Trispan Mechanism of Action





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Pharmacotherapeutic group: corticosteroids, glucocorticoids. ATC code: H02A B08.
Pharmacology: Pharmacodynamics: Mechanism of action: Triamcinolone hexacetonide is used on account of its anti-inflammatory properties for the treatment of rheumatic diseases. The action of glucocorticoids is mediated via binding to a specific glucocorticoid receptor, thereby affecting the transcription of various genes.
Pharmacodynamic effects: The active principle of triamcinolone hexacetonide is triamcinolone acetonide. This is not a prodrug of the free triamcinolone alcohol, but rather a substance in its own right, with a significantly greater affinity for its receptor.
Binding affinities of commercially available glucocorticoids to their receptor - relative receptor affinity (Rohdewald et al., 1984). (See table.)

Click on icon to see table/diagram/image

Triamcinolone hexacetonide has a minor systemic glucocorticoid effect, measured as suppression of endogenous cortisol secretion. It possesses only a very slight mineralocorticoid effect.
Clinical efficacy and safety: Study results in the therapeutic indications stated show the benefit of triamcinolone hexacetonide. The pharmacological profile corresponds with the known effects of glucocorticoids. The safety profile is consistent with that of other representatives of the substance group, without any signs of new safety concerns. Thus, Trispan is a medicinal product with good clinical efficacy and acceptable safety.
Paediatric population: 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 alike. Published studies demonstrate efficacy and safety in children and adolescents for the treatment of juvenile idiopathic arthritis (JIA).
Pharmacokinetics: Triamcinolone hexacetonide is available as a microcrystalline suspension. The low water solubility of the molecule is due to the tertiary butyl acetate residue at C21. Following release from the crystalline depot, hydrolytic cleavage to triamcinolone acetonide occurs via esterases (tissue enzymes). The plasma levels thus reached are lower and the half­-life longer than with injection of a triamcinolone acetonide preparation.
Paediatric population: The pharmacokinetic properties of triamcinolone hexacetonide have only been studied in adults.
Toxicology: Preclinical safety data: Acute toxicity: Acute toxicity studies on various animal species have revealed no particular sensitivity (see Overdosage).
Chronic toxicity: Chronic toxicity studies have been performed on rats, dogs and monkeys. Depending on the dose, duration of treatment and method of administration, blood count changes, interference with the electrolyte balance, infections and hepatic changes have been recorded in addition to several fatalities.
The observed reduction of the adrenal cortex and lymphatic tissue is directly associated with the glucocorticoid effect. In rats and dogs, an effect on coagulation factors was observed in addition to the previously-mentioned phenomena, as well as a reduction in glycogen levels of the liver, cardiac and skeletal muscle.
Mutagenic and carcinogenic potential: No studies have been conducted to determine mutagenic potential. No long-term animal studies have been conducted to determine carcinogenic potential.
Toxicity to reproduction: The embryotoxic properties of triamcinolone have been studied in three rodent species (rat, mouse, hamster), in rabbits and in three non-human primate species (rhesus, baboon, capuchin). In the rodents and in the rabbit, cleft palates and intrauterine growth impairment occurred, whereby teratogenic effects were induced, e.g. in rats, by doses within the human therapeutic range. In the simian species, disturbances in chondrocranium cartilage formation were observed, leading to skull anomalies (encephalocele) and facial dysmorphia. In addition, malformations of the thymus and intrauterine growth impairment occurred. No experience is available regarding the safety of human use.
Local toxicity (tolerability): In local tolerability studies, dogs were administered a single injection of 100 mg/kg body weight subcutaneously. Minor swelling occurred at the injection site, but this is attributed to the large volume of injection (4.0 ml). Studies on guinea pigs showed that no signs of local reactions are present after a single intradermal injection. In animals receiving intradermal injections twice weekly for 4 weeks, minor histological changes were observed. However, there were no signs of abscess formation and the lesions were classified as non-progressive. In humans, local irritation and signs of intolerability are possible (see Adverse Reactions).
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