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Generic Name: Amlexanox
Class: EENT Drugs, Miscellaneous
VA Class: OR900
Chemical Name: 2-amino-7-isopropyl-5-oxo-5H-[1]benzopyrano[2,3-b] pyridine-3-carboxylic acid
Molecular Formula: C16H14N2O4
CAS Number: 68302-57-8


Aphthous ulcer healing agent.1

Uses for Aphthasol

Aphthous Ulcers

Treatment of aphthous ulcers in patients with normal immune systems.1

Safety and efficacy not established in immunocompromised patients.1

Aphthasol Dosage and Administration


Oral, Topical Use Only

Apply topically to oral cavity as a paste.1 Not for ophthalmic use.1

Apply paste as soon as possible after noticing aphthous ulcer symptoms.1 Apply 4 times daily, preferably following oral hygiene after breakfast, lunch, dinner, and at bedtime.1

Before application, dry ulcer(s) by gently patting with a soft, clean cloth.1 Wash hands and apply paste onto moistened index finger tip; dab paste with gentle pressure onto each ulcer in the mouth.1

Wash hands when application is finished.1



Aphthous Ulcers
Oral, Topical Use Only

Apply approximately 0.5 cm (¼ inch) onto each ulcer 4 times daily.1

Continue treatment until ulcer heals.1 If substantial healing or pain reduction has not occurred in 10 days, consult dentist or physician.1

Special Populations

Geriatric Patients

Select dosage with caution, usually starting at the low end of the dosage range, because of possible age-related decreases in hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.1

Cautions for Aphthasol


  • Known hypersensitivity to amlexanox or any ingredient in the formulation.1


Sensitivity Reactions

Hypersensitivity Reactions

Discontinue use if rash or contact mucositis occurs.1

Specific Populations


Category B.1


Distributed into milk in rats.1 Caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established.1

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.1 Other clinical experience has not identified differences in responses between geriatric and younger patients.1 Select dosage with caution.1 (See Geriatric Patients under Dosage and Administration.)

Common Adverse Effects

Transient pain, stinging, and/or burning at application site.1 3

Interactions for Aphthasol

No formal drug interaction studies to date.1

Aphthasol Pharmacokinetics



Not substantially absorbed through the active ulcer;1 systemic absorption occurs mostly via the GI tract.1 3

Peak serum concentrations attained 2.4 hours after a single oral application of 100 mg of paste (5 mg amlexanox).1 3

Steady-state concentrations reached within 1 week after multiple applications 4 times daily; no accumulation observed with ≤4 weeks of use.1 3



Distributed into milk in rats.1


Elimination Route

Approximately 17% of dose is excreted in urine as unchanged drug, hydroxylated metabolite, and conjugates.1 3


Approximately 3.5 hours (range: 2.4–4.6 hours).1 3



Oral, Topical Use Only




  • Accelerates healing of aphthous ulcers; precise mechanism of such effect unknown.1 2 3

  • Potent in vitro inhibitor of formation and/or release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils, and mononuclear cells.1 4 5

Advice to Patients

  • Importance of learning and adhering to proper administration techniques.1

  • Importance of initiating treatment as soon as possible after noticing symptoms of an aphthous ulcer.1

  • Importance of using until the ulcer heals or consulting a clinician if substantial healing or pain relief has not occurred in 10 days.1

  • Importance of discontinuing treatment if rash or contact mucositis occurs.1

  • Importance of avoiding contact with eyes; if ocular contact occurs, rinse eye(s) promptly.1

  • Keep out of reach of children.1

  • Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as concomitant illnesses.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.



Dosage Forms


Brand Names


Oral (Topical Use Only)





AHFS DI Essentials. © Copyright 2017, Selected Revisions April 1, 2008. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. Access Pharmaceuticals, Inc. Aphthasol (amlexanox) oral paste 5% prescribing information. Dallas, TX; 2004 Mar.

2. Khandwala A, Van Inwegen RG, Alfano MC. 5% amlexanox oral paste, a new treatment for recurrent minor aphthous ulcers: I. Clinical demonstration of acceleration of healing and resolution of pain. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 1997; 83:222-30. [PubMed 9117754]

3. Khandwala A, Van Inwegen RG, Charney MR et al. 5% amlexanox oral paste, a new treatment for recurrent minor aphthous ulcers: II. Pharmacokinetics and demonstration of clinical safety. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 1997; 83:231-8. [PubMed 9117755]

4. Saijo T, Kuriki H, Ashida Y et al. Mechanism of the action of amoxanox (AA-673), an orally active antiallergic agent. Int Arch Allergy Appl Immunol. 1985; 78:43-50. [PubMed 2411669]

5. Makino H, Saijo T, Ashida Y et al. Mechanism of action of an antiallergic agent, amlexanox (AA-673), in inhibiting histamine release from mast cells. Int Arch Allergy Appl Immunol. 1987; 82:66-71. [PubMed 2433225]

6. Discus Dental, Culver City, CA: Personal communication.