Glucocorticosteroids (GC) continue to be among the most frequently prescribed anti-inflammatory agents in dermatology and all of medicine, with a large number of disorders responding to these drugs. Clinical pharmacology and therapeutic use of GC in d...
Glucocorticosteroids (GC) continue to be among the most frequently prescribed anti-inflammatory agents in dermatology and all of medicine, with a large number of disorders responding to these drugs. Clinical pharmacology and therapeutic use of GC in dermatology are reviewed in this presentation. The major naturally occurring GC is cortisol (hydrocortisone). Under basal conditions, the adrenals produce approximately 20 mg of cortisol (equivalent to 5 mg of prednisone), with a diurnal peak around 8AM. All steroids, including GC, have the basic four-ring structure of cholesterol, with three hexane rings and one pentane ring. Modifications of cortisol result in compounds that have different potencies, mineralocorticoid effects, durations of action, metabolism and adverse effects. Systemic GC can be administered intralesionally, orally, intramuscularly, and intravenously. Intralesional GC administration allows direct access to either a relatively few lesions or a particularly resistant lesion. Triamcinolone acetonide is diluted to the desired concentration (2~40mg) and injected in small amounts into the lesion(s). Dermatologists occasionally use intramuscular (IM) administration of GC for control of acute dermatoses. There are several drawbacks to IM injection because of erratic absorption and lack of daily control of the dose. IM agents, such as betamethasone and dexamethasone, which have a duration of action of less than 1 week, may be preferred in self-limited dermatoses. Longer-acting IM agents that produce effects for about 3 weeks, such as triamcinolone acetonide and methylprednisolone acetate, should not be given more than about 4-6 times per year. When oral GCs are prescribed, prednisone and prednisolone are most commonly selected and usually administered daily or every other day; although for acute disease, split daily doses can be used. If less than 3-4 weeks, GC therapy can be stopped without tapering. Intravenous (IV) doses of GCs may be necessary in severe or life-threatening dermatologic conditions. A total daily dose of 2 mg/kg or more of methylprednisolone is given initially in divided doses every 6-8 hours. Another method of dosing is IV pulse therapy; methylprednisolone is given IV in doses of 0.5-1 g over 2 hours daily for 1-5 days. Topical GC regimens are available in a wide range of potencies and a variety of vehicles. Topical GCs can be categorized into seven classes based on potency ranging from the superpotent agents in class 1 to the very low potency agents in class 7, based on vasoconstrictor assays. The vehicle cangreatly influence the percutaneous absorption and therapeutic efficacy of GCs. In an attempt to develop GC compounds with optimal potency and minimal side effects, GC molecules that retain high activity in the skin and are quickly broken down into inactive metabolites have developed. Some of those compounds include budesonide, mometasone furoate, prednicarbate, methylprednisolone aceponate, alclometasone dipropionate, and fluticasone propionate.