Trimipramine for ADHD
Trimipramine causes a blockade of various serotonin, dopamine and α-adrenoceptors.
Trimipramine is an old tricyclic antidepressant
- Low monoamine reuptake inhibition from the synaptic cleft.
- Anticholinergic
- Antihistaminergic
- A potent 5-HT2 receptor antagonist1
- D2 receptor antagonist1 of the presynaptic D2 autoreceptor2
- Acts as FIASMA (functional inhibitor of acid sphingomyelinase)
- Increases the nocturnal release of prolactin3
- Attenuates the nocturnal release of cortisol3
- Significantly anxiolytic (anxiolytic) effect
Trimipramine was quite unsuccessful as an antidepressant.
Trimipramine is, however, valued by many doctors as an effective sleep aid without dependency potential. Trimipramine has a strong sleep-promoting effect on healthy people, 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 patients with sleep disorders4
- Empirically, a subjective improvement in sleep continuity has also been observed in the chronic treatment of depression.1
In contrast to almost all other tricyclic antidepressants, trimipramine does not impair REM sleep.41
Due to its anxiolytic effect, it calms and relaxes, and reduces mental spinning.
A sensible dosage as a sleeping pill (10 to 25 mg (10 to 25 drops) approx. 1/2 to 1 hour before going to bed) is significantly lower than the dosage as an antidepressant (up to 50 mg).
As the patent period for trimipramine has expired, it is not worthwhile conducting drug trials for the official approval of trimipramine as a sleeping pill, which would be very expensive. Its use as a sleeping pill will therefore remain permanently off-label.
Thesis:
We are considering whether the anxiolytic effect, which calms the amygdala, could be used as a stress-relieving medication. Individual sufferers have reported a positive and stress-relieving effect from an initial dosage of 1 to 2 mg during the day.
Side effects:
- Tardive dyskinesia
- Consequence of the D2 receptor blocking effect
Selsick (2018): Sleep Disorders in Psychiatric Patients A Practical Guide, S. 89 ↥ ↥ ↥ ↥
Sarholz, Assion (2005): Psychopharmaka in der Schmerztherapie. Arzneimitteltherapie 2005;23:213–7 ↥
Berger, Gastpar (1996): Trimipramine: a challenge to current concepts on antidepressives. Eur Arch Psychiatry Clin Neurosci. 1996;246(5):235-9. ↥ ↥
Riemann, Voderholzer, Cohrs, Rodenbeck, Hajak, Rüther, Wiegand, Laakmann, Baghai, Fischer, Hoffmann, Hohagen, Mayer, Berger (2002): Trimipramine in primary insomnia: results of a polysomnographic double-blind controlled study. Pharmacopsychiatry. 2002 Sep;35(5):165-74. doi: 10.1055/s-2002-34119. PMID: 12237787. n = 55 ↥ ↥ ↥ ↥
Wolf, Dykierek, Gattaz, Maras, Kohnen, Dittmann, Geuppert, Riemann, Berger (2001): Differential effects of trimipramine and fluoxetine on sleep in geriatric depression. Pharmacopsychiatry. 2001 Mar;34(2):60-5. doi: 10.1055/s-2001-15183. PMID: 11302565. n = 19 ↥