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Loperamide: Pediatric drug information

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

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
ALERT: US Boxed Warning
Torsades de pointes and sudden death

Cases of torsades de pointes, cardiac arrest, and death have been reported with the use of a higher than recommended dosage of loperamide.

Loperamide is contraindicated in pediatric patients <2 years of age.

Avoid dosages higher than recommended in adults and pediatric patients ≥2 years due to the risk of serious cardiac adverse reactions.

Brand Names: US
  • Anti-Diarrheal [OTC];
  • Diamode [OTC];
  • FT Anti-Diarrheal [OTC];
  • Imodium A-D [OTC]
Therapeutic Category
  • Antidiarrheal
Dosing: Pediatric
Diarrhea, acute

Diarrhea, acute: Note: Loperamide is not recommended for management of infectious diarrhea in pediatric patients (Devadason 2020; IDSA [Shane 2017]). For patients who are small for chronological age, consider dosing according to weight range and not by age group. Use lowest effective dose for shortest duration.

Children 2 to <12 years:

2 to 5 years weighing 13 to <21 kg: Oral: Initial: 1 mg with first loose stool followed by 1 mg/dose after each subsequent loose stool; maximum daily dose: 3 mg/day.

6 to 8 years weighing 21 to 27 kg: Oral: Initial: 2 mg with first loose stool followed by 1 mg/dose after each subsequent loose stool; maximum daily dose: 4 mg/day.

9 to 11 years weighing 27.1 to 43 kg: Oral: Initial: 2 mg with first loose stool followed by 1 mg/dose after each subsequent loose stool; maximum daily dose: 6 mg/day.

Children ≥12 years and Adolescents: Oral: Initial: 4 mg with first loose stool followed by 2 mg/dose after each subsequent loose stool; maximum daily dose: 8 mg/day.

Diarrhea, chronic; secondary to intestinal failure, short-bowel syndrome, or other noninfectious causes

Diarrhea, chronic; secondary to intestinal failure, short-bowel syndrome, or other noninfectious causes: Limited data available; dosing regimens variable: Note: Monitor patients closely for cardiac/respiratory adverse effects and dehydration. Dosage forms without sorbitol or alcohol are preferred in these patients (Ching 2007).

Infants ≥2 months and Children: Oral: 0.08 to 0.24 mg/kg/day in divided doses every 8 to 12 hours; maximum dose: 2 mg/dose (Buts 1975; Ching 2007). Dosing based on clinical experience and a case series of 10 pediatric patients (age range: 2 to 52 months) (Buts 1975; Ching 2007). In a case series of 6 infants and young children, higher dosing was described: Initial: 1 to 1.5 mg/kg/day in 4 divided doses, with subsequent dose decreased as stool output and diet tolerance improved and patient weight increased. Reported final dose range of 0.25 to 0.5 mg/kg/day in 2 divided doses was used long-term until patient achieved target weight and dietary goals; reported duration of therapy: 6 months to ~2 years (Sandhu 1983).

Irinotecan-induced diarrhea

Irinotecan-induced (delayed) diarrhea: Limited data available; consult individual protocols; some organizations have used the following:

Fixed dosing (Children's Oncology Group 2009; Pediatric Oncology Group of Ontario 2021):

Children ≥2 years and Adolescents:

<13 kg: Initial: 0.5 mg after the first loose bowel movement, followed by 0.5 mg every 3 hours while awake; during the night, may administer every 4 hours; maximum daily dose: 4 mg/day.

13 kg to <20 kg: Initial: 1 mg after the first loose bowel movement, followed by 1 mg every 4 hours; maximum daily dose: 6 mg/day.

20 kg to <30 kg: Initial: 2 mg after the first loose bowel movement, followed by 1 mg every 3 hours while awake; during the night, may administer 2 mg every 4 hours; maximum daily dose: 8 mg/day.

30 kg to <43 kg: Initial: 2 mg after the first loose bowel movement, followed by 1 mg every 2 hours while awake; during the night, may administer 2 mg every 4 hours; maximum daily dose: 12 mg/day.

≥43 kg: Initial: 4 mg after the first loose bowel movement, followed by 2 mg every 4 hours; maximum daily dose: 16 mg/day.

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

Altered kidney function: Children ≥2 years: Oral:

Mild to severe impairment: No dosage adjustment necessary.

Hemodialysis, intermittent: Unlikely to be dialyzed (highly protein bound).

Peritoneal dialysis: Unlikely to be dialyzed (highly protein bound).

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer labeling. Due to possible effects on first-pass metabolism, use with caution and monitor closely for signs of CNS toxicity.

