새로운 멜라토닌성 약물들
New Melatonergic Agents
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초록
Melatonin is a major chronobiological regulator and has been used for the treatment of sleep problems including insomnia, parasomnia, and circadian rhythm sleep disorders. Because of melatonin’s short half-life, its suitability as a drug is limited. Thus, the development of prolonged-release melatonin and other melatonergic receptor agonists with a longer duration of action were needed. Ramelteon, non-indolic melatonergic agonist is the first drug approved in the USA for the treatment of insomnia. It showed highly selective melatonin MT1/MT2 receptor affinities which are believed to mediate the circadian rhythm whereas, negligible affinity for the MT3 receptor and other receptors in brain. This selective receptor affinity may explain the lack of significant adverse effect and lack of dependency or drug abuse potential. Another non-indolic melatonergic agonist is agomelatine initially evaluated for its chronobiotic effect. After its serotonergic effect was discovered, it was investigated as an antidepressant. There are studies indicating usefulness in controlling anxiety disorder and in seasonal affective disorder. Some studies showed agomelatine has a potential usefulness in improving sleep architecture. Tasimelteon is also an non-indolic melatonergic agonist which has high affinity for both MT1/MT2 receptors in humans and showed a similar affinity to melatonin. TIK-301, an indolic melatonin analogue also displays a high affinity towards melatonin MT1/MT2 receptors. Recently, TIK-301 has been shown that it also acts as an antagonist of the serotonin receptor subtype 5-HT2B and 5-HT2c, more potent than agomelatine. To elucidate efficacy and safety of newly developed melatonergic drugs, longer term multicenter clinical trials are needed.
Abstract
Melatonin is a major chronobiological regulator and has been used for the treatment of sleep problems including insomnia, parasomnia, and circadian rhythm sleep disorders. Because of melatonin’s short half-life, its suitability as a drug is limited. Thus, the development of prolonged-release melatonin and other melatonergic receptor agonists with a longer duration of action were needed. Ramelteon, non-indolic melatonergic agonist is the first drug approved in the USA for the treatment of insomnia. It showed highly selective melatonin MT1/MT2 receptor affinities which are believed to mediate the circadian rhythm whereas, negligible affinity for the MT3 receptor and other receptors in brain. This selective receptor affinity may explain the lack of significant adverse effect and lack of dependency or drug abuse potential. Another non-indolic melatonergic agonist is agomelatine initially evaluated for its chronobiotic effect. After its serotonergic effect was discovered, it was investigated as an antidepressant. There are studies indicating usefulness in controlling anxiety disorder and in seasonal affective disorder. Some studies showed agomelatine has a potential usefulness in improving sleep architecture. Tasimelteon is also an non-indolic melatonergic agonist which has high affinity for both MT1/MT2 receptors in humans and showed a similar affinity to melatonin. TIK-301, an indolic melatonin analogue also displays a high affinity towards melatonin MT1/MT2 receptors. Recently, TIK-301 has been shown that it also acts as an antagonist of the serotonin receptor subtype 5-HT2B and 5-HT2c, more potent than agomelatine. To elucidate efficacy and safety of newly developed melatonergic drugs, longer term multicenter clinical trials are needed.
참고문헌 (45)
- 조용원, "Epidemiology of Insomnia in Korean Adults: Prevalence and Associated Factors", Journal of Clinical Neurology, 5(1), pp.20~23 (2009), 대한신경과학회
- Vgontzas AN, "Sleep and its disorders", Annu Rev Med, 50, pp.387~400 (1999)
- Montgomery P, "A systematic review of non-pharmacological therapies for sleep problems in later life", Sleep Med Rev, 8, pp.47~62 (2004)
- Morin CM, "Nonpharmacologic treatment of chronic insomnia. An American Academy of Sleep Medicine review", Sleep, 22, pp.1134~1156 (1999)
- Nowell PD, "Benzodiazepines and zolpidem for chronic insomnia: a meta-analysis of treatment efficacy", JAMA, 278, pp.2170~2717 (1997)
- Mandrioli R, "Metabolism of benzodiazepine and non-benzodiazepine anxiolytic-hypnotic drugs: an analytical point of view", Curr Drug Metab, 11, pp.815~829 (2010)
- Zammit G, "Comparative tolerability of newer agents for insomnia", Drug Saf, 32, pp.735~748 (2009)
- Bellon A, "Searching for new options for treating insomnia: are melatonin and ramelteon beneficial?", J Psychiatr Pract, 12, pp.229~243 (2006)
- Lerner AB, "Isolation of melatonin, a pineal factor that lightens melanocytes", J Am Chem Soc, 80, pp.2587~ (1958)
- Hardeland R, "Investigational melatonin receptor agonists", Expert Opin Investig Drugs, 19, pp.747~764 (2010)
- Mor M, "Recent advances in the development of melatonin MT(1) and MT(2) receptor agonists", Expert Opin Ther Pat, 20, pp.1059~1077 (2010)
