Usage
Dexrabeprazole + Levosulpiride is prescribed for the treatment of gastroesophageal reflux disease (GERD), acidity, heartburn, peptic ulcers (gastric and duodenal), dyspepsia, and irritable bowel syndrome (IBS). It is also used in the treatment of Zollinger-Ellison syndrome and Helicobacter pylori infection. This combination medication falls under the pharmacological classifications of proton pump inhibitor (PPI) and prokinetic agent.
Dexrabeprazole, a PPI, reduces stomach acid production by irreversibly blocking the H+/K+ ATPase enzyme system of gastric parietal cells. Levosulpiride, a prokinetic, increases gastrointestinal motility and tone, and prevents acid reflux by increasing the pressure of the lower esophageal sphincter.
Alternate Names
While “Dexrabeprazole + Levosulpiride” is the standard generic name, regional variations may exist. Brand names for this combination include Dexol L, Rabalkem LS, and Veloz L, among others.
How It Works
Pharmacodynamics: Dexrabeprazole inhibits the final step of gastric acid secretion, resulting in profound and sustained suppression of gastric acid production. Levosulpiride, as a prokinetic, enhances the tone and motility of the upper gastrointestinal tract, thus accelerating gastric emptying and transit time. It also acts as an antiemetic by antagonizing dopamine D2 receptors in the chemoreceptor trigger zone.
Pharmacokinetics: Dexrabeprazole is rapidly absorbed after oral administration, reaching peak plasma concentrations within 1-2 hours. It is extensively metabolized by the liver via CYP enzymes, primarily CYP2C19 and CYP3A4. Elimination occurs mainly through renal excretion. Levosulpiride is also well-absorbed orally, with peak plasma levels attained in approximately 1.5-2 hours. It undergoes limited hepatic metabolism and is primarily excreted unchanged in the urine.
Mode of Action: Dexrabeprazole binds to the H+/K+ ATPase enzyme in the apical membrane of gastric parietal cells, forming a disulfide bond and irreversibly inactivating the enzyme. This inhibits both basal and stimulated gastric acid secretion. Levosulpiride acts by increasing the release of acetylcholine in the myenteric plexus of the gastrointestinal tract, leading to increased motility. It also blocks dopamine D2 receptors, exerting antiemetic effects.
Elimination Pathways: Dexrabeprazole is eliminated primarily through renal excretion (approximately 90%), with the remaining 10% excreted in the feces. Levosulpiride is mainly excreted unchanged in the urine (approximately 66%), with about 20% excreted in the feces.
Dosage
Standard Dosage
Adults: The typical adult dose is one capsule containing Dexrabeprazole 10mg + Levosulpiride 75mg once daily, preferably before meals. Treatment duration varies depending on the condition, usually ranging from 4 to 8 weeks for GERD and peptic ulcers.
Children: The safety and efficacy of this combination have not been established in children, therefore it is not recommended for use in patients under 18 years of age.
Special Cases:
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Elderly Patients: Dose adjustment may be necessary in elderly patients due to potential age-related decline in renal and hepatic function.
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Patients with Renal Impairment: Dose adjustments should be made based on the degree of renal impairment.
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Patients with Hepatic Dysfunction: Use with caution and dose adjustment may be needed. Severe hepatic impairment is a contraindication.
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Patients with Comorbid Conditions: Consider individualizing the dose and closely monitoring patients with comorbid conditions, particularly cardiovascular diseases or a history of breast cancer.
Clinical Use Cases
Specific dosage recommendations for clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations are not generally established for this combination. In these settings, individual patient needs should guide the decision-making process.
Dosage Adjustments
Dose adjustments may be necessary for patients with renal/hepatic impairment. Close monitoring of electrolytes, particularly magnesium, is recommended during long-term therapy.
Side Effects
Common Side Effects:
Headache, nausea, vomiting, abdominal pain, diarrhea, dizziness, flatulence, constipation, weakness, sleepiness, flu-like symptoms, dry mouth, and infection.
Rare but Serious Side Effects:
Allergic reactions (rash, itching, swelling), gynecomastia (breast enlargement in males), galactorrhea (milk production unrelated to breastfeeding), extrapyramidal symptoms (movement disorders), cardiac arrhythmias (irregular heartbeat), hypomagnesemia (low magnesium), osteoporosis (weak and brittle bones), and liver dysfunction.
