Source: Health Sciences Authority (SG) Revision Year: 2024 Publisher: Indrugco Pte Ltd 221 Henderson Rd #07-20, Singapore 159557
Pharmacotherapeutic group: psycho-analeptics, antidepressants
ATC code: N06AX05. Other antidepressants.
Trazodone is a triazolopyridine derivative which is effective in the treatment of all types of depression, including depression associated with anxiety and sleep disorders (ATC code: N06AX05), and is characterised by a short onset of action (approximately one week).
Trazodone is a serotonin re-uptake inhibitor and an antagonist of 5-HT2 receptors, the activation of which is commonly associated with insomnia, anxiety, psychomotor agitation and sexual function disorders.
Unlike other psychotropic drugs, trazodone is not contraindicated in glaucoma or micturition disorders and it does not have extrapyramidal effects. Additionally, since it does not potentiate adrenergic transmission and is virtually devoid of anticholinergic activity, it does not have the typical effects of tricyclic antidepressants on heart conduction.
Trazodone hydrochloride is a potent antidepressant. It also has anxiety reducing activity. Trazodone hydrochloride is a triazolopyridine derivative chemically unrelated to known tricyclic, tetracyclic and other antidepressant agents. It has negligible effect on noradrenaline re-uptake mechanisms. Whilst the mode of action of Trazodone hydrochloride is not known precisely, its antidepressant activity may concern noradrenergic potentiation by mechanisms other than uptake blockade. A central antiserotonin effect may account for the drug's anxiety reducing properties.
Trazodone is rapidly absorbed from the gastro-intestinal tract and extensively metabolised. Paths of metabolism of Trazodone include n-oxidation and hydroxylation. The metabolic m-chlorophenylpiperazine is active. Trazodone is excreted in the urine almost entirely in the form of its metabolites, either in free or in conjugated form. The elimination of Trazodone is biphasic, with a terminal elimination half-life of 5 to 13 hours. Trazodone is excreted in breast milk. There was an approximate two-fold increase in terminal phase half-life and significantly higher plasma concentrations of Trazodone in 10 subjects aged 65 to 74 years compared with 12 subjects aged 23 to 30 years following a 100 mg dose of Trazodone. It was suggested that there is an age-related reduction in the hepatic metabolism of Trazodone. In vitro studies in human liver microsomes show that trazodone is metabolised by cytochrome P4503A4 (CYP3A4) to form m-chlorophenylpiperazine. Whilst significant, the role of this pathway in the total clearance of trazodone in vivo has not been fully determined.
There are no pre-clinical safety data of relevance to the prescriber which are additional to that already included in other sections of the product information.
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