Dosing: Adult

(For additional information see "Loperamide: Drug information")

Diarrhea, acute

Diarrhea, acute (including Travelers' diarrhea):

Note: In patients with known or suspected dysentery (eg, fever ≥38.3°C [101°F] and bloody or mucoid stools), some experts consider use of loperamide with close monitoring as long as antibiotics are also given (ACG [Riddle 2016]; IDSA [Hill 2006]; LaRocque 2022). Although often avoided in patients with Clostridioides difficile infection, some experts consider use of loperamide with close monitoring as an adjunct to antibiotic therapy if such patients have major fluid losses and no ileus or colonic distention (IDSA/SHEA [McDonald 2018]; Kelly 2021).

Oral: Initial: 4 mg, followed by 2 mg after each loose stool; maximum: 16 mg/day (OTC: 8 mg/day). Limit use to ≤48 hours (ACG [Riddle 2016]; manufacturer's labeling).

Diarrhea, cancer treatment-induced

Diarrhea, cancer treatment-induced (off-label use): Oral: Initial: 4 mg, followed by 2 mg every 2 to 4 hours or after each loose stool; for diarrhea persisting >24 hours, administer 2 mg every 2 hours (or 4 mg every 4 hours). Continue until 12 hours have passed without a loose bowel movement (Andreyev 2014; Benson 2004; Sharma 2005). Note: Doses >16 mg/day may not provide benefit; consider alternative therapy for diarrhea persisting ≥48 hours (Andreyev 2014; Benson 2004).

Neratinib-induced diarrhea, prophylaxis: Oral: 4 mg 3 times daily (days 1 to 14 of neratinib therapy), followed by 4 mg twice daily (days 15 to 56 of neratinib therapy), followed by 4 mg as needed up to a maximum of 16 mg/day (days 57 to 365 of neratinib therapy) (Nerlynx prescribing information). Note: Antidiarrheal prophylaxis is recommended during the first 56 days of neratinib therapy; initiate with the first neratinib dose. After day 56, titrate dose to achieve 1 to 2 bowel movements/day. Additional antidiarrheal medication may be required for loperamide-refractory diarrhea.

Irinotecan-induced delayed diarrhea: Oral: 4 mg after first loose stool or first sign of frequent bowel movements, then 2 mg every 2 hours (4 mg every 4 hours at night) until 12 hours have passed without a loose bowel movement (Rothenberg 1996; Sharma 2005).

Diarrhea, chronic

Diarrhea, chronic:

Oral: Initial: 4 mg, followed by 2 mg after each loose stool; maximum: 16 mg/day (manufacturer's labeling). Note: Doses >16 mg/day (eg, up to 40 to 64 mg/day) may be required in some cases (eg, short bowel syndrome). Experience with doses >16 mg/day is generally limited to observational data in specialized centers with close monitoring (DiBaise 2021; Hollington 2004; Mackowski 2015).

Maintenance dosage: Once diarrhea is controlled, use lowest dosage required to control symptoms; usual maintenance dose: 4 to 8 mg/day as a single dose or in divided doses (eg, 2 mg before meals) (Wald 2021; manufacturer's labeling). If clinical improvement is not observed after ≥10 days of maximally tolerated dosage, symptoms are unlikely to be controlled by further administration. Note: In patients with irritable bowel syndrome with alternating diarrhea and constipation, treatment should be limited to short courses as needed (Wald 2021; manufacturer's labeling).

Enterocutaneous fistula or ileostomy, high-output

Enterocutaneous fistula (off-label use) or ileostomy (labeled use), high-output:

Note: Avoid use of liquid formulations; propylene glycol content may increase output (de Vries 2017; Parli 2018).

Initial:

Enterocutaneous fistula: Oral: 4 mg administered 3 to 4 times per day (Parli 2018; Stein 2021).

Ileostomy: Oral: 2 mg administered 2 to 3 times per day (Landmann 2022; Parli 2018).

Dosage adjustment: May increase dose in 2 mg/day increments if fistula output remains elevated (maximum: 16 mg/day) (Parli 2018; manufacturer's labeling). Note: Doses >16 mg/day may be required in refractory cases. Experience with doses >16 mg/day is generally limited to observational data in specialized centers with close monitoring (de Vries 2017; Hollington 2004; Mackowski 2015; Parli 2018).

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

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Altered kidney function: Mild to severe impairment: No dosage adjustment necessary (manufacturer's labeling).

Hemodialysis, intermittent (thrice weekly): Unlikely to be dialyzed (highly protein bound): No supplemental dose or dosage adjustment necessary (expert opinion).

Peritoneal dialysis: Unlikely to be dialyzed (highly protein bound): No dosage adjustment necessary (expert opinion).

CRRT: No dosage adjustment necessary (expert opinion).

PIRRT (eg, sustained, low-efficiency diafiltration): No dosage adjustment necessary (expert opinion).