Long-Term Effects:
Osteoporosis and hypomagnesemia can occur with prolonged use.
Adverse Drug Reactions (ADR):
Severe allergic reactions, including anaphylaxis, and QT interval prolongation require immediate medical intervention.
Contraindications
Absolute contraindications include hypersensitivity to any component of the medication, gastrointestinal bleeding, mechanical obstruction, or perforation. Severe hepatic impairment is also contraindicated. Relative contraindications include pregnancy, breastfeeding, history of cardiac arrhythmias, pheochromocytoma, epilepsy, mania, and hypomagnesemia.
Drug Interactions
This combination can interact with several medications, including warfarin, methotrexate, digoxin, ketoconazole, itraconazole, atazanavir, nelfinavir, clopidogrel, iron supplements, and other drugs affecting the central nervous system. It may also interact with antacids containing aluminum or magnesium hydroxide, as they can decrease the absorption of dexrabeprazole.
Pregnancy and Breastfeeding
The safety of Dexrabeprazole + Levosulpiride during pregnancy and lactation has not been established. It is generally not recommended during pregnancy, and caution is advised during breastfeeding.
Drug Profile Summary
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Mechanism of Action: Dexrabeprazole: Proton pump inhibitor; Levosulpiride: Prokinetic and antiemetic.
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Side Effects: Headache, nausea, dizziness, diarrhea; rarely: allergic reactions, extrapyramidal symptoms, cardiac arrhythmias.
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Contraindications: Hypersensitivity, gastrointestinal bleeding/obstruction/perforation, severe hepatic impairment.
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Drug Interactions: Warfarin, methotrexate, digoxin, ketoconazole, itraconazole, others.
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Pregnancy & Breastfeeding: Not recommended during pregnancy; caution advised during breastfeeding.
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Dosage: Adults: Dexrabeprazole 10mg + Levosulpiride 75mg once daily before meals.
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Monitoring Parameters: Magnesium levels, liver function tests, cardiac function (ECG), and extrapyramidal symptoms.
Popular Combinations
While Dexrabeprazole + Levosulpiride itself is a common combination, in some cases it is used along with antibiotics for the eradication of H. pylori infection.
Precautions
Standard precautions include screening for allergies and pre-existing conditions. Alcohol should be avoided as it can exacerbate gastrointestinal issues and interact with levosulpiride. Caution with driving or operating machinery is advised due to potential dizziness and drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Dexrabeprazole + Levosulpiride?
A: The standard adult dosage is one capsule of Dexrabeprazole 10mg + Levosulpiride 75mg once daily, preferably before a meal. Dose adjustments may be necessary in elderly patients, and those with renal or hepatic impairment.
Q2: Can this medication be used in children?
A: No, its safety and effectiveness in children have not been established.
Q3: What are the common side effects?
A: Common side effects include headache, nausea, diarrhea, dizziness, and abdominal pain.
Q4: Are there any serious side effects?
A: Rare but serious side effects include allergic reactions, extrapyramidal symptoms, cardiac arrhythmias, and hypomagnesemia.
Q5: What are the contraindications?
A: Contraindications include hypersensitivity, gastrointestinal bleeding, obstruction or perforation, and severe liver disease.
Q6: Can pregnant or breastfeeding women take this medication?
A: It is not generally recommended during pregnancy. Caution should be exercised during breastfeeding.
Q7: What are the potential drug interactions?
A: This combination may interact with warfarin, methotrexate, digoxin, antifungals, and several other medications.
Q8: What precautions should be taken while using this drug?
A: Patients should avoid alcohol and be cautious when driving or operating machinery due to potential side effects like dizziness and drowsiness. Monitoring for hypomagnesemia during long-term therapy is important.
Q9: How does this combination work?
A: Dexrabeprazole reduces stomach acid production, while levosulpiride improves gastrointestinal motility and reduces acid reflux.
Q10: Is it safe to take this medication for a prolonged period?
A: Long-term use may increase the risk of osteoporosis and hypomagnesemia. Therefore, regular monitoring of these parameters is crucial during extended treatment.
