loperamide (OTC)

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Brand and Other Names:Imodium, K-Pek II, more...NeoDiaral, Diaraid

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

liquid

  • 1mg/5mL
  • 1mg/7.5mL

suspension

  • 1mg/7.5mL

tablet

  • 2mg

capsule

  • 2mg

tablet chewable

  • 2mg
more...

Acute Diarrhea

4 mg initially, then 2 mg after each loose stool; not to exceed 16 mg/day (8 mg/day for self-medication); discontinue if no improvement seen within 48 hours

Chronic Diarrhea

4 mg initially, then 2 mg after each loose stool until controlled, and then 4-8 mg/day in divided doses

Traveler's Diarrhea

4 mg after first loose stool, then 2 mg after each subsequent stool; not to exceed 8 mg/day

Dosage Forms & Strengths

liquid

  • 1mg/5mL
  • 1mg/7.5mL

suspension

  • 1mg7.5mL

tablet

  • 2mg

capsule

  • 2mg

tablet chewable

  • 2mg
more...

Acute Diarrhea

First Day of Treatment

  • 2-6 years (13-20 kg): 1 mg q8hr PO
  • 6-8 years: (20-30 kg): 2 mg q12hr PO
  • 8-12 years (>30 kg): 2 mg q8hr PO

Second & Subsequent Doses

  • 0.1 mg/kg PO after each loose stool; not to exceed dose recommended for first 24 hours 

Chronic Diarrhea

0.08-0.24 mg/kg/day PO divided q12hr 

Traveler's Diarrhea

<6 years: Safety and efficacy not established

6-8 years: 2 mg after first loose stool, then 1 mg after each subsequent stool; not to exceed 4 mg/day

8-12 years: 2 mg after first loose stool, then 1 mg after each subsequent stool; not to exceed 6 mg/day

>12 years: 4 mg after first loose stool, then 2 mg after each subsequent stool; not to exceed 8 mg/day

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Interactions

Interaction Checker

and loperamide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Dizziness

            Fatigue

            Abdominal pain

            Constipation

            Nausea

            Dry mouth

            Angioedema

            Bullous eruptions

            Flatulence

            Rash

            Postmarketing Reports

            Pancreatitis

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            Warnings

            Contraindications

            Hypersensitivity, bloody diarrhea, high fever, infectious diarrhea, pseudomembranous colitis

            Patients in whom constipation must be avoided

            Abdominal pain without diarrhea

            Avoid use as primary therapy with acute dysentery (bloody stools and high fever, acute ulcerative colitis, bacterial enterocolitis [caused by Salmonella, Shigella, and Campylobacter), pseudomembranous colitis associated with antibiotic use)

            Age <2 years

            Cautions

            May cause drowsiness or dizziness, which may impair physical abilities to operate heavy machinery or tasks requiring mental alertness

            Hypersensitivity reactions reported, including anaphylaxis, rash, urticaria, and rare cases of Steven’s Johnson syndrome or toxic epidermal necrolysis

            Discontinue if no improvement seen within 48 hours in patients with acute diarrhea, symptoms worsen, or abdominal swelling or bulging develops

            Discontinue promptly if constipation, abdominal pain or distention, blood in stool, or ileus develops; do not use when peristalsis inhibition should be avoided (ie, due to potential for ileus, megacolon, or toxic megacolon)

            Discontinue therapy if symptoms of abdominal distention occur in patients with AIDS; cases of toxic megacolon reported with infectious colitis, resulting from viral or bacterial pathogens

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

            Use of higher than recommended doses or abuse of loperamide can result in serious cardiac adverse events, including QT interval prolongation, Torsades de Pointes, or other ventricular arrhythmias, syncope, and cardiac arrest; in cases of abuse, individuals often use other drugs together with loperamide in attempts to increase its absorption and penetration across the blood-brain barrier, inhibit loperamide metabolism, and enhance its euphoric effects

            Potential toxic dose in patients <6 years: 0.4 mg/kg  

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            Pregnancy & Lactation

            Pregnancy category: B

            Lactation: Not known if distributed in breast milk; use caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Slows intestinal motility through opioid receptor; has direct effects on circular and longitudinal muscle; reduces fecal volume; increases viscosity

            Absorption

            Bioavailability: 0.3%

            Onset: 1-3 hr

            Duration: 41 hr

            Peak plasma time: 5 hr (capsule); 2.5 hr (liquid)

            Distribution

            Poor penetration through blood-brain barrier

            Metabolism

            Significant first-pass metabolism, resulting in very low plasma level of drug

            Metabolites: Glucuronide (inactive)

            Elimination

            Elimination half-life: 7-14 hr

            Excretion: Feces (30-40%), urine (1%)

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            Images

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