Amlexanox (Mucosal-Local)

VA CLASSIFICATION
Primary: OR900

Commonly used brand name(s): Aphthasol.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antiulcer agent (topical)—

Indications

Accepted

Stomatitis, aphthous (treatment)—Amlexanox is indicated for the treatment of aphthous stomatitis (aphthous ulcers) in people with normal immune systems. ^{01}


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    298.3 ^{01}

Mechanism of action/Effect:

The exact mechanism of action is unknown. In vitro studies show amlexanox to inhibit the formation and release of histamine and leukotrienes from mast cells, neutrophils, and mononuclear cells. ^{01}

Absorption:

The maximum serum concentration is approximately 120 nanograms per mL following oral application of 100 mg of amlexanox oral paste. Most of the systemic absorption of amlexanox is via the gastrointestinal tract, and the amount absorbed directly through the active ulcer is not a significant portion of the applied dose. ^{01}



Half-life:


Elimination:

3.5 ± 1.1 hours. ^{01}


Elimination:
    Renal—Up to 17% of the total dose may be excreted in the urine. ^{01}


Precautions to Consider

Carcinogenicity

Amlexanox was not found to be carcinogenic following oral administration to rats for 2 years and mice for 18 months. ^{01}

Mutagenicity

In vitro and in vivo animal studies found no mutagenic potential of amlexanox. ^{01}

Pregnancy/Reproduction
Fertility—
Amlexanox did not significantly affect fertility of rats when it was administered at 200 times the estimated human daily dose on a mg per square meter of body surface area (mg/m ²). ^{01}

Pregnancy—
Adequate and well-controlled studies in humans have not been done. Amlexanox was not found to be teratogenic when administered to rats and rabbits at doses 200 and 600 times, respectively, the estimated human daily dose on a mg/m ² basis. ^{01}

FDA Pregnancy Category B. ^{01}

Breast-feeding

Amlexanox was found in the milk of lactating rats. Problems in humans have not been documented. ^{01}

Pediatrics

Appropriate studies on the relationship of age to the effects of amlexanox have not been performed in the pediatric population. Safety and efficacy have not been established. ^{01}


Geriatrics


No information is available on the relationship of age to the effects of amlexanox in geriatric patients. ^{01}

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
Sensitivity to amlexanox or other components of the formulation^{01}
Immune deficiency conditions in patients who are immunocompromised     (safety and efficacy have not been assessed ^{01})




Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent
    
Burning, stinging, or pain at application site^{01}

Incidence rare
    
Contact mucositis ^{01}(inflammation of mucous membranes)
    
diarrhea^{01}
    
nausea^{01}





Overdose
For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

There are no reports of human ingestion overdose. Ingestion of a tube containing 5 grams of paste would result in systemic exposure below the maximum nontoxic dose of amlexanox in animals and produce side effects such as diarrhea and vomiting. ^{01}


Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Amlexanox (Mucosal-Local) .
In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to amlexanox or other components of the formulation

Proper use of this medication
Applying the paste as soon as symptoms occur ^{01}

Applying a small amount of paste (approximately 1/4 inch), using gentle pressure, to each ulcer in the mouth ^{01}

Washing hands immediately after applying paste ^{01}

Using paste until ulcers are healed, but not longer than 10 days ^{01}

Avoiding application in or near the eyes ^{01}

» Proper dosing
Missed dose: Applying as soon as possible; not applying if almost time for the next dose ^{01}

» Proper storage ^{01}


General Dosing Information
Apply as soon as possible after noticing the symptoms of an aphthous ulcer.

Amlexanox paste should be applied four times a day, preferably following oral hygiene after breakfast, lunch, and dinner and at bedtime.

Avoid contact with eyes.

Safety and efficacy have not been assessed in immunocompromised individuals.


Topical Dosage Forms

AMLEXANOX ORAL PASTE

Usual adult dose
Aphthous stomatitis
Topical, to aphthous ulcers four times a day, until healed. Use is not recommended for longer than ten days. ^{01}


Usual pediatric dose
Safety and efficacy have not been established. ^{01}

Strength(s) usually available
U.S.—


5% (Rx) [Aphthasol (benzyl alcohol) (gelatin) (glyceryl monostearate) (mineral oil) (pectin) (petrolatum) (sodium carboxymethylcellulose)]^{01}

Packaging and storage:
Store at controlled room temperature, preferably between 15 and 30 ºC (59 and 86 ºF). ^{01}

Auxiliary labeling:
   • Avoid contact with eyes.

Developed: 08/10/1998

References

1. Aphthasol package insert (Block Drug Co—US), New 12/96, Rec 4/97.