Mosapride + Simethicone

Usage

Mosapride + Simethicone is prescribed for the relief of dyspepsia symptoms, such as bloating, abdominal distension, early satiety, and slow transit constipation. It also helps relieve gas, gas pains, and heartburn.

• Pharmacological Classification:

  • Mosapride: Gastroprokinetic agent (serotonin 5-HT4 receptor agonist)
  • Simethicone: Antiflatulent

• Mechanism of Action: Mosapride increases gastrointestinal motility and accelerates gastric emptying by enhancing acetylcholine release in the enteric nervous system. Simethicone reduces the surface tension of gas bubbles in the GI tract, causing them to combine and be expelled more easily.

Alternate Names

• Mosapride Citrate + Simethicone
• Mosapride Citrate Dihydrate/Simethicone

Some brand names include (but may not be limited to): Acicare Oral Gel, Mosid MPS, Mozax MPS, Regmotil MPS, and others. Availability may vary by region.

How It Works

• Mosapride:

  • Pharmacodynamics: Acts as a selective 5-HT4 receptor agonist, stimulating acetylcholine release, increasing gastrointestinal motility and gastric emptying.
  • Pharmacokinetics: Rapidly absorbed orally, reaching peak plasma concentration in about 0.8 hours. Highly protein-bound (99%). Metabolized primarily in the liver by CYP3A4. Excreted in urine and feces.

• Simethicone:

  • Pharmacodynamics: Reduces surface tension of gas bubbles, promoting their coalescence and expulsion. Physiologically inert.
  • Pharmacokinetics: Not absorbed systemically. Passes through the GI tract unchanged and is eliminated in the feces.

Dosage

Standard Dosage

Adults: One tablet, containing 5 mg of mosapride citrate and 200 mg of simethicone (or 10 mg mosapride and 125 mg - 200 mg simethicone depending on the formulation), three times a day, before meals.

Children: Use of the combination product is contraindicated in children. Simethicone may be used as a single agent for children according to its pediatric dosing guidelines, but mosapride use is generally avoided in pediatrics as its safety and effectiveness hasn’t been established.

Special Cases:

• Elderly Patients: Reduced dosage of mosapride (e.g., 7.5 mg/day) is recommended due to potential age-related decline in hepatic and renal function. Close monitoring is advised.
• Patients with Renal Impairment: Use with caution. Dosage adjustment of mosapride may be needed.
• Patients with Hepatic Dysfunction: Use with caution. Dosage adjustment of mosapride may be required as it is metabolized in the liver.
• Patients with Comorbid Conditions: Careful evaluation is necessary. Adjust dosages based on specific patient needs and consult specialist if necessary.

Clinical Use Cases

The Mosapride + Simethicone combination is not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations.

Side Effects

Common Side Effects: Diarrhea, loose stools, dry mouth, abdominal pain, headache, dizziness, nausea, insomnia, fatigue.

Rare but Serious Side Effects: Allergic reactions (rash, hives, itching); QT prolongation (with mosapride); irregular heartbeat (with mosapride).

Long-Term Effects: Not well-documented. Some trials show use for up to two years with good tolerance, but close monitoring of patients is necessary in prolonged usage.

Contraindications

• Hypersensitivity to mosapride or simethicone.
• Gastrointestinal hemorrhage.
• Mechanical bowel obstruction.
• Perforation of the GI tract.
• Pregnancy and breastfeeding.
• Children (for the combination product).

Drug Interactions

• Mosapride: Erythromycin (may increase mosapride plasma concentrations); anticholinergic agents (may decrease mosapride’s effects).
• Simethicone: Levothyroxine (may decrease absorption of levothyroxine).

Pregnancy and Breastfeeding

Contraindicated in both pregnancy and breastfeeding. Mosapride’s safety during pregnancy and breastfeeding hasn’t been established. It’s unknown if mosapride is excreted in breast milk. Simethicone is considered generally safe during pregnancy when used alone, but the combination is avoided.

Drug Profile Summary

• Mechanism of Action: Mosapride: 5-HT4 receptor agonist, increases GI motility. Simethicone: Reduces surface tension of gas bubbles.
• Side Effects: Diarrhea, dry mouth, abdominal pain, headache, dizziness, QT prolongation (mosapride).
• Contraindications: Hypersensitivity, GI bleeding, bowel obstruction, pregnancy, breastfeeding, children (for the combination product).
• Drug Interactions: Mosapride: Erythromycin, anticholinergics. Simethicone: Levothyroxine.
• Pregnancy & Breastfeeding: Contraindicated.
• Dosage: Adults: One tablet (5 mg mosapride/200 mg simethicone or other formulation) three times daily before meals. Elderly: Reduced dose.
• Monitoring Parameters: Electrolytes, liver function, ECG (for mosapride), symptom resolution.

Popular Combinations

Mosapride and simethicone are often prescribed together as a fixed-dose combination. Mosapride is also sometimes combined with pancreatin or pantoprazole in some markets. Always check local availability.

Precautions

• General Precautions: Pre-screening for allergies, metabolic disorders, and hepatic/renal dysfunction is important.
• Pregnant Women: Contraindicated.
• Breastfeeding Mothers: Contraindicated.
• Children & Elderly: Combination product is contraindicated in children. Reduced dose for elderly.
• Lifestyle Considerations: Avoid alcohol while taking mosapride. Alcohol may worsen some potential side effects such as drowsiness.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Mosapride + Simethicone?

A: Adults: One tablet (typically 5 mg mosapride/200 mg simethicone or similar formulations) three times daily before meals. Elderly patients: Reduced dose (e.g. 7.5mg/day). Children: Contraindicated.

Q2: What are the primary uses of this combination?

A: Relief of dyspepsia symptoms (bloating, distension, early satiety, slow transit constipation), gas, gas pains, and heartburn.

Q3: What is the mechanism of action of each component?

A: Mosapride is a prokinetic agent (5-HT4 receptor agonist), stimulating gut motility. Simethicone is an antiflatulent, reducing surface tension of gas bubbles.

Q4: What are the common side effects?

A: Diarrhea, dry mouth, abdominal pain, headache, and dizziness are the most common side effects.

Q5: Are there any serious drug interactions to be aware of?

A: Mosapride can interact with erythromycin, increasing mosapride levels, and with anticholinergics, decreasing its efficacy. Simethicone can interact with levothyroxine and similar thyroid medications, decreasing their absorption.

Q6: Can this medication be used during pregnancy or breastfeeding?

A: No, it is contraindicated during both pregnancy and breastfeeding.

Q7: Are there any specific precautions for elderly patients?

A: Yes, a reduced dosage is recommended due to potential age-related decline in hepatic and renal function.

Q8: Can this drug be prescribed to children?

A: The combination product is not recommended for use in children as its safety and efficacy hasn’t been established. Simethicone may be used alone as directed by a doctor.

Q9: How should I counsel patients on lifestyle modifications while taking this medication?

A: Advise patients to avoid alcohol while on mosapride due to possible increased drowsiness and other side effects.

Q10: What should I do if a patient experiences persistent side effects?

A: If a patient experiences persistent or bothersome side effects, reassess their medication regimen. Consider dosage adjustments, alternative medications, or additional management strategies. For severe adverse drug reactions, discontinue the medication immediately and initiate appropriate medical management.