The Experts below are selected from a list of 1548 Experts worldwide ranked by ideXlab platform
Joel C. Marrs - One of the best experts on this subject based on the ideXlab platform.
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Indiplon: A Nonbenzodiazepine Sedative–Hypnotic for the Treatment of Insomnia
The Annals of pharmacotherapy, 2008Co-Authors: Joel C. MarrsAbstract:Objective:To review the pharmacology, pharmacokinetics, pharmacodynamics, efficacy data, and adverse effects of indiplon in the treatment of transient and chronic insomnia in adult and geriatric patients.Data Sources:A literature search was conducted using MEDLINE (1966–May 2006), International Pharmaceutical Abstracts (1970–May 2008), and Cochrane database (2007) (or the key words indiplon or NBI-34060. References cited in the articles were reviewed for additional Information. Abstract data were included only in the absence of significant published data.Study Selection and Data Extraction:English-language literature reporting animal and human clinical studies was reviewed to evaluate data on the pharmacology, pharmacokinetics, pharmacodynamics, efficacy, and adverse effects of indiplon. Clinical trials selected for inclusion were limited to those with human subjects, with the accepted Inclusion of pharmacology data in animals.Data Synthesis:Indiplon Is a Nonbenzodiazepine sedative-hypnotic that exhibits ...
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indiplon a Nonbenzodiazepine sedative hypnotic for the treatment of insomnia
Annals of Pharmacotherapy, 2008Co-Authors: Joel C. MarrsAbstract:Objective:To review the pharmacology, pharmacokinetics, pharmacodynamics, efficacy data, and adverse effects of indiplon in the treatment of transient and chronic insomnia in adult and geriatric patients.Data Sources:A literature search was conducted using MEDLINE (1966–May 2006), International Pharmaceutical Abstracts (1970–May 2008), and Cochrane database (2007) (or the key words indiplon or NBI-34060. References cited in the articles were reviewed for additional Information. Abstract data were included only in the absence of significant published data.Study Selection and Data Extraction:English-language literature reporting animal and human clinical studies was reviewed to evaluate data on the pharmacology, pharmacokinetics, pharmacodynamics, efficacy, and adverse effects of indiplon. Clinical trials selected for inclusion were limited to those with human subjects, with the accepted Inclusion of pharmacology data in animals.Data Synthesis:Indiplon Is a Nonbenzodiazepine sedative-hypnotic that exhibits ...
Toshiharu Shiba - One of the best experts on this subject based on the ideXlab platform.
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binding and neuropharmacological profile of zaleplon a novel Nonbenzodiazepine sedative hypnotic
European Journal of Pharmacology, 2002Co-Authors: Hideaki Noguchi, Kazuhiro Kitazumi, Megumi Mori, Toshiharu ShibaAbstract:Abstract The binding properties of CL284,846 (zaleplon), a novel Nonbenzodiazepine sedative/hypnotic, at benzodiazepine receptor subtypes were evaluated. Zaleplon was 14.3 times more potent at inhibiting [ 3 H]flunitrazepam binding to membrane preparations of the cerebellum than to membrane preparations of the spinal cord. The γ-aminobutyric acid (GABA) ratio of zaleplon was 2.07. Zaleplon produced significant increases in muscimol binding similar to those of diazepam, and it was antagonized by flumazenil. Furthermore, zaleplon showed little affinity for other receptors. Spectral analysis of the electroencephalogram (EEG) of rabbits showed that zaleplon and 3-methyl-6-[3-(trifluoromethyl) phenyl]-1,2,4,-triazolo [4,3-β] pyridazine (CL218,872), an ω 1 receptor-selective compound (1 mg/kg, i.v., respectively), produced large increases in energy of the delta frequency band without affecting the energy of the alpha and beta frequency bands. In contrast, intravenous administration of triazolam and zopiclone increased the energy of the beta frequency band at doses of 0.1 and 2 mg/kg, respectively. In addition, the zaleplon-induced increase in the energy of the delta frequency band was antagonized by pretreatment with flumazenil (1 mg/kg, i.v.), which did not affect the spontaneous EEG alone. The present results clearly demonstrate that zaleplon is a selective full agonist of the ω 1 receptor subtype, and thus, zaleplon may induce responses closely resembling the physiological pattern of slow wave sleep.
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Binding and neuropharmacological profile of zaleplon, a novel Nonbenzodiazepine sedative/hypnotic.
