Oxetacaine

Usage

• Oxetacaine is prescribed for the relief of pain associated with oral and esophageal lesions, such as those caused by oral mucositis, esophagitis, and peptic ulcers. It is also used to alleviate pain from anal fissures and hemorrhoids when applied topically. It is often used in combination with antacids like aluminum hydroxide and magnesium hydroxide to treat GERD (Gastroesophageal Reflux Disease), gastritis, peptic ulcers, hyperacidity, heartburn, indigestion, and other gastrointestinal diseases.

• Pharmacological Classification: Local anesthetic.

• Mechanism of Action: Oxetacaine blocks nerve signals in the mucous membranes, leading to a localized numbing effect that alleviates pain and discomfort.

Alternate Names

• Oxethazaine
• Brand Names: Alucain, Fencaine, Magocain, Mezain, Neocane, Oxeway, Soothing, Sowecaine, Topicaine, Emoren. (Note: Availability of brands varies by region).

How It Works

• Pharmacodynamics: Oxetacaine acts locally by reversibly binding to sodium channels in nerve membranes, blocking nerve impulse transmission and producing anesthesia. It does not lose its activity in acidic environments, making it suitable for use in the gastrointestinal tract.
• Pharmacokinetics: When administered orally, absorption may vary depending on the formulation. Topical application results in localized action. Metabolism and elimination pathways are not extensively documented but likely involves hepatic metabolism and renal excretion.
• Mode of Action: Blocks sodium channels in nerve cell membranes.
• Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Sodium channel blocker.
• Elimination Pathways: Primarily hepatic metabolism and renal excretion.

Dosage

Standard Dosage

Adults:

• Oral: 10-15ml (containing 1000mg sucralfate and 20mg oxetacaine) four times daily on an empty stomach approximately 1 hour before meals and at bedtime for 4-8 weeks for gastric and duodenal ulcers and GERD. Topical Dosage varies based on the application. Dosage might change as the condition improves. As of today, these are the latest guidelines.

Children:

• Safety and efficacy not established in children younger than 12 or 14 years of age. For older children (over 12), the recommended oral dose is 10-20 mg/kg 1 hour before meals, with a maximum dose of 80 mg/kg/day or 2000 mg/day. It is important to consult with a pediatrician for the appropriate dosage.

Special Cases:

• Elderly Patients: Use with caution due to potential decreased renal function. Monitor for aluminium toxicity if given in combination with sucralfate.
• Patients with Renal Impairment: Dose reduction may be needed.
• Patients with Hepatic Dysfunction: Use with caution.
• Patients with Comorbid Conditions: Close monitoring needed, especially in patients with diabetes.

Clinical Use Cases

• Intubation: Not typically used.
• Surgical Procedures: May be used for postoperative pain management in certain procedures.
• Mechanical Ventilation: No specific dosage adjustments; assess individual patient needs.
• Intensive Care Unit (ICU) Use: Dosage adjusted according to patient’s condition.
• Emergency Situations: Not typically used.

Dosage Adjustments:

Adjustments needed for renal impairment, hepatic dysfunction, elderly patients, children, and those with comorbid conditions. Consult with a nephrologist or hepatologist when necessary.

Side Effects

Common Side Effects

• Constipation, dizziness, drowsiness, dry mouth, nausea, vomiting, upset stomach, flatulence, blurred vision, diarrhea, itching, skin rash.

Rare but Serious Side Effects

• Allergic reactions (rash, itching, swelling, dizziness, difficulty breathing), glossitis, fainting.

Long-Term Effects

• Not well established; prolonged use of aluminum-containing antacids can lead to aluminum accumulation and potential toxicity in patients with renal impairment.

Adverse Drug Reactions (ADR)

• Severe allergic reactions, severe gastrointestinal disturbances, blood in the stool.

Contraindications

• Hypersensitivity to oxetacaine or any component of the formulation.
• Active gastrointestinal bleeding.
• Delayed gastric emptying.
• Severe kidney problems.
• Hypophosphatemia (low phosphate levels).
• Hypermagnesemia (high magnesium levels).

