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Sample records for barbiturates

  1. [On the history of barbiturates].

    Science.gov (United States)

    Norn, Svend; Permin, Henrik; Kruse, Edith; Kruse, Poul R

    2015-01-01

    Throughout the history of humanity, numerous therapeutic agents have been employed for their sedative and hypnotic properties such as opium, henbane (Hyoscyamus niger) and deadly nightshade (Atropa belladonna), but also alcohol and wine. In the 19th century potassium bromide was introduced as a sedative - and antiepileptic drug and chloral hydrate as sedative-hypnotics. A new era was reached by the introduction of barbiturates. The story started with the chemist Adolf von Baeyer. His breakthrough in the synthesis of new agents as barbituric acid and indigo and his education of young chemists was of great importance for the science of organic chemistry and the development of the dye and medicine industry in the late 19th century. The next important step was the development of barbiturates. The pioneers were Josef von Mering and Emil Fischer. Using the Grimaux-method they synthesized various barbiturates. It was von Mering who got the idea of introducing ethyl groups in the inactive barbituric acid to obtain sedatives, but the synthesis was succeeded by the chemist Emil Fischer. Experiments with dogs clearly showed sedative and hypnotic effect of the barbiturates and the oral administration of barbital (Veronal) confirmed the effect in humans. Barbital was commercialized in 1903 and in 1911 phenobarbital (Luminal) was introduced in the clinic, and this drug showed hypnotic and antiepileptic effects. Thereafter a lot of new barbiturates appeared. Dangerous properties of the drugs were recognized as abuse, addiction, and poisoning. An optimum treatment of acute barbiturate intoxication was obtained by the "Scandinavian method", which was developed in the Poison Centre of the Bispebjerg Hospital in Copenhagen. The centre was established by Carl Clemmesen in 1949 and the intensive care treatment reduced the mortality of the admitted persons from 20% to less than 2%. To-day only a few barbiturates are used in connection with anaesthesia and for the treatment of epilepsy

  2. Extracorporeal treatment for barbiturate poisoning

    DEFF Research Database (Denmark)

    Mactier, Robert; Laliberté, Martin; Mardini, Joelle;

    2014-01-01

    The EXTRIP (Extracorporeal Treatments in Poisoning) Workgroup conducted a systematic review of barbiturate poisoning using a standardized evidence-based process to provide recommendations on the use of extracorporeal treatment (ECTR) in patients with barbiturate poisoning. The authors reviewed all...... articles, extracted data, summarized key findings, and proposed structured voting statements following a predetermined format. A 2-round modified Delphi method was used to reach a consensus on voting statements, and the RAND/UCLA Appropriateness Method was used to quantify disagreement. 617 articles met...... depression necessitating mechanical ventilation, shock, persistent toxicity, or increasing or persistently elevated serum barbiturate concentrations despite treatment with multiple-dose activated charcoal. (3) Intermittent hemodialysis is the preferred mode of ECTR, and multiple-dose activated charcoal...

  3. Barbiturates for acute traumatic brain injury.

    OpenAIRE

    Roberts, I.; Sydenham, E

    2012-01-01

    BACKGROUND: Raised intracranial pressure (ICP) is an important complication of severe brain injury, and is associated with high mortality. Barbiturates are believed to reduce ICP by suppressing cerebral metabolism, thus reducing cerebral metabolic demands and cerebral blood volume. However, barbiturates also reduce blood pressure and may, therefore, adversely effect cerebral perfusion pressure. OBJECTIVES: To assess the effects of barbiturates in reducing mortality, disability and raised ICP ...

  4. Application of thermoresponsive HPLC to forensic toxicology: determination of barbiturates in human urine

    OpenAIRE

    Kanno, Sanae; Watanabe, Kanako; HIRANO, SEISHIRO; Yamagishi, Itaru; Gonmori, Kunio; Minakata, Kayoko; Suzuki, Osamu

    2009-01-01

    A high-performance liquid chromatography (HPLC) method has been developed for the assays of five barbiturates in human urine using a new thermoresponsive polymer separation column, which is composed of N-isopropylacrylamide polymer. According to elevating the column temperature from 10 ℃ to 50 ℃, five barbiturates, such as metharbital, primidone, phenobarbital, mephobarbital and pentobarbital, became well separated by this method. Five barbiturates showed good linearity in the range of 0.2-10...

  5. PPL catalyzed four-component PASE synthesis of 5-monosubstituted barbiturates: Structure and pharmacological properties.

    Science.gov (United States)

    Bihani, Manisha; Bora, Pranjal P; Verma, Alakesh K; Baruah, Reshita; Boruah, Hari Prasanna Deka; Bez, Ghanashyam

    2015-12-15

    Enzymatic four-component reactions are very rare although three-component enzymatic promiscuous reactions are widely reported. Herein, we report an efficient PASE protocol for the synthesis of potentially lipophilic zwitterionic 5-monosubstituted barbiturates by four component reaction of mixture of ethyl acetoacetate, hydrazine hydrate, aldehyde and barbituric acid in ethanol at room temperature. Seven different lipases were screened for their promiscuous activity towards the synthesis of 5-monosubstituted barbiturates and the lipase from porcine pancreas (PPL) found to give optimum efficiency. The zwitterionic 5-monosubstituted barbiturates with pyrazolyl ring showed promising pharmacological activity upon screening for antibacterial and apoptotic properties.

  6. Molecular modeling-based antioxidant arylidene barbiturates as urease inhibitors.

    Science.gov (United States)

    Khan, Khalid Mohammed; Ali, Muhammad; Wadood, Abdul; Zaheer-ul-Haq; Khan, Momin; Lodhi, Muhammad Arif; Perveen, Shahnaz; Choudhary, Muhammad Iqbal; Voelter, Wolfgang

    2011-09-01

    Previously we have reported arylidene barbiturates 1-18 as a novel class of antioxidants; however, their urease inhibitory potential has not yet been explored. In this communication, molecular docking studies were used to predict the potential ligands from compounds 1-18 which culminated in the identification of certain new urease inhibitors. Ligands were screened in vitro for their urease inhibitory potential. Compound 1, as deduced from modeling studies, was found to be the most active urease inhibitor (13.0 ± 1.2 μM), when compared with the standard thiourea (IC₅₀=21.1 ± 0.3 μM). All of the compounds were found to be nontoxic to Artemia salina in brine shrimp lethality bioassay.

  7. Supramolecular assemblies and molecular recognition of amphiphilic schiff bases with barbituric acid in organized molecular films.

    Science.gov (United States)

    Jiao, Tifeng; Liu, Minghua

    2005-02-24

    A bolaform Schiff base, N,N'-bis(salicylidene)-1,10-decanediamine (BSC10), has been synthesized and its interfacial hydrogen bond formation or molecular recognition with barbituric acid was investigated in comparison with that of a single chain Schiff base, 2-hydroxybenzaldehyde-octadecylamine (HBOA). It has been found that while HBOA formed a monolayer at the air/water interface, the bolaform Schiff base formed a multilayer film with ordered layer structure on water surface. When the Schiff bases were spread on the subphase containing barbituric acid, both of the Schiff bases could form hydrogen bonds with barbituric acid in situ in the spreading films. As a result, an increase of the molecular areas in the isotherms was observed. The in situ H-bonded films could be transferred onto solid substrates, and the transferred multilayer films were characterized by various methods such as UV-vis and FT-IR spectrosopies. Spectral changes were observed for the films deposited from the barbituric acid subphase, which supported the hydrogen bond formation between the Schiff bases and barbituric acid. By measuring the MS-TOF of the deposited films dissolved in CHCl3 solution, it was concluded that a 2:1 complex of HBOA with barbituric acid and a 1:2 complex of BSC10 with barbituric acid were formed. On the other hand, when the multilayer films of both Schiff bases were immersed in an aqueous solution of barbituric acid, a similar molecular recognition through the hydrogen bond occurred. A clear conformational change of the alkyl spacer in the bolaform Schiff base was observed during the complex formation with the barbituric acid.

  8. New method for spectrophotometric determination of quinones and barbituric acid through their reaction. A kinetic study

    Science.gov (United States)

    Medien, H. A. A.

    1996-11-01

    A new and sensitive spectrophotometric method is described for the determination of p-benzoquinone, p-chloranil and 1.4-naphthoquinone. The method is based on the reaction between quinones and barbituric acid, by which a color is developed with maximum absorption between 485 and 555 nm in 50% methyl alcohol-water mixture. The absorption of the product obeys Beer's law within the concentration range 0.025-05 mM of orginal quinone. The kinetics of the reaction between p-benzoquinone and barbituric acid was studied in a range of methyl alcohol-water mixtures. The reaction follows overall second order kinetics, first order in each of the reactants. The rate increases with increasing dielectric constant. The method was applied for determination of barbituric acid with p-benzoquinone in the concentration range of 0.025-0.345 mM. Other barbiturates do not interfere.

  9. Barbiturate bearing aroylhydrazine derivatives: Synthesis, NMR investigations, single crystal X-ray studies and biological activity

    Science.gov (United States)

    Giziroglu, Emrah; Sarikurkcu, Cengiz; Aygün, Muhittin; Basbulbul, Gamze; Soyleyici, H. Can; Firinci, Erkan; Kirkan, Bulent; Alkis, Ayse; Saylica, Tayfur; Biyik, Halil

    2016-03-01

    A series of barbituric acid aroylhydrazine derivatives have been prepared from their corresponding 1,3-dimethyl-5-acetyl barbituric acid and aroylhydrazines. All compounds have been fully characterized by using FT-IR, multinuclear NMR (1H, 13C) and Mass (MS) spectrometry. We also describe the X-ray crystal structure of 3a, which crystallizes in the monoclinic P21/n space group. The crystal structure is stabilized with infinite linear chains of dimeric units. Furthermore, all compounds were investigated for their tyrosinase inhibition, antioxidative and antimicrobial activies. The results from biological activity assays have shown that all of compounds have excellent antioxidant, significant tyrosinase inhibition and moderate antimicrobial activity.

  10. Effect of Cross-linking Agent on Barbituric Acid-initiated Resin

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    To improve the tensile bond strength of dentin bonding agents, the adhesion between dentin and MMA resin was investigated by applying initiator systems containing 1-cyclohexyl-5-ethyl barbituric acid (CEB), copper acetyl acetonate (CAA), quaternary ammonium chloride (QAC), cupric ion, with the addition of TEGDMA, and pretreatment solution for dentin, and an HEMA primer. The effects of a cross-linking agent on barbituric acid-initiated dentin bonding resin were examined by measuring degree of conversion, molecular weight, hardness of bonding resin, and tensile bond strengths.

  11. Recognition of anesthetic barbiturates by a protein binding site: a high resolution structural analysis.

    Directory of Open Access Journals (Sweden)

    Simon Oakley

    Full Text Available Barbiturates potentiate GABA actions at the GABA(A receptor and act as central nervous system depressants that can induce effects ranging from sedation to general anesthesia. No structural information has been available about how barbiturates are recognized by their protein targets. For this reason, we tested whether these drugs were able to bind specifically to horse spleen apoferritin, a model protein that has previously been shown to bind many anesthetic agents with affinities that are closely correlated with anesthetic potency. Thiopental, pentobarbital, and phenobarbital were all found to bind to apoferritin with affinities ranging from 10-500 µM, approximately matching the concentrations required to produce anesthetic and GABAergic responses. X-ray crystal structures were determined for the complexes of apoferritin with thiopental and pentobarbital at resolutions of 1.9 and 2.0 Å, respectively. These structures reveal that the barbiturates bind to a cavity in the apoferritin shell that also binds haloalkanes, halogenated ethers, and propofol. Unlike these other general anesthetics, however, which rely entirely upon van der Waals interactions and the hydrophobic effect for recognition, the barbiturates are recognized in the apoferritin site using a mixture of both polar and nonpolar interactions. These results suggest that any protein binding site that is able to recognize and respond to the chemically and structurally diverse set of compounds used as general anesthetics is likely to include a versatile mixture of both polar and hydrophobic elements.

  12. Supramolecular chiral host-guest nanoarchitecture induced by the selective assembly of barbituric acid derivative enantiomers

    Science.gov (United States)

    Sun, Xiaonan; Silly, Fabien; Maurel, Francois; Dong, Changzhi

    2016-10-01

    Barbituric acid derivatives are prochiral molecules, i.e. they are chiral upon adsorption on surfaces. Scanning tunneling microscopy reveals that barbituric acid derivatives self-assemble into a chiral guest-host supramolecular architecture at the solid-liquid interface on graphite. The host nanoarchitecture has a sophisticated wavy shape pattern and paired guest molecules are nested insides the cavities of the host structure. Each unit cell of the host structure is composed of both enantiomers with a ratio of 1:1. Furthermore, the wavy patterns of the nanoarchitecture are formed from alternative appearance of left- and right-handed chiral building blocks, which makes the network heterochiral. The functional guest-host nanoarchitecture is the result of two-dimensional chiral amplification from single enantiomers to organizational heterochiral supramolecular self-assembly.

  13. Synthesis and mechanism of formation of oxadeazaflavines by microwave thermal cyclization of ortho-halobenzylidene barbiturates

    Energy Technology Data Exchange (ETDEWEB)

    Figueroa-Villar, J. Daniel; Oliveira, Sandra C.G. de, E-mail: figueroa@ime.eb.br [Grupo de Quimica Medicinal, Departamento de Quimica, Instituto Militar de Engenharia, Rio de Janeiro, RJ (Brazil)

    2011-09-15

    The thermal cyclization reaction of o-halobenzylidene barbiturates was developed as an efficient and simple method for the preparation of oxadeazaflavines. The use of solid state reaction conditions with microwave irradiation afforded the products in 5 min with 47 to 98% yield. Experimental synthetic results and thermogravimetric reaction analyses agree with the molecular modeling mechanism simulation, indicating that this reaction occurs through an intramolecular hetero-Diels-Alder cyclization followed by fast re-aromatization. (author)

  14. Allyl m-Trifluoromethyldiazirine Mephobarbital: An Unusually Potent Enantioselective and Photoreactive Barbiturate General Anesthetic

    Energy Technology Data Exchange (ETDEWEB)

    Savechenkov, Pavel Y.; Zhang, Xi; Chiara, David C.; Stewart, Deirdre S.; Ge, Rile; Zhou, Xiaojuan; Raines, Douglas E.; Cohen, Jonathan B.; Forman, Stuart A.; Miller, Keith W.; Bruzik, Karol S. (Harvard-Med); (Mass. Gen. Hosp.); (UIC)

    2012-12-10

    We synthesized 5-allyl-1-methyl-5-(m-trifluoromethyl-diazirynylphenyl)barbituric acid (14), a trifluoromethyldiazirine-containing derivative of general anesthetic mephobarbital, separated the racemic mixture into enantiomers by chiral chromatography, and determined the configuration of the (+)-enantiomer as S by X-ray crystallography. Additionally, we obtained the {sup 3}H-labeled ligand with high specific radioactivity. R-(-)-14 is an order of magnitude more potent than the most potent clinically used barbiturate, thiopental, and its general anesthetic EC{sub 50} approaches those for propofol and etomidate, whereas S-(+)-14 is 10-fold less potent. Furthermore, at concentrations close to its anesthetic potency, R-(-)-14 both potentiated GABA-induced currents and increased the affinity for the agonist muscimol in human {alpha}1{beta}2/3{gamma}2L GABA{sub A} receptors. Finally, R-(-)-14 was found to be an exceptionally efficient photolabeling reagent, incorporating into both {alpha}1 and {beta}3 subunits of human {alpha}1{beta}3 GABAA receptors. These results indicate R-(-)-14 is a functional general anesthetic that is well-suited for identifying barbiturate binding sites on Cys-loop receptors.

  15. Multi-Component synthesis and computational studies of three novel thio-barbituric acid carbohydrate derivatives

    Science.gov (United States)

    Gupta, Stuti; Khare, Naveen K.

    2017-01-01

    The thio-barbituric acid is convenient starting compound for the preparation of fused heterocycles and its 5-substituted derivatives which are pharmacologically one of the most important classes of compounds. The fused compounds of thio-barbituric acid, 4-(1R,2S,3S,4S)-1,2,3,4,5-tetrahydroxy pentyl-10-phenyl-1,3,6,8,9,10 hexahydro-2,7-dithiooxopyrido [2,3-d; 6,5'] dipyrimidine-4,5 diones (1), 4-(1S,2S,3S,4S)-1,2,3,4,5-tetrahydroxy pentyl-10-phenyl-1,3,6,8,9,10 hexahydro-2,7-dithiooxopyrido [2,3-d; 6,5'] dipyrimidine-4,5 diones (2), 3-(1R,2S,3S)-1,2,3,4-tetrahydroxy butyl-10-phenyl-1,3,6,8,9,10 hexahydro-2,7-dithiooxopyrido [2,3-d; 6,5'] dipyrimidine-4,5 diones (3) have been synthesized in single step by the condensation of thio-barbituric acid with sugars (L-rhamnose, L-fucose and L-arabinose) & aniline using para-toluene sulfonic acid (p-TSA) as an effective acid catalyst under refluxing conditions. The molecular structure and detailed spectroscopic analysis of all three novel synthesized thiones derivatives have been performed using experimental techniques like 1H, 13C NMR, 2D (COSY, HSQC, DEPT-135 and DEPT-90) as well as theoretical calculations by density functional theory (DFT) using B3LYP and 6-311G + (d, p) basis set. The strength and nature of weak intramolecular interactions have been studied by atom in molecule (AIM) approach. Global reactivity descriptors have been computed to predict reactivity and reactive sites in the molecule.

  16. A Greener, Efficient Approach to Michael Addition of Barbituric Acid to Nitroalkene in Aqueous Diethylamine Medium

    Directory of Open Access Journals (Sweden)

    Hany J. Al-Najjar

    2014-01-01

    Full Text Available An efficient method for the synthesis of a variety of pyrimidine derivatives 3a–t by reaction of barbituric acids 1a,b as Michael donor with nitroalkenes 2a–k as Michael acceptor using an aqueous medium and diethylamine is described. This 1,4-addition strategy offers several advantages, such as using an economic and environmentally benign reaction media, high yields, versatility, and shorter reaction times. The synthesized compounds were identified by 1H-NMR, 13C-NMR, CHN, IR, and MS. The structure of compound 3a was further confirmed by single crystal X-ray structure determination.

  17. Low risk of development of substance dependence for barbiturates and clobazam prescribed as antiepileptic drugs: results from a questionnaire study.

    Science.gov (United States)

    Uhlmann, Carmen; Fröscher, Walter

    2009-01-01

    There is no systematical research about the topic of dependence on antiepileptic drugs (AED) for patients with epilepsy, despite the fact that barbiturates and benzodiazepines comprise a potential risk of dependence. We hypothesize that there is no psychological substance dependence for patients with epilepsy, possibly because of their outcome expectations. The aim of the study was to examine these patients in terms of substance dependence. One hundred inpatients at the Lake Constance Epilepsy Center were asked about their experiences with AED in terms of dependence in a structured interview. We registered general statements about dependence of AED, markers for substance dependence, and outcome expectations. About 50% of the patients reported withdrawal symptoms and the development of tolerance, but less than 10% noticed loss of control and craving. Withdrawal symptoms and development of tolerance were significantly lower in a group of patients without barbiturates or clobazam versus patients with barbiturates or/and clobazam. There was no significant difference between these two groups in psychological criteria of dependence, that is, loss of control and craving. Outcome expectations of AED were clearly related to the efficacy against seizures, and only to a small amount to psychotropic effects. The study demonstrates that physiological variables of dependence are present more in patients with epilepsy with a permanent intake of barbiturates or clobazam, but psychological variables of dependence are rarely present in epileptic patients, with or without an intake of barbiturates and clobazam. These results confirm our hypothesis that substance dependence is not a major problem in benzodiazepines and barbiturates in patients with epilepsy. Outcome expectations seem to be related mainly to the anticonvulsant and not the psychotropic effect. This might be the reason for the absence of dependence.

  18. Nuclear magnetic resonance and molecular modeling study of exocyclic carbon-carbon double bond polarization in benzylidene barbiturates

    Science.gov (United States)

    Figueroa-Villar, J. Daniel; Vieira, Andreia A.

    2013-02-01

    Benzylidene barbiturates are important materials for the synthesis of heterocyclic compounds with potential for the development of new drugs. The reactivity of benzylidene barbiturates is mainly controlled by their exocyclic carbon-carbon double bond. In this work, the exocyclic double bond polarization was estimated experimentally by NMR and correlated with the Hammett σ values of the aromatic ring substituents and the molecular modeling calculated atomic charge difference. It is demonstrated that carbon chemical shift differences and NBO charge differences can be used to predict their reactivity.

  19. Synthesis, characterization, thermal behaviour and single crystal X-ray analysis of two new insensitive high energy density materials [8-hydroxyquinolinium 5-(2,4,6-trinitrophenyl)barbiturate (I) and 8-hydroxyquinolinium 5-(5-chloro-2,4-dinitrophenyl)-1,3-dimethyl barbiturate (II)

    Science.gov (United States)

    Manickkam, V.; Devi, P. Poornima; Kalaivani, D.

    2014-12-01

    Barbiturates I and II have been synthesized as maroon red and red orange coloured solids by mixing the ethanolic solutions of 2-chloro-1,3,5-trinitrobenzene ( TNCB), pyrimidine-2,4,6(1 H,3 H,5 H)-trione [barbituric acid ( BA)] and 8-hydroxyquinoline and 1,3-dichloro-4,6-dinitrobenzene ( DCDNB), 1,3-dimethylpyrimidine-2,4,6(1 H,3 H,5 H)-trione(1,3-dimethylbarbituric acid) and 8-hydroxyquinoline respectively. The structures of these two barbiturates have been predicted from the spectral studies (UV-VIS, IR, 1H NMR, 13C NMR, mass) and elemental analysis. Qualitative tests have been carried out to infer the presence of nitrogen and nitro groups and also chlorine atom in barbiturate II. Slow evaporation of ethanol-dimethylsulphoxide/ethanol solutions of barbiturate I/barbiturate II at 293 K yielded good for X-Ray diffraction crystals. Single crystal X-ray diffraction studies of the crystals further confirm the putative structures of the barbiturates. The asymmetric unit of the barbiturate I comprises of 8-hydroxyquinolinium cation, 5-(2,4,6-trinitrophenyl) barbiturate anion and a molecule of dimethylsulphoxide (DMSO), which is used as a recrystallizing solvent. It crystallizes in the triclinic system with space group (centrosymmetric). Barbiturate II crystallizes in the orthorhombic system with space group P212121 (non-centrosymmetric). Barbiturates I and II are stable towards an impact sensitivity test, when a weight of 2 kg mass hammer is dropped from a height of 160 cm of the instrument. TGA/ DTA analyses at four different heating rates (5, 10, 20, and 40 K/min) imply that they undergo exothermic decomposition (˜85%) in three different stages between 273 and 873 K. Activation energies for these decomposition processes have been calculated by employing Kissinger and Ozawa plots. Impact sensitivity test and activation energies have revealed that the titled barbiturates are insensitive high energy density materials ( IHEDMS).

  20. Barbiturate ingestion in three adult captive tigers (Panthera tigris and concomitant fatal botulism of one : clinical communication

    Directory of Open Access Journals (Sweden)

    J. H. Williams

    2011-05-01

    Full Text Available Zoo animals, including tigers, have been reported to suffer from barbiturate intoxication, with pentabarbitone being most commonly recorded. Clinical signs range from mild ataxia to general anaesthesia with recovery over hours to days with several factors affecting hepatic barbiturate metabolism and tissue partitioning. Botulism is an often fatal intoxication in man, animals, birds and certain fish. The occurrence in carnivores is uncommon to rare, with only 2 reports found of botulism in felids. This report relates to 3 adult captive cohabiting tigers that simultaneously developed signs of abdominal discomfort, progressive ataxia, recumbency and comatose sleep resembling stage 2 anaesthesia, alternating with periods of distracted wakefulness and ataxic movements. These signs occurred 4 days after being fed the carcass of a horse that had ostensibly died of colic and not been euthanased. The male tiger that was the dominant animal in the feeding hierarchy was worst affected and had to be given intravenous fluids. The female that was lowest in hierarchy was unaffected. After 48-72 hours of treatment at the Onderstepoort Veterinary Academic Hospital the females could eat and made an uneventful recovery. The male tiger showed partial recovery but died during the night a few hours after drinking water on his return to the owner. Necropsy revealed severe oesophageal dilation and impaction with decaying grass; some of this material and water were present in the pharynx and trachea, and had been aspirated causing acute widespread bronchopneumonia. Colon content tested negative for common pesticides but, together with liver, tested positive for barbiturate. Serum taken on the day of admission had tested negative for barbiturate and the residual serum from the 3 animals later tested negative for botulinum toxin. Colon and oesophageal content from the male at necropsy were positive for Clostridium botulinum toxin type C by the mouse bioassay

  1. Nucleobase-Based Barbiturates: Their Protective Effect against DNA Damage Induced by Bleomycin-Iron, Antioxidant, and Lymphocyte Transformation Assay

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    Bhaveshkumar D. Dhorajiya

    2014-01-01

    Full Text Available A number of nucleobase-based barbiturates have been synthesized by combination of nucleic acid bases and heterocyclic amines and barbituric acid derivatives through green and efficient multicomponent route and one pot reaction. This approach was accomplished efficiently using aqueous medium to give the corresponding products in high yield. The newly synthesized compounds were characterized by spectral analysis (FT-IR, 1H NMR, 13C NMR, HMBC, and UV spectroscopy and elemental analysis. Representative of all synthesized compounds was tested and evaluated for antioxidant, bleomycin-dependent DNA damage, and Lymphocyte Transformation studies. Compounds TBC > TBA > TBG showed highest lymphocyte transformation assay, TBC > TBA > BG showed inhibitory antioxidant activity using ABTS methods, and TBC > BPA > BAMT > TBA > 1, 3-TBA manifested the best protective effect against DNA damage induced by bleomycin.

  2. Piracetam and TRH analogues antagonise inhibition by barbiturates, diazepam, melatonin and galanin of human erythrocyte D-glucose transport

    OpenAIRE

    2004-01-01

    Nootropic drugs increase glucose uptake into anaesthetised brain and into Alzheimer's diseased brain. Thyrotropin-releasing hormone, TRH, which has a chemical structure similar to nootropics increases cerebellar uptake of glucose in murine rolling ataxia. This paper shows that nootropic drugs like piracetam (2-oxo 1 pyrrolidine acetamide) and levetiracetam and neuropeptides like TRH antagonise the inhibition of glucose transport by barbiturates, diazepam, melatonin and endogenous neuropeptide...

  3. Behaviour of Some Activated Nitriles Toward Barbituric Acid, Thiobarbituric Acid and 3-Methyl-1-Phenylpyrazol-5-one

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    M. M. Habashy

    2000-05-01

    Full Text Available The effect of some active methylene containing heterocyclic compounds, namely barbituric acid, thiobarbituric acid and 3-methyl-1-phenylpyrazol-5-one on a-cyano-3,4,5-trimethoxycinnamonitrile and ethyl a-cyano-3,4,5-trimethoxycinnamate (1a,b was investigated. The structure of the new products was substantiated by their IR,1H-NMR and mass spectra.

  4. Theoretical Studies on Electronic Spectra and Second-order Nonlinear Optical Properties of Barbituric Acid Derivatives Substituted with Schiff Base

    Institute of Scientific and Technical Information of China (English)

    SUN,Gang(孙刚); QIU,Yong-Qing(仇永清); SUN,Hai-Zhu(孙海珠); SU,Zhong-Min(苏忠民); FENG,Jing-Dong(冯静东); ZHU,Yu-Lan(朱玉兰)

    2004-01-01

    The structures of barbituric acid derivatives substituted with Schiff base were optimized using ab initio HF method at 6-31G basis set.Based on the optimized structures,the electronic spectra were obtained by INDO/CI method.The second-order nonlinear optical (NLO) coefficients βu were calculated according to the sum-over-states (SOS) formula.In addition,the effect of conjugation on electronic spectra and second-order NLO coefficients was investigated.The influence of exchange between C and N atoms as well as the substituted effect on the barbituric acid was discussed.It was indicated that the exchange between C and N atoms on Schiff base is important for enhancing the NLO coefficient of the whole molecule with donor and acceptor (D-A).Meanwhile significant changes in electron donation and acception were observed as substituents changes positions.Among the designed models,molecule 1b has maximal βμ value of 124.65 × 10-30 esu.About molecule 1b,barbituric acid is considered as an accepted electronic group and the position of N atom on Schiff base is close to it.

  5. Evolution of Cerebral Atrophy in a Patient with Super Refractory Status Epilepticus Treated with Barbiturate Coma

    Science.gov (United States)

    George, Pravin; Nattanmai, Premkumar; Ahrens, Christine; Hantus, Stephen; Sarwal, Aarti

    2017-01-01

    Introduction. Status epilepticus is associated with neuronal breakdown. Radiological sequelae of status epilepticus include diffusion weighted abnormalities and T2/FLAIR cortical hyperintensities corresponding to the epileptogenic cortex. However, progressive generalized cerebral atrophy from status epilepticus is underrecognized and may be related to neuronal death. We present here a case of diffuse cerebral atrophy that developed during the course of super refractory status epilepticus management despite prolonged barbiturate coma. Methods. Case report and review of the literature. Case. A 19-year-old male with a prior history of epilepsy presented with focal clonic seizures. His seizures were refractory to multiple anticonvulsants and eventually required pentobarbital coma for 62 days and midazolam coma for 33 days. Serial brain magnetic resonance imaging (MRI) showed development of cerebral atrophy at 31 days after admission to our facility and progression of the atrophy at 136 days after admission. Conclusion. This case highlights the development and progression of generalized cerebral atrophy in super refractory status epilepticus. The cerebral atrophy was noticeable at 31 days after admission at our facility which emphasizes the urgency of definitive treatment in patients who present with super refractory status epilepticus. Further research into direct effects of therapeutic coma is warranted. PMID:28182114

  6. Evolution of Cerebral Atrophy in a Patient with Super Refractory Status Epilepticus Treated with Barbiturate Coma

    Directory of Open Access Journals (Sweden)

    Christopher R. Newey

    2017-01-01

    Full Text Available Introduction. Status epilepticus is associated with neuronal breakdown. Radiological sequelae of status epilepticus include diffusion weighted abnormalities and T2/FLAIR cortical hyperintensities corresponding to the epileptogenic cortex. However, progressive generalized cerebral atrophy from status epilepticus is underrecognized and may be related to neuronal death. We present here a case of diffuse cerebral atrophy that developed during the course of super refractory status epilepticus management despite prolonged barbiturate coma. Methods. Case report and review of the literature. Case. A 19-year-old male with a prior history of epilepsy presented with focal clonic seizures. His seizures were refractory to multiple anticonvulsants and eventually required pentobarbital coma for 62 days and midazolam coma for 33 days. Serial brain magnetic resonance imaging (MRI showed development of cerebral atrophy at 31 days after admission to our facility and progression of the atrophy at 136 days after admission. Conclusion. This case highlights the development and progression of generalized cerebral atrophy in super refractory status epilepticus. The cerebral atrophy was noticeable at 31 days after admission at our facility which emphasizes the urgency of definitive treatment in patients who present with super refractory status epilepticus. Further research into direct effects of therapeutic coma is warranted.

  7. Chemical microenvironment mediated formation of organicnanostructures from self-assembly of melamine and barbituric acid derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHUANG; Jiaqi; (庄家骐); WANG; Gang; (王刚); Lü; Nan; (吕男); YANG; Wensheng; (杨文胜); JIANG; Yueshun; (姜月顺); LI; Tiejin; (李铁津)

    2002-01-01

    The recent progresses on constructing organic nanostructures from the self-assembly of melamine and barbituric acid derivatives are reviewed. By mediating the chemical microenvironment during the self-assembly, the information contained in the molecular components can be expressed at different levels, thus resulting in the formation of different organic nanostructures. When the assembly is carried out in anhydrous chloroform, a kind of asymmetric layered structure with a d value of 4.1 nm is obtained. When a little amount of polar solvent such as alcohol is contained in the chloroform, organic nanotubes with diameter of 6 nm and length of several hundreds of nanometers are observed. After being treated by appropriate polar solvents, the nanotubes are induced into supercoils with diameter of about 300 nm and length of several tens of microns. The sensitivity of the self-assembly process origins from the weak noncovalent intermolecular interactions between the molecular components. The enthalpy change of such interactions is pretty small, so slight change of the molecular structure or microenvironment could affect the primary equilibrium, resulting in the rearrangement and transformation of the supramolecular structure.

  8. Anti-inflammatory effects of novel barbituric acid derivatives in T lymphocytes.

    Science.gov (United States)

    Xu, Chenjia; Wyman, Arlene R; Alaamery, Manal A; Argueta, Shannon A; Ivey, F Douglas; Meyers, John A; Lerner, Adam; Burdo, Tricia H; Connolly, Timothy; Hoffman, Charles S; Chiles, Thomas C

    2016-09-01

    We have used a high throughput small molecule screen, using a fission yeast-based assay, to identify novel phosphodiesterase 7 (PDE7) inhibitors. One of the most effective hit compounds was BC12, a barbituric acid-based molecule that exhibits unusually potent immunosuppressive and immunomodulatory actions on T lymphocyte function, including inhibition of T cell proliferation and IL-2 cytokine production. BC12 treatment confers a >95% inhibition of IL-2 secretion in phytohaemagglutinin (PHA) plus phorbol-12-myristate-13-acetate (PMA) stimulated Jurkat T cells. The effect of BC12 on IL-2 secretion is not due to decreased cell viability; rather, BC12 blocks up-regulation of IL-2 transcription in activated T cells. BC12 also inhibits IL-2 secretion in human peripheral T lymphocytes stimulated in response to CD3/CD28 co-ligation or the combination of PMA and ionomycin, as well as the proliferation of primary murine T cells stimulated with PMA and ionomycin. A BC12 analog that lacks PDE7 inhibitory activity (BC12-4) displays similar biological activity, suggesting that BC12 does not act via PDE7 inhibition. To investigate the mechanism of inhibition of IL-2 production by BC12, we performed microarray analyses using unstimulated and stimulated Jurkat T cells in the presence or absence of BC12 or BC12-4. Our studies show these compounds affect the transcriptional response to stimulation and act via one or more shared targets to produce both anti-inflammatory and pro-stress effects. These results demonstrate potent immunomodulatory activity for BC12 and BC12-4 in T lymphocytes and suggest a potential clinical use as an immunotherapeutic to treat T lymphocyte-mediated diseases.

  9. Influence of hypothermia, barbiturate therapy, and intracranial pressure monitoring on morbidity and mortality after near-drowning.

    Science.gov (United States)

    Bohn, D J; Biggar, W D; Smith, C R; Conn, A W; Barker, G A

    1986-06-01

    We retrospectively evaluated the clinical and pathologic effects of hypothermia and high-dose barbiturate therapy on hypoxic/ischemic cerebral injury after near-drowning in children. Of 40 near-drowned patients admitted to the ICU, 13 died, seven had permanent cerebral damage, and 20 survived. Twenty-four patients (group 1) were treated with a regime of hyperventilation, hypothermia, and high-dose phenobarbitone while intracranial pressure (ICP) was continuously monitored. Of ten who died in this group, three were diagnosed as having cerebral death shortly after admission; autopsy revealed severe cerebral edema with herniation. The remaining seven nonsurvivors had severe cerebral hypoxia without raised ICP and had the features of severe adult respiratory distress syndrome and hypoxic/ischemic damage to other organs. Six of these seven patients developed septicemia which was invariably associated with a profound neutropenia. Sixteen patients (group 2) were treated with a similar protocol but without hypothermia. Three of these patients died but only one developed septicemia. Neutropenia after resuscitation from near-drowning seemed to indicate a poor prognosis; the mean polymorphonuclear leukocyte count in nonsurvivors (1.9 +/- 0.5 X 10(9) cell/L) was significantly (p less than .01) lower than that in survivors (6.4 +/- 1.1 X 10(9) cell/L). Hypothermia was associated with a decreased number of circulating PMNs but did not increase the number of neurologically intact survivors. Similarly, although barbiturates may control ICP, their use did not improve outcome. Because severe cerebral edema and herniation after near-drowning is usually associated with irreversible brain damage, measures to control brain swelling such as hypothermia and barbiturates will be of little benefit.(ABSTRACT TRUNCATED AT 250 WORDS)

  10. Synthesis of New Azo Dyes and Copper(II) Complexes Derived from Barbituric Acid and 4-Aminobenzoylhydrazone

    OpenAIRE

    GUP, Bülent KIRKAN and Ramazan

    2008-01-01

    Four new azo dyes, L1, L2, L3, and L4, were prepared by linking benzaldehyde p-aminobenzoylhydrazone (3) and p-hydroxybenzaldehyede p--aminobenzoylhydrazone (4) to barbituric acid and 1,3-dimethylbarbituric acid through diazo-coupling reactions. Reactions of the azo-dyes with copper chloride and bidentate ligand, 1,10-phenanthroline, produced mixed-ligand dinuclear complexes with general stoichiometry [Cu2L(phen)2]Cl2 (7, 8, 9, and 10). The structures of both azo dyes and their compl...

  11. Synthesis of barbituric acid containing nucleotides and their implications for the origin of primitive informational polymers.

    Science.gov (United States)

    Mungi, Chaitanya V; Singh, Sachin Kumar; Chugh, Jeetender; Rajamani, Sudha

    2016-07-27

    Given that all processes in modern biology are encoded and orchestrated by polymers, the origin of informational molecules had to be a crucial and significant step in the origin of life on Earth. An important molecule in this context is RNA that is thought to have allowed the transition from chemistry to biology. However, the RNA molecule is comprised of intramolecular bonds which are prone to hydrolysis, especially so under the harsh conditions of the early Earth. Furthermore, the formation of nucleotides with extant bases and their subsequent polymerization have both been problematic, to say the least. Alternate heterocycles, in contrast, have resulted in nucleosides in higher yields, suggesting a viable and prebiotically relevant solution to the longstanding "nucleoside problem". In the present study, we have synthesized a nucleotide using ribose 5'-monophosphate (rMP) and barbituric acid (BA), as the base analog, using dry-heating conditions that are thought to be prevalent in several regimes of the early Earth. Polymerization of the resultant monomers, i.e. BA-nucleotides, was also observed when dehydration-rehydration cycles were carried out at low pH and high temperature. The resulting RNA-like oligomers have intact bases unlike in reactions that were carried out with canonical nucleotides, which resulted in abasic sites under acidic conditions due to cleavage of the N-glycosidic linkages. Furthermore, the incorporation of BA directly into preformed sugar-phosphate backbones was also observed when rMP oligomers were subjected to heating with BA. The results from our aforementioned experiments provide preliminary evidence that BA could have been a putative precursor of modern nucleobases, which could have been incorporated into primitive informational polymers that predated the molecules of an RNA world. Moreover, they also highlight that the prebiotic soup, which would have been replete with alternate heterocycles, could have allowed the sampling of other

  12. Synthesis and Evaluation of Changes Induced by Solvent and Substituent in Electronic Absorption Spectra of New Azo Disperse Dyes Containig Barbiturate Ring

    Directory of Open Access Journals (Sweden)

    Hooshang Hamidian

    2013-01-01

    Full Text Available Six azo disperse dyes were prepared by diazotizing 4-amino hippuric acid and coupled with barbituric acid and 2-thiobarbituric acid. Then, the products were reacted with aromatic aldehyde, sodium acetate, and acetic anhydride, and oxazolone derivatives were formed. Characterization of the dyes was carried out by using UV-Vis, FT-IR, 1H NMR and 13C NMR, and mass spectroscopic techniques. The solvatochromic behavior of azo disperse dyes was evaluated in various solvents. The effects of substituents of aromatic aldehyde, barbiturate, and thiobarbiturate ring on the color of dyes were investigated.

  13. Reliability of self-reported use of amphetamine, barbiturates, benzodiazepines, cannabinoids, cocaine, methadone, and opiates among acutely hospitalized elderly medical patients

    DEFF Research Database (Denmark)

    Glintborg, B.; Olsen, L.; Poulsen, H.

    2008-01-01

    Undisclosed use of illicit drugs and prescription controlled substances is frequent in some settings. The aim of the present study was to estimate the reliability of self-reported use of amphetamine, barbiturates, benzodiazepines, cannabinoids, cocaine, methadone, and opiates among acutely...

  14. Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives

    Directory of Open Access Journals (Sweden)

    Assem Barakat

    2016-01-01

    Full Text Available A series of barbiturates derivatives synthesized and screened for different set of bioassays are described. The molecular structures of compounds 5a, 5d, and 5f were solved by single-crystal X-ray diffraction techniques. The results of bioassay show that compounds 4a, 4b, 4c, 4d, 4e, 4f, and 4g are potent antioxidants in comparison to the tested standards, butylated hydroxytoluene (BHT, and N-acetylcysteine. Compounds 4a–4e (IC50=101.8±0.8–124.4±4.4 μM and 4g (IC50=104.1±1.9 μM were more potent antioxidants than the standard (BHT, IC50=128.8±2.1 μM. The enzyme inhibition potential of these compounds was also evaluated, in vitro, against thymidine phosphorylase, α-glucosidase, and β-glucuronidase enzymes. Compounds 4c, 4h, 4o, 4p, 4q, 5f, and 5m were found to be potent α-glucosidase inhibitors and showed more activity than the standard drug acarbose, whereas compounds 4v, and 5h were found to be potent thymidine phosphorylase inhibitors, more active than the standard drug, 7-deazaxanthine. All barbiturates derivatives (4a–4x, 4z, and 5a–5m were found to be noncytotoxic against human prostate (PC-3, Henrietta Lacks cervical (HeLa and Michigan Cancer Foundation-7 breast (MCF-7 cancer cell lines, and 3T3 normal fibroblast cell line, except 4y which was cytotoxic against all the cell lines.

  15. Synthesis and Evaluation of Changes Induced by Solvent and Substituent in Electronic Absorption Spectra of New Azo Disperse Dyes Containig Barbiturate Ring

    OpenAIRE

    2013-01-01

    Six azo disperse dyes were prepared by diazotizing 4-amino hippuric acid and coupled with barbituric acid and 2-thiobarbituric acid. Then, the products were reacted with aromatic aldehyde, sodium acetate, and acetic anhydride, and oxazolone derivatives were formed. Characterization of the dyes was carried out by using UV-Vis, FT-IR, 1H NMR and 13C NMR, and mass spectroscopic techniques. The solvatochromic behavior of azo disperse dyes was evaluated in various solvents. The effects of substitu...

  16. Knoevenagel condensation of α,β-unsaturated aromatic aldehydes with barbituric acid under non-catalytic and solvent-free conditions

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    An efficient route for the synthesis of 5-(arylpropenylidine)-2,4,6-pyrimidinetrione 3 from an appropriate α,β-unsaturated aromatic aldehydes 1 and barbituric acid 2 under both non-catalytic and solvent-free microwave irradiation conditions was described. In this way, a range of biologically important compounds 3 was obtained in good to excellent yields (86-98 %) in a very short reaction time (30-80 s).

