Indication |
Used as a paste in the mouth to treat aphthous ulcers (canker sores). |
Pharmacodynamics |
Amlexanox is a mucoadhesive oral paste which has been clinically
proven to abort the onset, accelerate healing and resolve the pain of
aphthous ulcers (canker sores). It decreases the time ulcers take to
heal. Because amlexanox decreases the healing time, it also decreases
the pain you feel. Recent studies have also shown that the majority of
ulcers can be prevented by application of the paste during the prodromal
(pre-ulcerative) phase of the disease. Recurrent Aphthous Ulcers (RAU)
also known as Recurrent Aphthous Stomatitis (RAS) is recognized as the
most common oral mucosal disease known to man. Estimates suggest that
20% - 25% of the general population suffer at least one incidence of
aphthous ulcers each year. Amlexanox is also being investigated for its
anti-allergenic and anti-inflammatory properties. |
Mechanism of action |
As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox
has anti-inflammatory and antiallergic properties. It inhibits chemical
mediatory release of the slow-reacting substance of anaphylaxis (SRS-A)
and may have antagonistic effects on interleukin-3. When cells are under
stress, they release an inactive form of human fibroblast growth factor
1 (FGF-1), a potent mitogen (entity that causes mitosis). Amlexanox
binds to FGF1, increasing its conformational stability, sterically
blocking Cu(2+) induced oxidation which normally leads to activation of
FGF-1. |
Absorption |
No significant absorption directly through the active ulcer. Most of the systemic absorption is via the gastrointestinal tract. |
Volume of distribution |
Not Available |
Protein binding |
Not Available |
Metabolism |
Metabolized to hydroxylated and conjugated metabolites. |
Route of elimination |
Not Available |
Half life |
Elimination half-life is 3.5 ± 1.1 hours. |
Clearance |
Not Available |
Toxicity |
Not Available |