What is the appropriate dosing of loperamide (Loperamide hydrochloride) for treatment?

From the Guidelines

Loperamide should be dosed at 4 mg initially, followed by 2 mg every 2-4 hours or after every unformed stool, not to exceed 16 mg per day. This dosing regimen is based on the most recent and highest quality study available, which was published in 2018 in the Annals of Oncology 1. The study provides guidelines for the treatment of diarrhea in adult cancer patients and recommends loperamide as a first-line treatment for mild to moderate diarrhea.

Key Considerations

• The initial dose of loperamide should be 4 mg, followed by 2 mg every 2-4 hours or after every unformed stool, as recommended by the 2018 study in the Annals of Oncology 1.
• The maximum daily dose of loperamide should not exceed 16 mg, as stated in the 2018 study in the Annals of Oncology 1 and supported by other studies, such as the 2004 study in the Journal of Clinical Oncology 1.
• Loperamide should be discontinued if symptoms worsen or if diarrhea persists beyond 48 hours, as recommended by the 2018 study in the Annals of Oncology 1 and other studies, such as the 2017 study in the Journal of Travel Medicine 1.
• Patients should maintain adequate hydration while taking loperamide, as the medication only addresses the symptom of diarrhea rather than the underlying cause or fluid losses, as noted in the 2018 study in the Annals of Oncology 1 and other studies, such as the 2001 study in Alimentary Pharmacology and Therapeutics 1.

Additional Guidance

• Loperamide should be avoided in cases of bloody diarrhea, high fever, or suspected bacterial infection, as it may delay pathogen clearance, as recommended by the 2018 study in the Annals of Oncology 1 and other studies, such as the 2017 study in the Journal of Travel Medicine 1.
• Other opioids, such as tincture of opium, morphine, or codeine, can be used as alternative treatments for diarrhea, as noted in the 2018 study in the Annals of Oncology 1.
• Octreotide can be used as a second-line treatment for diarrhea that is refractory to loperamide, as recommended by the 2018 study in the Annals of Oncology 1.

From the FDA Drug Label

DOSAGE AND ADMINISTRATION Loperamide hydrochloride capsules are contraindicated in pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions (see CONTRAINDICATIONS) Avoid loperamide hydrochloride capsule dosages higher than recommended in adult or pediatric patients 2 years of age and older due to the risk of serious cardiac adverse reactions (See WARNINGS, OVERDOSAGE). (1 capsule = 2 mg) Patients should receive appropriate fluid and electrolyte replacement as needed Acute Diarrhea Adults and Pediatric Patients 13 Years and Older: The recommended initial dose is 4 mg (two capsules) followed by 2 mg (one capsule) after each unformed stool. The maximum daily dose is 16 mg (eight capsules). Pediatric Patients 2 Years to 12 Years of Age: In pediatric patients 2 years to 5 years of age (20 kg or less), the non-prescription liquid formulation (Imodium A-D 1 mg/5 mL) should be used; for ages 6 to 12, either loperamide hydrochloride capsules or Imodium A-D liquid may be used For pediatric patients 2 to 12 years of age, the following schedule for capsules or liquid will usually fulfill initial dosage requirements: Recommended First Day Dosage Schedule Two to five years (13 to 20 kg): 1 mg three times daily (3 mg total daily dosage) Six to eight years (20 to 30 kg): 2 mg twice daily (4 mg total daily dosage) Eight to twelve years (greater than 30kg): 2 mg three times daily (6 mg total daily dosage) Chronic Diarrhea Adults The recommended initial dose is 4 mg (two capsules) followed by 2 mg (one capsule) after each unformed stool until diarrhea is controlled, after which the dosage of loperamide hydrochloride capsules should be reduced to meet individual requirements When the optimal daily dosage has been established, this amount may then be administered as a single dose or in divided doses. The average daily maintenance dosage in clinical trials was 4 to 8 mg (two to four capsules per day). The maximum daily dosage is 16 mg (eight capsules per day)

The dosing of loperamide is as follows:

• Acute Diarrhea:
  • Adults and pediatric patients 13 years and older: initial dose of 4 mg, followed by 2 mg after each unformed stool, with a maximum daily dose of 16 mg.
  • Pediatric patients 2 to 12 years of age:
    • 2 to 5 years: 1 mg three times daily
    • 6 to 8 years: 2 mg twice daily
    • 8 to 12 years: 2 mg three times daily
• Chronic Diarrhea:
  • Adults: initial dose of 4 mg, followed by 2 mg after each unformed stool, with a maximum daily dose of 16 mg.
  • Maintenance dosage: 4 to 8 mg per day, administered as a single dose or in divided doses. 2

From the Research

Dosing of Loperamide

• The dosing of loperamide is not explicitly stated in the provided studies, but the efficacy and safety of different doses are discussed 3.
• A study comparing two doses of loperamide oxide (1 mg and 2 mg) found that both doses were equally effective in treating acute diarrhea in adults, with the lower dose being preferred 3.
• The study also found that the median time to complete relief was 27 hours 55 minutes for the 1-mg loperamide oxide group and 25 hours for the 2-mg loperamide oxide group 3.
• Another study found that loperamide was effective in relieving symptoms of diarrhea in patients with chronic diarrhea, with an average number of stools dropping from eight to two after 1 month of treatment 4.
• The safety and efficacy of loperamide have been established in several studies, with few adverse reactions reported 5, 6.
• Loperamide is considered to be free of abuse potential and has minimal central nervous system effects due to its low oral absorption and inability to cross the blood-brain barrier 5.