  17. Intermediates of Krebs cycle correct the depression of the whole body oxygen consumption and lethal cooling in barbiturate poisoning in rat.

    Science.gov (United States)

    Ivnitsky, Jury Ju; Schäfer, Timur V; Malakhovsky, Vladimir N; Rejniuk, Vladimir L

    2004-10-01

    Rats poisoned with one LD50 of thiopental or amytal are shown to increase oxygen consumption when intraperitoneally given sucinate, malate, citrate, alpha-ketoglutarate, dimethylsuccinate or glutamate (the Krebs cycle intermediates or their precursors) but not when given glucose, pyruvate, acetate, benzoate or nicotinate (energy substrates of other metabolic stages etc). Survival was increased with succinate or malate from control groups, which ranged from 30-83% to 87-100%. These effects were unrelated to respiratory depression or hypoxia as judged by little or no effect of succinate on ventilation indices and by the lack of effect of oxygen administration. Body cooling of comatose rats at ambient temperature approximately 19 degrees C became slower with succinate, the rate of cooling correlated well with oxygen consumption decrease. Succinate had no potency to modify oxygen consumption and body temperature in intact rats. A condition for antidote effect of the Krebs intermediate was sufficiently high dosage (5 mmol/kg), further dose increase made no odds. Repeated dosing of succinate had more marked protective effect, than a single one, to oxygen consumption and tended to promote the attenuation of lethal effect of barbiturates. These data suggest that suppression of whole body oxygen consumption with barbiturate overdose could be an important contributor to both body cooling and mortality. Intermediates of Krebs cycle, not only succinate, may have a pronounced therapeutic effect under the proper treatment regimen. Availability of Krebs cycle intermediates may be a limiting factor for the whole body oxygen consumption in barbiturate coma, its role in brain needs further elucidation.

  18. Molecular structure and spectroscopic investigations combined with hypoglycemic/anticancer and docking studies of a new barbituric acid derivative

    Science.gov (United States)

    Barakat, Assem; Soliman, Saied M.; Elshaier, Yaseen A. M. M.; Ali, M.; Al-Majid, Abdullah Mohammed; Ghabbour, Hazem A.

    2017-04-01

    The one-pot synthesis reaction of barbituric acid derivative, 1,3-cyclohexandione, and 4-fluorobenzaldehyde in water mediated by NHEt2 as base afforded 4 with excellent yield. The synthesized compound was characterized by spectrophotometric tools as well as X-ray single crystal diffraction technique. The stability of the nine possible isomers of the synthesized compound was studied using the B3LYP method and 6-31G(d,p) basis set. The electronic and spectroscopic properties of the most stable isomer were predicted. The UV-Vis absorption spectrum displayed two bands at 203 and 257 nm in the solvent chloroform. The latter was calculated at 235.6 nm (f = 0.1995) in the gas phase due to H-2→L (42%) and H-1→L+2 (14%) excitations. In solution, using chloroform as a solvent, a slight bathochromic shift to 237.6 nm with an increase in the absorption intensity (f = 0.2898) was predicted. The molecular orbital energy level diagram of this transition band was characterized mainly by π-π* transitions. The 13C and 1H NMR chemical shifts correlated well with the experimental data. The correlations had higher correlation coefficients (R2) when solvent effects were considered. The atomic charges were calculated using natural population analysis and the charged regions were presented using a molecular electrostatic potential (MEP) map. The synthesized compound was examined as a hypoglycemic agent via inhibition of α-glucosidase and β-glucuronidase enzymes. Its inhibitory activity against α-glucosidase was 10 times greater than the inhibitory activity of the standard drug acarbose (IC50 77.9 ± 0.3 μM and 840 ± 1.73 μM, respectively). Moreover, the target compound was evaluated for anticancer activity against MCF-7, H460, 3T3, and Hela cell lines. It demonstrated inhibitory activity against the MCF-7 and H460 cell lines with IC50 5.80 ± 0.12 and 19.6 ± 0.5 μM, respectively, in comparison to doxorubicin. The docking study was performed using the OpenEye program.

  19. 3D-QSAR Studies on Barbituric Acid Derivatives as Urease Inhibitors and the Effect of Charges on the Quality of a Model.

    Science.gov (United States)

    Ul-Haq, Zaheer; Ashraf, Sajda; Al-Majid, Abdullah Mohammed; Barakat, Assem

    2016-04-30

    Urease enzyme (EC 3.5.1.5) has been determined as a virulence factor in pathogenic microorganisms that are accountable for the development of different diseases in humans and animals. In continuance of our earlier study on the helicobacter pylori urease inhibition by barbituric acid derivatives, 3D-QSAR (three dimensional quantitative structural activity relationship) advance studies were performed by Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) methods. Different partial charges were calculated to examine their consequences on the predictive ability of the developed models. The finest developed model for CoMFA and CoMSIA were achieved by using MMFF94 charges. The developed CoMFA model gives significant results with cross-validation (q²) value of 0.597 and correlation coefficients (r²) of 0.897. Moreover, five different fields i.e., steric, electrostatic, and hydrophobic, H-bond acceptor and H-bond donors were used to produce a CoMSIA model, with q² and r² of 0.602 and 0.98, respectively. The generated models were further validated by using an external test set. Both models display good predictive power with r²pred ≥ 0.8. The analysis of obtained CoMFA and CoMSIA contour maps provided detailed insight for the promising modification of the barbituric acid derivatives with an enhanced biological activity.

  20. 3D-QSAR Studies on Barbituric Acid Derivatives as Urease Inhibitors and the Effect of Charges on the Quality of a Model

    Directory of Open Access Journals (Sweden)

    Zaheer Ul-Haq

    2016-04-01

    Full Text Available Urease enzyme (EC 3.5.1.5 has been determined as a virulence factor in pathogenic microorganisms that are accountable for the development of different diseases in humans and animals. In continuance of our earlier study on the helicobacter pylori urease inhibition by barbituric acid derivatives, 3D-QSAR (three dimensional quantitative structural activity relationship advance studies were performed by Comparative Molecular Field Analysis (CoMFA and Comparative Molecular Similarity Indices Analysis (CoMSIA methods. Different partial charges were calculated to examine their consequences on the predictive ability of the developed models. The finest developed model for CoMFA and CoMSIA were achieved by using MMFF94 charges. The developed CoMFA model gives significant results with cross-validation (q2 value of 0.597 and correlation coefficients (r2 of 0.897. Moreover, five different fields i.e., steric, electrostatic, and hydrophobic, H-bond acceptor and H-bond donors were used to produce a CoMSIA model, with q2 and r2 of 0.602 and 0.98, respectively. The generated models were further validated by using an external test set. Both models display good predictive power with r2pred ≥ 0.8. The analysis of obtained CoMFA and CoMSIA contour maps provided detailed insight for the promising modification of the barbituric acid derivatives with an enhanced biological activity.

  1. Daily isoflurane exposure increases barbiturate insensitivity in medullary respiratory and cortical neurons via expression of ε-subunit containing GABA ARs.

    Directory of Open Access Journals (Sweden)

    Keith B Hengen

    Full Text Available The parameters governing GABAA receptor subtype expression patterns are not well understood, although significant shifts in subunit expression may support key physiological events. For example, the respiratory control network in pregnant rats becomes relatively insensitive to barbiturates due to increased expression of ε-subunit-containing GABAARs in the ventral respiratory column. We hypothesized that this plasticity may be a compensatory response to a chronic increase in inhibitory tone caused by increased central neurosteroid levels. Thus, we tested whether increased inhibitory tone was sufficient to induce ε-subunit upregulation on respiratory and cortical neurons in adult rats. Chronic intermittent increases in inhibitory tone in male and female rats was induced via daily 5-min exposures to 3% isoflurane. After 7d of treatment, phrenic burst frequency was less sensitive to barbiturate in isoflurane-treated male and female rats in vivo. Neurons in the ventral respiratory group and cortex were less sensitive to pentobarbital in vitro following 7d and 30d of intermittent isoflurane-exposure in both male and female rats. The pentobarbital insensitivity in 7d isoflurane-treated rats was reversible after another 7d. We hypothesize that increased inhibitory tone in the respiratory control network and cortex causes a compensatory increase in ε-subunit-containing GABAARs.

  2. {sup 1} H and {sup 13} C NMR studies on the enoling of 5-benzyl barbituric acids; Estudos por H-1 e C-13 RMN da enolizacao de acidos 5-benzil barbituricos

    Energy Technology Data Exchange (ETDEWEB)

    Villar, Jose Daniel Figueroa; Santos, Nedina Lucia dos; Cruz, Elizabete Rangel [Instituto Militar de Engenharia (IME), Rio de Janeiro, RJ (Brazil). Secao de Quimica

    1991-12-31

    This work shows that the derivatives of the 5-benzyl barbituric acids hydroxylated at the ortho position of the aromatic ring only exist in the enol form. and that the alkylation of this hydroxyl gives products which exist mainly in the ketone form of the DMSO 5 refs., 2 figs., 2 tabs.

  3. Interactions between non-barbiturate injectable anesthetics and conventional antiepileptic drugs in the maximal electroshock test in mice--an isobolographic analysis.

    Science.gov (United States)

    Borowicz, Kinga K; Łuszczki, Jarogniew; Czuczwar, Stanisław J

    2004-03-01

    The aim of this study was the isobolographic evaluation of interactions between three non-barbiturate intravenous anesthetics and conventional antiepileptic drugs in the maximal electroshock-induced seizures in mice. Electroconvulsions were produced by means of an alternating current (ear-clip electrodes, 0.2-s stimulus duration, tonic hindlimb extension taken as the endpoint). Adverse effects were evaluated in the chimney test (motor performance) and passive avoidance task (long-term memory). Plasma levels of antiepileptic drugs were measured by immunofluorescence. Obtained results indicate that ketamine acts synergistically with valproate and carbamazepine. Also the combinations of propofol and valproate or phenobarbital led to synergistic interactions. An antagonism was found between etomidate and carbamazepine or phenobarbital. On the other hand, interactions between diphenylhydantoin and injectable anesthetics proved to be additive. The only exception was the combination of diphenylhydantoin and propofol (1:3). Pharmacokinetic phenomena do not seem to interfere with the observed interactions, since none of anesthetics influenced the free plasma concentrations of antiepileptic drugs. Referring to undesired effects, only propofol impaired long-term memory. Although propofol did not disturbed motor coordination, it enhanced motor impairment caused by carbamazepine and diphenylhydantoin. Results of the present study suggest that etomidate needs to be avoided in epileptic patients due to a possibility of negative interactions with some antiepileptic drugs and seizure precipitation.

  4. A new synthetic methodology for the preparation of biocompatible and organo-soluble barbituric- and thiobarbituric acid based chitosan derivatives for biomedical applications

    Energy Technology Data Exchange (ETDEWEB)

    Shahzad, Sohail [Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000 (Pakistan); Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100 (Pakistan); Shahzadi, Lubna [Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000 (Pakistan); Mahmood, Nasir [Department of Allied Health Sciences and Chemical Pathology, Department of Human Genetics and Molecular Biology, University of Health Sciences, Lahore (Pakistan); Siddiqi, Saadat Anwar [Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000 (Pakistan); Rauf, Abdul [Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100 (Pakistan); Manzoor, Faisal; Chaudhry, Aqif Anwar [Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000 (Pakistan); Rehman, Ihtesham ur [Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000 (Pakistan); Department of Materials Science and Engineering, The Kroto Research Institute, The University of Sheffield, North Campus, Broad Lane, Sheffield, S3 7HQ (United Kingdom); Yar, Muhammad, E-mail: drmyar@ciitlahore.edu.pk [Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000 (Pakistan)

    2016-09-01

    Chitosan's poor solubility especially in organic solvents limits its use with other organo-soluble polymers; however such combinations are highly required to tailor their properties for specific biomedical applications. This paper describes the development of a new synthetic methodology for the synthesis of organo-soluble chitosan derivatives. These derivatives were synthesized from chitosan (CS), triethyl orthoformate and barbituric or thiobarbituric acid in the presence of 2-butannol. The chemical interactions and new functional motifs in the synthesized CS derivatives were evaluated by FTIR, DSC/TGA, UV/VIS, XRD and {sup 1}H NMR spectroscopy. A cytotoxicity investigation for these materials was performed by cell culture method using VERO cell line and all the synthesized derivatives were found to be non-toxic. The solubility analysis showed that these derivatives were readily soluble in organic solvents including DMSO and DMF. Their potential to use with organo-soluble commercially available polymers was exploited by electrospinning; the synthesized derivatives in combination with polycaprolactone delivered nanofibrous membranes. - Highlights: • Development of a new synthetic methodology • Synthesis of organo-soluble chitosan (CS) derivatives • VERO cells proliferation • Nanofibrous membranes from the synthesized chitosan derivatives and polycaprolactone.

  5. One barbiturate and two solvated thiobarbiturates containing the triply hydrogen-bonded ADA/DAD synthon, plus one ansolvate and three solvates of their coformer 2,4-diaminopyrimidine.

    Science.gov (United States)

    Hützler, Wilhelm Maximilian; Egert, Ernst; Bolte, Michael

    2016-09-01

    A path to new synthons for application in crystal engineering is the replacement of a strong hydrogen-bond acceptor, like a C=O group, with a weaker acceptor, like a C=S group, in doubly or triply hydrogen-bonded synthons. For instance, if the C=O group at the 2-position of barbituric acid is changed into a C=S group, 2-thiobarbituric acid is obtained. Each of the compounds comprises two ADA hydrogen-bonding sites (D = donor and A = acceptor). We report the results of cocrystallization experiments of barbituric acid and 2-thiobarbituric acid, respectively, with 2,4-diaminopyrimidine, which contains a complementary DAD hydrogen-bonding site and is therefore capable of forming an ADA/DAD synthon with barbituric acid and 2-thiobarbituric acid. In addition, pure 2,4-diaminopyrimidine was crystallized in order to study its preferred hydrogen-bonding motifs. The experiments yielded one ansolvate of 2,4-diaminopyrimidine (pyrimidine-2,4-diamine, DAPY), C4H6N4, (I), three solvates of DAPY, namely 2,4-diaminopyrimidine-1,4-dioxane (2/1), 2C4H6N4·C4H8O2, (II), 2,4-diaminopyrimidine-N,N-dimethylacetamide (1/1), C4H6N4·C4H9NO, (III), and 2,4-diaminopyrimidine-1-methylpyrrolidin-2-one (1/1), C4H6N4·C5H9NO, (IV), one salt of barbituric acid, viz. 2,4-diaminopyrimidinium barbiturate (barbiturate is 2,4,6-trioxopyrimidin-5-ide), C4H7N4(+)·C4H3N2O3(-), (V), and two solvated salts of 2-thiobarbituric acid, viz. 2,4-diaminopyrimidinium 2-thiobarbiturate-N,N-dimethylformamide (1/2) (2-thiobarbiturate is 4,6-dioxo-2-sulfanylidenepyrimidin-5-ide), C4H7N4(+)·C4H3N2O2S(-)·2C3H7NO, (VI), and 2,4-diaminopyrimidinium 2-thiobarbiturate-N,N-dimethylacetamide (1/2), C4H7N4(+)·C4H3N2O2S(-)·2C4H9NO, (VII). The ADA/DAD synthon was succesfully formed in the salt of barbituric acid, i.e. (V), as well as in the salts of 2-thiobarbituric acid, i.e. (VI) and (VII). In the crystal structures of 2,4-diaminopyrimidine, i.e. (I)-(IV), R2(2)(8) N-H...N hydrogen-bond motifs are preferred and, in two

  6. The Clinical Curative Effect and Prognosis of Barbiturate Coma Therapy in Severe Head Trauma%巴比妥昏迷疗法在重型颅脑创伤中的临床疗效及预后研究分析

    Institute of Scientific and Technical Information of China (English)

    高华

    2015-01-01

    Objective:To summarize the barbiturate coma therapy in clinical curative effect and prognosis of severe head trauma. Method:82 patients of severe craniocerebral trauma were selected in our hospital from February 2013 to August 2014 during the period of accepted the diagnosis and treatment,and randomly divided into two groups, 41 cases in each group.The control group were underwent routine therapy,while the experimental group was treated barbiturate coma therapy,at the same time,two groups’ treatment and prognosis were contrasted and analyzed. Result:Two groups 24 hours and 48 hours after treatment gived the real-time monitoring,the test results showed that the two groups in the cavity of cerebrospinal fluid pressure and cerebral blood flow and other clinical indicators were dropped. Compared with control group,the experimental group patients clinical index fell more,the difference was statistically significant(P<0.05).Conclusion:The clinical barbiturate coma therapy on the clinical curative effect and prognosis of severe head trauma effect is significant,in addition to being able to control the cerebrospinal fluid pressure in patients with cranial cavity,maximize the cerebral perfusion,at the same time also can improve the patients’ symptoms of cerebral ischemia or hypoxia,plays a comprehensive protection for the brain,thus it has the high feasibility and is worth promoting.%目的:总结巴比妥昏迷疗法在重型颅脑创伤中的临床疗效及预后情况。方法:本次研究资料选自2013年2月-2014年8月期间在本院接受诊治的82例重型颅脑创伤患者,将其随机分为两组,每组各41例患者。对照组接受常规治疗,而试验组则接受巴比妥昏迷疗法,对比及分析两组患者的治疗情况以及预后情况。结果:两组患者治疗24、48 h后给予进行实时监测,其检测结果表明两组患者在颅腔内脑脊液的压力、脑血流量等临床指标方面均有所下降,且与对照

  7. Circadian manifestations of barbiturate habituation, addiction and withdrawal in the rat

    Energy Technology Data Exchange (ETDEWEB)

    Ehret, C. F.; Peraino, C.; Meinert, J. C.; Groh, K. R.

    1979-01-01

    The present study uses circadian rhythm observations on rats to include diverse habituation and drug ingestion (phenobarbital) circumstances, including a comparison of the effect of pre-entrainment cycles of programmed feeding and illumination and subsequent conditions of exposure of duration sufficient to permit a steady-state in the appearance of circadian patterns derived from core-temperature telemetry and from automated food-consumption measurements. Finally, measurements were permitted to continue long enough after the drug was withdrawn from the diet to allow characterization of an abstinence syndrome, indicative of addiction.

  8. The synthesis of 5-(1- sup 11 C)ethyl barbiturates from labelled malonic esters

    Energy Technology Data Exchange (ETDEWEB)

    Gee, A.; Laangstroem, B. (Uppsala Univ. (Sweden). Dept. of Organic Chemistry)

    1991-01-01

    The synthesis of ({sup 11}C)phenobarbital, ({sup 11}C)pentobarbital and({sup 11}C)amobarbital labelled in the 5-(1-{sup 11}C)ethyl position is reported. The malonic esters R- CH(CO{sub 2}Et){sub 2} R phenyl-, 1-methylbutyl-, and 3- methylbutyl- were alkylated with (1-{sup 11}C)ethyl iodide prepared from ({sup 11}C)carbon dioxide. Ring closure of the 2-(1-{sup 11}C)ethyl-labelled malonic esters with urea afforded 5-(1-{sup 11}C)ethyl-phenobarbital,-phenobarbital, -pentobarbital and -amobarbital synthesis times of 42-47 min, counted from ({sup 11}C) carbon dioxide. In typical syntheses starting with 3 GBq pentobarbitol and (81 mCi) ({sup 11}C)carbon dioxide, 150-215 MBq (4-6 mCi) were produced in 25-30% decay corrected -amobarbital radiochemical yields with radiochemical purities greater than 98%. (author).

  9. The effect of two barbiturates on the development of three calliphoridae species (Diptera) of forensic importance

    OpenAIRE

    2008-01-01

    Resumo: A Entomologia Forense utiliza dados de desenvolvimento e aspectos ecológicos de insetos necrófagos com o objetivo de auxiliar as investigações criminais, entre outros, no cálculo da estimativa do intervalo pós-morte (IPM). Igualmente, pode-se caracterizar a causa da morte quando essas drogas são detectadas em insetos imaturos que se alimentam dos corpos em decomposição. Além disso, os insetos podem servir como uma ferramenta alternativa para análises toxicológicas na ausência de tecid...

  10. Amphetamines, Barbiturates and Hallucinogens; An Analysis of Use, Distribution, and Control. Final Report.

    Science.gov (United States)

    McGlothlin, William H.

    This report is the third of three monographs to provide perspectives on the use, distribution, and control of illicit drugs. The first, conducted in 1971, described the prevalence, use patterns, sources, distribution, and economics of the marihuana market. The second (1972) estimated the cost, benefits, and potential of approaches to narcotic…

  11. 4 CFR 25.8 - Alcoholic beverages and narcotics.

    Science.gov (United States)

    2010-01-01

    ... alcoholic beverages, narcotic drugs, hallucinogens, marijuana, barbiturates, or amphetamines is prohibited..., marijuana, barbiturate, or amphetamine. This prohibition shall not apply in cases where the drug is...

  12. 32 CFR 228.9 - Prohibition on narcotics and illegal substances.

    Science.gov (United States)

    2010-07-01

    ... narcotic drug, hallucinogen, marijuana, barbiturate or amphetamine is prohibited. Operation of a motor..., hallucinogens, marijuana, barbiturates or amphetamines is also prohibited. These prohibitions shall not apply...

  13. Drug: D02615 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available PTICS N05C HYPNOTICS AND SEDATIVES N05CB Barbiturates, combinations N05CB02 Barbiturates in combination with other drugs D02615 Chlorpromazine - promethazine mixt PubChem: 17396785 ...

  14. 肉桂醛巴比妥酸复合热稳定剂的制备与应用%Preparation and Application of Compound Heat Stabilizer of Cinnamaldehyde Barbituric Acid

    Institute of Scientific and Technical Information of China (English)

    张建超; 邬素华; 杨文梅; 郑确; 郭晓静

    2015-01-01

    合成肉桂醛巴比妥酸(CBA),并将其与硬脂酸钙(CaSt2)及水滑石(LDH)进行复配,系统研究复合热稳定体系中各组分之间的配比对PVC静态和动态热稳定性能及加工性能的影响.结果表明:CaSt2与CBA存在很好的协同作用,LDH能显著提高复合热稳定体系的热稳定性,通过实验筛选出CBA/CaSt2/LDH的最佳配比为5/2/3.

  15. Benzodiazepines should still be first-line treatment for alcohol withdrawal

    DEFF Research Database (Denmark)

    Askgaard, Gro; Pottegård, Anton; Fink-Jensen, Anders

    2017-01-01

    In this review, we summarize the evidence for benzodiazepines and barbiturates as alcohol withdrawal treatment and outline a treatment guideline. A number of randomized controlled trials (RCTs) indicate that benzodiazepine treatment decreases alcohol withdrawal seizures and is safe....... For barbiturates, only a few RCTs have been undertaken, and barbiturates were not found to be superior to benzodiazepines. Consequently, we suggest that benzodiazepines should still be first-line treatment for alcohol withdrawal....

  16. 10 CFR 710.8 - Criteria.

    Science.gov (United States)

    2010-01-01

    ... marijuana, cocaine, amphetamines, barbiturates, narcotics, etc.) except as prescribed or administered by a... limited to, criminal behavior, a pattern of financial irresponsibility, conflicting allegiances,...

  17. Synthesis and in vivo evaluation of 5-chloro-5-benzobarbiturates as new central nervous system depressants

    Energy Technology Data Exchange (ETDEWEB)

    Vieira, Andreia A.; Gomes, Niele M.; Matheus, Maria E.; Figueroa-Villar, Jose D., E-mail: figueroa@ime.eb.b [Instituto Militar de Engenharia (IME), Rio de Janeiro, RJ (Brazil). Dept. de Chemistry. Medicinal Chemistry Grupo; Fernandes, Patricia D. [Universidade Federal do Rio de Janeiro (UFRJ), RJ (Brazil). Inst. de Ciencias Biomedicas. Lab. de Farmacologia da Inflamacao e do Oxido Nitrico

    2011-07-01

    A new family of barbiturates, 5-chloro-5-benzylbarbituric acids, was prepared using a simple efficient synthetic method from aromatic aldehydes and barbituric acid, followed by reduction and chlorination with trichloro-isocyanuric acid, affording overall yields of 53 to 70%. The in vivo evaluation with mice showed that these compounds present tranquilizing activity. (author)

  18. Drug: D00712 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ) classification [BR:br08303] N NERVOUS SYSTEM N01 ANESTHETICS N01A ANESTHETICS, GENERAL N01AF Barbiturates, plain...5C HYPNOTICS AND SEDATIVES N05CA Barbiturates, plain N05CA15 Methohexital D00712 Methohexital sodium (USP) C

  19. Drug: D01071 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available eutic Chemical (ATC) classification [BR:br08303] N NERVOUS SYSTEM N01 ANESTHETICS N01A ANESTHETICS, GENERAL N01AF Barbiturates, plain...S AND SEDATIVES N05CA Barbiturates, plain N05CA16 Hexobarbital D01071 Hexobarbita

  20. Drug: D04985 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available S SYSTEM N01 ANESTHETICS N01A ANESTHETICS, GENERAL N01AF Barbiturates, plain N01AF01 Methohexital D04985 Met...hohexital (USP/INN) N05 PSYCHOLEPTICS N05C HYPNOTICS AND SEDATIVES N05CA Barbiturates, plain

  1. Drug: D00714 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available TC) classification [BR:br08303] N NERVOUS SYSTEM N01 ANESTHETICS N01A ANESTHETICS, GENERAL N01AF Barbiturates, plain...ATIVES N05CA Barbiturates, plain N05CA19 Thiopental D00714 Thiopental sodium (JP16/USP/INN) Target-based cla

  2. 脑电双频指数在监测重度颅脑损伤合并顽固性颅内高压患者的巴比妥盐昏迷中的应用%The Use of Bispectral Index to Monitor Barbiturate Coma in Severely Brain-Injured Patients with Refractory Intracranial Hypertension

    Institute of Scientific and Technical Information of China (English)

    Vincent Cottenceau; 沙欢欢; Laurent Petit; Fran(c)oise Masson; Dominique Guehl; Julien Asselineau; Jean-Fran(c)ois Cochard; Catherine Pinaquy; Alain Leger; Fran(c)ois Sztark

    2010-01-01

    背景在重症创伤性颅脑损伤(TBI)患者运用巴比妥盐治疗中,通常将暴发-抑制模式的脑电图(EEG)作为监测指标.双频指数(BIS)是脑电图的衍生物,并且考虑到了皮层电静止.本研究测定一定范围内的BIS是否可以预测一个特殊的暴发-抑制模式.方法前瞻性收入l1例应用巴比妥盐治疗的TBI患者.每天记录1小时EEG,每5分钟从原始EEG上计算1分钟的暴发数量及抑制率[抑制率(SREEG):从EEG上得到的前60秒皮层电静止所占的百分率],并与BIS-XPTM监测仪上伴行的数据对比[BIS和抑制商(SRBIS)].巴比妥盐昏迷的最佳水平定义为脑电图上每分钟有2~5个暴发发生.根据所得数据求出最佳水平的BIS预测值范围,对每一例数据都测定其精确度.结果 SREEG和SRBIS一致性很高[组间相关系数0.94(95%可信区间:0.90~0.96)].SREEG和BIS之间有显著相关性.在某些受试者中观察到显著不一致性.BIS值在6~15范围之间时预测精确度最高.结论应用巴比妥盐治疗的重症创伤性颅脑损伤患者,BIS和SREEG有很高相关性.当BIS值<6时巴比妥盐输注速率需要降低,而当BIS值>15时,则需要升高.BIS和抑制图形的关系应该周期性地通过EEG模拟信号(BIS-XPTM所示)来校正.

  3. Solid State Synthesis of 5-(Substituted indole-3-ylmethylidene)(Thio)Barbituric Acid under Microwave Irradiation%微波辐射固相合成5-(取代吲哚基-3-次甲基)(硫代)巴比妥酸

    Institute of Scientific and Technical Information of China (English)

    王俊岭

    2010-01-01

    在无溶剂、无催化剂、微波辐射条件下,取代吲哚-3-甲醛与(硫代)巴比妥酸通过Knoevenagel缩合反应,合成了一系列5-(取代吲哚基-3-次甲基)(硫代)巴比妥酸.最佳反应条件为:n(吲哚-3-甲醛):n(巴比妥酸)=1.2 : 1.0,微波辐射时间8 min,微波功率500 W,产率68.4%~82.8%.

  4. Pionerer bag barbituraterne

    DEFF Research Database (Denmark)

    Norn, Svend; Permin, Henrik; Kruse, Edith

    2015-01-01

    was of great importance for the science of organic chemistry and the development of the dye and medicine industry in the late 19th century. The next important step was the development of barbiturates. The pioneers were Josef von Mering and Emil Fischer. Using the Grimaux-method they synthesized various...... as a sedative - and antiepileptic drug and chloral hydrate as sedative-hypnotics. A new era was reached by the introduction of barbiturates. The story started with the chemist Adolf von Baeyer. His breakthrough in the synthesis of new agents as barbituric acid and indigo and his education of young chemists...

  5. Hiccups

    Science.gov (United States)

    ... Examples include: Encephalitis Meningitis Multiple sclerosis Stroke Traumatic brain injury Tumors Metabolic disorders and drugs Long-term hiccups can be triggered by: Alcoholism Anesthesia Barbiturates Diabetes Electrolyte imbalance Kidney failure Steroids Tranquilizers ...

  6. Bilirubin Test

    Science.gov (United States)

    ... than females. African Americans routinely show lower bilirubin concentrations than non-African Americans. Strenuous exercise may increase bilirubin levels. Drugs that can decrease total bilirubin include barbiturates, caffeine, penicillin, and high doses of salicylates. The drug ...

  7. Restrictions in means for suicide: an effective tool in preventing suicide

    DEFF Research Database (Denmark)

    Nordentoft, Merete; Qin, Ping; Helweg-Larsen, Karin

    2007-01-01

    , overall suicide mortality and method-specific suicide mortality in Denmark were compared with official information about availability of barbiturates and analgesics and carbon monoxide in vehicle exhaust and household gas. Restrictions on availability of household gas with carbon monoxide content...... and barbiturates was associated with a decline in the number of suicides and suicides by self-poisoning with these compounds after controlling for the effect of calender year. Restricted access occurred concomittantly with a 55 percent decrease in suicide rate....

  8. Large-scale virtual screening for the identification of new Helicobacter pylori urease inhibitor scaffolds.

    Science.gov (United States)

    Azizian, Homa; Nabati, Farzaneh; Sharifi, Amirhossein; Siavoshi, Farideh; Mahdavi, Mohammad; Amanlou, Massoud

    2012-07-01

    Here, we report a structure-based virtual screening of the ZINC database (containing about five million compounds) by computational docking and the analysis of docking energy calculations followed by in vitro screening against H. pylori urease enzyme. One of the compounds selected showed urease inhibition in the low micromolar range. Barbituric acid and compounds 1a, 1d, 1e, 1f, 1g, 1h were found to be more potent urease inhibitors than the standard inhibitor hydroxyurea, yielding IC(50) values of 41.6, 83.3, 66.6, 50, 58.8, and 60 μM, respectively (IC(50) of hydroxyurea = 100 μM). 5-Benzylidene barbituric acid has enhanced biological activities compared to barbituric acid. Furthermore, the results indicated that among the substituted 5-benzylidene barbiturates, those with para substitution have higher urease inhibitor activities. This may be because the barbituric acid moiety is closer to the bimetallic nickel center in unsubstituted or para-substituted than in ortho- or meta-substituted analogs, so it has greater chelating ability.

  9. Effects of Himanthalia elongata on the central nervous system of mice.

    Science.gov (United States)

    Anca, J M; Lamela, M; Cadavid, I; Calleja, J M

    1990-05-01

    The effects of a Himanthalia elongata extract were studied on the CNS of mice. A rich protein solution obtained from the seaweed was assayed for myorelaxant, anticonvulsant and analgesic activity and for its effects on spontaneous locomotor activity, amphetamine-induced hypermotility, exploratory behaviour, barbiturate-induced sleep, and body temperature. Very significant reductions in spontaneous motor activity, hypermotility and exploratory behaviour were found. The extract prolonged barbiturate-induced sleep and postponed pentylenetetrazol-induced death. Weak myorelaxant, hypothermic and analgesic effects were also observed, showing that H. elongata can depress the CNS.

  10. An Efficient Microwave-assisted Synthesis of Pyrido[2,3-d]pyrimidine Derivatives

    Institute of Scientific and Technical Information of China (English)

    TU Shujiang; WU Shanshan; HAN Zhengguo; HAO Wenjuan

    2009-01-01

    A series of new pyrido[2,3-d]pyrimidine derivatives were synthesized by multi-component reactions of equi-molar amount of aromatic aldehydes with barbituric acids (barbituric acid or 1,3-dimethylbarbituric acid) and 5-amino-2-methylbenzo[d]thiazol in mixed solvent of glacial acetic acid and ethylene glycol without catalyst under microwave irradiation. This one-pot method has the advantage of good yields (90%-93%), simple workup proce-dure and short reaction time (5 min).

  11. Medical Readings on Drug Abuse.

    Science.gov (United States)

    Byrd, Oliver E.

    Summaries are presented of over 150 articles in the recent medical and psychiatric literature. Topics covered are: effects of drugs, tobacco, alcohol, drugs used in medicine, vapor sniffing, marijuana, barbiturates, tranquilizers, amphetamines, methamphetamine, lysergic acid diethylamide, other hallucinogens, heroin and the opiates, psychiatric…

  12. Drugs and Personality: Extraversion-Introversion.

    Science.gov (United States)

    Spotts, James V.; Shontz, Franklin C.

    1984-01-01

    Administered the Eysenck Personality Inventory as part of a larger battery of tests to chronic users of drugs (N=43) to determine how drug use influences personality. Results showed that cocaine and opiates users were more introverted; and amphetamine users, barbiturates users and nonusers were more extraverted. (LLL)

  13. DIETARY EXPOSURE OF PHENOBARBITAL TO MALE AND FEMALE CD1 MICE FOR 2 OR 7 DAYS: EXAMINATION OF IN-LIFE, HEPATOCELLULAR ENZYME, PROLIFERATION, AND GENE EXPRESSION RESPONSES.

    Science.gov (United States)

    Phenobarbital (PB) is a barbiturate used to relieve anxiety and control epilepsy. PB is also an archetypical inducer of the constitutive androstane receptor (CAR), resulting in liver hypertrophy in humans and both liver hypertrophy and hyperplasia in rodents. In this study, male ...

  14. The Ro 15-1788 cue: Evidence for benzodiazepine agonist and inverse agonist properties

    NARCIS (Netherlands)

    Vry, J. De; Slangen, J.L.

    1985-01-01

    Rats discriminating Ro 15–1788 (10 mg/kg, i.p.) from vehicle completely generalized this cue to typical benzodizepines, and partially generalized it to barbiturates, pentylenetetrazol, CGS 8216, β-CCM and PK 8165. CL 218 872, Ro 5–4864, phenytoine, progabide, propranolol, yohimbine and various CNS s

  15. Restrictions in Availability of Drugs Used for Suicide

    DEFF Research Database (Denmark)

    Nordentoft, Merete

    2007-01-01

    Availability of drugs with high lethality has been hypothesized to increase the risk of self-poisoning suicides. A literature search concerning deliberate self-poisoning and the effect of restricting access to drugs was conducted, and the effect of restrictions in availability of barbiturates, tr...

  16. Rapid and efficient synthesis of fused heterocyclic pyrimidines under ultrasonic irradiation.

    Science.gov (United States)

    Mosslemin, Mohammad Hossein; Nateghi, Mohammad Reza

    2010-01-01

    Some fused heterocyclic pyrimidines have been synthesized in high yields using ultrasound irradiation in a one-pot, three-component and efficient process by condensation reaction of barbituric acids, aldehydes and a series of enamines in water. Prominent among the advantages of this new method are operational simplicity, good yields in short reaction times and easy work-up procedures employed.

  17. [Selected Readings for the Professional Working with Drug Related Problems.

    Science.gov (United States)

    Wisconsin Univ., Madison.

    A bibliography of selected readings compiled at the University of Wisconsin for the National Drug Education Training Program. These selected readings include information on narcotics, amphetamines, mescaline, psilogybin, hallucinogens, LSD, barbiturates, alcohol, and other stimulants. The intended user of this bibliography is the professional…

  18. Butallylonal 1,4-dioxane hemisolvate

    Directory of Open Access Journals (Sweden)

    Ulrich J. Griesser

    2010-10-01

    Full Text Available The asymmetric unit of the title compound [systematic name: 5-(1-bromoprop-2-en-1-yl-5-sec-butylpyrimidine-2,4,6-trione 1,4-dioxane hemisolvate], C11H15BrN2O3·0.5C4H8O2, contains one half-molecule of 1,4-dioxane and one molecule of butallylonal, with an almost planar barbiturate ring [largest deviation from the mean plane = 0.049 (5 Å]. The centrosymmetric dioxane molecule adopts a nearly ideal chair conformation. The barbiturate molecules are linked together by an N—H...O hydrogen bond, giving a single-stranded chain. Additionally, each dioxane molecule acts as a bridge between two antiparallel strands of hydrogen-bonded barbiturate molecules via two hydrogen bonds, N—H...O(dioxaneO...H—N. Thus, a ladder structure is obtained, with the connected barbiturate molecules forming the `stiles' and the bridging dioxane molecules the `rungs'.

  19. Personnel Security Research - Prescreening and Background Investigations

    Science.gov (United States)

    1986-06-01

    NO Hallucinogens YES NO Opium YES NO (LSD, STP, PCP) THC YES NO Barbiturates YES NO Heroin YES NO Any synthetic or cure-type drugs, such as Methadone ...intoxicating products of the hemp plant, cannabis sative (including hashish) or any synthesis thereof. LSD - Lysergic acid diethylamid; a dangerous drug

  20. A Psychophysiologic Study of Weakening Traumatic Combat Memories with Post-Reactivation Propranolol

    Science.gov (United States)

    2011-06-01

    confounding substances, including opiates, barbiturates, and methadone , at the time of the script-driven imagery procedure. When the analyses were repeated...the mechanism underlying those effects. REFERENCES [1] Nader K, Schafe GE, Le Doux JE. Fear memories require protein synthesis in the

  1. Comparison Of The Direct Costs, Length Of Recovery, And Incidence Of Post Operative Anti Emetic Use After Anesthesia Induction With Propofol Or A 1:1 Mixture Of Thiopental And Propofol

    Science.gov (United States)

    1999-10-01

    by previous injection of lidocaine (Stolting, 1991). It is associated with a period of apnea when first administered that quickly resolves. Apnea... pharmacodynamics of induction agents will help the provider to make informed choices when using these agents. Barbiturates such as thiopental have been shown to

  2. Synthesis and characterization of barbitones as antimicrobial agents

    Directory of Open Access Journals (Sweden)

    H. G. SANGANI

    2006-06-01

    Full Text Available Barbitones (3 were synthesised by the condensation of chalcones (2 with barbituric acid. The structure of the synthesized compounds were assigned on the basis of elemental analyses, IR, NMR and mass spectral studies. All the products were evaluated for their in vitro antimicrobial activity against various strains of bacteria and fungi.

  3. Drugs of abuse and tranquilizers in Dutch surface waters, drinking water and wastewater: Results of screening monitoring 2009

    NARCIS (Netherlands)

    van der Aa, N.G.F.M.; Dijkman, E.; Bijlsma, L.; Emke, E.; van de Ven, B.M.; van Nuijs, A.L.N.; de Voogt, P.

    2011-01-01

    In the surface waters of the rivers Rhine and Meuse, twelve drugs that are listed in the Dutch Opium act were detected at low concentrations. They are from the groups amphetamines, tranquilizers (barbiturates and benzodiazepines) opiates and cocaine. During drinking water production, most compounds

  4. Efficacy of Adjunctive Sleep Interventions for PTSD

    Science.gov (United States)

    2009-03-01

    CBC, diabetes & liver func.), EKG, urine drug screens for amphetamines , marijuana, heroin, barbiturate, PCP alcohol and other narcotics, pregnancy...blood count & chem., thyroid func, electrolytes, CBC, diabetes & liver func. EKG Urine drug screens for amphetamines , marijuana, heroin...Recommendations Subject 210675 research file lacked documentation of routine laboratory results or urine drug screen. 6.0 STUDY PROCEDURES—For PRZ or

  5. Hair Follicle Bulb as a Biodosimeter for Low-Level VX Vapor Exposure: Initial Studies Validating the Presence of Potential Protein Biomarkers of Exposure in the Sprague-Dawley Rat Whisker Follicle

    Science.gov (United States)

    2006-10-01

    amphetamine , methamphetamine, heroin, marijuana, and steroids), therapeutic drugs (e.g. ephedrine, benzodiazepines, and barbiturates), and inorganic heavy...if any, of a particular substance in the hair. Immunoassay , High Performance Liquid Chromatography (HPLC), 7 Capillary Electrophoresis (CE), Gas...analysis is that successful analysis is possible even months after exposure. Other sample sources for testing, such as urine , offer an immediate

  6. 10 CFR 26.185 - Determining a fitness-for-duty policy violation.

    Science.gov (United States)

    2010-01-01

    ...., benzodiazepines in the first case, barbiturates in the second) and are listed in the licensee's or other entity's... medical condition poses a potential risk to public health and safety as a result of the individual being impaired while on duty. If the MRO determines that such a risk exists, he or she shall ensure that...

  7. Remote Photoregulated Ring Gliding in a [2]Rotaxane via a Molecular Effector.

    Science.gov (United States)

    Tron, Arnaud; Pianet, Isabelle; Martinez-Cuezva, Alberto; Tucker, James H R; Pisciottani, Luca; Alajarin, Mateo; Berna, Jose; McClenaghan, Nathan D

    2017-01-06

    A molecular barbiturate messenger, which is reversibly released/captured by a photoswitchable artificial molecular receptor, is shown to act as an effector to control ring gliding on a distant hydrogen-bonding [2]rotaxane. Thus, light-driven chemical communication governing the operation of a remote molecular machine is demonstrated using an information-rich neutral molecule.

  8. Evaluation of Fenton's Reagent and Activated Persulfate for Treatment of a Pharmaceutical Waste Mixture in Groundwater

    DEFF Research Database (Denmark)

    Bennedsen, Lars Rønn; Søgaard, Erik Gydesen; Kakarla, Prasad

    Groundwater beneath the Kærgård Plantage megasite in Denmark are contaminated with a complex mixtu of pharmaceutical wastes, including sulfonamides, barbiturates, aniline, pyridine chlorinated solvents, mercury, and cyanide.  Regulatory agencies in Denmark are now in the process of evaluating...

  9. Brain carbonic acid acidosis after acetazolamide

    DEFF Research Database (Denmark)

    Heuser, D; Astrup, J; Lassen, N A;

    1975-01-01

    In cats in barbiturate anesthesia extracellular pH and potassium were continously recorded from brian cortex by implanted microelectrodes. Implantation of the electrodes preserved the low permeability of the blood-brain-barrier to HCO3-minus and H+ions as indicated by the development of brain aci...

