Mosapride + Rabeprazole

Usage

• Mosapride + Rabeprazole is prescribed for the treatment of gastroesophageal reflux disease (GERD), including symptoms like heartburn, acid regurgitation, and stomach pain. It is also used to treat peptic ulcers, acidity, and dyspepsia (indigestion).
• Pharmacological classification: This combination drug falls under two classifications:
  • Rabeprazole: Proton Pump Inhibitor (PPI)
  • Mosapride: Prokinetic Agent
• Mechanism of Action: Rabeprazole decreases gastric acid production by inhibiting the H+/K+-ATPase proton pump in the parietal cells of the stomach. Mosapride enhances gastrointestinal motility by stimulating 5-HT4 receptors, increasing acetylcholine release, and increasing the pressure of the lower esophageal sphincter, which helps prevent acid reflux.

Alternate Names

• No widely recognized alternate names exist for the combination itself. The components have the following alternate names:
  • Rabeprazole sodium
  • Mosapride citrate
• Brand Names: Rabeflux, Veloz M, Happi-M are among the brand names. Several other brands may also exist, especially in regional markets within India.

How It Works

• Pharmacodynamics: Rabeprazole suppresses gastric acid secretion, providing relief from GERD symptoms and promoting ulcer healing. Mosapride increases the rate of gastric emptying and improves esophageal motility.
• Pharmacokinetics:
  • Rabeprazole: Absorbed in the intestine, metabolized by CYP450 enzymes, primarily CYP2C19, eliminated via both renal and hepatic routes.
  • Mosapride: Undergoes hepatic metabolism primarily by CYP3A4. Eliminated via renal and hepatic routes. Concomitant use of Mosapride increases the peak plasma concentration (Cmax) and the area under the time-concentration curve (AUC) of Rabeprazole.
• Mode of Action: Rabeprazole inhibits the H+/K+-ATPase in gastric parietal cells, blocking acid secretion. Mosapride is a 5-HT4 receptor agonist, enhancing acetylcholine release and stimulating gastrointestinal motility.
• Elimination Pathways: Primarily renal and hepatic excretion for both drugs.

Dosage

Standard Dosage

Adults:

One capsule containing 20 mg Rabeprazole and 15 mg Mosapride once daily, usually before a meal, for 4-8 weeks.

Children:

Not recommended for children due to lack of established safety and efficacy data.

Special Cases:

• Elderly Patients: Use with caution. Dose adjustments may be necessary depending on renal and hepatic function.
• Patients with Renal Impairment: Use with caution. Dose adjustment may be necessary depending on the degree of impairment.
• Patients with Hepatic Dysfunction: Use with caution. Dose adjustments may be necessary depending on the degree of impairment.
• Patients with Comorbid Conditions: Use with caution in patients with cardiac conditions (especially QT prolongation) or diabetes.

Clinical Use Cases

Not typically used in settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Its primary role is in the outpatient management of GERD and related conditions.

Dosage Adjustments

Dose adjustments are based on individual patient factors such as age, renal or hepatic impairment, comedications, and treatment response.

Side Effects

Common Side Effects:

Nausea, stomach pain, diarrhea, flatulence, headache, dizziness, weakness, sleepiness, flu-like symptoms, dry mouth, insomnia.

Rare but Serious Side Effects:

Hypomagnesemia (long-term use), osteoporosis and related fractures (long-term use), cardiac arrhythmias (QT prolongation), severe allergic reactions (anaphylaxis, angioedema), kidney problems.

Long-Term Effects:

Osteoporosis-related fractures, hypomagnesemia.

Adverse Drug Reactions (ADR):

Severe allergic reactions, severe hypomagnesemia, drug-induced lupus, Clostridium difficile-associated diarrhea.

Contraindications

• Hypersensitivity to Rabeprazole, Mosapride, or other PPIs.
• Gastrointestinal bleeding, obstruction, or perforation.
• Concomitant use with Rilpivirine.
• Pregnancy (unless absolutely necessary).
• Breastfeeding (unless absolutely necessary).
• Children.

Drug Interactions

• CYP450 Interactions: Rabeprazole is metabolized by CYP450 enzymes (mainly CYP2C19). Inhibitors (e.g., ketoconazole, itraconazole) or inducers (e.g., phenytoin) may alter its levels. Mosapride is metabolized by CYP3A4. Its interaction with other CYP3A4 inhibitors/inducers needs careful consideration.
• Other Drug Interactions: NSAIDs (increased risk of GI bleeding), warfarin, methotrexate, atazanavir, ketoconazole, itraconazole, clopidogrel, diazepam, zolpidem. Mosapride may interact with other prokinetic agents (e.g., metoclopramide) or anticholinergics which may reduce GI motility.
• OTC Drugs/Supplements: St. John’s Wort.
• Food and lifestyle factors: Alcohol (may worsen GERD symptoms and increase the risk of GI bleeding). Avoid smoking.

