Glucocorticoids triamcinolone acetonide

Chemical structures of several glucocorticoids. The acetonide-substituted derivatives (eg, triamcinolone acetonide) have increased surface activity and are useful in dermatology. Dexamethasone is identical to betamethasone except for the configuration of the methyl group at C16 in betamethasone it is beta (projecting up from the plane of the rings) in dexamethasone it is alpha. 

Glucocorticoids given intrathecally can cause a rise in cerebrospinal fluid protein and carry the risk of arachnoiditis (SED-8, 820). Chemical meningitis has been reported after two intrathecal injections of methylpredni-solone acetate (450) and after lumbar facet joint block (SEDA-17, 450). Intraspinal injections of hydrocortisone for multiple sclerosis apparently led in one case to a cauda equina syndrome, with subsequent ulceromutilating acro-pathy (SEDA-17, 450). Intra-discal injections of triamcinolone acetonide in a number of French cases led to disk or epidural calcification, sometimes symptomless (SEDA-17, 450). 

Figure 2 Lung and liver glucocorticoid receptor occupancy after administration of 100 (Xg/kg triamcinolone acetonide (TA) intravenous administration (A) and intratracheal (B) administration of a triamcinolone acetonide solution, micronized TA powder (C) and Kenalog TA crystal suspension (D). Data taken from Ref. (133) and (134).

Figure 3 Lung and liver glucocorticoid receptor occupancy after intratracheal administration of 100 Xg/kg triamcinolone acetonide phosphate solution (TAP, A), liposomal preparation of triamcinolone acetonide (B) and intratracheal administration of 200 nm TAP liposomes (C, intermediate release liposomes) and 800 nm TAP liposomes (D, slow release liposomes). Data taken from Ref. 69.

The therapeutic effectiveness of topically applied corticosteroids is attributed primarily to their antiinflammatory activity. The relative efficacy of topical corticosteroids appears to be in the following order hydrocortisone, prednisolone, betamethasone < hydrocortisone valerate or butyrate, betamethasone valerate, triamcinolone acetonide, flucinolone acetonide < betamethasone dipropionate, fluocino-nide. In addition to the nature of the corticosteroid, its solubility, and, to a lesser extent, the concentration used, clinical efficacy is influenced by the formulation of the preparation. Glucocorticoids appear to have greater efficacy when formulated in ointment bases than in cream or lotion vehicles. This could be attributed to the occlusive effect provided by ointments. The application of an occlusive dressing further enhances penetration and persistence of the steroid (reservoir effect) in the stratum corneum. " ... 

Intralesional preparations of glucocorticoids include insoluble preparations of triamcinolone acetonide (kenalog-10, others) and triamcinolone hexacetonide (kenolog-40 and aristospan), which solubihze gradually and therefore have a prolonged duration of action. 

Agonists Glucocorticoids Cortisol (hydrocortisone), prednisone Dexamethasone, triamcinolone, beclomethasone Triamcinolone acetonide... 

Triamcinolone to be used topically is generally dispensed as its more potent and lipophilic acetonide, a 16a,17a-methylenedioxy cyclic ketal or isopropylidene derivative (Fig. 33.14) (see Inhaled and Intranasal Glucocorticoids). It is effective in the treatment of psoriasis and other corticoid-sensitive dermatologic conditions. Topically, triamcinolone acetonide is a more potent derivative of triamcinolone and is approximately eight times more active than prednisolone. The side effects of the drug, however, have occurred with sufficient frequency ... 

Topical glucocorticoids can aid in alleviating dermatitis (see Table 20-2). These include dexamethasone (Decadron) cream, hydrocortisone ointment or cream, methylprednisolone acetate (Medrol) ointment, triamcinolone acetonide (Aristocort), and flurandrenolide (Cordran). 

Classes of compounds such as beta-blockers, p2-agonists, and glucocorticoids are typically detected in urine as the unchanged parent compound. However, it is important to be aware that the same compound can be present in different formulations that have different chromatographic retention times and produce different diagnostic ions that must be separately detected by LC-MS/MS (Table 3). For example, the synthetic glucocorticoid triamcinolone is also available as the acetonide and hexacetonide derivatives (Fig. lb). 

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