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; use with caution.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Central nervous system: Dizziness (1%)

Gastrointestinal: Constipation (2% to 5%), abdominal cramps (≤3%), nausea (≤3%)

<1%, postmarketing, and/or case reports: Abdominal discomfort, abdominal distention, abdominal pain, anaphylactic shock, anaphylactoid reaction, angioedema, bullous rash (rare), drowsiness, dyspepsia, erythema multiforme (rare), fatigue, flatulence, hypersensitivity reaction, megacolon, paralytic ileus, pruritus, skin rash, Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare), toxic megacolon, urinary retention, urticaria, vomiting, xerostomia

Contraindications

Hypersensitivity to loperamide or any component of the formulation; abdominal pain without diarrhea; children <2 years; acute dysentery; acute ulcerative colitis; bacterial enterocolitis (caused by Salmonella, Shigella, and Campylobacter); pseudomembranous colitis associated with broad-spectrum antibiotic use.

Canadian labeling: Additional contraindications (not in the US labeling): When constipation should be avoided; when the inhibition of peristalsis should be avoided

OTC labeling: When used for self-medication, do not use if stool is bloody or black.

Warnings/Precautions

Concerns related to adverse effects:

• Allergic reactions: Rare cases of anaphylaxis and anaphylactic shock have been reported.

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

• GI effects: Discontinue promptly if constipation, abdominal pain, abdominal distension, blood in stool, or ileus develop. Do not use when peristalsis inhibition should be avoided due to potential for ileus, megacolon and/or toxic megacolon.

• Torsades de pointes and sudden death: [US Boxed Warning]: Cases of torsades de pointes, cardiac arrest, and death have been reported with the use of a higher than recommended dosage. Contraindicated in pediatric patients <2 years. Avoid dosages higher than recommended in patients ≥2 years due to the risk of serious cardiac adverse reactions. Cases of syncope and ventricular tachycardia have been reported in adults receiving the recommended dose of loperamide. Cases of cardiac arrest, syncope, and respiratory depression have been reported in pediatric patients <2 years. Avoid use in patients with risk factors for QT prolongation (eg, congenital long QT syndrome, history of cardiac arrhythmias or other cardiac conditions, elderly, electrolyte abnormalities) and in combination with others drugs known to prolong the QT interval.

Disease-related concerns:

• AIDS: Stop therapy at the first sign of abdominal distention; cases of toxic megacolon have occurred in patients with AIDS and infectious colitis (due to viral or bacterial pathogens).

• Hepatic impairment: Use with caution in patients with hepatic impairment due to reduced first-pass metabolism; monitor for signs of CNS toxicity.

Special populations:

• Older adult: Use with caution in elderly patients; may be more susceptible to drug-associated effects on the QT interval.

• Pediatric: OTC use is contraindicated in patients <2 years of age due to risks of respiratory depression or cardiac adverse events. Response to loperamide may be variable in pediatric patients due to increased risk of dehydration secondary to diarrhea; use with caution.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.

Other warnings/precautions:

• Appropriate use: Loperamide is a symptom-directed treatment; if an underlying diagnosis is made, other disease-specific treatment may be indicated. Concurrent fluid and electrolyte replacement is often necessary in all age groups depending upon severity of diarrhea.

• Duration of use: If diarrhea lasts longer than 2 days, symptoms worsen, or abdominal swelling or bulging develops, discontinue use and consult healthcare provider.

• Self medication (OTC use): Consult health care provider prior to using, if taking antibiotics, if pregnant or breastfeeding, or in the presence of fever, mucus in stool, or a history of liver disease. Serious heart problems may occur if taken more than directed.

Warnings: Additional Pediatric Considerations

When managing acute dysentery, concurrent fluid and electrolyte replacement is often necessary in all age groups depending upon severity of diarrhea; young pediatric patients are particularly susceptible to dehydration and electrolyte imbalances. Antidiarrheal agents are not recommended as part of the management of acute gastroenteritis in infants and children due to risk of serious adverse events (CDC 2003; Red Book [AAP 2021]). A meta-analysis evaluating the use of loperamide for adjunct treatment of acute bacterial gastroenteritis in pediatric patients identified that infants and children who are <3 years of age, malnourished, or moderately to severely dehydrated, or those with bloody diarrhea have a higher risk of serious adverse events (ileus, lethargy, death) even at therapeutic doses (≤0.25 mg/kg/day of loperamide); the potential benefit of loperamide therapy does not outweigh risks; use should be avoided in pediatric patients (IDSA [Shane 2017]; Li 2007). Although data suggest that older children with milder infection and adolescents may see benefit from loperamide therapy, including decreased duration of diarrhea and stool counts, use is not recommended (IDSA [Shane 2017]); if used, patients should be monitored closely for adverse effects or worsening of infection (CDC 2003; Li 2007).

Although OTC use is contraindicated in ages <2 years, loperamide may be necessary in young pediatric patients with intestinal failure or short-bowel syndrome (Buts 1975; Ching 2007; Sandhu 1983). Response to loperamide may be variable in pediatric patients due to increased risk of dehydration secondary to diarrhea; use with caution and monitor for adverse effects.