European journal of pharmacology, 2002Co-Authors: Hideaki Noguchi, Kazuhiro Kitazumi, Megumi Mori, Toshiharu ShibaAbstract:The binding properties of CL284,846 (zaleplon), a novel Nonbenzodiazepine sedative/hypnotic, at benzodiazepine receptor subtypes were evaluated. Zaleplon was 14.3 times more potent at inhibiting [3H]flunitrazepam binding to membrane preparations of the cerebellum than to membrane preparations of the spinal cord. The gamma-aminobutyric acid (GABA) ratio of zaleplon was 2.07. Zaleplon produced significant increases in muscimol binding similar to those of diazepam, and it was antagonized by flumazenil. Furthermore, zaleplon showed little affinity for other receptors. Spectral analysis of the electroencephalogram (EEG) of rabbits showed that zaleplon and 3-methyl-6-[3-(trifluoromethyl) phenyl]-1,2,4,-triazolo [4,3-beta] pyridazine (CL218,872), an omega(1) receptor-selective compound (1 mg/kg, i.v., respectively), produced large increases in energy of the delta frequency band without affecting the energy of the alpha and beta frequency bands. In contrast, intravenous administration of triazolam and zopiclone increased the energy of the beta frequency band at doses of 0.1 and 2 mg/kg, respectively. In addition, the zaleplon-induced increase in the energy of the delta frequency band was antagonized by pretreatment with flumazenil (1 mg/kg, i.v.), which did not affect the spontaneous EEG alone. The present results clearly demonstrate that zaleplon is a selective full agonist of the omega(1) receptor subtype, and thus, zaleplon may induce responses closely resembling the physiological pattern of slow wave sleep.
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Binding and neuropharmacological profile of zaleplon, a novel Nonbenzodiazepine sedative/hypnotic
European Journal of Pharmacology, 2001Co-Authors: Hideaki Noguchi, Kazuhiro Kitazumi, Megumi Mori, Toshiharu ShibaAbstract:Abstract The binding properties of CL284,846 (zaleplon), a novel Nonbenzodiazepine sedative/hypnotic, at benzodiazepine receptor subtypes were evaluated. Zaleplon was 14.3 times more potent at inhibiting [ 3 H]flunitrazepam binding to membrane preparations of the cerebellum than to membrane preparations of the spinal cord. The γ-aminobutyric acid (GABA) ratio of zaleplon was 2.07. Zaleplon produced significant increases in muscimol binding similar to those of diazepam, and it was antagonized by flumazenil. Furthermore, zaleplon showed little affinity for other receptors. Spectral analysis of the electroencephalogram (EEG) of rabbits showed that zaleplon and 3-methyl-6-[3-(trifluoromethyl) phenyl]-1,2,4,-triazolo [4,3-β] pyridazine (CL218,872), an ω 1 receptor-selective compound (1 mg/kg, i.v., respectively), produced large increases in energy of the delta frequency band without affecting the energy of the alpha and beta frequency bands. In contrast, intravenous administration of triazolam and zopiclone increased the energy of the beta frequency band at doses of 0.1 and 2 mg/kg, respectively. In addition, the zaleplon-induced increase in the energy of the delta frequency band was antagonized by pretreatment with flumazenil (1 mg/kg, i.v.), which did not affect the spontaneous EEG alone. The present results clearly demonstrate that zaleplon is a selective full agonist of the ω 1 receptor subtype, and thus, zaleplon may induce responses closely resembling the physiological pattern of slow wave sleep.
Sarah L. Anderson - One of the best experts on this subject based on the ideXlab platform.
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novel class of medications orexin receptor antagonists in the treatment of insomnia critical appraisal of suvorexant
Nature and Science of Sleep, 2016Co-Authors: Jessica L Norman, Sarah L. AndersonAbstract:Insomnia, a highly prevalent disorder, can be detrimental to patients' overall health and worsen existing comorbidities. Patients may have acute episodes of insomnia related to a traumatic event, but more commonly insomnia occurs chronically. While proper sleep hygiene and behavioral therapy play important roles in the nonpharmacologic management of short-term and chronic insomnia, medications may also be required. Historically, insomnia has been treated with agents such as benzodiazepines, Nonbenzodiazepine receptor agonists, and melatonin agonists. Dual orexin receptor antagonists represent a new class of medications for the treatment of insomnia, which block the binding of wakefulness-promoting neuropeptides orexin A and orexin B to their respective receptor sites. Suvorexant (Belsomra) is the first dual orexin receptor antagonist to be approved in the US and Japan and has demonstrated efficacy in decreasing time to sleep onset and increasing total sleep time. Its unique mechanism of action, data to support efficacy and safety over 12 months of use, and relative lack of withdrawal effects when discontinued may represent an alternative for patients with chronic insomnia who cannot tolerate or do not receive benefit from more traditional sleep agents. Suvorexant is effective and well tolerated, but precautions exist for certain patient populations, including females, obese patients, and those with respiratory disease. Suvorexant has only been studied vs placebo, and hence it is unknown how it directly compares with other medications approved by the US Food and Drug Administration for insomnia. Suvorexant is not likely to replace benzodiazepines or Nonbenzodiazepine receptor antagonists as a first-line sleep agent but does represent a novel option for the treatment of patients with chronic insomnia.
