Usage
Itopride + Methylpolysiloxane is prescribed for the short-term relief of symptoms associated with functional dyspepsia (non-ulcer dyspepsia) and constipation. These symptoms include epigastric pain, postprandial fullness (feeling full after eating), early satiety (feeling full quickly), upper abdominal discomfort, anorexia, heartburn, nausea, and vomiting. It helps relieve bloating and gas by breaking down gas bubbles in the digestive tract.
Pharmacological Classification:
- Itopride: Gastroprokinetic agent, Dopamine D2 receptor antagonist, Acetylcholinesterase inhibitor
- Methylpolysiloxane: Antiflatulent, Antifoaming agent
Mechanism of Action:
Itopride works by increasing the movement of the intestines. It achieves this by blocking dopamine D2 receptors and inhibiting acetylcholinesterase. Both actions result in increased acetylcholine concentration, a neurotransmitter that promotes gut motility. Methylpolysiloxane relieves bloating and gas by reducing the surface tension of gas bubbles, causing them to combine and be expelled more readily.
Alternate Names
Some alternate names or brand names for Itopride + Methylpolysiloxane include Itokine MPS, Gi-Tune MPS, Motiza MPS, and Itza MPS.
How It Works
Pharmacodynamics:
Itopride enhances acetylcholine activity, resulting in increased gastrointestinal motility and reduced nausea and vomiting. Methylpolysiloxane physically reduces the surface tension of gas bubbles, leading to their coalescence and easier passage.
Pharmacokinetics:
- Itopride: Rapidly absorbed, reaching peak plasma concentration in about 30-45 minutes. Bioavailability is approximately 60%. Highly protein-bound (96%). Metabolized extensively in the liver, primarily by flavin-containing monooxygenase 3 (FMO3) and, to a lesser extent, by CYP3A4. Primarily excreted in the urine, with an elimination half-life of about 6 hours.
- Methylpolysiloxane: Not absorbed systemically. Passes through the GI tract unchanged and is eliminated in the feces.
Mode of Action:
Itopride increases acetylcholine by antagonizing dopamine D2 receptors and inhibiting acetylcholinesterase. This promotes gastric motility, strengthens lower esophageal sphincter pressure, speeds up gastric emptying, and improves gastroduodenal coordination. Itopride’s action on D2 receptors in the chemoreceptor trigger zone (CTZ) contributes to its antiemetic properties. Methylpolysiloxane reduces surface tension of gas bubbles, which decreases their stability, facilitates their coalescence and finally promotes their elimination.
Dosage
Standard Dosage
Adults:
The standard dose is 50 mg of Itopride and 125 mg of Methylpolysiloxane taken orally three times a day before meals.
Children:
The safety and efficacy in children under 16 years old have not been established. It is generally not recommended for pediatric use unless specifically directed by a healthcare professional.
Special Cases:
- Elderly Patients: Dose adjustments may be necessary due to age-related decline in renal and hepatic function. A lower starting dose with careful titration is advised.
- Patients with Renal Impairment: Use with caution. Dosage adjustments may be necessary based on creatinine clearance.
- Patients with Hepatic Dysfunction: Use with caution. Dosage adjustments may be required due to decreased Itopride metabolism.
- Patients with Comorbid Conditions: Careful consideration of drug interactions and potential dose adjustments is necessary in patients with conditions like diabetes or cardiovascular disease.
Clinical Use Cases
Itopride + Methylpolysiloxane is not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dose adjustments are crucial for patients with renal or hepatic impairment, elderly patients, and those with specific comorbid conditions. Consider individual patient characteristics, concomitant medications, and potential drug interactions.
Side Effects
Common Side Effects:
Diarrhea, stomach pain, headache, dizziness, nausea, increased saliva production, and allergic reactions (rash, itching).
Rare but Serious Side Effects:
Liver toxicity (jaundice, elevated liver enzymes), blood disorders (leukopenia, thrombocytopenia, anemia), and hypersensitivity reactions.
Long-Term Effects:
Limited data are available on long-term effects. Periodic monitoring of liver function and complete blood count (CBC) is recommended.
Adverse Drug Reactions (ADR):
Clinically significant ADRs requiring immediate intervention include anaphylactoid reactions, signs of liver toxicity (jaundice, right upper quadrant pain), and blood dyscrasias (unusual bleeding/bruising, fatigue, pallor).
Contraindications
Hypersensitivity to Itopride, Methylpolysiloxane, or any components of the formulation. Gastrointestinal hemorrhage, mechanical gastrointestinal obstruction, and gastrointestinal perforation are absolute contraindications.
