Corticosteroid structure activity relationship

Oral and injectable systemic corticosterois are steroid hormones prescribed to decrease inflammation in diseases and conditions such as arthritis (rheumatoid arthritis, for example), ulcerative colitis, Crohn's disease, asthma, bronchitis, some skin rashes, and allergic or inflammatory conditions that involve the nose and eyes. Examples of systemic corticosteroids include hydrocortisone (Cortef), cortisone, prednisone (Prednisone Intensol), prednisolone (Orapred, Prelone), and methylprednisolone (Medrol, Depo-Medrol, Solu-Medrol). Some of the side effects of systemic corticosteroids are swelling of the legs, hypertension, headache, easy bruising, facial hair growth, diabetes, cataracts, and puffiness of the face.

Geriatric Use : Clinical studies of prednisolone sodium phosphate , USP, oral solution did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience with prednisolone sodium phosphate has not identified differences in responses between the elderly and younger patients. However, the incidence of corticosteroid-induced side effects may be increased in geriatric patients and appear to be dose-related. Osteoporosis is the most frequently encountered complication , which occurs at a higher incidence rate in corticosteroid-treated geriatric patients as compared to younger populations and in age-matched controls. Losses of bone mineral density appear to be greatest early on in the course of treatment and may recover over time after steroid withdrawal or use of lower doses (., ≤5 mg/day). Prednisolone doses of mg/day or higher have been associated with an increased relative risk of both vertebral and nonvertebral fractures, even in the presence of higher bone density compared to patients with involutional osteoporosis.

Corticosteroids have been used as drug treatment for some time. Lewis Sarett of Merck & Co. was the first to synthesize cortisone, using a complicated 36-step process that started with deoxycholic acid, which was extracted from ox bile . [43] The low efficiency of converting deoxycholic acid into cortisone led to a cost of US $200 per gram. Russell Marker , at Syntex , discovered a much cheaper and more convenient starting material, diosgenin from wild Mexican yams . His conversion of diosgenin into progesterone by a four-step process now known as Marker degradation was an important step in mass production of all steroidal hormones, including cortisone and chemicals used in hormonal contraception . [44] In 1952, . Peterson and . Murray of Upjohn developed a process that used Rhizopus mold to oxidize progesterone into a compound that was readily converted to cortisone. [45] The ability to cheaply synthesize large quantities of cortisone from the diosgenin in yams resulted in a rapid drop in price to US $6 per gram, falling to $ per gram by 1980. Percy Julian's research also aided progress in the field. [46] The exact nature of cortisone's anti-inflammatory action remained a mystery for years after, however, until the leukocyte adhesion cascade and the role of phospholipase A2 in the production of prostaglandins and leukotrienes was fully understood in the early 1980s.

Allergic sensitivity to a topical corticosteroid is usually only picked up when an eczematous dermatitis being treated by a topical corticosteroid fails to respond to treatment or worsens. In cases of persistent or exacerbating dermatitis treated with corticosteroid preparations, corticosteroid sensitivity should be considered. However, it may also be due to irritation from or allergy to other components of the preparation such as preservatives . Lanolin , ethylenediamine , quaternium-15 and the antibacterial agent neomycin , are all known to be potent sensitisers.

Corticosteroid structure activity relationship

corticosteroid structure activity relationship

Allergic sensitivity to a topical corticosteroid is usually only picked up when an eczematous dermatitis being treated by a topical corticosteroid fails to respond to treatment or worsens. In cases of persistent or exacerbating dermatitis treated with corticosteroid preparations, corticosteroid sensitivity should be considered. However, it may also be due to irritation from or allergy to other components of the preparation such as preservatives . Lanolin , ethylenediamine , quaternium-15 and the antibacterial agent neomycin , are all known to be potent sensitisers.

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