• 제목/요약/키워드: Barbiturates

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Sleep-Aids Derived from Natural Products

  • Hu, Zhenzhen;Oh, Seikwan;Ha, Tae-Woo;Hong, Jin-Tae;Oh, Ki-Wan
    • Biomolecules & Therapeutics
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    • 제26권4호
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    • pp.343-349
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    • 2018
  • Although drugs such as barbiturates and benzodiazepines are often used for the treatment of insomnia, they are associated with various side effects such as habituations, tolerance and addiction. Alternatively, natural products with minimal unwanted effects have been preferred for the treatment of acute and/or mild insomnia, with additional benefits of overall health-promotion. Basic and clinical researches on the mechanisms of action of natural products have been carried out so far in insomnia treatments. Recent studies have been focusing on diverse chemical components available in natural products, with an interest of developing drugs that can improve sleep duration and quality. In the last 15 years, our co-workers have been actively looking for candidate substances from natural products that can relieve insomnia. This review is, therefore, intended to bring pharmacological data regarding to the effects of natural products on sleep duration and quality, mainly through the activation of $GABA_A$ receptors. It is imperative that phytochemicals will provide useful information during electroencephalography (EEG) analysis and serve as an alternative medications for insomnia patients who are reluctant to use conventional drugs.

Interethnic Variations of CYP2C19 Genetic Polymorphism

  • Tassaneeyakul, Wongwiwat;Tassaneeyakul, Wichittra
    • Toxicological Research
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    • 제17권
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    • pp.145-155
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    • 2001
  • Cytochrome P4502C19 (CYP2C19) is one of human polymorphic xenobiotic-metabolizing enzymes. The enzyme has been reported to catalyze more than 70 substrates, involving more than 100 reactions. These include several classes of therapeutic agents (e.g. anti-microbial. cardiovascular, psycho-active, etc.), sex hormones and insecticides. Associations of the CYP2C19 genotype/phenotype with individual differences in drug efficacy (e.g. diazepam, omeprazole, proguanil) and toxicity (e.g. mephenytoin, barbiturates) have been documented by many investigators. At least 11 allelic variants of CYP2C19 gene were reported to date. Most of the mutant alleles found in the poor metabolizer (PM) led to the production of truncated and/or inactive proteins. Except for the exon 6, single-nucleotide mutations were reported in all nine exons of the gene. Genetic polymorphism of CYP2C19 shows marked interethnic variation with the population frequencies of PM phenotype ranging from 1∼2% up to more than 50%. The prevalence of CYP2C19 PM tends to be higher in Asian and certain Pacific Islanders than other race or ethnic specificity. Genotyping results of CYP2C19 also revealed that there are different proportions of individual mutant alleles among ethnic populations. This may, in part, explains the interethnic difference in the metabolism of certain drugs (i.e. diazepam), though they were from the same CYP2C19 phenotype. Recently, our research group has studied the genotype and phenotype of CYP2C19 and found that the PM frequency (7∼8%) in Thais is lower than other Asian populations. Molecular and clinical impacts of this finding warrant to further investigation.

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Carbamazepine으로 유발된 Bronchiolitis Obliterans Organizing Pneumonia 1예 (A Case of Carbamazepine Induced Bronchiolitis Obliterans Organizing Pneumonia)

  • 옥경선;박봉건;김희숙;이혜경;진성림;진재용;이혁표;김주인;최수전;염호기
    • Tuberculosis and Respiratory Diseases
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    • 제48권5호
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    • pp.794-801
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    • 2000
  • 약제 유발성 BOOP의 경우는 약을 중단하여도 증상과 방사선학적 소견이 호전되지 않을 수 있고 부신피질스테로이드를 사용한 후 뚜렷한 호전을 보일 수 있기 때문에 BOOP를 일으킬 수 있는 약제에 대한 인지가 진단과 치료에 중요하다. 저자들은 carbamazepine에 의한 BOOP 1예를 경험하였기에 보고하는 바이다.

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약물을 이용한 의식진정시 발생한 부작용에 대한 치험례 (CLINICAL STUDY ON THE SIDE EFFECTS OF THE CONSCIOUS SEDATION)

  • 김현식;한국재;이창섭;이상호
    • 대한소아치과학회지
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    • 제24권4호
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    • pp.823-829
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    • 1997
  • The patients visiting pediatric dental office have been being younger than the previous, and they were often combined with systemic disease. But, we aren't able to perform the verbal communication, because of their impediment and youthfullness. And, we can't carry out the behavior control via physical restraint, as the developed social structure and the attitude of children and their parents. So, the importance and concerning of conscious sedation using sedative medicine are increased by time and time. Among the various conscious sedation, Chloral Hydrate and Nitrous Oxide inhalation are most popularly used, and barbiturates, benzodiazepine, opioids and hydroxyzine are used often. But, these medications have some side-effects and adverse reactions, may be failed to sedate the children. And limited use of medically compromised patients, especially for ASA class III, IV or more dangerous patients. We, the Department of Pediatric Dentistry, Chosun University have met some dangerous situation due to unfavorable pharmacogenic reactions, but we can control the situation and get well healed results. The below results are common situations and their solutions during conscious sedation. 1. By the intravenous administration, thrombophlebitis is the most common side-effects, but it may be healed with time without any special treatment. 2. Under the definitive guidelines about conscious-sedation, we can perform a safe conscious sedation for ASA class III patients. 3. When adversed reaction of Benzodiazepine is occured, it could be cared effectively with benzodiazepine antagonist, named Flumazenil.

