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Trazodone
- indication:For the treatment of depression.
- pharmacologypharmacology:
- mechanism: Trazodone binds at 5-HT2 receptor, it acts as a serotonin agonist at high doses and a serotonin antagonist at low doses. Like fluoxetine, trazodone's antidepressant activity likely results from blockage of serotonin reuptake by inhibiting serotonin reuptake pump at the presynaptic neuronal membrane. If used for long time periods, postsynaptic neuronal receptor binding sites may also be affected. The sedative effect of trazodone is likely the result of alpha-adrenergic blocking action and modest histamine blockade at H1 receptor. It weakly blocks presynaptic alpha2-adrenergic receptors and strongly inhibits postsynaptic alpha1 receptors. Trazodone does not affect the reuptake of norepinephrine or dopamine within the CNS.
- toxicity: LD<sub>50</sub>=96mg/kg (i.v. in mice)
- absorprion: Rapidly and almost completely absorbed following oral administration. Food may decrease the rate and extent of absorption.
- halflife: Undergoes biphasic elimination with an initial phase t<sub>1/2 &alpha;</sub> of 3-6 hours and a terminal phase t<sub>1/2 &beta;</sub> of 5-9 hours.
- roouteelimination:
- volumedistribution:
- clearance: