Usage
- Beta-Cyclodextrin + Loperamide is prescribed for the treatment of acute and chronic diarrhea.
- Pharmacological classification: Antidiarrheal (antimotility agent).
- Loperamide slows intestinal motility, while beta-cyclodextrin enhances loperamide’s solubility and stability, improving its effectiveness.
Alternate Names
- Akme-Entoquol (brand name)
How It Works
- Pharmacodynamics: Loperamide, a μ-opioid receptor agonist, reduces acetylcholine and prostaglandin release, slowing intestinal motility. This decreases peristalsis, increases fluid and electrolyte absorption, and reduces stool frequency and volume. It also increases anal sphincter tone. Beta-cyclodextrin increases loperamide solubility and bioavailability.
- Pharmacokinetics: Loperamide is well absorbed orally. It undergoes significant first-pass metabolism in the liver. Beta-cyclodextrin enhances its absorption and reduces first-pass metabolism. It’s excreted primarily through the biliary route with some renal excretion. The elimination half-life is approximately 11 hours.
- Mode of Action: Loperamide binds to μ-opioid receptors in the intestinal wall, inhibiting peristalsis.
- Elimination pathways: Primarily hepatic metabolism and biliary excretion, with some renal excretion.
Dosage
Standard Dosage
Adults:
- Acute Diarrhea: 4 mg initially, followed by 2 mg after each loose stool. Maximum daily dose: 8 mg for over-the-counter use and 16 mg for prescription use.
- Chronic Diarrhea: 2 mg twice daily, adjustable up to 16 mg/day.
Children:
- Use and dose must be determined by a doctor.
- Ages 9-11: 2 mg after the first loose stool, then 1 mg after each subsequent loose stool. Maximum 6 mg/24 hours.
- Ages 6-8: 2 mg twice daily (20-30 kg); 2 mg three times daily (>30 kg).
- Ages 2-5: 1 mg three times daily (13-20 kg).
- Not recommended for children under 2 years old.
Special Cases:
- Elderly Patients: Use with caution due to increased risk of adverse effects, especially QT prolongation. Close monitoring is essential.
- Patients with Renal Impairment: Caution advised, but dose adjustment isn’t usually required.
- Patients with Hepatic Dysfunction: Use cautiously as impaired metabolism may increase CNS side effects.
- Patients with Comorbid Conditions: Use with caution in patients with diabetes, alcohol dependence, or liver disease due to potential excipients.
Clinical Use Cases
Dosing for specific clinical scenarios like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations should be determined on a case-by-case basis by the treating physician, considering patient-specific factors.
Dosage Adjustments
Dose modifications are necessary for hepatic or renal dysfunction, metabolic disorders, or genetic polymorphisms.
Side Effects
Common Side Effects:
- Constipation
- Abdominal pain or discomfort
- Nausea
- Dizziness
- Drowsiness
Rare but Serious Side Effects:
- Toxic megacolon
- Paralytic ileus
- Cardiac arrhythmias (including QT prolongation and Torsades de Pointes)
- Hypersensitivity reactions (rash, itching, swelling)
Contraindications
- Patients under 2 years of age.
- Patients with known hypersensitivity to loperamide or any component of the formulation.
- Patients with acute dysentery (bloody stools and high fever).
- Patients with bacterial enterocolitis caused by invasive organisms, including Salmonella, Shigella, and Campylobacter.
- Patients with pseudomembranous colitis associated with broad-spectrum antibiotic use.
- Patients with intestinal obstruction.
Drug Interactions
- Drugs that inhibit or induce CYP3A4 and P-glycoprotein can alter loperamide levels.
- Concomitant use with other drugs that prolong the QT interval should be avoided.
- Cholestyramine may decrease loperamide absorption.
Pregnancy and Breastfeeding
- Pregnancy: Loperamide should be used during pregnancy only if clearly needed.
- Breastfeeding: Loperamide is excreted in breast milk. Use with caution.
Drug Profile Summary
- Mechanism of Action: μ-opioid receptor agonist, slows intestinal motility.
- Side Effects: Constipation, abdominal pain, nausea, dizziness. Rarely, cardiac arrhythmias and ileus.
- Contraindications: Age <2 years, hypersensitivity, acute dysentery, bacterial enterocolitis, pseudomembranous colitis, intestinal obstruction.
- Drug Interactions: CYP3A4 inhibitors/inducers, QT prolonging drugs, cholestyramine.
- Pregnancy & Breastfeeding: Use with caution.
- Dosage: Varies based on age, condition, and clinical response. See dosage section.
- Monitoring Parameters: Stool frequency and consistency, hydration status, electrolyte levels, cardiac function (ECG in certain cases).
Popular Combinations
No specific popular combinations noted. Combination therapy may be determined based on the cause and characteristics of the diarrhea.
Precautions
- Underlying medical conditions should be considered before use.
- Alcohol and other CNS depressants should be avoided.
- Driving and operating machinery should be avoided until effects are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Beta-Cyclodextrin + Loperamide?
A: See dosage section above for detailed information.
Q2: What is the maximum daily dose of Loperamide?
A: For adults, the maximum daily dose is 8 mg for over-the-counter use and 16 mg for prescription use.
Q3: Can Loperamide be used in children?
A: It’s not recommended for children under 2 years old. Dosing for older children should be determined by a physician.
Q4: What are the most common side effects of Loperamide?
A: Constipation, abdominal pain/discomfort, nausea, dizziness, and drowsiness.
Q5: What are the serious side effects of Loperamide?
A: Toxic megacolon, paralytic ileus, and cardiac arrhythmias, including QT prolongation and Torsades de Pointes.
Q6: Are there any drug interactions with Loperamide?
A: Yes, interactions exist with CYP3A4 inhibitors/inducers, QT prolonging drugs, and cholestyramine.
Q7: Can Loperamide be used during pregnancy and breastfeeding?
A: Use with caution during pregnancy only if clearly needed. It’s excreted in breast milk; use cautiously during breastfeeding.
Q8: What precautions should be taken when prescribing Loperamide?
A: Assess underlying conditions, avoid alcohol and CNS depressants, and advise against driving/operating machinery until effects are known.
Q9: How does Beta-cyclodextrin enhance the effects of Loperamide?
A: It enhances the drug’s solubility, and bioavailability, making it more readily absorbed and potentially effective.