Pregnancy and Breastfeeding

• Pregnancy: Not recommended unless absolutely necessary. Potential risks to the fetus should be carefully weighed against benefits.
• Breastfeeding: Not recommended unless absolutely necessary. Drug excretion in breast milk and potential neonatal effects are not well-established.

Drug Profile Summary

• Mechanism of Action: Rabeprazole: PPI, inhibits H+/K+-ATPase. Mosapride: Prokinetic, 5-HT4 agonist.
• Side Effects: Nausea, headache, diarrhea, dizziness; rarely, hypomagnesemia, osteoporosis, cardiac arrhythmias.
• Contraindications: Hypersensitivity, GI bleeding/obstruction, Rilpivirine, pregnancy/breastfeeding, children.
• Drug Interactions: CYP450 interactions, NSAIDs, warfarin, methotrexate, and others (see detailed section).
• Pregnancy & Breastfeeding: Not generally recommended.
• Dosage: 20 mg Rabeprazole + 15 mg Mosapride once daily before meals. Adjustments needed for specific populations.
• Monitoring Parameters: Monitor magnesium levels with prolonged use. Assess for signs of GI bleeding. Monitor renal and hepatic function if needed.

Popular Combinations

The combination of Rabeprazole and Mosapride itself is a frequently used combination in clinical practice for enhancing the efficacy of GERD treatment. It addresses both acid secretion and motility issues.

Precautions

• General Precautions: Assess for allergies, hepatic/renal dysfunction, and cardiac history before initiating therapy. Screen for Clostridium difficile infection before and during treatment if indicated.
• Specific Populations:
  • Pregnant Women: Avoid unless absolutely necessary. Weigh the benefits against potential risks.
  • Breastfeeding Mothers: Avoid unless absolutely necessary. Consider the risk to the neonate.
  • Children & Elderly: Not recommended for children. Use cautiously in the elderly.
  • Lifestyle Considerations: Avoid alcohol and smoking, as they may exacerbate GERD symptoms. Caution patients about dizziness/drowsiness and potential driving impairment.

FAQs (Frequently Asked Questions)

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

A: The typical dose is one capsule (or tablet) containing 20 mg Rabeprazole and 15 mg Mosapride taken once daily before a meal.

Q2: How does Mosapride enhance the efficacy of Rabeprazole?

A: Mosapride improves gastric motility, which complements Rabeprazole’s acid-suppressing effects and helps improve GERD symptoms. It also improves Rabeprazole’s pharmacokinetics, specifically its Cmax and AUC.

Q3: What are the serious side effects to watch out for with long-term use?

A: Hypomagnesemia and osteoporosis-related fractures are potential long-term risks. Monitoring magnesium levels is important, especially with extended use.

Q4: Can this combination be used in pregnant or breastfeeding women?

A: It is generally avoided in pregnancy and breastfeeding unless absolutely necessary. The potential risks to the fetus or neonate should be carefully weighed against the benefits.

Q5: What are the key drug interactions to consider?

A: Interactions with CYP450 substrates, NSAIDs, warfarin, methotrexate, atazanavir, and other medications are important to note. Concomitant use with Rilpivirine is contraindicated.

Q6: Are there any dietary recommendations while on this medication?

A: Avoiding alcohol and foods that trigger GERD symptoms (e.g., spicy, fatty foods) is advised. Consuming a balanced diet rich in fiber is also beneficial.

Q7: Can Mosapride + Rabeprazole be used in patients with liver or kidney problems?

A: Use with caution in patients with hepatic or renal impairment. Dose adjustments may be necessary.

Q8: What should I do if a patient misses a dose?

A: Take the missed dose as soon as remembered, unless it’s close to the next scheduled dose. Do not double the dose.

Q9: Is it safe to drive while taking this medication?

A: Dizziness and drowsiness can occur. Advise patients to avoid driving or operating machinery if these side effects are experienced.

Q10: What is the duration of treatment with Mosapride + Rabeprazole?

A: Treatment duration varies depending on the condition and individual patient response, typically ranging from 4 to 8 weeks. Longer courses may be necessary in some cases.