Diara^® Express (Tablets) 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

Antidiarrheal agent. It reduces the tone and motility of the intestinal smooth muscles, apparently by binding to opioid receptors in the intestinal wall.

It inhibits the release of acetylcholine and prostaglandins, reducing peristalsis and increasing the transit time of intestinal contents.

It increases the tone of the anal sphincter. The effect occurs quickly and lasts for 4-6 hours.

Pharmacokinetics

After oral administration, the absorption of loperamide is about 40%, it undergoes intensive first-pass metabolism in the liver.

A small amount of unchanged loperamide enters the systemic circulation. It does not cross the blood-brain barrier.

It is metabolized in the liver.

The elimination half-life (T_1/2) is 9-14 hours. It is excreted in the bile with feces in the form of conjugated metabolites, a small part is excreted in the urine.

Indications

Symptomatic treatment of acute and chronic diarrhea of various origins (including allergic, emotional, drug-induced, radiation-induced; due to changes in diet and food composition, due to malabsorption and maldigestion; as an adjunctive agent in diarrhea of infectious origin). Regulation of bowel movements in patients with ileostomy.

ICD codes

Dosage Regimen

Tablets

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

For chronic diarrhea, the initial dose is 2 mg, 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.

Adverse Reactions

From the digestive system: abdominal pain, bloating, nausea, constipation, dry mouth.

From the central nervous system: increased fatigue, drowsiness, dizziness.

Allergic reactions: skin rash.

Contraindications

Intestinal obstruction; constipation, abdominal distension, subileus, acute dysentery (as monotherapy), acute ulcerative colitis, pseudomembranous colitis caused by the use of broad-spectrum antibiotics; children under 4 years of age, first trimester of pregnancy, hypersensitivity to loperamide.

Use in Pregnancy and Lactation

Contraindicated in the first trimester of pregnancy. In the second and third trimesters of pregnancy, Loperamide can be prescribed in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Since a small amount of loperamide is found in breast milk, use during breastfeeding is not recommended.

Use in Hepatic Impairment

Use with caution in patients with impaired liver function, with hepatic insufficiency.

Pediatric Use

Contraindicated in children under 4 years of age.

Special Precautions

Use with caution in hepatic insufficiency.

Should not be used in clinical situations where inhibition of intestinal peristalsis is required.

If there is no effect after 2 days of using loperamide, it is necessary to clarify the diagnosis and exclude an infectious origin of diarrhea.

Use with caution in patients with impaired liver function.

In case of loperamide overdose, naloxone is used as an antidote.

Drug Interactions

It is believed that concomitant use of cholestyramine may reduce the effectiveness of loperamide.

Concomitant use with co-trimoxazole, ritonavir increases the bioavailability of loperamide, which is due to inhibition of its first-pass metabolism in the liver.

In case of loperamide overdose, naloxone is used as an antidote.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

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.