• Title/Summary/Keyword: benzodiazepine

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Changes of Renal Peripheral Benzodiazepine Receptor in the Stress/Anxiety Response

  • Ha, Jeoung-Hee;Lee, Kwang-Hun;Cheung, Seung-Douk;Park, Hyung-Bae;Lee, Maan-Gee;Choi, Hyoung-Chul;Sohn, Uy-Dong;Lee, Kwang-Youn;Kim, Won-Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.1 no.5
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    • pp.523-528
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    • 1997
  • Peripheral benzodiazepine receptor(PBR) has been indentified in various peripheral tissues including kidney. The physiological and pharmacological functions of PBR are still uncertain, althought it has been suggested that these are associated with the regulation of stress/anxiety response. Diazepam progeny, which were exposed to diazepam perinatally, was reported to be an animal model of chronic anxiety. However, PBR in the diazepam progenies are not known yet. In the present study, therefore, we examined the changes of PBR in the stress/anxiety response. Dams of rats were given injection of diazepam or vehicle during puerperium. Diazepam progenies showed increased level of anxiety on the performance of elevated plus maze, and increased Bmax of PBR. Saturation experiments followed by scatchard analysis of the results showed that the increase in the density of PBR and the affinity of the PBR remained unchanged. Forced swim stress increased anxiety on the plus maze in both groups of rats. In contrast to control, diazepam progenies did not show further upregulation of renal PBR immediately after swimming stress, but still higher than control. From the above results, it may be concluded that upregulation of renal PBR is associated with chronic anxiety as well as stress-induced response.

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Steroidogenic acute regulatory protein (StAR) and peripheral-type benzodiazepine receptor (PBR) are decreased in human apoptotic embryos

  • Lee, Hyo-Jin;Kim, Jin-Hee;Yang, Hyun-Won
    • Animal cells and systems
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    • v.15 no.3
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    • pp.211-218
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    • 2011
  • Fragmentation in human pre-implantation embryos has been suggested as the process of apoptosis. We have previously demonstrated a direct relationship between the increased reactive oxygen species (ROS) and apoptosis in human pre-implantation embryos. ROS is known to suppress the function of mitochondria in which steroidogenic acute regulatory protein (StAR) and peripheral-type benzodiazepine receptor (PBR) are presented. Therefore, the purpose of this study was to examine the expression of StAR and PBR in human pre-implantation embryos and to evaluate whether reduction of these proteins is associated with apoptosis. Apoptosis was detected by annexin V-fluorescein isothiocyanate (FITC) and mitochondrial membrane potential was measured by 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethyl-benzimidazolyl-carbocyanine iodide (JC-1). Immunofluorescence staining and Western blotting were applied to examine the expression of StAR and PBR in the embryos. Lipid droplets in the embryos were stained with Oil Red O. The fragmented pre-implantation embryos were stained with annexin V-FITC, but not the normal ones. The mitochondria with active membrane potential were present less in the fragmented embryos compared with the non-fragmented embryos. We also confirmed that both StAR and PBR were expressed in the embryos and their expression levels were lower in the fragmented ones. In addition, the number and size of lipid droplets were increased in the fragmented embryos. The present study provides evidence that reduction of StAR and PBR in human pre-implantation embryos is associated with an increase in the lipid droplets leading to apoptosis.

Availability of Toxicologic Screening Tests in the Emergency Department (응급센터에서 시행하는 약물선별현장검사의 유용성)

  • Um, In-Kyung;Park, Jong-Su;Han, Kap-Su;Cho, Han-Jin;Choi, Sung-Hyuck;Lee, Sung-Woo;Hong, Yun-Sik
    • Journal of The Korean Society of Clinical Toxicology
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    • v.9 no.1
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    • pp.26-29
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    • 2011
  • Purpose: The role of a point of care test (POCT) is currently becoming important when treating patients and making decisions in the emergency department. It also plays a role for managing patients presenting with drug intoxication. But the availability of the test has not yet been studied in Korea. Therefore, we investigated the utility and the availability of POCT for drug screening used in the emergency department. Methods: This was a retrospective study for those patients with drug intoxication between January 2007 and December 2010 in an urban emergency department. Results: Between the study period, 543 patients were examined with a Triage$^{(R)}$-TOX Drug Screen. Among those, 248 (45.7%) patients showed negative results and 295 (54.3%) patients showed positive results. The sensitivity of the test for benzodiazepine, acetaminophen and tricyclic antidepressants were 85.9%, 100%, 79.2%, respectively. Conclusion: POCT of drug screening in emergency department showed good accuracy especially in patient with benzodiazepine, acetaminophen and tricyclic antidepressant intoxication. Therefore, it can be useful diagnostic tool for the management of intoxicated patients.