  10. 5-[1-(1,3-Dimethyl-2,4,6-trioxohexahydropyrimidin-5-yl-2-oxopropyl]-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H-trione

    Directory of Open Access Journals (Sweden)

    Manfred Steimann

    2013-08-01

    Full Text Available The title compound, C15H18N4O7, is a product of the substitution reaction of 5,5-dibromo-1,3-dimethylbarbituric acid with sodium sulfide in aqueous acetone. In the crystal, molecules display neither intermolecular nor intramolecular hydrogen bonding and the two barbiturate rings adopt the keto form.

  11. 3-Hydroxy-2'-methoxy-6-methylflavone

    DEFF Research Database (Denmark)

    Karim, Nasiara; Gavande, Navnath; Wellendorph, Petrine

    2011-01-01

    detected using holeboard, actimeter and horizontal wire tests and only weak barbiturate potentiating effects on the loss of righting reflex test. Taken together, these data suggest that 3-OH-2'MeO6MF is an anxiolytic without sedative and myorelaxant effects acting through positive allosteric modulation...

  12. Decompressive Craniectomy and Traumatic Brain Injury: A Review

    Science.gov (United States)

    Alvis-Miranda, Hernando; Castellar-Leones, Sandra Milena; Moscote-Salazar, Luis Rafael

    2013-01-01

    Intracranial hypertension is the largest cause of death in young patients with severe traumatic brain injury. Decompressive craniectomy is part of the second level measures for the management of increased intracranial pressure refractory to medical management as moderate hypothermia and barbiturate coma. The literature lack of concepts is their indications. We present a review on the state of the art. PMID:27162826

  13. Drug: D07321 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07321 Drug Vinylbital (INN); Vinylbitone C11H16N2O3 224.1161 224.2563 D07321.gif A...HOLEPTICS N05C HYPNOTICS AND SEDATIVES N05CA Barbiturates, plain N05CA08 Vinylbital D07321 Vinylbital (INN)

  14. 21 CFR 250.11 - Thyroid-containing drug preparations intended for treatment of obesity in humans.

    Science.gov (United States)

    2010-04-01

    ... nervous system stimulants, with or without one or more additional drug substances such as barbiturates or.... (b) Combinations of thyroid or other thyrogenic drugs with central nervous system stimulants with or... treatment of obesity in humans. 250.11 Section 250.11 Food and Drugs FOOD AND DRUG...

  15. Utah Drop-Out Drug Use Questionnaire.

    Science.gov (United States)

    Governor's Citizen Advisory Committee on Drugs, Salt Lake City, UT.

    This questionnaire assesses drug use practices in high school drop-outs. The 79 items (multiple choice or apply/not apply) are concerned with demographic data and use, use history, reasons for use/nonuse, attitudes toward drugs, availability of drugs, and drug information with respect to narcotics, amphetamines, LSD, Marijuana, and barbiturates.…

  16. A Novel and Efficient Five-Component Synthesis of Pyrazole Based Pyrido[2,3-d]pyrimidine-diones in Water: A Triply Green Synthesis

    Directory of Open Access Journals (Sweden)

    Majid M. Heravi

    2016-04-01

    Full Text Available A novel one pot synthesis of pyrazolo[4′,3′:5,6]pyrido[2,3-d]pyrimidine-diones, via a five-component reaction, involving, hydrazine hydrate, ethyl acetoacetate, and 1,3-dimethyl barbituric acid, an appropriate aryl aldehydes and ammonium acetate catalyzed via both of heterogeneous and homogeneous catalysis in water, is reported.

  17. Determination of sedative hypnotics in sewage sludge by pressurized liquid extraction with high-performance liquid chromatography and tandem mass spectrometry.

    Science.gov (United States)

    Arbeláez, Paula; Granados, Judith; Borrull, Francesc; Marcé, Rosa Maria; Pocurull, Eva

    2014-12-01

    This paper describes a method for the determination of eight sedative hypnotics (benzodiazepines and barbiturates) in sewage sludge using pressurized liquid extraction and liquid chromatography with tandem mass spectrometry. Pressurized liquid extraction operating conditions were optimized and maximum recoveries were reached using methanol under the following operational conditions: 100ºC, 1500 psi, extraction time of 5 min, one extraction cycle, flush volume of 60% and purge time of 120 s. Pressurized liquid extraction recoveries were higher than 88% for all the compounds except for carbamazepine (55%). The repeatability and reproducibility between days, expressed as relative standard deviation (n = 5), were lower than 6 and 10%, respectively. The detection limits for all compounds were lower than 12.5 μg/kg of dry weight. The method was applied to determine benzodiazepines and barbiturates in sewage sludge from urban sewage treatment plants, and carbamazepine showed the highest concentration (7.9-18.9 μg/kg dry weight).

  18. N,N-Diethylanilinium 2,4-dioxo-5-(2,4,6-trinitrophenyl-1,2,3,4-tetrahydropyrimidin-6-olate

    Directory of Open Access Journals (Sweden)

    Manickam Buvaneswari

    2011-12-01

    Full Text Available In the crystal structure of the title molecular salt, C10H16N+·C10H4N5O9−, the components are linked through a N—H...O hydrogen bonds. R22(8 ring motifs are formed between inversion-related barbiturate residues. Two intramoleculer N—H...O hydrogen bonds are observed in the anion. The dihedral angle between 2,4,6-trinitrophenyl and barbiturate rings is 53.6 (2°. The N,N-diethylamine substituent is disordered and was modeled as two geometrically equivalent conformers with occupancies of 0.737 (2 and 0.273 (2.

  19. Coma blisters in 2 children on anticonvulsant medication.

    Science.gov (United States)

    Basu, Anna; Brown, Sara; Kirkham, Nigel; Ramesh, Venkateswaran; Leech, Suzy; Devlin, Anita

    2009-08-01

    Blister formation and eccrine sweat gland necrosis have been recognized to occur in states of impaired consciousness and were first reported following barbiturate intoxication. Their etiology is complex and cannot simply be explained by pressure effects. Now that barbiturates are less frequently used, clinicians are likely to be less aware of the phenomenon of coma blister formation; however, newer drugs have also been associated with the occurrence of coma blisters. We describe 2 new associations of coma blisters and anticonvulsants in children. In the first child, blisters recurred on multiple occasions along with obtundation and edema. Our aims are to alert clinicians to the occurrence of coma blisters in children sedated on anticonvulsant medications and to report the new finding of recurrent coma blisters.

  20. Alum (KAI(SO4)2·12H2O) Catalyzed Multicomponent Transformation: Simple, Efficient, and Green Route to Synthesis of Functional- ized Spiro[chromeno[2,3-d]pyrimidine-5,3'-indoline]-tetraones in Ionic Liquid Media

    Institute of Scientific and Technical Information of China (English)

    Mirhosseini Moghaddam, Mojtaba; Bazgir, Ayoob; Mohammad Mehdi, Akhondi; Ghahremanzadeh, Ramin

    2012-01-01

    The combination of isatin, barbituric acid, and cyclohexane-1,3-dione derivatives in the presence of alum (KAI(SO4)2· 12H2O) as a catalyst for 15 min was found to be a suitable and efficient method for the synthesis of spiro[chromeno[2,3-d]pyrimidine-5,3'-indoline]-tetraones.

  1. Synthesis of spiro[benzo[ℎ]quinoline-7,3'- indolines] via a three-component condensation reaction

    Indian Academy of Sciences (India)

    Abbas Rahmati; Miranda Eskandari-Vashareh

    2014-01-01

    An efficient one-pot synthesis of a new series of spiro[benzo[ℎ]quinoline-7,3'-indoline] was accomplished simply by the reaction of an isatin, naphthalen-1-amine and a CH-acid (,-dimethylbarbituric acid, barbituric acid, dimedone or 1,3-indandion) in acetic acid. During this process, the effects of solvent and temperature have been investigated on the yield of reactions.

  2. Persistant hiccups due to the use of intravenous metilprednisolone in a patient wit relapsing remitting multiple sclerosis: a case report and literature review

    OpenAIRE

    Yıldız Değirmenci1; Ayhan Öztürk; Burçin Çamuşoğlu

    2016-01-01

    Hiccups can be defined as the sudden, uncontrolled contractions of the diaphragm, followed by immediate inspiration and closure of the glottis over the trachea. Various etiologies are responsible for this reflex action such as instrumentations, gastrointestinal, cardiovascular, toxic-metabolic factors, and drugs. Most common drugs that may trigger hiccups are opioids, barbiturates, some antibiotics, chemotherapeutic agents, and steroids. Since steroids are one of the most common drugs in neur...

  3. Anaesthetics may change the shape of isolated type I hair cells.

    Science.gov (United States)

    Scarfone, E; Ulfendahl, M; Figueroa, L; Flock, A

    1991-08-01

    Type I hair cells isolated from animals anaesthetised with barbiturates or ether were found to be shorter and to lack a prominent 'neck' region when compared to cells isolated from non-anaesthetised animals. Ketamine did not have this effect. The changes observed could have important implications for the physiology of inner ear receptors. These findings infer that care should be taken in the choice of anaesthetics used in studies on cells from the inner ear.

  4. Evaluation of methods of rapid mass killing of segregated early weaned piglets

    OpenAIRE

    Whiting, Terry L.; Steele, Gregory G.; Wamnes, Steinar; Green, Chris

    2011-01-01

    The operational logistics of mass killing of healthy, surplus piglets by manual blunt force trauma, controlled blunt force trauma, intraperitoneal injection of barbiturate, and free bullet were recorded. Objective performance variables evaluated were, speed of application, human resource and input cost, animal restraint required, and failure rate. Subjective evaluation of esthetics and difficulty of application indicated manual blunt force trauma is an unacceptable technique. Under field cond...

  5. Associations of Adverse Clinical Course and Ingested Substances among Patients with Deliberate Drug Poisoning: A Cohort Study from an Intensive Care Unit in Japan

    Science.gov (United States)

    Ichikura, Kanako; Takeuchi, Takashi

    2016-01-01

    Objectives Some patients with deliberate drug poisoning subsequently have an adverse clinical course. The present study aimed to examine whether the type of drugs ingested and psychiatric diagnoses were related to an adverse clinical course. Methods We conducted a cohort study of patients with deliberate drug poisoning admitted to the intensive care unit of a university hospital located in Tokyo, Japan, between September 2006 and June 2013. Intensive care unit (ICU) stay of ≥4 days was used as a primary outcome measure, while the incidence of aspiration pneumonitis was used as a secondary outcome measure. Ingested substances and psychiatric diagnoses were used as explanatory variables. Results Of the 676 patients with deliberate drug poisoning, 88% had a history of psychiatric treatment and 82% had ingested psychotropic drugs. Chlorpromazine-promethazine-phenobarbital combination drug (Vegetamin®) ranked fifth among the most frequently ingested substances in cases of deliberate drug poisoning and had the highest incidence of prolonged ICU stay (20%) and aspiration pneumonitis (29%). The top three major classes consisted of benzodiazepines (79%), new-generation antidepressants (25%), and barbiturates/non-barbiturates (23%). Barbiturate overdose was independently associated with increased odds of both prolonged ICU stay (8% vs. 17%; odds ratio [OR], 2.97; 95% confidence interval [CI], 1.60–5.55) and aspiration pneumonitis (8% vs. 24%; OR, 3.83; 95% CI, 2.18–6.79) relative to those associated with overdose of only other sedative-hypnotics (i.e., benzodiazepines). Conclusion These results suggest that judicious prescribing of barbiturates by psychiatrists could reduce the risk of an adverse clinical course when a patient attempts an overdose. PMID:27560966

  6. Substance Use and Mental Health Risk Factors for Servicemembers: Findings from U.S. Department of Defense Health Related Behavior Surveys

    Science.gov (United States)

    2011-04-01

    methamphetamine, tranquilizers or muscle relaxers, sedatives or barbiturates, pain relievers, and anabolic steroids . “Nonmedical use” was defined as any use of...cognitive injuries, their consequences , and service to assist recovery (pp. 87–161). San Monica, CA Rand Corporation. [9] Seal, K. H., Metzler, T. J... consequences among active duty military personnel. Addictive Behaviors, 36, 608–614. [20] Reiger, D. A., Farmer, M. E., Rae, D. S., Locke, B. Z., Keith, S

  7. Synthesis of Malononitrile-Condensed Disperse Dyes and Application on Polyester and Nylon Fabrics

    OpenAIRE

    2014-01-01

    An active methylene compound, malononitrile, was introduced into the structures of a series of disperse dyes previously prepared by coupling phloroglucinol, barbituric acid, and α and β-naphtho to 4-amino-3-nitrobenzaldehyde. The dyes were purified by recrystallization from ethanol. The purity of the dyes was examined by thin-layer chromatography (TLC) and the dyes were characterized by visible absorption and Fourier transform infrared spectroscopy (FTIR). The malononitrile-condensed dyes pro...

  8. Spice: A New Legal Herbal Mixture Abused by Young Active Duty Military Personnel

    Science.gov (United States)

    2012-01-01

    kinase, serum ethanol level ᝺ mg/dL, and urine drug screen was neg- ative for amphetamines , barbiturates, benzodi- azepines, cocaine, methadone...ABSTRACT. Spice is an herbal mixture smoked for euphoria and mixed with synthetic cannabinoids that are undetected on urine drug screens. Spice use has...increased in the military because it is con- sidered legal and is not detected on urine drug screen. The authors describe 3 cases of Spice use in

  9. Drug: D01310 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available vous system and sensory organs 11 Agents affecting central nervous system 112 Hypnotics and sedatives, anxio...137 260.2647 D01310.gif Sedative-hypnotic Therapeutic category: 1125 ATC code: N05CA06 Barbiturates GABAA-re...D01310 Drug Secobarbital sodium (JAN/USP); Seconal sodium (TN) C12H17N2O3. Na 260.1

  10. Evaluation of anticonvulsant drugs during pregnancy in a population-based Hungarian study.

    Science.gov (United States)

    Czeizel, A E; Bod, M; Halász, P

    1992-01-01

    The Hungarian Case-Control Surveillance of Congenital Anomalies, from 1980-1987, involved 10,698 malformed cases and 21,546 non-malformed controls. Ninety-five pregnant women were treated by 144 anticonvulsants excluding diazepam and barbiturates. The rate of anticonvulsant use was 2.9 times higher in pregnant women having malformed offspring than in control mothers and this difference was greater in polytherapy than in monotherapy.

  11. Evaluation of Fenton's Reagent and Activated Persulfate for Treatment of a Pharmaceutical Waste Mixture in Groundwater

    DEFF Research Database (Denmark)

    Bennedsen, Lars Rønn; Søgaard, Erik Gydesen; Kakarla, Prasad

    2010-01-01

    Soil and groundwater beneath the Kærgård Plantage megasite in Denmark are contaminated with a complex mixture of pharmaceutical wastes, including sulfonamides, barbiturates, aniline, pyridine chlorinated solvents (DNAPL), benzene, toluene, mercury, and cyanide. Regulatory agencies in Denmark...... of the bench scale results for MFR and ASP for treating a complex pharmaceutical waste mixture in the soil and groundwater beneath the Kærgård Plantage megasite....

  12. Molecular Component Structures Mediated Formation of Self-assemblies

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Molecular recognition directed self-assemblies from complementary molecular components, melamine and barbituric acid derivatives were studied by means of NMR, fluorescence, and TEM. It was found that both the process of the self-assembly and the morphologies of the result ed self-assemblies could be mediated by modifying the structures of the molecular components used. The effect of the structures of the molecular components on the formation of the self-as semblies was discussed in terms of intermolecular interactions.

  13. Alternate Sources for Propellant Ingredients.

    Science.gov (United States)

    1976-07-07

    ricinoleates (castor oil) Cobalt naphthenate Shellac Elba solvent Ni troform Ammonium oxalate Sodium barbiturate Cateqory 6: Materials with...with the compound. MAPO: Category 1, P, K. Triz(2- methyl -l-aziridinyl) phosphine oxide (MAPO) is used as a crosslinking agent for polymers containing...elements, ranging from 0.001% tin to 0.03% for molybdenum. Glyceryl Mono-and Tri- ricinoleates : Category 5, S, F. These esters are found in castor oil

  14. Toxicological Assessment of ABATE (Tradename) (0,0,0’,0’-Tetramethyl-0,0’-Thio-Di-P-Phenylene Phosphorothioate) Administered Orally and Dermally to Mated and Nonmated Female Rabbits, April 1983.

    Science.gov (United States)

    1983-11-02

    The body louse, Pediculus humanus humanus (). (2) The head louse, Pediculus humanus cepitis (DeGeer). (3) The pubic louse, Pthirus pubis (L). b. To...means of an intravenous overdose of barbiturate. At this time, the brains were removed from two fetuses from each litter for the determination of brain...Animals of all groups were received In good condition and showed a smooth, shiny hair coat. A few had diarrhea for 2-3 days after arrival, but this

  15. Increased GABA(A receptor ε-subunit expression on ventral respiratory column neurons protects breathing during pregnancy.

    Directory of Open Access Journals (Sweden)

    Keith B Hengen

    Full Text Available GABAergic signaling is essential for proper respiratory function. Potentiation of this signaling with allosteric modulators such as anesthetics, barbiturates, and neurosteroids can lead to respiratory arrest. Paradoxically, pregnant animals continue to breathe normally despite nearly 100-fold increases in circulating neurosteroids. ε subunit-containing GABA(ARs are insensitive to positive allosteric modulation, thus we hypothesized that pregnant rats increase ε subunit-containing GABA(AR expression on brainstem neurons of the ventral respiratory column (VRC. In vivo, pregnancy rendered respiratory motor output insensitive to otherwise lethal doses of pentobarbital, a barbiturate previously used to categorize the ε subunit. Using electrode array recordings in vitro, we demonstrated that putative respiratory neurons of the preBötzinger Complex (preBötC were also rendered insensitive to the effects of pentobarbital during pregnancy, but unit activity in the VRC was rapidly inhibited by the GABA(AR agonist, muscimol. VRC unit activity from virgin and post-partum females was potently inhibited by both pentobarbital and muscimol. Brainstem ε subunit mRNA and protein levels were increased in pregnant rats, and GABA(AR ε subunit expression co-localized with a marker of rhythm generating neurons (neurokinin 1 receptors in the preBötC. These data support the hypothesis that pregnancy renders respiratory motor output and respiratory neuron activity insensitive to barbiturates, most likely via increased ε subunit-containing GABA(AR expression on respiratory rhythm-generating neurons. Increased ε subunit expression may be critical to preserve respiratory function (and life despite increased neurosteroid levels during pregnancy.

  16. Second-order Nonlinear Optical Properties of a Series of Azulene Derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHOU,Xin(周新); REN,Ai-Min(任爱民); FENG,Ji-Kang(封继康); LIU,Xiao-Juan(刘孝娟); SHU,Chia-Chen(许振锋)

    2004-01-01

    The first hyperpolarizabilities of a series of novel azulenic-barbituric acid chromophores have been studied by using 12 excitation wavelengths, ranging from 900 to 1907 nm. The dispersion relation of the first hyperpolarizabilities of chromophores holds the same tendency as the experimental results. In addition, the static first hyperpolarizability β0 of molecules was calculated by means of the Sum-Over-States (SOS) expression and the two-level formula respectively. The results show that these molecules possess large static first hyperpolarizabilities and the β0 value increases as the donor or acceptor strength enhances; the distorted degree of molecules has also an important influence on the β0 value.

  17. Abuse and dependence liability of benzodiazepine-type drugs: GABA(A) receptor modulation and beyond.

    Science.gov (United States)

    Licata, Stephanie C; Rowlett, James K

    2008-07-01

    Over the past several decades, benzodiazepines and the newer non-benzodiazepines have become the anxiolytic/hypnotics of choice over the more readily abused barbiturates. While all drugs from this class act at the GABA(A) receptor, benzodiazepine-type drugs offer the clear advantage of being safer and better tolerated. However, there is still potential for these drugs to be abused, and significant evidence exists to suggest that this is a growing problem. This review examines the behavioral determinants of the abuse and dependence liability of benzodiazepine-type drugs. Moreover, the pharmacological and putative biochemical basis of the abuse-related behavior is discussed.

  18. Synthesis and Self-Assembly of Donor–Acceptor–Donor Based Oligothiophenes and Their Optoelectronic Properties

    DEFF Research Database (Denmark)

    Siram, Raja Bhaskar Kanth; Tandy, Kristen; Horecha, Marta;

    2011-01-01

    In this work, the synthesis of an oligothiophene having a donor–acceptor–donor (D–A–D) chromophore with hydrogen bonding groups is described. The D–A–D molecule was demonstrated to self-organize via intermolecular H-bonding between barbituric acid units. Interactions between the oligothiophene...... subunits were also found to be important, affording nanoribbons that could be observed by atomic force and transmission electron microscopy. The applicability of the oligothiophene for organic electronic applications was investigated by fabricating organic field-effect transistors (OFETs) and organic...

  19. Effect of pomegranate (Punica granutum) and rosemary (Rosmarinus officinalis L.) extracts on shelf-life for chilled Greenland halibut (Reinhardtius hippoglossoides) fillets in modified atmosphere packaging at 2 ºC

    DEFF Research Database (Denmark)

    Ünalan, U.; Dalgaard, Paw; Korel, F.

    2011-01-01

    ) at 2 °C. Parameters that were monitored were: microbiological (aerobic plate counts (APC), lactic acid bacteria (LAB), Lactobacillus spp., and Photobacterium phosphoreum), biochemical (pH, thio-barbituric acid (TBA), trimethylamine (TMA) and total-volatile-nitrogen (TVN)), and sensory (color, flavor...... and texture) attributes. For microbiological results, irrespective of treatments, APC reached levels ≥107 CFU/g during storage. The spoilage microflora of fillets in MAP was dominated by LAB, but the concentration of Lactobacillus was very low. During storage, P.phosphoreum was not detected in any sample...

  20. Polyurethane Foams with Pyrimidine Rings

    Directory of Open Access Journals (Sweden)

    Kania Ewelina

    2014-09-01

    Full Text Available Oligoetherols based on pyrimidine ring were obtained upon reaction of barbituric acid with glycidol and alkylene carbonates. These oligoetherols were then used to obtain polyurethane foams in the reaction of oligoetherols with isocyanates and water. The protocol of foam synthesis was optimized by the choice of proper kind of oligoetherol and synthetic composition. The thermal resistance was studied by dynamic and static methods with concomitant monitoring of compressive strength. The polyurethane foams have similar physical properties as the classic ones except their enhanced thermal resistance. They stand long-time heating even at 200°C. Moreover thermal exposition of foams results generally in increase of their compressive strength.

  1. [Guillain-Barre syndrome as a result of poisoning with a mixture of "kompot"(Polish heroin) and drugs].

    Science.gov (United States)

    Gawlikowski, T; Winnik, L

    2001-01-01

    Guillain-Barré Syndrome is the most common form of polineuropathy. It is suggested that some infectious, immune and allergic factors are involved in developing the syndrome. "Kompot" or "Polish heroine", a domestic product, is produced from poppy straw or juice of poppy head (Papaver somniferum) and it is administered intravenously. "Kompot" shows variable contents of heroine, 6-MAM, 3-MAM, morphine, acetylo-codeine and codeine as well as papaverine, thebaine and narcotine. The case history of a young man dependent on "Polish heroine" who developed the Guillain-Barré Syndrome due to severe intoxication induced by home made heroine, barbiturates and benzodiazepines is described.

  2. Effectiveness of lorazepam-assisted interviews in an adolescent with dissociative amnesia A case report

    Institute of Scientific and Technical Information of China (English)

    Yuna Seo; Mi-Hee Shin; Sung-Gon Kim; Ji-Hoon Kim

    2013-01-01

    To facilitate gathering information during a psychiatric interview, some psychiatrists advocate augmenting the interview using drugs. Rather than barbiturates, benzodiazepines have been used for drug-assisted interviews. Dissociative amnesia is one of the indications for these interviews. Herein, we present the case of a 15-year-old female who was diagnosed as having dissociative amnesia because of conflicts with her friends. She was administered a lorazepam-assisted interview to aid recovery of her memories. In this case, a small dose of lorazepam was sufficient to recover her memories without any adverse effects.

  3. Coma blisters sans coma.

    Science.gov (United States)

    Heinisch, Silke; Loosemore, Michael; Cusack, Carrie A; Allen, Herbert B

    2012-09-01

    Coma blisters (CBs) are self-limited lesions that occur in regions of pressure during unconscious states classically induced by barbiturates. We report a case of CBs sans coma that were histologically confirmed in a 41-year-old woman who developed multiple tense abdominal bullae with surrounding erythema following a transatlantic flight. Interestingly, the patient was fully conscious and denied medication use or history of medical conditions. A clinical diagnosis of CBs was confirmed by histopathologic findings of eccrine gland necrosis, a hallmark of these bulIous lesions.

  4. Study on New Process of Synthesizing Pyrimidine%嘧啶合成新工艺研究

    Institute of Scientific and Technical Information of China (English)

    魏常喜; 戴立言; 王晓钟; 陈英奇

    2009-01-01

    研究了重要的医药中间体嘧啶的合成工艺,以尿素和丙二酸二乙酯为原料,在甲醇钠催化下合成巴比妥酸,并用三氯氧磷在N,N-二甲基苯胺催化下加氯成2,4,6-三氯嘧啶,将2,4,6-三氯嘧啶以钯碳催化,加氢脱氯得到嘧啶.得出每一步的最佳工艺条件,巴比妥酸合成:配料摩尔比1:1.1:1.2(丙二酸二乙酯:尿素:甲醇钠),回流,2 h;2,4,6-三氯嘧啶合成:配料摩尔比5:1(三氯氧磷:巴比妥酸),100~105℃,2 h;嘧啶合成:配料摩尔比5:1(氧化镁:2,4,6-三氯嘧啶),溶剂体积比3:1(水:乙醇),0.1 MPa,14 h,60℃.%The new process of preparing pyrimidine which is widely used as pharmaceutical intermediate was studied. Beginning from the raw material-- urea and diethyl malonate, barbituric acid was prepared with sodium methoxide as catalyst, then 2,4,6-trichloropyrimidine was synthesized by reacting of barbituric acid with phosphorus oxychloride in the presence of N,N-dimethylaniline. The object compound was prepared from 2,4,6-trichloropyrimidine by catalytic hydrogenation with palladium-charcoal as catalyst. The optimum reaction conditions for every reaction step were studied. For preparing barbituric acid, the mole ratio of diethyl malonate, urea and sodium methoxide was 1 : 1.1 : 1.2, and the mixture was refluxed 2 hours; for preparing 2,4,6-trichloropyrimidine, the mole ratio of phosphorus oxychloride and barbituric acid was 5 : 1, and the reaction was run at 100 - 105 ℃ for 2 hours; for preparing pyrimidine, the mole ratio of magnesium oxide and 2,4,6-trichloropyrimidine was 5 :1, the volume ratio of water and ethanol was 3 : 1 and the reaction was run at 0. 1 Mpa and 60 ℃ for 14 hours.

  5. Reactions of 3-Formylchromone with Active Methylene and Methyl Compounds and Some Subsequent Reactions of the Resulting Condensation Products

    Directory of Open Access Journals (Sweden)

    M. Lácova

    2005-08-01

    Full Text Available This review presents a survey of the condensations of 3-formylchromone with various active methylene and methyl compounds, e.g. malonic or barbituric acid derivatives, five-membered heterocycles, etc. The utilisation of the condensation products for the synthesis of different heterocyclic systems, which is based on the ability of the γ-pyrone ring to be opened by the nucleophilic attack is also reviewed. Finally, the applications of microwave irradiation as an unconventional method of reaction activation in the synthesis of condensation products is described and the biological activity of some chromone derivatives is noted.

  6. Synthesis and in vitro Antibacterial Activities of 5-(2,3,4,5- Tetrahydro-1 H-chromeno[2,3-dJpyrimidin-5-yl)pyrimidione Derivatives%Synthesis and in vitro Antibacterial Activities of 5-(2,3,4,5- Tetrahydro-1 H-chromeno[2,3-dJpyrimidin-5-yl)pyrimidione Derivatives

    Institute of Scientific and Technical Information of China (English)

    Cheng, Qingfang; Wang, Qifa; Tan, Ting; Wang, Mingxiao; Chen, Na

    2012-01-01

    A series of novel 5-(2,3,4,5-tetrahydro-lH-chromeno[2,3-d]pyrimidin-5-yl)pyrimidione derivatives have been synthesized from substituted salicylaldehydes and barbituric acid or 2-thiobarbituric acid in water catalyzed by phase transfer catalysis of triethylbenzyl ammonium chloride (TEBA). Elemental analysis, IR, 1HNMR, and 13C NMR elucidated the structures of all the newly synthesized compounds. In vitro antimicrobial activities of synthesized compounds have been investigated against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudornonas aeruginosa. These newly synthesized derivatives exhibited significant in vitro antibacterial activity.

  7. Synthesis of Malononitrile-Condensed Disperse Dyes and Application on Polyester and Nylon Fabrics

    Directory of Open Access Journals (Sweden)

    Yusuf Y. Lams

    2014-01-01

    Full Text Available An active methylene compound, malononitrile, was introduced into the structures of a series of disperse dyes previously prepared by coupling phloroglucinol, barbituric acid, and α and β-naphtho to 4-amino-3-nitrobenzaldehyde. The dyes were purified by recrystallization from ethanol. The purity of the dyes was examined by thin-layer chromatography (TLC and the dyes were characterized by visible absorption and Fourier transform infrared spectroscopy (FTIR. The malononitrile-condensed dyes produced deeper colours and shades with better fastness to wash, light, and perspiration on application to polyester and nylon fabrics when compared to their uncondensed analogue.

  8. The Effect of Simplified Bonding Agents on the Bond Strength to Dentin of Self-Activated Dual-Cure Resin Cements

    Science.gov (United States)

    2013-04-26

    barbituric acids , aromatic sulphonate amides and tert-butyl peroxymaleic acid in dental adhesive resin. J Polym Sci 1999;72:1655- 1668. Lee Ann...is the aim of this study to verify the accuracy of the claim so that clinicians can take advantage of its properties with the comfort of knowing it...the Incompatibilities between Simplified Dental Adhesives and Self-Cure Resin Cements……………..……30 I. Eliminate the Acid -Base Reaction…………..……………31

  9. The effects of individual housing on mice and rats

    DEFF Research Database (Denmark)

    Krohn, Thomas Cæcius; Sørensen, Dorte Bratbo; Ottesen, Jan Lund

    2006-01-01

    , growth, and behaviour was introduced, rather as a model for psychoneurosis than through any concern for animal welfare. Today, it is often stated as common knowledge in laboratory animal science textbooks that individual housing as well as isolation of rats and mice has an effect on physiology...... these animals individually without negative impact on welfare, eg by providing special housing improvements. A range of studies have shown that individual housing or isolation has effects on corticosterone, the open field behaviour, barbiturate sleeping time and the metabolism of different pharmaceuticals...

  10. Incranial hypertension management

    Directory of Open Access Journals (Sweden)

    David Gonçalves Nordon

    2009-09-01

    Full Text Available ABSTRACT Intracranial hypertension is a hazardous and common situation in the emergency room. Every effort must be made in order to avoid or reduce its secondary lesions. Advanced Trauma Life Support in the first evaluation is important, along with head computerized tomography, which is useful to identify surgical cases or anatomical lesions, and intracranial pressure monitoring. Mannitol is the mostly used drug to reduce intracranial pressure, but it must be used attentively, otherwise it may cause hypovolemic shock. Barbiturate coma and decompressive craniectomy are reserved to the refractory cases, as second tier procedures.

  11. Three-component synthesis of pyrano[2,3-d]-pyrimidine dione derivatives facilitated by sulfonic acid nanoporous silica (SBA-Pr-SO3H and their docking and urease inhibitory activity

    Directory of Open Access Journals (Sweden)

    Ghodsi Mohammadi Ziarani

    2013-01-01

    Full Text Available A straightforward and efficient method for the synthesis of pyrano[2,3-d]pyrimidine diones derivatives from the reaction of barbituric acid, malononitrile and various aromatic aldehydes using SBA-Pr-SO3H as a nanocatalyst is reported.ResultsReactions proceed with high efficiency under solvent free conditions. Urease inhibitory activity of pyrano[2,3-d]pyrimidine diones derivatives were tested against Jack bean urease using phenol red method. Three compounds of 4a, 4d and 4l were not active in urease inhibition test, but compound 4a displayed slight urease activation properties. Compounds 4b, 4k, 4f, 4e, 4j, 4g and 4c with hydrophobic substitutes on phenyl ring, showed good inhibitory activity (19.45-279.14 muM.DiscussionThe compounds with electron donating group and higher hydrophobic interaction with active site of enzyme prevents hydrolysis of substrate. Electron withdrawing groups such as nitro at different position and meta-methoxy reduced urease inhibitory activity. Substitution of both hydrogen of barbituric acid with methyl group will convert inhibitor to activator.

  12. Three-component synthesis of pyrano[2,3-d]-pyrimidine dione derivatives facilitated by sulfonic acid nanoporous silica (SBA-Pr-SO3H and their docking and urease inhibitory activity

    Directory of Open Access Journals (Sweden)

    Ziarani Ghodsi Mohammadi

    2013-01-01

    Full Text Available Abstract Background A straightforward and efficient method for the synthesis of pyrano[2,3-d]pyrimidine diones derivatives from the reaction of barbituric acid, malononitrile and various aromatic aldehydes using SBA-Pr-SO3H as a nanocatalyst is reported. Results Reactions proceed with high efficiency under solvent free conditions. Urease inhibitory activity of pyrano[2,3-d]pyrimidine diones derivatives were tested against Jack bean urease using phenol red method. Three compounds of 4a, 4d and 4l were not active in urease inhibition test, but compound 4a displayed slight urease activation properties. Compounds 4b, 4k, 4f, 4e, 4j, 4g and 4c with hydrophobic substitutes on phenyl ring, showed good inhibitory activity (19.45-279.14 μM. Discussion The compounds with electron donating group and higher hydrophobic interaction with active site of enzyme prevents hydrolysis of substrate. Electron withdrawing groups such as nitro at different position and meta-methoxy reduced urease inhibitory activity. Substitution of both hydrogen of barbituric acid with methyl group will convert inhibitor to activator.

  13. Syntheses, structural elucidation, thermal properties, theoretical quantum chemical studies (DFT and biological studies of barbituric–hydrazone complexes

    Directory of Open Access Journals (Sweden)

    Amina A. Soayed

    2015-03-01

    Full Text Available Condensation of barbituric acid with hydrazine hydrate yielded barbiturichydrazone (L which was characterized using IR, 1H NMR and mass spectra. The Co(II, Ni(II and Cu(II complexes derived from this ligand have been synthesized and structurally characterized by elemental analyses, spectroscopic methods (IR, UV–Vis and ESR and thermal analyses (TGA, DTG and DTA and the structures were further elucidated using quantum chemical density functional theory. Complexes of L were found to have the ML.nH2O stoichiometry with either tetrahedral or octahedral geometry. The ESR data showed the Cu(II complex to be in a tetragonal geometry. Theoretical investigation of the electronic structure of metal complexes at the TD-DFT/B3LYP level of theory has been carried out and discussed. The fundamental vibrational wavenumbers were calculated and a good agreement between observed and scaled calculated wavenumbers was achieved. Thermal studies were performed to deduce the stabilities of the ligand and complexes. Thermodynamic parameters, such as the order of reactions (n, activation energy ΔE∗, enthalpy of reaction ΔH∗ and entropy ΔS∗ were calculated from DTA curves using Horowitz–Metzger method. The ligand L and its complexes have been screened for their antifungal and antibacterial activities and were found to possess better biological activities compared to those of unsubstituted barbituric acid complexes.

  14. Hypnotics and Sedatives

    Science.gov (United States)

    Kabra, Pokar M.; Koo, Howard Y.; Marton, Laurence J.

    In recent years, most large hospitals have observed a marked increase in the admission of patients suffering from drug overdose. Overdose of narcotic drugs, such as the opiates, represent less of a problem on a day-to-day basis than do overdoses of prescribed drugs, such as sedatives and hypnotics. Clinical signs and symptoms for a narcotic drug overdose are very distinct, and in the majority of cases can be easily recognized by the attending physicians without the help of a toxicology laboratory. Loomis (1) reported that the majority of fatal poisonings owed to one, or a combination, of four agents: barbiturates, carbon monoxide, ethyl alcohol, and salicylates. Berry (2) estimated that 5-5'-disubstituted barbiturates were the second commonest cause of fatal poisoning in England, and that the frequency of their use was increasing. Other nonbarbiturate hypnotics involved in coma-producing incidents include glutethimide (Doriden®), methyprylon (Noludar®), and meprobamate (3, 4). In the last five years, diazepam (Valium®) has become one of the leading misused drugs (5).

  15. 静脉麻醉药的研究进展%Research progress of intravenous anesthetics

    Institute of Scientific and Technical Information of China (English)

    浦鹏飞

    2012-01-01

    Intravenous anesthetics is classified into the barbiturates and non-barbiturates. Although great progress has been made in the intravenous anesthetic pharmacokinetic-pharmacodynamic knowledge and intravenous anesthesia, no intravenous anesthetics at the present is considered to be ideal in all respects. Therefore, it is still urgent to find approaches to create an ideal anesthetic state, which is secure, smooth and easy to control.%静脉麻醉药主要分为巴比妥类药物和非巴比妥类药物,虽然静脉麻醉药药代动力学-药效学知识和静脉麻醉技术均取得了长足进步,但目前还无一种在各方面都十分理想的静脉麻醉药,所以实现安全、易控、平稳和苏醒迅速的理想麻醉状态仍是摆在我们面前最严峻的问题.

  16. Accurate and computationally efficient prediction of thermochemical properties of biomolecules using the generalized connectivity-based hierarchy.

    Science.gov (United States)

    Sengupta, Arkajyoti; Ramabhadran, Raghunath O; Raghavachari, Krishnan

    2014-08-14

    In this study we have used the connectivity-based hierarchy (CBH) method to derive accurate heats of formation of a range of biomolecules, 18 amino acids and 10 barbituric acid/uracil derivatives. The hierarchy is based on the connectivity of the different atoms in a large molecule. It results in error-cancellation reaction schemes that are automated, general, and can be readily used for a broad range of organic molecules and biomolecules. Herein, we first locate stable conformational and tautomeric forms of these biomolecules using an accurate level of theory (viz. CCSD(T)/6-311++G(3df,2p)). Subsequently, the heats of formation of the amino acids are evaluated using the CBH-1 and CBH-2 schemes and routinely employed density functionals or wave function-based methods. The calculated heats of formation obtained herein using modest levels of theory and are in very good agreement with those obtained using more expensive W1-F12 and W2-F12 methods on amino acids and G3 results on barbituric acid derivatives. Overall, the present study (a) highlights the small effect of including multiple conformers in determining the heats of formation of biomolecules and (b) in concurrence with previous CBH studies, proves that use of the more effective error-cancelling isoatomic scheme (CBH-2) results in more accurate heats of formation with modestly sized basis sets along with common density functionals or wave function-based methods.

  17. Acid-base equilibrium in aqueous solutions of 1,3-dimethylbarbituric acid as studied by 13C NMR spectroscopy

    Science.gov (United States)

    Gryff-Keller, A.; Kraska-Dziadecka, A.

    2011-12-01

    13C NMR spectra of 1,3-dimethylbarbituric acid in aqueous solutions of various acidities and for various solute concentrations have been recorded and interpreted. The spectra recorded at pH = 2 and below contain the signals of the neutral solute molecule exclusively, while the ones recorded at pH = 7 and above only the signals of the appropriate anion, which has been confirmed by theoretical GIAO-DFT calculations. The signals in the spectra recorded for solutions of pH acid-base equilibrium. The kinetic data determined this way have been used to clarify the mechanisms of these processes. The numerical analysis has shown that under the investigated conditions deprotonation of the neutral solute molecules undergoes not only via a simple transfer of the C-H proton to water molecules but also through a process with participation of the barbiturate anions. Moreover, the importance of tautomerism, or association, or both these phenomena for the kinetics of the acid-base transformations in the investigated system has been shown. Qualitatively similar changes of 13C NMR spectra with the solution pH variation have been observed for the parent barbituric acid.

  18. Management and treatment of gamma butyrolactone withdrawal syndrome: a case report and review.

    Science.gov (United States)

    Ghio, Lucio; Cervetti, Alice; Respino, Matteo; Belvederi Murri, Martino; Amore, Mario

    2014-07-01

    Gamma butyrolactone (GBL) is an increasingly popular drug of abuse that is readily available in most countries, and it is often purchased over the Internet. In addition to the acute hazards of intoxication and overdose, users who are dependent on GBL can also experience severe withdrawal reactions, including hallucinations, agitation, confusion, delusions, delirium, rhabdomyolysis, and seizures. Most of the existing literature suggests the use of a high-dose benzodiazepine as a first-line treatment for GBL withdrawal. However, several cases of resistance to benzodiazepines have been observed, which likely reflect some pharmacological differences between benzodiazepines and GBL. Specifically, the effects of benzodiazepines are primarily mediated by gamma-aminobutyric acid (GABA)-A receptors, while GBL and its analogues act mainly at GABA-B receptors, with possible additional effects via the ionotropic GABA-A receptors. In this regard, recent studies have found that GBL and its analogues possess a high affinity for a specific form of extrasynaptic GABA-A receptors that are strongly activated by barbiturates, such as phenobarbital, but that are insensitive to benzodiazepines. Taken together, these findings suggest that barbiturates could be evaluated as first-choice agents for the treatment of GBL/gamma hydroxybutyrate (GHB) withdrawal instead of benzodiazepines. In support of this view, we describe a clinical case of difficult to manage GBL withdrawal symptoms in a 42-year-old male. We also review the literature on treatment options for GBL/GHB withdrawal, including benzodiazepine-resistant withdrawal.

