Psychiatr. pro Praxi, 2010; 11(4): 170-172

Pharmacological profile of agomelatin

doc.MUDr.Ján Pečeňák, CSc.
Psychiatrická klinika LF UK a FN Bratislava

Agomelatine is newly registered antidepressant with different mechanism of action in comparison with older drugs. Its structure is similar

to melatonin. Agomelatine has agonistic properties to melatonin MT1 and MT2 receptors and antagonistic effect on 5-HT2C receptors.

It modulates circadian rhythms and has influence on turnover of dopamine a noradrenalin in prefrontal cortex. Agomelatine is rapidly

absorbed; absorption is independent on food intake. Biological availability is low because of high first-pass effect. Hepatic isoenzyme

CYP 1A2 is the main way of metabolism. Inhibitors of CYP1A2 increase plasmatic level of agomelatine. The starting dose of 25 mg/day

is recommended. In the case of insufficient clinical response, the dosage can be increased to 50 mg/day after two weeks of treatment.

The drug should be used before sleep. Occurrence of increased plasmatic transaminases levels in registration studies is the reason for

performing liver function tests in recommended intervals.

Keywords: agomelatine, pharmacodynamics, pharmacokinetics, adverse effects

Published: December 1, 2010  Show citation

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Pečeňák J. Pharmacological profile of agomelatin. Psychiatr. praxi. 2010;11(4):170-172.
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    References

    1. CHMP ASSESSMENT REPORT FOR Valdoxan. http://www.ema.europa.eu/humandocs/PDFs/EPAR/valdoxan/H-915en6.pdf. Prístup 18. 2. 2010.
    2. Hardeland R. New approaches in the management of insomnia: weighing the advantages of prolonged-release melatonin and synthetic melatoninergic agonists. Neuropsychiatr Dis Treat. 2009; 5: 341-354. Go to original source... Go to PubMed...
    3. Millan MJ, Gobert A, Lejeune F, et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine 2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J Pharmacol Exp Ther. 2003, 306(3): 954-964. Go to original source... Go to PubMed...
    4. Šonka K, Nevšímalová S. Melatonin známe 50 let. Co o něm víme a jak jej můžeme použít. Neurol. pro praxi 2008; 9: 104-108.
    5. Hirsch-Rodriguez E, Imbesi M, Manev R, et al. The pattern of melatonin receptor expression in the brain may influence antidepressant treatment. Med Hypotheses. 2007; 69: 120-124. Go to original source... Go to PubMed...
    6. Popoli M. Agomelatine: innovative pharmacological approach in depression. CNS Drugs 2009; 23(Suppl 2): 27-34. Go to original source... Go to PubMed...
    7. Alex K. 5-HT2C serotonin receptors: cellular localization and control of dopaminergic pathways in the rat brain. Thesis for the degree of doctor of philosophy. Case Western Reserve University. http://www.ohiolink.edu, prístup 22. 4. 2009.
    8. Valdoxan. Súhrn charakteristických vlastností lieku. http://www.ema.europa.eu/humandocs/Humans/EPAR/valdoxan/valdoxan.htm. Prístup 18. 2. 2010.
    9. Zupancic M, Guilleminault C. Agomelatine: a preliminary review of a new antidepressant. CNS Drugs 2006; 20(12): 981-992. Go to original source... Go to PubMed...
    10. Lôo H, Hale A, D'haenen H. Determination of the dose of agomelatine, a melatoninergic agonist and selective 5-HT (2C) antagonist, in the treatment of major depressive disorder: a placebo-controlled dose range study. Int Clin Psychopharmacol 2002; 17(5): 239-247. Go to original source... Go to PubMed...
    11. Kennedy SH, Rizvi S, Fulton K, Rasmussen J. A doubleblind comparison of sexual functioning, antidepressant efficacy, and tolerability between agomelatine and venlafaxine XR. J Clin Psychopharmacol 2008; 28(3): 329-333. Go to original source... Go to PubMed...
    12. Montgomery SA, Kennedy SH, Burrows GD, et al. Absence of discontinuation symptoms with agomelatine and occurrence of discontinuation symptoms with paroxetine: a randomized, double-blind, placebo-controlled discontinuation study. Int Clin Psychopharmacol 2004; 19(5): 271-280. Go to original source... Go to PubMed...
    13. Švestka J. Agomelatin - nové melatonergní a serotoninergní antidepresivum. Psychiatrie 2005; 9(4): 303-310.

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