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Silica Sulfuric Acid as a Mild and Efficient Reagent for the Synthesis of 1,4-Diazepine and 1,5-Benzodiazepine Derivatives (Silica Sulfuric Acid를 이용한 효율적인 1,4-diazepine and 1,5-benzodiazepine 유도체의 합성)

  • Joshi, Y.C.;Saingar, Shalini;Kavita, Kavita;Joshi, P.;Kumar, Rajesh
    • Journal of the Korean Chemical Society
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    • v.55 no.4
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    • pp.638-643
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    • 2011
  • The synthesis of biologically active 1H-1,4-diazepines 4a-d and 3H-1,5-benzodiazepines 5a-d in good yields, from the heterocyclization reaction of 2-(4-methylthio benzenesulfonyl)-1,3-dimethyl/1-methyl-3-phenyl/1,3-diphenyl/1-methyl-3-ethoxy propane-1,3-dione 3a-d with ethylenediamine (EDA) and o-phenylenediamine (o-PDA), respectively, in the presence of silica sulfuric acid (SSA) is described. The novel ${\beta}$-diketones/${\beta}$-ketoesters 3a-d were synthesized by the condensation reaction of 4-methylthiobenzenesulfonyl chloride 1 with various ${\beta}$-diketones/${\beta}$-ketoesters 2a-d. All structures of the newly synthesized compounds were elucidated by elemental analysis and spectral studies. The compounds 4a-d and 5a-d have been screened for antimicrobial, antifungal and anthelmintic activity.

Zolpidem Use and Risk of Fracture in Elderly Insomnia Patients

  • Kang, Dong-Yoon;Park, So-Young;Rhee, Chul-Woo;Kim, Ye-Jee;Choi, Nam-Kyong;Lee, Joong-Yub;Park, Byung-Joo
    • Journal of Preventive Medicine and Public Health
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    • v.45 no.4
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    • pp.219-226
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    • 2012
  • Objectives: To evaluate the risk of fractures related with zolpidem in elderly insomnia patients. Methods: Health claims data on the entire South Korean elderly population from January 2005 to June 2006 were extracted from the Health Insurance Review and Assessment Service database. We applied a case-crossover design. Cases were defined as insomnia patients who had a fracture diagnosis. We set the hazard period of 1 day length prior to the fracture date and four control periods of the same length at 5, 10, 15, and 20 weeks prior to the fracture date. Time independent confounding factors such as age, gender, lifestyle, cognitive function level, mobility, socioeconomic status, residential environment, and comorbidity could be controlled using the case-crossover design. Time dependent confounding factors, especially co-medication of patients during the study period, were adjusted by conditional logistic regression analysis. The odds ratios and their 95% confidence intervals (CIs) were estimated for the risk of fracture related to zolpidem. Results: One thousand five hundred and eight cases of fracture were detected in insomnia patients during the study period. In our data, the use of zolpidem increased the risk of fracture significantly (adjusted odds ratio [aOR], 1.72; 95% CI, 1.37 to 2.16). However, the association between benzodiazepine hypnotics and the risk of fracture was not statistically significant (aOR, 1.00; 95% CI, 0.83 to 1.21). Likewise, the results were not statistically significant in stratified analysis with each benzodiazepine generic subgroup. Conclusions: Zolpidem could increase the risk of fracture in elderly insomnia patients. Therefore zolpidem should be prescribed carefully and the elderly should be provided with sufficient patient education.

