Usage
- Esomeprazole + Itopride is prescribed for conditions like gastroesophageal reflux disease (GERD), peptic ulcers, gastric ulcers (especially those caused by H. pylori), heartburn, dyspepsia, and Zollinger-Ellison syndrome.
- Pharmacological classification: This combination drug falls under two classifications:
- Esomeprazole: Proton Pump Inhibitor (PPI)
- Itopride: Gastroprokinetic agent/ Dopamine D2 receptor antagonist and Acetylcholinesterase inhibitor.
- Mechanism of Action: Esomeprazole reduces gastric acid secretion by inhibiting the proton pump in the stomach lining. Itopride improves gastric motility by increasing acetylcholine levels and blocking dopamine D2 receptors, promoting faster emptying of the stomach and improved coordination of gastrointestinal movement.
Alternate Names
- This combination doesn’t have a universally recognized International Nonproprietary Name (INN). It’s usually referred to as “esomeprazole and itopride” or “esomeprazole + itopride.”
- Brand Names: Several brand names exist, including Sompraz IT, Nexpro IT, Esovag IT, Emostrum IT, Pileca, and Esokem IT.
How It Works
- Pharmacodynamics: Esomeprazole profoundly suppresses gastric acid secretion, leading to increased gastric pH. Itopride enhances gastric motility, accelerates gastric emptying, reduces lower esophageal sphincter pressure and improves gastro-duodenal coordination.
- Pharmacokinetics:
- Esomeprazole is rapidly absorbed after oral administration and is extensively metabolized by the liver (CYP2C19 and CYP3A4 enzymes). Elimination is primarily renal.
- Itopride is also well-absorbed orally and metabolized by the liver (mainly by flavin-containing monooxygenase 3 (FMO3)). It is primarily excreted in the urine.
- Mode of Action: Esomeprazole irreversibly binds to the H+/K+-ATPase enzyme (proton pump) in gastric parietal cells, blocking the final step of acid production. Itopride increases acetylcholine levels by inhibiting acetylcholinesterase and antagonizes dopamine D2 receptors, both of which contribute to increased gastric motility.
- Elimination pathways: Both drugs are primarily eliminated through renal excretion, with some hepatic metabolism.
Dosage
Standard Dosage
Adults:
- The usual recommended dosage is 40 mg esomeprazole and 150 mg itopride, taken once daily before meals, preferably in the morning. Duration of therapy depends on the indication and clinical response.
Children:
- This combination is generally not recommended for children under 12 years of age, as safety and efficacy have not been established in this population.
Special Cases:
- Elderly Patients: Dose adjustment may be needed in patients with severe liver or kidney impairment.
- Patients with Renal Impairment: Caution and dose adjustment might be necessary based on creatinine clearance.
- Patients with Hepatic Dysfunction: Dose reduction is often needed due to decreased metabolism.
- Patients with Comorbid Conditions: Careful evaluation and dose adjustments might be required in patients with other conditions like heart problems.
Clinical Use Cases
The dosage for Esomeprazole + Itopride in clinical scenarios like Intubation, Surgical Procedures, Mechanical Ventilation, Intensive Care Unit (ICU) use and Emergency situations needs to be individualized based on patient’s condition, considering the use of intravenous administration of Esomeprazole if oral route isn’t feasible and using Itopride with caution in critical care settings.
Dosage Adjustments
Dose modifications based on individual patient-specific factors like renal/hepatic dysfunction, metabolic disorders, or genetic polymorphisms should be made cautiously and under careful monitoring.
Side Effects
Common Side Effects
Headache, diarrhea, nausea, abdominal pain, flatulence, constipation, dizziness, dry mouth, increased salivation.
Rare but Serious Side Effects
Severe allergic reactions (anaphylaxis), liver dysfunction, severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis), hypomagnesemia, blood disorders, cardiac arrhythmias.
Long-Term Effects
Osteoporosis, vitamin B12 deficiency.
Adverse Drug Reactions (ADR)
Clinically significant ADRs include those mentioned above under “Rare but Serious Side Effects.” These necessitate immediate intervention.
