Aphthasol contains 5% amlexanox in an adhesive oral paste. Chemically, amlexanox is 2-amino-7-isopropyl-5-oxo-5H-[1]benzopyrano[2,3-b] pyridine-3-carboxylic acid. It has a molecular formula of C₁₆H₁₄N₂O₄ and has a molecular weight of 298.30. Amlexanox is odorless, white to yellowish-white crystalline powder. The structural formula is:

Each gram of beige colored oral paste contains 50 mg of amlexanox in an adhesive oral paste base consisting of benzyl alcohol, gelatin, glyceryl monostearate, mineral oil, pectin, petrolatum, and sodium carboxymethylcellulose.

Last updated on RxList: 6/2/2009

Amlexanox oral paste, 5%, is indicated for the treatment of aphthous ulcers in people with normal immune systems.

The paste should be applied as soon as possible after noticing the symptoms of an aphthous ulcer and should be used four times daily, preferably following oral hygiene after breakfast, lunch, dinner, and at bedtime. Squeeze a dab of paste approximately ¼ inch (0.5 cm) onto a finger tip. With gentle pressure, dab the paste onto each ulcer in the mouth. Use of the medication should be continued until the ulcer heals. If significant healing or pain reduction has not occurred in 10 days, consult your dentist or physician.

Amlexanox oral paste, 5%, is supplied in 5 gram tubes (NDC10158-059-01). Amlexanox oral paste, 5%, should be stored at controlled room temperature, 15°-30°C (59°- 86°F).

Manufactured for: Oral Health Care Division, Block Drug Company, Inc., Jersey City, NJ 07302. By Reedco, Inc., Humacao, Puerto Rico 00791. June 2002.

Last updated on RxList: 6/2/2009

Adverse reactions considered related or possibly related to amlexanox oral paste, 5%, were not reported by more than 5% of patients. Adverse reactions reported by 1-2% of patients were transient pain, stinging and/or burning at the site of application. Infrequent ( < 1%) adverse reactions in the clinical studies were contact mucositis, nausea, and diarrhea.

No information provided.

Last updated on RxList: 6/2/2009

No information provided.

General

Wash hands immediately after applying amlexanox oral paste, 5%, directly to ulcers with the finger tips. In the event that a rash or contact mucositis occurs, discontinue use.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Amlexanox was not carcinogenic when administered orally to rats for two years and to mice for 18 months. In vitro (Ames) and in vivo (mouse micronucleus) mutagenicity tests of amlexanox were negative. Amlexanox at doses up to two hundred times the projected human daily dose, on a mg/m² basis, did not significantly affect fertility or general reproductive performance in rats.

Pregnancy Category B

Teratology studies were performed with rats and rabbits at doses up to two hundred and six hundred times, respectively, the projected human daily dose, on a mg/m² basis. No adverse fetal effects were observed. At doses up to two hundred times the projected human daily dose, on a mg/m² basis, amlexanox did not have significant effect on peri- and postnatal development of rat fetuses. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers

Amlexanox was found in the milk of lactating rats; therefore, caution should be exercised when administering amlexanox oral paste, 5%, to a nursing woman.

Pediatric Use

Safety and effectiveness of amlexanox oral paste, 5%, in pediatric patients have not been established.

Geriatric Use

Clinical studies of Aphthasol did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Last updated on RxList: 6/2/2009

There are no reports of human ingestion overdosage. Ingestion of a full tube of 5 grams of paste would result in systemic exposure well below the maximum nontoxic dose of amlexanox in animals. Gastrointestinal upset such as diarrhea and vomiting could result from an overdose.

Amlexanox oral paste, 5%, is contraindicated in patients with known hypersensitivity to amlexanox or other ingredients in the formulation.

Last updated on RxList: 6/2/2009

The mechanism of action by which amlexanox accelerates healing of aphthous ulcers is unknown. In vitro studies have demonstrated amlexanox to be a potent inhibitor of the formation and/or release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils and mononuclear cells. Given orally to animals, amlexanox has demonstrated anti-allergic and anti-inflammatory activities and has been shown to suppress both immediate and delayed type hypersensitivity reactions. The relevance of these activities of amlexanox to its effects on aphthous ulcers has not been established.

Pharmacokinetics and Metabolism

After a single oral application of 100 mg of paste (5 mg amlexanox), maximal serum levels of approximately 120 ng/ml are observed at 2.4 hours. 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. The half-life for elimination was 3.5 +/- 1.1 hours in healthy individuals. Approximately 17% of the dose is eliminated into the urine as unchanged amlexanox, a hydroxylated metabolite, and their conjugates. With multiple applications four times daily, steady state levels were reached within one week, and no accumulation was observed with up to four weeks of usage.

