Usage
- Levosulpiride + Rabeprazole is prescribed for the treatment of gastroesophageal reflux disease (GERD), acidity, heartburn, peptic ulcers (duodenal and gastric ulcers), Zollinger-Ellison syndrome, Helicobacter pylori infection, irritable bowel syndrome (IBS), functional dyspepsia, and to improve regurgitation. It may also offer benefits for non-erosive reflux disease (NERD).
- Pharmacological Classification: This is a combination drug containing a proton pump inhibitor (PPI) and a prokinetic agent.
- Mechanism of Action: Rabeprazole inhibits gastric acid secretion by irreversibly blocking the H+/K+-ATPase enzyme system (proton pump) in parietal cells of the stomach. Levosulpiride, a prokinetic, enhances gastrointestinal motility and accelerates gastric emptying by increasing acetylcholine release and antagonizing dopamine D2 receptors. This combined action reduces acid reflux and improves digestive function.
Alternate Names
- No widely recognized alternate names exist for this combination product itself. However, the individual components have various names. Rabeprazole sodium is the active form of Rabeprazole. Levosulpiride is sometimes referred to as Levosulpride.
- Brand Names: This combination is marketed under various brand names like Rablet L, Domat LSR, Cyra LS, Amalgard LSR, Kritcid-L, Inreap-LSR and others. Brand names may vary regionally.
How It Works
- Pharmacodynamics: Rabeprazole suppresses gastric acid secretion. Levosulpiride enhances gastric motility and accelerates gastric emptying. It also increases lower esophageal sphincter pressure, preventing reflux.
- Pharmacokinetics: Rabeprazole is absorbed rapidly after oral administration and metabolized by the liver (CYP450 enzymes, primarily CYP2C19). Levosulpiride is also absorbed orally, with limited hepatic metabolism and predominantly renal excretion.
- Mode of Action: Rabeprazole binds to the proton pump, inhibiting the final step of acid secretion. Levosulpiride antagonizes dopamine D2 receptors and facilitates acetylcholine release, enhancing gastrointestinal motility.
- Elimination Pathways: Rabeprazole is primarily eliminated through hepatic metabolism, while Levosulpiride is mainly excreted renally.
Dosage
Standard Dosage
Adults:
- The standard dose is one capsule of Rabeprazole 20 mg + Levosulpiride 75 mg once daily, taken at least 30 minutes before a meal, preferably in the morning. The duration of treatment depends on the condition.
Children:
- This combination is generally not recommended for children as its safety and effectiveness have not been established in pediatric populations.
Special Cases:
- Elderly Patients: Dosage adjustments may be necessary based on renal function.
- Patients with Renal Impairment: Dose reduction is required for severe renal dysfunction.
- Patients with Hepatic Dysfunction: Caution should be exercised in patients with hepatic impairment, and dose adjustments may be needed.
- Patients with Comorbid Conditions: Caution is advisable in patients with cardiovascular diseases, electrolyte imbalances (hypomagnesemia), psychiatric disorders, or a history of seizures. Dose adjustments and close monitoring may be necessary.
Clinical Use Cases
- Dosing for specific clinical situations like intubation, surgical procedures, mechanical ventilation, or ICU use varies and should be determined on a case-by-case basis by the attending physician, considering patient factors and the specific context.
- Emergency Situations: This combination is not typically used in emergency situations like status epilepticus or cardiac arrest.
Dosage Adjustments
- Dose modifications may be needed in patients with renal or hepatic impairment, based on individual patient parameters and clinical response.
Side Effects
Common Side Effects:
- Headache, dizziness, nausea, diarrhea, abdominal pain, constipation, flatulence, asthenia (weakness), and flu-like symptoms.
Rare but Serious Side Effects:
- Severe allergic reactions (anaphylaxis), Stevens-Johnson syndrome, toxic epidermal necrolysis, pancreatitis, hypomagnesemia, Clostridium difficile-associated diarrhea, cardiac arrhythmias (QT interval prolongation), extrapyramidal symptoms (movement disorders), gynecomastia (breast enlargement in males), galactorrhea (abnormal milk production), menstrual irregularities.
Long-Term Effects:
- Osteoporosis, vitamin B12 deficiency, and hypomagnesemia are potential complications of long-term use.