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Novel class of medications, orexin receptor antagonists, in the treatment of insomnia – critical appraisal of suvorexant
Nature and science of sleep, 2016Co-Authors: Jessica L Norman, Sarah L. AndersonAbstract:Insomnia, a highly prevalent disorder, can be detrimental to patients' overall health and worsen existing comorbidities. Patients may have acute episodes of insomnia related to a traumatic event, but more commonly insomnia occurs chronically. While proper sleep hygiene and behavioral therapy play important roles in the nonpharmacologic management of short-term and chronic insomnia, medications may also be required. Historically, insomnia has been treated with agents such as benzodiazepines, Nonbenzodiazepine receptor agonists, and melatonin agonists. Dual orexin receptor antagonists represent a new class of medications for the treatment of insomnia, which block the binding of wakefulness-promoting neuropeptides orexin A and orexin B to their respective receptor sites. Suvorexant (Belsomra) is the first dual orexin receptor antagonist to be approved in the US and Japan and has demonstrated efficacy in decreasing time to sleep onset and increasing total sleep time. Its unique mechanism of action, data to support efficacy and safety over 12 months of use, and relative lack of withdrawal effects when discontinued may represent an alternative for patients with chronic insomnia who cannot tolerate or do not receive benefit from more traditional sleep agents. Suvorexant is effective and well tolerated, but precautions exist for certain patient populations, including females, obese patients, and those with respiratory disease. Suvorexant has only been studied vs placebo, and hence it is unknown how it directly compares with other medications approved by the US Food and Drug Administration for insomnia. Suvorexant is not likely to replace benzodiazepines or Nonbenzodiazepine receptor antagonists as a first-line sleep agent but does represent a novel option for the treatment of patients with chronic insomnia.
Hideaki Noguchi - One of the best experts on this subject based on the ideXlab platform.
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binding and neuropharmacological profile of zaleplon a novel Nonbenzodiazepine sedative hypnotic
European Journal of Pharmacology, 2002Co-Authors: Hideaki Noguchi, Kazuhiro Kitazumi, Megumi Mori, Toshiharu ShibaAbstract:Abstract The binding properties of CL284,846 (zaleplon), a novel Nonbenzodiazepine sedative/hypnotic, at benzodiazepine receptor subtypes were evaluated. Zaleplon was 14.3 times more potent at inhibiting [ 3 H]flunitrazepam binding to membrane preparations of the cerebellum than to membrane preparations of the spinal cord. The γ-aminobutyric acid (GABA) ratio of zaleplon was 2.07. Zaleplon produced significant increases in muscimol binding similar to those of diazepam, and it was antagonized by flumazenil. Furthermore, zaleplon showed little affinity for other receptors. Spectral analysis of the electroencephalogram (EEG) of rabbits showed that zaleplon and 3-methyl-6-[3-(trifluoromethyl) phenyl]-1,2,4,-triazolo [4,3-β] pyridazine (CL218,872), an ω 1 receptor-selective compound (1 mg/kg, i.v., respectively), produced large increases in energy of the delta frequency band without affecting the energy of the alpha and beta frequency bands. In contrast, intravenous administration of triazolam and zopiclone increased the energy of the beta frequency band at doses of 0.1 and 2 mg/kg, respectively. In addition, the zaleplon-induced increase in the energy of the delta frequency band was antagonized by pretreatment with flumazenil (1 mg/kg, i.v.), which did not affect the spontaneous EEG alone. The present results clearly demonstrate that zaleplon is a selective full agonist of the ω 1 receptor subtype, and thus, zaleplon may induce responses closely resembling the physiological pattern of slow wave sleep.
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Binding and neuropharmacological profile of zaleplon, a novel Nonbenzodiazepine sedative/hypnotic.
European journal of pharmacology, 2002Co-Authors: Hideaki Noguchi, Kazuhiro Kitazumi, Megumi Mori, Toshiharu ShibaAbstract:The binding properties of CL284,846 (zaleplon), a novel Nonbenzodiazepine sedative/hypnotic, at benzodiazepine receptor subtypes were evaluated. Zaleplon was 14.3 times more potent at inhibiting [3H]flunitrazepam binding to membrane preparations of the cerebellum than to membrane preparations of the spinal cord. The gamma-aminobutyric acid (GABA) ratio of zaleplon was 2.07. Zaleplon produced significant increases in muscimol binding similar to those of diazepam, and it was antagonized by flumazenil. Furthermore, zaleplon showed little affinity for other receptors. Spectral analysis of the electroencephalogram (EEG) of rabbits showed that zaleplon and 3-methyl-6-[3-(trifluoromethyl) phenyl]-1,2,4,-triazolo [4,3-beta] pyridazine (CL218,872), an omega(1) receptor-selective compound (1 mg/kg, i.v., respectively), produced large increases in energy of the delta frequency band without affecting the energy of the alpha and beta frequency bands. In contrast, intravenous administration of triazolam and zopiclone increased the energy of the beta frequency band at doses of 0.1 and 2 mg/kg, respectively. In addition, the zaleplon-induced increase in the energy of the delta frequency band was antagonized by pretreatment with flumazenil (1 mg/kg, i.v.), which did not affect the spontaneous EEG alone. The present results clearly demonstrate that zaleplon is a selective full agonist of the omega(1) receptor subtype, and thus, zaleplon may induce responses closely resembling the physiological pattern of slow wave sleep.
