Indication |
For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. |
Pharmacodynamics |
Like other topical corticosteroids, desoximetasone has
anti-inflammatory, antipruritic, and vasoconstrictive properties. Once
absorbed through the skin, topical corticosteroids are handled through
pharmacokinetic pathways similar to systemically administered
corticosteroids. Desoximetasone is a potent topical corticosteroid that
should not be used with occlusive dressings. It is recommended that
treatment should be limited to 2 consecutive weeks and therapy should be
discontinued when adequate results have been achieved. |
Mechanism of action |
The precise mechanism of the antiinflammatory activity of topical
steroids in the treatment of steroid-responsive dermatoses, in general,
is uncertain. However, corticosteroids are thought to act by the
induction of phospholipase A2 inhibitory proteins,
collectively called lipocortins. This is achieved first by the drug
binding to the glucocorticoid receptors which then translocates into the
nucleus and binds to DNA causing various activations and repressions of
genes. It is postulated that these proteins control the biosynthesis of
potent mediators of inflammation such as prostaglandins and
leukotrienes by inhibiting the release of their common precursor
arachidonic acid. Arachidonic acid is released from membrane
phospholipids by phospholipase A2. |
Absorption |
Topical corticosteroids can be absorbed from intact healthy skin.
The extent of percutaneous absorption of topical corticosteroids is
determined by many factors, including the vehicle and the integrity of
the epidermal barrier. Occlusion, inflammation and/or other disease
processes in the skin may also increase percutaneous absorption. |
Volume of distribution |
Not Available |
Protein binding |
Bound to plasma proteins in varying degrees. |
Metabolism |
Metabolized, primarily in the liver, and then excreted by the kidneys. |
Route of elimination |
Corticosteroids are bound to plasma proteins in varying degrees,
are metabolized primarily in the liver and excreted by the kidneys. Some
of the topical corticosteroids and their metabolites are also excreted
into the bile.Pharmacokinetic studies in men with Desoximetasone Cream
USP, 0.25% with tagged desoximetasone showed a total of 5.2% ± 2.9%
excretion in urine (4.1% ± 2.3%) and feces (1.1% ± 0.6%) |
Half life |
The half-life of the material was 15 ± 2 hours (for urine) and 17 ± 2 hours (for feces) between the third and fifth trial day. |
Clearance |
Not Available |
Toxicity |
Topically applied desoximetasone can be absorbed in sufficient
amounts to produce systemic effects. Symptoms of overdose include
thinning of skin and suppression of adrenal cortex (decreased ability to
respond to stress). |