Agomelatine for ADHD

The trade name of agomelatine is Valdoxan.

Effect:

• Agonistic on melatonin MT1 receptor
• Agonistic on melatonin MT2 receptor
• Blockade of the serotonin 5HT-2-B receptor in the suprachiasmatic nucleus¹
• Blockade of the serotonin 5HT-2-C receptor in the suprachiasmatic nucleus¹
• Is designed to increase the expression of the cytoskeleton-associated protein (ARC) in the PFC²
  • Should lead to an optimization of learning, consolidation of long-term memory and improved survival of neurons
• Modulation of glutamatergic neurotransmission in regions associated with mood and cognition²

Agomelatine moderates the synchronization of circadian rhythms.³⁴² It is therefore particularly worth considering if the sleep rhythm is shifted backwards (which is common in ADHD sufferers).

70 to 80 % of all children with ADHD have sleep disorders.
In adults with ADHD, the figure is probably between 20 and 30%.

Sleep is an eminently effective therapeutic agent for ADHD, as for all other disorders of the stress regulation system. One hour more sleep at night reduces the cortisol level in the morning by 21%.

It is possible that agomelatonin not only has a sleep-promoting and antidepressant effect, but also has an independent effect on ADHD: the effectiveness of agomelatonin was compared with that of methylphenidate in a randomized double-blind study with n = 54 children. Both medications performed comparably in the parents’ and teachers’ assessment of the children. Naturally, the children treated with agomelatine had fewer sleep disorders.⁵ Agomelatine has hardly been researched as an ADHD medication.

• Agomelatine causes a 5HT2C receptor blockade, which indirectly causes an increase in noradrenaline and dopamine in the frontal cortex.¹
• However, agomelatine does not increase the dopamine level in the nucleus accumbens and in the striatum,¹ where the dopamine deficit in ADHD causes the problems with drive and motivation as well as with attention regulated by motivation.
• The noradrenaline level in the frontal cortex is increased in a dose-dependent manner, with adrenergic activity in the nucleus coeruleus increasing at the same time.¹

MPH and amphetamine drugs, on the other hand, have a dopamine-increasing effect on the PFC and striatum.

Agomelatine is metabolized by:⁶

• Cytochrome P450 1A2 (CYP1A2) (90 %)
• CYP2C9/2C19 (10%)

For agomelatine as a sleep aid, see also ⇒ sleeping pills / sleep medication suitable for ADHD In the article ⇒ Sleep problems with ADHD.