Characteristics of elderly patients with acute poisoning (노인 중독 환자의 특성)

  • Kim, Bo-Kyeong;Jung, Si-Young;Jung, Koo-Young
    • Journal of The Korean Society of Clinical Toxicology
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    • v.8 no.2
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    • pp.61-68
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    • 2010
  • Purpose: Poisoning is a major health problem for the elderly, and poisoning can cause fatal side effects. However, the characteristics and clinical features of elderly patients with acute poisoning have not been well studied in the previous domestic research. So, we tried to analyze the clinical characteristics and toxic substances of the patients who were 65 years old or older and who were admitted to the regional emergency medical center due to acute poisoning. Methods: We retrospectively reviewed the medical records and poisoning protocols of the patients who were 65 years of age or older and who had with acute poisoning and who visited the ED in our emergency center from January 2005 to December 2009. We collected the demographic information, the gender, the underlying diseases, the causes and toxic substances, the initial presentation, the treatment and the outcomes. Results: A total of 2179 poisoned patients visited the hospital during 5 years, and among them 244 were 65 years of age or older (11.2%). The mean age was $75.6{\pm}6.9$ years and the male:female ratio was 1:1.7. The most common cause of poisoning was suicide (73.4%) and the most common source of poisonous substances was their own drugs. Of the substances used for poisoning, benzodiazepine was the most common drug (25.8%), followed by sedatives other than benzodiazepine (25.4%), insecticide (12.7%), chemical agents (12.3%) and herbicides (8.2%). The most common initial presentation was mental change (64.8%). When comparing the factors between the three elderly groups, there was no difference in gender, the cause, the substances and the underlying disease. The outcomes of treatment included ICU admission (56.1%), a good condition at discharge (12.7%) and admission to a general ward (12.7%). The overall mortality rate was 10.2% for the elderly patients. Conclusion: In this Korean study, unlike the foreign studies, the most common cause of poisoning in elderly patients was intentional poisoning. The admission rate was 68.8% and mortality rate was 10.2%.

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Anti-nociceptive and anti-inflammatory activities of the essential oil isolated from Cupressus arizonica Greene fruits

  • Fakhri, Sajad;Jafarian, Safoora;Majnooni, Mohammad Bagher;Farzaei, Mohammad Hosein;Mohammadi-Noori, Ehsan;Khan, Haroon
    • The Korean Journal of Pain
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    • v.35 no.1
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    • pp.33-42
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    • 2022
  • Background: Cupressus arizonica Greene is a coniferous tree with great importance in fragrance and pharmaceutical industries. Essential oils from C. arizonica (EC) have shown potential antioxidant, and anti-microbial activities. This study aimed at investigating the anti-nociceptive and anti-inflammatory effects/mechanisms of EC. Methods: The EC was evaluated for anti-nociceptive and anti-inflammatory activities on male Wistar rats using a formalin test and carrageenan-induced paw edema, respectively. Also, we pre-treated some of the animals with naloxone and flumazenil in the formalin test to find out the possible contributions of opioid and benzodiazepine receptors to EC anti-nociceptive effects. Finally, gas chromatography/mass spectrometry (GC/MS) analysis was used to identify the EC's constituents. Results: EC in intraperitoneal doses of 0.5 and 1 g/kg significantly decrease the nociceptive responses in both early and late phases of the formalin test. From a mechanistic point of view, flumazenil administration 20 minutes before the most effective dose of EC (1 g/kg) showed a meaningful reduction in the associated anti-nociceptive responses during the early and late phases of the formalin test. Naloxone also reduced the anti-nociceptive role of EC in the late phase. Furthermore, EC at the doses of 1, 0.5, and 0.25 g/kg significantly reduced paw edema from 0.5 hours after carrageenan injection to 4 hours. GC/MS analysis showed that isolated EC is a monoterpene-rich oil with the major presence of α-pinene (71.92%), myrcene (6.37%), δ-3-carene (4.68%), β-pinene (3.71%), and limonene (3.34%). Conclusions: EC showed potent anti-nociceptive and anti-inflammatory activities with the relative involvement of opioid and benzodiazepine receptors.

