Usage
This combination medication is prescribed for the symptomatic relief of gastrointestinal disorders associated with hyperacidity, such as:
- Gastritis
- Esophagitis
- Peptic ulcers (gastric and duodenal)
- Hiatal hernia
- Heartburn (including during pregnancy)
- Indigestion
- Stomach upset
Pharmacological Classification:
This is a combination product containing:
- Aluminium hydroxide and Magnesium hydroxide: Antacids
- Oxetacaine: Local anesthetic
Mechanism of Action:
Aluminium hydroxide and magnesium hydroxide neutralize excess stomach acid, thus increasing gastric pH and reducing irritation to the gastrointestinal mucosa. Oxetacaine provides local anesthetic action, numbing the affected area and offering relief from pain associated with ulcers or acid injury in the stomach.
Alternate Names
While no specific international nonproprietary name exists for this combination, it may be referred to as a combination antacid with local anesthetic.
Several brand names exist depending on the region and manufacturer. These include:
- Mucaine gel
- Kascito-O gel
- Gastrocam
- Ancool
- Allugel
- Geltazine
How It Works
Pharmacodynamics:
Aluminium hydroxide and magnesium hydroxide chemically react with gastric acid (HCl) to form neutral salts and water, thereby increasing intragastric pH. Oxetacaine inhibits voltage-gated sodium channels in neuronal membranes, resulting in a localized anesthetic effect.
Pharmacokinetics:
- Absorption: Oxetacaine is absorbed systemically when administered alone, but its absorption is reduced when combined with aluminum and magnesium hydroxide. Aluminum and magnesium hydroxide are poorly absorbed systemically.
- Metabolism: Oxetacaine is metabolized in the liver.
- Elimination: Oxetacaine is primarily excreted in the urine. Aluminum and magnesium are primarily excreted in the feces. Patients with renal impairment may experience aluminum and magnesium accumulation.
Mode of Action:
Aluminum and magnesium hydroxide work through chemical neutralization. Oxetacaine blocks sodium channels, preventing depolarization of nerve fibers and inhibiting pain signal transmission.
Receptor Binding, Enzyme Inhibition, Neurotransmitter Modulation:
This combination does not involve receptor binding, enzyme inhibition, or neurotransmitter modulation.
Elimination Pathways:
- Aluminum and magnesium are primarily eliminated through fecal excretion.
- Oxetacaine is metabolized in the liver and excreted via the kidneys.
Dosage
Dosage guidelines are general and should be individualized based on patient needs. Always consult with a healthcare professional for personalized guidance.
Standard Dosage
Adults:
The standard dose is typically 10-20 mL or 1-2 tablets, taken 20 minutes to 1 hour after meals and at bedtime, as needed. The daily maximum dose is generally 80 mL or the equivalent in tablets.
Children:
This medication is generally NOT recommended for children under 12 years old. Safety and efficacy in this age group have not been fully established. For children above 12, a lower dose is recommended under strict medical supervision.
Special Cases:
- Elderly Patients: Use with caution due to potential for altered drug handling and comorbidities. Careful monitoring is required.
- Patients with Renal Impairment: Use with extreme caution due to reduced aluminum and magnesium clearance. Dose adjustments are necessary, and close monitoring of serum levels is advised.
- Patients with Hepatic Dysfunction: As oxetacaine is metabolized in the liver, use cautiously and adjust dose as needed in patients with hepatic impairment.
- Patients with Comorbid Conditions: Careful consideration is needed for patients with conditions like diabetes, heart failure, and other metabolic disorders. Consult specialists accordingly.
Clinical Use Cases
This drug combination is not typically used for intubation, surgical procedures, mechanical ventilation, or in the ICU or emergency situations. Its primary role is symptomatic relief in outpatient settings for the above-mentioned gastrointestinal conditions.
Dosage Adjustments
Dosage adjustments are essential based on patient-specific factors such as renal function, hepatic function, age, and other comorbidities. Close monitoring and individualized therapy are critical.
Side Effects
Common Side Effects:
- Constipation
- Diarrhea
- Nausea
- Drowsiness
- Dizziness
Rare but Serious Side Effects:
- Allergic reactions (rash, itching, swelling)
- Hypomotility of bowel leading to obstruction or ileus (especially in the elderly and those with renal impairment)
- Hypermagnesemia (particularly in children with renal impairment or dehydration)
- Hyperaluminemia
Long-Term Effects:
Long-term, high-dose use, particularly in patients with renal impairment, has been associated with dementia and microcytic anemia.
