Usage
Mosapride is prescribed for the symptomatic treatment of functional dyspepsia (also known as chronic gastritis) and gastroesophageal reflux disease (GERD). It alleviates symptoms such as heartburn, nausea, vomiting, and upper abdominal discomfort. Pharmacologically, it is classified as a gastroprokinetic agent, specifically a selective serotonin 5-HT4 receptor agonist. Mosapride’s mechanism of action involves stimulating 5-HT4 receptors in the gastrointestinal tract, leading to increased release of acetylcholine and enhanced gastrointestinal motility and gastric emptying.
Alternate Names
Mosapride is also known as Mosapride Citrate or Mosapride Citrate Hydrate. Brand names include Gasmotin, Gutmovin, GASTIIN CR, mosar®, mosar® plus, Mazt and MT PRIDE 5 among others. International variations exist, such as Agimosarid (VN), Anamotin (KR, PH), and Biotonus (PE).
How It Works
Pharmacodynamics: Mosapride acts as a selective 5-HT4 receptor agonist, primarily in the enteric nervous system of the gastrointestinal tract. This action results in increased acetylcholine release, enhancing gastric emptying and promoting coordinated peristaltic activity in the stomach and small intestine.
Pharmacokinetics: Mosapride is rapidly absorbed after oral administration, reaching peak plasma concentrations within 0.5 to 1.4 hours. It has a volume of distribution of 1.7 to 3.5 L/kg and is approximately 97-99% bound to plasma proteins. Mosapride is metabolized primarily in the liver by CYP3A4, with its main metabolite being the des-4-fluorobenzyl compound. It is eliminated through both renal and hepatic pathways, with approximately 1% excreted unchanged in urine and 10% excreted as the active metabolite. The elimination half-life of mosapride is 1.4–2.5 hours, and around 4.3 hours for the metabolite.
Mode of Action: Mosapride selectively binds to and activates 5-HT4 receptors located on presynaptic cholinergic neurons in the myenteric plexus. This activation enhances acetylcholine release, causing increased gastric motility and peristalsis.
Elimination Pathways: Excretion occurs via both urine and feces. Less than 1% of an administered dose is excreted in urine as unchanged drug, while around 7% is excreted as its main metabolite (des-4-fluorobenzyl mosapride).
Dosage
Standard Dosage
Adults:
The standard adult dosage is 5 mg three times daily, taken orally before or after meals. The maximum daily dosage should not exceed 15 mg.
Children:
The safety and efficacy of Mosapride in pediatric patients have not been established. There are no officially established pediatric dosage recommendations. Unofficial sources suggest 0.3 mg/kg/day in 2-3 divided doses, but this should be approached cautiously.
Special Cases:
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Elderly Patients: Due to potential age-related decline in hepatic and renal function, a lower starting dose of 2.5 mg three times daily (7.5mg/day) is recommended for elderly patients. Close monitoring is essential, and further dose adjustments may be necessary.
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Patients with Renal Impairment: In patients with renal impairment, caution is warranted, and starting dose should not exceed 2.5 mg three times a day. Closely monitor for adverse effects. Specific dosage recommendations are limited.
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Patients with Hepatic Dysfunction: In patients with hepatic impairment, a reduced starting dose of 2.5 mg three times daily (7.5mg/day) is recommended. Closely monitor the patient’s condition, since mosapride is metabolized in the liver.
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Patients with Comorbid Conditions: In patients with comorbid conditions, exercise caution and adjust the dosage as needed.
Clinical Use Cases
There are no specific dosage recommendations for the listed clinical scenarios (Intubation, Surgical Procedures, Mechanical Ventilation, ICU Use, and Emergency Situations). Mosapride’s primary use is for functional dyspepsia and GERD. It is occasionally used as an adjunct treatment prior to barium enema X-ray examinations. The dosage in such cases would generally align with the standard adult dose, with adjustments made based on patient-specific factors.
Dosage Adjustments
Dose modification is crucial for elderly patients, those with renal or hepatic dysfunction, and those with specific metabolic disorders or genetic polymorphisms that may affect drug metabolism. Start with a lower dose and titrate based on clinical response and tolerance.
Side Effects
Common Side Effects
Diarrhea, dry mouth, abdominal pain/cramps, headache, dizziness, malaise, insomnia, nausea, unusual tiredness and weakness.
Rare but Serious Side Effects
Fulminant hepatitis, serious hepatic dysfunction (accompanied by a marked increase in AST, ALT, and γ-GTP), jaundice (some cases fatal), QT interval prolongation, irregular heartbeat.