Drug Interactions
- Anticholinergic drugs: May reduce Itopride’s prokinetic effects.
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, erythromycin): May increase Itopride levels.
- CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine): May decrease Itopride levels.
- Hormonal contraceptives: Itopride may reduce the effectiveness of birth control pills.
- Cyclosporine: Co-administration is contraindicated due to significantly increased risk of liver toxicity.
- Warfarin: Careful monitoring is essential due to the potential for Itopride to alter warfarin’s anticoagulant effects.
Pregnancy and Breastfeeding
Pregnancy: Itopride should be avoided during pregnancy unless the potential benefits outweigh the risks. Human data is limited, and although animal studies show no teratogenic effects, caution is advised.
Breastfeeding: Itopride is excreted in animal milk; excretion in human milk is unknown. Exercise caution during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Itopride increases acetylcholine, promoting gastrointestinal motility and reducing nausea/vomiting. Methylpolysiloxane breaks down gas bubbles.
- Side Effects: Diarrhea, stomach pain, headache, dizziness, nausea, increased saliva production. Rarely: liver toxicity, blood disorders, hypersensitivity.
- Contraindications: Hypersensitivity, GI hemorrhage, obstruction, or perforation.
- Drug Interactions: Anticholinergics, CYP3A4 inhibitors/inducers, hormonal contraceptives, cyclosporine, warfarin.
- Pregnancy & Breastfeeding: Avoid during pregnancy unless clearly necessary. Exercise caution during breastfeeding.
- Dosage: 50 mg Itopride + 125 mg Methylpolysiloxane three times daily before meals. Adjustments are needed for elderly patients and those with hepatic/renal impairment.
- Monitoring Parameters: Liver function tests (LFTs), complete blood count (CBC) (especially during long-term use).
Popular Combinations
Itopride is sometimes combined with proton pump inhibitors (PPIs) like rabeprazole or pantoprazole to treat gastroesophageal reflux disease (GERD) and functional dyspepsia. However, it is usually just Itopride and not the combination containing Methylpolysiloxane.
Precautions
- General Precautions: Pre-screening for allergies, renal/hepatic function, and gastrointestinal conditions is vital.
- Pregnant Women: Avoid unless absolutely necessary. Thoroughly discuss risks and benefits with a physician.
- Breastfeeding Mothers: Use with caution and monitor the infant for adverse effects.
- Children & Elderly: Not recommended for children under 16. Dose adjustments may be needed for the elderly.
- Lifestyle Considerations: Lifestyle modifications like a high-fiber diet, increased fluid intake, and regular exercise can be helpful. Limit alcohol consumption.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Itopride + Methylpolysiloxane?
A: The standard adult dose is 50 mg Itopride + 125 mg Methylpolysiloxane, taken orally three times daily before meals. Dose adjustments are necessary for elderly patients and those with renal or hepatic impairment. It is not recommended for children under 16.
Q2: What are the primary uses of Itopride + Methylpolysiloxane?
A: It is used for symptomatic relief of functional dyspepsia (non-ulcer dyspepsia) and constipation.
Q3: What is the mechanism of action of Itopride?
A: It blocks dopamine D2 receptors and inhibits acetylcholinesterase, ultimately increasing acetylcholine and promoting gut motility. It also acts on D2 receptors in the CTZ to reduce nausea/vomiting.
Q4: How does Methylpolysiloxane work?
A: It works by physically disrupting gas bubbles in the gut, facilitating their passage.
Q5: What are the common side effects?
A: Common side effects include diarrhea, stomach pain, headache, dizziness, nausea, and increased saliva production.
Q6: Are there any serious side effects?
A: Yes. Rare but serious side effects include liver toxicity, blood disorders, and hypersensitivity reactions. Prompt medical attention is required if these occur.
Q7: What are the contraindications for this medication?
A: Contraindications include hypersensitivity, gastrointestinal hemorrhage, mechanical obstruction, and perforation.
Q8: Can Itopride + Methylpolysiloxane be used during pregnancy or breastfeeding?
A: It should be avoided during pregnancy unless the benefits outweigh the risks. Caution is also advised during breastfeeding due to potential drug excretion in breast milk.
Q9: What monitoring parameters should be followed for patients using this medication?
A: Liver function tests and complete blood counts should be monitored, especially with prolonged use.
Q10: How should this medication be taken?
A: It should be taken orally, three times a day, before meals.
