Indication |
Used topically as an antiinflammatory in the treatment of steroid-responsive dermatoses |
Pharmacodynamics |
Hydrocortamate is a synthetic glucocorticoid used for its
anti-inflammatory or immunosuppressive properties to treat inflammation
due to corticosteroid-responsive dermatoses. Glucocorticoids are a class
of steroid hormones characterised by an ability to bind with the
cortisol receptor and trigger a variety of important cardiovascular,
metabolic, immunologic and homeostatic effects. Glucocorticoids are
distinguished from mineralocorticoids and sex steroids by having
different receptors, target cells, and effects. Technically, the term
corticosteroid refers to both glucocorticoids and mineralocorticoids,
but is often used as a synonym for glucocorticoid. Glucocorticoids
suppress cell-mediated immunity. They act by inhibiting genes that code
for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and
TNF-alpha, the most important of which is the IL-2. Reduced cytokine
production limits T cell proliferation. Glucocorticoids also suppress
humoral immunity, causing B cells to express lower amounts of IL-2 and
IL-2 receptors. This diminishes both B cell clonal expansion and
antibody synthesis. The diminished amounts of IL-2 also leads to fewer T
lymphocyte cells being activated. |
Mechanism of action |
Hydrocortamate binds to the cytosolic glucocorticoid receptor.
After binding the receptor the newly formed receptor-ligand complex
translocates itself into the cell nucleus, where it binds to many
glucocorticoid response elements (GRE) in the promoter region of the
target genes. The DNA bound receptor then interacts with basic
transcription factors, causing the increase in expression of specific
target genes. The anti-inflammatory actions of corticosteroids are
thought to involve lipocortins, phospholipase A2 inhibitory proteins
which, through inhibition arachidonic acid, control the biosynthesis of
prostaglandins and leukotrienes. The immune system is suppressed by
corticosteroids due to a decrease in the function of the lymphatic
system, a reduction in immunoglobulin and complement concentrations, the
precipitation of lymphocytopenia, and interference with
antigen-antibody binding. |
Absorption |
Not Available |
Volume of distribution |
Not Available |
Protein binding |
Not Available |
Metabolism |
Primarily hepatic via CYP3A4 |
Route of elimination |
Not Available |
Half life |
Not Available |
Clearance |
Not Available |
Toxicity |
Side effects include burning, itching, irritation, dryness,
folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation,
perioral dermatitis, allergic contact dermatitis, maceration of the
skin, secondary infection, skin atrophy, striae, miliaria. |