Some dosage forms may contain propylene glycol; in neonates, large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule, Oral, as hydrochloride:

FT Anti-Diarrheal: 2 mg [contains fd&c blue #1 (brilliant blue), peg-40 hydrog castor oil(cremophor rh40)]

Imodium A-D: 2 mg [contains fd&c blue #1 (brilliant blue), peg-40 hydrog castor oil(cremophor rh40)]

Generic: 2 mg

Solution, Oral, as hydrochloride:

FT Anti-Diarrheal: 1 mg/7.5 mL (120 mL) [contains fd&c blue #1 (brilliant blue), propylene glycol, quinoline yellow (d&c yellow #10), sodium benzoate; mint flavor]

Imodium A-D: 1 mg/7.5 mL (120 mL, 240 mL) [contains fd&c blue #1 (brilliant blue), propylene glycol, quinoline yellow (d&c yellow #10), sodium benzoate]

Imodium A-D: 1 mg/7.5 mL (120 mL, 240 mL) [contains fd&c blue #1 (brilliant blue), propylene glycol, quinoline yellow (d&c yellow #10), sodium benzoate; mint flavor]

Generic: 1 mg/7.5 mL (120 mL)

Tablet, Oral, as hydrochloride:

Anti-Diarrheal: 2 mg [scored]

Anti-Diarrheal: 2 mg [DSC] [contains corn starch, fd&c blue #1 (brill blue) aluminum lake, quinoline (d&c yellow #10) aluminum lake]

Anti-Diarrheal: 2 mg [scored; contains corn starch, fd&c blue #1 (brill blue) aluminum lake, quinoline (d&c yellow #10) aluminum lake]

Anti-Diarrheal: 2 mg [contains fd&c blue #1 (brill blue) aluminum lake, quinoline yellow (d&c yellow #10)]

Anti-Diarrheal: 2 mg [contains fd&c blue #1 (brilliant blue), quinoline yellow (d&c yellow #10)]

Diamode: 2 mg [scored; contains fd&c blue #1 (brill blue) aluminum lake, quinoline (d&c yellow #10) aluminum lake]

FT Anti-Diarrheal: 2 mg [scored; gluten free; contains fd&c blue #1 (brill blue) aluminum lake, quinoline (d&c yellow #10) aluminum lake]

Imodium A-D: 2 mg [DSC]

Imodium A-D: 2 mg [scored]

Generic: 2 mg

Generic Equivalent Available: US

Yes

Pricing: US

Capsules (Imodium A-D Oral)

2 mg (per each): $0.59

Capsules (Loperamide HCl Oral)

2 mg (per each): $0.13 - $1.37

Solution (Imodium A-D Oral)

1 mg/7.5 mL (per mL): $0.05

Solution (Loperamide HCl Oral)

1 mg/7.5 mL (per mL): $0.04

Tablets (Imodium A-D Oral)

2 mg (per each): $0.53

Tablets (Loperamide HCl Oral)

2 mg (per each): $0.07 - $0.12

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: Pediatric

Oral: Drink plenty of fluids to help prevent dehydration.

Oral solution: Shake well before administering dose.

Administration: Adult

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

Oral solution: Shake well before administering dose.

Cancer treatment-induced diarrhea: Consider administering 30 minutes prior to eating 4 times daily to slow gastrocolic reflex (Andreyev 2014).

Storage/Stability

Store between 20°C and 25°C (68°F and 77°F).

Use

Prescription products: Treatment of acute nonspecific diarrhea (FDA approved in ages ≥2 years and adults); treatment of chronic diarrhea associated with inflammatory bowel disease and reduction of ileostomy discharge volume (FDA approved in adults); has also been used for chronic diarrhea due to multiple causes, including short-bowel syndrome, organic lesions, idiopathic (functional diarrhea), and late-onset irinotecan-induced.

OTC products: Control symptoms of diarrhea, including traveler's diarrhea (FDA approved in ages ≥6 years and adults).

Medication Safety Issues
Sound-alike/look-alike issues:

Imodium A-D may be confused with Indocin

Loperamide may be confused with furosemide, Lomotil

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]).

International issues:

Indiaral [France] may be confused with Inderal and Inderal LA brand names for propranolol [US, Canada, and multiple international markets]

Lomotil: Brand name for loperamide [Mexico, Philippines], but also the brand name for diphenoxylate [US, Canada, and multiple international markets]

Lomotil [Mexico, Philippines] may be confused with Ludiomil brand name for maprotiline [multiple international markets]

Metabolism/Transport Effects

Substrate of CYP2B6 (minor), CYP2C8 (minor), CYP2D6 (minor), CYP3A4 (minor), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

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

Dietary Considerations

Some products may contain sodium.

