Dimethicone + Levosulpiride

Usage

This combination medication is prescribed for gastrointestinal issues, primarily functional dyspepsia (indigestion) and constipation. It addresses symptoms like nausea, vomiting, bloating, fullness, and difficulty passing stools. It can also be used to treat gastroesophageal reflux disease (GERD) and Irritable Bowel Syndrome (IBS). In some cases, it is used to manage some psychiatric conditions like schizophrenia and depression at lower doses.

• Pharmacological Classification: Antidyspeptic (Levosulpiride) and Antiflatulent (Dimethicone).

• Mechanism of Action: Levosulpiride, a prokinetic, increases acetylcholine release, stimulating gastrointestinal motility and reducing gastric reflux. Dimethicone, an antifoaming agent, reduces the surface tension of gas bubbles in the gut, facilitating their passage.

Alternate Names

• Levosulpiride + Dimethicone/Polydimethylsiloxane
• Neopride MPS (Brand name)

How It Works

• Pharmacodynamics: Levosulpiride acts as a prokinetic by increasing acetylcholine release, which enhances gastrointestinal motility and decreases gastric reflux. Dimethicone reduces the surface tension of gas bubbles, promoting their coalescence and expulsion. Levosulpiride can also act on dopamine receptors in the central nervous system, producing antiemetic and mood-altering effects.

• Pharmacokinetics:

  • Levosulpiride: Absorbed orally, metabolized in the liver, and primarily excreted in urine.
  • Dimethicone: Not absorbed systemically; passes through the GI tract unchanged and is eliminated in feces.

• Mode of Action: Levosulpiride increases gastrointestinal motility. Dimethicone defoams gas bubbles present in the gut. This combined action reduces surface tension and hence improves symptoms of gas and bloating.

• Receptor binding, enzyme inhibition, or neurotransmitter modulation: Levosulpiride primarily acts as a dopamine D2 receptor antagonist in the central and peripheral nervous systems. This action influences acetylcholine release and affects gastrointestinal motility.

• Elimination pathways: Levosulpiride is metabolized in the liver and excreted primarily in the urine. Dimethicone is not absorbed systemically and is eliminated unchanged in the feces.

Dosage

Standard Dosage

Adults:

One tablet (Levosulpiride 25mg + Dimethicone 125mg) three times a day, taken orally before meals. Some sources recommend bedtime administration for constipation. This dosage may require adjustments based on individual factors.

Children:

Safety and effectiveness for children under 14 years old have not been established. Use is generally not recommended. Some off-label pediatric use of just dimethicone exists for flatulence, but even this is not generally recommended for children under two.

Special Cases:

• Elderly Patients: Dose reduction may be necessary due to the increased risk of postural hypotension, sedation, and extrapyramidal effects.
• Patients with Renal Impairment: Dosage adjustments are required for moderate to severe renal impairment. Consult a nephrologist for appropriate recommendations.
• Patients with Hepatic Dysfunction: Caution is advised. Dosage adjustments may be needed based on the severity of impairment.
• Patients with Comorbid Conditions: Use with caution in patients with heart disease (especially those with QTc prolongation risk factors), epilepsy, history of cerebrovascular events, pheochromocytoma, gastrointestinal hemorrhage, mechanical obstruction, or perforation.

Clinical Use Cases

This combination of Dimethicone and Levosulpiride is not typically indicated for Intubation, Surgical Procedures, Mechanical Ventilation, Intensive Care Unit (ICU) use, or Emergency Situations.

Dosage Adjustments

Modifications may be necessary based on renal/hepatic dysfunction, metabolic disorders, or genetic polymorphisms affecting drug metabolism.

Side Effects

Common Side Effects:

Headache, fatigue, drowsiness, constipation, extrapyramidal symptoms (e.g., tremors, muscle stiffness), increased prolactin levels.

Rare but Serious Side Effects:

Neuroleptic malignant syndrome (NMS), characterized by high fever, muscle rigidity, altered mental status, and autonomic dysfunction; cardiac arrhythmias (QT prolongation).

Long-Term Effects:

Tardive dyskinesia (involuntary, repetitive movements), hyperprolactinemia (can lead to galactorrhea, amenorrhea, and sexual dysfunction).

Adverse Drug Reactions (ADR):

Any signs of NMS, severe extrapyramidal symptoms, allergic reactions, and significant QTc prolongation require immediate medical attention.

