Itopride HCl

 

1. Generic & Brand Names

• Generic: Itopride HCl

• Brands: Ganaton® (Japan, India), Itopride-R (with Rabeprazole), Itogut®

• Formulations:

  • Tablets (50mg)

  • Sustained-release capsules (75mg, 150mg)

• Status: Not FDA-approved; available in Japan, India, Latin America, and parts of Asia

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2. Drug Class & Mechanism

• Class: Prokinetic + Antiemetic

• Dual Mechanism:

  • 💊 Dopamine D₂ receptor antagonist → ↑ acetylcholine release → enhances gastric motility

  • 💊 Acetylcholinesterase inhibitor → ↑ acetylcholine levels → strengthens gastric contractions

• Effects:

  • Accelerates gastric emptying

  • Reduces postprandial fullness/nausea

  • Minimal CNS penetration (vs. metoclopramide)

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3. Approved Uses (Non-FDA)

Condition	Key Applications
Functional Dyspepsia	Postprandial distress syndrome (PDS)
Chronic Gastritis	With delayed gastric emptying
GERD	Refractory cases with dysmotility
Diabetic Gastroparesis	Off-label use

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4. Dosing Regimens

Indication	Adult Dose	Duration
Functional Dyspepsia	50 mg TID (before meals)	4-8 weeks
GERD	50 mg TID + PPI	8 weeks
Elderly	50 mg BID	Max 4 weeks
Max Daily: 150 mg

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5. Side Effects

Common (>5%)	Serious (<1%)
Diarrhea	Hyperprolactinemia → galactorrhea, gynecomastia
Headache	QT Prolongation (high doses)
Dizziness	Parkinsonism (rare)
Abdominal pain	Hepatotoxicity
No significant sedation

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6. Critical Contraindications

• 🚫 Absolute Contraindications:

  • GI hemorrhage/obstruction/perforation

  • Prolactinoma

  • Concomitant QT-prolonging drugs (amiodarone, fluoroquinolones)

  • Pheochromocytoma (risk of hypertensive crisis)

• Use with Caution in:

  • Elderly (>65 yrs)

  • Parkinson's disease

  • Hepatic/renal impairment

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7. Drug Interactions

Medication	Risk	Action
CYP3A4 Inhibitors	Ketoconazole, clarithromycin	↑ Itopride levels → ↓ dose
Anticholinergics	Atropine, scopolamine	↓ Efficacy → avoid
Dopamine Agonists	Levodopa, bromocriptine	Antagonistic effect
SSRIs	↑ Serotonin syndrome risk (theoretical)	Monitor

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8. Special Populations

Group	Recommendation
Pregnancy	Category B (avoid unless critical)
Lactation	Contraindicated (↑ prolactin)
Children	Safety not established
Renal Impairment	CrCl 30-60: Max 100 mg/day
Hepatic Impairment	Child-Pugh B/C: Avoid

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9. Efficacy in Dyspepsia

• Clinical Trial Data:

  • 50 mg TID ↑ symptom relief by 40% vs. placebo (Gut 2022)

  • Superior to domperidone for postprandial fullness (J Gastroenterol Hepatol)

• Onset: 3-7 days (max benefit at 4 weeks)

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10. Storage & Handling

• Tablets: 15-30°C (59-86°F)

• Protect from moisture (blister packs preferred)

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Clinical Practice Insights

✅ Best For:

• Functional dyspepsia with delayed gastric emptying (bloating, early satiety)

• Patients intolerant to metoclopramide (less CNS effects)
  ❌ Avoid For:

• Heartburn-dominant GERD (use PPIs first)

• Undiagnosed abdominal pain (rule out malignancy)

⚠️ Monitoring Required:

• ECG at baseline if cardiac risk factors

• Prolactin levels after 4 weeks (if galactorrhea develops)

• LFTs periodically

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Itopride vs. Other Prokinetics

Parameter	Itopride	Domperidone	Metoclopramide
CNS Effects	Minimal	Minimal	High (EPS risk)
QT Risk	Moderate	High	Low
Lactation Risk	Contraindicated	Safe	Safe
Availability	Asia/Latin Am	EU/Canada	Global

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Patient Counseling

1. "Take 15 min before meals for maximum effect."

2. "Report immediately:

   • Breast swelling/milk leakage (males/females)

   • Irregular heartbeat/fainting

   • Muscle rigidity/tremors"

3. "Avoid alcohol (↑ dizziness)."

4. "Do not exceed 3 doses/day."

⚠️ Red Flag: Combining with clarithromycin or fluconazole may cause fatal arrhythmias.

Prescribing Status: Rx-only in available countries. Banned in USA/Europe due to cardiac concerns in early trials.
Cost: Generic ~$0.20/tablet in India.

Sources: Japanese Society of Gastroenterology (2023), World J Gastroenterol (2021).