Usage
- Amlexanox 5% oral paste is prescribed for the treatment of aphthous ulcers (canker sores) in patients with normal immune systems. It promotes faster healing and reduces discomfort associated with these ulcers.
- Pharmacological classification: Anti-inflammatory, immunomodulator.
- Mechanism of action: While not fully elucidated, amlexanox appears to inhibit the release of inflammatory mediators like histamine and leukotrienes from mast cells, neutrophils, and mononuclear cells. It may also form a protective layer over the ulcer, facilitating healing.
Alternate Names
- No widely used alternate names.
- Brand names: Aphthasol.
How It Works
- Pharmacodynamics: Amlexanox reduces inflammation and pain associated with aphthous ulcers. It accelerates healing by potentially modulating the immune response and creating a protective barrier over the ulcer.
- Pharmacokinetics: After oral application, systemic absorption is minimal. Most of the drug is absorbed through the gastrointestinal tract, not directly through the ulcer. Peak serum levels are reached in about 2.4 hours after a single 100mg dose of 5% paste (5mg amlexanox). The elimination half-life is approximately 3.5 hours.
- Mode of action: Inhibition of inflammatory mediator release (histamine, leukotrienes) from immune cells.
- Receptor binding/enzyme inhibition/neurotransmitter modulation: The precise mechanisms are not fully understood, but it is known to inhibit certain protein kinases (TBK1 and IKKε).
- Elimination pathways: Primarily hepatic metabolism with renal excretion.
Dosage
Standard Dosage
Adults:
- Apply a ¼ inch (0.5 cm) ribbon of paste to each ulcer 4 times daily (after breakfast, lunch, dinner, and at bedtime) after oral hygiene.
- Continue until the ulcer heals, usually within 10 days. Consult a physician if no improvement is seen within 10 days.
Children:
- Safety and efficacy in children under 12 have not been established. For adolescents aged 12-17 years, similar dosing as adults may be followed under physician guidance.
Special Cases:
- Elderly Patients: Start at the low end of the dosing range due to potential age-related decrease in hepatic, renal, or cardiac function.
- Patients with Renal Impairment: Dosage adjustment may be needed based on creatinine clearance.
- Patients with Hepatic Dysfunction: Dose adjustments may be required due to potential alterations in drug metabolism.
- Patients with Comorbid Conditions: Caution advised in patients with compromised immune systems. Individualized dosing may be necessary.
Clinical Use Cases
Amlexanox oral paste is specifically indicated for aphthous ulcers. It is not indicated for use in clinical scenarios like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Consider dose reduction in patients with significant hepatic or renal impairment. Monitor for adverse effects and adjust dosage as needed.
Side Effects
Common Side Effects
- Transient pain, stinging, or burning sensation at the application site.
Rare but Serious Side Effects
- Allergic reactions: Rash, hives, itching, difficulty breathing, swelling of the face, lips, tongue, or throat.
- Severe dizziness
- Contact mucositis (inflammation of the mucous membranes).
Long-Term Effects
No significant long-term side effects have been reported.
Adverse Drug Reactions (ADR)
- Allergic reactions requiring immediate medical attention (as described above).
Contraindications
- Hypersensitivity to amlexanox or any component of the formulation.
Drug Interactions
- Clinically significant drug interactions are unlikely due to minimal systemic absorption. However, inform your physician about all medications, including OTC drugs and supplements, being taken.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: B. Animal studies have not shown fetal harm, but there are no adequate studies in pregnant women. Use only if clearly needed.
- Breastfeeding: Amlexanox is present in rat milk; caution advised while breastfeeding. Discuss risks and benefits with your physician.
Drug Profile Summary
- Mechanism of Action: Inhibits inflammatory mediator release.
- Side Effects: Local irritation, burning, stinging; rarely allergic reactions.
- Contraindications: Hypersensitivity.
- Drug Interactions: Unlikely due to low systemic absorption.
- Pregnancy & Breastfeeding: Category B; caution advised in breastfeeding.
- Dosage: ¼ inch ribbon applied 4 times daily to each ulcer.
- Monitoring Parameters: Observe for ulcer healing, resolution of pain, and adverse effects.
Popular Combinations
- Amlexanox is typically used as a single agent for aphthous ulcers.
Precautions
- General Precautions: Screen for allergies, assess immune status.
- Specific Populations: See sections on dosage for elderly, renal/hepatic impairment, pregnancy and breastfeeding.
- Lifestyle Considerations: No specific lifestyle restrictions are necessary.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Amlexanox?
A: Adults and children over 12: Apply a ¼ inch ribbon of paste to each ulcer 4 times a day.
Q2: How long does it take for Amlexanox to work?
A: Most patients experience relief within a few days, and ulcers usually heal within 10 days.
Q3: What should I do if my ulcer doesn’t heal after 10 days of using Amlexanox?
A: Consult your physician.
Q4: Can Amlexanox be used in children?
A: Safety and efficacy haven’t been established in children under 12. Adolescent use (12-17 years) should be under physician guidance.
Q5: Is Amlexanox safe during pregnancy?
A: Pregnancy Category B. Use with caution and only if clearly needed.
Q6: Can I use Amlexanox while breastfeeding?
A: It is present in rat milk. Discuss the risks and benefits with your physician.
Q7: What are the common side effects of Amlexanox?
A: Local irritation, burning, or stinging at the application site.
Q8: Are there any serious side effects of Amlexanox?
A: Rarely, allergic reactions may occur. Seek immediate medical attention if you experience difficulty breathing, swelling, or hives.
Q9: Can Amlexanox interact with other medications I’m taking?
A: Clinically significant interactions are unlikely due to low systemic absorption. However, inform your physician about all medications you’re using.
Q10: How should Amlexanox be stored?
A: Store at room temperature away from excessive heat and moisture, and out of the reach of children.
