Authors: Cardinali, Daniel P; Pandi-Perumal, Seithikurippu R; Srinivasan, Venkataramanujan; Spence, D Warren; Trakht, Ilya

Source: Expert Review of Endocrinology and Metabolism, Volume 3, Number 2, March 2008 , pp. 269-279(11)

Publisher: Expert Reviews

Abstract:

Melatonin, a hormone secreted by the pineal gland, has been successfully employed to improve sleep in both normal patients and insomniacs, and for the treatment of circadian rhythm sleep disorders. Melatonergic MT₁ and MT₂ receptors exist in high concentrations in the suprachiasmatic nucleus of the hypothalamus and have been shown to be instrumental for the sleep-promoting and circadian rhythm-regulating effects of melatonin. A lack of consistency among reports on the therapeutic efficacy of melatonin has been attributed to differences in melatonins bioavailability and the short half-life of the hormone. In view of the need for longer acting melatonergic agonists that improve sleep efficiency without causing drug abuse or dependency, ramelteon (Rozerem, Takeda) was developed. Ramelteon, which acts via MT₁/MT₂ melatonergic agonism, has been found clinically effective for improving total sleep time and sleep efficiency in insomniacs. Agomelatine (Valdoxan, Servier) is another MT₁/MT₂ melatonergic agonist that also displays antagonist activity at 5-HT_2C serotonin receptors. Agomelatine has been found effective in treating depression and sleep disorders in patients with major depressive disorder. A slow-release preparation of melatonin (Circadin, Neurim) has been shown to be effective in treating sleep disorders in the elderly population.

Keywords: agomelatine; antidepressant; Circadin; insomnia; major depressive disorder; melatonin; melatonin receptors; ramelteon

Document Type: Research article

DOI: http://dx.doi.org/10.1586/17446651.3.2.269

Affiliations: 1: Departamento de Fisiologa, Facultad de Medicina, UBA Paraguay 2155, 1121 Buenos Aires, Argentina., Email: dcardinali@fmed.uba.ar

Publication date: 2008-03-01

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