Chemical formula: C₂₁H₂₇FO₆ Molecular mass: 394.434 g/mol PubChem compound: 31307
Triamcinolone acetonide is a more potent derivative of triamcinolone and is approximately 8 times more potent than prednisone. Although the precise mechanism of corticosteroid anti-allergic action is unknown, corticosteroids are very effective in the treatment of allergic diseases in man. Also, local injections are thought to have an anti-inflammatory effect.
Triamcinolone nasal spray does not have an immediate effect on allergic signs and symptoms. An improvement in some patient symptoms may be seen within the first day of treatment and relief may be expected in 3 to 4 days. When triamcinolone nasal spray is prematurely discontinued symptoms may not recur for several days.
In clinical studies performed in adults and children at doses up to 440 mcg/day intranasally, no suppression of the Hypothalamic-Pituitary-Adrenal (HPA) axis has been observed.
The anti-inflammatory potency of triamcinolone on a milligram by milligram comparison is approximately five times that of hydrocortisone. Triaminolone has practically no mineralocorticoid effect, so no sodium retention occurs.
The efficacy and safety of triamcinolone hexacetonide in children and adolescents are based on the well-researched effects of glucocorticoids, which are the same in children and adults. Published studies and current therapeutic guidelines for treatment of Juvenile Idiopathic Arthritis (JIA) indicate efficacy and safety in children and adolescents for the treatment of JIA.
Single dose intranasal administration of 220 micrograms of triamcinolone nasal spray in normal adult subjects and in adult patients with allergic rhinitis demonstrated minimal absorption of triamcinolone. The mean peak plasma concentration was approximately 0.5 ng/mL (range 0.1 to 1 ng/mL) and occurred at 1.5 hours post dose. The mean plasma drug concentration was less than 0.06 ng/mL at 12 hours and below the assay detection limit at 24 hours. The average terminal half life was 3.1 hours. Dose proportionality was demonstrated in normal subjects and in patients following a single intranasal dose of 110 micrograms or 220 micrograms triamcinolone nasal spray. Following multiple doses in paediatric patients, plasma drug concentrations, AUC, Cmax and Tmax were similar to those values observed in adult patients.
The hexacetonide ester is almost insoluble in water, so dissolution is slow and the effect in the tissue of the injection site lasts for a long time, from a few weeks to several months. Generally, the onset of effect after triamcinolone hexacetonide administration occurs after 24 hours and normally lasts for 4 to 6 weeks.
Triamcinolone is hydrolysed by human serum in vitro (43% hydrolysed after 24 hours), but following intra-articular injection, the substance does not disperse in situ.
In pre-clinical studies, only the effects typical of glucocorticosteroids were observed
Like other corticosteroids, triamcinolone has been shown to be teratogenic in rats and rabbits. Teratogenic effects which occurred in the rat and in the rabbit included cleft palate and/or internal hydrocephaly and axial skeletal defects. Teratogenic effects, including CNS and cranial malformations, have also been observed in non-human primates.
No evidence of mutagenicity was detected in in vitro gene mutation tests.
Carcinogenicity assays in rodents show no increase in the incidence of individual tumour types.
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