Clinical Studies

The safety of amlexanox oral paste, 5%, was established in a study in which 100 patients with aphthous ulcers applied the medication four times daily for 28 days with no significant topical or systemic adverse effects. The effectiveness was demonstrated in three controlled clinical studies of patients with mild to moderate aphthous ulcers which evaluated 464 patients receiving amlexanox oral paste, 5%, 465 patients receiving a placebo paste, and 195 patients receiving no treatment. Amlexanox oral paste, 5%, was shown to accelerate healing of aphthous ulcers in a statistically significant manner as compared to both vehicle and no treatment.

Amlexanox oral paste, 5%, versus no treatment

In the combined database of the two studies including a no treatment group, there was a significant difference in the rate of ulcer healing which translated to a reduction of 1.6 days in the median time to complete healing and a reduction of 1.3 days in the median time to complete pain relief. After 3 days of treatment there was a significant difference in both percent of patients with complete healing of ulcers (21% vs. 8%) and percent of patients with complete resolution of pain (44% vs. 20%).

Amlexanox oral paste, 5%, versus vehicle

In the combined database of the three studies, there was a significant difference in the rate of ulcer healing which translated into a reduction of 0.7 days in the median time to complete healing, and a reduction of 0.7 days in the median time to complete pain relief. After 4 days of treatment there was a significant difference in both percent of patients with complete healing of ulcers (37% vs. 27%) and percent of patients with complete resolution of pain (60% vs. 49%).

Pain relief occurred in conjunction with healing of the ulcers. Amlexanox oral paste, 5%, by itself, was not shown to be an analgesic medication. The safety and effectiveness of the product in immunocompromised individuals has not been assessed.

Cumulative % of Patients with Healed Ulcers

Results for amlexanox, 5%, vs. vehicle are based on three clinical trials. Results for amlexanox, 5%, vs. no treatment are based on two clinical trials.
* denotes statistically significant superiority of amlexanox, 5%, vs. vehicle and no treatment.
# denotes statistically significant superiority of amlexanox, 5%, vs. no treatment.
Error bars represent Standard Error of the Mean.

Last updated on RxList: 6/2/2009

1. Apply the paste as soon as possible after noticing the symptoms of an aphthous ulcer. Continue to use the paste four times daily, preferably following oral hygiene after breakfast, lunch, dinner, and at bedtime.
2. Dry the ulcer(s) by gently patting it with a soft, clean cloth.
3. Wash your hands before applying the Aphthasol.
4. Moisten the tip of your index finger.
5. Squeeze a dab of paste approximately 1/4 inch (0.5 cm) onto a finger tip.
6. Gently dab the Aphthasol on to the ulcer. Repeat the process if you have more than one ulcer.
7. Wash your hands when you are done applying Aphthasol.
8. Wash eyes promptly if they should come in contact with the paste.
9. Use the paste until the ulcer heals. If significant healing or pain relief has not occurred in 10 days, consult your dentist or physician.
10. Keep out of the reach of children.

Last updated on RxList: 6/2/2009

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

AMLEXANOX - MUCOUS MEMBRANE

(am-LEX-a-nox)

COMMON BRAND NAME(S): Aphthasol

USES: This medication is used to treat mouth (canker) sores. Canker sores usually heal on their own after 7 to 10 days. This medication helps the sore heal faster so that you can eat/speak more comfortably.

HOW TO USE: Use this medication in the mouth only. Use it as soon as you notice a canker sore forming, usually 4 times daily or as directed by your doctor. Use this medication until the sore heals.

The best time to apply the medication is after brushing/flossing after meals and at bedtime. Wash your hands before applying the medication. Dry the canker sore by patting gently with a soft, clean cloth. Wet the tip of your index finger with a little water, and squeeze a pea-sized amount of the medication onto the fingertip. Gently dab the medication onto the sore. Repeat these steps if you have more than 1 canker sore. Wash your hands after using.

Do not to get the medication in the eyes. If you do get the medication in the eyes, flush with plenty of water.

Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same times each day.

Tell your doctor/dentist if your condition worsens or does not improve greatly after 10 days.

SIDE EFFECTS: Temporary pain, stinging, or burning at the application site may occur. If any of these effects persist or worsen, tell your doctor/dentist or pharmacist promptly.

Remember that your doctor/dentist has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor/dentist immediately if any of these unlikely but serious side effects occur: increased mouth sores, nausea, diarrhea.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using amlexanox, tell your doctor/dentist or pharmacist if you are allergic to it; or if you have any other allergies.

Before using this medication, tell your doctor/dentist or pharmacist your medical history, especially of: immune system problems.

Avoid alcohol and nicotine because these products can irritate the sores.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.

Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: This medication may be harmful if swallowed. If overdose or swallowing is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose or swallowing may include: diarrhea, vomiting.

NOTES: Do not share this medication with others.

To help heal mouth sores, drink plenty of fluids, practice good oral hygiene (e.g., brushing and flossing regularly), and avoid irritating/acidic foods like citrus fruits and juices (e.g., grapefruit, orange, lemon), tomatoes, and spicy/salty foods. Eat foods cold or at room temperature. Warmer foods might irritate your mouth and throat.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C). Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.