Skip to Content

Loperamide

Pronunciation

Pronunciation

(loe PER a mide)

Index Terms

  • Loperamide HCl
  • Loperamide Hydrochloride

Dosage Forms

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

Capsule, Oral, as hydrochloride:

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

Generic: 2 mg

Liquid, Oral, as hydrochloride:

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

Imodium A-D: 1 mg/7.5 mL (30 mL [DSC], 120 mL, 240 mL, 360 mL [DSC]) [contains brilliant blue fcf (fd&c blue #1), fd&c yellow #10 (quinoline yellow), propylene glycol, sodium benzoate; mint flavor]

Generic: 1 mg/5 mL (5 mL, 10 mL, 118 mL)

Suspension, Oral, as hydrochloride:

Generic: 1 mg/7.5 mL (120 mL)

Tablet, Oral, as hydrochloride:

Anti-Diarrheal: 2 mg [DSC]

Anti-Diarrheal: 2 mg [scored]

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

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

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

Diamode: 2 mg [scored]

Imodium A-D: 2 mg [scored; contains brilliant blue fcf (fd&c blue #1), fd&c yellow #10 (quinoline yellow)]

Imodium A-D: 2 mg [scored; contains fd&c blue #1 aluminum lake, fd&c yellow #10 aluminum lake]

Loperamide A-D: 2 mg

Tablet Chewable, Oral, as hydrochloride:

Imodium A-D: 2 mg [DSC] [contains fd&c blue #1 aluminum lake, fd&c yellow #10 aluminum lake; cool mint flavor]

Brand Names: U.S.

  • Anti-Diarrheal [OTC]
  • Diamode [OTC]
  • Imodium A-D [OTC]
  • Loperamide A-D [OTC]

Pharmacologic Category

  • Antidiarrheal

Pharmacology

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

Absorption

Poor

Distribution

Poor penetration into brain

Metabolism

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

Excretion

Feces

Time to Peak

Liquid: 2.5 hours; Capsule: ~5 hours

Half-Life Elimination

9.4 to 14.4 hours

Use: Labeled Indications

Diarrhea:

Rx labeling: Control and symptomatic relief of chronic diarrhea associated with inflammatory bowel disease in adults; acute nonspecific diarrhea in patients ≥2 years; to reduce volume of ileostomy discharge

OTC labeling: Control of symptoms of diarrhea, including Traveler's diarrhea

Use: Unlabeled

Cancer treatment-induced diarrhea (eg, irinotecan induced); chronic diarrhea caused by bowel resection

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.

Documentation of allergenic cross-reactivity for antidiarrheals is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity can not be ruled out with certainty.

Dosing: Adult

Acute diarrhea: Oral: Initial: 4 mg, followed by 2 mg after each loose stool (maximum: 16 mg/day)

Chronic diarrhea: Oral: Initial: 4 mg, followed by 2 mg after each loose stool (maximum: 16 mg/day); maintenance dose should be slowly titrated downward to minimum required to control symptoms (usual: 4 to 8 mg/day as a single dose or in divided doses; maximum: 16 mg/day). If clinical improvement is not observed after at least 10 days of treatment with 16 mg/day, symptoms are unlikely to be controlled by further administration; treatment may be continued if diarrhea cannot be adequately controlled with diet or other therapy.

Traveler's diarrhea: Oral: Initial: 4 mg after first loose stool, followed by 2 mg after each subsequent stool (maximum dose: 8 mg/day)

Cancer treatment-induced diarrhea (off-label use): Oral: 4 mg followed by 2 mg every 4 hours or after each unformed stool; Maximum: 16 mg/day (Benson, 2004) or 4 mg followed by 2 mg every 2 hours (4 mg every 4 hours at night) until 12 hours have passed without a loose bowel movement (Sharma, 2005)

Irinotecan-induced delayed diarrhea (off-label use): Oral: 4 mg after first loose or frequent bowel movement, then 2 mg every 2 hours (4 mg every 4 hours at night) until 12 hours have passed without a bowel movement (Rothenberg, 1996)

Dosing: Geriatric

Refer to adult dosing; use with caution.

Dosing: Pediatric

Acute diarrhea: Oral: Children ≥2 years and Adolescents:

Initial (first 24 hours):

2 to 5 years (13 to 20 kg): 1 mg 3 times daily

6 to 8 years (20 to 30 kg): 2 mg twice daily

8 to 12 years (>30 kg): 2 mg 3 times daily

≥13 years: Refer to adult dosing

Maintenance:

2 to 5 years (13 to 20 kg): After the first 24 hours, 0.1 mg/kg/dose after each loose stool (maximum: 3 mg/day).

6 to 8 years (20 to 30 kg): After the first 24 hours, 0.1 mg/kg/dose after each loose stool (maximum: 4 mg/day).

8 to 12 years (>30 kg): After the first 24 hours, 0.1 mg/kg/dose after each loose stool (maximum: 6 mg/day).

≥13 years: Refer to adult dosing.

Traveler's diarrhea: Oral: Children ≥6 years and Adolescents:

6 to 8 years: 2 mg after first loose stool, followed by 1 mg after each subsequent stool (maximum dose: 4 mg/day)

9 to 11 years: 2 mg after first loose stool, followed by 1 mg after each subsequent stool (maximum dose: 6 mg/day)

≥12 years: Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment necessary.

Dosing: Hepatic Impairment

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

Administration

Shake liquid well before administering dose.

Dietary Considerations

Some products may contain sodium.

Storage

Store at room temperature.

Drug Interactions

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

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

Highest Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Lumacaftor: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. Lumacaftor may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

MiFEPRIStone: May enhance the QTc-prolonging effect of QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying). Management: Though the drugs listed here have uncertain QT-prolonging effects, they all have some possible association with QT prolongation and should generally be avoided when possible. Consider therapy modification

Moderate Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

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

Ranolazine: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Adverse Reactions

1% to 10%:

Central nervous system: Dizziness (1%)

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

<1% (Limited to important or life-threatening): 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

ALERT: U.S. 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.

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 patients: Stop therapy at the first sign of abdominal distention; cases of toxic megacolon have occurred in AIDS patients with 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.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

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

• Pediatric: Use with caution in young children as response may be variable because of dehydration. Contraindicated in children <2 years.

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.

Monitoring Parameters

Signs of CNS toxicity in patients with hepatic impairment.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse effects have not been observed in animal reproduction studies. Information related to loperamide use in pregnancy is limited and data is 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).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue or loss of strength and energy. Have patient report immediately to prescriber severe dizziness, passing out, tachycardia, abnormal heartbeat, severe nausea; severe vomiting; abdominal pain; constipation; abdominal edema; bloating; black, tarry, or bloody stools; urinary retention; or change in amount of urine passed (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Hide