Adverse Drug Reactions (ADR):
Clinically significant ADRs include allergic reactions and signs of hypermagnesemia or hyperaluminemia, requiring immediate intervention.
Contraindications
- Hypersensitivity to any of the ingredients
- Severe renal impairment
- Hypophosphatemia
- Severe abdominal pain with potential bowel obstruction
- Debilitated patients
Drug Interactions
This combination may interact with various medications, including:
- Tetracycline antibiotics
- Quinolone antibiotics (e.g., ciprofloxacin, levofloxacin)
- Digoxin
- Iron supplements
- Aspirin
- Certain anti-diabetic medications
- Vitamins (e.g., ascorbic acid, cholecalciferol)
- Citrates (can lead to increased aluminum absorption)
- Alcohol (can increase stomach acid production)
Pregnancy and Breastfeeding
- Pregnancy: Use cautiously during pregnancy, especially in the first trimester. Consult a physician before use.
- Breastfeeding: Minimal amounts of aluminum and magnesium hydroxide and no simethicone (when included in some formulations) are excreted in breast milk. It is generally considered safe during breastfeeding when used as directed, but consultation with a physician is recommended.
Drug Profile Summary
- Mechanism of Action: Neutralization of gastric acid (aluminum and magnesium hydroxide), local anesthetic effect (oxetacaine).
- Side Effects: Constipation, diarrhea, nausea, drowsiness, dizziness, rare allergic reactions.
- Contraindications: Hypersensitivity, severe renal impairment, hypophosphatemia, bowel obstruction, debilitated state.
- Drug Interactions: Tetracyclines, quinolones, digoxin, iron, aspirin, certain anti-diabetics, vitamins, citrates.
- Pregnancy & Breastfeeding: Use cautiously, consult a physician.
- Dosage: 10-20 mL or 1-2 tablets after meals and at bedtime, up to 4 times daily. Maximum 80 mL/day.
- Monitoring Parameters: Renal function tests, serum aluminum and magnesium levels (especially in long-term use and renal impairment).
Popular Combinations
This combination often includes simethicone (an anti-flatulent) in some formulations.
Precautions
- Pre-existing medical conditions, including renal and hepatic impairment, should be evaluated.
- Use with caution in elderly patients and pregnant/breastfeeding women.
- Avoid alcohol and citrate-containing foods and beverages.
- Monitor for side effects.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aluminium Hydroxide + Magnesium + Oxetacaine?
A: The standard adult dose is 10-20 mL or 1-2 tablets, taken 20 minutes to 1 hour after meals and at bedtime, up to four times a day. Not recommended for children under 12.
Q2: What are the common side effects?
A: Common side effects include constipation, diarrhea, nausea, drowsiness, and dizziness.
Q3: Can pregnant women take this medication?
A: Use with caution during pregnancy, particularly in the first trimester. Consult with a physician before use.
Q4: How does this medication interact with other drugs?
A: It can interact with several medications, including tetracyclines, quinolones, digoxin, iron supplements, and others. Always inform your doctor about all other medications you are taking.
Q5: What conditions is this medication contraindicated in?
A: Contraindications include hypersensitivity to any component, severe renal impairment, hypophosphatemia, bowel obstruction, and severely debilitated states.
Q6: What are the long-term effects of using this medication?
A: Long-term high-dose use, especially in patients with renal impairment, may lead to dementia and microcytic anemia. Regular monitoring of renal function and serum levels is advised.
Q7: Can I take this medication with alcohol?
A: Alcohol should be avoided as it can increase stomach acid production, counteracting the effects of the antacids.
Q8: How does this medication work on a cellular level?
A: Aluminum and magnesium hydroxide neutralize stomach acid by chemical reaction. Oxetacaine blocks sodium channels, preventing pain signal transmission.
Q9: What should I do if I miss a dose?
A: If you miss a dose, take the next dose as scheduled. Do not double the dose.
Q10: What are the signs of an overdose?
A: Overdose can lead to exacerbated side effects like constipation (aluminum hydroxide) or diarrhea (magnesium hydroxide). In severe cases, bowel obstruction or ileus may occur. Seek medical attention immediately if an overdose is suspected.