Adverse Drug Reactions (ADR):
- Any signs of severe allergic reactions, hepatic dysfunction, severe skin reactions, cardiac events, or neurological symptoms should prompt immediate medical attention.
Contraindications
- Hypersensitivity to rabeprazole, levosulpiride, substituted benzamides, or any components of the formulation.
- Gastrointestinal bleeding, mechanical gastrointestinal obstruction, prolactinoma, pheochromocytoma, epilepsy, and severe hepatic impairment.
- Pregnancy and breastfeeding (unless benefits outweigh the risks).
Drug Interactions
- Antacids (containing aluminum and magnesium hydroxide), ketoconazole, itraconazole, atazanavir, nelfinavir, digoxin, warfarin, methotrexate, tacrolimus, mycophenolate mofetil, sucralfate, cisapride.
- CYP450 interactions: Rabeprazole is metabolized by CYP2C19. Avoid concomitant use with strong CYP2C19 inhibitors.
- Alcohol should be avoided, as it may exacerbate GERD symptoms and increase the risk of adverse effects.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: There is limited data on the use of this combination in pregnancy. It is generally avoided unless the benefits clearly outweigh potential risks to the fetus.
- Breastfeeding: This combination may pass into breast milk. Use caution and consider the potential risks to the infant.
Drug Profile Summary
- Mechanism of Action: Rabeprazole inhibits gastric acid secretion. Levosulpiride improves gastric motility.
- Side Effects: Headache, dizziness, nausea, diarrhea, abdominal pain. Rarely: severe allergic reactions, extrapyramidal symptoms.
- Contraindications: Hypersensitivity, GI bleeding/obstruction, prolactinoma, pheochromocytoma, epilepsy, severe hepatic impairment.
- Drug Interactions: Antacids, antifungals, digoxin, warfarin, methotrexate, immunosuppressants.
- Pregnancy & Breastfeeding: Generally avoided.
- Dosage: 20 mg Rabeprazole + 75 mg Levosulpiride once daily before meals.
- Monitoring Parameters: Liver function tests, renal function tests, magnesium levels, complete blood count (especially with prolonged use), and cardiac monitoring (ECG in patients at risk for arrhythmias) if clinically indicated.
Popular Combinations
- Rabeprazole is often combined with antibiotics (e.g., amoxicillin, clarithromycin) for the eradication of H. pylori.
Precautions
- Evaluate for underlying medical conditions, including renal and hepatic function, before starting treatment.
- Close monitoring is necessary in patients with cardiovascular or psychiatric conditions.
- Advise patients to avoid alcohol and driving if experiencing drowsiness or dizziness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Levosulpiride + Rabeprazole?
A: The usual dose is one capsule (20 mg Rabeprazole + 75 mg Levosulpiride) daily, 30 minutes before a meal. Dosage may be adjusted based on the individual’s condition and response to therapy.
Q2: Can this combination be used in children?
A: It is generally not recommended for pediatric patients due to limited safety and efficacy data.
Q3: What are the common side effects?
A: Common side effects include headache, dizziness, nausea, diarrhea, and abdominal pain.
Q4: Are there any serious side effects to be aware of?
A: Yes, rare but serious side effects include severe allergic reactions, heart rhythm problems, and movement disorders.
Q5: What are the contraindications for this drug?
A: Contraindications include hypersensitivity, gastrointestinal bleeding/obstruction, pheochromocytoma, and severe liver disease.
Q6: Can I take this medication while pregnant or breastfeeding?
A: It’s generally avoided during pregnancy and breastfeeding due to limited safety information. Consult with a doctor.
Q7: How does this combination interact with other medications?
A: It can interact with several medications, including antacids, antifungals, and certain heart medications. Provide a complete medication list to your doctor.
Q8: What precautions should I advise my patients to take while on this medication?
A: Patients should avoid alcohol, be cautious when driving, and report any unusual symptoms immediately.
Q9: How long should a patient take this combination?
A: The duration of treatment varies depending on the condition being treated. The prescribing physician should determine the appropriate length of therapy.
Q10: Should I monitor any specific lab parameters while a patient is on this drug?
A: Monitoring may include liver and kidney function tests, magnesium levels, and complete blood counts, especially with long-term use. Cardiac monitoring (ECG) might be necessary in specific cases.
