Usage
Ilaprazole + Levosulpiride is prescribed for the short-term treatment of gastroesophageal reflux disease (GERD), acidity, indigestion, heartburn, peptic ulcers (gastric and duodenal), functional dyspepsia, and other peptic disorders. It is particularly beneficial for patients who do not respond adequately to proton-pump inhibitors (PPIs) alone.
Pharmacological Classification:
- Ilaprazole: Proton Pump Inhibitor (PPI)
- Levosulpiride: Prokinetic agent, atypical antipsychotic
Mechanism of Action: This combination medication addresses both acid production and gut motility. Ilaprazole suppresses gastric acid secretion, while Levosulpiride promotes faster emptying of the stomach.
Alternate Names
This combination is marketed under various brand names like Iladac L, Blockcid L, and Ilapil LS. International and regional variations of the name may exist.
How It Works
Pharmacodynamics: Ilaprazole irreversibly binds to the H+/K+ ATPase enzyme (proton pump) in the parietal cells of the stomach, reducing gastric acid secretion. Levosulpiride is a dopamine D2 receptor antagonist, increasing acetylcholine release in the GI tract, which enhances gut motility and accelerates gastric emptying.
Pharmacokinetics:
- Ilaprazole: Metabolized primarily in the liver by CYP3A4 and CYP2C19 enzymes.
- Levosulpiride: Metabolized in the liver. Elimination pathways for both drugs are primarily hepatic, though some renal excretion may occur.
Dosage
Standard Dosage
Adults: One capsule/tablet of Ilaprazole (10mg) + Levosulpiride (75mg) orally, preferably one hour before a meal, usually in the morning. The treatment duration depends on the patient’s response and clinical condition, as determined by the physician.
Children: Generally not recommended for children under 14 years old due to limited safety and efficacy data.
Special Cases:
- Elderly Patients: Use with caution due to increased risk of side effects (e.g., elevated prolactin levels, bone fractures). Dosage adjustments may be necessary.
- Patients with Renal Impairment: Exercise caution. Dose adjustment may be needed based on creatinine clearance.
- Patients with Hepatic Dysfunction: Use with caution. Dose adjustments may be necessary due to impaired metabolism.
- Patients with Comorbid Conditions: Evaluate carefully, especially in patients with a history of gastrointestinal bleeding, intestinal obstruction, osteoporosis, hypomagnesemia, pheochromocytoma, epilepsy, mania, or Clostridium difficile-associated diarrhea.
Clinical Use Cases
Dosage in specific clinical settings (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations) should be individualized based on patient needs and should adhere to standard adult dosing with adjustments as needed. There are no fixed protocols using Ilaprazole + Levosulpiride in these settings.
Dosage Adjustments:
Dosage modification should be considered based on individual patient characteristics like renal/hepatic function, other metabolic disorders, or genetic polymorphisms affecting drug metabolism. Always prioritize patient safety and tailor the dosage accordingly.
Side Effects
Common Side Effects:
Headache, nausea, vomiting, gas, dry mouth, dizziness, diarrhea, fatigue.
Rare but Serious Side Effects:
Neuroleptic Malignant Syndrome (NMS), Extrapyramidal Symptoms (EPS), tardive dyskinesia, hyperprolactinemia (especially with Levosulpiride).
Long-Term Effects:
Osteoporosis, hypomagnesemia, vitamin B12 deficiency (with long-term PPI use).
Adverse Drug Reactions (ADR):
Any signs of NMS (fever, muscle rigidity, altered mental status), severe EPS, or allergic reactions require immediate medical attention.
Contraindications
Hypersensitivity to either drug, gastrointestinal hemorrhage or mechanical obstruction, prolactin-dependent tumors (e.g., prolactinoma), pheochromocytoma.
