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Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Agomelatine a melatonin receptor agonist has additional antagonist action on a serotonin receptor, 5HT2C. It is approved for use in depression and also used in sleep disorder associated with depression as it helps to maintain sleep duration (Levitan et al., 2015).
Drug interactions
Published in Alan Weiss, The Electroconvulsive Therapy Workbook, 2018
Agomelatine is an antidepressant that has its primary action on melatonin. Little is known about the safety of agomelatine and ECT, as there have been no published case reports. Owing to its novel mechanism of action, it is unlikely to have an impact on seizure threshold or recovery.
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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
The effects of renal function on agomelatine pharmacokinetics were investigated in a study of healthy subjects and patients with severe impaired renal function. In the renal impairment patients, exposure to agomelatine increased more than 25% compared to healthy subjects. The available safety data from the clinical trials did not demonstrate any significant tolerability or safety issues with the use of agomelatine compared to placebo among patients with mildly to moderately impaired renal function. Although agomelatine can be used in patients with renal impairment, such patients should be monitored more closely. (Howland RH. Critical appraisal and update on the clinical utility of agomelatine, a melatonergic agonist, for the treatment of major depressive disease in adults. Neuropsychiatr Dis Treat. 2009; 5: 563–76.)
The preclinical discovery and development of agomelatine for the treatment of depression
Published in Expert Opinion on Drug Discovery, 2020
George Konstantakopoulos, Stefanos Dimitrakopoulos, Panayiota G. Michalopoulou
There has been an ongoing debate on the role of agomelatine in the treatment of depression. Its unique mechanism of action offers an alternative to monoaminergic antidepressants, especially for patients that are non-responders or experience side-effects that cannot be tolerated. Moreover, recent meta-analytic studies including large sample sizes suggest that agomelatine is a justified first-line choice for managing depression. However, its long-term efficacy is not yet well established and more studies examining its effect on relapse prevention are needed. Although agomelatine has a favorable safety and tolerance profile, the issue of hepatotoxicity and regular blood monitoring still raises clinician concern. Moreover, further exploration of agomelatine’s potential for the treatment of anxiety disorders, depression co-morbid with physical illness, and other mental disorders is also justified by the initial findings.
Effect of binary combinations of solvent systems on permeability profiling of pure agomelatine across rat skin: a comparative study with statistically optimized polymeric nanoparticles
Published in Drug Development and Industrial Pharmacy, 2020
Mahesh Shinde, Nikhil Bali, Shahadev Rathod, Megha Karemore, Pramod Salve
Agomelatine, a naphthalene homolog of melatonin, is a selective MT1/MT2 agonist and serotonin 5-HT2c receptor antagonist [8]. It is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (∼30 mg/mL) but slightly soluble in water (0.022 mg/mL) and has low biological half-life of 1–2 h coupled with extensive hepatic first-pass metabolism and low oral bioavailability of 5–10% [9]. A conventional tablet dosage form of agomelatine is available commercially but due to low oral bioavailability frequent dose administration is required. Furthermore, for effective treatment of depression, drug administration for at least a period of one year is highly recommended to minimize the risk of recurrence of depressive episodes [3,6,9]. However, literature survey reports that around 40% patients discontinue the drug treatment within a one month while 56% patients’ shows noncompliance to treatment schedules within 4 months [10]. Thus, for critical management of depression, alternative treatment strategy which can maintain the steady state drug plasma concentration for prolong period with patience compliance is desirable.
Tasimelteon for treating non-24-h sleep-wake rhythm disorder
Published in Expert Opinion on Pharmacotherapy, 2019
Shohei Nishimon, Mari Nishimon, Seiji Nishino
We summarized their pharmacodynamic characterizations (Table 1) [73–75]. Although all can bind to the MT1 and MT2 receptor, the binding affinity differs in each compound [76]. Agomelatine especially has a unique pharmacological profile. It is recognized as the melatonergic antidepressant whereas the others are pure MT1 and MT2 receptor agonists [77,78]. Melatonin and ramelteon have higher affinity for the MT1 receptor (Ki value: 0.081 nM and 0.014 nM, respectively) compared with the MT2 receptor (0.383 nM and 0.112 nM, respectively) [44,68]. Agomelatine exhibits the same affinity for the MT1 receptor (0.10 nM) and MT2 receptor (0.12 nM), and it has a similar action as the 5-HT2C serotonin receptor antagonist (6.15 nM) [79]. The effect on 5-HT2C serotonin receptor may contribute to the antidepressant efforts. Characteristically, tasimelteon has a higher affinity for the MT2 receptor (0.0692 nM), which synchronizes the circadian phase shift compared with the MT1 receptor (0.304 nM) [40]. Therefore, we assumed that tasimelteon significantly regulates endogenous circadian rhythm and improves sleep efficiency.