Usage
- This combination medication is prescribed for the treatment of peptic ulcers (gastric and duodenal), gastritis, heartburn, acidity, bloating, and gas. It is also used for symptomatic relief of gastroesophageal reflux disease (GERD).
- Pharmacological Classification: This is a combination product containing a mucosal protectant (Sucralfate), antiflatulent (Simethicone), and a local anesthetic (Oxetacaine). Thus, it can be classified as an antiulcer, antiflatulent and local anesthetic agent.
- Mechanism of Action: Sucralfate forms a protective barrier over ulcers, protecting them from stomach acid and promoting healing. Simethicone reduces the surface tension of gas bubbles, aiding in their expulsion. Oxetacaine provides local anesthetic action, relieving pain associated with ulcers.
Alternate Names
- No widely recognized alternate names exist for this specific combination. However, the individual components have other names (e.g., Sucralfate is also known as aluminum sucrose sulfate).
- Brand Names: Brand names vary depending on the manufacturer and region. Examples found in the sources provided include: Coatz AF, GESUCRAL-O, RALF Ox (Sucralfate + Oxetacaine combination).
How It Works
- Pharmacodynamics: Sucralfate selectively binds to the ulcer base, forming a protective barrier against pepsin, acid, and bile. Simethicone disperses and prevents the formation of mucus-entrapped gas pockets in the gastrointestinal tract. Oxetacaine, as a local anesthetic, inhibits nerve impulse transmission, providing pain relief.
- Pharmacokinetics: Sucralfate has minimal systemic absorption. Simethicone is not absorbed and is excreted unchanged in feces. Oxetacaine is minimally absorbed with rapid metabolism.
- Mode of Action: Sucralfate acts locally at the ulcer site. Simethicone works by altering the surface tension of gas bubbles. Oxetacaine acts by blocking sodium channels in nerve membranes, thereby inhibiting depolarization and nerve impulse transmission.
- Elimination Pathways: Sucralfate is primarily excreted in feces. Simethicone is eliminated unchanged in feces. Oxetacaine is primarily metabolised and eliminated rapidly.
Dosage
Standard Dosage
Adults:
- The standard dosage varies depending on the product formulation and is typically 1 g (or 10 mL suspension containing 1 g Sucralfate) four times a day on an empty stomach, 1 hour before meals and at bedtime. The dose may be reduced to 1 g twice daily for maintenance therapy. Duration of treatment can be up to 8 weeks.
Children:
- The safety and efficacy of this combination have not been established in children. Its use in children is generally not recommended, especially below 12 years of age. For children above 12, the usage and dosage should be determined by a healthcare professional, with careful evaluation of potential risks and benefits. Consult a pediatrician for specific dosing.
Special Cases:
- Elderly Patients – Dose adjustments might be necessary based on kidney function. Renal impairment may necessitate a reduction in dosage. Careful monitoring of aluminium levels might be required.
- Patients with Renal Impairment – Dosage modifications may be needed due to altered elimination. Closely monitor renal function. Aluminium accumulation may occur and monitoring would be required.
- Patients with Hepatic Dysfunction – Specific dose adjustments are not typically required, however, exercise caution.
- Patients with Comorbid Conditions – For example, diabetes mellitus requires careful blood glucose monitoring, as Sucralfate may affect glycemic control. Dose adjustments in antidiabetic medication may be required in patients with Diabetes Mellitus.
Clinical Use Cases
- Dosage guidelines for specific clinical use cases are not explicitly defined for this specific combination. Dosing recommendations for Sucralfate in the context of stress ulcer prophylaxis are available in some sources.
Dosage Adjustments
- Dose modifications are based primarily on renal function.
Side Effects
Common Side Effects
- Constipation
- Diarrhea
- Dry mouth
- Nausea
- Dizziness
Rare but Serious Side Effects
- Allergic reactions (e.g., rash, itching, swelling, difficulty breathing)
- Bezoar formation (especially in patients with delayed gastric emptying)
Long-Term Effects
- Aluminum accumulation (potential concern in patients with renal impairment)
Adverse Drug Reactions (ADR)
- Severe allergic reactions (anaphylaxis) require immediate medical attention.
