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.
- 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.
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.
- Tardive dyskinesias
- 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 ↥