  19. Review of pharmacokinetic models for target controlled infusions in anesthesia

    Directory of Open Access Journals (Sweden)

    Subash Kennedy Sivasubramaniam

    2014-06-01

    Full Text Available Intravenous injection of anesthetic drugs dates back to the 17th Century when opium and chloral hydrate have been injected intravenously. It was not until the 1930s intravenous anesthesia became popular with the invention of barbiturates.Early intravenous anesthetic agents such as barbiturates were ideal for induction of anesthesia, but not suitable for maintenance of anesthesia. Most of these drugs accumulated significantly with increasing durations of infusion and also resulted in cardiorespiratory depression. The invention of propofol and shorter acting opioid analgesics such as remifentanil and alfentanil have revolutionized intravenous anesthesia. The rapid onset and offset of these drugs lends itself to being suitable agents for maintenance of anesthesia over prolonged periods of time. Detailed understanding of the pharmacokinetics of propofol and remifentanil, combined with technological advances in intravenous pumps capable of accurate delivery of drugs have resulted in great development of the field of total intravenous anesthesia and target controlled infusions. I would like to discuss, in this article, the pharmacokinetics and pharmacokinetic models behind these intravenous infusion pumps. [Int J Basic Clin Pharmacol 2014; 3(3.000: 417-423

  20. Desorption electrospray ionization (DESI) with atmospheric pressure ion mobility spectrometry for drug detection.

    Science.gov (United States)

    Roscioli, Kristyn M; Tufariello, Jessica A; Zhang, Xing; Li, Shelly X; Goetz, Gilles H; Cheng, Guilong; Siems, William F; Hill, Herbert H

    2014-04-01

    Desorption electrospray ionization (DESI) was coupled to an ambient pressure drift tube ion mobility time-of-flight mass spectrometer (IM-TOFMS) for the direct analysis of active ingredients in pharmaceutical samples. The DESI source was also coupled with a standalone IMS demonstrating potential of portable and inexpensive drug-quality testing platforms. The DESI-IMS required no sample pretreatment as ions were generated directly from tablets and cream formulations. The analysis of a range of over-the-counter and prescription tablet formations was demonstrated for amphetamine (methylphenidate), antidepressant (venlafaxine), barbiturate (Barbituric acid), depressant (alprazolam), narcotic (3-methylmorphine) and sympatholytic (propranolol) drugs. Active ingredients from soft and liquid formulations, such as Icy Hot cream (methyl salicylate) and Nyquil cold medicine (acetaminophen, dextromethorphan, doxylamine) were also detected. Increased sensitivity for selective drug responses was demonstrated through the formation of sodiated adduct ions by introducing small quantities of NaCl into the DESI solvent. Of the drugs and pharmaceuticals tested in this study, 68% (22 total samples) provided a clear ion mobility response at characteristic mobilities either as (M + H)(+), (M - H)(-), or (M + Na)(+) ions.

  1. Substance abuse and psychiatric co-morbidity as predictors of premature mortality in Swedish drug abusers a prospective longitudinal study 1970 - 2006

    Directory of Open Access Journals (Sweden)

    Hesse Morten

    2011-07-01

    Full Text Available Abstract Background Few longitudinal cohort studies have focused on the impact of substances abused and psychiatric disorders on premature mortality. The aim of the present study was to identify predictors of increased risk of drug related death and non drug related death in substance abusers of opiates, stimulants, cannabis, sedatives/hypnotics, hallucinogens and alcohol over several decades. Methods Follow-up study of a consecutive cohort of 561 substance abusers, admitted to a detoxification unit January 1970 to February 1978 in southern Sweden, and followed up in 2006. Demographic and clinical data, substance diagnoses and three groups of psychiatric diagnoses were identified at first admission. Causes of death were coded according to ICD-10 and classified as drug related deaths or non drug related deaths. To identify the incidence of some probable risk factors of drug related premature death, the data were subjected to a competing risks Cox regression analysis. Results Of 561 patients in the cohort, 11 individuals had either emigrated or could not be located, and 204/561 patients (36.4% were deceased by 2006. The cumulative risk of drug related death increased more in the first 15 years and leveled out later on when non drug related causes of death had a similar incidence. In the final model, male gender, regular use of opiates or barbiturates at first admission, and neurosis were associated with an increased risk of drug related premature death, while cannabis use and psychosis were associated with a decreased risk. Neurosis, mainly depression and/or anxiety disorders, predicted drug related premature death while chronic psychosis and personality disorders did not. Chronic alcohol addiction was associated with increased risk of non drug related death. Conclusions The cohort of drug abusers had an increased risk of premature death to the age of 69. Drug related premature death was predicted by male gender, the use of opiates or barbiturates

  2. The influence of additives on the morphology and stability of roll-to-roll processed polymer solar cells studied through ex situ and in situ X-ray scattering

    DEFF Research Database (Denmark)

    Zawacka, Natalia Klaudia; Andersen, Thomas Rieks; Andreasen, Jens Wenzel

    2014-01-01

    The effect of twelve different additives on organic solar cells with an active layer based on poly-3- hexylthiophene (P3HT) and phenyl-C61-butyric acid methyl ester (PCBM) has been studied in this work and tested for suitability in roll-to-roll slot-die coating. Three of the twelve additives......-Vis Spectroscopy and Small Angle X-ray Scattering (SAXS) for cells prepared with 1-chloronaphthalene (CN), N-methyl-2-pyrrolidone (NMP) and 1,3-dimethyl-barbituric acid (BARB) as processing additives. The studies suggested that the use of these additives resulted in films with improved morphology and electrical...... increased the solar cell efficiency while the rest showed no effect or a negative influence on the efficiency and coatability. In cases where the additive caused an increase in performance the relation to surface topography and the structure was investigated using Atomic Force Microscopy (AFM), UV...

  3. The thermodynamics of general and local anesthesia

    CERN Document Server

    Graesboll, Kaare; Heimburg, Thomas

    2014-01-01

    General anesthetics are known to cause depression of the freezing point of transitions in biomembranes. This is a consequence of ideal mixing of the anesthetic drugs in the membrane fluid phase and exclusion from the solid phase. Such a generic law provides physical justification of the famous Meyer-Overton rule. We show here that general anesthetics, barbiturates and local anesthetics all display the same effect on melting transitions. Their effect is reversed by hydrostatic pressure. Thus, the thermodynamic behavior of local anesthetics is very similar to that of general anesthetics. We present a detailed thermodynamic analysis of heat capacity profiles of membranes in the presence of anesthetics. This analysis is able to describe experimentally observed calorimetric profiles and permits prediction of the anesthetic features of arbitrary molecules. In addition, we discuss the thermodynamic origin of the cutoff-effect of long-chain alcohols and the additivity of the effect of general and local anesthetics.

  4. [Suicidal poisoning with benzodiazepines].

    Science.gov (United States)

    Chodorowski, Z; Sein Anand, J

    1997-01-01

    In the period from 1987 to 1996, 103 patients with suicidal benzodiazepines poisoning were treated, including 62 women and 41 men from 16 to 79 (mean 34) years old. 23 persons were poisoned only by benzodiazepines, in 80 remaining cases intoxications were mixed eg. including benzodiazepines and alcohol, tricyclic antidepressants, barbiturates, opioids, phenothiazines. The main causes of suicides were mainly depression, drug addiction and alcoholism. Nobody died in the benzodiazepines group, while mortality rate in the group of mixed poisoning was 4%. Prescribing benzodiazepines by physicians was quite often not justified and facilitated, among others, accumulation of the dose sufficient for suicide attempt. Flumazenil was efficient for leading out from coma in 86% of cases with poisoning only by benzodiazepines and 13% of cases with mixed intoxications mainly containing benzodiazepines and alcohol or carbamazepine.

  5. Substance Abuse and Psychiatric Co-morbidity as Predictors of Premature Mortality in Swedish Drug Abusers: A Prospective Longitudinal Study 1970-2006

    DEFF Research Database (Denmark)

    Nyhlén, Anna; Fridell, Mats; Bäckström, Martin

    2011-01-01

    Background Few longitudinal cohort studies have focused on the impact of substances abused and psychiatric disorders on premature mortality. The aim of the present study was to identify predictors of increased risk of drug related death and non drug related death in substance abusers of opiates...... with a decreased risk. Neurosis, mainly depression and/or anxiety disorders, predicted drug related premature death while chronic psychosis and personality disorders did not. Chronic alcohol addiction was associated with increased risk of non drug related death. Conclusions The cohort of drug abusers had...... and barbiturate abusers over the observed period of 37 years, while stimulant abuse did not have any impact. Alcohol contributed to non drug related death. Keywords: drug related death; risk factor; gender; competing risks Cox regression; cohort study; Predictors...

  6. Drug histories and criminality of inmates of local jails in the United States (1978): implications for treatment and rehabilitation of the drug abuser in a jail setting.

    Science.gov (United States)

    Barton, W I

    1982-04-01

    A survey by the Department of Justice in 1978 of inmates of local jails in the United States found that 68% had ever used drugs like heroin, cocaine, marijuana, amphetamines, or barbiturates outside a treatment program, and without a doctor's prescription. Offenses for which relatively larger proportions of inmates reported drug use included robbery, burglary, auto theft, larceny, and drug offenses. During the month prior to jail, 44% of inmates reported using drugs. Some 21% of convicted inmates reported being under the influence of drugs at the time of an offense for which convicted. One-fourth of inmates reporting drug use had ever been enrolled in drug treatment. Treatment and rehabilitation of the drug abuser in a jail setting is discussed.

  7. Deaths among drug addicts in Denmark in 1987-1991

    DEFF Research Database (Denmark)

    Kringsholm, Birgitte; Kaa, Elisabet; Steentoft, Anni

    1994-01-01

    increased by 1 year in the period. The main drug of abuse was heroin, in most cases supplemented by various other drugs, and in almost all cases taken intravenously. In about one-third of the cases each year there was information of abuse of alcohol in addition. In the poisoning cases, the main drug......In the period 1987–1991 a total of 739 fatalities among drug addicts was investigated at the three University Institutes of Forensic Medicine in Denmark. The annual number rose from 130–140 in the first 4 years to 192 in 1991, and 80% were males. The mean and median age for both males and females....... In about half of the methadone poisoning cases, there was information of methadone treatment at the time of death. The other half obviously obtained the methadone completely illegally. Ketobemidone was the third most frequent drug of poisoning, while propoxyphene and barbituric acid only were found...

  8. Validation of a method for the targeted analysis of 96 drugs in hair by UPLC-MS/MS

    DEFF Research Database (Denmark)

    Montesano, Camilla; Johansen, Sys Stybe; Nielsen, Marie Katrine Klose

    2014-01-01

    in drug facilitated assaults (DFA); however, chronic use (compliance) can also be examined. The method has been fully validated for the drugs included in the study. The accuracy of the method was demonstrated by the analysis of certified authentic hair samples containing common drugs of abuse. The hair......The method presented in this study allows the screening and quantification of 96 drugs, from different groups: opiates, amphetamines, hallucinogens, benzodiazepines, antihistamines, antidepressants, antipsychotics, barbiturates and other sedatives, muscle relaxants, etc. in hair. Drugs...... are extracted from 10mg of washed hair in 18h by a mixture of methanol:acetonitrile:ammonium formate (pH 5.3). Absolute recovery ranged from 70% to 106% for 75% of the analytes. The limits of detection in the low pg/mg range, may allow the detection of single dose drug exposure, with possible application...

  9. [Irreversible coma following hypoglycemia in Sheehan syndrome with adrenocortical insufficiency].

    Science.gov (United States)

    Sas, A M; Meynaar, I A; Laven, J S; Bakker, S L; Feelders, R A

    2003-08-23

    A 24-year-old woman of Somali origin delivered at term after an uncomplicated pregnancy. Post-partum haemorrhage resulted in hypovolaemic shock which was treated by hysterectomy. Five days later she became comatose due to unrecognised hypoglycaemia which caused severe irreversible brain damage and status epilepticus. Treatment in the intensive care unit with artificial respiration, prednisolone, desmopressin, inotropic support, barbiturates and an anaesthetic under EEG guidance was unsuccessful. The patient died 28 days post-partum. The hypoglycaemia was due to a combination of (a) inadequate glucose intake and (b) lack of counter-regulatory mechanisms due to a deficiency of steroids and growth hormone as a result of loss of pituitary function (Sheehan syndrome) together with adrenocortical insufficiency. The combination of Sheehan syndrome and primary adrenocortical insufficiency has not been described previously in the literature.

  10. The use of extracorporeal life support in adolescent amlodipine overdose

    Science.gov (United States)

    Persad, Elizabeth A.; Raman, Lakshmi; Thompson, Marita T.; Sheeran, Paul W.

    2012-01-01

    Calcium channel blocker (CCB) toxicity is associated with refractory hypotension and can be fatal. A 13 year old young woman presented to the emergency department(ED) six hours after an intentional overdose of amlodipine, barbiturates, and alcohol. She remained extremely hypotensive despite the administration of normal saline and calcium chloride and despite infusions of norepinephrine, epinephrine, insulin, and dextrose. Due to increasing evidence of end organ dysfunction, Extracorporeal Life Support (ECLS) was initiated 9 hours after presentation to the ED. The patient's blood pressure and end organ function immediately improved after cannulation. She was successfully decannulated after 57 hours of ECLS and was neurologically intact. Patients with calcium channel blocker overdose who are resistant to medical interventions may respond favorably to early ECLS. PMID:23559727

  11. Primate study suggests pentobarbital may help protect the brain during radiation therapy

    Energy Technology Data Exchange (ETDEWEB)

    Skolnick, A.

    1990-08-01

    Radiation therapy, an often indispensable treatment for a wide range of brain tumors, is a double-edged sword, especially when used to treat children. Research reported at the 72nd Annual Meeting of the Endocrine Society, in Atlanta, Ga., now suggests that pentobarbital and perhaps other barbiturates may help protect the brain from radiation-induced damage, especially to the pituitary and hypothalmus, where such damage can lead to serious, life-long problems for children. Jeffrey J. Olson, MD, now assistant professor of neurosurgery at Emory University School of Medicine, Atlanta, reported the results of a study of the radioprotective effects of pentobarbital on the brain of a primate, which he and colleagues at the National Institute of Neurological Disorders and Stroke recently completed.

  12. Identification and management of alcohol withdrawal syndrome.

    Science.gov (United States)

    Mirijello, Antonio; D'Angelo, Cristina; Ferrulli, Anna; Vassallo, Gabriele; Antonelli, Mariangela; Caputo, Fabio; Leggio, Lorenzo; Gasbarrini, Antonio; Addolorato, Giovanni

    2015-03-01

    Symptoms of alcohol withdrawal syndrome (AWS) may develop within 6-24 h after the abrupt discontinuation or decrease of alcohol consumption. Symptoms can vary from autonomic hyperactivity and agitation to delirium tremens. The gold-standard treatment for AWS is with benzodiazepines (BZDs). Among the BZDs, different agents (i.e., long-acting or short-acting) and different regimens (front-loading, fixed-dose or symptom-triggered) may be chosen on the basis of patient characteristics. Severe withdrawal could require ICU admission and the use of barbiturates or propofol. Other drugs, such as α2-agonists (clonidine and dexmetedomidine) and β-blockers can be used as adjunctive treatments to control neuroautonomic hyperactivity. Furthermore, neuroleptic agents can help control hallucinations. Finally, other medications for the treatment for AWS have been investigated with promising results. These include carbamazepine, valproate, sodium oxybate, baclofen, gabapentin and topiramate. The usefulness of these agents are discussed.

  13. Ten-minute analysis of drugs and metabolites in saliva by surface-enhanced Raman spectroscopy

    Science.gov (United States)

    Shende, Chetan; Inscore, Frank; Maksymiuk, Paul; Farquharson, Stuart

    2005-11-01

    Rapid analysis of drugs in emergency room overdose patients is critical to selecting appropriate medical care. Saliva analysis has long been considered an attractive alternative to blood plasma analysis for this application. However, current clinical laboratory analysis methods involve extensive sample extraction followed by gas chromatography and mass spectrometry, and typically require as much as one hour to perform. In an effort to overcome this limitation we have been investigating metal-doped sol-gels to both separate drugs and their metabolites from saliva and generate surface-enhanced Raman spectra. We have incorporated the sol-gel in a disposable lab-on-a-chip format, and generally no more than a drop of sample is required. The detailed molecular vibrational information allows chemical identification, while the increase in Raman scattering by six orders of magnitude or more allows detection of microg/mL concentrations. Measurements of cocaine, its metabolite benzoylecgonine, and several barbiturates are presented.

  14. Rare, potentially fatal, poorly understood propofol infusion syndrome

    Directory of Open Access Journals (Sweden)

    Eva Annen

    2012-09-01

    Full Text Available We present the case of a 7-year old boy with traumatic brain injury who received propofol during 38 h. Thirty-six hours after cessation of propofol infusion asystole occurred. After immediate mechanical and medical resuscitation, unreactive dilated pupils were observed. The following computed tomography scan revealed a generalized brain edema with transtentorial herniation. Prolonged bradyarrhythmia, rhabdomyolysis, and peracute renal failure were observed. Despite immediate craniectomy, barbiturate treatment, hemofiltration, and recovery of appropriate cardiac function, the patient died four days after discontinuation of propofol. In this case, metabolic acidosis, cardiac failure, rhabdomyolysis, and renal failure are in accordance with the symptoms of propofol infusion syndrome (PRIS, while seizure, brain edema, and transtentorial herniation could be caused by traumatic brain injury. However, it may be assumed that the entire clinical picture was caused by PRIS. This view could be explained by a common loss of function of ryanodine receptors in patients presenting with PRIS.

  15. Acute severe poisoning in Spain: clinical outcome related to the implicated drugs.

    Science.gov (United States)

    Frati, M E; Marruecos, L; Porta, M; Martín, M L; Laporte, J R

    1983-10-01

    The 91 patients over the age of 10 (57 women and 32 men) with severe self-poisoning admitted to the ICU of a general hospital in Barcelona during the period 1974-1980 have been retrospectively studied. Previous suicidal attempts have been identified among 32 patients; 26 patients presented a history of personality disorders, and 19 had a neurological disease, a chronic physical illness, or a history of alcoholism. Sedative-hypnotic drugs were involved in about half the number of cases, and one fifth of total cases were due to tricyclic antidepressants and phenothiazines. Paracetamol was only involved in 2 cases, and heroin in another 2 cases. Many of the most severe morbidity manifestations were related to overdoses by intermediate-acting barbiturates. Two out of a total of 5 deaths were related to butalbitone overdose. Butalbitone had been ingested as a fixed-dose combination containing butalbitone, propyphenazone, and caffeine, which is freely dispensed as an analgesic in Spain.

  16. Physiological antioxidant system and oxidative stress in stomach cancer patients with normal renal and hepatic function

    Directory of Open Access Journals (Sweden)

    E Prabhakar Reddy

    2010-04-01

    Full Text Available Role of free radicals has been proposed in the pathogenesis of many diseases. Gastric cancer is a common disease worldwide, and leading cause of cancer death in India. Severe oxidative stress produces reactive oxygen species (ROS and induces uncontrolled lipid peroxidation. Albumin, uric acid (UA and Bilirubin are important physiological antioxidants. We aimed to evaluate and assess the role of oxidative stress (OS and physiological antioxidant system in stomach cancer patients. Lipid peroxidation measured as plasma Thio Barbituric Acid Reactive substances (TBARS, was found to be elevated significantly (p=0.001 in stomach cancer compared to controls along with a decrease in plasma physiological antioxidant system. The documented results were due to increased lipid peroxidation and involvement of physiological antioxidants in scavenging free radicals but not because of impaired hepatic and renal functions.

  17. The use of extracorporeal life support in adolescent amlodipine overdose

    Directory of Open Access Journals (Sweden)

    Elizabeth A Persad

    2012-01-01

    Full Text Available Calcium channel blocker (CCB toxicity is associated with refractory hypotension and can be fatal. A 13 year old young woman presented to the emergency department(ED six hours after an intentional overdose of amlodipine, barbiturates, and alcohol. She remained extremely hypotensive despite the administration of normal saline and calcium chloride and despite infusions of norepinephrine, epinephrine, insulin, and dextrose. Due to increasing evidence of end organ dysfunction, Extracorporeal Life Support (ECLS was initiated 9 hours after presentation to the ED. The patient′s blood pressure and end organ function immediately improved after cannulation. She was successfully decannulated after 57 hours of ECLS and was neurologically intact. Patients with calcium channel blocker overdose who are resistant to medical interventions may respond favorably to early ECLS.

  18. Hydrogen bonding in tight environments

    DEFF Research Database (Denmark)

    Pirrotta, Alessandro; Solomon, Gemma C.; Franco, Ignacio

    2016-01-01

    The single-molecule force spectroscopy of a prototypical class of hydrogen-bonded complexes is computationally investigated. The complexes consist of derivatives of a barbituric acid and a Hamilton receptor that can form up to six simultaneous hydrogen bonds. The force-extension (F-L) isotherms...... of the host-guest complexes are simulated using classical molecular dynamics and the MM3 force field, for which a refined set of hydrogen bond parameters was developed from MP2 ab initio computations. The F-L curves exhibit peaks that signal conformational changes during elongation, the most prominent...... of which is in the 60-180 pN range and corresponds to the force required to break the hydrogen bonds. These peaks in the F-L curves are shown to be sensitive to relatively small changes in the chemical structure of the host molecule. Thermodynamic insights into the supramolecular assembly were obtained...

  19. Spontaneous formation and base pairing of plausible prebiotic nucleotides in water.

    Science.gov (United States)

    Cafferty, Brian J; Fialho, David M; Khanam, Jaheda; Krishnamurthy, Ramanarayanan; Hud, Nicholas V

    2016-04-25

    The RNA World hypothesis presupposes that abiotic reactions originally produced nucleotides, the monomers of RNA and universal constituents of metabolism. However, compatible prebiotic reactions for the synthesis of complementary (that is, base pairing) nucleotides and mechanisms for their mutual selection within a complex chemical environment have not been reported. Here we show that two plausible prebiotic heterocycles, melamine and barbituric acid, form glycosidic linkages with ribose and ribose-5-phosphate in water to produce nucleosides and nucleotides in good yields. Even without purification, these nucleotides base pair in aqueous solution to create linear supramolecular assemblies containing thousands of ordered nucleotides. Nucleotide anomerization and supramolecular assemblies favour the biologically relevant β-anomer form of these ribonucleotides, revealing abiotic mechanisms by which nucleotide structure and configuration could have been originally favoured. These findings indicate that nucleotide formation and selection may have been robust processes on the prebiotic Earth, if other nucleobases preceded those of extant life.

  20. Use of toxicity assays for evaluating the effectiveness of groundwater remediation with Fenton’s reagent

    DEFF Research Database (Denmark)

    Kusk, Kresten Ole; Bennedsen, Lars; Christophersen, Mette;

    2011-01-01

    A chemical dump site adjacent to the Danish North Sea holds a variety of constituents from pharmaceutical production including sulfonamides, barbiturates, aniline, pyridine, phenols, benzene, toluene, chlorinated solvents, lithium, copper, lead, mercury, etc. An on-going pilot scale project...... for toxicity and contaminant chemistry. Organisms exposed to a mixture will react to all contaminants present and, consequently, the toxic effect will represent a sum effect. In contrast, chemical analyses yield information on individual or possibly groups of contaminants but not necessarily all...... the contaminants. Thus, using a combination of chemical analyses and toxicity assays yields a more robust understanding of the contaminated site and the risk it poses to the environment. Ground water samples were tested via toxicity assay using algae, crustaceans, luminescent bacteria, nitrifying bacteria...

  1. Use of toxicity assays for evaluating the effectiveness of groundwater remediation with Fenton’s reagent

    DEFF Research Database (Denmark)

    Kusk, Kresten Ole; Bennedsen, Lars Rønn; Christophersen, Mette;

    A chemical dump site adjacent to the Danish North Sea holds a variety of constituents from pharmaceutical production including sulfonamides, barbiturates, aniline, pyridine, phenols, benzene, toluene, chlorinated solvents, lithium, copper, lead, mercury, etc. An on-going pilot scale project...... for toxicity and contaminant chemistry. Organisms exposed to a mixture will react to all contaminants present and, consequently, the toxic effect will represent a sum effect. In contrast, chemical analyses yield information on individual or possibly groups of contaminants but not necessarily all...... the contaminants. Thus, using a combination of chemical analyses and toxicity assays yields a more robust understanding of the contaminated site and the risk it poses to the environment. Ground water samples were tested via toxicity assay using algae, crustaceans, luminescent bacteria, nitrifying bacteria...

  2. [Treatment of head injury coma with prolonged pentobarbital anaesthesia (author's transl)].

    Science.gov (United States)

    Artru, F; Guerin, J M; Latarjet, J; Deleuze, R

    1981-04-11

    Forty-five patients in deep coma resulting from head injury were treated with pentobarbital in doses adjusted to maintain serum barbiturate levels between 15 and 25 mg/l and short burst suppression phases on EEG. Brain death occurred in 20%. The overall mortality rate was 60%, no death being attributable to treatment; 24% of the patients were able to resume active life. Patients with non-reactive pupils during the early phase of coma were compared with patients of similar ages and neurological symptoms non treated with pentobarbital. In treated patients the incidence of brain death was reduced by 50% and the mortality rate by 25% (p less than 0.05), without increase in deaths from intercurrent complications and in severe sequelae among survivors.

  3. ASPECTOS MORFOLÓGICOS DO PROVENTRÍCULO E VENTRÍCULO GÁSTRICO DE Crypturellus parvirostris (WAGLER, 1827

    Directory of Open Access Journals (Sweden)

    Vinícius Bentivóglio Costa Silva

    2013-03-01

    Full Text Available The aim of the present study was to evaluate the morphological characteristics of the proventriculus and gastric ventricle of Crypturellus parvirostris. Two adult males were used, with a mean weight of 939 ± 12.7 g, from the region of Araguaína, State of Tocantins. After capture, the birds were euthanized through intravenous application of 2.5% sodium thiopental until barbiturate coma was attained. Then, they were necropsied and their organs and viscera were evaluated morphologically. The anatomical and histological characteristics of the proventriculus and gastric ventricle of C. parvirostris were similar to those of other tinamid species, but there is a lack of morphological data related to the family Tinamidae.

  4. [Pharmacological treatment of syndromes of aggressivity].

    Science.gov (United States)

    Itil, T M

    1978-01-01

    In the treatment of violent-aggressive behavior, four major groups of drugs emerged: 1. Major tranquilizers in the treatment of aggressive-violent behavior associated with psychotic syndromes. 2. Anti-epileptic drugs such as diphenylhydantoin and barbiturates in the treatment of aggressive-violent behavior within the epileptic syndrome. 3. Psychostimulants in the treatment of aggressive behavior of adolescents and children within behavior disturbances. 4. Anti-male hormones such as cyproterone acetate in the treatment of violent-aggressive behavior associated with pathological sexual hyperactivity. Whereas each category of drug is predominantly effective in one type of aggressive syndrome, it may also be effective in other conditions as well. Aggression as a result of a personality disorder is most difficult to treat with drugs.

  5. Elevated striatal Fos immunoreactivity following 6-hydroxydopamine lesioning of the rat is mediated by excitatory amino acid transmission.

    Science.gov (United States)

    Cooper, A J; Wooller, S; Mitchell, I J

    1995-07-14

    Pharmacological depletion of dopaminergic neurotransmission can result in an elevation in striatal Fos levels. This elevation may occur as a direct result of decreased dopaminergic neurotransmission or indirectly via elevated corticostriatal glutamatergic neurotransmission which occurs secondary to dopamine depletion. To test the hypothesis that elevated N-methyl-D-aspartic acid (NMDA)-mediated corticostriatal transmission may underlie the increase in striatal Fos levels upon dopamine depletion, rats were unilaterally 6-hydroxydopamine lesioned under anaesthesia induced by either barbiturate or the NMDA antagonist, ketamine. Following surgery the animals remained under light anaesthesia for 6 h prior to sacrifice and quantification of striatal Fos immunoreactivity. The results demonstrate that dopamine depletion following 6-hydroxydopamine lesioning can result in elevated striatal Fos levels which can be attenuated by contiguous treatment with an NMDA antagonist. This suggests that the increase in striatal Fos levels observed following dopamine depletion may occur as a result of elevated cytoplasmic calcium levels in the striatal cells.

  6. Coma blisters in children: case report and review of the literature.

    Science.gov (United States)

    Bosco, Laura; Schena, Donatella; Colato, Chiara; Biban, Paolo; Girolomoni, Giampiero

    2013-12-01

    Coma-induced blisters is a rare condition associated with prolonged impairment of conscious level, which is relatively well-known in adults following overdose with barbiturates. However, it has been very rarely described in children. A case of coma-bullae occurring in an 11-year-old child with meningoencephalitis is herein reported. The bullous lesions occurred on the limbs and trunks, and evolved into necrotic ulcers in a few days. No correlation with any drug overdosage was found. A skin biopsy revealed epidermal and eccrine sweat gland necrosis with abundant neutrophils, and thrombosis of the vessels in the lower dermis. A comprehensive review of the literature showed that only 5 cases of coma-bullae in children have been published so far. Coma blistering resolves spontaneously within days or weeks. Diagnosis of coma-bullae may require careful clinical-pathologic correlation to exclude other blistering diseases in children.

  7. Anticonvulsant medications: an iatrogenic cause of tic disorders.

    Science.gov (United States)

    Burd, L; Kerbeshian, J; Fisher, W; Gascon, G

    1986-06-01

    A review of the relationship between anticonvulsant medications and tics is presented. Data on 5 patients in whom anticonvulsants, either caused tics or exacerbated existing tic disorders is discussed. Discontinuation of the medication resulted in a decrease in the frequency of tickings in all patients. The effects of anticonvulsants on the reticular system are discussed. It is felt that it may be important for clinicians to consider carefully the use of barbiturate anticonvulsants, especially phenobarbital, in children with tics or a family history of tics. Tic disorders caused or exacerbated by exposure to anticonvulsant medications appear to be more common than previously reported, and in some patients the tics may not remit with discontinuation of the medication.

  8. A non-invasive method of qualitative and quantitative measurement of drugs.

    Science.gov (United States)

    Westerman, S T; Gilbert, L M

    1981-09-01

    Methods for quick qualitative and quantitative evaluation of drug intake are needed, especially during emergency situations such as drug overdose and alcohol intoxication. The electronystagmograph was used in an attempt to develop a non-invasive method for identification of drug intake, and to study the effects of alcohol and other drugs on the vestibular system. Results of the study reveal that alcohol, diazepam, opiates, barbiturates, cocaine, marijuana, and hallucinogenic drugs produce a characteristic printout pattern which can be evaluated qualitatively. This method is a practical, non-invasive, objective procedure that provides rapid assessment of quality of drug intake. Its potential uses are extensive, including such possibilities as evaluation of drug intake in emergency drug overdose situations, monitoring anesthesia during surgery, evaluating drug intake in women about to deliver, (as well as the effects on the newborn), and determining whether or not persons who are being tested on a polygraph are under the influence of drugs.

  9. Prolonged treatment of refractory status epilepticus in a child.

    Science.gov (United States)

    Sahin, M; Riviello, J J

    2001-02-01

    Barbiturate anesthesia, which is commonly used for refractory status epilepticus, is an effective treatment, but with many significant complications. The relationship between the duration of this extreme therapy and the ultimate outcome of refractory status epilepticus has not been well studied. We report a 7-year-old girl who presented with refractory status epilepticus secondary to presumed encephalitis with a focal lesion on cranial magnetic resonance imaging. She was treated for 70 days with high-dose antiepileptic drugs and recovered with a residual seizure disorder. This case suggests that, if the status epilepticus is due to a reversible cause such as encephalitis, neurologic recovery may occur despite this very prolonged course of extreme therapy.

  10. 1-Phenoxy-2-propanol is a useful anaesthetic for gastropods used in neurophysiology.

    Science.gov (United States)

    Wyeth, Russell C; Croll, Roger P; Willows, A O Dennis; Spencer, Andrew N

    2009-01-30

    Anaesthesia is often used in neurophysiological, surgical, and neuroanatomical protocols. Several anaesthetics, including magnesium chloride, volatiles (halothane, etc.), and barbiturates, have been used in gastropod neurobiology. 1-Phenoxy-2-propanol (PP) is another anaesthetic option that has not yet been used extensively. We provide an analysis of the neural, muscular and behavioural effects of PP in gastropods. PP eliminates action potentials and reduces muscular contraction force in Hermissenda crassicornis, and eliminates behavioural activity in Tritonia diomedea. Our results show these effects are reversible, with complete action potential recovery, at least partial muscular recovery, and full behavioural recovery. Survival after surgery in T. diomedea was longer with PP than without anaesthetic, and PP also reduced contraction during tissue fixation in Lymnaea stagnalis. Moreover, PP can be bath applied, has low toxicity, and is biodegradable. Thus, PP is an effective anaesthetic in three species of gastropods, and useful in neurophysiological dissection, surgical, and fixation protocols.

  11. Neonatal abstinence syndrome: Pharmacologic strategies for the mother and infant.

    Science.gov (United States)

    Kraft, Walter K; Stover, Megan W; Davis, Jonathan M

    2016-04-01

    Opioid use in pregnancy has increased dramatically over the past decade. Since prenatal opioid use is associated with numerous obstetrical and neonatal complications, this now has become a major public health problem. In particular, in utero opioid exposure can result in neonatal abstinence syndrome (NAS) which is a serious condition characterized by central nervous system hyperirritability and autonomic nervous system dysfunction. The present review seeks to define current practices regarding the approach to the pregnant mother and neonate with prenatal opiate exposure. Although the cornerstone of prenatal management of opioid dependence is opioid maintenance therapy, the ideal agent has yet to be definitively established. Pharmacologic management of NAS is also highly variable and may include an opioid, barbiturate, and/or α-agonist. Genetic factors appear to be associated with the incidence and severity of NAS. Establishing pharmacogenetic risk factors for the development of NAS has the potential for creating opportunities for "personalized genomic medicine" and novel, individualized therapeutic interventions.

  12. Fixed drug eruption due to paracetamol

    Directory of Open Access Journals (Sweden)

    Anjali Kushwah

    2013-12-01

    Full Text Available Fixed drug eruption is a common type of drug eruption seen in dermatology OPD’s. Usually it is seen with sulphonamides, salicylates, tetracyclines, oxyphenbutazones, dapsone, barbiturates, phenolphthalein, morphine, codeine, quinine, phenacetin, erythromycin, griseofulvin, mebendazole etc. We hereby report a case of fixed drug eruption due to single dose of oral paracetamol in an otherwise healthy male after one hour of consuming it. A provisional diagnosis of Paracetamol induced fixed drug eruption was made. Paracetamol was stopped and patient advised never to take Paracetamol in future. Patient was managed with prednisolone 10mg /day, cetirizine 10 mg/day, and amoxicillin 500 mg twice a day and mometasone + fusidic acid cream to be applied over the lesions. [Int J Basic Clin Pharmacol 2013; 2(6.000: 833-835

  13. Spindle-like activity appearing during paradoxical sleep in rats with iron-induced cortical focus.

    Directory of Open Access Journals (Sweden)

    Uezu,Eiko

    1982-06-01

    Full Text Available Under barbiturate anesthesia, male Wistar rats weighing 250-300 g were injected with 2.5 microliters of 0.2 M FeCl3 solution into the left sensori-motor cortex to induce an epileptic focus with minimal abnormal activities. Polygraphy started 1 week after the surgery, showed a spindle-like hypersynchronous activity that appeared not only in the slow wave sleep period but also during paradoxical sleep (PS. This activity had a frequency of 8-14 Hz. The amplitude was more than 200 mu v in the right (non-injected side cortex but very small in the left cortex (injected side. Isolated spike discharges were observed in an ECoG of slow wave sleep. Apart from this activity there was nothing resembling the usual sleep spindles.

  14. Part-body and multibody effects on absorption of radio-frequency electromagnetic energy by animals and by models of man

    Science.gov (United States)

    Gandhi, O. P.; Hagmann, M. J.; Dandrea, J. A.

    1979-01-01

    Fine structure in the whole-body resonant curve for radio-frequency energy deposition in man can be attributed to part-body resonances. As for head resonance, which occurs near 350 MHz in man, the absorptive cross section is nearly three times the physical cross section of the head. The arm has a prominent resonance at 150 MHz. Numerical solutions, antenna theory, and experimental results on animals have shown that whole-body energy deposition may be increased by 50 percent or more because of multiple bodies that are strategically located in the field. Empirical equations for SARs are also presented along with test data for several species of laboratory animals. Barbiturate anesthesia is sufficiently disruptive of thermoregulation that delta Ts of colonic temperature yield energy dose values in several mammals that compare quite favorably with those based on whole-body calorimetry.

  15. The ketogenic diet as broad-spectrum treatment for super-refractory pediatric status epilepticus: challenges in implementation in the pediatric and neonatal intensive care units.

    Science.gov (United States)

    Cobo, Nicole H; Sankar, Raman; Murata, Kristina K; Sewak, Sarika L; Kezele, Michele A; Matsumoto, Joyce H

    2015-02-01

    Refractory status epilepticus carries significant morbidity and mortality. Recent reports have promoted the use of the ketogenic diet as an effective treatment for refractory status epilepticus. We describe our recent experience with instituting the ketogenic diet for 4 critically ill children in refractory status epilepticus, ranging in age from 9 weeks to 13.5 years after failure of traditional treatment. The ketogenic diet allowed these patients to be weaned off continuous infusions of anesthetics without recurrence of status epilepticus, though delayed ketosis and persistently elevated glucose measurements posed special challenges to effective initiation, and none experienced complete seizure cessation. The ease of sustaining myocardial function with fatty acid energy substrates compares favorably over the myocardial toxicity posed by anesthetic doses of barbiturates and contributes to the safety profile of the ketogenic diet. The ketogenic diet can be implemented successfully and safely for the treatment of refractory status epilepticus in pediatric patients.

  16. FIXED DRUG ERUPTION DUE TO METRONIDAZOLE: REVIEW OF LITERATURE AND A CASE REPORT

    Directory of Open Access Journals (Sweden)

    Wahlang JB

    2012-03-01

    Full Text Available Fixed drug eruption (FDE is common type of drug eruption seen in skin clinics. FDE usually occurs within hours of administration of the offending agent. Most commonly implicated are sulphonamides, salicylates, oxyphenbutazones, tetracycline, dapsone, chlordiazepoxide, barbiturates, phenolphthalein, morphine, codeine,quinine and derivatives, phenacetin, erythromycin, griseofulvin, mebendazole, meprobamate etc. We hereby report a case of fixed drug eruption on glans penis due to metronidazole, a nitroimidazole-derivative clinically indicated in trichomoniasis, amebiasis, giardiasis, anaerobic and mixed antibacterial infections. A patientadministered metronidazole IV developed erythematous superficial non-tender ulceration over the glans penis on the second day of treatment with Inj. Metronidazole. A provisional diagnosis of metronidazole induced fixed drug eruption was made, metronidazole inj. was stopped and the patient was managed with Tab. Prednisolone30mg/day tapered over 10 days and Fusidic acid+Betamethasone cream.

  17. Uptake and incorporation of pyrimidines in Euglena gracilis.

    Science.gov (United States)

    Wasternack, C H

    1976-08-01

    In photoorganotrophically grown cells of Euglena gracilis the uptake and incorporation degree of 12 different pyrimidines were tested. The rate of uptake of pyrimidines has distinct maxima in the late log phase and in the stationary phase of cell multiplication. The kinetics of uptake are linear in the first 2 h, do not show saturation at various concentrations and increase with the concetrations. No accumulation of the pyrimidines at various concentrations could be observed in the first 2 h of incubation. Membrane inhibitors as uranyl acetate inhibit the uptake of the reference substance alpha-AIB, which is wellknown transported by an active transport mechanism, but have no effect on uptake rate of uracil and cytosine. It could not be observed an energy requirement tested in temperature dependence and with electron transport inhibitors. Uptake of uridine, uracil, barbituric acid and alpha-AIB is inhibited by cycloheximide in a different manner after 5 - 10 min.

  18. Binding of (/sup 3/H)ethyl-. beta. -carboline-3-carboxylate to brain benzodiazepine receptors. Effect of drugs and anions

    Energy Technology Data Exchange (ETDEWEB)

    Williams, E.F.; Paul, S.M.; Rice, K.C.; Skolnick, P. (National Institutes of Health, Bethesda, MD (USA)); Cain, M. (Wisconsin Univ., Milwaukee (USA). Dept. of Chemistry)

    1981-09-28

    It is reported that in contrast to the changes in affinity of (/sup 3/H)benzodiazepines elicited by halide ions, barbiturates, and pyrazolopyridines, the apparent affinity of ..beta..-(/sup 3/H)CCE (ethyl-..beta..-carboline-3-carboxylate) is unaffected by these agents. Furthermore, Scatchard analysis of ..beta..-(/sup 3/H)CCE binding to cerebral cortical and cerebellar membranes revealed a significantly greater number of binding sites than was observed with either (/sup 3/H)diazepam or (/sup 3/H)flunitazepam, suggesting that at low concentrations benzodiazepines selectively label a subpopulation of the receptors labelled with ..beta..-(/sup 3/H)CCE. Alternatively, ..beta..-(/sup 3/H)CCE may bind to sites that are distinct from those labelled with (/sup 3/H)-benzodiazepines.

  19. Structural determinants for the inhibitory ligands of orotidine-5′-monophosphate decarboxylase

    Energy Technology Data Exchange (ETDEWEB)

    Meza-Avina, Maria Elena; Wei, Lianhu; Liu, Yan; Poduch, Ewa; Bello, Angelica M.; Mishra, Ram K.; Pai, Emil F.; Kotra, Lakshmi P. (TGRI); (Toronto)

    2010-06-14

    In recent years, orotidine-5{prime}-monophosphate decarboxylase (ODCase) has gained renewed attention as a drug target. As a part of continuing efforts to design novel inhibitors of ODCase, we undertook a comprehensive study of potent, structurally diverse ligands of ODCase and analyzed their structural interactions in the active site of ODCase. These ligands comprise of pyrazole or pyrimidine nucleotides including the mononucleotide derivatives of pyrazofurin, barbiturate ribonucleoside, and 5-cyanouridine, as well as, in a computational approach, 1,4-dihydropyridine-based non-nucleoside inhibitors such as nifedipine and nimodipine. All these ligands bind in the active site of ODCase exhibiting distinct interactions paving the way to design novel inhibitors against this interesting enzyme. We propose an empirical model for the ligand structure for rational modifications in new drug design and potentially new lead structures.

  20. Langmuir monolayer and Langmuir-Blodgett films formed by a melamine-headed azobenzene-derived amphiphile: interfacial assembly affected by host-guest interaction.

    Science.gov (United States)

    Xu, Weihong; Wang, Yanhua; Xiao, Yunxia; Liu, Fang; Lu, Guo-Yuan

    2009-04-09

    A novel azobenzene-derived amphiphile with a melamine head, 2Azo-2C12H2-melamine, has been synthesized. pi-A isotherm measurements displayed that this amphiphile is able to form a stable Langmuir monolayer on both pure water and barbituric acid (BA)- or thymine (T)-containing subphases. The collapse surface pressure and limiting molecular area of its Langmuir monolayer on pure water are 40 mN/m and 0.56 nm2, respectively. However, when barbituric acid or thymine was introduced into the subphase, the corresponding pi-A isotherms of the monolayers exhibited a lower collapse surface pressure (22 mN/m for BA, 21 mN/m for T) and smaller limiting molecular area (0.54 nm2 for BA and 0.52 nm2 for T). UV-vis and FT-IR studies of the LB films formed by 2Azo-2C12H25-melamine have also been carried out. The results indicated that the LB films of 2Azo-2C12H25-melamine deposited from pure water undergo distinct collapse of the H-aggregate upon UV irradiation, while the LB films deposited from a BA- or T-containing subphase retain the H-aggregate. The host-guest-interaction-induced blockage of azobenzene photoisomerization should be responsible for the stabilized H-aggregate. A 1:1 host/guest binding mode to form a linear supramolecular polymeric chain has been proposed in the Langmuir monolayers formed on a BA- or T-containing subphase. The current results suggest that the host-guest interaction should be an effective means to manipulate the interfacial assembly of azobenzene-derived amphiphiles.

