Amlexanox

Approved Indications:

• Recurrent Aphthous Stomatitis (RAS): Indicated for the treatment of aphthous ulcers (canker sores) of the oral mucosa to reduce healing time, pain, and ulcer size.
• Minor Aphthous Ulcers: Provides local symptomatic relief and accelerates healing.

Clinically Accepted Off-label Uses:

• Oral ulcers in Behçet’s disease: Used for symptomatic relief and ulcer resolution in recurrent oral ulcers associated with Behçet’s syndrome.
• Oral Lichen Planus (erosive form): Occasionally used off-label to relieve local inflammation and pain.
• Post-traumatic or irritant oral ulcers: Used to reduce healing time in select cases.

Adults and Adolescents (≥12 years):

• Dose: Apply approximately 0.5 cm of the 5% paste directly to each ulcer.
• Frequency: 4 times daily (preferably after meals and at bedtime).
• Method: Dab gently onto the ulcer surface using a clean fingertip; do not rub.
• Duration: Continue for 5–10 days or until ulcer resolution.

Pediatric Use (<12 years):

• Not routinely recommended; safety and efficacy not established. Use only under physician guidance.

Elderly:

• No dose adjustment required. Use with standard adult regimen unless medically indicated.

Special Populations:

• Renal Impairment: No dosage adjustment necessary due to negligible systemic absorption.
• Hepatic Impairment: No specific dose adjustment required; however, clinical judgment should prevail in moderate to severe hepatic dysfunction.

Amlexanox is a topical anti-inflammatory and anti-allergic agent. It inhibits the release of histamine, leukotrienes, and other inflammatory mediators from mast cells and neutrophils. The drug also acts as a selective inhibitor of IκB kinase (IKK), which prevents activation of nuclear factor-kappa B (NF-κB), a key transcription factor in inflammatory gene expression. This inhibition reduces cytokine production, resulting in reduced inflammation, pain, and accelerated healing of oral ulcers.

• Absorption: Minimal systemic absorption through intact oral mucosa; acts locally.
• Distribution: Remains localized at the site of application; systemic distribution is clinically insignificant.
• Metabolism: If absorbed, presumed to undergo hepatic metabolism.
• Elimination: Small amounts absorbed may be excreted via urine.
• Half-life: Not clinically relevant due to low systemic availability.
• Bioavailability: Low systemic bioavailability; primarily for topical effect.
• Onset of Action: Partial relief often begins within 24–48 hours of use.

• Pregnancy: FDA Pregnancy Category C. Animal studies show some risk; no well-controlled studies in humans. Use only if clearly needed.
• Lactation: Unknown if excreted in breast milk; due to low systemic absorption, risk to the nursing infant is considered minimal. Caution advised.
• Summary: Not contraindicated in pregnancy or lactation, but use only when benefits outweigh potential risks.

• Primary Class: Topical Anti-inflammatory Agent
• Subclass: Oral Ulcer Healing Agent / Anti-allergic Topical Agent
• Form: Mucosal paste formulation for localized effect

• Hypersensitivity to amlexanox or any component of the formulation
• Known allergic reaction to other topical anti-inflammatory pastes
• Use in children under 12 years without supervision
• Do not apply to infected, bleeding, or non-aphthous ulcers

• Hypersensitivity reactions (e.g., localized rash, swelling, itching); discontinue if reactions occur
• Avoid use in ulcers of infectious origin (e.g., viral, fungal, or bacterial lesions)
• Do not ingest the paste; accidental swallowing may lead to mild GI discomfort
• Avoid eating or drinking immediately after application to ensure therapeutic effect
• Not intended for ophthalmic or intranasal use
• Long-term use not studied; limit use to 10 days unless directed by a physician

Common (usually mild and localized):

• Stinging or burning at the site of application
• Mild tingling or irritation of the oral mucosa
• Transient metallic taste

Less Common:

• Local swelling or erythema
• Ulcer enlargement (rare and usually reversible upon discontinuation)

Rare but Serious:

• Hypersensitivity reaction including lip or facial swelling
• Allergic dermatitis

Note: Most adverse effects are local and self-limiting.

• Drug-Drug: No clinically significant interactions reported due to limited systemic absorption
• Drug-Food: Eating or drinking immediately after application may reduce drug adherence to mucosa
• Drug-Alcohol: No interactions documented
• Enzyme System: No known impact on CYP450 isoenzymes

• No recent FDA or EMA changes in approved use or warnings for amlexanox
• Continued inclusion in clinical guidelines as a safe and effective agent for aphthous ulcer management
• Investigational systemic applications in asthma and metabolic disorders remain unapproved

• Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C–30°C
• Protect from light and moisture
• Do not freeze
• Keep cap tightly closed after each use
• No refrigeration or reconstitution required
• Keep out of reach of children