PROTHIADEN Capsule, hard Ref.[11083] Active ingredients: Dosulepin

Source: Health Products Regulatory Authority (IE)  Revision Year: 2020  Publisher: Teofarma S.R.L., Valle Salimbene (PV), Via F. LLI Cervi, 8 CAP 27010, Italy

5.1. Pharmacodynamic properties

Dosulepin is a tricyclic antidepressant which acts by inhibiting the re-uptake of monoamine neurotransmitters into presynaptic neurone at central nervous system, so producing a clinical antidepressant effect.

Dosulepin, in common with other tricyclics, inhibits the reuptake of noradrenaline and 5-hydroxytryptamine, with a significantly greater action on the uptake of noradrenaline. In addition, dosulepin inhibits the neuronal uptake of dopamine.

As a consequence of its effects on monoamine levels, dosulepin appears to produce adaptive changes in the brain

Similarly to other tricyclic antidepressants, it has anticholinergic, antihistaminic and anti-α1 adrenergic effects.

5.2. Pharmacokinetic properties

Dosulepin is readily absorbed from the gastrointestinal tract and extensively metabolised in the liver. Metabolites include northiaden, dosulepin-S-oxide and northiaden-S-oxide. Dosulepin is excreted in the urine, mainly in the form of metabolites; appreciable amounts are also excreted in the faeces. A half-life of about 50 hours has been reported for dosulepin and its metabolites.

5.3. Preclinical safety data

Not applicable.

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