Generic
Loperamide + Simethicone
2 brands available in the market
At a glance
Loperamide + Simethicone is used for the symptomatic treatment of acute diarrhea associated with gas-related abdominal discomfort including bloating, cramping, or flatulence in adults and adolescents over 12 years.
Description
Loperamide binds to opioid receptors in the gut wall, reducing peristalsis, increasing intestinal transit time, and enhancing resorption of water and electrolytes. Simethicone is a surface-active agent with anti-foaming properties that relieves gas-related symptoms associated with diarrhea.
Indications
- Acute diarrhea with gas-related abdominal discomfort (bloating, cramping, flatulence) - adults and adolescents 12 years and older
Therapeutic class
Anti-diarrheal & Anti-motility Drugs
Pharmacological class
Opioid Receptor Agonist + Anti-foaming Agent
Pharmacology
Loperamide binds to opioid receptors in the gut to reduce peristalsis and increase water resorption. Simethicone is a surfactant that breaks down gas bubbles to relieve bloating and flatulence.
Mechanism of action
Controls diarrhea by reducing peristalsis and relieves bloating and flatulence by breaking down gas bubbles.
Dosage
Adults and 12 years+:
- 2 tablets after the first loose stool
- 1 tablet after each subsequent loose stool
- Maximum 4 tablets/day
- Maximum 2 days use
Children (6-11 years): 1 tablet after first loose stool; ½ tablet after each subsequent; max 2-3 tablets/day (age-dependent), 2 days max
Administration
- Take by mouth
- Take with a full (250 mL) glass of water
- Chewable tablets should be chewed fully and swallowed
- Take on an empty stomach (1 hour before or 2 hours after a meal)
Missed dose
Not generally applicable (short-term use); consult doctor if needed.
Side effects
Common Side Effects:
- Dysgeusia (2.6%)
- Nausea (1.6%)
Precautions & warnings
- Treatment of diarrhea is only symptomatic; discontinue if no improvement within 48 hours
- Caution in hepatic impairment (risk of CNS toxicity)
- Use under medical supervision in severe hepatic dysfunction
- Ensure adequate fluid intake (to prevent dehydration)
Contraindications
- Hypersensitivity to the drug or any ingredients
- Children under 2 years
- Patients in whom constipation must be avoided
- Acute dysentery (blood in stools and elevated temperature)
- Bacterial enterocolitis caused by invasive organisms (Salmonella, Shigella, Campylobacter)
- Acute ulcerative colitis or pseudomembranous colitis
Drug interactions
- Quinidine or ritonavir (P-glycoprotein inhibitors): 2-3 fold increase in loperamide plasma levels
- Itraconazole and gemfibrozil: 3-13 fold increase in loperamide plasma levels (without CNS effects)
- Ketoconazole: 5-fold increase in loperamide plasma levels
- Oral desmopressin: 3-fold increase in desmopressin plasma levels
Food interactions
Loperamide + Simethicone may cause excessive drowsiness with alcohol.
Use in pregnancy
Use in Pregnancy: Safety in human pregnancy not established; animal studies show no teratogenic or embryotoxic properties. Avoid use during first trimester unless clinically justified.
Use in lactation
Use in Lactation: Small amounts of loperamide may appear in breast milk; not recommended during breastfeeding.
Pediatric use
Use with special caution in children under 12 years (variability of response and difficulty swallowing); contraindicated in children under 2 years.
Geriatric use
No dose adjustment required in elderly (>65 years).
Renal / hepatic impairment
Hepatic Impairment: No pharmacokinetic data available; caution due to reduced first-pass metabolism.
Overdose effects
Overdose: QT interval and QRS complex prolongation have been reported.
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Loperamide + Simethicone