Drug Interactions

• Antacids (aluminum or magnesium hydroxide).
• Antibiotics (tetracyclines, fluoroquinolones).
• Anticonvulsants (phenytoin, oxcarbazepine).
• Thyroid medications (levothyroxine, thiamazole).
• H2-receptor antagonists (cimetidine).
• Other local anesthetics.
• CNS depressants.
• Pain killers (aspirin).
• Anti-asthma medications (albuterol, ipratropium).
• Anti-diabetic medications (glipizide).
• Vitamins (D3, C).
• Citric fruits.
• Alcohol.

Pregnancy and Breastfeeding

• Pregnancy Safety Category: Not definitively established. Consult a doctor before use.
• Breastfeeding: Safety not established. Consult a doctor before use.

Drug Profile Summary

• Mechanism of Action: Local anesthetic, blocks sodium channels.
• Side Effects: Constipation, dizziness, drowsiness, dry mouth, nausea, allergic reactions.
• Contraindications: Hypersensitivity, active GI bleeding, severe renal impairment.
• Drug Interactions: Antacids, antibiotics, anticonvulsants, thyroid medications.
• Pregnancy & Breastfeeding: Consult a doctor before use.
• Dosage: Adult: 10ml suspension four times daily; pediatric: consult pediatrician, special cases: consult doctor.
• Monitoring Parameters: Renal function, electrolyte levels.

Popular Combinations

• Oxetacaine is frequently combined with sucralfate and/or antacids (aluminum hydroxide and magnesium hydroxide). The rationale for this combination is to provide comprehensive relief from peptic ulcer symptoms by addressing both the pain and the underlying acidity.

Precautions

• General Precautions: Assess for allergies, renal/hepatic impairment, concomitant medications.
• Specific Populations: Caution in pregnant/breastfeeding women, children, and the elderly.
• Lifestyle Considerations: Limit alcohol consumption; may cause drowsiness, affecting driving ability.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Oxetacaine?

A: Adults: Typically 10 ml of oral suspension (containing 1000mg sucralfate and 20mg oxetacaine), four times a day. For children: Consult with a pediatrician. For elderly patients and those with renal/hepatic impairment: Dose adjustment may be necessary.

Q2: How does Oxetacaine work?

A: Oxetacaine is a local anesthetic that blocks nerve signals, providing a numbing effect to relieve pain in the mouth, esophagus, or other affected areas.

Q3: What are the common side effects of Oxetacaine?

A: Common side effects may include constipation, dizziness, drowsiness, dry mouth, nausea, diarrhea.

Q4: Is Oxetacaine safe during pregnancy or breastfeeding?

A: The safety of Oxetacaine during pregnancy and breastfeeding is not fully established. Consult a doctor before use.

Q5: What are the contraindications for Oxetacaine use?

A: Oxetacaine is contraindicated in patients with hypersensitivity to the drug, active gastrointestinal bleeding, delayed gastric emptying, and severe renal impairment.

Q6: Does Oxetacaine interact with other medications?

A: Yes, it may interact with antacids, antibiotics, anticonvulsants, thyroid medications, and other drugs. Inform your doctor about all your medications.

Q7: Can Oxetacaine be used in children?

A: The safety and efficacy in children under 12 or 14 years have not been established. The use and dosage should be determined by a doctor for older children.

Q8: How should Oxetacaine be stored?

A: Store at room temperature, away from excessive heat, moisture, and direct sunlight. Keep out of reach of children.

Q9: What should I do if I miss a dose of Oxetacaine?

A: Take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not double the dose to catch up.

Q10: Can I take oxetacaine with or without food?

A: You should preferably take oxetacaine on an empty stomach, approximately 1 hour before meals. However, in certain cases such as dyspepsia or stomach ulcers, it can also be taken with snacks or with meals. Consult your doctor for specific advice.