Pregnancy Considerations

Adverse effects have not been observed in animal reproduction studies. Information related to loperamide use in pregnancy is limited and data are conflicting (Einarson 2000; Källén 2008). For acute diarrhea in pregnant women, some clinicians recommend oral rehydration and dietary changes; loperamide in small amounts may be used only if symptoms are disabling (Wald 2003).

Monitoring Parameters

Stool output, CNS toxicity assessment, respiratory and cardiac status (particularly in very young pediatric patients).

Mechanism of Action

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

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Poor.

Distribution: Poor penetration into brain.

Protein binding: ~95%.

Metabolism: Hepatic via oxidative N-demethylation; CYP2C8 and CYP3A4 (major) and CYP2B6 and CYP2D6 (minor) role in N-demethylation.

Half-life elimination: 9.1 to 14.4 hours.

Time to peak, plasma: Liquid: 2.5 hours; Capsule: ~5 hours.

Excretion: Feces.

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

  • (AE) United Arab Emirates: Imodium | Lomidex | Lopodium;
  • (AR) Argentina: Colifilm | Contem | Custey | Dotalsec | Elcoman | Espaven sec | Excelentia antidiarreico | Fada loperamida | Ionet | Lanseka | Lefa Enteril L | Loperamida | Loperamida cevallos | Loperamida fabra | Loperamida ilab | Loperamida vannier | Loperix | Lovopren | Minicam | Nodiar | Normasec | Plexol | Plorinoc | Regulane | Regulane cb | Suprasec | Viltar;
  • (AT) Austria: Enterobene | Imodium | Imosec | Loperamid | Loperamid sandoz;
  • (AU) Australia: Amcal Anti Diarrh | Apohealth diarrhoea relief | Blooms the chemist diarrhoea relief | Chemists own diarrhoea relief | Cm diarrhoea rlf | Diarrhoea Relief | Gastrex | Gastro lieve | Gastrostop | Harmonise | Imodium | Lopedium | Lorrex | O/n diarrhoea rel | Pharmacy care anti diarrhoea | Soul pattinson diarrhoea | Tw diarrhoea rlf;
  • (BD) Bangladesh: Dirocap | Dirolin | Imotil | Lomid | Lomosec | Lopamid | Lopan | Loper | Loperin | Loperodium | Nomotil;
  • (BE) Belgium: Ercestop | Imodium | Imodium aktuapharma | Loperamide Eurogenerics | Loperamide merck-generics | Loperamide Mylan | Loperamide Ratiopharm | Loperamide sandoz | Loperamide teva generics belgium | Toriac;
  • (BF) Burkina Faso: Diarloc | Loperamide;
  • (BG) Bulgaria: Diarostad | Imodium | Imomed | Lopedium | Loperamid | Vacontil;
  • (BR) Brazil: Cloridrato de loperamida | Closecs | Diafuran | Diarresec | Diasec | Disteran | Enterocler | Enterosec | Imosec | Intestin | Kaosec | Loperamida | Loperin | Magnostase | Obstar;
  • (CH) Switzerland: Amavita loperamid | Binaldan nouvelle formule | Imodium | Loperamid | Loperamid HelvePharm | Loperamid sandoz | Loperamid spirig hc | Loperamid streuli | Loperamid zentiva | Loperamid-mepha | Sun store loperamid;
  • (CI) Côte d'Ivoire: Adco loperamide | Creatimo | Diarloc | Diarum | Loperamide denk | Loperium;
  • (CL) Chile: Capent | Coliper | Lopediar | Loperamida | Salvacoll | Sikim;
  • (CN) China: Fu xie ding | Imodium | Loperamide | Lopermide | Yi meng ting;
  • (CO) Colombia: Adbriotico | Diarmicin | Imodium | Loperamida | Loperamida clorhidrato | Loperamida MK | Novadiar | Pangetan nf | Plenterox | Sindiar | Stomalix;
  • (CZ) Czech Republic: Imodium | Lopacut | Loperamid dr.max | Loperamide aurovitas | Loperon;
  • (DE) Germany: Azuperamid | Boxolip | D-stop | Duralopid | Endialop | Endiaron l | Imodium | Imodium akut | Imodium n | Lop | Lop dia | Lopa hemopharm | Lopacut | Lopalind | Lopedium | Lopepham | Lopera | Loperamerck | Loperamid | Loperamid AbZ akut | Loperamid akut | Loperamid al | Loperamid Aristo | Loperamid axicur | Loperamid Elac | Loperamid puren | Loperamid sandoz | Loperamide heumann | Loperhoe | Loperhoe akut | Lopetrans | Sanifug;