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음주운전자 275명 혈액 중 마약류 및 남용약물의 분석 (Distribution of Abused Drugs in 275 Alcohol-positive Blood Samples of Korean Driver)

  • 최혜영;이주선;최상길;김은미;김재균;김영운;임미애;정희선
    • 약학회지
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    • 제52권2호
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    • pp.137-146
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    • 2008
  • Even though driving under the influence of drug (DUID) is a worldwide problem, we, Korea has no regulation system yet except for alcohol, and there are little cases reported related to DUID. In order to investigate the type of abused drugs for drivers in Korea, we tried to analyze controlled and non-controlled drugs in alcohol-positive blood samples. 275 whole bloods, which were positive for alcohol on the roadside test, were collected from the police for two months ($Nov.{\sim}Dec.$ 2006). The analytical strategy was constituted of three steps: First, alcohol in blood samples were confirmed and quantified by gas chromatography. Second, controlled drugs were screened by $Evidence_{investigator}\;^{TM}$ (Randox, U.K.) as preliminary test. It was based on immunoassay by biochip array analyzer. Nine groups of drug abuse were screened: amphetamines, methamphetamines, cannabis, cocaine, opiates, barbiturates, methadone, benzodiazepines I (oxazepam) & II (lorazepam). Finally, confirmation of these drugs was performed by GC-MS. Blood samples were extracted by solid-phase extraction by $RapidTrace^{TM}$ (Zymark, U.S.A.). After trimethylsilyl (TMS) derivatization, eluates were analyzed to GC-MS. Total 49 drugs were investigated in this study including controlled drugs, antidepressants, 1st generation antihistamines, dextromethorphan, nalbuphine, ketamine, etc. For rapid detection, we developed the automated identification system. It was made up a new software, "DrugMan", modified Chemstation data analysis menu and newly developed macro modules. A series of peak selection, identification and reporting of the results were performed automatically by this system. Concentrations of alcohol in 275 blood samples were ranged from 0.011 to 0.249% (average, 0.119%). Among 149 blood samples, just six samples (4.0%) were showed positive results to the immunoassay: one methamphetamine and five benzodiazepines group I. By GC-MS confirmation, only benzodiazepines were detected and methamphetamine was not detected from immunoassay positive blood sample. Besides these drugs, 5 chlorpheniramines, dextromethorphan, diazepam, doxylamine, ibuprofen, lidocaine and topiramate were also detected in whole bloods by GC-MS. Conclusively, the frequency of drug abuse for Korean drivers was relatively low. There was none case which illegal drug was detected. However these results were limited to alcohol positive blood samples, so it is necessary to analyze more samples including alcohol negative blood.

백서에서 동통에 미치는 Phenobarbital 효과의 재평가 (Reevaluation of the Effect of Phenobarbital on the Response to Pain in Rat)

  • 소병겸;김기원;고명규;양원모;조규박
    • 대한약리학회지
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    • 제22권2호
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    • pp.88-95
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    • 1986
  • 백서에서 열판법을 이용하여 과민동통을 일으키는 약물로 알려진 phenobarbital의 동통에 대한 효과를 재검토하고 그 기전을 알고저 phenobarbital 단기 또는 장기처리에 의한 뇌내 ${\beta}-endorphin$함량, opiate 수용체 및 시험관내 실험으로 functional opiate 수용체의 변동유무를 검토하여 다음과 같은 결과를 얻었다. 1) 마취에 미달하는 용량의 phenobarbital 1회 복강내 투여는 일시적인 HPL단축에 이어 이를 지연시켰고 phenobarbital 장기 처리는 HPL을 현저히 지연시켰다. 2) Naloxone 자체는 HPL을 현저히 단축시켰고, naloxone처리는 phenobarbital의 HPL 지연 효과를 억제하였다. 3) Phenobarbital 1회 복강내 투여는 뇌내 ${\beta}-endorphin$ 함량에 영향을 미치지 못하였으나 phenobarbital 장기처리는 이를 현저히 증가시켰다. 4) Phenobarbital 1회 복강내 투여는 [3H]-morphine binding에 영향을 미치지 못하였으나, phenobarbital 장기처리는 Kd치와는 달리 Bmax를 현저히 감소시켰다. 5) Phenobarbital 장기처리에 의한 HPL변동, 뇌내 ${\beta}-endorphin$함량변동 그리고 opiate receptor Bmax변동 삼자간에는 유의한 상관관계가 있었다. 6) 적출vas deferens 표본에서 phenobarbital 장기처리는 morphine의 ID50은 증가시키고 maximum effect는 감소시키나 naloxone에 대한 $pA_2 $치에는 영향을 미치지 못하였다. 이상의 실험성적은 phenobarbital이 일시적인 과민동통 효과에 이어 진통효과를 갖고 있으며, phenobarbital의 진통효과는 뇌내 ${\beta}-endorphin$함량 증가와 이로 인한 functional opiate 수용체의 숫적 변동에 기인함을 시사하였다.

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