Drug Interactions
Ilaprazole can interact with drugs metabolized by CYP3A4 and CYP2C19. Levosulpiride can interact with drugs affecting dopamine levels. Avoid concomitant use with:
- Ketoconazole, Itraconazole, Posaconazole
- Erlotinib
- Warfarin, Phenprocoumon
- Atazanavir
- Methotrexate
- Fluvoxamine
- Rifampicin
- St. John’s Wort
- Antipsychotics (e.g., Chlorpromazine, Haloperidol)
- Antidepressants (e.g., Fluoxetine, Sertraline)
- Dopamine agonists (e.g., Levodopa, Bromocriptine)
- Antihypertensives (e.g., Methyldopa, Clonidine)
- Alcohol
Pregnancy and Breastfeeding
Pregnancy: Consult a physician. Use only if the benefits clearly outweigh the risks. Pregnancy Safety Category C (Levosulpiride).
Breastfeeding: The drugs can pass into breast milk. Consult a physician before use.
Drug Profile Summary
- Mechanism of Action: Ilaprazole reduces gastric acid; Levosulpiride enhances GI motility.
- Side Effects: Headache, nausea, dizziness, diarrhea, EPS, NMS (rare).
- Contraindications: Hypersensitivity, GI bleeding, prolactin-dependent tumors.
- Drug Interactions: Azole antifungals, Warfarin, Methotrexate, several others.
- Pregnancy & Breastfeeding: Consult a doctor before use.
- Dosage: 10mg Ilaprazole + 75mg Levosulpiride once daily before a meal.
- Monitoring Parameters: Magnesium levels, bone density (with long-term use), prolactin levels.
Popular Combinations
Information on popular combinations not found in the provided sources.
Precautions
- General Precautions: Pre-screening for allergies, metabolic disorders, and organ dysfunction is essential.
- Specific Populations: Use with caution in pregnant/breastfeeding women, children, and the elderly.
- Lifestyle Considerations: Avoid alcohol and smoking. Caution while driving or operating machinery due to potential drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ilaprazole + Levosulpiride?
A: The standard adult dose is 10mg Ilaprazole + 75mg Levosulpiride once daily before a meal. Adjustments may be necessary for elderly patients and those with renal or hepatic impairment. Not generally recommended for children under 14.
Q2: What are the primary uses of this combination?
A: It’s primarily prescribed for GERD, peptic ulcers, functional dyspepsia, and other acid-related disorders, particularly in cases where PPIs alone are insufficient.
Q3: What is the difference between Ilaprazole and Levosulpiride?
A: Ilaprazole is a PPI that reduces acid production, while Levosulpiride is a prokinetic agent that improves gastric emptying. Their combined effect provides broader symptom relief.
Q4: Are there any serious side effects I should be aware of?
A: While generally well-tolerated, rare but serious side effects like Neuroleptic Malignant Syndrome (NMS) and Extrapyramidal Symptoms (EPS) can occur, requiring immediate medical intervention.
Q5: Can this medication be used during pregnancy or breastfeeding?
A: It’s crucial to consult a physician before using this medication during pregnancy or while breastfeeding, as the drugs can cross the placenta and are excreted in breast milk.
Q6: What are the common drug interactions with Ilaprazole + Levosulpiride?
A: It can interact with various medications, including antifungals, anticoagulants, some antibiotics, and certain antipsychotics. Provide a comprehensive medication list to your physician to assess potential interactions.
Q7: What precautions should patients take while on this medication?
A: Patients should avoid alcohol and smoking, exercise caution when driving, and inform their doctor about any pre-existing medical conditions or other medications they are taking.
Q8: What should I do if a dose is missed?
A: Take the missed dose as soon as remembered unless it’s close to the next scheduled dose. Do not double the dose to catch up.
Q9: Can long-term use of this medication cause any problems?
A: Long-term PPI use has been associated with an increased risk of osteoporosis, hypomagnesemia, and vitamin B12 deficiency. Regular monitoring is recommended for patients on prolonged therapy.
