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https://www.readbyqxmd.com/read/29303950/cns-drug-development-lessons-learned-part-4-the-role-of-brain-circuitry-and-genes-tasimelteon-as-an-example
#1
Sheldon H Preskorn
This is the fourth in a series of columns discussing the rational and targeted development of drugs to affect specific central nervous system (CNS) circuits in specific ways based on knowledge gained by molecular biology and the human genome project. The first column in this series described 6 CNS drugs with novel mechanisms of action developed over the last 25 years. The second column discussed differences between syndromic diagnoses as exemplified by the third through the fifth editions of the Diagnostic and Statistical Manual of Mental Disorders (DSM III through DSM-5) and the new approach to psychiatric diagnoses championed by the National Institute of Mental Health in their Research Domain Criteria Initiative...
November 2017: Journal of Psychiatric Practice
https://www.readbyqxmd.com/read/29300899/tissue-distribution-of-suvorexant-in-three-forensic-autopsy-cases
#2
Brian Waters, Kenji Hara, Natsuki Ikematsu, Mio Takayama, Aya Matsusue, Masayuki Kashiwagi, Shin-Ichi Kubo
Suvorexant (Belsomra®) is a relatively new insomnia medication that has been available in USA and Japan since 2014. It is a dual orexin receptor antagonist that promotes sleep by inhibiting the binding of orexin neurons to the OX1R and OX2R receptors. In this report, we describe the detection and quantitation of suvorexant from the postmortem specimens of three separate autopsy cases handled by our department. Suvorexant was identified by fast gas chromatography/mass spectrometry during routine screening, and quantitated by a fully validated liquid chromatography-tandem mass spectroscopy method...
December 28, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29289556/chronopathophysiological-implications-of-orexin-in-sleep-disturbances-and-lifestyle-related-disorders
#3
REVIEW
Hiroshi Tsuneki, Tsutomu Wada, Toshiyasu Sasaoka
Sleep, a mysterious behavior, has recently been recognized as a crucial factor for health and longevity. The daily sleep/wake cycle provides the basis of biorhythms controlling whole-body homeostasis and homeodynamics; therefore, disruption of sleep causes several physical and psychological disorders, including cardiovascular disease, obesity, diabetes, cancer, anxiety, depression, and cognitive dysfunction. However, the mechanism linking sleep disturbances and sleep-related disorders remains unknown. Orexin (also known as hypocretin) is a neuropeptide produced in the hypothalamus...
December 28, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29237271/suvorexant-for-the-treatment-of-insomnia-in-patients-with-alzheimer-s-disease
#4
Atsushi Hamuro, Minoru Honda, Yuya Wakaura
No abstract text is available yet for this article.
December 1, 2017: Australian and New Zealand Journal of Psychiatry
https://www.readbyqxmd.com/read/29225076/crystal-structures-of-human-orexin-2-receptor-bound-to-the-subtype-selective-antagonist-empa
#5
Ryoji Suno, Kanako Terakado Kimura, Takanori Nakane, Keitaro Yamashita, Junmei Wang, Takaaki Fujiwara, Yasuaki Yamanaka, Dohyun Im, Shoichiro Horita, Hirokazu Tsujimoto, Maki S Tawaramoto, Takatsugu Hirokawa, Eriko Nango, Kensuke Tono, Takashi Kameshima, Takaki Hatsui, Yasumasa Joti, Makina Yabashi, Keiko Shimamoto, Masaki Yamamoto, Daniel M Rosenbaum, So Iwata, Tatsuro Shimamura, Takuya Kobayashi
Orexin peptides in the brain regulate physiological functions such as the sleep-wake cycle, and are thus drug targets for the treatment of insomnia. Using serial femtosecond crystallography and multi-crystal data collection with a synchrotron light source, we determined structures of human orexin 2 receptor in complex with the subtype-selective antagonist EMPA (N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide) at 2.30-Å and 1.96-Å resolution. In comparison with the non-subtype-selective antagonist suvorexant, EMPA contacted fewer residues through hydrogen bonds at the orthosteric site, explaining the faster dissociation rate...
