• 생약학회지
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• 제30권2호
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• pp.211-215
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• 1999

This study was aimed to evaluate an agonistic activity to benzodiazepine receptor of several medicinal plants, which have been used as sedatives in oriental medicine. Methanol extracts of medicinal plants which were used in this study inhibited the binding of $[^3H]Ro15-1788$, a selective benzodiazepine receptor antagonist to benzodiazepine receptor of rat cortices. Inhibitory activity of Cyperus rotundus was observed to be the highest among the tested medicinal plants. Methanol extracts of Cyperus rotundus and Zizypus jujuba inhibited a $[^3H]flunitrazepam$, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of $[3H]flunitrazepam$ binding by Cyperus rotundus and Zizypus jujuba, and these positive GABA shifts supported the strong possibility of agonistic activity to benzodiazepine receptor. From these results, it may be concluded that the substance or substances with neurochemical properties characteristic of a benzodiazepine receptor agonist may be important components and contribute to the sedative property of these medicinal plants.

• 수면정신생리
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• 제6권1호
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• pp.5-18
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• 1999

A growing number of people are concerned about their sleep. There are many people with chronic sleep disorders. Sedativehypnotics including benzodiazepine and non-benzodiazepine have been widely used in chronic insomniacs. It is widely accepted that current hypnotics are efficient in alleviating subjective symptoms of insomnia. Non-benzodiazepine hypnotics include zolpidem, zopiclone, and melatonin. These novel non-benzodiazepine hypnotics that have efficacy comparable to benzodiazepines were developed with more understanding of benzodiazepine receptor pharmacology. Their unique pharmacologic profiles may offer few significant advantages in terms of adverse effects of benzodiazepines. However, most of hypnotics including non-benzodiazepine have some of dependence, tolerance, impaired daytime function and rebound insomnia. Currently, it is accepted that combination therapy with pharmacologic and behavioral intervention is the most effective for chronic insomniacs.

• 대한불안의학회지
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• 제1권1호
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• pp.25-30
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• 2005

In the 40 years since the first benzodiazepine was brought into clinical use there has been a substantial growth in understanding the molecular basis of action of these drugs and the role of their receptors in anxiety disorders. Benzodiazepine receptors are present throughout the brain with the highest concentration in cortex, and it potentiate and prolong the synaptic action of the inhibitory neurotransmitter GABA. Central benzodiazepine receptors and $GABA_A$ receptors are part of the same macromolecular complex. Abnormalities of these $GABA_A$-benzodiazepine receptors as a result of drug challenge tests and neuroimaging studies may underlie some anxiety disorders. The role of $GABA_A$-benzodiazepine receptors in the action of benzodiazepine and as a factor in anxiety disorder, in both animal and humans including knock-out and knock in technique, may lead to new anxiolytics that have potentially significant therapeutic gains without unwanted side effects.

• 생약학회지
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• 제30권3호
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• pp.284-289
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• 1999

In order to find active ingradients having an agonistic activity to benzodiazepine receptor from Gastrodia elata Blume (Orchidaceae) which has been used as an anticonvulsant in oriental medicine, one component and some fractions were separated from the butanol extract of the rhizomes of this plant and evaluated for their activities on GABA/benzodiazepine receptor in vitro. As a result, one crude mixture (F4f) obtained from the most active fraction (F4) inhibited significantly the binding of $[^3H]Ro15-1788$, a selective benzodiazepine receptor antagonist, to benzodiazepine receptor of rat cortices. GABA significantly enhanced the inhibition of $[^3H]flunitrazepam$ binding by F4f, and this positive GABA shift supported the strong possibility of the agonistic activity of F4f to benzodiazepine receptor.

• 생명과학회지
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• 제10권4호
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• pp.374-379
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• 2000

This study was attempted to evaluate an agonistic activity to benzodiazepine receptor of several medicinal pants, which have been used as sedatives in oriental medicine. The activities of the methanol extracts of composite preparation of oriental drugs were compared with those of the simple drugs, furthermore, the active fraction was found out from the simple preparation. Inhibitory effects of composite preparations, Cyperus rotundus/Acorus gramineus, Thuja orientalis/Euphoria longan, Thuja orientalis/Albizzia julibrissin, on the binding of ${[^3H]}$Ro15-1788, a selective benszodiazepine receptor antagonist to benzodiazepine receptor of rat cortices, were observed to be lower than those of corresponding simple preparations. These unexpected results suggest that some components of the composite druge may rather act as an obstacle, not to show the sinergistic effect. The methanol extracts of Cyperus rotundus having the highest activity were fractionated using polar and nonpolar solvents to give ethylacetate and hexane fractions, respectively. The ethylacetate fraction containing relatively polar components exhibited much higher activity than the hexane fraction, which consiste of nonpolar agonist, binding to benzodiazepine receptor. However, in the presence of GABA, this fraction inhibited ${[^3H]}$flunitrazepan binding, and these positive GABA shift supported the strong possibility of agonistic activity to benzodiazepine receptro. As a result, it may be concluded that the substance or substances with neurochemical properties as a benzodiazepine receptor agonist may contribute to the sedative property of Cyperus rotundus.

• 대한임상독성학회지
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• 제6권1호
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• pp.45-48
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• 2008

A 57-year-old man was transferred to our emergency department with decreased mental status after organophosphate intoxication. He had a four year history of benzodiazepine and hypnotic medication use for chronic insomnia and a depressive mood disorder. He had no previous history of seizures, diabetes mellitus, and hypertension. By hospital day 5, the patient was noted to be awake and to have repetitive jerking movements involving the left upper extremity, and appeared apathetic, depressed and less responsive to external stimuli. A benzodiazepine withdrawal syndrome was subsequently apparent when he developed several generalized tonic clonic seizures and status epilepticus. Using a continuous midazolam intravenous infusion, we successfully controlled the refractory seizure without complications. We present a rare case of status epilepticus from a benzodiazepine withdrawal that developed during the treatment for organophosphate intoxication.