  1. Plurality of anxiety and depression alteration mechanism by oleanolic acid.

    Science.gov (United States)

    Fajemiroye, James O; Galdino, Pablinny M; Florentino, Iziara F; Da Rocha, Fabio F; Ghedini, Paulo C; Polepally, Prabhakar R; Zjawiony, Jordan K; Costa, Elson A

    2014-10-01

    Our study sought to evaluate the anxiolytic and antidepressant activities of oleanolic acid as well as the neural mechanisms involved. Animal models such as barbiturate sleep-induction, light-dark box, elevated plus maze, forced swimming test, tail suspension test and open field test were conducted. Male Albino Swiss mice were treated orally with vehicle 10 mL/kg, fluoxetine 20 mg/kg, imipramine 15 mg/kg, diazepam 1 mg/kg or oleanolic acid 5-40 mg/kg. Pretreatment (intraperitoneal) of animals with pentylenetetrazole (PTZ) 20 mg/kg, 1-(2-methoxyphenyl)-4-[4- (2-phthalimido) butyl]piperazine hydrobromide (NAN-190) 0.5 mg/kg, p-chlorophenylalanine methyl ester (PCPA) 100 mg/kg or α-methyl-p-tyrosine (AMPT) 100 mg/kg, WAY100635 (WAY) 0.3 mg/kg, prazosin (PRAZ) 1 mg/kg, yohimbine 2 mg/kg as well as monoamine oxidase assay and hippocampal brain-derived neurotrophic factor (BDNF) quantification were carried out. Oleanolic acid potentiated the hypnotic effect of barbiturate and demonstrated an anxiolytic effect in both the light-dark box and elevated plus maze. This effect was not reversed by PTZ. Acute and/or chronic oral treatment of mice with oleanolic acid (5-20 mg/kg) elicited an antidepressant effect in the forced swimming test and the tail suspension test without interfering with the locomotor activity. The antidepressant effect of oleanolic acid was attenuated by NAN-190, AMPT, PCPA, WAY and PRAZ. Although monoamine oxidase activity remained unaltered by oleanolic acid, chronic administration of oleanolic acid augmented hippocampal BDNF level. These findings demonstrate multiple mechanisms of the anxiolytic and antidepressant effect of oleanolic acid.

  2. Biochemical, Histological And Histochemical Studies On The Effect Of Sodium Barbital On The Renal Tissue Of Albino Mice

    Directory of Open Access Journals (Sweden)

    Samia M. Sakr*, Shadia Ali Radwan*, Aziza M. El Wessemy

    2008-03-01

    Full Text Available Introduction:Anaesthetic drugs are nowadays used on a large scale in surgical operations as well as in other various medical purposes. Sodium barbital is a derivative of barbituric acid and is widely used on short surgical operations and other various medication. However, such anaesthetic drug has been reported to evoke many serious alterations as a result of its application. Materials and Methods:The experimental animals (30 mice-weighing 25-30 g were divided into 3 groups (10/group, the first group served as a control group (i.e. injection with saline, while the other two groups were treated daily with the therapeutic dose of 60 mg/kg.b.wt sodium barbital (i.p. for 7 days (short-term group and 21 days (long-term group as repeated daily doses. Blood sera and kidney samples were collected for physiological, histological and histochemical studies. Results:The results obtained showed a significant increase in urea, blood urea nitrogen, uric acid and creatinine levels in all treated groups. On the other hand serum total protein and albumin levels showed a significant decrease in both treated groups, while the globulin showed a significant decrease only in the long term group. The applied dose of sodium barbital caused histophathological alterations in the renal tissue mainly in the cortex such as damage and shrinkage of the Malpighian corpuscles, cloudy swelling and necrosis of the cells of the proximal convoluted tubules. Also, distal convoluted tubules exhibited degenerated features. In the histochemical studies, polysaccharides were progressively reduced in both short and long-term groups, while the total proteins showed a reduction in the short term group and considerably increase in the long term group. Conclusion: So these results came to conclusion that barbiturates should be prohibited and carefully used specially when prescribed as tranquilizer

  3. Drug screening in urine by cloned enzyme donor immunoassay (CEDIA) and kinetic interaction of microparticles in solution (KIMS): a comparative study.

    Science.gov (United States)

    Schwettmann, Lutz; Külpmann, Wolf-Rüdiger; Vidal, Christian

    2006-01-01

    Two commercially available drug-screening assays were evaluated: the Roche kinetic interaction of microparticles in solution (KIMS) assay and the Microgenics cloned enzyme donor immunoassay (CEDIA). Urine samples from known drug-abuse patients were analyzed for amphetamines, barbiturates, benzodiazepines, benzoylecgonine, cannabinoids, LSD, methadone and opiates. Samples with discordant findings for the two assays were analyzed by gas chromatography/mass spectrometry (GC/MS) or gas chromatography/electron capture detection (GC/ECD). Amphetamines showed 96.0% concordant results, with two false positive findings by CEDIA, three by KIMS and a further two false negatives by KIMS. Barbiturates showed 99.4% concordant results, with one false negative by KIMS. Benzodiazepines showed 97.4% concordant results, with two false negatives by KIMS (cutoff 100 microg/L, CEDIA cutoff 300 microg/L). Benzoylecgonine showed 17.8% concordant positive and 82.2% concordant negative results and no false finding by either assay. Cannabinoids showed 99.3% concordant results, with one sample negative by KIMS at a cutoff of 50 microg/L and positive by CEDIA (cutoff 25 microg/L). For LSD, 6.7% of findings were not in agreement. Methadone showed 97.5% concordant results, with two false positives by CEDIA, and one false positive and one false negative by KIMS. Opiates showed 96.9% concordant results, with no false KIMS results, but four false positives by CEDIA. The results indicate that the agreement of the CEDIA and KIMS results for the eight drugs is rather good (93.3-100%).

  4. Hypnotic effect of ecdysterone isolated from Pfaffia glomerata (Spreng. Pedersen Efeito hipinótico de ecdisterona isolada de Pfaffia glomerata (Spreng. Pedersen

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    Raquel Fenner

    2008-06-01

    Full Text Available In this study the depressant effect of fractions from P. glomerata was initially evaluated using the mice barbiturate sleeping time test as reference. The fractions tested were the CHCl3, the EtOAc, the n-BuOH and the aqueous fraction obtained from P. glomerata subterraneous parts. Only the pretreatment with the lipophilic fraction (CHCl3: EtOAc, 1:1, w/w increased the barbiturate sleeping time (i.p 500 mg/kg; v.o. 1000 mg/kg. Ecdysterone, the main substance isolated from this lipophilic fraction, was identified by spectroscopic methods and its content in the ethanol extract was determined as 1.4% (w/w by HPLC. In order to investigate the hypothesis of ecdysterone displaying a depressant effect on nervous central system, an evaluation toward the hypnotic-sedative and anxiolytic effects of this drug was carried out. Ecdysterone 100 mg/kg, i.p, increased the barbiturate sleeping time without provoking hypothermia; when administered by oral route its minimal effective dose was 400 mg/kg. On the other hand, ecdysterone (100 mg/kg, i.p; 400 mg/kg, p.o did not impair motor coordination and was ineffective on pentylenetetrazole-induced convulsion, elevated plus-maze and step-down inhibitory avoidance tests, indicating that at these doses the drug does not present an anxiolytic profile and does not cause manifest neurotoxic effects as well. In conclusion, the lipophilic fraction from P. glomerata presents a hypnotic effect being ecdysterone one of the compounds responsible for this CNS activity.Neste trabalho foi avaliado, em roedores, o efeito depressor das frações clorofórmio (CHCl3, acetato de etila (EtOAc e n-butanol, obtidas das partes subterrâneas de Pfaffia glomerata, empregando-se o teste de tempo de sono barbitúrico como referência. Somente a fração lipofílica (CHCl3:EtOAc, 1:1, m/m (i.p. 500 mg/kg; v.o. 1000 mg/kg potenciou o tempo de sono induzido por pentobarbital. A ecdisterona foi isolada e identificada como constituinte majorit

  5. Fatores associados à hipertensão intracraniana em crianças e adolescentes vítimas de traumatismo crânio-encefálico grave Factors associated with intracranial hypertension in children and teenagers who suffered severe head injuries

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    Sérgio Diniz Guerra

    2010-02-01

    Full Text Available OBJETIVO: Analisar fatores associados à ocorrência de hipertensão intracraniana em pacientes pediátricos vítimas de traumatismo crânio-encefálico (TCE grave. MÉTODOS: Coorte com coleta retrospectiva do período de 1998 a 2003. Incluídos pacientes entre 0 e 16 anos com TCE, pontuação 20 mmHg com necessidade de tratamento e HIC refratária, acima de 25 mmHg, com necessidade de coma barbitúrico ou craniectomia descompressiva. Foi realizada análise univariada, seguida de multivariada, sendo consideradas significativas as variáveis com p OBJECTIVE: To analyze factors associated with intracranial hypertension in pediatric patients who suffered severe head injuries. METHODS: Retrospective cohort study, with data collected from September 1998 through August 2003, including patients aged 0 to 16 who suffered severe head injuries, Glasgow score 20 mmHg requiring treatment, while refractory IH was ICP over 25 mmHg requiring barbiturates or decompressive craniectomy. Univariate analysis was followed by multivariate analysis; variables were considered significant if p < 0.05. RESULTS: Ages ranged from 2 months to 16 years, median age 9.7 (6.0-2.3 years. Glasgow scores ranged from 3 to 8, median 6 (4-7. Traffic accidents were responsible for 79.5% of events. Monitoring devices were installed, on average, 14 hours after trauma, median time 24 hours. One hundred and three patients (78% had IH, while 57 (43.2% had refractory IH. In multivariate analysis, younger age ranges were associated with IH relative risk = 1.67 (1.03-2.72; p = 0.037, and abnormal postures were associated with refractory IH relative risk = 2.25 (1.06-4.78. The group mortality rate was 51.5%; it was correlated with use of barbiturates in refractory IH and low cerebral perfusion pressure at the intensive care unit. CONCLUSIONS: IH and refractory IH were frequent events in pediatric patients who suffered severe head injuries. The younger the patient, the greater the chance of

  6. Iron deficiency induces changes in riboflavin secretion and the mitochondrial electron transport chain in hairy roots of Hyoscyamus albus.

    Science.gov (United States)

    Higa, Ataru; Mori, Yuko; Kitamura, Yoshie

    2010-07-15

    Hyoscyamus albus hairy roots secrete riboflavin under Fe-deficient conditions. To determine whether this secretion was linked to an enhancement of respiration, both riboflavin secretion and the reduction of 2,3,5-triphenyltetrazolium chloride (TTC), as a measure of respiration activity, were determined in hairy roots cultured under Fe-deficient and Fe-replete conditions, with or without aeration. Appreciable TTC-reducing activity was detected at the root tips, at the bases of lateral roots and in internal tissues, notably the vascular system. TTC-reducing activity increased under Fe deficiency and this increase occurred in concert with riboflavin secretion and was more apparent under aeration. Riboflavin secretion was not apparent under Fe-replete conditions. In order to examine which elements of the mitochondrial electron transport chain might be involved, the effects of the respiratory inhibitors, barbiturate, dicoumarol, malonic acid, antimycin, KCN and salicylhydroxamic acid (SHAM) were investigated. Under Fe-deficient conditions, malonic acid affected neither root growth, TTC-reducing activity nor riboflavin secretion, whereas barbiturate and SHAM inhibited only root growth and TTC-reducing activity, respectively, and the other compounds variously inhibited growth and TTC-reducing activity. Riboflavin secretion was decreased, in concert with TTC-reducing activity, by dicoumarol, antimycin and KCN, but not by SHAM. In Fe-replete roots, all inhibitors which reduced riboflavin secretion in Fe-deficient roots showed somewhat different effects: notably, antimycin and KCN did not significantly inhibit TTC-reducing activity and the inhibition by dicoumarol was much weaker in Fe-replete roots. Combined treatment with KCN and SHAM also revealed that Fe-deficient and Fe-replete roots reduced TTC in different ways. A decrease in the Fe content of mitochondria in Fe-deficient roots was confirmed. Overall, the results suggest that, under conditions of Fe deficiency in H

  7. Spatial analysis of drug-related hospital admissions: an auto-Gaussian model to estimate the hospitalization rates in Italy

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    Emanuela Colasante

    2008-12-01

    Full Text Available

    Introduction: The aim of this study is to evaluate, even if partially, how much the drug use phenomenon impacts on the Italian National Heatlh System throughout the estimation at local level (Local Health Unit of the hospitalization rate caused by substance use and abuse such as opiates, barbiturates-sedativeshypnotics, cocaine and cannabis, and keeping in mind the phenomenon distribution in the space and so the fact that what happens in a specific area depends on what is happening in the neighbourhoods close to it (spatial autocorrelation.

    Methods: Data from hospital discharge database were provided by the Ministry of Health and an auto- Gaussian model was fitted. The spatial trend can be a function of other explanatory variables or can simply be modeled as a function of spatial location. Both models were fitted and compared using the number of subjects kept in charge by Drug Addiction Services and the number of beds held by hospitals as covariates.

    Results: Concerning opiates use related hospitalizations, results show areas where the phenomenon was less prominent in 2001 (Lombardy, part of Liguria, Umbria, part of Latium, Campania, Apulia and Sicily. In the following years, the hospitalization rates increased in some areas, such as the north of Apulia, part of Campania and Latium. A dependence of the opiates related hospitalization rates on the rate of subjects kept in charge by the Drug Addiction Services is highlighted. Concerning barbiturates-sedatives-hypnotics consumption, the best model is the one without covariates and estimated hospitalization rates are lower then 3 per thousand. The model with only the covariate “rate of subjects kept in charge by Drug Addiction Services” has been used both for cocaine and cannabis. In these two cases, more than a half of the Local Health Units report hospitalization rates lower than 0.5 per thousand

  8. Assessment of changes in Intracranial Pressure (ICP after the implementation of therapeutic measures for Intracranial Hypertation (IH

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    Nikoletta Arapoglou

    2014-07-01

    Full Text Available The Traumatic Brain Injury (TBI constitutes the leading cause of death and permanent disability in all age groups and, by far, at ages 19-27 years. The morbidity and mortality remain high and depend on the neurological status of patients at admission, the treatment in the Intensive Care Unit (ICU, surgery and postoperative rehabilitation and recovery. The prevention and treatment factors that may maintain or exacerbate the IH is a very important and fundamental issue in neurological intensive therapy. Aim: The aim of the present systematic review was to investigate the effectiveness of various therapeutic measures for the treatment of intracranial hypertension. Material and Method: The methodology used was to review the Greek and international bibliographic databases (Iatrotek, Pubmed, Cinahl, Scopus,. The keywords used to search for the study was: "Hyperventilation", "therapeutic hypothermia", "hyperosmolar therapy", "corticosteroids", "traumatic brain injury" and were the last 15 years. Results: Hyperventilation, the hyperosmolar therapy, barbiturates, patient position, sedatives-neuromuscular blocking agents, therapeutic hypothermia, corticosteroids and some aggressive surgical methods (decompressive craniotomy and drainage of CSF make up the puzzle of modern intensive care patients with severe TBI. The cornerstone for the control of intracranial hypertension are the hyperosmolar therapy, therapeutic hypothermia and patient position (supine-neutral to 30o-45o inclination. With skepticism, seems to treat hyperventilation, sedatives-neuromuscular blocking agents, the barbiturate coma and surgical methods of treatment. This is due to the plurality of complications that causing. Last but not least, corticosteroids have been implicated as a measure which does nothing to help patients with increased ICP, contrary aggravates their condition. Conclusions: Direct surgical treatment of IH accompanied by better results in terms of mortality, morbidity

  9. Use of propofol and other nonbenzodiazepine sedatives in the intensive care unit.

    Science.gov (United States)

    Angelini, G; Ketzler, J T; Coursin, D B

    2001-10-01

    Sedatives continue to be used on a routine basis in critically ill patients. Although many agents are available and some approach an ideal, none are perfect. Patients require continuous reassessment of their pain and need for sedation. Pathophysiologic abnormalities that cause agitation, confusion, or delirium must be identified and treated before unilateral administration of potent sedative agents that may mask potentially lethal insufficiencies. The routine use of standardized and validated sedation scales and monitors is needed. It is hoped that reliable objective monitors of patients' level of consciousness and comfort will be forthcoming. Each sedative agent discussed in this article seems to have a place in the ICU pharmacologic armamentarium to ensure the safe and comfortable delivery of care. Etomidate is an attractive agent for short-term use to provide the rapid onset and offset of sedation in critically ill patients who are at risk for hemodynamic instability but seem to need sedation or anesthesia to perform a procedure or manipulate the airway. Ketamine administered through intramuscular injection or intravenous infusion provides quick, intense analgesia and anesthesia and allows patients to tolerate limited but painful procedures. The risk/benefit ratio associated with the use of this neuroleptic agent must be weighed carefully. Ketamine is contraindicated in patients who lack normal intracranial compliance or who have significant myocardial ischemia. Barbiturates are reserved mainly to induce coma in patients at risk for severe CNS ischemia, which frequently is associated with refractory intracranial hypertension, or in patients with status epilepticus. When administered in high doses, these drugs have prolonged sedative and depressant effects. Judicious hemodynamic monitoring is required when barbiturate coma is induced. Haloperidol is indicated in the treatment of delirium. Patients should be monitored for extrapyramidal side effects and, when they

  10. Uso não-médico de medicamentos psicoativos entre escolares do ensino fundamental e médio no Sul do Brasil Non-medical use of psychoactive medicines among elementary and high school students in Southern Brazil

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    Tatiane da Silva Dal Pizzol

    2006-01-01

    Full Text Available O objetivo do presente estudo é investigar a prevalência de uso não-médico de medicamentos entre escolares da rede de ensino público e privado de Passo Fundo, Rio Grande do Sul, Brasil, e sua distribuição em relação a fatores sócio-demográficos. Por meio de um delineamento transversal, foi aplicado um questionário de autopreenchimento a 5.057 estudantes a partir da quinta série do ensino fundamental até o terceiro ano do ensino médio. O questionário continha perguntas sobre o uso, sem receita médica, de anfetamínicos, ansiolíticos, barbitúricos, anticolinérgicos, opiáceos, orexígenos e anabolizantes. Da amostra, 7,7% consumiram ansiolíticos alguma vez na vida, 6,4% consumiram anfetamínicos, 2,2%, anabolizantes, e 1,1%, barbitúricos. Estudantes do sexo feminino apresentaram maior consumo de ansiolíticos e anfetamínicos, enquanto que o consumo de anabolizantes foi maior no sexo masculino. O padrão de consumo de medicamentos psicoativos é semelhante ao observado em adultos, sugerindo a necessidade de inclusão de crianças e adolescentes nas campanhas educativas para prevenção do uso indevido de medicamentos.The objective of this study is to assess the prevalence of and risk factors for the non-medical use of psychoactive medicines among students at public and private schools of Passo Fundo, Southern Brazil. A cross-sectional study was carried out using a questionnaire administered to 5,057 students from the 5th grade of elementary school to the 3rd year of high school. The questionnaire contained questions about the use of amphetamines, tranquilizers, barbiturates, anticholinergics, opioids, appetite stimulants, and anabolic steroids. Of the sample total, 7.7% had consumed tranquilizers sometime during their lives, 6.4% had used amphetamines, 2.2% had used anabolic steroids, and 1.1% had used barbiturates. Female students reported significantly greater consumption of tranquilizers and amphetamines, while anabolic

  11. Clinical profile and treatment outcome of febrile infection-related epilepsy syndrome in South Indian children

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    Sandeep B Patil

    2016-01-01

    Full Text Available Purpose: To describe the clinical features and outcome of febrile infection-related epilepsy syndrome (FIRES, a catastrophic epileptic encephalopathy, in a cohort of South Indian children. Materials and Methods: We performed a retrospective chart review of a cohort of children with previously normal development who presented with status epilepticus or encephalopathy with recurrent seizures following a nonspecific febrile illness during the period between January 2007 and January 2012. They were divided into two groups super refractory status epilepticus (SRSE and refractory status epilepticus (RSE depending on the duration and severity of the seizures. Key Findings: Fifteen children who met the inclusion criteria were included for the final analysis. The age of the children at presentation ranged 3-15 years (median 6.3 years. All the children presented with prolonged or recurrent seizures occurring 1-12 days (median 4 days after the onset of fever. Eight children had SRSE while seven children had refractory seizures with encephalopathy. Cerebrospinal fluid (CSF analysis was done in all the children in the acute phase, and the cell count ranged 0-12 cells/μL (median 2 cells/μL with normal sugar and protein levels. Initial neuroimaging done in all children (MRI in 10 and CT in 5, and it was normal in 13 children. Treatment modalities included multiple antiepileptic drugs (AEDs (4-9 drugs (median 5 drugs. Midazolam (MDZ infusion was administered in seven patients. Eight patients required barbiturate coma to suppress the seizure activity. The duration of the barbiturate coma ranged 2-90 days (median 3 days. Steroids were used in 14 children and intravenous immunoglobulin (2 g/kg in 7 children. Three children died in the acute phase. All children were maintained on multiple AEDs till the last follow-up, the number of AEDs ranged 1-6 (median 5 AEDs. The patients with super refractory status in the acute phase were found to be more severely disabled

  12. Central effects of citral, myrcene and limonene, constituents of essential oil chemotypes from Lippia alba (Mill.) n.e. Brown.

    Science.gov (United States)

    do Vale, T Gurgel; Furtado, E Couto; Santos, J G; Viana, G S B

    2002-12-01

    Citral, myrcene and limonene (100 and 200 mg/kg body wt., i.p.), constituents of essential oils from Lippia alba chemotypes, decreased not only the number of crossings but also numbers for rearing and grooming, as measured by the open-field test in mice. Although muscle relaxation detected by the rota rod test was seen only at the highest doses of citral (200 mg/kg body wt.) and myrcene (100 and 200 mg/kg body wt.), this effect was observed even at the lowest dose of limonene (50 mg/kg body wt.). Also, citral and myrcene (100 and 200 mg/kg body wt.) increased barbiturate sleeping time as compared to control. Limonene was also effective at the highest dose, and although citral did not increase the onset of sleep, it increased the duration of sleep, which is indicative of a potentiation of sleeping time. Citral (100 and 200 mg/kg body wt.) increased 2.3 and 3.5 times, respectively, the barbiturate sleeping time in mice. Similar effects were observed for myrcene and limonene at the highest dose (200 mg/kg body wt.) which increased the sleeping time around 2.6 times. In the elevated-plus maze, no effect was detected with citral up to 25 mg/kg body wt., while at a high dose it decreased by 46% the number of entries in the open arms. A smaller but significant effect was detected with limonene (5 mg/kg body wt.). While myrcene (10 mg/kg body wt.) decreased only by 22% the number of entries in the open arms, this parameter was decreased by 48% at the highest dose. Our study showed that citral, limonene and myrcene presented sedative as well as motor relaxant effects. Although only at the highest dose, they also produced a potentiation of the pentobarbital-induced sleeping time in mice, which was more intense in the presence of citral. In addition, neither of them showed an anxiolytic effect, but rather a slight anxiogenic type of effect at the higher doses.

  13. Purification of Soybean Agglutinin and Its Agglutination Activity Toward Different Cancer Cell Lines%大豆凝集素的纯化及其凝集不同肿瘤细胞的探讨

    Institute of Scientific and Technical Information of China (English)

    荆剑; 赵翔; 张页

    2003-01-01

    A novel and efficient method for purification of soybean agglutinin(SBA) from soybean was reported.The method was characterized by selective extraction of SBA from soybean homogenate with barbiturate buffer(pH 6.2) ,removal of impurity by hydroxyapatite,and the final purification of SBA by guaran affinity chromatography.The purified SBA showed a single band of 27.5kD by SDS-PAGE.The lowest concentration of SBA that caused agglutination of the rabbit red blood cells was 0.31 mg/L.Agglutination of different cancer cell lines by the purified SBA was examined.Strong agglutination of the human nasopharyngeal CNE cells.mouse Lewis lung carcinoma cells.and rat mammary adenocarcinoma R3230AC cells was observed.However,SBA could not agglutinate the human hepatocellular carcinoma BEL-7402cells,suggesting that unlike the above-mentioned three cell lines,the BEL-7402 cells may not express N-acetylgalactosamine(GalNAc) or galactose(Gal) residues in significant amount at the non-reducing terminals of their cell surface glycans.

  14. Design of new and potent diethyl thiobarbiturates as urease inhibitors: a computational approach.

    Science.gov (United States)

    Wadood, Abdul; Riaz, Muhammad; Mulk, Amir Ul; Khan, Momin; Haleem, Sobia Ahsan; Shams, Sulaiman; Gul, Sahib; Ahmed, Ayaz; Qasim, Muhammad; Ali, Farman; Ul-Haq, Zaheer

    2014-01-01

    Urease is an important enzyme both in agriculture and medicine research. Strategies based on urease inhibition is critically considered as the first line treatment of infections caused by urease producing bacteria. Since, urease possess agro-chemical and medicinal importance, thus, it is necessary to search for the novel compounds capable of inhibiting this enzyme. Several computational methods were employed to design novel and potent urease inhibitors in this work. First docking simulations of known compounds consists of a set of arylidine barbiturates (termed as reference) were performed on the Bacillus pasteurii (BP) urease. Subsequently, two fold strategies were used to design new compounds against urease. Stage 1 comprised of the energy minimization of enzyme-ligand complexes of reference compounds and the accurate prediction of the molecular mechanics generalized born (MMGB) interaction energies. In the second stage, new urease inhibitors were then designed by the substitution of different groups consecutively in the aryl ring of the thiobarbiturates and N, N-diethyl thiobarbiturates of the reference ligands.. The enzyme-ligand complexes with lowest interaction energies or energies close to the calculated interaction energies of the reference molecules, were selected for the consequent chemical manipulation. This was followed by the substitution of different groups on the 2 and 5 positions of the aryl ring. As a result, several new and potent diethyl thiobarbiturates were predicted as urease inhibitors. This approach reflects a logical progression for early stage drug discovery that can be exploited to successfully identify potential drug candidates.

  15. Halothane anaesthesia and liver damage A review of the literature on this and associated hazards

    CERN Document Server

    Spoor, N L

    1977-01-01

    In radiological protection the decision to use bronchopulmonary lavage, or not to use it, will occasionally rest on a comparison of risks: on the one hand the long-term radiological risk and, on the other, the short-term risks from the operation itself (after several repetitions) and from multiple exposure to the anaesthetic agents, thiopentone (or other barbiturate) and halothane. The purpose of this review was to find a numerical estimate for the risk of irreversible liver damage from multiple exposure to halothane in a healthy male aged between 20 and 60 years. The many reports which have appeared since 1970 have shown that halothane hepatitis is probably a specific, but rare, pathological condition and that the risks from halothane exposure are no greater than those from other anaesthetics. The facts suggest that there is an increased risk associated with multiple exposure. If for the average patient the mortality risk from one anaesthetic exposure to halothane is 1 in 10 sup 5 , the risk from two further...

  16. Effect of carboxymethyl cellulose edible coating containing Zataria multiflora essential oil and grape seed extract on chemical attributes of rainbow trout meat

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    Mojtaba Raeisi

    2014-06-01

    Full Text Available Meat products, especially fish meat, are very susceptible to lipid oxidation and microbial spoilage. In this study, first, gas chromatography mass spectrometry (GC-MS analysis of Zataria multiflora essential oil (ZEO components was done and then two concentrations of ZEO, (1% and 2% and two concentrations of grape seed extract (GSE, (0.5% and 1% were used in carboxymethyl cellulose coating alone and in combination, and their antioxidant effects on rainbow trout meat were evaluated in a 20-day period using thiobarbituric acid reactive substances (TBARS test. Their effects on total volatile basic nitrogen (TVBN and pH were evaluated as well. The main components of ZEO are thymol and carvacrol. These components significantly decreased production of thio-barbituric acid (TBA, TVBN and pH level of fish meat. The initial pH, TVBN and TBA content was 6.62, 12.67 mg N per 100 g and 0.19 mg kg-1, respectively. In most treatments significant (p < 0.05 effects on aforementioned factors was seen during storage at 4 ˚C. The results indicated that use of ZEO and GSE as a natural antioxidant agents was effective in reducing undesirable chemical reactions in storage of fish meat.

  17. Acute treatment with pentobarbital alters the kinetics of in vivo receptor binding in the mouse brain

    Energy Technology Data Exchange (ETDEWEB)

    Sakiyama, Yojiro [Division of Clinical Research, National Institute of Radiological Sciences, Inage-ku, Chibashi 263-8555 (Japan)]. E-mail: yojiro.sakiyama@pfizer.com; Saito, Masao [Department of Medical Science, Institute of Medical Electronics, University of Tokyo, Bunkyo-ku, Tokyo 113-0033 (Japan); Inoue, Osamu [Department of Medical Physics, School of Allied Health Science, Faculty of Medicine, Osaka University, Suita, Osaka 565-0871 (Japan)

    2006-05-15

    The effect of pentobarbital, a sedative-hypnotic barbiturate, on the in vivo binding of benzodiazepine receptors in the mouse brain was investigated. Dose-related changes in the apparent binding of [{sup 3}H]Ro15-1788 ([{sup 3}H]flumazenil) in the cerebral cortex, cerebellum and pons-medulla were observed by pretreatment with pentobarbital. For quantification of the kinetic properties of the in vivo binding of [{sup 3}H]Ro15-1788, time courses of radioactivity following its injection were examined, and kinetic analysis was performed using the compartment model. The time courses of radioactivity following injection of [{sup 3}H]Ro15-1788 with 3 mg/kg Ro15-1788 were used as input function. In all regions studied, rate constants between input compartment and specific binding compartment were significantly decreased by pentobarbital. However, no significant alterations in the binding potential (BP=K {sub 3}/K {sub 4}) of benzodiazepine receptors by pentobarbital were observed in any of the regions. A saturation experiment indicated that the decrease in the input rate constant (K {sub 3}), which includes both the association rate constant (k {sub on}) and the number of binding sites available (B {sub max}), was mainly due to decrease in k {sub on}. These results suggest that apparent increases in binding at 20 min after tracer injection were due to the decrease in the association and dissociation rates of binding in vivo.

  18. Increase in phorbol ester binding in liver microsomes after chronic administration of phenobarbital

    Energy Technology Data Exchange (ETDEWEB)

    Menez, J.F.; Deitrich, R.A. (Univ. of Colorado, Denver (United States))

    1991-03-15

    The effect of chronic administration of phenobarbital on the binding of phorbol-12,13-dibutyrate (({sup 3}H)PDBu), an activator of protein kinase C (PKC), was examined in rat liver microsomes. A significant increase in the number of binding sites was observed in microsomes of Fisher 344 rats. However, no change appeared in liver cytosol binding of PDBu. Consequently, a translocation process of PKC is unlikely. The increase in ({sup 3}H)PDBu binding in liver microsomes is significant 24 h. after one injection of phenobarbital and reaches its maximum in 2 days. In other strains of rats (ACI and lean Zucker), significant differences were found in the increase of ({sup 3}H)PDBu binding in microsomes. Fisher 344 were the most sensitive, lean Zucker rats, the least sensitive. Those results parallel the pentoxy-resorufin O demethylase activity in the microsomes of the same animals. EC{sub 50} values for inhibition of ({sup 3}H)PDBu binding by pentobarbital were determined in control microsomes from Fisher and Zucker rats. In Fisher rats, ({sup 3}H)PDBu binding in microsomes was found to be more sensitive to the inhibitory effect of pentobarbital than in lean Zucker rats, which suggests that the more microsomes are inhibited in vitro the greater the increase in PKC in microsomes following chronic barbiturate treatment.

  19. Medical treatment of neuro diseases of dogs and cats / Fármacos utilizados no tratamento das afecções neurológicas de cães e gatos

    Directory of Open Access Journals (Sweden)

    Ronaldo Cassimiro da Costa

    2010-09-01

    Full Text Available A revision of the current literature regarding medical management of neurological diseases of dogs and cats is presented. The indications, doses, and duration of the recommended treatment of several medications are reviewed. The authors have reviewed analgesic, antibiotic, anticonvulsants, barbiturates, anticolinesterasics, antifungals, antifibrinolytics, steroidal and non-steroidal antiinflammatory, antineoplastics, antipsychotics, anxiolytics, antidepressants, free radical scavengers, diuretics, drugs used in the treatment of micturition disorders, phytotherapeutics, nutraceuticals, muscle relaxant and vitamins.Este trabalho compreende uma revisão da literatura, dos diferentes fármacos utilizados na terapêutica das afecções neurológicas de cães e gatos, assim como sua indicação, dosagens, e duração do tratamento. Nesse contexto incluíram-se analgésicos, antibióticos, anticonvulsivantes, barbitúricos, anticolinesterásicos, antifúngicos, antifibrinolíticos, antiinflamatórios esteróides e não esteróides, antineoplásicos, antipsicóticos, ansiolíticos, antidepressivos, antioxidantes e varredores de radicais livres, diuréticos, fármacos utilizados nos distúrbios da micção, fitoterápicos, modificadores do metabolismo articular (nutracêuticos, relaxantes musculares e vitaminas.

  20. Life threatening central nervous system manifestations and hypothermia due to maneb intoxication in a child: a case report.

    Science.gov (United States)

    de Tollenaer, S M; Buysse, Cmp; van den Anker, J N; Touw, D J; de Hoog, M

    2006-12-01

    Maneb, manganese ethylene-bis-dithiocarbamate, is a fungicide pesticide used in the agriculture and bulb flower culture sector. Toxicological effects for humans have been reported in literature and are diverse. They vary from allergic reactions (dermatitis, conjunctivitis, and bronchitis), central nervous system effects (muscarinic, nicotinic, central and extrapyramidal) and renal toxicity (acute renal failure).A 7-year old girl was admitted to the pediatric intensive care unit because of status epilepticus. Physical examination showed respiratory insufficiency, convulsions, and severe hypothermia (32.5 degrees C). The patient was intubated and her convulsions were successfully treated with benzodiazepines. Except for a combined metabolic and respiratory acidosis and hyperglycemia, diagnostic investigations on admission (full blood count, electrolytes, liver and renal functions, cerebrospinal fluid investigation, toxicology screening of blood and urine for barbiturates and benzodiazepines, blood culture, herpes PCR, and a CT scan of the brain) were normal. Within 24 hours, there was a complete recovery of all neurological signs. Within 72 hours, the patient was discharged from the hospital. Liquid chromatography-mass spectrometric investigation of her blood showed amounts of maneb, which can explain all symptoms and signs. However, effects of this magnitude on the central nervous system have not previously been reported in humans.

  1. [Interventional neuroradiology. Drug treatment, monitoring and function tests].

    Science.gov (United States)

    Laurent, A; Gobin, Y P; Launay, F; Aymard, A; Casasco, A; Merland, J J

    1994-04-23

    Specialized monitoring as well as function tests and drug therapy play an ever growing role in neuroradiological procedures. The particular route of administration and the territories involved in neuroradiology require special precautions. Anaesthesia must enable the operators to monitor the central nervous system since the patients must remain totally immobilized for several hours. Catheterization is made safe by careful asepsia and antibiotic prophylaxis and by preventing embolic events, particularly in neuro-cervico-facial interventions where an anticoagulant protocol is important. Arterial spasms can be prevented or cured with calcium inhibitors. The safety of the procedure itself is guaranteed by various function tests including sensitivity to ischaemia using anaesthetic barbiturates, controlled clampings or the lidocaine test. Undesirable effects of both emboli (e.g. toxicity of cyanoacrylate glue) and embolization (e.g. subsequent venous thrombosis) can be prevented by adapted anti-inflammatory drugs. Herein, we describe the routine monitoring conditions, drugs prescribed and function tests performed at the Therapeutic Angiography Department of the Lariboisière Hospital, Paris.

  2. The effects of exposure of {sup 60}Co on the oxidant/antioxidant status among radiation victims

    Energy Technology Data Exchange (ETDEWEB)

    Demir, Mustafa E-mail: mmdemir@e-kolay.net; Konukoglu, Dildar; Kabasakal, Levent; Yelke, Hakan Kadir; Ergen, Kadir; Ahmed, Sabbir

    2002-07-01

    This retrospective study has been performed with radiation victims who were accidentally exposed to a {sup 60}Co source and its release into the environment. The aim of the study was to assess the effects of elevated radiation exposures on plasma level, on erythrocyte thio barbituric acid reactive substance (TBARS) level and on erythrocyte glutathione (GSH) levels. Patients were treated in different hospitals with different symptoms such as nausea, vomiting, dizziness, along with severe anemia in some patients. Blood samples were collected 3-5 days following the radiation accident. Increases in plasma (6.25{+-}0.90 nmol ml{sup -1}) and erythrocyte TBARS levels (330.5{+-}30.5 {mu}mol gHb{sup -1}) were found in comparison to a healthy group (3.72{+-}0.68 nmol ml{sup -1} and 150.7{+-}20.5 {mu}mol gHb{sup -1}, respectively) at a significant level (p<0.001). Erythrocyte GSH levels (5.2{+-}0.30 {mu}mol gHb{sup -1}) were found to be decreased among the victims (healthy group: 10.2{+-}0.7 {mu}mol gHb{sup -1}) at the same significance level (p<0.001). These observations confirm a significant change induced by radiation in the oxidant/antioxidant status among the victims. It is suggested here that antioxidant supplementation therapy might be effective in preventing the harmful effects of {sup 60}Co radiation among radiation victims.

  3. Cognitive functions of epileptic patients on monotherapy with phenobarbitone and healthy controls

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    Mônica M. Bigarella

    1991-06-01

    Full Text Available Quantitative measurements have indicated that heredity, cerebral damage, psycho-social aspects, ictal and inter-ictal phenomena and antiepileptic drugs may interfere in the cognitive dysfunction of epileptic patients. In the present study objective methods included immediate and late recall and recognition of pictures, Stroop test and auditory selection. Twenty patients with symptomatic localized epilepsy aged 17-52 years (27±10, mean ±sd were compared to age and socially matched healthy controls. Patients were on therapeutic serum concentrations (25±12 m/mi of phenobarbitone and had active epilepsy with 1.94 generalized tonic-clonic, 0.85 simple partial and 6.28 complex partial seizures monthly (means. Patients performed worse than controls in all 6 tests (p<0.05 to p<0.001, indicating a generalized cognitive deficit related to seizures and/or barbiturate therapy. We suggest further studies should be carried out in populations with uniform monotherapeutic regimens and epileptic syndromes in order to isolate factors related to the cognitive dysfunction of epileptic patients.

  4. The profile evolution of acute severe poisoning in Spain.

    Science.gov (United States)

    Nogué, S; Marruecos, L; Nolla, J; Monteís, J; Ferrer, A; Civeira, E

    1992-12-01

    About 5% of the patients admitted to emergency departments with poisonings are seriously ill and need admission to intensive care units (ICUs). This paper presents the result of three multicentric studies carried out in Spain during the last ten years. A study was made of 6 ICUs in 1980, 41 in 1987 and 15 in 1990 with a total of 596 patients. The average age (36) remained stable throughout, but the number of female cases decreased each time. The most frequent cause (79%) was attempted suicide. The products used most frequently were therapeutic drugs (82, 71 and 58%) followed by drugs of abuse, and then agricultural, household and industrial products. We observed a progressive decrease in barbiturates (54, 15 and 2%) and an increase in benzodiazepines and cyclic antidepressants. Therapeutic methods used were mostly gastric lavage (64%), activated charcoal (35%), forced diuresis (43%), extracorporeal therapy (11%) and antidotes. The mortality rate fluctuated between 6.4 and 9.1%, being significantly higher with poisoning by non-therapeutic drugs. In conclusion, the most common poisoning admitted to our ICUs was by psychoactive drugs in suicide attempts. We observed the under-use of activated charcoal and an excessive usage of kidney and extracorporeal methods. The prognosis was worse for poisonings with non-therapeutic drugs.

  5. [Obstetric and gynecologic anesthesia reported in the "Revista Española de Obstetricia y Ginecología" (1916-1936)].

    Science.gov (United States)

    Llorente, A; Giménez, M C; Figueira, A; Montero, G

    1994-01-01

    This study follows the evolution of anesthesia in gynecology and obstetrics in Spain between 1916 and 1936. Research included revising all articles and references concerning anesthesiology appearing in the Revista Española de Obstetricia y Ginecologia over the 20 years during which that journal was published. Eighty-three articles were found: 18 (21.6%) original research reports, 37 (44.6%) reviews of the Spanish professional literature and 28 (33.7%) summaries and descriptions of meetings of scientific organizations. Spanish references constituted 39.8% with the remaining 60.2% coming from European and Hispano-American sources. Twenty-four (34.9%) were related to spinal anesthesia, 15 (18%) covered various methods for analgesia during childbirth and 14 (16.8%) were on barbiturates. The remaining articles referred to rectally administered anesthesia, local anesthesia, inhalatory anesthesia and pain in gynecology. In conclusion, our review reveals the strong international contacts in Spanish gynecology during this period, as well as the interest of gynecologists and obstetricians in various anesthetic techniques and the rapid incorporation of new methods into their therapeutic arsenal.

  6. Crystal structure of 4-aminopyridinium 5-(5-chloro-2,4-dinitrophenyl-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-olate hemihydrate

    Directory of Open Access Journals (Sweden)

    Manickkam Vaduganathan

    2014-10-01

    Full Text Available The title molecular salt, C5H7N2+·C12H8ClN4O7−·0.5H2O, crystallizes as a hemihydrate. The two rings in the barbiturate anion are not coplanar but make a dihedral angle of 43.17 (16°. The two nitro groups deviate from the ring to which they are attached; the nitro group ortho with respect to the ring junction is more deviated [39.3 (4°] than that in the para position [4.2 (5°], probably to overcome steric hindrance. As a result of this, the latter nitro group is more involved in delocalizing the negative charge of the anion than the former nitro group. In the crystal, the cations and anions are linked via N—H...O hydrogen bonds forming zigzag chains along [10-1]. The chains are linked by O—H...O and C—H...O hydrogen bonds, forming slabs lying parallel to (10-1. Further C—H...O hydrogen bonds link the slabs, forming a three-dimensional structure.