Contraindications

Hypersensitivity to Levosulpiride or Dimethicone; gastrointestinal bleeding, mechanical obstruction, or perforation; pheochromocytoma; prolactin-dependent tumors (e.g., pituitary prolactinoma); Parkinson’s disease; epilepsy; severe renal or hepatic impairment; pregnancy (unless benefits clearly outweigh risks); breastfeeding.

Drug Interactions

• Antacids and Sucralfate: Reduce Levosulpiride absorption. Administer at least 2 hours apart.
• Alcohol: Increases sedation.
• Antihypertensives: May enhance hypotensive effects.
• Anticholinergics: May increase anticholinergic side effects.
• Levodopa: Antagonizes Levodopa’s effects.
• Drugs prolonging QT interval: Increased risk of arrhythmias.
• CYP450 interactions are not primary concern here, but it is advisable to check on them as well.

Pregnancy and Breastfeeding

• Pregnancy: Not recommended unless benefits outweigh risks. Potential fetal harm is not well established.
• Breastfeeding: Levosulpiride is excreted in breast milk. Breastfeeding is contraindicated while taking this medication.

Drug Profile Summary

• Mechanism of Action: Levosulpiride: Prokinetic (increases acetylcholine); Dimethicone: Antiflatulent (reduces gas bubble surface tension).
• Side Effects: Headache, fatigue, drowsiness, constipation, extrapyramidal symptoms, increased prolactin.
• Contraindications: Hypersensitivity, GI obstruction/bleeding, pheochromocytoma, epilepsy, prolactin-dependent tumors, Parkinson’s disease.
• Drug Interactions: Antacids, alcohol, antihypertensives, anticholinergics, Levodopa.
• Pregnancy & Breastfeeding: Generally contraindicated.
• Dosage: Adults: 25mg Levosulpiride + 125mg Dimethicone TID before meals. Adjustments may be necessary.
• Monitoring Parameters: Liver function tests, prolactin levels, ECG (in patients with cardiac risk factors), extrapyramidal symptoms.

Popular Combinations

This medication is itself a combination. Additional medications may be prescribed depending on the specific clinical picture, such as proton pump inhibitors for GERD.

Precautions

• General Precautions: Pre-screening for allergies, metabolic disorders, and organ dysfunction is essential.
• Specific Populations: Standard precautions for pregnant women, breastfeeding mothers, children, elderly, and those with relevant comorbid conditions apply.
• Lifestyle Considerations: Avoid alcohol. Caution with activities requiring mental alertness (e.g., driving).

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Dimethicone + Levosulpiride?

A: The standard adult dosage is 25mg Levosulpiride + 125mg Dimethicone three times daily, taken before meals. Dosage adjustments may be needed for the elderly, patients with renal/hepatic impairment, and those with comorbid conditions.

Q2: Can this medication be used during pregnancy or breastfeeding?

A: It’s generally contraindicated during pregnancy and breastfeeding. Consult a doctor to assess the benefit-risk ratio in individual cases.

Q3: What are the common side effects?

A: Common side effects include headache, fatigue, drowsiness, constipation, and extrapyramidal symptoms.

Q4: What are the serious side effects?

A: Rare but serious side effects include neuroleptic malignant syndrome (NMS) and cardiac arrhythmias (QT prolongation).

Q5: What are the contraindications for this drug?

A: Contraindications include hypersensitivity, GI obstruction/bleeding, pheochromocytoma, epilepsy, prolactin-dependent tumors, Parkinson’s disease.

Q6: How does Levosulpiride work in this combination?

A: Levosulpiride is a prokinetic agent that increases acetylcholine, stimulating gut motility and reducing reflux.

Q7: What is the role of Dimethicone in this combination?

A: Dimethicone acts as an antiflatulent by reducing the surface tension of gas bubbles in the gut.

Q8: Are there any drug interactions I should be aware of?

A: Yes, it interacts with antacids, alcohol, antihypertensives, anticholinergics, and Levodopa.

Q9: What monitoring parameters should be considered?

A: Liver function tests, prolactin levels, ECG (in cardiac risk patients), and monitoring for extrapyramidal symptoms are advisable.

Q10: Can this combination be used for nausea and vomiting?

A: Yes, Levosulpiride has antiemetic properties, which can help manage nausea and vomiting. However, the combination is primarily indicated for dyspepsia and constipation relief.