  • (DK) Denmark: Imolope;
  • (DO) Dominican Republic: Alka ad | Diarrexanol | Imodium | Lopefar | Lopemida | Loperamida | Loperamida Denk | Loperil | Lopirin | Peristal | Prodom;
  • (EC) Ecuador: Imodium | Lopediar | Loperamida MK | Loperamide | Loridin | Novalop | Velaral;
  • (EE) Estonia: Imodium | Lopacut | Lopedium | Lopedium express | Loperamid | Loperamidum-ratiopharm | Vacontil;
  • (EG) Egypt: Imodium | Loperasin | Lopodium | Motijust | Sedomid;
  • (ES) Spain: Diarfin | Elissan | Fortasec | Imodium | Imosec | Loperamida belmac | Loperamida inkey | Loperamida rimafar | Loperan | Loperkey | Taguinol;
  • (ET) Ethiopia: Vacontil;
  • (FI) Finland: Imocur | Imodium | Imodium orion | Lopacut | Lopex;
  • (FR) France: Altocel | Antidiar | Delalande diarrhee | Diaretyl cooper | Dysentec | Dyspagon | Ercestop | Gastrowell Loperamide | Imodium | Imodiumliquicaps | Imossel | Indiaral | Lodiarid | Lopelin | Loperamide | Loperamide Almus | Loperamide arrow | Loperamide biogaran | Loperamide cristers | Loperamide evolugen | Loperamide g gam | Loperamide gifrer | Loperamide gnr | Loperamide hexal | Loperamide ivax | Loperamide Lyoc | Loperamide merck | Loperamide Phr | Loperamide Qualimed | Loperamide Ratiopharm | Loperamide ratiopharm conseil | Loperamide rpg | Loperamide sandoz | Loperamide teva | Loperamide zydus | Loperium | Nabutil | Nimaz | Peracel;
  • (GB) United Kingdom: Arret | Diafix | Diah limit | Diaquitte | Diareze | Diarid | Diarrhoea Relief | Diasorb | Diocalm | Diocalm ultra | Diocaps | Dioraleze | Entrocalm | Imodium | Imodium IBS Relief | Imodium jan | Lodiar | Loperagen | Loperamide | Loperamide Almus | Loperamide cox | Loperamide Galpharm | Loperamide kent | Loperamide sandoz | Loritax | Norimode | Normaloe;
  • (GH) Ghana: Eskamide;
  • (GR) Greece: Imodium | Neo enteroseptol | Neo-Septol;
  • (HK) Hong Kong: APO Loperamide | Bf-Loperamide | Colodium | Diacalm | Diacure | Diastop | Diatabs Reformulated | Eurodium | Imocon | Imodium | Imotol | Karenamide | Liderium | Lopa | Lopaine | Loper | Lopera | Loperamide | Loperamil | Loperax | Loperin | Loperium | Lopermide | Miraton | Nt diorea | Pera | Qualiper | Reximide | Sanpo | Synodium | Tedium | Undiarrhea | Uni-Motil | Vacontil | Vidaperamide;
  • (HR) Croatia: Lordiar | Seldiar;
  • (HU) Hungary: Enterobene | Huma-loperamide | Imodium | Lopacut | Lopedium | Loperacap;
  • (ID) Indonesia: Alphamid | Amerol | Antidia | Bidium | Colidium | Diadium | Diaramid | Diasec | Diastrix | Gradilex | Imodan | Imodium | Imomed | Imore | Imosa | Inamid | Lexadium | Licodium | Lodia | Lomodium | Lopamid | Loperamide | Loperil | Loremid | Mecodiar | Midix | Motilex | Normotil | Normudal | Opox | Oramide | Primodiar | Primodium | Renamid | Rhomuz | Tanitril | Tracodia | Xepare | Zeroform;
  • (IE) Ireland: Arret | Boots diarrhoea relief | Imodium;
  • (IL) Israel: Imodium | Loperid | Loperium | Rekamid | Rekamide | Shilshul X | Stopit;
  • (IN) India: Allexit | Alstop | Andial | Diarlop | Diarsec | El par | Eldoper | Imodium | Lomide | Lomin | Lopamide | Loparet | Loperam | Loperamide | Loperamide HCL | Lopipen | Lopox | Lopramide | Loramyl | Lupidium | Peeceeo | Ridol | Rokamide | Roko | Sestil ad | Starlop | Tropamide;
  • (IQ) Iraq: As entros top | Diarastop | Loperamide awa | Loprasaf | Lopratil;
  • (IT) Italy: Clarimide Diarrea | Diarstene | Diarstop | Dissenten | Dissenten antidiarrea | Imodium | Lopemid | Loperamide | Loperamide aurobindo | Loperamide doc;
  • (JO) Jordan: Imodium | Imotril | Loperium | Razentil | Vacontil;