  7. Can anesthetic treatment worsen outcome in status epilepticus?

    Science.gov (United States)

    Sutter, Raoul; Kaplan, Peter W

    2015-08-01

    Status epilepticus refractory to first-line and second-line antiepileptic treatments challenges neurologists and intensivists as mortality increases with treatment refractoriness and seizure duration. International guidelines advocate anesthetic drugs, such as continuously administered high-dose midazolam, propofol, and barbiturates, for the induction of therapeutic coma in patients with treatment-refractory status epilepticus. The seizure-suppressing effect of anesthetic drugs is believed to be so strong that some experts recommend using them after benzodiazepines have failed. Although the rationale for the use of anesthetic drugs in patients with treatment-refractory status epilepticus seems clear, the recommendation of their use in treating status epilepticus is based on expert opinions rather than on strong evidence. Randomized trials in this context are lacking, and recent studies provide disturbing results, as the administration of anesthetics was associated with poor outcome independent of possible confounders. This calls for caution in the straightforward use of anesthetics in treating status epilepticus. However, there are still more questions than answers, and current evidence for the adverse effects of anesthetic drugs in patients with status epilepticus remains too limited to advocate a change of treatment algorithms. In this overview, the rationale and the conflicting clinical implications of anesthetic drugs in patients with treatment-refractory status epilepticus are discussed, and remaining questions are elaborated. This article is part of a Special Issue entitled "Status Epilepticus".

  8. Preliminary results of the global audit of treatment of refractory status epilepticus.

    Science.gov (United States)

    Ferlisi, M; Hocker, S; Grade, M; Trinka, E; Shorvon, S

    2015-08-01

    The treatment of refractory and super refractory status epilepticus is a "terra incognita" from the point of view of evidence-based medicine. As randomized or controlled studies that are sufficiently powered are not feasible in relation to the many therapies and treatment approaches available, we carried out an online multinational audit (registry) in which neurologists or intensivists caring for patients with status epilepticus may prospectively enter patients who required general anesthesia to control the status epilepticus (SE). To date, 488 cases from 44 different countries have been collected. Most of the patients had no history of epilepsy and had a cryptogenic etiology. First-line treatment was delayed and not in line with current guidelines. The most widely used anesthetic of first choice was midazolam (59%), followed by propofol and barbiturates. Ketamine was used in most severe cases. Other therapies were administered in 35% of the cases, mainly steroids and immunotherapy. Seizure control was achieved in 74% of the patients. Twenty-two percent of patients died during treatment, and four percent had treatment actively withdrawn because of an anticipated poor outcome. The neurological outcome was good in 36% and poor in 39.3% of cases, while 25% died during hospitalization. Factors that positively influenced outcome were younger age, history of epilepsy, and low number of different anesthetics tried. This article is part of a Special Issue entitled "Status Epilepticus".

  9. The historical significance of anaesthesia events at Pearl Harbor.

    Science.gov (United States)

    Crowhurst, Ja

    2014-07-01

    Up to the end of World War II, less than 10% of the general anaesthetics administered was with intravenous barbiturates. The remaining 90% of anaesthetics given in the USA were with diethyl ether. In the United Kingdom and elsewhere, chloroform was also popular. Diethyl ether administration was a relatively safe and simple procedure, often delegated to nurses or junior doctors with little or no specific training in anaesthesia. During the Japanese attack on the US bases at Pearl Harbor, with reduced stocks of diethyl ether available, intravenous Sodium Pentothal(®), a most 'sophisticated and complex' drug, was used with devastating effects in many of those hypovolaemic, anaemic and septic patients. The hazards of spinal anaesthesia too were realised very quickly. These effects were compounded by the dearth of trained anaesthetists. This paper presents the significance of the anaesthesia tragedies at Pearl Harbor, and the discovery in the next few years of many other superior drugs that caused medical and other health professionals to realise that anaesthesia needed to be a specialist medical discipline in its own right. Specialist recognition, aided by the foundation of the National Health Service in the UK, the establishment of Faculties of Anaesthesia and appropriate training in pharmacology, physiology and other sciences soon followed. Modern anaesthesiology, as we understand it today, was born and a century or more of ether anaesthesia finally ceased.

  10. Substance abuse in victims of fire.

    Science.gov (United States)

    Barillo, D J; Goode, R

    1996-01-01

    Ethanol or drug use may increase the risk of fire-related injury or death. This study was performed to quantify the role of substance abuse in fatal fires occurring in New Jersey over a 7-year period. Records of all the fatalities of fire reported to the State Medical Examiners Office between 1985 and 1991 were retrospectively examined. Blood assay results for ethanol were positive in 215 of the 727 (29.5%) fatalities of fire tested. For this group, the mean blood-ethanol level was 193.9 mg/dl. Blood or urine assay results for substances of abuse were positive in 78 of the 534 (14.6%) fatalities tested. The most commonly detected illicit substances were cocaine, benzodiazepines, barbiturates, and cannabinoids. The test results were positive for both ethanol and drug use in 36 victims. Forty percent of all the fatalities of fire were aged younger than 11 or older than 70. In contradistinction, 75% of drug-positive fatalities of fire and 58% of ethanol-positive fatalities of fire were between the ages of 21 and 50, suggesting that inebriation may impair the ability to escape from fire. Substance abusers in middle life are a previously unrecognized group at higher risk of injury or death in a fire.

  11. Pain perception and anaesthesia in research frogs.

    Science.gov (United States)

    Guénette, Sarah Annie; Giroux, Marie-Chantal; Vachon, Pascal

    2013-01-01

    Frogs possess pain receptors and pathways that support processing and perception of noxious stimuli however the level of organization is less well structured compared to mammals. It was long believed that the experience of pain was limited to 'higher' phylums of the animal kingdom. However, it is now commonly accepted that amphibians possess neuro-anatomical pathways conductive of a complete nociceptive experience. Xenopus laevis frogs have been one of the most popular aquatic research models for developmental studies and genetic research. These frogs have been extensively use in research for their eggs, that can be collected following hormonal stimulation either naturally or by surgical intervention. Many anaesthetics have been used in amphibians such as bath solutions of MS-222, benzocaine and eugenol as well as systemic injections of ketamine or tiletamine, barbiturates, propofol and gas administrations of methoxyflurane, halothane and isoflurane. Most of these anaesthetic drugs produce variability in depth and duration of anaesthesia. MS-222 appears to be one of the most reliable anaesthetics. This review will focus on the evidence of pain perception in frogs and will compare the effectiveness and limitations of different anaesthetics used in Xenopus leavis frogs.

  12. Actions of insecticides on the insect GABA receptor complex

    Energy Technology Data Exchange (ETDEWEB)

    Bermudez, I.; Hawkins, C.A.; Taylor, A.M.; Beadle, D.J. (School of Biological and Molecular Sciences, Oxford Polytechnic, Headington, Oxford (England))

    1991-01-01

    The actions of insecticides on the insect gamma-aminobutyric acid (GABA) receptor were investigated using (35S)t-butylbicyclophosphorothionate (( 35S)TBPS) binding and voltage-clamp techniques. Specific binding of (35S)TBPS to a membrane homogenate derived from the brain of Locusta migratoria locusts is characterised by a Kd value of 79.3 {plus minus} 2.9 nM and a Bmax value of 1770 {plus minus} 40 fmol/mg protein. (35S)TBPS binding is inhibited by mM concentrations of barbiturates and benzodiazepines. In contrast dieldrin, ivermectin, lindane, picrotoxin and TBPS are inhibitors of (35S)TBPS binding at the nanomolar range. Bicuculline, baclofen and pyrethroid insecticides have no effect on (35S)TBPS binding. These results are similar to those obtained in electrophysiological studies of the current elicited by GABA in both Locusta and Periplaneta americana central neurones. Noise analysis of the effects of lindane, TBPS, dieldrin and picrotoxin on the cockroach GABA responses reveals that these compounds decrease the variance of the GABA-induced current but have no effect on its mean open time. All these compounds, with the exception of dieldrin, significantly decrease the conductance of GABA-evoked single current.

  13. Pathophysiology and Treatment of Severe Traumatic Brain Injuries in Children.

    Science.gov (United States)

    Allen, Kimberly A

    2016-02-01

    Traumatic brain injuries (TBIs) in children are a major cause of morbidity and mortality worldwide. Severe TBIs account for 15,000 admissions annually and a mortality rate of 24% in children in the United States. The purpose of this article is to explore pathophysiologic events, examine monitoring techniques, and explain current treatment modalities and nursing care related to caring for children with severe TBI. The primary injury of a TBI is because of direct trauma from an external force, a penetrating object, blast waves, or a jolt to the head. Secondary injury occurs because of alterations in cerebral blood flow, and the development of cerebral edema leads to necrotic and apoptotic cellular death after TBI. Monitoring focuses on intracranial pressure, cerebral oxygenation, cerebral edema, and cerebrovascular injuries. If abnormalities are identified, treatments are available to manage the negative effects caused to the cerebral tissue. The mainstay treatments are hyperosmolar therapy; temperature control; cerebrospinal fluid drainage; barbiturate therapy; decompressive craniectomy; analgesia, sedation, and neuromuscular blockade; and antiseizure prophylaxis.

  14. Distinct roles of the Y1 and Y2 receptors on neuropeptide Y-induced sensitization to sedation.

    Science.gov (United States)

    Naveilhan, P; Canals, J M; Arenas, E; Ernfors, P

    2001-09-01

    Intracranial injection of neuropeptide Y (NPY) increases the sensitivity to sodium pentobarbital and ketamin sedation and has similar properties as GABA agonists on sleep. Mice sensitive to sedation have increased levels of NPY in many brain regions and Y1(-/-) mice show a marked resistance to barbiturates. Here we characterized the role of the NPY Y receptors in anesthetic-induced sedation. We show that Y1 and Y2, but not Y5, receptors participate in the modulation of sedation. Administration of a Y1 agonist increased the sodium pentobarbital-induced sedation and Y1(-/-) mice were less sensitive to this anesthetic. However, Y2(-/-) mice display increased sensitivity, showing that Y2 modulates GABAergic induced sedation both pharmacologically and physiologically and has a functionally opposing role to the Y1 receptor. Analysis of Y1(-/-)/Y2(-/-) double mutant mice show that increased sensitivity by Y1 occurs independent of the Y2 receptor, while the decreased sensitivity mediated by Y2 depend on an intact Y1 receptor. In contrast to sodium pentobarbital, both Y1 and Y2 receptors increase the sensitivity in a collaborative fashion to NMDA antagonist-induced sedation. These data demonstrate the physiological and pharmacological impact of the Y1 and Y2 receptors on sedation.

  15. All about ketamine premedication for children undergoing ophtalmic surgery

    Science.gov (United States)

    Altiparmak, Başak; Akça, Başak; Yilbaş, Aysun Ankay; Çelebi, Nalan

    2015-01-01

    Ketamine is a non-barbiturate cyclohexamine derivative which produces a state of sedation, immobility, analgesia, amnesia, and dissociation from the environment. One of the most important advantages of ketamine premedication is production of balanced sedation with less respiratory depression and less changes in blood pressure or heart rate. As its effects on intracranial pressure, the possible effect of ketamine on intraocular pressure has been controversial overtime. In this study, we aimed to demostrate all the advantages and possible side effects of ketamine premedication in 100 children with retinablastoma undergoing ophthalmic surgery. All the children were premedicated with ketamine 5 mg kg-1 15 minutes before the examination orally and peroperative complications, reaction to intravenous catheter insertion, need for additive dose and intraocular pressures of children were recorded. We showed that ketamine administration orally is a safe and effective way of premedication for oncologic patients undergoing examination under general anaesthesia. The incidence of agitation, anxiety at parental separation and reaction to insertion of intravenous catheter was very low while adverse side effects were seen rarely. Intraocular pressure which is very important for most of the ophthalmic surgery patients remained in normal ranges. PMID:26885101

  16. Drugs Used in Sexual Assaults: Features and Toxicological Investigations

    Directory of Open Access Journals (Sweden)

    Pinar Efeoglu

    2013-06-01

    Full Text Available Drugs used in sexual assault, which are also called as date rape drugs, are common phenomenon of crime in many countries. In a typical scenario, a perpetrator adds a date-rape drug which has sedative effect into alcoholic or non-alcoholic beverage of an unsuspecting person. After drug administration, mostly amnesia and symptoms such as confussion, loss of memory, lack of muscle control, dizziness occur. The main drugs in sexual assaults are benzodiazepines such as γ-hydroxy butyrate and its analogs, clonazepam, alprazolam, flunitrazepam, oxazepam, ketamine, barbiturates, antidepressants, cocaine and stimulants. Most of these drugs are colorless, odorless and highly soluble in alcohol or other beverages quickly. They are rapidly absorbed and eliminated after oral administration. A victim may complain to police or other legal forces after several days due to emotional trauma as shame, fear, doubt and disbelief. For this reason, It is important to know what time the sample is taken from the victim to confirm the presence of the drug. In this study, we will present a general approach to date-rape drugs used in sexual assault. [Archives Medical Review Journal 2013; 22(3.000: 418-425

  17. [Anesthesia in the pleuropulmonary complications surgery of tuberculosis: a 79 cases study].

    Science.gov (United States)

    Kane, O; Diouf, E; Beye, M D; Diarra, O; Ndoye Diop, M; Diouf, M; Ndiaye, M; Ka Sall, B

    2003-01-01

    Reported is a retrospective study carried out from Aristide Le Dantec Hospital in patients who underwent pleuropulmonary surgery after tuberculosis complication, from June 1995 to June 1999. The aim of this study was to evaluate the anaesthesiology procedures and outcomes of tuberculosis pleuropulmonary complications surgery. Seventy nine patients were studied. Their mean age was 34.63 years, and the sex ratio was 3.14. They all underwent general anaesthesia procedures with barbituric, morphinics et myorelaxants drugs. The peroperative complications noted were distributed as follow: 50 cases of haemorrhage needing transfusion, 18 cases of hypotension associated to the anaesthesia. In the intensive care period, we have noticed 30 atelectasia cases associated to a spastic bronchopathy, 3 cases of pulmonary oedema and 1 case of pulmonary infarctus. In the postoperative period, 8 cases of hemodynamic instability occurred, including 5 cases of cardiovascular collapsus treated by filling, and 2 septic shocks cases. An infectious bronchopneumopathy was noticed on 11 patients with two cases of septicaemia. The mortality rate was 6.3% (5 cases of death). The pleuropulmonary surgery in tuberculosis complication is very haemorrhagic, and therefore require an adequate preoperative preparation.

  18. Concurrent and simultaneous polydrug use: latent class analysis of an Australian nationally representative sample of young adults.

    Directory of Open Access Journals (Sweden)

    Lake-Hui eQuek

    2013-11-01

    Full Text Available Background: Alcohol use and illicit drug use peak during young adulthood (around 18-29 years of age, but comparatively little is known about polydrug use in nationally representative samples of young adults. Drawing on a nationally representative cross-sectional survey (Australian National Drug Strategy Household Survey, this study examines polydrug use patterns and associated psychosocial risk factors among young adults (n = 3,333; age 19-29. Method: The use of a broad range of licit and illicit drugs were examined, including alcohol, tobacco, cannabis, cocaine, hallucinogens, ecstasy, ketamine, GHB, inhalants, steroids, barbiturates, meth/amphetamines, heroin, methadone/buprenorphine, other opiates, painkillers and tranquillizers/sleeping pills. Latent class analysis was employed to identify patterns of polydrug use. Results: Polydrug use in this sample was best described using a 5-class solution. The majority of young adults predominantly used alcohol only (52.3%, alcohol and tobacco (34.18%. The other classes were cannabis, ecstasy, and licit drug use (9.4%, cannabis, amphetamine derivative, and licit drug use (2.8%, and sedative and alcohol use (1.3%. Young adult males with low education and/or high income were most at risk of polydrug use. Conclusion: Almost half of young adults reported polydrug use, highlighting the importance of post-high school screening for key risk factors and polydrug use profiles, and the delivery of early intervention strategies targeting illicit drugs.

  19. Evaluation of a human on-site urine multidrug test for emergency use with dogs.

    Science.gov (United States)

    Teitler, Joan B

    2009-01-01

    A rapid, human on-site urine multidrug test was used to screen canine urine samples for the presence of five illegal drugs and drugs from three commonly abused drug classes. Each sample was sent to a toxicology laboratory for gas chromatography/mass spectrometry (GC/MS) validation. On-site test results and GC/MS assays confirmed that the human on-site test kit did identify barbiturates, opiates, benzodiazepines, and amphetamines/methamphetamines in urine from dogs that had received these common illicit drugs/drug classes either intravenously and/or orally. However, neither the on-site test kit nor the GC/MS individual assays for marijuana or methadone, a synthetic opiate, were effective in identifying marijuana and methadone in urine from dogs with suspected or known exposure. No index of suspicion was seen for exposure to phencyclidines or cocaine during the study period, and no exposures were indicated by the on-site test results. Overall, the test is a rapid, readily available, affordable, and useful complement to the veterinarian's clinical consideration and professional judgment.

  20. Urine levels of drugs for which Triage DOA screening was positive.

    Science.gov (United States)

    Moriya, Fumio

    2009-04-01

    The purpose of this study was to investigate the relationship between urine levels of target drugs of abuse for which Triage DOA gave positive results, as well as the cut-off levels for these drugs. Thirty-eight forensic urine samples positive for commonly abused drugs were involved. Of these samples, 12 were positive for barbiturates (BAR), 11 for benzodiazepines (BZO), 8 for opiates (OPI), 7 for amphetamines (AMP), and 4 for tricyclic antidepressants (TCA). In the BAR-positive urine samples, phenobarbital, amobarbital or barbital was detected at concentrations higher than cut-off levels. In the BZO-positive samples, diazepam, nordiazepam, triazolam, nitrazepam and/or midazolam was detected at concentrations lower than cut-off levels; in the triazolam-involved urine, alpha-hydroxytriazolam, a metabolite of triazolam, showed concentrations higher than cut-off level. In the AMP-positive samples, methamphetamine was detected at concentrations higher than cut-off level. Urine samples positive for OPI contained total dihydrocodeine, codeine or morphine at concentrations higher than cut-off levels. In TCA-positive samples, amitriptyline was detected at concentrations higher or lower than cut-off level, and clomipramine was detected at a concentration much lower than cut-off level. Metabolites of BZO and TCA, which are not typically analyzed by instrumental procedures, may cross-react to varying degrees with the antibodies used for Triage DOA.

  1. Urine drug testing of chronic pain patients: licit and illicit drug patterns.

    Science.gov (United States)

    Cone, Edward J; Caplan, Yale H; Black, David L; Robert, Timothy; Moser, Frank

    2008-10-01

    Chronic pain patients are frequently maintained on one or more powerful opioid medications in combination with other psychoactive medications. Urine tests provide objective information regarding patient compliance status. Little information is available on testing this unique population. The goal of this study was to characterize drug disposition patterns in urine specimens collected from a large population of pain patients. Confirmation data for 10,922 positive specimens were collated into 11 drug Classes. The number of drug/metabolites tested (#) and number of confirmed positive specimens were as follows: amphetamines (7), 160; barbiturates (5), 308; benzodiazepines (6), 2397; cannabinoids (1), 967; carisoprodol (2), 611; cocaine (1), 310; fentanyl (1), 458; meperidine (2), 58; methadone (2), 1209; opiates (7), 8996; and propoxyphene (2), 385. Subdivision into 19 distinct drug Groups allowed characterization of drug use patterns. Of the 10,922 positive specimens, 15,859 results were reported as positive in various drug Classes, and 27,197 drug/metabolites were measured by gas chromatography-mass spectrometry. The frequency of illicit drug use (cannabis, cocaine, ecstasy) was 10.8%. Being the first study of this type, these data present a large array of information on licit and illicit drug use, drug detection frequencies, drug/metabolite patterns, and multi-drug use combinations in pain patients.

  2. False-positive interferences of common urine drug screen immunoassays: a review.

    Science.gov (United States)

    Saitman, Alec; Park, Hyung-Doo; Fitzgerald, Robert L

    2014-09-01

    Urine drug screen (UDS) immunoassays are a quick and inexpensive method for determining the presence of drugs of abuse. Many cross-reactivities exist with other analytes, potentially causing a false-positive result in an initial drug screen. Knowledge of these potential interferents is important in determining a course of action for patient care. We present an inclusive review of analytes causing false-positive interferences with drugs-of-abuse UDS immunoassays, which covers the literature from the year 2000 to present. English language articles were searched via the SciFinder platform with the strings 'false positive [drug] urine' yielding 173 articles. These articles were then carefully analyzed and condensed to 62 that included data on causes of false-positive results. The discussion is separated into six sections by drug class with a corresponding table of cross-reacting compounds for quick reference. False-positive results were described for amphetamines, opiates, benzodiazepines, cannabinoids, tricyclic antidepressants, phencyclidine, lysergic acid diethylamide and barbiturates. These false-positive results support the generally accepted practice that immunoassay positive results are considered presumptive until confirmed by a second independent chemical technique.

  3. Positive predictive values of abused drug immunoassays on the Beckman Synchron in a veteran population.

    Science.gov (United States)

    Dietzen, D J; Ecos, K; Friedman, D; Beason, S

    2001-04-01

    The pressure to reduce the cost of analytic testing makes it tempting to discontinue routine confirmation of urine specimens positive for drugs of abuse by immunoassay. Beyond the economic motivation, the requirement for confirmation should be driven by the positive predictive value of the screening tests. We have quantitated positive predictive values of our screening immunoassays in a large metropolitan Veterans Affairs Medical Center. We reviewed the confirmatory rate of urine specimens positive for drugs of abuse with Beckman Synchron reagents from June 1998 to June 1999 and tabulated the false-positive screening rate. There were 175 instances of false-positive screens during the 13 months we analyzed. Positive predictive values ranged from 0% (amphetamine) to 100% (THC). We determined that the low positive predictive value of the amphetamine assay in our laboratory was primarily due to the use of ranitidine (Zantac). Urine specimens containing greater than 43 microg/mL ranitidine were positive in our amphetamine assay. This concentration is routinely exceeded in our patients taking ranitidine. In our clinical and analytic setting, the Beckman THC assay did not require confirmation. The positive predictive values of the Beckman opiate, cocaine, barbiturate, propoxyphene, and methadone immunoassays dictate routine confirmatory testing in specimens that screen positive for these substances. Finally, because of its extreme sensitivity to ranitidine, the Beckman amphetamine assay has little utility in our laboratory setting.

  4. Screening and confirmation of 62 drugs of abuse and metabolites in urine by ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry.

    Science.gov (United States)

    Tsai, I-Lin; Weng, Te-I; Tseng, Yufeng J; Tan, Happy Kuy-Lok; Sun, Hsiao-Ju; Kuo, Ching-Hua

    2013-01-01

    An ultra-high-performance liquid chromatography--quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) method for the screening and confirmation of 62 drugs of abuse and their metabolites in urine was developed in this study. The most commonly abused drugs, including amphetamines, opioids, cocaine, benzodiazepines (BZDs) and barbiturates, and many other new and emerging abused drugs, were selected as the analytes for this study. Urine samples were diluted 5-fold with deionized water before analysis. Using a superficially porous micro-particulate column and an acetic acid-based mobile phase, 54 basic and 8 acidic analytes could be detected within 15 and 12 min in positive and negative ionization modes, respectively. The MS collision energies for the 62 analytes were optimized, and their respective fragmentation patterns were constructed in the in-house library for confirmatory analysis. The coefficients of variation of the intra- and inter-day precision of the analyte responses all were urine samples from patients undergoing methadone treatment were analyzed by the developed UHPLC-QTOF-MS method, and the results were compared with the immunoassay method.

  5. Therapeutic implications of melatonin in cerebral edema.

    Science.gov (United States)

    Rathnasamy, Gurugirijha; Ling, Eng-Ang; Kaur, Charanjit

    2014-12-01

    Cerebral edema/brain edema refers to the accumulation of fluid in the brain and is one of the fatal conditions that require immediate medical attention. Cerebral edema develops as a consequence of cerebral trauma, cerebral infarction, hemorrhages, abscess, tumor, hypoxia, and other toxic or metabolic factors. Based on the causative factors cerebral edema is differentiated into cytotoxic cerebral edema, vasogenic cerebral edema, osmotic and interstitial cerebral edema. Treatment of cerebral edema depends on timely diagnosis and medical assistance. Pragmatic treatment strategies such as antihypertensive medications, nonsteroidal anti-inflammatory drugs, barbiturates, steroids, glutamate and N-methyl-D-aspartate receptor antagonists and trometamol are used in clinical practice. Although the above mentioned treatment approaches are being used, owing to the complexity of the mechanisms involved in cerebral edema, a single therapeutic strategy which could ameliorate cerebral edema is yet to be identified. However, recent experimental studies have suggested that melatonin, a neurohormone produced by the pineal gland, could be an effective alternative for treating cerebral edema. In animal models of stroke, melatonin was not only shown to reduce cerebral edema but also preserved the blood brain barrier. Melatonin's beneficial effects were attributed to its properties, such as being a potent anti-oxidant, and its ability to cross the blood brain barrier within minutes after its administration. This review summarizes the beneficial effects of melatonin when used for treating cerebral edema.

  6. Long-Lasting Effects of GABA Infusion Into the Cerebral Cortex of the Rat

    Science.gov (United States)

    Montiel, Teresa; Almeida, Daniel; Arango, Iván; Calixto, Eduardo; Casasola, César; Brailowsky, Simón

    2000-01-01

    In electrophysiological terms, experimental models of durable information storage in the brain include long-term potentiation (LTP), long-term depression, and kindling. Protein synthesis correlates with these enduring processes. We propose a fourth example of long-lasting information storage in the brain, which we call the GABA-withdrawal syndrome (GWS). In rats, withdrawal of a chronic intracortical infusion of GABA, a ubiquitous inhibitory neurotransmitter, induced epileptogenesis at the infusion site. This overt GWS lasted for days. Anisomycin, a protein synthesis inhibitor, prevented the appearance of GWS in vivo. Hippocampal and neocortical slices showed a similar post-GABA hyperexcitability in vitro and an enhanced susceptibility to LTP induction. One to four months after the epileptic behavior disappeared, systemic administration of a subconvulsant dose of pentylenetetrazol produced the reappearance of paroxysmal activity. The long-lasting effects of tonic GABAA receptor stimulation may be involved in long-term information storage processes at the cortical level, whereas the cessation of GABAA receptor stimulation may be involved in chronic pathological conditions, such as epilepsy. Furthermore, we propose that GWS may represent a common key factor in the addiction to GABAergic agents (for example, barbiturates, benzodiazepines, and ethanol). GWS represents a novel form of neurono-glial plasticity. The mechanisms of this phenomenon remain to be understood. PMID:10709209

  7. Refractory High Intracranial Pressure following Intraventricular Hemorrhage due to Moyamoya Disease in a Pregnant Caucasian Woman

    Science.gov (United States)

    Montiel, Virginie; Grandin, Cécile; Goffette, Pierre; Fomekong, Edward; Hantson, Philippe

    2009-01-01

    Intraventricular hemorrhage during pregnancy is usually followed by a poor recovery. When caused by moyamoya disease, ischemic or hemorrhagic episodes may complicate the management of high intracranial pressure. A 26-year-old Caucasian woman presented with generalized seizures and a Glasgow Coma Score (GCS) of 3 during the 36th week of pregnancy. The fetus was delivered by caesarean section. The brain CT in the mother revealed bilateral intraventricular hemorrhage, a callosal hematoma, hydrocephalus and right frontal ischemia. Refractory high intracranial pressure developed and required bilateral ventricular drainage and intensive care treatment with barbiturates and hypothermia. Magnetic resonance imaging and cerebral angiography revealed a moyamoya syndrome with rupture of the abnormal collateral vascular network as the cause of the hemorrhage. Intracranial pressure could only be controlled after the surgical removal of the clots after a large opening of the right ventricle. Despite an initially low GCS, this patient made a good functional recovery at one year follow-up. Management of refractory high intracranial pressure following moyamoya related intraventricular bleeding should require optimal removal of ventricular clots and appropriate control of cerebral hemodynamics to avoid ischemic or hemorrhagic complications. PMID:20508823

  8. Treatment of drug-induced seizures.

    Science.gov (United States)

    Chen, Hsien-Yi; Albertson, Timothy E; Olson, Kent R

    2016-03-01

    Seizures are a common complication of drug intoxication, and up to 9% of status epilepticus cases are caused by a drug or poison. While the specific drugs associated with drug-induced seizures may vary by geography and change over time, common reported causes include antidepressants, stimulants and antihistamines. Seizures occur generally as a result of inadequate inhibitory influences (e.g., gamma aminobutyric acid, GABA) or excessive excitatory stimulation (e.g. glutamate) although many other neurotransmitters play a role. Most drug-induced seizures are self-limited. However, status epilepticus occurs in up to 10% of cases. Prolonged or recurrent seizures can lead to serious complications and require vigorous supportive care and anticonvulsant drugs. Benzodiazepines are generally accepted as the first line anticonvulsant therapy for drug-induced seizures. If benzodiazepines fail to halt seizures promptly, second line drugs include barbiturates and propofol. If isoniazid poisoning is a possibility, pyridoxine is given. Continuous infusion of one or more anticonvulsants may be required in refractory status epilepticus. There is no role for phenytoin in the treatment of drug-induced seizures. The potential role of ketamine and levetiracetam is promising but not established.

  9. Imprinting of cerebral cytochrome P450s in offsprings prenatally exposed to cypermethrin augments toxicity on rechallenge

    Science.gov (United States)

    Singh, Anshuman; Agrahari, Anita; Singh, Radhadutt; Yadav, Sanjay; Srivastava, Vikas; Parmar, Devendra

    2016-11-01

    Epigenetic studies were carried in the rat offsprings, born to dams treated with cypermethrin (orally; 5.0 mg/kg) from gestation day (GD) 5 to 21 and rechallenged with cypermethrin (orally; 10 mg/kg for 6 days), at adulthood (12 weeks) to understand the mechanism underlying the overexpression of cerebral cytochrome P450s (CYPs) in exposed offsprings. The data revealed alterations in histone H3 acetylation and DNA methylation in promoter regions of CYP1A- and 2B- isoenzymes in the brain isolated from rechallenged animals. Further, bisulphite sequencing revealed critical CpG methylation changes in BARBIE BOX (Barbiturate response element) and BTE (Basal transcription element) in promoter of CYP2B1 in the brain isolated from rechallenged animals. Western blotting and DNA laddering/fragmentation studies revealed a greater magnitude of increase in the signalling pathways associated with apoptosis in the rechallenged animals. The data have indicated that overexpression of cerebral CYPs could be due to the imprinting of CYPs. Further, increased apoptosis observed in the rechallenged offsprings has suggested that these epigenetic changes in CYPs may predispose the prenatally exposed offsprings to the neurotoxic effects of other centrally acting drugs and chemicals when subsequently rechallenged later at life.

  10. The role of serendipity in the discovery of the clinical effects of psychotropic drugs: beyond of the myth.

    Science.gov (United States)

    López-Muñoz, Francisco; Baumeister, Alan A; Hawkins, Mike F; Alamo, Cecilio

    2012-01-01

    The serendipity is the faculty for making a discovery through a combination of accident and sagacity. In psychopharmacology, the serendipity played a key role in the discovery of many psychotropic drugs, although there are marked disputes in this regard, possibly due to semantic differences in relation to the meaning of this term. We have implemented an operational definition of serendipity based on the discovery of something unexpected or not sought intentionally, irrespective of the systematic process leading to the accidental observation. The present paper analyses some representative examples of discoveries in the field of psychopharmacology according to different serendipitous intervention patterns. Following this approach there would be four different imputability patterns: pure serendipitous discoveries (valproic acid/valproate); serendipitous observation leading to a non-serendipitous discoveries (imipramine); non-serendipitous discoveries secondarily associated with serendipitous observation (barbiturates); non-serendipitous discoveries (haloperidol). We can conclude that pure serendipitous discoveries in this field are not very frequent, most common being a mixed pattern; an initial serendipitous observation which leads to a non-serendipitous discovery of clinical utility. This is the case of imipramine, lithium salts, chlorpromazine or meprobamate.

  11. [Development and application of electroanalytical methods in biomedical fields].

    Science.gov (United States)

    Kusu, Fumiyo

    2015-01-01

    To summarize our electroanalytical research in the biomedical field over the past 43 years, this review describes studies on specular reflection measurement, redox potential determination, amperometric acid sensing, HPLC with electrochemical detection, and potential oscillation across a liquid membrane. The specular reflection method was used for clarifying the adsorption of neurotransmitters and their related drugs onto a gold electrode and the interaction between dental alloys and compound iodine glycerin. A voltammetric screening test using a redox potential for the antioxidative effect of flavonoids was proposed. Amperometric acid sensing based on the measurement of the reduction prepeak current of 2-methyl-1,4-naphthoquinone (VK3) or 3,5-di-tert-buty1-1,2-benzoquinone (DBBQ) was applied to determine acid values of fats and oils, titrable acidity of coffee, and enzyme activity of lipase, free fatty acids (FFAs) in serum, short-chain fatty acids in feces, etc. The electrode reactions of phenothiazines, catechins, and cholesterol were applied to biomedical analysis using HPLC with electrochemical detection. A three-channel electrochemical detection system was utilized for the sensitive determination of redox compounds in Chinese herbal medicines. The behavior of barbituric acid derivatives was examined based on potential oscillation measurements.

  12. Coma blisters in two postoperative patients.

    Science.gov (United States)

    Chacon, Anna H; Farooq, Uzma; Choudhary, Sonal; Yin, Natalie; Nolan, Bridgit; Shiman, Michael; Milikowski, Clara; Izakovic, Jan; Elgart, George W

    2013-05-01

    Coma blisters are self-limited cutaneous bullae that occur in the setting of loss of consciousness because of a drug, illness, or accident, with the most common settings being barbiturate overdose and neurological disorders. The etiology behind coma blisters is poorly understood and is not related to underlying infections or autoimmune conditions. The clinical presentation consists of bullae, erosions, and violaceous plaques usually involving sites of pressure. The skin lesions usually occur within 48-72 hours of the start of a coma and resolve within 2-4 weeks. We present one case of a 5-month-old infant with severe valvular disease who required surgical repair. He was placed on extra corporeal membrane oxygenation and developed multiple tense coma blisters during the course of therapy. Skin biopsy revealed a noninflammatory subepidermal blister with necrosis of the overlying epidermis and necrosis of the eccrine ducts. We also present a second case of an 18-year-old female patient who underwent surgical resection of a benign mandibular tumor. She subsequently developed bullae on both arms 4 days after surgery. The skin biopsy showed a necrotic epidermis, a subepidermal blister, and diffuse necrosis of the eccrine coils.

  13. Membrane damage by bile salts: the protective function of phospholipids.

    Science.gov (United States)

    Martin, G P; Marriott, C

    1981-12-01

    The direct toxicity of sodium deoxycholate (SDC) and lysophosphatidylcholine (LPC) to biological membranes was assessed by measurement of goldfish overturn time. When phosphatidylcholine (PC) was incorporated into the aqueous media, the toxicity of both SDC and LPC was reduced, as indicated by increased overturn time. Fish were also pretreated for various times in media containing (a) 1 mM SDC and (b) 1 mM SDC with 1 mM PC. Subsequent transfer to solution, 100 mg litre-1 quinalbarbitone sodium showed that reciprocal overturn times for fish treated using method (a) increased linearly with duration of pretreatment up to a limiting value, obtained after 20 min exposure; 40 min exposure to 1 mM SDC was directly toxic. Fish pretreated using regimen (b) survived longer when challenged with barbiturate, and the reciprocal overturn times were a linear function of time of pretreatment up to at least 40 min. PC also provided protection against membrane damage caused by the synthetic surfactant sodium dodecyl sulphate. Mixed micelle formation between PC and surfactant is thought to account for the protective effects. The results are of significance in the consideration of reflux hypothesis for the aetiology of gastric ulceration and also the possible formulation of drug delivery systems intended to enhance absorption whilst minimizing gastrointestinal damage.

  14. New-Onset Refractory Status Epilepticus: More Investigations, More Questions

    Directory of Open Access Journals (Sweden)

    Philippe Dillien

    2016-06-01

    Full Text Available A 27-year-old previously healthy woman was admitted to the hospital with recurrent seizures. Status epilepticus developed that became refractory to third-line therapy with propofol and barbiturates. The patient had a very extensive diagnostic workup including autoimmune, viral and genetic investigations. A tentative immune therapy was proposed with high doses of steroids and plasma exchanges. Our patient had an inherited heterozygous single nucleotide variant in the sequence c.1280A>G [p.Lys427Arg] of the SMC3 gene that was insufficient to explain the seizures. Surprisingly, IgM antibodies against Japanese encephalitis virus were positive on the serum drawn 11 days after symptom onset, as detected by ELISA and the immunofluorescence antibody (IFA technique. IgG antibodies were also positive using the IFA technique, but not with ELISA. The same investigations as well as the detection of the viral genome by the q-RT-PCR technique were negative on cerebrospinal fluid. Despite the suspicion of a viral infection, we concluded that our patient had a new-onset refractory status epilepticus of cryptogenic origin. Termination of the status epilepticus was obtained after 47 days, with a possible benefit from the introduction of ketamine.

  15. Neurologic management following cardiac arrest.

    Science.gov (United States)

    Bircher, N G

    1989-10-01

    Optimal neurologic outcome after cardiac arrest requires careful attention to the details of both intracranial and extracranial homeostasis. A high index of suspicion regarding the potential causes and complications of cardiac arrest facilitates discovery and treatment of problems before they adversely affect neurologic outcome. The future is bright for resuscitation research: Our fundamental understanding of cerebral ischemia and its consequences has dramatically improved, and this knowledge can hopefully be transferred to clinical useful modes of therapy. However, the transition from a promising, therapeutically effective intervention in animals to the demonstration that treatment is effective following cardiac arrest in humans is an important and difficult step. The patient population is heterogeneous before the insult, the duration and severity of the insult are variable, and the effectiveness of cardiopulmonary resuscitation varies among institutions. Therefore, the only means of demonstrating clinical efficacy is the performance of a large clinical trial. The Resuscitation Research Center at the University of Pittsburgh has developed and coordinated a multicenter, multinational team of investigators who have completed one definitive trial of postarrest barbiturate therapy and are currently completing a similar trial using a calcium entry blocker. Despite the formidable obstacles posed by such comprehensive efforts, they provide the mechanism for determining whether the cost of a new treatment modality is justified by the likelihood of improved mortality or morbidity.

  16. Interlaboratory studies with the Chinese hamster V79 cell metabolic cooperation assay to detect tumor-promoting agents

    Energy Technology Data Exchange (ETDEWEB)

    Bohrman, J.S.; Burg, J.R.; Elmore, E.; Gulati, D.K.; Barfknecht, T.R.; Niemeier, R.W.; Dames, B.L.; Toraason, M.; Langenbach, R.

    1988-01-01

    Three laboratories participated in an interlaboratory study to evaluate the usefulness of the Chinese hamster V79 cell metabolic cooperation assay to predict the tumor-promoting activity of selected chemical. Twenty-three chemicals of different chemical structures (phorbol esters, barbiturates, phenols, artificial sweeteners, alkanes, and peroxides) were chosen for testing based on in vivo promotion activities, as reported in the literature. Assay protocols and materials were standardized, and the chemicals were coded to facilitate unbiased evaluation. A chemical was tested only once in each laboratory, with one of the three laboratories testing only 15 out of 23 chemicals. Dunnett's test was used for statistical analysis. Chemicals were scored as positive (at least two concentration levels statistically different than control), equivocal (only one concentration statistically different), or negative. For 15 chemicals tested in all three laboratories, there was complete agreement among the laboratories for nine chemicals. For the 23 chemicals tested in only two laboratories, there was agreement on 16 chemicals. With the exception of the peroxides and alkanes, the metabolic cooperation data were in general agreement with in vivo data. However, an overall evaluation of the V79 cell system for predicting in vivo promotion activity was difficult because of the organ specificity of certain chemicals and/or the limited number of adequately tested nonpromoting chemicals.

  17. Rapid ultraviolet monitoring of multiple psychotropic drugs with a renewable microfluidic device.

    Science.gov (United States)

    Sheng, Jin; Lei, Jianping; Ju, Huangxian; Song, Chaojin; Zhang, Daming

    2010-10-29

    A rapid method for sensitive ultraviolet detection of multiple psychotropic drugs in human plasma was developed on a low-cost and expediently fabricated hybrid microfluidic device. The device was composed of one fused-silica capillary with a sampling fracture, a poly(methyl methacrylate) board with four reservoirs, and a printed circuit board. At the optimal separation and detection conditions, the baseline separation of three kinds of psychotropic drugs including barbiturates (phenobarbital and barbital), benzodiazepines (nitrazepam, clonazepam, chlordiazepoxide, alprazolam and diazepam) and tricyclic antidepressant drugs (amitriptyline) was achieved within 200 s with separation efficiency up to 3.80 × 10(5) plates m(-1). The linear ranges for ultraviolet detection were from 2.0 to 1000.0 μg mL(-1) for chlordiazepoxide and 1.0 to 1000.0 μg mL(-1) for other seven drugs. Combining with solid-phase extraction, this novel protocol could successfully be used to screen naturally existing psychotropic drugs in a known human plasma sample. The minimum detectable concentration was down to 27 ng mL(-1) for phenobarbital spiked in plasma. This work provided a promising way to initially screen different psychotropic drugs with high resolution, rapid separation and low-cost.

  18. Therapeutic approaches to cerebral vasospasm complicating ruptured aneurysm

    Directory of Open Access Journals (Sweden)

    Mohamed Barbarawi

    2009-10-01

    Full Text Available Cerebral vasospasm is a serious complication of ruptured aneurysm. In order to avoid short- and long-term effects of cerebral vasospasm, and as there is no single or optimal treatment modality employed, we have instituted a protocol for the prevention and treatment of vasospasm in patients suffering aneurysmal sub-arachnoid hemorrhage (SAH. We then reviewed the effectiveness of this protocol in reducing the mortality and morbidity rate in our institution. In this study we present a retrospective analysis of 52 cases. Between March 2004 and December 2008 52 patients were admitted to our service with aneurysmal SAH. All patients commenced nimodipine, magnesium sulphate (MgSO4 and triple H therapy. Patients with significant reduction in conscious level were intubated, ventilated and sedated. Intracranial pressure (ICP monitoring was used for intubated patients. Sodium thiopental coma was induced for patients with refractory high ICP; angiography was performed for diagnosis and treatment. Balloon angioplasty was performed if considered necessary. Using this protocol, only 13 patients (25% developed clinical vaso-spasm. Ten of them were given barbiturates to induce coma. Three patients underwent transluminal balloon angioplasty. Four out of 52 patients (7.7% died from severe vasospasm, 3 patients (5.8% became severely disabled, and 39 patients (75% were discharged in a condition considered as either normal or near to their pre-hemorrhage status. Our results confirm that the aforementioned protocol for treatment of cerebral vasospasm is effective and can be used safely.