November 27, 2017: Structure
https://www.readbyqxmd.com/read/29112763/insight-into-reduction-of-wakefulness-by-suvorexant-in-patients-with-insomnia-analysis-of-wake-bouts
#6
Vladimir Svetnik, Ellen S Snyder, Peining Tao, Thomas E Scammell, Thomas Roth, Christopher Lines, W Joseph Herring
Objectives: To examine the duration and frequency of wake bouts underlying the wakefulness-after-sleep-onset (WASO) reduction with suvorexant. Methods: We analyzed polysomnogram recordings from clinical trials involving 1518 insomnia patients receiving suvorexant (40/30mg, 20/15mg) or placebo to determine: 1) the number of, and time spent in, long or short wake bouts, 2) the association between sleep quality and bout characteristics. We also compared wake and sleep bout characteristics of suvorexant in insomnia patients versus zolpidem in healthy subjects undergoing experimentally-induced transient insomnia...
November 3, 2017: Sleep
https://www.readbyqxmd.com/read/29066641/adverse-reaction-with-suvorexant-for-insomnia-acute-worsening-of-depression-with-emergence-of-suicidal-thoughts
#7
Jeremy Petrous, Kevin Furmaga
A 59-year-old woman on daily peritoneal dialysis for end-stage renal failure received care at an outpatient psychiatric clinic for her diagnoses that include major depressive disorder, generalised anxiety disorder and insomnia disorder. Although there was partial improvement in the patient's mood and anxiety symptoms with antidepressant treatment, insomnia remained a persistent complaint despite adequate trials of different sleep medications. The novel hypnotic, suvorexant (Belsomra, Merck & Co.) was then initiated at the recommended bedtime dose of 10 mg and was followed by a 15 mg dose the following night...
October 23, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28994603/suvorexant-scientifically-interesting-utility-uncertain
#8
Nicholas A Keks, Judy Hope, Simone Keogh
OBJECTIVE: Suvorexant, a new hypnotic, is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance, and is used long-term. This paper will briefly review suvorexant. RESULTS: Orexin is a hypothalamic peptide which promotes wakefulness. By blocking orexin receptors, suvorexant induces sleep. Peaking 2 h after ingestion, it has a half-life of 12 h and is hepatically metabolized mainly by CYP3A. Kinetics are not affected by age but concentrations are higher in females and obese patients...
December 2017: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/28992822/therapy-update-for-insomnia-in-the-elderly
#9
Sum Lam, Lucy O Macina
OBJECTIVE: To offer an update on insomnia in older adults and treatment options. DATA SOURCES: A search of PubMed using the terms "insomnia" and "older adults" was performed. Current guidelines, review articles, and drug database and manufacturer package inserts were utilized to provide relevant information. STUDY SELECTION: All English-language articles from 2012 to February 2017 and their bibliographies were reviewed for relevance. Current guidelines from the American College of Physicians, the American Academy of Sleep Medicine, and the American Geriatrics Society's Beers criteria were reviewed...
October 1, 2017: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
https://www.readbyqxmd.com/read/28798520/suvorexant
#10
REVIEW
(no author information available yet)
No abstract text is available yet for this article.
June 2017: Australian Prescriber
https://www.readbyqxmd.com/read/28767209/preventive-effects-of-suvorexant-on-delirium-a-randomized-placebo-controlled-trial
#11
RANDOMIZED CONTROLLED TRIAL
Kotaro Hatta, Yasuhiro Kishi, Ken Wada, Takashi Takeuchi, Shigeo Ito, Akiko Kurata, Kazunori Murakami, Manabu Sugita, Chie Usui, Hiroyuki Nakamura
OBJECTIVE: No highly effective pharmacologic interventions to prevent delirium have been identified. We examined whether suvorexant, a potent and selective orexin receptor antagonist, is effective for the prevention of delirium. METHODS: We conducted a multicenter, rater-blinded, randomized, placebo-controlled clinical trial in intensive care units and regular acute wards between April 2015 and March 2016. Eligible patients were 65 to 89 years old, newly admitted due to emergency, and able to take medicine orally and had an expected stay or life expectancy of 48 hours or more...
