| Recommended Dose and Dosage Regimen | The recommended starting dose of loperamide for acute diarrhea in adults is usually 4 mg (two tablets) taken orally after the first loose stool, followed by 2 mg (one tablet) after each subsequent loose stool, up to a maximum of 16 mg per day. For chronic diarrhea, the initial dose may be higher, typically 4 mg (two tablets) taken orally, followed by 2 mg (one tablet) after each loose stool, up to a maximum of 8 mg per day. Dosage adjustments may be necessary based on individual response and severity of symptoms. Follow your healthcare provider’s instructions regarding dosing. |
| Frequency of Administration | Loperamide is typically administered as needed after each loose stool. |
| Route of Administration | Loperamide is administered orally in the form of tablets or oral solution. |
| Mechanism of Action (MOA) | Loperamide is a synthetic opioid agonist that acts on opioid receptors in the gastrointestinal tract, particularly the mu-opioid receptors in the intestinal wall. It slows intestinal motility and increases transit time, leading to enhanced water and electrolyte absorption and firmer stools. Loperamide also decreases fecal volume and frequency of bowel movements. |
| Pharmacokinetics (PK) | Loperamide is well absorbed after oral administration, with peak plasma concentrations achieved within 2-5 hours. It undergoes extensive first-pass metabolism in the liver to its active metabolite, desmethyl loperamide. The elimination half-life of loperamide is approximately 9-14 hours. Loperamide and its metabolites are excreted mainly in the feces. |
| Pharmacodynamics (PD) | Loperamide exerts its pharmacodynamic effects by binding to opioid receptors in the intestinal wall, inhibiting peristalsis and prolonging intestinal transit time. This results in increased absorption of water and electrolytes from the intestinal lumen, leading to reduced stool frequency and improved stool consistency. Loperamide does not cross the blood-brain barrier to a significant extent, minimizing central nervous system effects. |
| Pathophysiology | Loperamide is indicated for the symptomatic treatment of acute diarrhea and the reduction of stool frequency and volume in chronic diarrhea associated with inflammatory bowel disease (IBD), irritable bowel syndrome (IBS), or other gastrointestinal disorders. It is also used for the management of travelers’ diarrhea. |
| Primary Indications | Acute diarrhea, chronic diarrhea associated with IBD or IBS, travelers’ diarrhea. |
| Contraindications | Contraindications to loperamide use include hypersensitivity to loperamide or its components, abdominal distension without diarrhea, acute abdominal conditions (e.g., pseudomembranous colitis, bacterial enterocolitis), and acute dysentery characterized by bloody stools and fever. Use caution in patients with hepatic impairment or severe dehydration. |
| Purpose of Taking Medication | The purpose of loperamide therapy is to relieve symptoms of diarrhea by slowing intestinal motility, increasing water and electrolyte absorption, and firming stools, thereby reducing stool frequency and fluid loss. Loperamide helps restore bowel function and alleviate discomfort associated with diarrhea. |
| Usage Instructions | Take loperamide exactly as directed by your healthcare provider or as indicated on the package label. The initial dose is typically taken after the first loose stool, followed by additional doses as needed after subsequent loose stools, up to the maximum daily dose. Do not exceed the recommended dose or duration of treatment. |
| Precautions and Care | Patients taking loperamide should be advised to maintain adequate hydration and electrolyte balance, especially in cases of acute diarrhea or dehydration. Avoid excessive use of loperamide and seek medical attention if symptoms worsen or persist for more than 48 hours. Loperamide should not be used as a substitute for rehydration therapy in severe cases of diarrhea or in children under 2 years of age. |
| Dietary Considerations | There are no specific dietary restrictions associated with loperamide use. However, maintaining a balanced diet and adequate fluid intake is important for overall gastrointestinal health and hydration, especially during episodes of diarrhea. |
| Missed Dose | If a dose of loperamide is missed, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and resume your regular dosing schedule. Do not double the dose to make up for a missed one. |
| Possible Side Effects | Common side effects of loperamide may include constipation, abdominal cramps, bloating, dizziness, and drowsiness. Rare but serious side effects may include toxic megacolon, paralytic ileus, and severe allergic reactions. Prolonged or excessive use of loperamide may lead to dependence or abuse. |
| Storage and Disposal | Store loperamide tablets and oral solution at room temperature away from moisture and heat. Keep the medication out of reach of children and pets. Dispose of unused or expired medication according to local regulations. |
| Overdose or Emergency | In case of overdose or emergency, seek medical attention or contact a poison control center immediately. Symptoms of loperamide overdose may include severe constipation, ileus, urinary retention, central nervous system depression, and respiratory depression. |
| Monitoring and Laboratory Tests | Routine laboratory tests are typically not required during loperamide therapy. However, patients with chronic diarrhea should be monitored for signs of dehydration, electrolyte imbalances, and underlying gastrointestinal conditions. |
