Usage
- Levosulpiride + Pantoprazole 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 also addresses acidity, indigestion, heartburn, peptic ulcers, and functional dyspepsia. GERD occurs when stomach acid flows back into the esophagus, causing irritation and heartburn. Peptic ulcers are sores in the lining of the stomach or intestine. Functional dyspepsia involves persistent indigestion with no clear organic cause.
- Pharmacological Classification: This combination drug includes a proton pump inhibitor (Pantoprazole) and a prokinetic agent (Levosulpiride).
- Mechanism of Action: Pantoprazole inhibits gastric acid secretion by blocking the H+/K+ ATPase enzyme system in gastric parietal cells. Levosulpiride is a dopamine D2 receptor antagonist that enhances gastrointestinal motility and accelerates gastric emptying. It also acts as a 5-HT4 receptor agonist.
Alternate Names
- No widely recognized alternate names exist for this specific drug combination.
- Brand Names: Pansec L, Pantostrum LS, P-PPi-L, Pan-L.
How It Works
- Pharmacodynamics: Pantoprazole suppresses gastric acid secretion, while Levosulpiride increases gastrointestinal motility, leading to faster emptying of the stomach. Levosulpiride’s action on 5-HT4 receptors also contributes to its therapeutic effect by reducing nausea and vomiting.
- Pharmacokinetics: Pantoprazole is rapidly absorbed after oral administration. It’s metabolized primarily in the liver by CYP450 enzymes (mainly CYP2C19 and CYP3A4). Elimination is primarily through renal excretion of metabolites. Levosulpiride is also absorbed orally. It’s metabolized to a lesser extent than Pantoprazole and excreted primarily through the kidneys.
- Mode of Action: Pantoprazole irreversibly binds to the H+/K+ ATPase pump, thereby inhibiting gastric acid secretion. Levosulpiride, as a D2 receptor antagonist, blocks dopamine’s inhibitory effect on gastrointestinal motility, promoting contractions and faster emptying. Its 5-HT4 receptor agonism enhances this effect.
- Receptor Binding, Enzyme Inhibition: Pantoprazole acts through enzyme inhibition (H+/K+ ATPase), while Levosulpiride binds to dopamine D2 and 5-HT4 receptors.
- Elimination Pathways: Pantoprazole is primarily eliminated renally after hepatic metabolism, while Levosulpiride is predominantly excreted renally with less extensive metabolism.
Dosage
Standard Dosage
Adults:
One capsule containing 40 mg Pantoprazole and 75 mg Levosulpiride is administered orally once daily, typically before a meal. Treatment duration is usually 4 to 8 weeks, but can be extended based on the individual’s response and medical condition.
Children:
This drug combination’s safety and efficacy haven’t been established in children, so its use is generally avoided in this population.
Special Cases:
- Elderly Patients: Exercise caution in elderly patients, especially with renal impairment. Dose adjustments may be needed. Monitor for postural hypotension and extrapyramidal side effects.
- Patients with Renal Impairment: Use with caution in mild to moderate renal impairment. Dose/dosage frequency reduction may be needed. Contraindicated in severe renal impairment.
- Patients with Hepatic Dysfunction: Pantoprazole dose should not exceed 20 mg daily in severe hepatic impairment. Avoid Levosulpiride due to lack of sufficient information.
- Patients with Comorbid Conditions: Exercise caution in patients with a history of cardiac arrhythmias, psychiatric disorders, or long-term use due to potential risk for osteoporosis and hypomagnesemia.
Clinical Use Cases
The dosage information provided primarily focuses on the treatment of GERD and dyspepsia. Information on dosage in specific clinical use cases such as intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations is not found in the provided sources.
Dosage Adjustments
Dose adjustments may be necessary in patients with renal or hepatic impairment. Elderly patients might also require adjustments.
Side Effects
Common Side Effects
Headache, diarrhea, nausea, abdominal pain, vomiting, flatulence, joint pain, dizziness, dry mouth.
Rare but Serious Side Effects
Neuroleptic malignant syndrome, extrapyramidal symptoms (dyskinesia, dystonia), QT prolongation, hypomagnesemia, osteoporosis.
Long-Term Effects
Osteoporosis, hypomagnesemia, vitamin B12 deficiency.
Adverse Drug Reactions (ADR)
Hypersensitivity reactions, Stevens-Johnson syndrome.