- Rajaratnam SMW, "Melatonin and melatonin analogues", Sleep Med Clin, 4, pp.179~193 (2009)
- Wilson SJ, "British Association for Psychopharmacology consensus statement on evidence-based treatment of insomnia, parasomnias and circadian rhythm disorders", J Psychopharmacol, 24, pp.1577~1601 (2010)
- Haimov I, "Sleep disorders and melatonin rhythms in elderly people", BMJ, 309, pp.167~ (1994)
- National Institutes of Health, "National Institutes of Health State of the Science Conference statement on Manifestations and Management of Chronic Insomnia in Adults", Sleep, 28, pp.1049~1057 (2005)
- Kato K, "Neurochemical properties of ramelteon (TAK-375), a selective MT1", MT2 receptor agonist, 2005, pp.48, 301~310
- Miyamoto M, "Pharmacology of ramelteon, a selective MT1", MT2 receptor agonist: a novel therapeutic drug for sleep disorders, 2009, pp.15, 32~51
- Cajochen C, "TAK-375 Takeda", Curr Opin Investig Drugs, 6, pp.114~121 (2005)
- Greenblatt DJ, "Age and gender effects on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic agent acting via melatonin receptors MT1 and MT2", J Clin Pharmacol, 47, pp.485~496 (2007)
- McGechan A, "Ramelteon", CNS Drugs, 19, pp.1057~1065 (2005)
- Karim A, "Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia", J Clin Pharmacol, 46, pp.140~148 (2006)
- Erman M, "An efficacy, safety, and dose-response study of Ramelteon in patients with chronic primary insomnia", Sleep Med, 7, pp.17~24 (2006)
- Roth T, "Effects of ramelteon on patient-reported sleep latency in older adults with chronic insomnia", Sleep Med, 7, pp.312~318 (2006)
- Mayer G, "Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic primary insomnia", Sleep, 32, pp.351~360 (2009)
- Uchiyama M, "Long-term safety and efficacy of ramelteon in Japanese patients with chronic insomnia", Sleep Med, 12, pp.127~133 (2011)
- Richardson G, "Effects of long-term exposure to ramelteon, a melatonin receptor agonist, on endocrine function in adults with chronic insomnia", Hum Psychopharmacol, 24, pp.103~111 (2009)
- Karim A, "Effects of fluconazole and ketoconazole on the pharmacokinetics of ramelteon (TAK-375) in normal healthy male and female subjects", Sleep, 27, pp.A53~A54 (2004)
- "Physician’s desk reference" (2010), Thomson PDR
- Millan MJ, "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, 306, pp.954~964 (2003)
- Manikandan S, "Agomelatine: a novel melatonergic antidepressant", J Pharmacol Pharmacother, 1, pp.122~123 (2010)
- Bertaina-Anglade V, "Antidepressant-like effects of agomelatine (S 20098) in the learned helplessness model", Behav Pharmacol, 17, pp.703~713 (2006)
- Lôo 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, 17, pp.239~247 (2002)
- den Boer JA, "Clinical efficacy of agomelatine in depression: the evidence", Int Clin Psychopharmacol, 21(Suppl 1), pp.S21~S24 (2006)
- Quera Salva MA, "Major depressive disorder, sleep EEG and agomelatine: an open-label study", Int J Neuropsycho-pharmacol, 10, pp.691~696 (2007)
- Lopes MC, "Non-REM sleep instabi-lity in patients with major depressive disorder: subjective improvement and improvement of non-REM sleep instability with treatment (Agome-latine)", Sleep Med, 9, pp.33~41 (2007)
- Srinivasan V, "Melatonin agonists in primary insomnia and depression-associated insomnia: are they superior to sedative-hypnotics?", Prog Neuropsychopharmacol Biol Psychiatry, 35, pp.913~923 (2011)
- Zupancic M, "Agomelatine: a preliminary review of a new antidepressant", CNS Drugs, 20, pp.981~992 (2006)
- Kasper S, "Efficacy of the novel antidepressant agomelatine on the circadian rest-activity cycle and depressive and anxiety symptoms in patients with major depressive disorder: a randomized, double-blind comparison with sertraline", J Clin Psychiatry, 71, pp.109~120 (2010)
- Millan MJ., "Multi-target strategies for the improved treatment of depressive states: conceptual foundations and neuronal substrates, drug discovery and therapeutic application", Pharmacol Ther, 110, pp.135~370 (2006)
- Kennedy SH, "Agomelatine in the treatment of major depressive disorder: potential for clinical effectiveness", CNS Drugs, 24, pp.479~499 (2010)
- McAllister-Williams RH, "The use of antidepressants in clinical practice: focus on agomelatine", Hum Psycho-pharmacol, 25, pp.95~102 (2010)
- Rajaratnam SM, "Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials", Lancet, 373, pp.482~491 (2009)
- Mulchahey JJ, "A single blind, placebo controlled, across groups dose escalation study of the safety, tolerability, pharmacokinetics and pharmacodynamics of the melatonin analog beta-methyl-6-chloromelatonin", Life Sci, 75, pp.1843~1856 (2004)
- Zemlan FP, "The efficacy and safety of the melatonin agonist beta-methyl-6-chloromelatonin in primary insomnia: a randomized, placebo-con-trolled, crossover clinical trial", J Clin Psychiatry, 66, pp.384~390 (2005)
- Claustrat B, "The basic physiology and pathophysiology of melatonin", Sleep Med Rev, 9, pp.11~24 (2005)