  • (JP) Japan: Beltessa | Beltessa chemiphar | Cagudalin | Clalet | Fululondo | Fussen | Kaizac | Lonbanin | Lopecald | Lopemic | Lopemin | Lopena | Loperamide emec | Loperamide HCL | Loperan | Loperanil | Loseramin | Lospolia | Marupi geridome | Miropin | Rospolia | Signal geridome | Sparamid | Taipemin | Trot;
  • (KE) Kenya: Adco loperamide | Astodium | Dialin | Diarril | Dissenten | Eldoper | Immobulk | Immolab | Imodium | Imotil | Lomide | Lopedium | Loperamide | Lopeshal;
  • (KR) Korea, Republic of: Daeil loperamide | Daewha loperamide hcl | Gl loperamide hcl | Lamid | Lopaine | Lopamide | Lopamin | Lopera | Loperamide | Loperamide HCL | Loperi | Loperin | Lopestop | Lopidine | Lopirem | Lopmin | Lopo | Maped | Noberan | Noparon | Peramine | Rheofen | Samnam loperamide;
  • (KW) Kuwait: Imodium | Lopodium;
  • (LB) Lebanon: Imodium | Imorivo | Loperamide | Loperamide arrow | Loperium;
  • (LT) Lithuania: Diarrheel | Imodium | Imodium Original | Lopacut | Lopedium | Lopedium express | Lopedium t | Loperamid | Loperamidum wzf polfa;
  • (LU) Luxembourg: Dyspagon | Ercestop | Imodium | Lopedium | Loperamid | Loperamide Eurogenerics;
  • (LV) Latvia: Imodium | Lopacut | Lopedium | Lopedium express | Loperamid | Roko;
  • (MA) Morocco: Imodium | Loperium | Stadiar;
  • (MX) Mexico: Acanol | Acqta | Apopera | Degortkap | Deroser | Diaperol | Dilostop | Dipera | Exclefin | Hurplex | Imodium | Lomotil | Lop | Loperamida | Loperamida gi serr | Loperamida landsteiner | Lorabest | Nodiamex | Pramidal | Raxamida | Rediarin | Tac Alto | Tarmin | Valfam | Wayper;
  • (MY) Malaysia: Anpromide | Beamodium | Colodium | Diatrol | Imocap | Imodium | Imotab | Lomide | Lomodium | Loperamide | Loperax | Loperium | Lopermide | Lopex | Loramide | Modim | Primodium | Reximide | Vacontil;
  • (NG) Nigeria: Alapharm loperamide | Amakin loperamide | Diaflush | Diamotil | Diaoff | Diareasec | Diarrex | Dondiam | Lodium | Lokel's loperamide | Loperamide | Loperamide bp | Olidiacure | P one loperamide | Palomide | Phinodiom | Rgi loperamide | Sunymet loperamide | Swiperamide | Talibex loperamide | Teka loperamide | Tivapramide | Zimotil | Zukcure;
  • (NL) Netherlands: Diacure | Diarem | Diarree remmer | Diarreeremmende | Diarreeremmer htp loperamide hcl | Diarreeremmer loperamide hcl | Diarreeremmer Loperamide Hcl Ham | Idyl diarreeremmer loperamide hcl | Imodium | Jumbo diarreeremmer loperamide hcl | Livsane diarreeremmer loperamide hcl | Loperamide | Loperamide HCL | Loperamide hcl flx | Loperamide HCl Kring | Loperamide Hcl Merck | Loperamide Hcl PCH | Loperamide Hcl Sandoz | Rxt loperamide hcl | San loperamide hcl;
  • (NO) Norway: Imodium | Imodium a-d | Imodium n | Imolopera | Lopacut | Loperamid | Loperamid norfri | Salvacolina | Travello;
  • (NZ) New Zealand: APO Loperamide | Diafix | Diamide | Dicap | Gastro-stop | Imodium | Nodia | Pharmacy health diarrhoea relief;
  • (PE) Peru: Antidiarr | Desitin | Donafan | Donalab | Donamed F | Donapharm | Imodium | Lofer | Lopediar | Loperam | Loperamida | Loperamida clorhidrato | Lusafan f | Peripharm | Pevitrel | Tap forte | Tobafan forte | Toban | Toban f;
  • (PH) Philippines: Byerrhea | Chrisolop | Diamide | Diarhemide | Diarin | Diasten | Diaster | Diastop | Diatabs | Dli-loperamide hydrochloride | Harvimide | Imodium | Lbx | Lodarest | Lomotil | Loniper | Lopen | Loperamide | Loperamide Pacif | Lopran | Lopromin | Lorban | Lormide | Rodderhea | Stoform | Tgp loper | Tymedon | Vexil;
  • (PK) Pakistan: Adromide | Coliper | Diastop | Dilop | Emod | Floramex | Glodium | Hoff | Imodium | Jamide | Lomide | Lopamide | Lopedium | Lopemid | Loperam | Loperamid | Lopium | Lopramex | Lopran | Stodium | Tabromide;