Long-Term Effects
Data on long-term complications from prolonged Mosapride use is limited, but rodent studies have shown an increased risk of liver (hepatocellular adenoma) and thyroid (follicular cell adenoma) tumors at very high doses. Therefore, prolonged use without clear clinical benefit is not advised.
Adverse Drug Reactions (ADR)
Serious ADRs include fulminant hepatitis, hepatic dysfunction, and jaundice, which may be fatal. QT interval prolongation and severe hypersensitivity reactions are also possible.
Contraindications
Mosapride is contraindicated in patients with:
- Known hypersensitivity to Mosapride or any component of the formulation.
- Gastrointestinal hemorrhage, mechanical obstruction, or perforation.
- Patients with a history of QT interval prolongation or other significant cardiac arrhythmias.
Drug Interactions
Mosapride is primarily metabolized by CYP3A4. Concomitant use with CYP3A4 inhibitors (e.g., erythromycin, ketoconazole, itraconazole, clarithromycin) may increase Mosapride plasma levels. Concomitant administration with CYP3A4 inducers may decrease its efficacy. Anticholinergic agents may attenuate Mosapride’s prokinetic effects. Monitor closely when using with drugs that prolong the QT interval (e.g., amiodarone, sotalol). Interactions with some antipsychotics (e.g. haloperidol) have also been reported. Avoid alcohol, smoking, and grapefruit juice as these may alter drug levels or increase the risk of side effects.
Pregnancy and Breastfeeding
The safety of Mosapride during pregnancy has not been established. Use only if the potential benefits outweigh the potential risks to the fetus. Mosapride is excreted in breast milk. Avoid Mosapride during breastfeeding or discontinue breastfeeding if Mosapride therapy is essential.
Drug Profile Summary
- Mechanism of Action: 5-HT4 receptor agonist, increases acetylcholine release, enhances gastrointestinal motility.
- Side Effects: Diarrhea, dry mouth, abdominal pain, headache, dizziness, serious hepatic dysfunction (rare).
- Contraindications: Hypersensitivity, GI bleeding/obstruction/perforation, QT prolongation.
- Drug Interactions: CYP3A4 inhibitors/inducers, anticholinergics, QT prolonging agents.
- Pregnancy & Breastfeeding: Avoid if possible due to safety concerns.
- Dosage: Adults: 5 mg TID. Elderly/Hepatically impaired: 2.5 mg TID. Pediatric: Not established.
- Monitoring Parameters: Liver function tests (LFTs), electrolytes (especially potassium), ECG in high-risk individuals for QT prolongation.
Popular Combinations
No specific “popular” drug combinations are widely recognized for Mosapride.
Precautions
- General Precautions: Screen for pre-existing liver/kidney disease, assess cardiac history (QT prolongation risk).
- Specific Populations: Pregnant/Breastfeeding: Avoid unless absolutely necessary. Children: Safety not established. Elderly: Reduced dose.
- Lifestyle Considerations: Avoid alcohol, smoking.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Mosapride?
A: The standard adult dose is 5 mg taken orally three times daily before or after meals. Elderly or hepatically impaired patients should begin with 2.5 mg three times daily.
Q2: What are the common side effects of Mosapride?
A: Common side effects include diarrhea, dry mouth, headache, abdominal pain, dizziness, and malaise.
Q3: What are the contraindications for Mosapride?
A: Contraindications include known hypersensitivity to Mosapride, gastrointestinal hemorrhage, mechanical obstruction or perforation, and conditions that predispose to QT prolongation.
Q4: How does Mosapride interact with other medications?
A: Mosapride interacts with CYP3A4 inhibitors and inducers, anticholinergics, and drugs that prolong the QT interval.
Q5: Can Mosapride be used during pregnancy or breastfeeding?
A: Mosapride’s safety during pregnancy or breastfeeding has not been established. Use it only if the benefits outweigh the potential risks.
Q6: How should Mosapride be administered?
A: Mosapride is administered orally, typically three times a day before or after meals.
Q7: What should be monitored in patients taking Mosapride?
A: Monitor liver function tests, electrolytes, and, for high-risk individuals, ECG for QT prolongation.
Q8: How long should a patient take Mosapride?
A: Treatment duration should be based on the patient’s response to therapy. If symptoms don’t improve within 2 weeks, reconsider continuing Mosapride.
Q9: What is the mechanism of action of Mosapride?
A: Mosapride is a selective 5-HT4 receptor agonist. This action enhances acetylcholine release, thus improving gastrointestinal motility and gastric emptying.
Q10: Is Mosapride safe for pediatric use?
A: Safety and efficacy have not been established in children. Use with caution and at a reduced dosage, if necessary. Limited information suggests a starting point of 0.3 mg/kg/day divided into 2-3 doses. However, this isn’t an official recommendation.
