Usage
Esomeprazole + Levosulpiride is prescribed for the treatment of gastroesophageal reflux disease (GERD), particularly in patients who haven’t responded well to a proton pump inhibitor (PPI) alone. It is also used to treat other acid-related disorders like peptic ulcers and dyspepsia.
Pharmacological Classification:
- Esomeprazole: Proton Pump Inhibitor (PPI)
- Levosulpiride: Prokinetic agent, Dopamine D2 receptor antagonist
Mechanism of Action:
This combination drug works through two distinct mechanisms:
- Esomeprazole inhibits the H+/K+ ATPase pump in gastric parietal cells, thus reducing gastric acid secretion.
- Levosulpiride increases acetylcholine release and improves gastrointestinal motility, aiding in faster gastric emptying.
Alternate Names
While there isn’t a universally recognized alternate name, the drug may be referred to by the generic names of its components. Some possible ways to refer to this combination include:
- Esomeprazole/Levosulpiride
- Levosulpiride/Esomeprazole
- Esomeprazole magnesium + Levosulpiride
Brand Names: Some popular brand names include Esomac L, Esomeprazole and Levosulpiride Tablets and others.
How It Works
Pharmacodynamics:
- Esomeprazole: Suppresses gastric acid secretion by irreversibly binding to the proton pump.
- Levosulpiride: Enhances gastric motility and improves the pressure of the lower esophageal sphincter.
Pharmacokinetics:
- Esomeprazole: Absorbed in the small intestine, metabolized by the liver (CYP2C19 and CYP3A4 enzymes), and excreted primarily through the kidneys.
- Levosulpiride: Absorbed in the gastrointestinal tract, minimal hepatic metabolism, eliminated primarily by the kidneys.
Mode of Action:
- Esomeprazole: Inhibits the final step of gastric acid production by blocking the H+/K+ ATPase pump, which exchanges potassium for hydrogen ions across parietal cell membranes.
- Levosulpiride: Acts as a dopamine D2 receptor antagonist in the gastrointestinal tract, enhancing acetylcholine release, thus increasing peristalsis and improving gastric emptying.
Elimination: Via renal/hepatic excretion.
Dosage
Standard Dosage
Adults:
The usual dose is one capsule (40mg Esomeprazole + 75mg Levosulpiride) once daily, taken orally on an empty stomach, preferably an hour before meals. Treatment duration is typically 4-8 weeks but depends on the specific condition.
Children:
This combination is generally not recommended for use in children below 18 years as its safety and efficacy have not been established in this population.
Special Cases:
- Elderly Patients: Exercise caution. Dose adjustments may be needed in patients with renal impairment. Elderly patients are more susceptible to side effects like postural hypotension, sedation, and extrapyramidal symptoms.
- Patients with Renal Impairment: Use with caution in mild to moderate renal impairment; dose reduction might be necessary. Contraindicated in severe renal impairment.
- Patients with Hepatic Dysfunction: Avoid in patients with hepatic impairment as a precautionary measure.
- Patients with Comorbid Conditions: Specific adjustments may be required for patients with certain comorbidities like diabetes or cardiovascular disease. Consult a physician for personalized guidance.
Clinical Use Cases
The use of Esomeprazole + Levosulpiride is primarily focused on GERD management. Its use in the specific clinical settings you mentioned (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations) is not specifically indicated. Other medications are preferred for gastric acid suppression in these situations.
Dosage Adjustments
Dose adjustments are necessary based on patient-specific factors like renal/hepatic dysfunction.
Side Effects
Common Side Effects:
Headache, abdominal pain, diarrhea, constipation, nausea, vomiting, flatulence, dry mouth, dizziness, rash, pruritus, somnolence, breast pain/tenderness.
Rare but Serious Side Effects:
Severe allergic reactions, extrapyramidal symptoms (movement disorders), cardiac arrhythmias, and hypomagnesemia (low magnesium).
Long-Term Effects:
Long-term PPI use might be associated with an increased risk of bone fractures, Clostridium difficile infection, vitamin B12 deficiency, and fundic gland polyps.
Adverse Drug Reactions (ADR):
Any severe or unusual side effects, like angioedema or Stevens-Johnson syndrome, should be reported immediately.
Contraindications
- Hypersensitivity to Esomeprazole, Levosulpiride, or substituted benzimidazoles.
- Concurrent use of rilpivirine.
- Gastrointestinal bleeding, mechanical obstruction, or perforation.
- Severe renal or hepatic impairment.
