Agomelatine: Its Role in the Management of Major Depressive Disorder

Cardinali, Daniel P.; Vidal, María Florencia; Vigo, Daniel Eduardo

doi:10.4137/cmpsy.s7989

Cited by 12 publications

(7 citation statements)

References 195 publications

(216 reference statements)

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“…Melatonin's sleep-facilitating properties have been found to be useful for treating insomnia symptoms in elderly and depressive patients. A recently introduced melatonin analog, agomelatine, is also effective for the treatment of major depressive disorder and bipolar affective disorder (Cardinali et al, 2012b).…”

Section: The Sleep-wake Cycle a Window Of The Circadian Timing Systemmentioning

confidence: 99%

Some implications of melatonin use in chronopharmacology of insomnia

Golombék

Pandi-Perumal²,

Brown

et al. 2015

European Journal of Pharmacology

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The last decade has witnessed the emergence of new chronopharmacological perspectives. In the case of sleep disorders, the accumulating evidence suggests that even a minor dysfunction in the biological clock can impact broadly upon body physiology causing increases in sleep onset latency, phase delays or advances in sleep initiation, frequent nocturnal awakenings, reduced sleep efficiency, delayed and shortened rapid eye movement sleep and increased periodic leg movements, among others. Thus, restoration of the adequate circadian pattern of proper sleep hygiene, targeted exposure to light and the use of chronobiotic drugs, such as melatonin, which affect the output phase of clock-controlled circadian rhythms, can help to recover the sleep-wake cycle. The optimization of drug effects and/or minimization of toxicity by timing medications with regard to biological rhythms is known as chronotherapeutics. While chronotherapeutical approaches have been particularly successful in the treatment of hypertension, allergies and some forms of cancer, a time-dependent pharmacological approach can be also effective when dealing with sleep disruptions like insomnia. A large proportion of patients under benzodiazepine (BZD)/Z drug treatment fail to achieve a complete and sustained recovery and are left with residual symptoms, like tolerance or dependency, that make relapse or recurrence more likely, and poorer quality of life a reality. Thus the chronic and extensive use of BZD/Z drugs has become a public health issue and has led to multiple campaigns to reduce both prescription and consumption of BZD/Z-drugs. This short review discusses available data on the efficacy of melatonin to reduce chronic BZD use in insomnia patients.

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Section: The Sleep-wake Cycle a Window Of The Circadian Timing Systemmentioning

confidence: 99%

Some implications of melatonin use in chronopharmacology of insomnia

Golombék

Pandi-Perumal²,

Brown

et al. 2015

European Journal of Pharmacology

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“…It displays an overall selectivity (>100-folds) for MT 1 and MT 2 receptors as compared to other receptor sites.…”

Section: Introductionmentioning

confidence: 99%

“…As AGO addresses sleep disturbances as well as depressive symptoms and has early onset of action, even in severely depressed patients, it stands alone among the antidepressants for effective management of major depressive disorders (MDD) [1].…”

Section: Introductionmentioning

confidence: 99%

“…And this may exhibit clinically as improvements in mood, anxiety and sleep-wake cycles with MDD, indicate that AGO is a potentially useful treatment for major depressive episodes in adults [1,3]. The literature survey reveals several methods for determination of AGO in plasma by High Performance Liquid Chromatographic (HPLC) method with fluorescence detection [4,5], UV detection [6][7][8] and mass spectrometry [9,10].…”

Section: Introductionmentioning

confidence: 99%

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Stability-Indicating Chromatographic Methods for Determination of Agomelatine in Drug Substance and Drug Product

Rizk¹,

Taha²,

El‐Alamin³

et al. 2017

Pharm Anal Acta

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Three sensitive and validated chromatographic methods were developed for determination of Agomelatine (AGO) in the presence of its degradation products in drug substance and drug product. The first and second methods were normal thin layer chromatographic (NP-TLC) and reversed phase thin layer chromatographic (RP-TLC) methods. Mobile phase consisting of ethyl acetate-ammonia (33%)-methanol (8.5:0.5:1, v/v/v) was used for NP-TLC while for RP-TLC using 0.1% triethylamine (TEA): acetonitrile (60:40 v/v) at pH=2. The chromatograms were scanned at 230 and 280 nm and determined in the range of 0.1-4 and 0.3-4 μg/spot with mean percentage recovery of 99.89 ± 1.141 and 100.01 ± 1.062 for NP-TLC and RP-TLC respectively.The third method was Micellar Liquid Chromatographic (MLC) method using C 18 column and a mobile phase consisting of 0.1 M Sodium Dodecyl Sulphate (SDS), 15% butan-1-ol, 0.2% TEA in water adjusted to pH=3. The UV detection was achieved at 230 nm and determined in the range of 0.5-5 µg/mL with mean percentage recovery of 100.13 ± 0.970. The proposed methods were successfully applied as stability indicating methods under different stressed conditions according to the International Conference of Harmonization (ICH) guidelines. The methods showed good selectivity, repeatability, linearity and sensitivity according to the evaluation of the validation parameters.

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“…Several studies 14 15 16 17 showed that hippocampal volume decreased in patients with stress-related major depression, which might be due to glial and neuronal atrophy or loss related in part to increases in corticosteroids and excitatory amino acids; such relationships have been demonstrated in animal models 18 19 20 , while still under investigation in humans 21 22 . Meanwhile, Agomelatine, a recently marketed antidepressant drug, was reported to induce neurogenesis and cell proliferation in the ventral part of dentate gyrus, resulting to the rapid and early increase in maturation at a critical period of neuronal development, which likely influences the functional integration of new born cells into hippocampal circuitry.…”

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confidence: 99%

Scaffold Hopping Toward Agomelatine: Novel 3, 4-Dihydroisoquinoline Compounds as Potential Antidepressant Agents

Yang

Ang

Long

et al. 2016

Sci Rep

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A scaffold-hopping strategy toward Agomelatine based on in silico screening and knowledge analysis was employed to design novel antidepressant agents. A series of 3, 4-dihydroisoquinoline compounds were selected for chemical synthesis and biological assessment. Three compounds (6a-1, 6a-2, 6a-9) demonstrated protective effects on corticosterone-induced lesion of PC12 cells. Compound 6a-1 also displayed low inhibitory effects on the growth of HEK293 and L02 normal cells and it was further evaluated for its potential antidepressant effects in vivo. The forced swim test (FST) results revealed that compound 6a-1 remarkably reduced the immobility time of rats and the open field test (OFT) results indicated a better general locomotor activity of the rats treated with compound 6a-1 than those with Agomelatine or Fluoxetine. Mechanism studies implied that compound 6a-1 can significantly reduce PC12 cell apoptosis by up-regulation of GSH and down-regulation of ROS in corticosterone-induced lesion of PC12 cells. Meanwhile, the down-regulation of calcium ion concentration and up-regulation of BDNF level in PC12 cells may account for the neuroprotective effects. Furthermore, compound 6a-1 can increase cell survival and cell proliferation, promote cell maturation in the rat hippocampus after chronic treatment. The acute toxicity data in vivo indicated compound 6a-1 exhibited less hepatotoxicity than Agomelatine.

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Agomelatine: Its Role in the Management of Major Depressive Disorder

Cited by 12 publications

References 195 publications

Some implications of melatonin use in chronopharmacology of insomnia

Some implications of melatonin use in chronopharmacology of insomnia

Stability-Indicating Chromatographic Methods for Determination of Agomelatine in Drug Substance and Drug Product

Scaffold Hopping Toward Agomelatine: Novel 3, 4-Dihydroisoquinoline Compounds as Potential Antidepressant Agents

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