Hydrocortisone acetate

Absorption

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.

Toxicity

Side effects include inhibition of bone formation, suppression of calcium absorption and delayed wound healing

Chemical properties

white powder

The Uses of Hydrocortisone acetate

Hydrocortisone acetate is used to treat hemorrhoids and itching/swelling in the rectum and anus. It is used to treat certain intestinal problems (such as ulcerative colitis of the rectum and other rectal/anal inflammatory conditions).

The Uses of Hydrocortisone acetate

Glucocorticoid

Indications

For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addisons disease). It is also used to treat many immune and allergic disorders, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.

What are the applications of Application

Hydrocortisone 21-acetate is a corticosteroid with anti-inflammatory properties

Definition

ChEBI: Cortisol 21-acetate is a tertiary alpha-hydroxy ketone and a cortisol ester.

brand name

Cortef Acetate (Pharmacia & Upjohn); Cortifoam (Schwarz Pharma); Cortril (Pfizer); Dricort (Ingram); Hydrocortone (Merck).

Pharmacokinetics

Hydrocortisone is the most important human glucocorticoid. It is essential for life and regulates or supports a variety of important cardiovascular, metabolic, immunologic and homeostatic functions. Topical hydrocortisone is 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.

Clinical Use

Corticosteroid:

Local inflammation of joints and soft tissue

Drug interactions

Potentially hazardous interactions with other drugs
Aldesleukin: avoid concomitant use.
Antibacterials: metabolism accelerated by rifampicin; metabolism possibly inhibited by erythromycin; concentration of isoniazid possibly reduced.
Anticoagulants: efficacy of coumarins and phenindione may be altered.
Antiepileptics: metabolism accelerated by carbamazepine, phenobarbital, fosphenytoin, phenytoin and primidone.
Antifungals: increased risk of hypokalaemia with amphotericin - avoid; metabolism possibly inhibited by itraconazole and ketoconazole.
Antivirals: concentration possibly increased by ritonavir.
Ciclosporin: rare reports of convulsions in patients on ciclosporin and high-dose corticosteroids
. Cobicistat: concentration of hydrocortisone possibly increased - increased risk of adrenal suppression.
Diuretics: enhanced hypokalaemic effects of acetazolamide, loop diuretics and thiazide diuretics.
Vaccines: high dose corticosteroids can impair immune response to vaccines - avoid concomitant use with live vaccines.

Metabolism

Primarily hepatic via CYP3A4

Metabolism

Hydrocortisone is metabolised in the liver and most body tissues to hydrogenated and degraded forms such as tetrahydrocortisone and tetrahydrocortisol. These are excreted in the urine, mainly conjugated as glucuronides, with a very small proportion of unchanged hydrocortisone.

Purification Methods

The acetate recrystallises from Me2CO/Et2O or aqueous Me2CO as hygroscopic monoclinic crystals. UV has max at 242 nm (A1cm 1% 390) in MeOH. Its solubility at 25o is: H2O (0.001%), EtOH (0.45%), MeOH (0.04%), Me2CO (1.1%), CHCl3 (0.5%), Et2O (0.15%), and it is very soluble in Me2NCHO. [Wendler et al. J Am Chem Soc 74 3630 1952; Antonucci et al. J Org Chem 18 7081 1953, Beilstein 8 IV 3424.]