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Binding and neuropharmacological profile of zaleplon, a novel Nonbenzodiazepine sedative/hypnotic
European Journal of Pharmacology, 2001Co-Authors: Hideaki Noguchi, Kazuhiro Kitazumi, Megumi Mori, Toshiharu ShibaAbstract:Abstract The binding properties of CL284,846 (zaleplon), a novel Nonbenzodiazepine sedative/hypnotic, at benzodiazepine receptor subtypes were evaluated. Zaleplon was 14.3 times more potent at inhibiting [ 3 H]flunitrazepam binding to membrane preparations of the cerebellum than to membrane preparations of the spinal cord. The γ-aminobutyric acid (GABA) ratio of zaleplon was 2.07. Zaleplon produced significant increases in muscimol binding similar to those of diazepam, and it was antagonized by flumazenil. Furthermore, zaleplon showed little affinity for other receptors. Spectral analysis of the electroencephalogram (EEG) of rabbits showed that zaleplon and 3-methyl-6-[3-(trifluoromethyl) phenyl]-1,2,4,-triazolo [4,3-β] pyridazine (CL218,872), an ω 1 receptor-selective compound (1 mg/kg, i.v., respectively), produced large increases in energy of the delta frequency band without affecting the energy of the alpha and beta frequency bands. In contrast, intravenous administration of triazolam and zopiclone increased the energy of the beta frequency band at doses of 0.1 and 2 mg/kg, respectively. In addition, the zaleplon-induced increase in the energy of the delta frequency band was antagonized by pretreatment with flumazenil (1 mg/kg, i.v.), which did not affect the spontaneous EEG alone. The present results clearly demonstrate that zaleplon is a selective full agonist of the ω 1 receptor subtype, and thus, zaleplon may induce responses closely resembling the physiological pattern of slow wave sleep.
Timothy P. Rohrig - One of the best experts on this subject based on the ideXlab platform.
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The Use of Z-Drugs to Facilitate Sexual Assault.
Forensic science review, 2010Co-Authors: T L Stockham, Timothy P. RohrigAbstract:Zolpidem, zopiclone, and zaleplon are commonly referred to as the "Z-drugs." The Z-drugs are Nonbenzodiazepine hypnotics indicated for the short-term treatment of insomnia. Since becoming widely prescribed as sleep aids in the United States, they are increasingly being detected in a variety of forensic specimens. We present a comprehensive overview of the basic chemistry, pharmacodynamics, and pharmacokinetics of zolpidem, zopiclone, and zaleplon, including their interaction with other prescription drugs and ethanol, findings in drug-facilitated sexual assault (DFSA) casework, and methods of analysis.
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Zolpidem
Forensic Science Medicine and Pathology, 2005Co-Authors: Timothy P. Rohrig, Christine M. MooreAbstract:Zolpidem (Ambien), a Nonbenzodiazepine hypnotic, is indicated for the short-term treatment of insomnia. Because it has become the most widely prescribed sleep aid in the United States, it is being increasingly detected in a variety of forensic specimens, and its interaction with other medications is being questioned. We present a comprehensive overview of the basic chemistry, pharmacokinetics, and pharmacodynamics of zolpidem; its interaction with other prescription drugs; its effects on driving and motor skills; and its analysis and interpretation in forensic casework.
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Zolpidem : Forensic aspects for the toxicologist and pathologist.
Forensic science medicine and pathology, 2005Co-Authors: Timothy P. Rohrig, Christine MooreAbstract:Zolpidem (Ambien), a Nonbenzodiazepine hypnotic, is indicated for the short-term treatment of insomnia. Because it has become the most widely prescribed sleep aid in the United States, it is being increasingly detected in a variety of forensic specimens, and its interaction with other medications is being questioned. We present a comprehensive overview of the basic chemistry, pharmacokinetics, and pharmacodynamics of zolpidem; its interaction with other prescription drugs; its effects on driving and motor skills; and its analysis and interpretation in forensic casework.