September 2017: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/28741623/effects-of-suvorexant-a-dual-orexin-hypocretin-receptor-antagonist-on-impulsive-behavior-associated-with-cocaine
#12
Taylor A Gentile, Steven J Simmons, Mia N Watson, Krista L Connelly, Eugen Brailoiu, Yanan Zhang, John W Muschamp
Hypothalamic hypocretin (orexin) peptides mediate arousal, attention, and reward processing. Fibers containing orexins project to brain structures that govern motivated behavior, including the ventral tegmental area (VTA). A number of psychiatric conditions, including attention deficit hyperactivity disorder (ADHD) and substance use disorders, are characterized by deficits in impulse control, however the relationship between orexin and impulsive behavior is incompletely characterized. The effects of systemic or centrally administered orexin receptor (OXR) antagonists on measures of impulsive-like behavior in rats were evaluated using the five-choice serial reaction time task (5-CSRTT) and delay discounting procedures...
July 25, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28725169/postoperative-delirium-after-pharyngolaryngectomy-with-esophagectomy-a-role-for-ramelteon-and-suvorexant
#13
Eisuke Booka, Yasuhiro Tsubosa, Teruaki Matsumoto, Mari Takeuchi, Takashi Kitani, Masato Nagaoka, Atsushi Imai, Tomoyuki Kamijo, Yoshiyuki Iida, Ayako Shimada, Katsushi Takebayashi, Masahiro Niihara, Keita Mori, Tetsuro Onitsuka, Hiroya Takeuchi, Yuko Kitagawa
BACKGROUND: Postoperative delirium is common after extensive surgery, and is known to be associated with sleeping medications. In this study, we aimed to investigate the relationships between sleeping medications and postoperative delirium after pharyngolaryngectomy with esophagectomy. METHODS: We performed a retrospective analysis of 65 patients who underwent pharyngolaryngectomy with esophagectomy at Shizuoka Cancer Center Hospital between January 2012 and March 2016...
2017: Esophagus: Official Journal of the Japan Esophageal Society
https://www.readbyqxmd.com/read/28671376/insomnia-pharmacologic-therapy
#14
REVIEW
Eric Matheson, Barry L Hainer
Insomnia accounts for more than 5.5 million visits to family physicians each year. Although behavioral interventions are the mainstay of treatment, pharmacologic therapy may be necessary for some patients. Understanding the risks and benefits of insomnia medications is critical. Controlled-release melatonin and doxepin are recommended as first-line agents in older adults; the so-called z-drugs (zolpidem, eszopiclone, and zaleplon) should be reserved for use if the first-line agents are ineffective. For the general population with difficulty falling asleep, controlled-release melatonin and the z-drugs can be considered...
July 1, 2017: American Family Physician
https://www.readbyqxmd.com/read/28663311/the-use-of-physiology-based-pharmacokinetic-and-pharmacodynamic-modeling-in-the-discovery-of-the-dual-orexin-receptor-antagonist-act-541468
#15
RANDOMIZED CONTROLLED TRIAL
Alexander Treiber, Ruben de Kanter, Catherine Roch, John Gatfield, Christoph Boss, Markus von Raumer, Benno Schindelholz, Clemens Muehlan, Joop van Gerven, Francois Jenck
The identification of new sleep drugs poses particular challenges in drug discovery owing to disease-specific requirements such as rapid onset of action, sleep maintenance throughout major parts of the night, and absence of residual next-day effects. Robust tools to estimate drug levels in human brain are therefore key for a successful discovery program. Animal models constitute an appropriate choice for drugs without species differences in receptor pharmacology or pharmacokinetics. Translation to man becomes more challenging when interspecies differences are prominent...
September 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28631980/orexin-research-patent-news-from-2016
#16
REVIEW
Christoph Boss, Catherine Roch
The orexin system consists of two G-protein-coupled receptors, orexin 1 and orexin 2 and two endogenous ligands, orexin A and orexin B . It is evolutionarily highly conserved. It is involved in the promotion of wakefulness as well as in anxiety and addictive disorders. In addition, its activation via the Ox1 receptor triggers apoptosis in several cancer cell lines. Dual orexin receptor antagonists are successfully used to treat primary insomnia. The major open questions are now related to the clinical validation of Ox1 selective antagonists...