Contraindications
- Hypersensitivity to esomeprazole, itopride or any of the components of the formulation.
- Gastrointestinal bleeding, mechanical obstruction, or perforation.
- Concomitant use with nelfinavir (antiretroviral drug).
- Severe liver disease.
- Pregnancy and breastfeeding (use with caution and only if potential benefits outweigh the risks).
Drug Interactions
- Clopidogrel (reduced antiplatelet effect).
- Warfarin (altered coagulation parameters).
- Atazanavir, nelfinavir (decreased antiretroviral efficacy).
- Methotrexate (increased toxicity).
- Tacrolimus (increased levels).
- Diazepam (increased sedation).
- Citalopram, escitalopram (potential for QT prolongation).
- Anticholinergics (may counteract itopride’s prokinetic effects).
Interactions may also occur with over-the-counter drugs, supplements, and food (e.g., alcohol, grapefruit juice). Always obtain a thorough medication history.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Consult a healthcare professional. Limited data suggests potential risks to the fetus. Use only if the benefits clearly outweigh the risks.
- Data regarding drug excretion in breast milk is limited. Exercise caution or consider alternative options.
Drug Profile Summary
- Mechanism of Action: Esomeprazole inhibits gastric acid secretion, itopride enhances gastric motility.
- Side Effects: Headache, diarrhea, nausea, abdominal pain, dizziness. Rarely: severe allergic reactions, liver problems, hypomagnesemia.
- Contraindications: Hypersensitivity, GI bleeding/obstruction, nelfinavir use, severe liver disease.
- Drug Interactions: Clopidogrel, warfarin, atazanavir, methotrexate, diazepam, citalopram.
- Pregnancy & Breastfeeding: Use with caution; consult a physician.
- Dosage: Adults: 40 mg esomeprazole + 150 mg itopride once daily before meals.
- Monitoring Parameters: Liver function tests, magnesium levels (with long-term use), cardiac rhythm (in susceptible individuals).
Popular Combinations
- Esomeprazole + Itopride is itself a popular combination addressing both gastric acid secretion and motility issues.
Precautions
- Evaluate for allergies, hepatic/renal function, and concomitant medications.
- Use with caution in pregnancy/breastfeeding.
- Not recommended for children under 12.
- Monitor for magnesium levels and possible drug interactions.
- Advise patients about potential dizziness and avoid alcohol.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Esomeprazole + Itopride?
A: The standard adult dose is 40 mg esomeprazole and 150 mg itopride once daily before a meal. Dosage adjustments might be necessary for special populations.
Q2: Can Esomeprazole + Itopride be used in children?
A: Generally not recommended for children under 12, as safety and efficacy have not been established in this population.
Q3: What are the major contraindications for this drug?
A: Hypersensitivity, gastrointestinal bleeding/obstruction, concomitant use with nelfinavir, and severe liver disease.
Q4: How does Esomeprazole + Itopride interact with clopidogrel?
A: Esomeprazole can reduce the antiplatelet effect of clopidogrel, potentially increasing the risk of cardiovascular events.
Q5: Are there any long-term side effects associated with this combination?
A: Yes, long-term use of esomeprazole can lead to osteoporosis and vitamin B12 deficiency. Hypomagnesemia is also possible.
Q6: Can this medication be used during pregnancy or breastfeeding?
A: Limited data is available, suggesting potential risks. Use with caution and only when potential benefits outweigh the risks. Consult a doctor.
Q7: What lifestyle recommendations should be given to patients with GERD?
A: Advise patients to avoid trigger foods (spicy, fatty foods, chocolate, caffeine), eat smaller meals, maintain a healthy weight, and avoid lying down after eating.
Q8: What should be done in case of an overdose?
A: Supportive and symptomatic treatment should be provided. Contact a poison control center for guidance.
Q9: How does Itopride enhance gastric motility?
A: It inhibits acetylcholinesterase, increasing acetylcholine levels, and blocks dopamine D2 receptors, both leading to increased gastric motility.