  19. Alcohol and marijuana effects on ocular tracking.

    Science.gov (United States)

    Flom, M C; Brown, B; Adams, A J; Jones, R T

    1976-12-01

    Experienced alcohol and marijuana users were instructed to track with their eyes a small spot that moved horizontally back and forth in pendular (sinusoidal) motion across a 7.5-degree field. The frequency of spot oscillation was gradually increased from 0.5 to 3.0 Hz in 40 sec. Eye movement recordings showed the frequency at which smooth tracking and, soon thereafter, saccadic tracking broke down. These smooth and saccadic cutoff frequencies were reduced after administration of alcohol, but not after marijuana or placebo. For low alcohol doses, smooth tracking was impaired and saccadic tracking was unaffected, much like an effect previously reported for barbiturates. Alcohol seems to affect smooth tracking by increasing the central processing time required to generate the appropriate eye movement. It affects saccadic tracking by slightly decreasing saccadic velocity and to a greater extent by increasing latency time, part of which may be devoted to central processing. The site of action of alcohol appears to be central to both the paramedian pontine reticular formation and the flocculus of the cerebellum.

  20. Study of orotidine 5'-monophosphate decarboxylase in complex with the top three OMP, BMP, and PMP ligands by molecular dynamics simulation.

    Science.gov (United States)

    Jamshidi, Shirin; Jalili, Seifollah; Rafii-Tabar, Hashem

    2015-01-01

    Catalytic mechanism of orotidine 5'-monophosphate decarboxylase (OMPDC), one of the nature most proficient enzymes which provides large rate enhancement, has not been fully understood yet. A series of 30 ns molecular dynamics (MD) simulations were run on X-ray structure of the OMPDC from Saccharomyces cerevisiae in its free form as well as in complex with different ligands, namely 1-(5'-phospho-D-ribofuranosyl) barbituric acid (BMP), orotidine 5'-monophosphate (OMP), and 6-phosphonouridine 5'-monophosphate (PMP). The importance of this biological system is justified both by its high rate enhancement and its potential use as a target in chemotherapy. This work focuses on comparing two physicochemical states of the enzyme (protonated and deprotonated Asp91) and three ligands (substrate OMP, inhibitor, and transition state analog BMP and substrate analog PMP). Detailed analysis of the active site geometry and its interactions is properly put in context by extensive comparison with relevant experimental works. Our overall results show that in terms of hydrogen bond occupancy, electrostatic interactions, dihedral angles, active site configuration, and movement of loops, notable differences among different complexes are observed. Comparison of the results obtained from these simulations provides some detailed structural data for the complexes, the enzyme, and the ligands, as well as useful insights into the inhibition mechanism of the OMPDC enzyme. Furthermore, these simulations are applied to clarify the ambiguous mechanism of the OMPDC enzyme, and imply that the substrate destabilization and transition state stabilization contribute to the mechanism of action of the most proficient enzyme, OMPDC.

  1. Exploring the potential effect of Ocimum sanctum in vincristine-induced neuropathic pain in rats

    Directory of Open Access Journals (Sweden)

    Jaggi Amteshwar

    2010-01-01

    Full Text Available Abstract The present study was designed to investigate the ameliorative potential of Ocimum sanctum and its saponin rich fraction in vincristine-induced peripheral neuropathic pain in rats. Peripheral neuropathy was induced in rats by administration of vincristine sulfate (50 μg/kg i.p. for 10 consecutive days. The mechanical hyperalgesia, cold allodynia, paw heat hyperalgesia and cold tail hyperalgesia were assessed by performing the pinprick, acetone, hot plate and cold tail immersion tests, respectively. Biochemically, the tissue thio-barbituric acid reactive species (TBARS, super-oxide anion content (markers of oxidative stress and total calcium levels were measured. Vincristine administration was associated with the development of mechanical hyperalgesia, cold allodynia, heat and cold hyperalgesia. Furthermore, vincristine administration was also associated with an increase in oxidative stress and calcium levels. However, administration of Ocimum sanctum (100 and 200 mg/kg p.o. and its saponin rich fraction (100 and 200 mg/kg p.o. for 14 days significantly attenuated vincristine-induced neuropathic pain along with decrease in oxidative stress and calcium levels. It may be concluded that Ocimum sanctum has ameliorative potential in attenuating chemotherapy induced-painful neuropathic state, which may be attributed to decrease in oxidative stress and calcium levels. Furthermore, saponin rich fraction of Ocimum sanctum may be responsible for its noted beneficial effect in neuropathic pain in rats.

  2. Ameliorative potential of Ocimum sanctum in chronic constriction injury-induced neuropathic pain in rats

    Directory of Open Access Journals (Sweden)

    GURPREET KAUR

    2015-03-01

    Full Text Available The present study was designed to investigate the ameliorative potential of Ocimumsanctum and its saponin rich fraction in chronic constriction injury-induced neuropathic pain in rats. The chronic constriction injury was induced by placing four loose ligatures around the sciatic nerve, proximal to its trifurcation. The mechanical hyperalgesia, cold allodynia, paw heat hyperalgesia and cold tail hyperalgesia were assessed by performing the pinprick, acetone, hot plate and cold tail immersion tests, respectively. Biochemically, the tissue thio-barbituric acid reactive species, super-oxide anion content (markers of oxidative stress and total calcium levels were measured. Chronic constriction injury was associated with the development of mechanical hyperalgesia, cold allodynia, heat and cold hyperalgesia along with an increase in oxidative stress and calcium levels. However, administration of Ocimumsanctum (100 and 200 mg/kg p.o. and its saponin rich fraction (100 and 200 mg/kg p.o. for 14 days significantly attenuated chronic constriction injury-induced neuropathic pain as well as decrease the oxidative stress and calcium levels. It may be concluded that saponin rich fraction of Ocimum sanctum has ameliorative potential in attenuating painful neuropathic state, which may be attributed to a decrease in oxidative stress and calcium levels.

  3. Survey of patients with acute poisoning seen in the Emergency Department of the University Hospital of Gent between 1983 and 1990.

    Science.gov (United States)

    Verstraete, A G; Buylaert, W A

    1995-12-01

    In a prospective study of 4234 patients with acute poisoning in the Emergency Department of the University Hospital of Gent in Belgium between 1983 and 1990, we observed a decline in the number of poisonings from 665 in 1983 to 424 in 1990. This was due to a decrease in the number of deliberate self-poisonings. Fifty-six per cent of patients were female and the most prevalent age group was 20 to 24 years. There was no seasonal variation. The substances most frequently taken were benzodiazepines (55% of the deliberate self-poisonings), ethanol in combination with other substances (35.8%), barbiturates and older hypnotics (18.6%), non-narcotic analgesics (13.3%) and tricyclic antidepressants (11.6%). Carbon monoxide accounted for 65.1% of all the accidental poisonings. With regard to treatment, a reduction in gastric lavage was observed. The patients were transferred to the intensive care unit (29.2%), the psychiatry ward (23.6%) or discharged home (27.8%). Only 0.3% of the patients died in the Emergency Department.

  4. An investigation of the effect of thiamine pyrophosphate on cisplatin-induced oxidative stress and DNA damage in rat brain tissue compared with thiamine: thiamine and thiamine pyrophosphate effects on cisplatin neurotoxicity.

    Science.gov (United States)

    Turan, M I; Cayir, A; Cetin, N; Suleyman, H; Siltelioglu Turan, I; Tan, H

    2014-01-01

    This study investigated the effects of thiamine pyrophosphate (TPP) at dosages of 10 and 20 mg/kg on oxidative stress induced in rat brain tissue with cisplatin and compared this with thiamine. Cisplatin neurotoxicity represents one of the main restrictions on the drug being given in effective doses. Oxidative stress is considered responsible for cisplatin toxicity. Our results showed that cisplatin increased the levels of oxidant parameters such as lipid peroxidation (thio barbituric acid reactive substance (TBARS)) and myeloperoxidase (MPO) in brain tissue and suppressed the effects of antioxidants such as total glutathione (GSH) and superoxide dismutase (SOD). TPP, especially at a dosage of 20 mg/kg, significantly reduced TBARS and MPO levels that increase with cisplatin administration compared with the thiamine group, while TPP significantly increases GSH and SOD levels. In addition, the level of 8-Gua (guanine), a product of DNA damage, was 1.7 ± 0.12 8-hydroxyl guanine (8-OH Gua)/105 Gua in brain tissue in the control group receiving cisplatin, compared with 0.97 ± 0.03 8-OH Gua/105 Gua in the thiamine pyrophosphate (20 mg/kg) group and 1.55 ± 0.11 8-OH Gua/105 Gua in the thiamine (20 mg/kg) group. These results show that thiamine pyrophosphate significantly prevents oxidative damage induced by cisplatin in brain tissue, while the protective effect of thiamine is insignificant.

  5. Biochemical, textural, microbiological and sensory attributes of gutted and ungutted sutchi catfish (Pangasianodon hypophthalmus) stored in ice.

    Science.gov (United States)

    Viji, P; Tanuja, S; Ninan, George; Lalitha, K V; Zynudheen, A A; Binsi, P K; Srinivasagopal, T K

    2015-06-01

    Pangasianodon hypophthalmus (sutchi catfish) is a fresh water catfish extensively being cultured in the South East Asian countries in the recent years. The present study provides the first report on the effects of gutting on the quality characteristics of aquacultured sutchi catfish stored in ice. pH of whole ungutted and gutted catfish didn't show significant difference (p > 0.05) during ice storage period. Total Volatile Base Nitrogen (TVB-N), Alpha Amino Nitrogen (AAN), Free Fatty Acids (FFA) and Thio Barbituric Acid Reactive Substance (TBARS) were lower in gutted fish compared to whole ungutted fish at any particular day during ice storage. However, gutted fish expressed higher rate of primary lipid oxidation than ungutted fish. Textural degradation of the fish muscle as indicated by hardness, cohesiveness, springiness and chewiness was lower in gutted fish. Results of sensory evaluation revealed that gutting has significantly improved the sensory quality of the fish. However, microbiological analysis revealed higher Total Plate Count (TPC) and Enterobactereaceae count in gutted fish. The shelf life of gutted and whole ungutted sutchi cat fish as determined by microbiological analysis was 16-18 days and 18-20 days respectively while storage in ice.

  6. Evaluation of nootropic potential of Ocimum sanctum Linn. in mice.

    Science.gov (United States)

    Joshi, Hanumanthachar; Parle, Milind

    2006-02-01

    Dementia is one of the age related mental problems and a characteristic symptom of various neurodegenerative disorders including Alzheimer's disease. Certain drugs like diazepam, barbiturates and alcohol disrupt learning and memory in animals and man. However, a new class of drugs known as nootropic agents is now used in situations where there is organic disorder in learning abilities. The present work was undertaken to assess the potential of O. sanctum extract as a nootropic and anti-amnesic agent in mice. Aqueous extract of dried whole plant of O. sanctum ameliorated the amnesic effect of scopolamine (0.4 mg/kg), diazepam (1 mg/kg) and aging induced memory deficits in mice. Elevated plus maze and passive avoidance paradigm served as the exteroceptive behavioral models. O. sanctum extract decreased transfer latency and increased step down latency, when compared to control (piracetam treated), scopolamine and aged groups of mice significantly. O. sanctum preparations could of beneficial in the treatment of cognitive disorders such as dementia and Alzheimer's disease.

  7. Pentobarbital Toxicity after Self-Administration of Euthasol Veterinary Euthanasia Medication

    Directory of Open Access Journals (Sweden)

    Steven Jason Crellin

    2016-01-01

    Full Text Available Suicide attempt via sodium pentobarbital is uncommon. A 48-year-old woman with a history of depression and prior suicide attempt was found unresponsive by her veterinarian spouse near a syringe containing pink solution. Upon EMS’ arrival, the patient was experiencing apnea, hypoxemia, and miotic pupils; her blood glucose level measured 73 mg/dL. She was bradycardic and administered atropine with transient improvement in heart rate and transported to an emergency department; 2 mg of intravenous naloxone was administered without effect. She was endotracheally intubated via rapid sequence intubation. Rapid urine drug screening detected both benzodiazepines and barbiturates. The patient was transferred to an intensive care unit where she demonstrated a nearly absent radial pulse. Emergent fasciotomy to the left forearm and carpal tunnel was performed for acute compartment syndrome; “Euthasol” had been self-administered into the antecubital fossa. Expanded toxicological analysis via liquid chromatography/mass spectroscopy detected caffeine, atropine, 7-aminoclonazepam, phenytoin, citalopram, and naproxen. The patient’s coma resolved over 48 hours and she was successfully extubated without complication. Emergency physicians must closely monitor patients exposed to veterinary euthanasia agents who develop central nervous system and respiratory depression, hypothermia, bradycardia, hypotension, or skin injury. Consultation with a regional poison center and medical toxicologist is recommended.

  8. Drugs of abuse consumption in health professionals (physicians and nurses from two outpatient services of first level attention in Bogota

    Directory of Open Access Journals (Sweden)

    Lara-Hidalgo Catalina

    2012-03-01

    Full Text Available We conducted a study to establish the prevalence of drugs of abuse consumption in physiciansand nurses in two health institutions in Bogota outpatient identify the frequency of consumption,to establish the prevalence of alcoholism using the CAGE questionnaire and explore the interestparticipate in prevention or reduction of consumption in the workplace. Materials and methods: Across-sectional study by applying an anonymous survey. Results: There were 58 questionnaires (38in physicians and 20 nurses. The substances most consumed in both groups were alcohol, cigarettesand energy drinks, followed on medical by marijuana in nursing followed by barbiturates, antidepressants,amphetamines and opiates. The prevalence of alcoholism was greater than 8% in bothgroups. 58% of physicians and 70% of nurses would participate in the design of occupational healthprograms to reduce the consumption of psychoactive substances. Conclusions: The use of drugs ofabuse is higher that found in the literature for most of the substances in the general population andis similar to the revised health personnel. It recommends the formulation and implementation ofcorporate policy within the framework of occupational health work of these institutions, aimed atreducing and preventing the consumption of psychoactive substances.

  9. Synthesis and PASS-assisted in silico approach of some novel 2-substituted benzimidazole bearing a pyrimidine-2, 4, 6(trione system as mucomembranous protector

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    Bijo Mathew

    2013-01-01

    Full Text Available Purpose: The present paper demonstrates the utility of PASS computer-aided program and makes a clear comparison of predicted and observed pharmacological properties of some novel 5-[(2E-1-(1H-benzimidazol-2-yl-3-substituted phenylprop-2-en-1-ylidene] pyrimidine-2, 4, 6 (1H, 3H, 5H-triones (5a-f. Materials and Methods: The synthesis of the titled derivatives were achieved by the reaction between 2E-1-(1H-benzimidazol-2-yl-3-phenylprop-2-en-1-ones (4a-f and barbituric acid in the presence of catalytic amount of acetic acid medium. All the final structures were assigned on the basis of IR, 1 HNMR and mass spectra analysis. All the newly synthesized compounds were screened for their antiulcer activity in the pylorus-ligated rats. Results: Compounds 5b, 5e and 5c showed a percentage protection of (69.58, 69.56 and 67.17 at a dose of 50 mg/kg b.w. when compared to standard omeprazole (77.37%, 2 mg/kg b.w.. Conclusion: Scanning of stomach specimens using electron microscope revealed that the mice treated with standard and synthetic derivatives had no injury observed in stomach mucosa, which is identical to that of the control animal.

  10. Legacy of a Chemical Factory Site: Contaminated Groundwater Impacts Stream Macroinvertebrates.

    Science.gov (United States)

    Rasmussen, Jes J; McKnight, Ursula S; Sonne, Anne Th; Wiberg-Larsen, Peter; Bjerg, Poul L

    2016-02-01

    Legislative and managing entities of EU member states face a comprehensive task because the chemical and ecological impacts of contaminated sites on surface waters must be assessed. The ecological assessment is further complicated by the low availability or, in some cases, absence of ecotoxicity data for many of the compounds occurring at contaminated sites. We studied the potential impact of a contaminated site, characterised by chlorinated solvents, sulfonamides, and barbiturates, on benthic macroinvertebrates in a receiving stream. Most of these compounds are characterised by low or unknown ecotoxicity, but they are continuously discharged into the stream by way of a long-lasting source generating long-term chronic exposure of the stream biota. Our results show that taxonomical density and diversity of especially sediment dwelling taxa were reduced by >50 % at the sampling sites situated in the primary inflow zone of the contaminated GW. Moreover, macroinvertebrate communities at these sampling sites could be distinguished from those at upstream control sites and sites situated along a downstream dilution gradient using multidimensional scaling. Importantly, macroinvertebrate indices currently used did not identify this impairment, thus underpinning an urgent need for developing suitable tools for the assessment of ecological effects of contaminated sites in streams.

  11. The effect of dietary alfalfa and flax sprouts on rabbit meat antioxidant content, lipid oxidation and fatty acid composition.

    Science.gov (United States)

    Dal Bosco, A; Castellini, C; Martino, M; Mattioli, S; Marconi, O; Sileoni, V; Ruggeri, S; Tei, F; Benincasa, P

    2015-08-01

    The aim of this study was to determine the effect of dietary supplementation with flax and alfalfa sprouts on fatty acid, tocopherol and phytochemical contents of rabbit meat. Ninety weaned New Zealand White rabbits were assigned to three dietary groups: standard diet (S); standard diet+20g/d of alfalfa sprouts (A); and standard diet+20g/d of flax sprouts (F). In the F rabbits the Longissimus dorsi muscle showed a higher thio-barbituric acid-reactive value and at the same time significantly higher values of alpha-linolenic acid, total polyunsaturated and n-3 fatty acids. Additionally n-3/n-6 ratio and thrombogenic indices were improved. The meat of A rabbits showed intermediate values of the previously reported examined parameters. Dietary supplementation with sprouts produced meat with a higher total phytoestrogen content. The addition of fresh alfalfa and flax sprouts to commercial feed modified the fat content, fatty acid and phytochemical profile of the meat, but the flax ones worsened the oxidative status of meat.

  12. Management of refractory status epilepticus in adults: still more questions than answers.

    Science.gov (United States)

    Rossetti, Andrea O; Lowenstein, Daniel H

    2011-10-01

    Refractory status epilepticus (RSE) is defined as status epilepticus that continues despite treatment with benzodiazepines and one antiepileptic drug. RSE should be treated promptly to prevent morbidity and mortality; however, scarce evidence is available to support the choice of specific treatments. Major independent outcome predictors are age (not modifiable) and cause (which should be actively targeted). Recent recommendations for adults suggest that the aggressiveness of treatment for RSE should be tailored to the clinical situation. To minimise intensive care unit-related complications, focal RSE without impairment of consciousness might initially be approached conservatively; conversely, early induction of pharmacological coma is advisable in generalised convulsive forms of the disorder. At this stage, midazolam, propofol, or barbiturates are the most commonly used drugs. Several other treatments, such as additional anaesthetics, other antiepileptic or immunomodulatory compounds, or non-pharmacological approaches (eg, electroconvulsive treatment or hypothermia), have been used in protracted RSE. Treatment lasting weeks or months can sometimes result in a good outcome, as in selected patients after encephalitis or autoimmune disorders. Well designed prospective studies of RSE are urgently needed.

  13. A review of our development of dental adhesives--effects of radical polymerization initiators and adhesive monomers on adhesion.

    Science.gov (United States)

    Ikemura, Kunio; Endo, Takeshi

    2010-03-01

    This paper reviews the development of dental adhesives by collating information of related studies from original scientific papers, reviews, and patent literatures. Through our development, novel radical polymerization initiators, adhesive monomers, and microcapsules were synthesized, and their effects on adhesion were investigated. It was found that 5-monosubstituted barbituric acid (5-MSBA)-containing ternary initiators in conjunction with adhesive monomers contributed to effective adhesion with good polymerization reactivity. Several kinds of novel adhesive monomers bearing carboxyl group, phosphonic acid group or sulfur-containing group were synthesized, and investigated their multi-purpose bonding functions. It was suggested that the flexible methylene chain in the structure of adhesive monomers played a pivotal role in their enhanced bonding durability. It was found that the combination of acidic monomers with sulfur-containing monomer markedly improved adhesion to enamel, dentin, porcelain, alumina, zirconia, non-precious metals and precious metals. A new poly(methyl methacrylate) (PMMA)-type adhesive resin comprising microencapsulated polymerization initiators was also found to exhibit both good formulation stability and excellent adhesive property.

  14. Update of Inpatient Treatment for Refractory Chronic Daily Headache.

    Science.gov (United States)

    Lai, Tzu-Hsien; Wang, Shuu-Jiun

    2016-01-01

    Chronic daily headache (CDH) is a group of headache disorders, in which headaches occur daily or near-daily (>15 days per month) and last for more than 3 months. Important CDH subtypes include chronic migraine, chronic tension-type headache, hemicrania continua, and new daily persistent headache. Other headaches with shorter durations (<4 h/day) are usually not included in CDH. Common comorbidities of CDH are medication overuse headache and various psychiatric disorders, such as depression and anxiety. Indications of inpatient treatment for CDH patients include poor responses to outpatient management, need for detoxification for overuse of specific medications (particularly opioids and barbiturates), and severe psychiatric comorbidities. Inpatient treatment usually involves stopping acute pain, preventing future attacks, and detoxifying medication overuse if present. Multidisciplinary integrated care that includes medical staff from different disciplines (e.g., psychiatry, clinical psychology, and physical therapy) has been recommended. The outcomes of inpatient treatment are satisfactory in terms of decreasing headache intensity or frequency, withdrawal from medication overuse, reducing disability, and improving life quality, although long-term relapse is not uncommon. In conclusion, inpatient treatment may be useful for select patients with refractory CDH and should be incorporated in a holistic headache care program.

  15. Microwave assisted one-pot catalyst free green synthesis of new methyl-7-amino-4-oxo-5-phenyl-2-thioxo-2,3,4,5-tetrahydro-1H-pyrano[2,3-d]pyrimidine-6-carboxylates as potent in vitro antibacterial and antifungal activity

    Directory of Open Access Journals (Sweden)

    Ajmal R. Bhat

    2015-11-01

    Full Text Available An efficiently simple protocol for the synthesis of methyl 7 amino-4-oxo-5-phenyl-2-thioxo-2, 3, 4,5-tetrahydro-1H-pyrano[2,3-d]pyrimidine-6-carboxylates via one-pot three component condensation pathway is established via microwave irradiation using varied benzaldehyde derivatives, methylcyanoacetate and thio-barbituric acid in water as a green solvent. A variety of functionalized substrates were found to react under this methodology due to its easy operability and offers several advantages like, high yields (78–94%, short reaction time (3–6 min, safety and environment friendly without used any catalyst. The synthesized compounds (4a–4k showed comparatively good in vitro antimicrobial and antifungal activities against different strains. The Compounds 4a, 4b, 4c, 4d 4e and 4f showed maximum antimicrobial activity against Staphylococcus aureus, Bacillus cereus (gram-positive bacteria, Escherichia coli, Klebshiella pneumonia, Pseudomonas aeruginosa (gram-negative bacteria. The synthesized compound 4f showed maximum antifungal activity against Aspergillus Niger and Penicillium chrysogenum strains. Streptomycin is used as standard for bacterial studies and Mycostatin as standards for fungal studies. Structure of all newly synthesized products was characterized on the basis of IR, 1H NMR, 13C NMR and mass spectral analysis.

  16. A Massive Overdose of Dalfampridine

    Directory of Open Access Journals (Sweden)

    Laura J. Fil

    2015-12-01

    Full Text Available Multiple sclerosis (MS is an immune mediated inflammatory disease that attacks myelinated axons in the central nervous system. Dalfampridine (4-aminopyridine was approved by the Food and Drug Administration in January 2010 for treatment of MS. Our patient was a 34-year-old male with a history of MS, who was brought to the emergency department after being found unresponsive. His current medications were valacyclovir, temazepam, dalfampridine (4-AP and a tysabri intravenous (IV infusion. Fifteen minutes after arrival the patient seized. The seizures were refractory to benzodiazepines, barbiturates and phenytoin. The 4-AP level was 530ng/mL (25ng/mL and 49ng/ mL. The patient stopped seizing on hospital day 3 and was discharged 14 days later with normal mental status and neurologic exam. 4-AP is a potassium channel blocker that blocks the potassium ion current of repolarization following an action potential. The blockade of the potassium channel at the level of the membrane widens the action potential and enhances the release of acetylcholine, thus increasing post-synaptic action potentials. The treatment of patients with 4-AP overdose is supportive. Animal data suggest that patients with toxic levels of 4-AP may respond to phenytoin. Our case illustrates the highest recorded level of 4-AP in an overdose. Our patient appeared to be refractory to a combination of high doses of anticonvulsants and only improved with time.

  17. AHR-11797: a novel benzodiazepine antagonist

    Energy Technology Data Exchange (ETDEWEB)

    Johnson, D.N.; Kilpatrick, B.F.; Hannaman, P.K.

    1986-03-01

    AHR-11797(5,6-dihydro-6-methyl-1-phenyl-/sup 3/H-pyrrolo(3,2,1-ij)quinazolin-3-one) displaced /sup 3/H-flunitrazepam (IC/sub 50/ = 82 nM) and /sup 3/H-Ro 15-1877 (IC/sub 50/ = 104 nM) from rat brain synaptosomes. AHR-11797 did not protect mice from seizures induced by maximal electroshock or subcutaneous Metrazol (scMET), nor did it induce seizures in doses up to the lethal dose. However, at 31.6 mg/kg, IP, it significantly increased the anticonvulsant ED/sub 50/ of chlordiazepoxide (CDPX) from 1.9 to 31.6 mg/kg, IP. With 56.7 mg/kg, IP, of AHR-11797, CDPX was inactive in doses up to 100 mg/kg, IP. AHR-11797 did not significantly increase punished responding in the Geller and Seifter conflict procedure, but it did attenuate the effects of diazepam. Although the compound is without anticonvulsant or anxiolytic activity, it did have muscle relaxant properties. AHR-11797 blocked morphine-induced Straub tail in mice (ED/sub 50/ = 31 mg/kg, IP) and it selectively suppressed the polysnaptic linguomandibular reflex in barbiturate-anesthetized cats. The apparent muscle relaxant activity of AHR-11797 suggests that different receptor sites are involved for muscle relaxant vs. anxiolytic/anticonvulsant activities of the benzodiazepines.

  18. Purification of high affinity benzodiazepine receptor binding site fragments from rat brain

    Energy Technology Data Exchange (ETDEWEB)

    Klotz, K.L.

    1984-01-01

    In central nervous system benzodiazepine recognition sites occur on neuronal cell surfaces as one member of a multireceptor complex, including recognition sites for benzodiazepines, gamma aminobutyric acid (GABA), barbiturates and a chloride ionophore. During photoaffinity labelling, the benzodiazepine agonist, /sup 3/H-flunitrazepam, is irreversibly bound to central benzodiazepine high affinity recognition sites in the presence of ultraviolet light. In these studies a /sup 3/H-flunitrazepam radiolabel was used to track the isolation and purification of high affinity agonist binding site fragments from membrane-bound benzodiazepine receptor in rat brain. The authors present a method for limited proteolysis of /sup 3/H-flunitrazepam photoaffinity labeled rat brain membranes, generating photolabeled benzodiazepine receptor fragments containing the agonist binding site. Using trypsin chymotrypsin A/sub 4/, or a combination of these two proteases, they have demonstrated the extent and time course for partial digestion of benzodiazepine receptor, yielding photolabeled receptor binding site fragments. These photolabeled receptor fragments have been further purified on the basis of size, using ultrafiltration, gel permeation chromatography, and sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) as well as on the basis of hydrophobicity, using a high performance liquid chromatography (HPLC) precolumn, several HPLC elution schemes, and two different HPLC column types. Using these procedures, they have purified three photolabeled benzodiazepine receptor fragments containing the agonist binding site which appear to have a molecular weight of less than 2000 daltons each.

  19. The history of benzodiazepines.

    Science.gov (United States)

    Wick, Jeannette Y

    2013-09-01

    After more than 50 years of experience with benzodiazepines, the American health care system has a love-hate relationship with them. In 1955, Hoffmann-La Roche chemist Leo Sternbach serendipitously identified the first benzodiazepine, chlordiazepoxide (Librium). By 1960, Hoffmann-La Roche marketed it as Librium, and it pursued molecular modifications for enhanced activity. Valium (diazepam) followed in 1963. Hoffmann-La Roche's competitors also began looking for analogues. Initially, benzodiazepines appeared to be less toxic and less likely to cause dependence than older drugs. A specific improvement was their lack of respiratory depression, a safety concern with barbiturates. Medical professionals greeted benzodiazepines enthusiastically at first, skyrocketing their popularity and patient demand. In the mid-to-late 1970s, benzodiazepines topped all "most frequently prescribed" lists. It took 15 years for researchers to associate benzodiazepines and their effect on gamma-aminobutyric acid as a mechanism of action. By the 1980s, clinicians' earlier enthusiasm and propensity to prescribe created a new concern: the specter of abuse and dependence. As information about benzodiazepines, both raising and damning, accumulated, medical leaders and legislators began to take action. The result: individual benzodiazepines and the entire class began to appear on guidelines and in legislation giving guidance on their use. Concurrently, clinicians began to raise concerns about benzodiazepine use by elderly patients, indicating that elders'lesser therapeutic response and heightened sensitivity to side effects demanded prescriber caution. The benzodiazepine story continues to evolve and includes modern-day issues and concerns beyond those ever anticipated.

  20. Plasticity in the tonotopic organization of the medial geniculate body in adult cats following restricted unilateral cochlear lesions.

    Science.gov (United States)

    Kamke, Marc R; Brown, Mel; Irvine, Dexter R F

    2003-05-12

    To investigate subcortical contributions to cortical reorganization, the frequency organization of the ventral nucleus of the medial geniculate body (MGv) in six normal adult cats and in eight cats with restricted unilateral cochlear lesions was investigated using multiunit electrophysiological recording techniques. The tonotopic organization of MGv in the lesioned animals, with severe mid-to-high frequency hearing losses, was investigated 40-186 days following the lesioning procedure. Frequency maps were generated from neural responses to pure tone bursts presented separately to each ear under barbiturate anesthesia. Consideration of the frequency organization in normal animals, and of the apparently normal representation of the ipsilateral (unlesioned) cochlea in lesioned animals, allowed for a detailed specification of the extent of changes observed in MGv. In the lesioned animals it was found that, in the region of MGv in which mid-to-high frequencies are normally represented, there was an "expanded representation" of lesion-edge frequencies. Neuron clusters within these regions of enlarged representation that had "new" characteristic frequencies displayed response properties (latency, bandwidth) very similar to those in normal animals. Thresholds of these neurons were not consistent with the argument that the changes merely reflect the residue of prelesion responses, suggesting a dynamic process of reorganization. The tonotopic reorganization observed in MGv is similar to that seen in the primary auditory cortex and is more extensive than the reorganization found in the auditory midbrain, suggesting that the auditory thalamus plays an important role in cortical plasticity.

  1. Refractory High Intracranial Pressure following Intraventricular Hemorrhage due to Moyamoya Disease in a Pregnant Caucasian Woman

    Directory of Open Access Journals (Sweden)

    Virginie Montiel

    2009-02-01

    Full Text Available Intraventricular hemorrhage during pregnancy is usually followed by a poor recovery. When caused by moyamoya disease, ischemic or hemorrhagic episodes may complicate the management of high intracranial pressure. A 26-year-old Caucasian woman presented with generalized seizures and a Glasgow Coma Score (GCS of 3 during the 36th week of pregnancy. The fetus was delivered by caesarean section. The brain CT in the mother revealed bilateral intraventricular hemorrhage, a callosal hematoma, hydrocephalus and right frontal ischemia. Refractory high intracranial pressure developed and required bilateral ventricular drainage and intensive care treatment with barbiturates and hypothermia. Magnetic resonance imaging and cerebral angiography revealed a moyamoya syndrome with rupture of the abnormal collateral vascular network as the cause of the hemorrhage. Intracranial pressure could only be controlled after the surgical removal of the clots after a large opening of the right ventricle. Despite an initially low GCS, this patient made a good functional recovery at one year follow-up. Management of refractory high intracranial pressure following moyamoya related intraventricular bleeding should require optimal removal of ventricular clots and appropriate control of cerebral hemodynamics to avoid ischemic or hemorrhagic complications.

  2. Desenvolvimento e validação de um método cromatográfico em fase gasosa para análise da 3,4-metilenodioximetanfetamina (ecstasy e outros derivados anfetamínicos em comprimidos Development and validation of a gas chromatography method for determination of ecstasy and amphetamines derivatives in tablets

    Directory of Open Access Journals (Sweden)

    Marcelo Carvalho Lasmar

    2007-06-01

    laboratories of toxicology of the development countries as Brazil. It was chosen for development and validation a gas chromatography method with flame ionization detection. The analytic validation results for MDMA, MDA and MDEA were linearity range of 1.0 to 500.0 µg/mL, intra and interassay coefficient of variation lower than 9.5% and quantification limit of 1.0 µg/mL. The detection limits were 0.7 µg/mL, 0.8 µg/mL and 0.6 µg/mL respectively to MDMA, MDA and MDEA. The method showed a good seletivity as the epinephrine, cocaine, amphetamine, methamphetamine, acethyl salicilic acid, diethyl barbituric acid, p-aminobenzoyl diethyl barbituric, paracetamol and caffeine presences did not interfere with the measurement of the three analytes.

  3. Avaliação dos efeitos depressores centrais do extrato etanólico das folhas de Synadenium umbellatum Pax. e de suas frações em camundongos albinos Evaluation of the central depressor effects of the ethanolic extract of the leaves of Synadenium umbellatum Pax. and its fractions in Swiss mice

    Directory of Open Access Journals (Sweden)

    Rodrigo Borges de Oliveira

    2008-09-01

    Full Text Available O Synadenium umbellatum Pax. (Euphorbiacea é uma planta nativa da África tropical conhecida como "cola-nota", "avelós", "cancerola", "milagrosa", dentre outros. A planta é utilizada pela população brasileira como detentora de propriedades antiinflamatória, analgésica, dentre outras. Foram avaliados os efeitos depressores sobre o sistema nervoso central (SNC do extrato etanólico das folhas de Synadenium umbellatum (EES e de suas frações - hexânica (FH, clorofórmica (FC e metanol/água (FM. Vários testes foram utilizados em camundongos machos albinos (Mus musculus, dentre eles, o sono induzido por barbitúrico, campo aberto e o teste do rota-rod. O EES foi testado nas doses de 25, 50 e 100 mg/kg, enquanto que a FH foi testada na dose de 10 mg/kg, a FC na dose de 20 mg/kg e a FM na dose de 25 mg/kg. O EES e as frações FH e FC, mas não a FM, apresentaram um possível efeito depressor sobre o SNC, visto que foram capazes de aumentar o tempo parado e diminuir o número de bolos fecais no campo aberto, além de potencializarem o sono induzido por barbitúrico. No teste do rota-rod, observou-se que o EES e as frações não foram capazes de causar incoordenação motora ou relaxamento muscular. Assim, conclui-se que o extrato etanólico e as frações FH e FC do Syandenium umbellatum Pax. possuem possível efeito depressor sobre o SNC.Synadenium umbellatum Pax. (Euphorbiacea is a native plant from tropical Africa known as "cola-nota", "avelós", "cancerola", "milagrosa", among others. The plant is used by Brazilian folks for having anti-inflammatory and analgesic properties, among others. It was evaluated the depressor effects over the central nervous system (CNS of the ethanolic extract of the leaves of Synadenium umbellatum (EES and its fractions - hexane (HF, chloroformic (CF and methanol/water fractions(MF. Several tests were used in Swiss mice (Mus musculus, among them, barbiturate-induced sleep, open field and rota-rod test. The

  4. [The effects of long-term sedation on intestinal function].

    Science.gov (United States)

    Zielmann, S; Grote, R

    1995-12-01

    by enteric tube in 30%, 35%, and 15% of cases, respectively. In group 3 deep sedation was necessary because of elevated intracranial pressure. In groups 4, 5, and 6, piritramide was administered for analgesia, and normal enteric tube feeding was achieved in 70%, 75%, and 90% of cases. The best results were seen in group 6, and these elderly patients needed smaller amounts of piritramide for analgesia. In groups 7, 8, 9, and 10, ketamine was given for analgesia, and complete enteric tube feeding was carried out in 75%, 30%, 45%, and 60% of these patients. The best results in the ketamine groups were found in combination with midazolam as the sedating drug; however, the patients in group 7 did not have elevated intracranial pressure, in contrast to the patients in groups 8, 9, and 10. The last group received the combination of sufentanil, midazolam and methohexitone to achieve a deep sedation. The rate of normal enteric tube feeding in these patients with severe head trauma was 30%. CONCLUSIONS. In patients with severe head trauma who need deep sedation to prevent dangerous high intracranial pressure, gastrointestinal motility disorders are very commonly found. The results obtained suggest that ketamine should be regarded as the analgesic drug of choice, combined with propofol rather than a high-dose barbiturate therapy. The combination of ketamine with midazolam and GABA is an unusual strategy for long-term sedation, which resulted from our own clinical studies directed at an effective and well-tolerated regime for this high-risk patient group. Obviously, high-dose barbiturates and short-acting opioids, especially when combined, make enteric tube feeding more difficult. Therefore, we recommend piritramide or ketamine for analgesia. The basic sedating drug is midazolam, in special cases combined with or replaced by propofol. The position of GABA in long-term sedation is not yet clear, but a lack of side effects on the gastrointestinal tract became evident in this stud

  5. Ciprofloxacin induced fixed drug eruption

    Directory of Open Access Journals (Sweden)

    M. Ravishankar

    2014-12-01

    Full Text Available Fixed drug eruption (FDE is a clinical entity occurring in the same site or sites each time the drug is administered. Acute lesions appear as sharply marginated erythematous plaques, which are usually found on lips, genitalia, abdomen, and legs. The eruptions usually occur within hours of administration of the offending agent and resolves spontaneously without scarring after few weeks of onset. Most common drugs causing FDE are sulfonamides, tetracyclines, salicylates, barbiturates, doxycycline, fluconazole, clarithromycin, etc. Ciprofloxacin, a widely used fluoroquinolone antimicrobial, induces cutaneous adverse drug reactions (ADRs in about 1-2% of treated patients. Urticaria, angioedema, maculopapular exanthems, and photosensitivity are the most frequently documented cutaneous adverse reactions. In this case report, the patient soon after taking ciprofloxacin tablets, developed itching in the lips, palms and in scrotal region. On continuing the treatment, the next day he developed fluid filled lesions over palm, knuckle, and hyperpigmentation. He gives a history of severe itching and rashes in scrotal region. He gives a history of similar complaints in the previous month after taking ciprofloxacin medication. There was no history of intake of any other medication. On examination, bullous lesions and pustules in finger webs, hyperpigmentation on knuckles, and scrotal erosions were seen. In the present case report, the patient presented with FDE immediately after oral administration of ciprofloxacin and got completely cured after stopping the drug and taking adequate treatment. According to the Naranjo's ADR probability scale (score=8, this ADR is categorized as a and ldquo;probable and rdquo; reaction to the drug. [Int J Basic Clin Pharmacol 2014; 3(6.000: 1096-1097

  6. Cerebral physiology and preservation during cardiac arrest Fisiología y preservación cerebral durante el paro cardíaco: vulnerabilidad del cerebro

    Directory of Open Access Journals (Sweden)

    Luis M. Gómez

    1991-03-01

    Full Text Available

    Cerebral physiology during cardiac arrest is discussed with particular Interest on selective neuronal damage. Previous concepts on brain tolerance to hypoxia are analyzed and new information about brain function prognosis after cardiac arrest is presented. Therapeutic alternatives for brain preservation are discussed with emphasis on the lack of effectiveness of barbiturates, the results of research with other drugs and the future role that blockers of excitatory neurotransmission may have as elements of cerebral preservation.

    Se hace una aproximación a la fisiología cerebral durante el paro cardíaco, destacando el concepto de darlo neuronal selectivo. Se presentan elementos que permiten modificar concepciones antiguas sobre la tolerancia del cerebro a la hipoxia severa. Además, se hace un nuevo planteamiento sobre el pronóstico cerebral luego de un paro cardíaco y se esbozan las alternativas terapéuticas utilizadas hasta la fecha para la preservación cerebral. Se hace énfasis en la inefectividad de los barbitúricos, en la investigación sobre la terapia con otras drogas y en el futuro abierto hacia los bloqueadores de los neurotransmisores excitadores, como elementos terapéuticos para la preservación cerebral.

  7. Chemical modification of ascorbic acid and evaluation of its lipophilic derivatives as inhibitors of secretory phospholipase A(2) with anti-inflammatory activity.

    Science.gov (United States)

    Mohamed, Riyaz; Dharmappa, K K; Tarannum, Shaista; Jameel, N M; Kannum, S A; Ashrafulla, H S; Rai, Lokanath; Souza, Cletus Jmd'; Shekhar, M A; Vishwanath, Bannikuppe S

    2010-12-01

    The halo 6-fatty acid esters of L-ascorbic acid 3a, 3b and 6-fatty acid esters of L-ascorbic acid 5a-g were achieved from L-ascorbic acid 1. Compounds 3a, 3b and 5a-g were evaluated for anti-oxidant, anti-lipid peroxidation, and secretory phospholipase A(2) (sPLA(2)) inhibition in vitro, and sPLA(2) induced mouse paw edema. All the derivatives retained their anti-oxidant property compared to ascorbic acid at 6 × 10(-4)M and are good inhibitors of lipid peroxidation at 1 mg ml(-1) as evaluated by 2, 2-Diphenyl-1-picrylhydrazyl radical and thio-barbituric acid methods, respectively. Compounds 5e and 5f significantly inhibited purified group I sPLA(2) from Naja naja and group II sPLA(2) from Vipera russelli, human synovial fluid and human pleural fluid with IC(50) value ranging from 64 ± 1.95 to 82 ± 1.3 and 48 ± 2.27 to 61 ± 2.23 μM, respectively. The compounds 5e and 5f also showed varying degree of potency in neutralizing indirect hemolytic activity of sPLA(2) at 50 μM concentration, and sPLA(2) induced mouse paw edema at the dose 3 mg/kg. Further docking studies also confirmed that compounds 5e and 5f have maximum interaction with increasing negative energy value. Single molecule possessing both anti-oxidant and anti-inflammatory activities is of great therapeutic significance in inflammatory disorders.

  8. Scale-up of organic reactions in ball mills: process intensification with regard to energy efficiency and economy of scale.

    Science.gov (United States)

    Stolle, Achim; Schmidt, Robert; Jacob, Katharina

    2014-01-01

    The scale-up of the Knoevenagel-condensation between vanillin and barbituric acid carried out in planetary ball mills is investigated from an engineering perspective. Generally, the reaction proceeded in the solid state without intermediate melting and afforded selectively only one product. The reaction has been used as a model to analyze the influence and relationship of different parameters related to operation in planetary ball mills. From the viewpoint of technological parameters the milling ball diameter, dMB, the filling degree with respect to the milling balls' packing, ΦMB,packing, and the filling degree of the substrates with respect to the void volume of the milling balls' packing, ΦGS, have been investigated at different reaction scales. It was found that milling balls with small dMB lead to higher yields within shorter reaction time, treaction, or lower rotation frequency, rpm. Thus, the lower limit is set considering the technology which is available for the separation of the milling balls from the product after the reaction. Regarding ΦMB,packing, results indicate that the optimal value is roughly 50% of the total milling beakers' volume, VB,total, independent of the reaction scale or reaction conditions. Thus, 30% of VB,total are taken by the milling balls. Increase of the initial batch sizes changes ΦGS significantly. However, within the investigated parameter range no negative influence on the yield was observed. Up to 50% of VB,total can be taken over by the substrates in addition to 30% for the total milling ball volume. Scale-up factors of 15 and 11 were realized considering the amount of substrates and the reactor volume, respectively. Beside technological parameters, variables which influence the process itself, treaction and rpm, were investigated also. Variation of those allowed to fine-tune the reaction conditions in order to maximize the yield and minimize the energy intensity.