October 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28584695/neuroendocrine-autonomic-and-metabolic-responses-to-an-orexin-antagonist-suvorexant-in-psychiatric-patients-with-insomnia
#17
Masaru Nakamura, Takahiko Nagamine
Aim: The aim of this study was to investigate the neuroendocrine, autonomic, and metabolic system responses to suvorexant in psychiatric subjects with insomnia. Design: This prospective study was conducted in Kusatsu Hospital in Hiroshima, Japan and included 40 psychiatric inpatients treated with suvorexant from December 2014 to April 2016. Methods: Questionnaire of Pittsburgh Sleep Quality Index (PSQI), Generalized Anxiety Disorder-7 (GAD-7), and Patient Health Questionnaire-9 (PHQ-9) scores were checked at baseline, Week 2, and Week 4, and fasting serum levels of prolactin, insulin, cortisol, noradrenaline, white blood cell count, and average pulse rate were measured at baseline and Week 4 and Week 8 after suvorexant initiation...
March 2017: Innovations in Clinical Neuroscience
https://www.readbyqxmd.com/read/28559480/in-vitro-and-in-silico-characterization-of-lemborexant-e2006-a-novel-dual-orexin-receptor-antagonist
#18
Carsten Theodor Beuckmann, Michiyuki Suzuki, Takashi Ueno, Kazuya Nagaoka, Tohru Arai, Hiroyuki Higashiyama
Orexin (hypocretin) neuropeptides have, among others, been implicated in arousal/sleep control, and antagonizing the orexin signaling pathway has been previously demonstrated to promote sleep in animals and humans. This mechanism opens up a new therapeutic approach to curb excessive wakefulness in insomnia disorder rather than to promote sleep-related signaling. Here we describe the preclinical pharmacological in vitro and in silico characterization of lemborexant ((1R,2S)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide)), a dual orexin receptor antagonist (DORA), as a novel experimental therapeutic agent for the symptomatic treatment of insomnia disorder and compare its properties to two other DORAs, almorexant and suvorexant...
August 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28520464/suvorexant-for-the-treatment-of-insomnia-in-adolescents
#19
Kentaro Kawabe, Fumie Horiuchi, Marina Ochi, Kayoko Nishimoto, Shu-Ichi Ueno, Yasunori Oka
OBJECTIVES: Suvorexant is the first dual orexin receptor antagonist for treating insomnia. This study aimed to evaluate the tolerability, efficacy, and safety of suvorexant on insomnia in adolescents. METHODS: Thirty patients (8 male and 22 female; mean standard deviation age: 15.7 ± 2.4 years; range: 10-20) with insomnia were administered suvorexant. Clinical background, persistence rate, the Clinical Global Impression (CGI), and the Athens Insomnia Scale (AIS) were compared between patients who continued and discontinued suvorexant treatment...
November 2017: Journal of Child and Adolescent Psychopharmacology
https://www.readbyqxmd.com/read/28447885/recovery-from-coma-post-cardiac-arrest-is-dependent-on-the-orexin-pathway
#20
Young-Jin Kang, Guilian Tian, Afsheen Bazrafkan, Maryam H Farahabadi, Matine Azadian, Hamidreza Abbasi, Brittany E Shamaoun, Oswald Steward, Yama Akbari
Cardiac arrest (CA) affects >550,000 people annually in the United States whereas 80-90% of survivors suffer from a comatose state. Arousal from coma is critical for recovery, but mechanisms of arousal are undefined. Orexin-A, a hypothalamic excitatory neuropeptide, has been linked to arousal deficits in various brain injuries. We investigated the orexinergic system's role in recovery from CA-related neurological impairments, including arousal deficits. Using an asphyxial CA and resuscitation model in rats, we examine neurological recovery post-resuscitation in conjunction with changes in orexin-A levels in cerebrospinal fluid (CSF) and orexin-expressing neurons...
October 1, 2017: Journal of Neurotrauma
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