Characteristics of Intravenous Midazolam Sedation with Nitrous Oxide in Pediatric Dental Treatment (소아환자에서 midazolam 정주 및 아산화질소 흡입진정법 하 치과치료의 특성)

  • Kim, Hyuntae;Song, Ji-Soo;Hyun, Hong-Keun;Kim, Young-Jae;Kim, Jung-Wook;Jang, Ki-Taeg;Lee, Sang-Hoon;Shin, Teo Jeon
    • Journal of the korean academy of Pediatric Dentistry
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    • v.47 no.1
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    • pp.53-61
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    • 2020
  • Midazolam is a short-acting benzodiazepine that is widely used in pediatric dental sedation. However, its clinical effectiveness as an intravenous sedative agent in children has not been widely documented. A retrospective study was conducted to evaluate the efficacy and safety of intravenous midazolam and nitrous oxide inhalation sedation in pediatric dental treatment. The subjects were 115 patients (118 cases) who received dental treatment under intravenous midazolam and nitrous oxide inhalation sedation. Demographic factors, general health status, sedation time, midazolam and nitrous oxide dosage, and success rate of sedation were evaluated from electronic medical records. Behavioral management was the main reason of choosing sedation. Mean duration of sedation was 56.7 minutes for surgical treatment, and 74.4 minutes for restorative treatment. The initial dosage of intravenous midazolam was 0.051 ± 0.019 mg/kg. In 34 cases (28.8%), additional midazolam of 0.036 ± 0.057 mg/kg was delivered during the treatment. The concentration of nitrous oxide was maintained between 40% and 50%. The success rate of sedation was 99% (n = 117). In 1 case, laryngospasm occurred and the patient was reversed with benzodiazepine antagonist, flumazenil. Intravenous midazolam sedation with nitrous oxide was shown to be clinically effective for the dental treatment in children, if administered by trained personnel and patients are carefully selected in accordance with guidelines.

Use of Midazolam Intranasal Spray for Dental Treatment of Autism Patients (자폐증 환자의 행동조절을 위한 Midazolam Intranasal Spray 사용사례)

  • Song, Young-Gyun;Lee, Suk Young;Kim, Seung-Oh
    • Journal of The Korean Dental Society of Anesthesiology
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    • v.12 no.4
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    • pp.223-227
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    • 2012
  • Autism patients in general have bad oral hygiene. It is hard for autism patients to get dental treatment as poor communication. Therefore, they may have to be treated by deep sedation or general anesthesia in numerous cases. However, this process requires induction with mask, so it is not easy to do for disobliging autism patient. Midazolam is a water-soluble benzodiazepine, has been used in pediatric dentistry or dentistry for the handicapped because of rapid onset. Midazolam can be administered through oral, rectal, intramuscular,intravenous, and intranasal (IN) routes. IN route of midazolam may be considered as effective way to allay for uncooperative autism patients before general anesthesia. In this case report, two autism patients required dental treatment. Intranasal spray of midazolam before general anesthesia was safe and effective procedure of behavioral management.

An Acute Postoperative Intractable Hyperventilation after an Endoscopic Third Ventriculostomy

  • Lee, Hae-Mi;Shin, Kyung-Bae;Kim, Seong-Ho;Jee, Dae-Lim
    • Journal of Korean Neurosurgical Society
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    • v.51 no.3
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    • pp.173-176
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    • 2012
  • This report describes a rare case of postoperative hyperventilation attack after an endoscopic third ventriculostomy in a 46-year-old woman. About 60 min after the termination of the operation, an intractable hyperventilation started with respiratory rate of 65 breaths/min and $EtCO_2$, 16.3 mm Hg. Sedation with benzodiazepine, thiopental sodium, fentanyl, and propofol/remifentanil infusion was tried under a rebreathing mask at a 4 L/min of oxygen. With aggressive sedative challenges, ventilation pattern was gradually returned to normal during the 22 hrs of time after the surgery. A central neurogenic hyperventilation was suspected due to the stimulating central respiratory center by cold acidic irrigation solution during the neuroendoscopic procedure.