Usage
- This combination medication is prescribed for the relief of symptoms associated with gastroesophageal reflux disease (GERD), such as heartburn, acid indigestion, and dyspepsia. It is also used to treat nausea and vomiting associated with diabetic gastroparesis. In acidity, this combination relieves excessive stomach acidity, preventing heartburn and indigestion. It promotes the movement of food in the stomach to prevent nausea or vomiting.
- Pharmacological Classification: Antacid (Magaldrate) and Prokinetic/Antiemetic (Metoclopramide)
- Mechanism of Action: Magaldrate neutralizes gastric acid, providing relief from heartburn. Metoclopramide increases the motility of the stomach and intestines, promoting faster emptying and reducing reflux. Metoclopramide is a dopamine D2 receptor antagonist in the chemoreceptor trigger zone, which reduces nausea and vomiting. It also increases acetylcholine release, enhancing gastrointestinal motility.
Alternate Names
- Metadrate
- Norper Suspension
- Megatech Syrup (Syrup Formulation)
- Tak-MD
How It Works
- Pharmacodynamics: Metoclopramide is a dopamine D2 receptor antagonist in the chemoreceptor trigger zone, reducing nausea and vomiting. It also increases acetylcholine release, enhancing gastrointestinal motility. Magaldrate neutralizes gastric acid through a chemical reaction, increasing gastric pH.
- Pharmacokinetics: Metoclopramide is rapidly absorbed orally. It is metabolized in the liver and excreted primarily in the urine. Magaldrate reacts locally in the stomach and is not absorbed systemically in substantial amounts.
- Mode of Action: Metoclopramide acts as a dopamine D2 receptor antagonist in the chemoreceptor trigger zone and increases acetylcholine release. Magaldrate chemically neutralizes gastric acid.
- Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Metoclopramide is a dopamine D2 receptor antagonist and enhances acetylcholine release.
- Elimination Pathways: Metoclopramide is metabolized in the liver and excreted primarily in the urine. Magaldrate reacts locally in the stomach and is not systemically absorbed in substantial amounts.
Dosage
Standard Dosage
Adults:
- GERD: 10-15 mg of Metoclopramide with 400-480 mg of Magaldrate, orally, four times a day, 30 minutes before meals and at bedtime. The maximum dose is 80mg of Metoclopramide per day. Treatment duration is generally 4 to 12 weeks. For dyspepsia, 1 to 2 teaspoons after meals and at bedtime.
- Diabetic Gastroparesis: 10 mg of Metoclopramide with 480 mg of Magaldrate, orally, four times a day, 30 minutes before meals and at bedtime for 2 to 8 weeks. Maximum dose is 40 mg of Metoclopramide per day.
Children:
- Dosage must be determined by a physician, considering the child’s age and weight. Pediatric dosages are generally not recommended for GERD. For children 1-18 years old, dosing is based on weight and administered up to three times a day via slow IV push. The maximum daily dose is 0.5 mg/kg. Oral liquid formulations have been associated with overdose in children, requiring careful administration.
Special Cases:
- Elderly Patients: Start with 5 mg four times daily; maximum dose 30 mg daily due to increased sensitivity to side effects.
- Patients with Renal Impairment: For Metoclopramide, if creatinine clearance is less than 40 mL/min, initial doses should be 50% of the usual recommended dose. Magaldrate should be used with caution to avoid hypermagnesemia.
- Patients with Hepatic Dysfunction: Dose reduction of Metoclopramide may be needed. For Magaldrate, no specific adjustments are available; caution is advised.
- Patients with Comorbid Conditions: Caution advised for patients with diabetes, cardiovascular disease, epilepsy, or other movement disorders. Pre-existing conditions such as gastrointestinal hemorrhage, mechanical obstruction, or perforation contraindicate use.
Clinical Use Cases
This combination is generally not used in clinical settings like intubation, surgical procedures, mechanical ventilation, or the ICU. Metoclopramide alone may be used in postoperative nausea and vomiting, and for small bowel intubation/radiologic examination of the upper GI tract (10 mg IV over 1-2 minutes).
Dosage Adjustments
Modifications should be based on renal function, hepatic function, and individual response. For patients who are poor CYP2D6 metabolizers, give 5 mg of Metoclopramide four times daily or 10 mg three times daily.
