Metoclopramide + Simethicone

Usage

Metoclopramide + Simethicone is prescribed for the relief of symptoms associated with gastrointestinal disorders such as dyspepsia, bloating, nausea, and vomiting. It combines a prokinetic agent (metoclopramide) with an anti-flatulent (simethicone).

Pharmacological Classification:

• Metoclopramide: Prokinetic, antiemetic
• Simethicone: Anti-flatulent

Mechanism of Action:

Metoclopramide increases gastrointestinal motility by enhancing the response to acetylcholine in the upper gastrointestinal tract. It also acts as a dopamine antagonist, reducing nausea and vomiting. Simethicone reduces the surface tension of gas bubbles, facilitating their coalescence and easier passage.

Alternate Names

This combination medication doesn’t have a single international nonproprietary name (INN). It is typically identified by the names of its two components. Brand names vary depending on the region and manufacturer.

Brand Names: (This list is not exhaustive and may vary by region) Some possible brand name combinations could exist but it is rare to find fixed-dose combination product. It is often co-prescribed or co-administered

How It Works

Pharmacodynamics (Metoclopramide):

Metoclopramide enhances gastric emptying and small bowel transit. Its antiemetic effect is through dopamine D2 receptor antagonism in the chemoreceptor trigger zone and vomiting center.

Pharmacokinetics (Metoclopramide):

• Absorption: Rapidly absorbed orally.
• Metabolism: Primarily hepatic via conjugation.
• Elimination: Renally excreted.

Pharmacodynamics (Simethicone):

Simethicone lowers the surface tension of gas bubbles in the stomach and intestines, leading to their combination and allowing easier expulsion.

Pharmacokinetics (Simethicone):

• Absorption: Not absorbed systemically.
• Metabolism: Not metabolized.
• Elimination: Excreted unchanged in the feces.

Dosage

Standard Dosage

Adults:

Metoclopramide: 10 mg orally, up to four times a day, 30 minutes before meals and at bedtime. Simethicone: 40-125 mg orally, four times a day, after meals and at bedtime. The combination may not be available as a fixed-dose product, requiring separate administration.

Children:

The dosage should be determined by a doctor. Simethicone is generally considered safe for use in children. Metoclopramide use in pediatrics requires careful consideration due to the risk of extrapyramidal side effects.

Special Cases:

• Elderly Patients: Start with a lower dose of metoclopramide due to potential increased sensitivity.
• Patients with Renal Impairment: Dose reduction of metoclopramide is necessary based on creatinine clearance.
• Patients with Hepatic Dysfunction: Dose reduction of metoclopramide may be required.
• Patients with Comorbid Conditions: Caution is advised in patients with Parkinson’s disease, depression, and other conditions.

Clinical Use Cases

Metoclopramide use in specific clinical situations like intubation, surgical procedures, or ICU settings should be carefully considered due to potential side effects and drug interactions. Simethicone is generally not indicated in these settings.

Dosage Adjustments

Dose adjustments are crucial for metoclopramide in renal and hepatic impairment based on the degree of dysfunction. Close monitoring is essential.

Side Effects

Common Side Effects:

• Metoclopramide: Restlessness, drowsiness, fatigue, diarrhea.
• Simethicone: Generally well-tolerated.

Rare but Serious Side Effects:

• Metoclopramide: Tardive dyskinesia (especially with prolonged use), neuroleptic malignant syndrome, extrapyramidal symptoms.

Long-Term Effects:

• Metoclopramide: Tardive dyskinesia can be a long-term consequence of chronic use.

Adverse Drug Reactions (ADR):

• Metoclopramide: Extrapyramidal reactions, hypersensitivity reactions.

Contraindications

• Metoclopramide: Gastrointestinal hemorrhage, mechanical obstruction, perforation, pheochromocytoma, epilepsy.
• Simethicone: Hypersensitivity to simethicone.

Drug Interactions

• Metoclopramide: Anticholinergics, CNS depressants, digoxin, levodopa.
• Simethicone: May interfere with the absorption of levothyroxine.

Pregnancy and Breastfeeding

• Metoclopramide: Use with caution during pregnancy, especially in the first trimester. It is excreted in breast milk.
• Simethicone: Generally considered safe during pregnancy and breastfeeding.

Drug Profile Summary

• Mechanism of Action: Metoclopramide: Prokinetic, antiemetic. Simethicone: Anti-flatulent.
• Side Effects: Metoclopramide: Extrapyramidal reactions, tardive dyskinesia. Simethicone: Generally well-tolerated.
• Contraindications: Metoclopramide: GI obstruction, hemorrhage, perforation.
• Drug Interactions: Metoclopramide: Anticholinergics, CNS depressants.
• Pregnancy & Breastfeeding: Metoclopramide: Use with caution. Simethicone: Generally safe.
• Dosage: Varies depending on the indication and patient factors.
• Monitoring Parameters: Metoclopramide: Extrapyramidal symptoms, vital signs.

Popular Combinations

Metoclopramide may be combined with other medications for specific gastrointestinal disorders. Simethicone is often included in antacid formulations.

Precautions

• Metoclopramide: Monitor for extrapyramidal reactions, particularly in elderly patients. Avoid prolonged use.
• Simethicone: Generally safe for use.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Metoclopramide + Simethicone?

A: Dosing varies based on the individual components and patient factors. It is recommended to consult appropriate resources and tailor the dosage accordingly. A typical adult dose might involve 10mg of metoclopramide up to four times daily and simethicone 40-125 mg four times daily, administered separately.

Q2: What are the common side effects of this combination?

A: Common side effects related to metoclopramide include drowsiness, fatigue, restlessness, and diarrhea. Simethicone is generally well-tolerated.

Q3: Are there any serious side effects I should be aware of?

A: Yes, metoclopramide carries a risk of tardive dyskinesia, especially with prolonged use. Extrapyramidal symptoms and neuroleptic malignant syndrome are also potential, though rare, adverse effects.

Q4: Can this combination be used in pregnant or breastfeeding women?

A: Simethicone is generally considered safe. Metoclopramide should be used with caution during pregnancy, especially in the first trimester, and during breastfeeding, as it is excreted in breast milk.

Q5: What are the contraindications to using metoclopramide + simethicone?

A: Metoclopramide is contraindicated in patients with gastrointestinal bleeding, mechanical obstruction, or perforation. It should also be avoided in patients with pheochromocytoma and epilepsy. Simethicone is contraindicated in individuals with hypersensitivity to it.

Q6: Are there any drug interactions I should be aware of?

A: Metoclopramide can interact with anticholinergic drugs, CNS depressants, digoxin, and levodopa. Simethicone may affect the absorption of certain medications, such as levothyroxine.

Q7: How should I adjust the dose in patients with renal or hepatic impairment?

A: Dose reduction of metoclopramide is crucial in patients with renal or hepatic impairment. Specific adjustments should be based on the severity of the dysfunction and creatinine clearance.

Q8: What are the key monitoring parameters for patients taking this combination?

A: Monitor patients for extrapyramidal symptoms, especially with metoclopramide use. Regularly assess vital signs and monitor renal and hepatic function if indicated.

Q9: Can this combination be used in children?

A: Simethicone can generally be used in children. Metoclopramide use requires careful consideration due to the risk of extrapyramidal effects. Consult pediatric dosing guidelines and exercise caution.