  • (PL) Poland: Aurostop | Dissenten | Imodium | Laremid | Lopacut | Loper | Loperamid | Loperamid apteo med | Loperamid Dr. Max | Loperamide aurovitas | Stoperan;
  • (PR) Puerto Rico: Anti Diarrheal | Diamode | Imodium | Imodium a-d | Imodium ad | Imogen | Loperamide HCL;
  • (PT) Portugal: Diastrolib | Imodium | Loperamida | Loperamida generis | Lopitum | Loride;
  • (PY) Paraguay: Contem | Diaxin nf | Imodium | Loremid | Teramotil;
  • (QA) Qatar: Imodium | Imodium Instant;
  • (RO) Romania: Enteramid | Enterium | Imodium | Lopedium | Lopegen | Lopemidol | Loperamid | Loperamid aurobindo | Loperamid bioeel | Loperamid dr.max | Loperamid laropharm | Loprid | Tammex akut;
  • (RU) Russian Federation: Diara | Enterobene | Imodium | Lopedium | Loperamid | Loperamide | Loperamide akrikhin | Loperamide grindex | Loperamide stada | Loperamide velpharm | Neo enteroseptol | Superilop | Vero loperamid;
  • (SA) Saudi Arabia: Imodium | Lopodium | Pms-loperamide;
  • (SE) Sweden: Dimor | Imodium | Imolopera | Lopacut | Loperamid abece | Loperamid apofri | Loperamid brown | Loperamid evolan | Loperamid medical valley | Loperamid Merck NM | Loperamid Mylan | Travello;
  • (SG) Singapore: Amerol | Colodium | Diatabs | Diatrol | Eldoper | Imodium | Loperamide | Loperamil | Loperax | Loramide | Lorpa | Vacontil;
  • (SI) Slovenia: Lopacut | Seldiar;
  • (SK) Slovakia: Belopera | Imodium | Lopacut | Loperamid | Loperamid dr.max | Tammex akut;
  • (SL) Sierra Leone: Diarreashif | Weldiarrhoel;
  • (TH) Thailand: Bismadium | Bismatril | Dainox | Daiven | Diamide | Dianox | Diara | Diarent | Diarine | Diarodil | Diretrol | Diven | Entermid | Ginzadium | Hawkpermide | Himlomide | Immotab | Imodine | Imodium | Imonox | Impelium | Impore | Leomide | Limadryl | Limatril | Lodil | Lomedil | Lomide | Lopedium | Lopela | Loperamide | Loperan | Lopercin | Loperdium | Loperia | Loperil | Lopermide | Lopil | Loramide | Lorapil | Manodium | Mantril | Mecodium | Medium | Miderlar | Modim | Monamide | Nopidium | Noxzy | Operium | Patardium | Peodium | Perasian | Permid | Phihadium | Profura | Pybutil | Remytil | Ropa | Sbob | Setonox | Sumedium | Tedium | Vacontil;
  • (TN) Tunisia: Diaretyl | Idium | Imodium | Indiaral | Sediaryl;
  • (TR) Turkey: Diadef | Imodium | Lopermid;
  • (TW) Taiwan: An Lih | Antidia | Cenloper | Emodine | Emose | Fulnin | Geline | Genlatin | Gerium | Hocular | Imocon | Imode | Imodine | Imodium | Imodium a-d | Imolex | Imoli | Imomide | Imora | Imosen | Iridine | Isidium | Julilin | Ker Li | Kuzomea | Lecotin | Liaid | Licolin | Liderium | Limodium | Lipitin | Liys | Loidium | Lolilin | Lopedin | Lopedium | Lopela | Lopemic | Loper | Lopera | Loperadin | Loperadium | Loperam | Loperamide | Loperamin | Loperdin | Loperin | Loperium | Lopetin | Moledium | Mori | Peramide | Ridan | Safe | Sanpo | Ufunin | Undiarrhea | Winlipan;
  • (UA) Ukraine: Imodium | Lopedium | Loperamid | Loperamid Kmp | Loperamid Rivopharm;
  • (UG) Uganda: Astodium | Dialin | Imodium | Kamodium | Loperaren;
  • (UY) Uruguay: Corol | Fadal | Imodium | Loper | Loperamida | Loperamida athena | Pramidef;
  • (VE) Venezuela, Bolivarian Republic of: Antilax | Glucitol | Imodium | Loperam | Loperamida | Loperamida cevallos;
  • (VN) Viet Nam: Imoboston | Lopetab | Parepemic;
  • (ZA) South Africa: Adco loperamide | Betaperamide | Cipla loperamide | Gastron | Imodium | Lenide-t | Norimode | Prodium | Rolab-loperamide;
  • (ZM) Zambia: Ar pramide | Colodium | Imodium | Lomodium | Lopamet | Lopamide | Loperamide denk | Loprade | Motionil | Roko;
  • (ZW) Zimbabwe: Imodium | Lockit
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