.29

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Administer with plenty of clear fluids to prevent dehydration. Administer non-chewable tablets with a full glass of water and on an empty stomach (1 hour before or 2 hours after a meal).

Administration: Pediatric

Oral: Administer with plenty of clear fluids to prevent dehydration.

Caplet: Administer non-chewable tablets with a full glass of water and on an empty stomach (1 hour before or 2 hours after a meal).

Chew tab: Chew dose and administer with water.

Use: Labeled Indications

Acute diarrhea and gas: Control of symptoms of diarrhea and gas (bloating, pressure, and cramps)

Medication Safety Issues
Pediatric patients: High-risk medication:

KIDs List: Loperamide, when used in pediatric patients <2 years of age with acute infectious diarrhea, is identified on the Key Potentially Inappropriate Drugs in Pediatrics (KIDs) list and should be avoided due to risk of ileus and lethargy (strong recommendation; high quality of evidence) (PPA [Meyers 2020]).

Metabolism/Transport Effects

Refer to individual components.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alvimopan: Loperamide may enhance the adverse/toxic effect of Alvimopan. Specifically, alvimopan gastrointestinal adverse effects may be increased. Loperamide may diminish the therapeutic effect of Alvimopan. Management: Consider avoiding coadministration of alvimopan and loperamide due to the risk of gastrointestinal adverse effects and pharmacologic antagonism. Risk D: Consider therapy modification

Desmopressin: Loperamide-Loperamide Oxide may increase the serum concentration of Desmopressin. Risk C: Monitor therapy

Eluxadoline: Loperamide-Loperamide Oxide may enhance the constipating effect of Eluxadoline. Risk C: Monitor therapy

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of Loperamide-Loperamide Oxide. Risk X: Avoid combination

Levoketoconazole: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Levoketoconazole. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

Lonafarnib: May increase the serum concentration of Loperamide. Management: When first using loperamide with lonafarnib, do not exceed a loperamide dose of 1 mg/day. If needed, the loperamide dose can then be slowly and cautiously increased according to the loperamide labeling. Risk D: Consider therapy modification

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

QuiNIDine: May enhance the CNS depressant effect of Loperamide-Loperamide Oxide. Loperamide-Loperamide Oxide may enhance the QTc-prolonging effect of QuiNIDine. QuiNIDine may increase the serum concentration of Loperamide-Loperamide Oxide. Risk C: Monitor therapy

QuiNINE: May enhance the QTc-prolonging effect of Loperamide-Loperamide Oxide. QuiNINE may increase the serum concentration of Loperamide-Loperamide Oxide. Risk C: Monitor therapy

Ramosetron: Loperamide-Loperamide Oxide may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Risk D: Consider therapy modification

Pregnancy Considerations

See individual agents.

Breastfeeding Considerations

See individual agents.

Dietary Considerations

Some products may contain sodium.

Mechanism of Action

Loperamide: Acts directly on circular and longitudinal intestinal muscles, through the opioid receptor, to inhibit peristalsis and prolong transit time; reduces fecal volume, increases viscosity, and diminishes fluid and electrolyte loss; demonstrates antisecretory activity. Loperamide increases tone on the anal sphincter.

Simethicone: Decreases the surface tension of gas bubbles thereby disperses and prevents gas pockets in the GI system.

Pharmacokinetics (Adult Data Unless Noted)

See individual agents.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Regulane af | Suprasec plus;
  • (AT) Austria: Imodium plus;
  • (AU) Australia: Anti diarrhoea plus | Apohealth Diarrhoea Relief Plus | Chemists' own diarrhoea relief plus | Gastrostop plus | Imodium Advanced | Pharmacy action diarrhoea plus gas relief | Pharmacy care anti diarrhoea plus | Pharmacy health diarrhoea relief plus | Priceline pharmacy diarrhoea relief plus;
  • (BE) Belgium: Imodium Duo;
  • (BG) Bulgaria: Imodium plus;
  • (BR) Brazil: Imodium plus;
  • (CH) Switzerland: Imodium Complex | Imodium plus;
  • (CI) Côte d'Ivoire: Diarzil;
  • (CZ) Czech Republic: Imodium plus;
  • (DE) Germany: Imodium akut complex | Imodium akut n duo;
  • (EG) Egypt: Imoflora | Motijust plust;
  • (ES) Spain: Imodium plus;
  • (ET) Ethiopia: Loflatil;
  • (FI) Finland: Lopedium comp;
  • (FR) France: Imodiumduo | Imossel duo;
  • (GB) United Kingdom: Imodium dual action relief | Imodium plus | Imodium Plus Comfort;
  • (GR) Greece: Imodium plus;
  • (HK) Hong Kong: Imodium plus;
  • (HR) Croatia: Imodium combo;
  • (HU) Hungary: Imorevin;
  • (IE) Ireland: Imodium plus;
  • (IL) Israel: Imodium plus;
  • (IN) India: Imosec-m;
  • (IT) Italy: Imodium diarrea e meteorismo | Losipaco;
  • (KE) Kenya: Loflatil;
  • (KR) Korea, Republic of: Loperin plus | Lopethicone;
  • (LT) Lithuania: Aloper;
  • (NL) Netherlands: Losimed duo;
  • (NO) Norway: Imodium Comp;
  • (NZ) New Zealand: Pharmacy health diarrhoea relief plus;
  • (PL) Poland: Imodium Multi Action | Imodium plus;
  • (PR) Puerto Rico: Imodium Advanced;
  • (PT) Portugal: Imodium plus;
  • (RU) Russian Federation: Imodium plus;
  • (SE) Sweden: Imodium plus | Imolopesim;
  • (SK) Slovakia: Imodium plus;
  • (SV) El Salvador: Intestinomicina ad+;
  • (TH) Thailand: Imodium plus;
  • (UA) Ukraine: Loflatil;
  • (UG) Uganda: Diarzil;
  • (VE) Venezuela, Bolivarian Republic of: Antilax plus;
  • (ZA) South Africa: Imodium plus
  1. Imodium Multi-Symptom Relief (loperamide hydrochloride and simethicone) chewable tablets [prescribing information]. Fort Washington, PA: McNeil Consumer Healthcare; received April 2017.
  2. Imodium Multi-Symptom Relief (loperamide hydrochloride and simethicone) caplet [prescribing information]. Fort Washington, PA: McNeil Consumer Healthcare; received March 2020.
  3. Meyers RS, Thackray J, Matson KL, et al. Key Potentially Inappropriate Drugs in Pediatrics: The KIDs List. J Pediatr Pharmacol Ther. 2020;25(3):175-191. [PubMed 32265601]
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