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Agomelatine for ADHD

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Agomelatine for ADHD

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The trade name of agomelatine is Valdoxan.

Effect:

  • Agonistic to melatonin MT1 receptor
  • Agonistic to melatonin MT2 receptor
  • Blockade of the serotonin 5HT-2-B receptor in the nucleus suprachiasmaticus1
  • Blockade of the serotonin 5HT-2 C receptor in the nucleus suprachiasmaticus1

Agomelatine moderates a synchronization of circadian rhythms.23 It is therefore particularly worth considering in the case of a retarded sleep rhythm (which is common in ADHD sufferers).

70 to 80% of all children with ADHD have sleep disorders.
For adults with ADHD, it’s probably between 20 and 30%.

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

It is possible that agomelatine not only has a sleep-promoting and antidepressant effect, but also an independent ADHD effect: the efficacy of agomelatonin was compared with that of methylphenidate in a randomized double-blind study with n = 54 children. Both medications performed comparably in parent and teacher ratings of the children. Naturally, children treated with agomelatine had less sleep disturbance.4 Agomelatine, moreover, has been little studied as an ADHD medication.

  • Agomelatine causes 5HT2C receptor blockade, which indirectly causes an increase in norepinephrine and dopamine in the frontal cortex.1
  • However, agomelatine does not increase dopamine levels in the nucleus accumbens and striatum,1 where the dopamine deficit in ADHD causes the problems with drive and motivation and with attention regulated by motivation.
  • Norepinephrine levels in the frontal cortex are increased in a dose-dependent manner, with a concomitant increase in adrenergic activity in the nucleus coeruleus.1

In contrast, MPH and amphetamine drugs have a dopamine-increasing effect on PFC and striatum.

Agomelatine is metabolized by:5

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

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

  1. Millan, Gobert, Lejeune, Dekeyne, Newman-Tancredi, Pasteau, Rivet, Cussac (2003): The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways; J Pharmacol Exp Ther. 2003 Sep;306(3):954-64. ↥ ↥ ↥ ↥ ↥

  2. Redman, Francis (2009): Entrainment of Rat Circadian Rhythms by the Melatonin Agonist S-20098 Requires Intact Suprachiasmatic Nuclei But Not the Pineal ↥

  3. Strat, Gorwood (2008): Agomelatine, an innovative pharmacological response to unmet needs; J Psychopharmacol. 2008 Sep;22(7 Suppl):4-8. doi: 10.1177/0269881108092593 ↥

  4. Salardini, Zeinoddini, Kohi, Mohammadi, Mohammadinejad, Khiabany, Shahriari, Akhondzadeh (2016): Agomelatine as a Treatment for Attention-Deficit/Hyperactivity Disorder in Children and Adolescents: A Double-Blind, Randomized Clinical Trial. J Child Adolesc Psychopharmacol. 2016 Jun 10. ↥

  5. valdoxan-epar-product-information_de ↥

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