Side Effects
Common Side Effects
- Diarrhea
- Drowsiness
- Dizziness
- Fatigue
- Headache
- Restlessness
- Tremor
- Altered taste
- Nausea or vomiting
- Insomnia
- Restlessness
- Edema
- Fatigue
Rare but Serious Side Effects
- Tardive dyskinesia (TD) - involuntary, repetitive body movements
- Neuroleptic Malignant Syndrome (NMS) - fever, muscle rigidity, altered mental status, autonomic instability
- Extrapyramidal symptoms (EPS) - muscle spasms, tremors, restlessness
- Methemoglobinemia
- Depression (including suicidal ideation)
- Anxiety
- Agitation
- Jaundice
Long-Term Effects
Adverse Drug Reactions (ADR)
- TD, NMS, severe EPS, and methemoglobinemia require immediate medical attention.
Contraindications
- Hypersensitivity to either Magaldrate or Metoclopramide
- Gastrointestinal hemorrhage, mechanical obstruction, or perforation
- Pheochromocytoma
- Epilepsy or seizure disorders
- Parkinson’s Disease or other movement disorders
Drug Interactions
- Antipsychotics (increased risk of EPS)
- Anticholinergics (reduced efficacy of metoclopramide)
- CNS depressants (increased sedation)
- Digoxin (reduced absorption)
- Dopamine agonists (e.g., cabergoline, pergolide)
- MAO inhibitors (e.g., isocarboxazid, linezolid)
- Alcohol (increased drowsiness and other CNS depressant effects)
- Certain antidepressants (e.g., fluoxetine, paroxetine)
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Metoclopramide: B (Consult with a physician before use during pregnancy)
- Magaldrate + Metoclopramide rarely shows harmful effects during pregnancy.
- Magaldrate + Metoclopramide can cause moderate side effects on breastfeeding women. If side effects occur, stop taking the drug and consult a doctor. This drug passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breastfeeding. Metoclopramide can also be used to increase breast milk supply, although it is not specifically indicated for this purpose.
Drug Profile Summary
- Mechanism of Action: Magaldrate neutralizes gastric acid; Metoclopramide is a dopamine antagonist and prokinetic agent.
- Side Effects: Diarrhea, drowsiness, dizziness, extrapyramidal symptoms, tardive dyskinesia (TD).
- Contraindications: GI hemorrhage, obstruction, perforation; pheochromocytoma, epilepsy.
- Drug Interactions: Antipsychotics, anticholinergics, CNS depressants.
- Pregnancy & Breastfeeding: Use with caution; consult a physician. May have undesirable effects on a nursing infant.
- Dosage: Varies; consult dosage guidelines above.
- Monitoring Parameters: Monitor for extrapyramidal symptoms, tardive dyskinesia, and neuroleptic malignant syndrome. Check blood pressure regularly.
Popular Combinations
This combination itself is used for treating GERD with nausea/vomiting. Combining separate antacids and prokinetics is more common than this fixed-dose combination.
Precautions
- Assess for hypersensitivity, renal/hepatic impairment.
- Monitor for EPS, TD, and other side effects.
- Caution in elderly patients and those with comorbid conditions.
- Avoid alcohol and other CNS depressants. Do not drive or operate machinery until the effects are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Magaldrate + Metoclopramide?
A: Dosage varies by condition and patient factors; see detailed dosage guidelines above. Always refer to the specific product label.
Q2: What are the common side effects?
A: Common side effects include diarrhea, drowsiness, dizziness, fatigue, headache, restlessness, tremor, and altered taste.
Q3: What are the serious side effects?
A: Tardive dyskinesia (TD), Neuroleptic Malignant Syndrome (NMS), Extrapyramidal Symptoms (EPS), Methemoglobinemia.
Q4: What are the contraindications for this medication?
A: Hypersensitivity to either drug, GI hemorrhage, mechanical obstruction or perforation, pheochromocytoma, epilepsy, and Parkinson’s disease.
Q5: Can this medication be used during pregnancy and breastfeeding?
A: Use with caution and consult with a physician. It may have undesirable effects on a nursing infant.
Q6: How does Magaldrate work?
A: Magaldrate neutralizes stomach acid, increasing gastric pH and providing relief from heartburn and acid indigestion.
Q7: How does Metoclopramide work?
A: Metoclopramide blocks dopamine receptors and increases acetylcholine, leading to increased gastric motility and reduced nausea and vomiting.
Q8: What should I do if a patient experiences side effects?
A: For common side effects, advise the patient to contact you if they persist or worsen. For serious side effects like TD or NMS, seek immediate medical attention.
Q9: What are the long-term risks of using this medication?
A: The most concerning long-term risk is tardive dyskinesia (TD), which can be irreversible. Limit treatment duration to 12 weeks unless absolutely necessary.
Q10: What are the key drug interactions to be aware of?
A: Interactions exist with antipsychotics, anticholinergics, CNS depressants, digoxin, dopamine agonists, MAO inhibitors, and alcohol. Always review a patient’s medication list.