- Phaeochromocytoma, pituitary prolactinoma, breast cancer.
- Epilepsy, mania.
- Concurrent use of levodopa or other antiparkinson drugs.
- Pregnancy and breastfeeding
Drug Interactions
Esomeprazole + Levosulpiride can interact with numerous medications, including:
- Painkillers: Aspirin, Naproxen
- Anti-HIV: Atazanavir, Nelfinavir
- Blood thinners: Clopidogrel, Warfarin, Cilostazol
- Antifungals: Ketoconazole, Itraconazole, Voriconazole
- Anticancer: Erlotinib, Methotrexate
- Antidepressants: Citalopram, Imipramine, Clomipramine, Duloxetine
- Antianxiety: Diazepam
- Anticonvulsants: Phenytoin
- Gastroprokinetic agents: Cisapride
- Cardiac medications: Digoxin
- Immunosuppressants: Tacrolimus
- Antituberculosis: Rifampicin
It may also interact with OTC drugs and supplements. Alcohol should be avoided, as it can worsen drowsiness and increase stomach acid production.
Pregnancy and Breastfeeding
This combination is not recommended for use during pregnancy and breastfeeding.
Drug Profile Summary
- Mechanism of Action: Esomeprazole inhibits gastric acid secretion; Levosulpiride enhances gastrointestinal motility.
- Side Effects: Headache, abdominal pain, diarrhea, constipation, nausea, vomiting. Rare but serious effects: extrapyramidal symptoms.
- Contraindications: Hypersensitivity, severe renal/hepatic impairment, gastrointestinal bleeding, pregnancy, breastfeeding.
- Drug Interactions: Interacts with multiple drugs including Warfarin, Diazepam and Ketoconazole.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: Usually, one capsule (40mg/75mg) once daily before meals.
- Monitoring Parameters: Renal and liver function, magnesium levels, signs of C. difficile infection, vitamin B12 levels.
Popular Combinations
While Esomeprazole + Levosulpiride itself is a combination, sometimes other medications for H. pylori eradication may be added. Such additions should be done with caution and after careful consideration of potential interactions.
Precautions
Screen for allergies, metabolic disorders, and organ dysfunction before prescribing. Consider age-specific precautions for children and the elderly (although it is not recommended for children under 18). Advise against driving if dizziness or blurred vision occurs. Caution patients to limit alcohol intake due to increased drowsiness and potential for worsening stomach acid production.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Esomeprazole + Levosulpiride?
A: The standard adult dose is 40mg Esomeprazole and 75mg Levosulpiride, taken as a single capsule once daily before a meal. It is not recommended for children under 18.
Q2: How does this combination work differently than Esomeprazole alone?
A: Esomeprazole reduces acid production, while Levosulpiride improves gastric motility and emptying. Combining them can be more effective for GERD than just reducing acid.
Q3: What are the main contraindications for this medication?
A: Contraindications include hypersensitivity, severe renal/hepatic impairment, gastrointestinal bleeding, pregnancy, breastfeeding, certain tumors (phaeochromocytoma, prolactinoma), and concurrent use of certain medications like rilpivirine and levodopa.
Q4: Are there any long-term risks associated with Esomeprazole + Levosulpiride?
A: Long-term use of PPIs like Esomeprazole can be associated with increased risks of bone fractures, C. difficile infection, vitamin B12 deficiency, and fundic gland polyps.
Q5: Can patients with renal impairment take this medication?
A: Use with caution in mild to moderate renal impairment with potential dose reduction; contraindicated in severe renal impairment.
Q6: What should I advise my patient regarding diet and lifestyle?
A: Patients should be advised to follow a healthy diet and limit alcohol intake, which can worsen GERD symptoms.
Q7: What are the most important drug interactions to be aware of?
A: Esomeprazole + Levosulpiride can interact with many drugs, including warfarin, diazepam, ketoconazole, certain antibiotics, and anti-HIV medications. Always review a patient’s full medication list.
A: Common side effects include headache, abdominal pain, diarrhea, constipation, nausea, and vomiting. Inform patients about the potential for rare but severe side effects, such as extrapyramidal symptoms, and to seek immediate medical attention if these occur.
Q9: Is it safe to prescribe this medication during pregnancy?
A: No, this medication is not recommended during pregnancy and breastfeeding.
Q10: How should I monitor a patient on this medication?
A: Monitor renal and liver function, magnesium levels, signs of C. difficile infection, and vitamin B12 levels, especially with long-term use. Observe the patient for any new or worsening gastrointestinal symptoms.
