Trimipramine for ADHD

Trimipramine causes blockade of various serotonin, dopamine, and α-adrenoceptors.
Trimipramine is a long-standing tricyclic antidepressant

• Low monoamine reuptake inhibition from the synaptic cleft.
• Anticholinerg
• Antihistaminerg
• A potent 5-HT2 receptor antagonist¹
• D2 receptor antagonist¹ of the presynaptic D2 autoreceptor²
• Acts as a FIASMA (functional inhibitor of acid sphingomyelinase)
• Enhances nocturnal prolactin secretion³
• Attenuates nocturnal cortisol secretion³
• Significantly anxiety-relieving (anxiolytic) effect

As an antidepressant, trimipramine was quite unsuccessful.

However, trimipramine is valued by many physicians as an effective sleep aid with no dependence potential. Trimipramine has a strong sleep-promoting effect in healthy individuals, depressives and subjects with sleep disorders:

• Reduced sleep onset latency⁴
• Higher sleep efficiency (at 100 mg)⁴
• Longer sleep times in depressed geriatric patients⁵, but not in those affected by sleep disorders⁴
• Empirically, subjective improvement in sleep continuity is also observed in chronic treatment of depression.¹

Unlike almost all other tricyclic antidepressants, trimipramine does not impair REM sleep.⁴¹

Due to its anxiolytic effect, it calms and relaxes, and reduces the mind’s wandering.

A reasonable dosage as a sleep aid (10 to 25 mg (10 to 25 drops) about 1/2 to 1 hour before going to bed) is much lower than the dosage as an antidepressant (there up to 50 mg).

Since the patent period of trimipramine has expired, drug trials for the official approval of trimipramine as a sleep aid are not worthwhile and would be very expensive. Its use as a sleep aid will therefore remain permanently off-label.

Thesis:
We are considering whether the anxiolytic effect, which calms the amygdala, could not be used as a stress-relieving medication. Individuals reported a positive and stress-relieving effect of an initial dosage of 1 to 2 mg during the day.

Side effects:

• Tardive dyskinesias
  • Consequence of the D2 receptor blocking effect