• Biomolecules & Therapeutics
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• 제5권4호
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• pp.325-330
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• 1997

Methanol extract of G. elata inhibited the binding of [/sup 3/H]Rol5-1788, a selective benzodiazepine receptor antagonest, to benzodiazepine receptor of rat cortices. Saturation experiments followed by Scatchard analysis of the results showed that the inhibition of [sub 3/H]Ro15-1788 binding by G. dlata. appeared to be com-petitive. These competitive inhibiton of the butanol fraction was observed to be higher than the methanol extract. Methanol extract of G. efara inhibited a [sub 3/H]flunitrazepam, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of [/sub 3/H]flunitrazepam binding by G. elata, and these "positive GABA shift" supported the strong possibility of agonestic activity to benzodiazepine receptor Butanol fraction was observed to be higher than crude extract by methanol in an agonistic activity to benzodiazepine receptor, furthermore enhanced the binding of [sub 3/H]SR95531 to GABA receptor. Butanol fraction of G. elata significantly diminished the pentylenetetrazole-induced lethality of mice. From these results, it can be concluded that substance or substances with neurochemical properties characteri- stic of a benzodiazepine receptor agonist may be important components, and contribute to the anticonvulsant property of G. elata.

• 대한불안의학회지
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• 제11권2호
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• pp.143-148
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• 2015

Objective : This study examined benzodiazepine prescription patterns of outpatients visiting the psychiatry department in a single general hospital in Korea. Methods : A retrospective descriptive analysis of benzodiazepine prescriptions was performed on a database from 2014 in a general hospital in Korea. We analyzed the following factors of adult outpatients: demographic factors such as sex and age, amount of benzodiazepine prescribed, treatment duration, and diagnosis based on the ICD-10. Results : In 2014, benzodiazepines were prescribed to 46.4% of the outpatients. Percentage of benzodiazepine prescription increased with age and was highest in the age group 40-59 years. Prescription was more prevalent in women and the prescription percentage increased by treatment duration. Patients with the F4 diagnosis (neurotic, stress-related and somatoform disorders) were the most highly prescribed group. For all diagnosis groups, prescription was more prevalent in females or similar for both sexes except for patients with F5 diagnosis (behavioral syndromes associated with physiological disturbances and physical factors), with males being more predominant. Conclusion : Despite the concern regarding the rate of benzodiazepine prescription and administration to geriatric patients, long-term prescription and usage among older patients is still prevalent.

• 동의신경정신과학회지
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• 제15권1호
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• pp.77-86
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• 2004

Objective : This study was performed to investigate the agonistic activity of Chunmajeongal-tang extract to the $GABA_A/benzodiazepine$ receptor complex. Methods : Male mice and Sprague-Dawley rats were used for this experiment. Chunmajeongal-tang Prescription was extracted with 80% methanol, evaporated in vacuo and dried with freeze dryer. The agonistic activity to the GABA/ benzodiazepine receptor complex and GABA transaminase activity were measured in vitro. Results : Chunmajeongal-tang extract inhibited dose-dependently the binding of [3H]Ro15-1788, an antagonist on GABA/benzodiazepine receptor complex, in rat cerebral cortices, showing $82.4{\pm}4.12%$ inhibition at a dose of 5.0 mg/kg. This extract inhibited dose-dependently the binding of [3H]flunitrazepam, an agonist on GABA/benzodiazepine receptor complex, in rat cerebral cortices, showing $5.6{\pm}1.24%$ inhibition. Furthermore, Chunmajeongal-tang extract inhibited the binding of [3H]flunitrazepam in the presence of GABA/NaCI with $13.2{\pm}0.44%$ inhibition, its inhibitory effect exhibited a positive GABA shift, which means that this extract activates a GABAergic neurotransmission.

• 약학회지
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• 제57권2호
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• pp.101-109
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• 2013

Depressive disorders are the most common psychiatric problem in the elderly. Most depression treatment guidelines emphasize treatment with antidepressant medication and recommend that benzodiazepine use be minimized for limited period, particularly to elderly patients. In order to evaluate appropriate use of antidepressants and benzodiazepine, retrospective review of prescriptions was performed. The study population are older than 65 years who had been newly diagnosed with major depressive disorder in specialty mental health at a community general hospital from January $1^{st}$, 2007 to October $31^{th}$, 2012 (N=373). Initial antidepressant accounted for 89.5% with SSRI, and escitalopram accounted for 60.9% of SSRI group. 79% or more of the patients were prescribed the recommended dosage. The maintenance rate for 4 weeks of initial antidepressant was 48% and 6 weeks was 39%. Treatment-discontinuation rate was 68% at 3 month. Alprazolam (short acting benzodiazepine) was prescribed the most, followed by clonazepam (long acting benzodiazepine) and then diazepam. 55% of patients received a duplicated prescription for short acting plus long acting benzodiazepine. 61% of patients used long acting benzodiazepines. Prescribed dosages of benzodiazepines were commonly within a recommended range, while no one was prescribed a appropriate period (up to 2 weeks) except for the early discontinued patients. Appropriate use of zolpidem was only 16.2%. The depressed elderly treated in specialty mental health mostly received long-term treatment with benzodiazepines in combination with antidepressants, guideline recommendations was not followed. Multidisciplinary interventions like audit and feedback of benzodiazepine use are needed and education for the elderly is needed to properly maintain antidepressant treatment.