Amcinonide (trade name Cyclocort) is a topical glucocorticoid used to treat itching, redness and swelling associated with several dermatologic conditions such as atopic dermatitis and allergic contact dermatitis. Amcinonide can also be classified as a multi-functional small molecule corticosteroid, which has been approved by the FDA and is currently marketed as an ointment, lotion, or cream. It acts as both a transcription factor for responses to glucocorticoids and modulator for other transcription factors while also regulating phospholipase A2 activity.
Medical Uses
Corticosteroids applied topically are used for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses, particularly dermatitis, eczema, and psoriasis. Cyclocort's active ingredient is Amcinonide, with inactive ingredients including petrolatum, benzyl alcohol, sorbitol, butylated hydroxyanisole, propyl gallate, citric acid, glycerin, and/ or propylene glycol. The specific inactive ingredients used depend on the dosage form (ointment, area, or lotion) and help the product retain its chemical and physical integrity while increasing the shelf-life.
Dermatitis, Psoriasis, & Eczema
0.1% Amcinonide cream or ointment is typically applied two to three times daily to treat dermatitis, psoriasis, and/ or eczema while the same strength lotion is usually only used twice daily. This information can be found on the FDA approved label or from the prescribing doctor or pharmacist. Occlusive dressings may be used to supplement Amcinonide treatment, particularly when treating psoriasis.
Adverse Effects
Amcinonide exhibits side effects common among other corticosteroids. While these reactions are uncommon for most delivery vehicles, the use of occlusive dressings increases the likelihood of such effects. These include burning, itching, skin dryness and irritation, acne/ pimples, skin atrophy, blistering, and/ or skin discoloration. While most side effects are mild, a medical professional should be contacted if severe rash, acne, skin deterioration, excessive hair growth, or abnormal weight gain occur. Following package insert instructions for a single topical dose, as detailed on the package insert, should not lead to any toxicities.
Pharmacology
Cyclocort is a synthetic corticosteroid created to imitate natural glucocorticoids. In order to do so, amcinonide acts as an agonist to target glucocorticoid receptors. After interacting with the receptor, endocytosis occurs at which point the drug can bind to DNA within the cell. Gene expression is subsequently modified to produce anti-inflammatory mediators while preventing the formation of inflammatory agents thus reducing overall inflammation and immune system response.
Mechanism of Action
The mechanism by which Amcinonide causes anti-inflammatory responses is unclear with current research focused on similar topical steroids that may possess the same mechanism. This is thought to occur via the induction of lipocortin (phospholipase A2 inhibitor proteins). Ongoing research predicts that Amcinonide prevents the release of arachidonic acid which, in turn, stops the synthesis of the inflammation mediators prostaglandins and leukotrienes. Phospholipase A2 normally causes membrane phospholipids to release arachidonic acid, therefore causing a cascade of reactions leading to inflammation of the skin. Due to Amcinonide's high affinity for the glucocorticoid receptor, a neuroactive ligand-receptor interaction occurs and the initial acid release is inhibited, thus helping to alleviate any itching/ burning symptoms.
Metabolism & Elimination
Amcinonide undergoes transdermal absorption with pharmacokinetic profiles similar to that of other corticosteroids administered systematically. Metabolism occurs mainly in the liver and its hepatic cells. The metabolized compound is predominately filtered through the kidneys and excreted in urine although a small amount is excreted in the bile.
History
Amcinonide was first developed in the United Kingdom in the 1960s and 1970s before being patented by the American Cyanamid company. Lederle Laboratories, most famous for the discovery of the antibacterial tetracycline drug class, began to manufacture of Amcinonide before being acquired by Cyanamid. In 1994, American Cyanamid and its Lederle Lab division was purchased by American Home Products (AHP) before eventually changing the company's name to Wyeth Pharmaceuticals in 2002. Wyeth Pharma was eventually purchased by rival Pfizer in 2009 for $68 billion although the manufacture of Amcinonide has since been discontinued by the company.