Loperamide (Tablets, Capsules) Instructions for Use

ATC Code

A07DA03 (Loperamide)

Active Substance

Loperamide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Symptomatic antidiarrheal drug

Pharmacotherapeutic Group

Antidiarrheal agent

Pharmacological Action

By binding to opioid receptors in the intestinal wall (stimulation of cholinergic and adrenergic neurons via guanine nucleotides), it reduces the tone and motility of the intestinal smooth muscle, slows the passage of intestinal contents, and reduces the secretion of fluid and electrolytes in the feces.

It increases the tone of the anal sphincter, promotes fecal retention, and reduces the urge to defecate.

The effect begins quickly and lasts for 4-6 hours.

Pharmacokinetics

Absorption is 40%.

Plasma protein binding (primarily to albumin) is 97%.

The half-life is 9-14 hours.

It poorly penetrates the blood-brain barrier.

It is almost completely metabolized in the liver by conjugation.

It is excreted primarily through the intestines, with a small portion via the kidneys (in the form of conjugated metabolites).

Indications

• Symptomatic treatment of acute (allergic, emotional, drug-induced, radiation) and chronic (in irritable bowel syndrome) diarrhea;
• Regulation of stool in patients with an ileostomy.

As an auxiliary medicinal product:

• Diarrhea of infectious origin.

ICD codes

Dosage Regimen

Tablets

For adults with acute diarrhea, the first dose is 4 mg, then 2 mg after each bowel movement in case of loose stools.

For chronic diarrhea, the first dose is 2 mg, and the maintenance dose is adjusted so that the stool frequency is 1-2 times per day (2-12 mg/day).

The maximum daily dose for adults is 12 mg.

For children aged 4-8 years: 1 mg 3-4 times/day for 3 days; 9-12 years: 2 mg 4 times/day for 5 days.

Capsules

Orally.

For adultswith acute and chronic diarrhea, 2 capsules (4 mg) are prescribed orally, then 1 capsule (2 mg) after each bowel movement in case of loose stools.

For chronic diarrhea, the dose is subsequently adjusted so that the stool frequency is 1-2 times/day, which is usually achieved with a maintenance dose of 2-4 capsules (4-8 mg/day).

The maximum daily dose is 8 capsules (16 mg). If there is no effect after taking 16 mg/day for 10 days, continuation of administration is not advisable.

For children over 6 years old, 1 capsule (2 mg) is prescribed after each bowel movement in case of loose stools. The maximum daily dose is 3 capsules (6 mg).

After stool normalization or if no stool occurs for 12 hours, treatment with loperamide should be discontinued.

For patients with renal failure, as well as elderly patients, no dosage regimen adjustment is required.

Adverse Reactions

Allergic reactions skin rash, itching, angioedema, in some cases – erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

From the digestive system dryness of the oral mucosa, abdominal pain or discomfort, nausea, vomiting, constipation, flatulence, intestinal colic, in some cases – intestinal obstruction.

From the CNS and peripheral nervous system fatigue, drowsiness, dizziness.

Other urinary retention.

Contraindications

• Hypersensitivity to the drug;
• Diverticulosis;
• Intestinal obstruction;
• Ulcerative colitis in the acute stage;
• Diarrhea due to acute pseudomembranous enterocolitis;
• Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• Pregnancy (first trimester);
• Lactation period;
• Loperamide in capsules is not prescribed to children under 6 years of age;
• As monotherapy – dysentery and other gastrointestinal infections.

With caution: hepatic insufficiency.

Use in Pregnancy and Lactation

Contraindicated during pregnancy (first trimester) and during lactation.

Use in Hepatic Impairment

With caution: hepatic insufficiency.

Use in Renal Impairment

For patients with renal failure, no dosage regimen adjustment is required.

Pediatric Use

Loperamide in capsules is not prescribed to children under 6 years of age.

For children over 6 years old, 1 capsule (2 mg) is prescribed after each bowel movement in case of loose stools. The maximum daily dose is 3 capsules (6 mg).

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Geriatric Use

For elderly patients, no dosage regimen adjustment is required.

Special Precautions

If there is no effect after 2 days of using loperamide, it is necessary to consult a doctor.

If constipation or flatulence develops during treatment, Loperamide should be discontinued.

In patients with impaired liver function, careful monitoring for signs of toxic CNS damage (stupor, impaired coordination of movements, drowsiness, miosis, muscle hypertonia, respiratory depression, increased fatigue, drowsiness, dizziness) is necessary.

Treatment with loperamide does not replace the correction of water-electrolyte balance that develops with diarrhea.

During the treatment of diarrhea (especially in children), it is necessary to replenish the loss of fluid and electrolytes.

Dehydration may contribute to a change in the response to Loperamide.

In some cases, in AIDS patients with infectious colitis of both viral and bacterial nature, toxic dilation of the colon may develop during treatment with loperamide.

Effect on ability to drive vehicles and operate machinery

During the treatment period, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms depression of the central nervous system (stupor, impaired coordination, drowsiness, miosis, muscular hypertension, respiratory depression, intestinal obstruction.

Treatment antidote – naloxone; considering that the duration of action of loperamide is longer than that of naloxone, repeated administration of the latter is possible.

Symptomatic treatment: activated charcoal, gastric lavage, artificial lung ventilation.

Medical observation is necessary for at least 48 hours.

Drug Interactions

Concomitant administration of loperamide (at a dose of 16 mg) with P-glycoprotein inhibitor drugs (quinidine, ritonavir) leads to a 2-3-fold increase in the plasma concentration of loperamide.

P-glycoprotein inhibitors may enhance the effect of loperamide on the CNS.

With the simultaneous use of 16 mg of loperamide and 600 mg of saquinavir, Loperamide reduces the clinical efficacy of saquinavir.

Storage Conditions

Store out of reach of children, in a dry, light-protected place, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

Over-the-counter.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.