Contraindications
- Hypersensitivity to any component of the medication
- Active gastrointestinal bleeding
- Severe renal impairment
- History of appendicitis or bowel obstruction
- Patients on a low-magnesium diet
- Recent bowel surgery
Drug Interactions
- Antacids (especially aluminum- or magnesium-containing antacids)
- Antibiotics (e.g., fluoroquinolones, tetracyclines)
- Antidiabetic medications (e.g., metformin, sulfonylureas)
- Anticoagulants (e.g., warfarin)
- Anticonvulsants (e.g., phenytoin)
- Thyroid medications (e.g., levothyroxine)
- Alcohol
- Nicotine
Pregnancy and Breastfeeding
- Pregnancy: Consult a physician before use. Sucralfate is classified as Pregnancy Category B; however, there are limited data on the combination product’s effects during pregnancy. Use only if clearly needed.
- Breastfeeding: Not recommended due to limited safety information and potential risk to the infant.
Drug Profile Summary
- Mechanism of Action: Sucralfate: mucosal protectant, Simethicone: antiflatulent, Oxetacaine: local anesthetic.
- Side Effects: Constipation, diarrhea, dry mouth, nausea, dizziness, allergic reactions.
- Contraindications: Hypersensitivity, active GI bleeding, severe renal impairment.
- Drug Interactions: Multiple drug interactions, see the “Drug Interactions” section for details.
- Pregnancy & Breastfeeding: Consult a physician if pregnant. Not recommended while breastfeeding.
- Dosage: Adults: typically 1g four times daily for ulcers. Pediatric use not established.
- Monitoring Parameters: Renal function, serum phosphate (for long-term use).
Popular Combinations
Although, information on popular combinations of the specific combination Oxetacaine + Simethicone + Sucralfate was not found in the provided sources, Sucralfate is sometimes combined with other antacids to provide additional relief from heartburn.
Precautions
- General Precautions: Renal impairment, history of bowel obstruction, and allergy to any component.
- Specific Populations: Pregnant women, breastfeeding mothers (avoid use), Children (safety not established).
- Lifestyle Considerations: Avoid alcohol and nicotine, as they can worsen symptoms. Caution when driving or operating machinery due to potential dizziness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Oxetacaine + Simethicone + Sucralfate?
A: The usual adult dose is 1 gram (or 10 ml of suspension containing 1g of Sucralfate) four times a day on an empty stomach, one hour before meals and at bedtime. It can be adjusted based on the patient’s response and renal function. Pediatric use is generally not recommended due to safety concerns.
Q2: What are the common side effects?
A: Common side effects include constipation, diarrhea, dry mouth, nausea, and dizziness.
Q3: Can I take this medication during pregnancy or while breastfeeding?
A: Consult your doctor if you are pregnant or planning to become pregnant. It’s generally not recommended while breastfeeding.
Q4: How does this medication interact with other drugs?
A: It can interact with a variety of medications, including antacids, antibiotics, antidiabetics, and thyroid medications. Provide your doctor with a complete list of your medications.
Q5: What conditions is this medication contraindicated in?
A: It should not be used in patients with hypersensitivity to any of its components, active gastrointestinal bleeding, or severe renal impairment. Inform your doctor about your medical history.
Q6: Can I drink alcohol while taking this medication?
A: It’s best to avoid alcohol, as it can irritate the stomach and worsen ulcer symptoms.
Q7: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it is almost time for your next dose. Do not double up on doses.
Q8: How long should I take this medication?
A: The duration of treatment depends on the specific condition and should be determined by your doctor. For duodenal ulcers, the treatment can last up to 8 weeks.
Q9: Are there any dietary restrictions while using this medication?
A: While there are no specific food interactions, following a healthy, balanced diet low in irritating foods can be beneficial for ulcer healing.
