KMLOPE CAPSULES

Indications

• Acute non-specific diarrhoea
• Chronic diarrhoea associated with inflammatory bowel disease
• Diarrhoea caused by chemotherapy or other medications

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing recommendations based on age and weight.

Adults: Refer to the BNF for specific adult dosing recommendations based on the condition being treated.

Mechanism of action

Lopramide exerts its effects by binding to the mu-opioid receptors in the gut wall. This action reduces gastrointestinal motility and increases the transit time of intestinal contents. It also enhances the absorption of fluids and electrolytes, contributing to the decrease in stool frequency and volume.

Pharmacodynamics

Lopramide possesses a strong affinity for peripheral opioid receptors and has minimal central nervous system penetration, which limits its potential for abuse and sedation. The drug inhibits the release of acetylcholine and prostaglandins, further reducing gastrointestinal motility and secretions. Its onset of action is typically within 1 hour, with effects lasting for several hours.

Pharmacokinetics

Lopramide is well-absorbed from the gastrointestinal tract, with peak plasma concentrations usually occurring within 5 hours after oral administration. It undergoes extensive first-pass metabolism in the liver, which reduces its bioavailability to about 0.3%. The drug is primarily excreted via the feces, with a half-life ranging from 10 to 14 hours. Renal impairment can affect its clearance, necessitating caution in such patients.

Contra-indications

• Hypersensitivity to loperamide or any of its excipients
• Acute dysentery (bloody diarrhea caused by bacteria)
• Acute ulcerative colitis
• Pseudomembranous colitis associated with the use of antibiotics
• Severe liver disease

Adverse effects

• Constipation
• Dizziness
• Fatigue
• Nausea
• Abdominal cramps
• Dry mouth
• Headache
• Somnolence

Interactions

• CNS depressants may enhance sedative effects
• Rifampicin may decrease loperamide efficacy
• Quinidine may increase loperamide plasma concentrations
• Drugs that inhibit CYP3A4 may increase loperamide levels

Precautions

• Use with caution in patients with liver impairment
• Monitor for signs of dehydration in patients with diarrhea
• Not recommended for use in children under 12 years without medical supervision
• Avoid in cases of bacterial enterocolitis

Pregnancy

Loperamide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Limited data on human use.

Breast-feeding

Loperamide is excreted in human milk, caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Capsules
• Tablets
• Oral solution