Contraindications
Hypersensitivity to Pantoprazole, Levosulpiride, or any component of the formulation, gastrointestinal bleeding, intestinal obstruction, severe renal impairment, severe hepatic impairment, pheochromocytoma, prolactinoma, concomitant use of levodopa or other antiparkinsonian drugs, concurrent use with rilpivirine-containing products.
Drug Interactions
- Pantoprazole interacts with drugs metabolized by CYP450 enzymes, such as ketoconazole, itraconazole, warfarin, and phenprocoumon. It can also affect the absorption of drugs like ketoconazole and itraconazole. Levosulpiride interacts with drugs that prolong the QT interval, such as certain antiarrhythmics and antipsychotics. It can also interact with alcohol and levodopa.
- CYP450 Interactions: Pantoprazole is primarily metabolized by CYP2C19 and CYP3A4, and it can inhibit these enzymes, affecting the metabolism of other drugs.
- Interactions with Commonly Prescribed Medications: Avoid concomitant use with ketoconazole, itraconazole, warfarin, phenprocoumon, levodopa, medications that prolong the QT interval.
- Over-the-Counter (OTC) drugs and supplements: Avoid concurrent use with antacids containing aluminum hydroxide and magnesium hydroxide, as they may interfere with the absorption of Pantoprazole.
- Food and lifestyle factors: Avoid alcohol consumption as it can worsen GERD symptoms and interact with Levosulpiride.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: This combination is contraindicated during pregnancy due to potential risks to the fetus.
- Breastfeeding: This combination is contraindicated while breastfeeding. Both drugs can pass into breast milk and may harm the infant.
Drug Profile Summary
- Mechanism of Action: Pantoprazole inhibits gastric acid secretion; Levosulpiride enhances gastric motility.
- Side Effects: Headache, diarrhea, nausea, dizziness, dry mouth; rarely, extrapyramidal symptoms, QT prolongation.
- Contraindications: Hypersensitivity, GI bleeding, severe renal/hepatic impairment, pheochromocytoma, prolactinoma, concomitant use with levodopa or rilpivirine-containing products.
- Drug Interactions: Ketoconazole, itraconazole, warfarin, phenprocoumon, levodopa, QT-prolonging drugs.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: 40 mg Pantoprazole + 75 mg Levosulpiride once daily before a meal.
- Monitoring Parameters: Liver function tests, magnesium levels, bone density (with long-term use), ECG (for QT prolongation).
Popular Combinations
This specific drug combination is itself considered a popular and readily available formulation for managing GERD and dyspepsia, and further combinations building on it are not mentioned in the sources.
Precautions
- General Precautions: Evaluate patients for pre-existing medical conditions like renal/hepatic impairment, cardiac arrhythmias, and psychiatric disorders.
- Specific Populations:
- Pregnant Women: Contraindicated.
- Breastfeeding Mothers: Contraindicated.
- Children & Elderly: Avoid use in children; use cautiously in elderly patients with dose adjustments as needed.
- Lifestyle Considerations: Avoid alcohol consumption; caution while driving or operating machinery due to potential dizziness or drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Levosulpiride + Pantoprazole?
A: The standard adult dosage is 40 mg Pantoprazole + 75 mg Levosulpiride, taken orally once daily, usually before a meal.
Q2: Can this combination be used in children?
A: No, the safety and efficacy haven’t been established in children.
Q3: What are the common side effects?
A: Common side effects include headache, diarrhea, nausea, abdominal pain, dizziness, and dry mouth.
Q4: What are the serious side effects I should watch out for?
A: Look for signs of neuroleptic malignant syndrome, extrapyramidal symptoms, and QT prolongation.
Q5: Are there any drug interactions I should be aware of?
A: Yes, this medication can interact with several drugs like ketoconazole, itraconazole, warfarin, levodopa, and drugs that prolong the QT interval.
Q6: Can I take this medication during pregnancy or while breastfeeding?
A: No, it’s contraindicated in both pregnancy and breastfeeding.
Q7: What precautions are necessary for elderly patients?
A: Dose adjustments may be needed and careful monitoring for side effects like postural hypotension and extrapyramidal symptoms is important.
Q8: What should patients with liver problems do?
A: Patients with severe liver impairment should not exceed 20 mg of Pantoprazole per day, and Levosulpiride should generally be avoided.
Q9: What should patients with kidney problems do?
A: The combination should be used with caution in patients with mild to moderate kidney issues, and dose adjustments may be necessary. It’s contraindicated in severe kidney disease.
Q10: What if a patient misses a dose?
A: If a dose is missed, take it as soon as remembered unless it’s close to the next scheduled dose. Do not double the dose to catch up.