  9. Dose-response relationship between alcohol use and blood pressure among drivers of commercial vehicles in Calabar, Southern Nigeria

    Directory of Open Access Journals (Sweden)

    Segun Bello

    2010-08-01

    Full Text Available Alcohol is a sedative/hypnotic with effects similar to those of barbiturates.1 The type of alcoholic beverages consumed depends on the social context and financial capability. Alcoholic beverages may be in form of beer, wine, dry gin. Drinking alcohol is an activity that many people enjoy; taking a few drinks occasionally is generally harmless. Most people do not have problems as a result of drinking alcohol in this manner, although this may predispose to heavy use. Heavy alcohol consumption has been shown in observational studies to have a strong positive association with elevated blood pressure.2-4 Further evidence have been shown by clinical trials5,6 that have demonstrated that reduction in alcohol intake among individuals who drink heavily (i.e. three or more drinks per day can lower blood pressure in normotensive and hypertensive men. Some studies have recorded a linear dose-response relationship sometimes starting with a consumption threshold of three drinks per day (30 g of ethanol.7-13 In others, the relationship has been non-linear especially in women, and some authors have speculated that ingestion of small quantities may reduce blood pressure.14-22 These discrepancies may reflect differences in investigational design, methods and populations.23 Many studies have been done in this area in developed countries like the United States, United Kingdom and Australia. This is however, not a commonly researched area in this part of the world. The aim of this study was to assess the relationship between alcohol consumption and blood pressure of drivers of commercial vehicles.

  10. Membrane Bistability in Thalamic Reticular Neurons During Spindle Oscillations

    Science.gov (United States)

    Fuentealba, Pablo; Timofeev, Igor; Bazhenov, Maxim; Sejnowski, Terrence J.; Steriade, Mircea

    2010-01-01

    The thalamic reticular (RE) nucleus is a major source of inhibition in the thalamus. It plays a crucial role in regulating the excitability of thalamocortical networks and in generating some sleep rhythms. Current-clamp intracellular recordings of RE neurons in cats under barbiturate anesthesia revealed the presence of membrane bistability in ~20% of neurons. Bistability consisted of two alternate membrane potentials, separated by ~17–20 mV. While non-bistable (common) RE neurons fired rhythmic spike-bursts during spindles, bistable RE neurons fired tonically, with burst modulation, throughout spindle sequences. Bistability was strongly voltage dependent and only expressed under resting conditions (i.e. no current injection). The transition from the silent to the active state was a regenerative event that could be activated by brief depolarization, whereas brief hyperpolarizations could switch the membrane potential from the active to the silent state. These effects outlasted the current pulses. Corticothalamic stimulation could also switch the membrane potential from silent to active states. Addition of QX-314 in the recording micropipette either abolished or disrupted membrane bistability, suggesting INa(p) to be responsible for its generation. Thalamocortical cells presented various patterns of spindling that reflected the membrane bistability in RE neurons. Finally, experimental data and computer simulations predicted a role for RE neurons’ membrane bistability in inducing various patterns of spindling in target thalamocortical cells. We conclude that membrane bistability of RE neurons is an intrinsic property, likely generated by INa(p) and modulated by cortical influences, as well as a factor that determines different patterns of spindle rhythms in thalamocortical neurons. PMID:15331618

  11. Pilot study of the efficacy and safety of lettuce seed oil in patients with sleep disorders

    Directory of Open Access Journals (Sweden)

    Yakoot M

    2011-06-01

    Full Text Available Mostafa Yakoot1, Sherine Helmy2, Kamal Fawal31Green Clinic Research Center, 2Pharco Pharmaceutical Company, 3Mamorah Psychiatric Hospital, Alexandria, EgyptBackground: Lactuca sativa (garden lettuce is a popular salad herb. It has been in use in folk medicine since ancient times as both an appetite stimulant and as an aid to sleep. L. sativa seed oil (Sedan® has demonstrated a pronounced sedative effect and potentiated the hypnotic effect of barbiturates in animal models. It also exhibited significant analgesic and anti-inflammatory activities. In this study, we evaluated the sedative and hypnotic effects of L. sativa in patients suffering from insomnia.Methods: Sixty patients suffering from insomnia with or without anxiety were randomized to receive capsules containing L. sativa seed oil 1000 mg (n = 30 or placebo (n = 30. All patients were asked to complete a verbal questionnaire before the start of the trial and 1 week after starting treatment.Results: Improvements in the modified State-Trait Anxiety Inventory and the Sleep rating scale scores were significantly greater in patients receiving L. sativa seed oil compared with those on placebo (P < 0.05. No side effects were found to be attributable to L. sativa seed oil at the given dosage.Conclusion: L. sativa seed oil was found to be a useful sleeping aid and may be a hazard-free line of treatment, especially in geriatric patients suffering from mild-to-moderate forms of anxiety and sleeping difficulties.Keywords: Lactuca sativa seed oil, insomnia, sleeping disorder, anxiety

  12. Evaluation of hepatoprotective and nephroprotective activity of aqueous extract of Vigna mungo (Linn. Hepper on rifampicin-induced toxicity in albino rats

    Directory of Open Access Journals (Sweden)

    M Nitin

    2012-01-01

    Full Text Available Aim: The objective of this study was to investigate the hepatoprotective and nephroprotective activity of aqueous extract of seeds of Vigna mungo (AEVM (fabaceae against rifampicin-induced liver and kidney damage in rats. Settings and Design: Albino rats of either sex (200-250 g were selected and divided in to eight groups of six animals in each. Four groups for hepatoprotective activity and four groups for nephroprotective activity. Group 1 was normal control, group 2 was positive control, group 3 was treated with standard drug, group 4 was treated with AEVM. Similarly it was done for nephroprotective activity. The results are evidenced on the basis of physical, biochemical, histological, and functional parameters. Materials and Methods: Drugs used are rifampicin, silymarin, diagnostic kits (SGPT, SGOT, ALP, and BIT for hepatoprotective activity. BUN, serum creatinine, and serum uric acid for nephroprotective activity. Seed powder of Vigna mungo was extracted with water. Preliminary phytochemical tests were done to identify the phytoconstituents. The hepatoprotective and nephroprotective activity of the AEVM were assessed in rifampicin-induced hepatotoxic and nephrotoxic rats. Statistical Analysis Used: One-way analysis of variance (ANOVA followed by "Tukey-Kramer" multiple comparison tests. Results: The AEVM showed the presence of amino acids, alkaloids, carbohydrates, flavonoids, glycosides, proteins, phytic acid, total phenolic compounds, saponins, and tannins. Rifampicin produced significant changes in physical (increased liver weight, decreased body weight, biochemical (increase in serum glutathione pyruvate transaminase (SGPT, oxaloacetate transaminase (SGOT, alkaline phosphatase (ALP and total bilirubin (BIT level, increase in blood urea nitrogen (BUN, serum creatinine, and serum uric acid level, histological (damage to hepatocytes, nephrons, and functional (barbiturates-induce sleeping time induced by rifampicin in liver and kidney

  13. Edible Film from Jack Bean Flour for Use as an Antioxidative Packaging Incorporating Extract of Green Tea

    Directory of Open Access Journals (Sweden)

    Triana Lindriati

    2015-01-01

    Full Text Available Addition of green tea’s extract in edible film’s matrix will improve film’s functionality. The film will has antioxidant properties and can protect food from rancidity and discoloration. In this research film based component was jack bean flour which has high content of carbohydrate and protein. The film had good mechanical and physical characters. The aim of this research was studying effect of green tea’s extract addition on phenolic, tannin concentration and antioxidant  activity of edible film. Extract of green tea was prepared with variation of temperature (28oC, 50oC and 100oC. The result showed that increasing of extraction temperature would increase phenolic content, tannin concentration and antioxidant  activity. When green tea extracted at 100oC phenolic concentration was 144.179 mg/g, tannin  was 50.345 mg/g and antioksidant activity was 58.8% (DPPH inhibition. After the extract was incorporated in to edible film, total phenolic concentration of film was 113.544 mg/g, tannin was 41.842 mg/g and antioxidant activity was 45.22%. Edible film with green tea addition, showed ability in inhibiting rancidity of peanut oil whereas peroxide value and TBA (Thio Barbituric Acid number of peanut oil was 11.5 meq O2/kg and 0.13 ml/g after edible film immersion in 5 days. Peroxide value and TBA number of peanut oil without edible film immersion was 20.3 meq O2/kg and 0.32 ml/g.

  14. Antihypertensive Effect of an Aqueous Extract of Passiflora nepalensis Wall

    Directory of Open Access Journals (Sweden)

    S S Patel

    2011-06-01

    Full Text Available Summary: The present study was designed to investigate the antihypertensive effect of an aqueous extract of the whole plant of Passiflora nepalensis wall (APN in renal hypertensive rats. Hypertension in experimental animals was induced by renal ischemia and reperfusion (IR. The blood pressure, pulse pressure and heart rate fell dose-dependently in renal hypertensive and normotensive rats after intravenous administration of 80, 160 and 320 mg/kg APN, suggesting that APN possesses antihypertensive, hypotensive and negative chronotropic effects. Renal IR significantly increased the levels of thio-barbituric acid reactive substances and reduced the levels of superoxide dismutase, catalase, and glutathione peroxidase (p<0.001 versus control in kidney, which was altered after intravenous administration of 160 and 320 mg/kg of APN, suggesting that APN protect kidney from IR injury (p<0.001 versus renal IR. Histological evaluation showed that renal IR increased, whereas APN decreased the focal glomerular necrosis, degeneration of tubular epithelium, necrosis in tubular epithelium, interstitial inflammatory infiltration, and congestion of blood vessels.   Industrial relevance: Herbal medicines are getting more importance in the treatment of high blood pressure because the modern synthetic medicines have side effects. A large proportion of the Indian population for their physical and psychological health needs depend on traditional system of medicine. Medicinal plants have become the focus of intense study in term of conservation as to whether their traditional uses are supported by actual pharmacological effects or merely based on folklore. Herbal medicines are free from side effects and less costly when compared to synthetic drugs. The present study will help the industry to produce herbal drugs with fewer side effects, which are affordable and more effective in the treatment of hypertension.

  15. [Selection and destruction--treatment of "unworthy-to-live" children in the Third Reich and the role of child and adolescent psychiatry].

    Science.gov (United States)

    Dahl, M

    2001-03-01

    During the period of National Socialism in Germany, many "asocial", mentally retarded or disabled minors were persecuted. Several measures had been discussed theoretically before, but the National Socialists put the theoretical proposals into practice. As a result children and adolescents were separated, sterilized or killed. In concentration camps so-called "depraved" minors were selected to get special education. The object of this effort was to adapt minors to the ideology of national socialism. After passing the law to sterilize patients with "hereditary diseases" in 1933 about 375.000 people were sterilized unvoluntarily. In 193/span>9 sterilizations came to an end except for adolescents at "high risk of reproduction". During the second world war more than 160.000 adult psychiatric patients were murdered. In addition to that, also a large number of disabled and mentally retarded minors were killed. This campaign was called child "euthanasia". Physicians tried to determine children's "value of life" by economic criteria. Children with negative ratings (i.e. inability to work or insufficient mental maturing) were killed by fasting "cures" or by barbiturates. Beyond that children were also used as research subjects. Their death was an accepted consequence. Physicians were also very interested in brain research. Finally, the relation to German child and adolescent psychiatry will be analysed. In the special political and social context of the Third Reich the German child and adolescent psychiatry became more significant. As a result of this the German association of child and adolescent psychiatry and allied professions was founded 1940 in Vienna. On this conference, some speakers suggested to persecute "asocial" minors. This suggestion was realized consequently. Up to now, the role of the German child and adolescent psychiatry has not been thoroughly discussed.

  16. [Management of convulsive status epilepticus in infants and children].

    Science.gov (United States)

    Hubert, P; Parain, D; Vallée, L

    2009-04-01

    Convulsive status epilepticus in childhood is a life threatening condition with serious risk of neurological sequelae which constitutes a medical emergency. Clinical and experimental data suggest that prolonged seizures can have immediate and long-term adverse consequences on the immature and developing brain. So the child who presents with a continuous generalized convulsive seizure lasting greater than five minutes should be promptly treated. The outcome is mainly determined by the underlying etiology, age and duration of status epilepticus. In children the mortality from status epilepticus ranges from 3 to 5% and the morbidity is two-fold higher. Mortality and morbidity are highest with status epilepticus associated with central nervous system infections, which is the most important cause of status epilepticus. There are few evidence-based data to guide management decisions for the child with status epilepticus. Immediate goals are stabilization of airways, breathing and circulation and termination of seizures. Benzodiazepines remain the first-line drugs recommended for prompt termination of seizures. As intravenous lorazepam is not available in France, we suggest clonazepam as the best choice for initial therapy. Rectal diazepam or buccal midazolam remain important options. Intravenous phenytoin/fosphenytoin and phenobarbital are the second-line drugs. Phenytoin is being increasingly substituted by fosphenytoin, but pediatric data are scarce and fosphenytoin is not authorized for use in France below five years old. In children, phenytoin is often preferred to phenobarbital, even though no comparative studies have demonstrated a better efficacy. To manage status epilepticus refractory to a benzodiazepine and administration of phenytoin and/or phenobarbital, many pediatricians today prefer high-dose midazolam infusion rather than thiopental to minimize serious side effects from barbiturate anesthesia. There is no benefit/risk ratio to support the use of propofol

  17. Controlling Access to Suicide Means

    Directory of Open Access Journals (Sweden)

    Miriam Iosue

    2011-12-01

    Full Text Available Background: Restricting access to common means of suicide, such as firearms, toxic gas, pesticides and other, has been shown to be effective in reducing rates of death in suicide. In the present review we aimed to summarize the empirical and clinical literature on controlling the access to means of suicide. Methods: This review made use of both MEDLINE, ISI Web of Science and the Cochrane library databases, identifying all English articles with the keywords “suicide means”, “suicide method”, “suicide prediction” or “suicide prevention” and other relevant keywords. Results: A number of factors may influence an individual’s decision regarding method in a suicide act, but there is substantial support that easy access influences the choice of method. In many countries, restrictions of access to common means of suicide has lead to lower overall suicide rates, particularly regarding suicide by firearms in USA, detoxification of domestic and motor vehicle gas in England and other countries, toxic pesticides in rural areas, barriers at jumping sites and hanging, by introducing “safe rooms” in prisons and hospitals. Moreover, decline in prescription of barbiturates and tricyclic antidepressants (TCAs, as well as limitation of drugs pack size for paracetamol and salicylate has reduced suicides by overdose, while increased prescription of SSRIs seems to have lowered suicidal rates. Conclusions: Restriction to means of suicide may be particularly effective in contexts where the method is popular, highly lethal, widely available, and/or not easily substituted by other similar methods. However, since there is some risk of means substitution, restriction of access should be implemented in conjunction with other suicide prevention strategies.

  18. Detection in superheated water chromatography

    Energy Technology Data Exchange (ETDEWEB)

    Chienthavorn, O

    1999-11-01

    Superheated water has been used successfully as an eluent in liquid chromatography and has been coupled to various modes of detection, ultraviolet (UV), fluorescence, and nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS). A number of compounds were examined on poly(styrene-divinylbenzene) (PS-DVB), polybutadiene (PBD), and octadecylsilyl bonded silica (ODS) column with isothermal and temperature programmes. The PS-DVB column was mostly used throughout the project as it was the most stable. Not only pure water could serve as superheated water mobile phase; inorganic buffered water and ion-pairing reagent with a concentration of 1-3 mM of the buffer and reagent were also exploited. It was shown that the pH could be controlled during the separation without salt precipitation and the separations followed a conventional reversed-phase HPLC method. Results from fluorescence detection showed good separation of a series of vitamins, such as pyridoxine, riboflavin, thiamine, and some analgesics. The relationship of riboflavin using the detection was linear and the detection limit was seven times higher than that of a conventional method. Simultaneous separation and identification using superheated water chromatography-NMR was demonstrated. With using a stop flow method, NMR spectra of model drugs, namely barbiturates, paracetamol, caffeine and phenacetin were obtained and the results agreed with reference spectra, confirming a perfect separation. A demonstration to obtain COSY spectrum of salicylamide was also performed. The method was expanded to the coupling of superheated water LC to NMR-MS. Results from the hyphenated detection method showed that deuteration and degradation happened in the superheated water conditions. The methyl group hydrogens of pyrimidine ring of sulfonamide and thiamine were exchanged with deuterium. Thiamine was decomposed to 4-methyl-5-thiazoleethanol and both were deuterated under the conditions. (author)

  19. A diaCEST MRI approach for monitoring liposomal accumulation in tumors.

    Science.gov (United States)

    Chan, Kannie W Y; Yu, Tao; Qiao, Yuan; Liu, Qiang; Yang, Ming; Patel, Himatkumar; Liu, Guanshu; Kinzler, Kenneth W; Vogelstein, Bert; Bulte, Jeff W M; van Zijl, Peter C M; Hanes, Justin; Zhou, Shibin; McMahon, Michael T

    2014-04-28

    Nanocarrier-based chemotherapy allows preferential delivery of therapeutics to tumors and has been found to improve the efficacy of cancer treatment. However, difficulties in tracking nanocarriers and evaluating their pharmacological fates in patients have limited judicious selection of patients to those who might most benefit from nanotherapeutics. To enable the monitoring of nanocarriers in vivo, we developed MRI-traceable diamagnetic Chemical Exchange Saturation Transfer (diaCEST) liposomes. The diaCEST liposomes were based on the clinical formulation of liposomal doxorubicin (i.e. DOXIL®) and were loaded with barbituric acid (BA), a small, organic, biocompatible diaCEST contrast agent. The optimized diaCEST liposomal formulation with a BA-to-lipid ratio of 25% exhibited 30% contrast enhancement at B1=4.7μT in vitro. The contrast was stable, with ~80% of the initial CEST signal sustained over 8h in vitro. We used the diaCEST liposomes to monitor the response to tumor necrosis factor-alpha (TNF-α), an agent in clinical trials that increases vascular permeability and uptake of nanocarriers into tumors. After systemic administration of diaCEST liposomes to mice bearing CT26 tumors, we found an average diaCEST contrast at the BA frequency (5ppm) of 0.4% at B1=4.7μT while if TNF-α was co-administered the contrast increased to 1.5%. This novel approach provides a non-radioactive, non-metallic, biocompatible, semi-quantitative, and clinically translatable approach to evaluate the tumor targeting of stealth liposomes in vivo, which may enable personalized nanomedicine.

  20. Herbal medicinals: selected clinical considerations focusing on known or potential drug-herb interactions.

    Science.gov (United States)

    Miller, L G

    1998-11-09

    Herbal medicinals are being used by an increasing number of patients who typically do not advise their clinicians of concomitant use. Known or potential drug-herb interactions exist and should be screened for. If used beyond 8 weeks, Echinacea could cause hepatotoxicity and therefore should not be used with other known hepatoxic drugs, such as anabolic steroids, amiodarone, methotrexate, and ketoconazole. However, Echinacea lacks the 1,2 saturated necrine ring associated with hepatoxicity of pyrrolizidine alkaloids. Nonsteroidal anti-inflammatory drugs may negate the usefulness of feverfew in the treatment of migraine headaches. Feverfew, garlic, Ginkgo, ginger, and ginseng may alter bleeding time and should not be used concomitantly with warfarin sodium. Additionally, ginseng may cause headache, tremulousness, and manic episodes in patients treated with phenelzine sulfate. Ginseng should also not be used with estrogens or corticosteroids because of possible additive effects. Since the mechanism of action of St John wort is uncertain, concomitant use with monoamine oxidase inhibitors and selective serotonin reuptake inhibitors is ill advised. Valerian should not be used concomitantly with barbiturates because excessive sedation may occur. Kyushin, licorice, plantain, uzara root, hawthorn, and ginseng may interfere with either digoxin pharmacodynamically or with digoxin monitoring. Evening primrose oil and borage should not be used with anticonvulsants because they may lower the seizure threshold. Shankapulshpi, an Ayurvedic preparation, may decrease phenytoin levels as well as diminish drug efficacy. Kava when used with alprazolam has resulted in coma. Immunostimulants (eg, Echinacea and zinc) should not be given with immunosuppressants (eg, corticosteroids and cyclosporine). Tannic acids present in some herbs (eg, St John wort and saw palmetto) may inhibit the absorption of iron. Kelp as a source of iodine may interfere with thyroid replacement therapies. Licorice

  1. The pharmaceutical industry and the German National Socialist Regime: I.G. Farben and pharmacological research.

    Science.gov (United States)

    López-Muñoz, F; García-García, P; Alamo, C

    2009-02-01

    Before the National Socialist party came to power, the German pharmaceutical industry constituted an international reference as far as the development of new medicines was concerned, having been responsible for synthetic analgesics (phenacetin, phenazones, acetylsalicylic acid), arsphenamine, barbiturates and sulfonamides. The year 1925 saw the founding of I.G. Farben (Interessen-Gemeinschaft Farbenindustrie AG), a conglomerate of companies that would monopolize the country's chemical production and come to own all its major pharmaceutical industries. During the World War II, I.G. Farben participated in numerous operations associated with the criminal activities of the Nazi executive, including the use of slave labour in plants built close to concentration camps, such as that at Auschwitz. With regard to medical and pharmacological research projects, I.G. Farben became involved in experimental programmes using patients from the Nazi regime's euthanasia programmes and healthy subjects recruited without their consent from concentration camps, on whom various pharmacological substances were tested, including sulfamide and arsenical derivatives and other preparations whose composition is not precisely known (B-1012, B-1034, 3382 or Rutenol, 3582 or Acridine), generally in relation to the treatment of infectious diseases, such as typhus, erysipelas, scarlet fever or paratyphoid diarrhoea. Furthermore, I.G. Farben played a decisive role in the German army's chemical warfare programme, contributing to the development of the first two neurotoxic substances, later known as 'nerve agents', tabun and sarin. Some of these activities came to light as a result of the one the famous Nuremberg Trials in 1947, which saw 24 executives and scientists from I.G. Farben brought to justice for, among other offences, the use of slave labour in the concentration camps and forced experimentation with drugs on prisoners.

  2. The HIV antiretroviral drug efavirenz has LSD-like properties.

    Science.gov (United States)

    Gatch, Michael B; Kozlenkov, Alexey; Huang, Ren-Qi; Yang, Wenjuan; Nguyen, Jacques D; González-Maeso, Javier; Rice, Kenner C; France, Charles P; Dillon, Glenn H; Forster, Michael J; Schetz, John A

    2013-11-01

    Anecdotal reports have surfaced concerning misuse of the HIV antiretroviral medication efavirenz ((4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one) by HIV patients and non-infected teens who crush the pills and smoke the powder for its psychoactive effects. Molecular profiling of the receptor pharmacology of efavirenz pinpointed interactions with multiple established sites of action for other known drugs of abuse including catecholamine and indolamine transporters, and GABAA and 5-HT(2A) receptors. In rodents, interaction with the 5-HT(2A) receptor, a primary site of action of lysergic acid diethylamine (LSD), appears to dominate efavirenz's behavioral profile. Both LSD and efavirenz reduce ambulation in a novel open-field environment. Efavirenz occasions drug-lever responding in rats discriminating LSD from saline, and this effect is abolished by selective blockade of the 5-HT(2A) receptor. Similar to LSD, efavirenz induces head-twitch responses in wild-type, but not in 5-HT(2A)-knockout, mice. Despite having GABAA-potentiating effects (like benzodiazepines and barbiturates), and interactions with dopamine transporter, serotonin transporter, and vesicular monoamine transporter 2 (like cocaine and methamphetamine), efavirenz fails to maintain responding in rats that self-administer cocaine, and it fails to produce a conditioned place preference. Although its molecular pharmacology is multifarious, efavirenz's prevailing behavioral effect in rodents is consistent with LSD-like activity mediated via the 5-HT(2A) receptor. This finding correlates, in part, with the subjective experiences in humans who abuse efavirenz and with specific dose-dependent adverse neuropsychiatric events, such as hallucinations and night terrors, reported by HIV patients taking it as a medication.

  3. Single-molecule force-conductance spectroscopy of hydrogen-bonded complexes

    Science.gov (United States)

    Pirrotta, Alessandro; De Vico, Luca; Solomon, Gemma C.; Franco, Ignacio

    2017-03-01

    The emerging ability to study physical properties at the single-molecule limit highlights the disparity between what is observable in an ensemble of molecules and the heterogeneous contributions of its constituent parts. A particularly convenient platform for single-molecule studies are molecular junctions where forces and voltages can be applied to individual molecules, giving access to a series of electromechanical observables that can form the basis of highly discriminating multidimensional single-molecule spectroscopies. Here, we computationally examine the ability of force and conductance to inform about molecular recognition events at the single-molecule limit. For this, we consider the force-conductance characteristics of a prototypical class of hydrogen bonded bimolecular complexes sandwiched between gold electrodes. The complexes consist of derivatives of a barbituric acid and a Hamilton receptor that can form up to six simultaneous hydrogen bonds. The simulations combine classical molecular dynamics of the mechanical deformation of the junction with non-equilibrium Green's function computations of the electronic transport. As shown, in these complexes hydrogen bonds mediate transport either by directly participating as a possible transport pathway or by stabilizing molecular conformations with enhanced conductance properties. Further, we observe that force-conductance correlations can be very sensitive to small changes in the chemical structure of the complexes and provide detailed information about the behavior of single molecules that cannot be gleaned from either measurement alone. In fact, there are regions during the elongation that are only mechanically active, others that are only conductance active, and regions where both force and conductance changes as the complex is mechanically manipulated. The implication is that force and conductance provide complementary information about the evolution of molecules in junctions that can be used to

  4. Neuro-intensive treatment targeting intracranial hypertension improves outcome in severe bacterial meningitis: an intervention-control study.

    Directory of Open Access Journals (Sweden)

    Martin Glimåker

    Full Text Available OBJECTIVE: To evaluate the efficacy of early intracranial pressure (ICP-targeted treatment, compared to standard intensive care, in adults with community acquired acute bacterial meningitis (ABM and severely impaired consciousness. DESIGN: A prospectively designed intervention-control comparison study of adult cases from September 2004 to January 2012. PATIENTS: Included patients were confirmed ABM-cases, aged 16-75 years, with severely impaired mental status on admission. Fifty-two patients, given ICP-targeted treatment at the neuro-intensive care unit, and 53 control cases, treated with conventional intensive care, were included. All the patients received intensive care with mechanical ventilation, sedation, antibiotics and corticosteroids according to current guidelines. Additional ICP-treatment in the intervention group included cerebrospinal fluid drainage using external ventricular catheters (n = 48, osmotherapy (n = 21, hyperventilation (n = 13, external cooling (n = 9, gram-doses of methylprednisolone (n = 3 and deep barbiturate sedation (n = 2 aiming at ICP 50 mmHg. MEASUREMENTS: The primary endpoint was mortality at two months and secondary endpoint was Glasgow outcome score and hearing ability at follow-up at 2-6 months. OUTCOMES: The mortality was significantly lower in the intervention group compared to controls, 5/52 (10% versus 16/53 (30%; relative risk reduction 68%; p<0.05. Furthermore, only 17 patients (32% in the control group fully recovered compared to 28 (54% in the intervention group (relative risk reduction 40%; p<0.05. CONCLUSIONS: Early neuro-intensive care using ICP-targeted therapy, mainly cerebrospinal fluid drainage, reduces mortality and improves the overall outcome in adult patients with ABM and severely impaired mental status on admission.

  5. Anaesthetic and other treatments of shell shock: World War I and beyond.

    Science.gov (United States)

    McKenzie, A G

    2012-03-01

    Post-traumatic stress disorder (PTSD) is an important health risk factor for military personnel deployed in modern warfare. In World War I this condition (then known as shell shock or 'neurasthenia') was such a problem that 'forward psychiatry' was begun by French doctors in 1915. Some British doctors tried general anaesthesia as a treatment (ether and chloroform), while others preferred application of electricity. Four British 'forward psychiatric units' were set up in 1917. Hospitals for shell shocked soldiers were also established in Britain, including (for officers) Craiglockhart War Hospital in Edinburgh; patients diagnosed to have more serious psychiatric conditions were transferred to the Royal Edinburgh Asylum. Towards the end of 1918 anaesthetic and electrical treatments of shell shock were gradually displaced by modified Freudian methods psychodynamic intervention. The efficacy of 'forward psychiatry' was controversial. In 1922 the War Office produced a report on shell shock with recommendations for prevention of war neurosis. However, when World War II broke out in 1939, this seemed to have been ignored. The term 'combat fatigue' was introduced as breakdown rates became alarming, and then the value of pre-selection was recognised. At the Maudsley Hospital in London in 1940 barbiturate abreaction was advocated for quick relief from severe anxiety and hysteria, using i.v. anaesthetics: Somnifaine, paraldehyde, Sodium Amytal. 'Pentothal narcosis' and 'narco-analysis' were adopted by British and American military psychiatrists. However, by 1945 medical thinking gradually settled on the same approaches that had seemed to be effective in 1918. The term PTSD was introduced in 1980. In the UK the National Institute for Health and Clinical Excellence (NICE) guidelines for management (2005) recommend trauma-focussed Cognitive Behavioural Therapy and consideration of antidepressants.

  6. Expression of pax-6 in rhesus monkey of optical defocus induced myopia and form deprivation myopia

    Institute of Scientific and Technical Information of China (English)

    钟兴武; 葛坚; 邓文国; 陈晓莲; 黄娟

    2004-01-01

    Background Pax-6 gene plays an important role in the process of eye development. This study was to determine the role of pax-6 in the axial myopia produced by hyperopic optical defocus and form deprivation in infant monkeys. Methods Among seven normal infant rhesus monkeys (aged 1 to 1.5 months), five wore -3.00 D spectacle lenses over their right eyes and zero-powered lenses over their left eyes. Monocular form deprivation was produced by eyelid fusion in two monkeys. Ten weeks later, the monkeys were sacrificed by an overdose of barbiturates and their eyes were removed immediately. A 5 mm×5 mm button of retina and sclera was taken from the posterior poles along with a 4-mm optic nerve. RNA was isolated separately from each of these three types of tissues. After that, reverse transcription polymerase chain reaction (RT-PCR) was used for determining gene expression in the retina, sclera and optic nerve. Semi-quantitative analyses were performed on the PCR products. Results As expected, the optically induced hyperopic defocus and the form deprivation produced myopic growth. For the lens-treatment monkeys, pax-6 gene expression in the retinas of the defocused eyes was significantly higher than in the retinas of the left eyes (t=5.703, P=0.005). However, there were no analogous significant differences between pax-6 expression in the scleras or the optic nerves. For the two form-deprived monkeys, there were no obvious differences in pax-6 gene expression in the retinas or the optic nerves. Conclusion The result that the expression of pax-6 was enhanced by hyperopic defocus in the infant monkey retina suggests that pax-6 may be involved in vision-dependent eye growth and emmetropization.

  7. Carotid and cranial nerve reconstruction after removal of cavernous sinus lesions.

    Science.gov (United States)

    Sekhar, L N; Sen, C N; Lanzino, G; Pomonis, S

    1991-12-01

    During the last 7 years, approximately 170 neoplasms, and 35 vascular lesions involving the cavernous sinus were treated by the first two authors. During the treatment of such lesions, the direct vein graft reconstruction of the internal carotid artery from the petrous to the supraclinoid or infraclinoid ICA was performed in 23 patients. Graft occlusion occurred in 3 patients and in one of these, it was successfully salvaged by placing a long venous graft from the extracranial ICA to the M3 segment of the middle cerebral artery. The latter 3 patients were neurologically normal. One patient with significant atherosclerotic disease suffered the dissection of the distal internal carotid artery with the graft being patent. The suturing technique. This patient eventually died. Two patients with severely compromised collateral circulation suffered minor strokes due to the temporary occlusion of the ICA. This has been avoided in the more recent patients by the adoption of brain protection techniques such as moderate hypothermia, induced hypertension, and barbiturate coma. Low dose heparin therapy during grafting and high dose intravenous steroids prior to the grafting also appear to be beneficial. Direct vein graft reconstruction of the intracavernous carotid artery is a valuable tool during the management of cavernous sinus lesions. The advantages and disadvantages of this technique as well as the pros and cons of other revascularization techniques will be discussed. During microsurgical removal of cavernous sinus lesions, the cranial nerves III-VI were reconstructed by direct resuture or by nerve grafting in 16 patients. In the majority of these patients, recovery of cranial nerve function was observed, which was very encouraging.(ABSTRACT TRUNCATED AT 250 WORDS)

  8. Investigation of therapeutic potential and molecular mechanism of vitamin P and digoxin in I/R-induced myocardial infarction in rat.

    Science.gov (United States)

    Singh, Harwinder; Kaur, Parneet; Kaur, Pradeep; Muthuraman, Arunachalam; Singh, Gurpreet; Kaur, Manjinder

    2015-05-01

    Ischemic-reperfusion (I/R) is a major event in the pathogenesis of ischemic heart disease that leads to higher rate of mortality. The study has been designed to investigate the therapeutic potential and molecular mechanism of vitamin P and digoxin in I/R-induced myocardial infarction in isolated rat heart preparation by using Langendorff apparatus. The animals were treated with vitamin P (50 and 100 mg/kg; p.o.) and digoxin (500 μg/kg) for 5 consecutive days. Digoxin served as a positive control in the present study. On the sixth day, the heart was harvested and induced to 30 min of global ischemia followed by 120 min of reperfusion using Langendorff apparatus. The coronary effluent was collected at different time intervals (i.e. basal, 1, 15, 30, 45, 60 and 120 min.) for the assessment of myocardial contractility function. In addition, creatine kinase-M and B subunits (CK-MB), lactate dehydrogenase (LDH1) and Na(+)-K(+)-ATPase activity along with oxidative tissue biomarkers (i.e. thio-barbituric acid reactive substances (TBARS) and reduced glutathione (GSH)) changes were estimated. The I/R of myocardium produced decrease in coronary flow rate; increase in CK-MB, LDH1 and Na(+)-K(+)-ATPase activity along with increase in TBARS and decrease in GSH levels as compared to normal group. The treatment with vitamin P (100 mg/kg) and digoxin (500 μg/kg) have produced a significant (p therapeutic medicine for the management of cardiovascular disorders.

  9. Estimation of the volume of distribution of some pharmacologically important compounds from their structural descriptor

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    MOHAMMAD H. FATEMI

    2011-07-01

    Full Text Available Quantitative structure–activity relationship (QSAR approaches were used to estimate the volume of distribution (Vd using an artificial neural network (ANN. The data set consisted of the volume of distribution of 129 pharmacologically important compounds, i.e., benzodiazepines, barbiturates, nonsteroidal anti-inflammatory drugs (NSAIDs, tricyclic anti-depressants and some antibiotics, such as betalactams, tetracyclines and quinolones. The descriptors, which were selected by stepwise variable selection methods, were: the Moriguchi octanol–water partition coefficient; the 3D-MoRSE-signal 30, weighted by atomic van der Waals volumes; the fragment-based polar surface area; the d COMMA2 value, weighted by atomic masses; the Geary autocorrelation, weighted by the atomic Sanderson electronegativities; the 3D-MoRSE – signal 02, weighted by atomic masses, and the Geary autocorrelation – lag 5, weighted by the atomic van der Waals volumes. These descriptors were used as inputs for developing multiple linear regressions (MLR and artificial neural network models as linear and non-linear feature mapping techniques, respectively. The standard errors in the estimation of Vd by the MLR model were: 0.104, 0.103 and 0.076 and for the ANN model: 0.029, 0.087 and 0.082 for the training, internal and external validation test, respectively. The robustness of these models were also evaluated by the leave-5-out cross validation procedure, that gives the statistics Q2 = 0.72 for the MLR model and Q2 = 0.82 for the ANN model. Moreover, the results of the Y-randomization test revealed that there were no chance correlations among the data matrix. In conclusion, the results of this study indicate the applicability of the estimation of the Vd value of drugs from their structural molecular descriptors. Furthermore, the statistics of the developed models indicate the superiority of the ANN over the MLR model.

  10. Suppression of motor cortical excitability in anesthetized rats by low frequency repetitive transcranial magnetic stimulation.

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    Paul A Muller

    Full Text Available Repetitive transcranial magnetic stimulation (rTMS is a widely-used method for modulating cortical excitability in humans, by mechanisms thought to involve use-dependent synaptic plasticity. For example, when low frequency rTMS (LF rTMS is applied over the motor cortex, in humans, it predictably leads to a suppression of the motor evoked potential (MEP, presumably reflecting long-term depression (LTD -like mechanisms. Yet how closely such rTMS effects actually match LTD is unknown. We therefore sought to (1 reproduce cortico-spinal depression by LF rTMS in rats, (2 establish a reliable animal model for rTMS effects that may enable mechanistic studies, and (3 test whether LTD-like properties are evident in the rat LF rTMS setup. Lateralized MEPs were obtained from anesthetized Long-Evans rats. To test frequency-dependence of LF rTMS, rats underwent rTMS at one of three frequencies, 0.25, 0.5, or 1 Hz. We next tested the dependence of rTMS effects on N-methyl-D-aspartate glutamate receptor (NMDAR, by application of two NMDAR antagonists. We find that 1 Hz rTMS preferentially depresses unilateral MEP in rats, and that this LTD-like effect is blocked by NMDAR antagonists. These are the first electrophysiological data showing depression of cortical excitability following LF rTMS in rats, and the first to demonstrate dependence of this form of cortical plasticity on the NMDAR. We also note that our report is the first to show that the capacity for LTD-type cortical suppression by rTMS is present under barbiturate anesthesia, suggesting that future neuromodulatory rTMS applications under anesthesia may be considered.

  11. Cyanuric acid hydrolase from Azorhizobium caulinodans ORS 571: crystal structure and insights into a new class of Ser-Lys dyad proteins.

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    Seunghee Cho

    Full Text Available Cyanuric acid hydrolase (CAH catalyzes the hydrolytic ring-opening of cyanuric acid (2,4,6-trihydroxy-1,3,5-triazine, an intermediate in s-triazine bacterial degradation and a by-product from disinfection with trichloroisocyanuric acid. In the present study, an X-ray crystal structure of the CAH-barbituric acid inhibitor complex from Azorhizobium caulinodans ORS 571 has been determined at 2.7 Å resolution. The CAH protein fold consists of three structurally homologous domains forming a β-barrel-like structure with external α-helices that result in a three-fold symmetry, a dominant feature of the structure and active site that mirrors the three-fold symmetrical shape of the substrate cyanuric acid. The active site structure of CAH is similar to that of the recently determined AtzD with three pairs of active site Ser-Lys dyads. In order to determine the role of each Ser-Lys dyad in catalysis, a mutational study using a highly sensitive, enzyme-coupled assay was conducted. The 10⁹-fold loss of activity by the S226A mutant was at least ten times lower than that of the S79A and S333A mutants. In addition, bioinformatics analysis revealed the Ser226/Lys156 dyad as the only absolutely conserved dyad in the CAH/barbiturase family. These data suggest that Lys156 activates the Ser226 nucleophile which can then attack the substrate carbonyl. Our combination of structural, mutational, and bioinformatics analyses differentiates this study and provides experimental data for mechanistic insights into this unique protein family.

  12. [Sedation and analgesia assessment tools in ICU patients].

    Science.gov (United States)

    Thuong, M

    2008-01-01

    Sedative and analgesic treatment administered to critically ill patients need to be regularly assessed to ensure that predefinite goals are well achieved as the risk of complications of oversedation is minimized. In most of the cases, which are lightly sedation patients, the goal to reach is a calm, cooperative and painless patient, adapted to the ventilator. Recently, eight new bedside scoring systems to monitor sedation have been developed and mainly tested for reliability and validity. The choice of a sedation scale measuring level of consciousness, could be made between the Ramsay sedation scale, the Richmond Agitation Sedation scale (RASS) and the Adaptation to The Intensive Care Environment scale-ATICE. The Behavioral Pain Scale (BPS) is a behavioral pain scale. Two of them have been tested with strong evidence of their clinimetric properties: ATICE, RASS. The nurses'preference for a convenient tool could be defined by the level of reliability, the level of clarity, the variety of sedation and agitation states represented user friendliness and speed. In fine, the choice between a simple scale easy to use and a well-defined and complex scale has to be discussed and determined in each unit. Actually, randomized controlled studies are needed to assess the potential superiority of one scale compared with others scales, including evaluation of the reliability and the compliance to the scale. The usefulness of the BIS in ICU for patients lightly sedated is limited, mainly because of EMG artefact, when subjective scales are more appropriated in this situation. On the other hand, subjective scales are insensitive to detect oversedation in patients requiring deep sedation. The contribution of the BIS in deeply sedation patients, patients under neuromuscular blockade or barbiturates has to be proved. Pharmacoeconomics studies are lacking.

  13. The role of psychopharmacology in the medical abuses of the Third Reich: from euthanasia programmes to human experimentation.

    Science.gov (United States)

    López-Muñoz, Francisco; Alamo, Cecilio; García-García, Pilar; Molina, Juan D; Rubio, Gabriel

    2008-12-16

    German psychiatry and pharmacology both enjoyed an extraordinary international reputation prior to the promulgation of the Third Reich. However, with the triumph of eugenic ideas and the imposition of a "racial hygiene" policy by the Nazi regime, various organs of the German health system saw themselves involved in a perverse system of social control, in which the illicit use of psychopharmacological tools became customary. In the present work, we review, from the historical perspective, the factors that helped to bring about this situation and we analyze the abuses (known and documented) committed through the specific use of psychotropic drugs during the Nazi period. Among such abuses we can identify the following illegitimate activities: the use of psychoactive drugs, mainly sedatives from the barbiturates family, in the different euthanasia programmes implemented by the Nazi authorities, in police activity and various types of repression, and for purely criminal and extermination purposes within the so-called "Final Solution"; psychopharmacological research on the mentally ill, without the slightest ethical requirements or legal justification; and the use of psychotropic agents in research on healthy subjects, recruited from concentration camps. Finally, we refer to the role of poisonous nerve agents (tabun, sarin and soman) as instruments of chemical warfare and their development by the German authorities. Many of these activities, though possibly only a small portion of the total - given the destruction of a great deal of documentation just before the end of World War II - came to light through the famous Nuremberg Trials, as well as through other trials in which specific persons were brought to justice unilaterally by individual Allied nations or by the authorities of the new German government after the War.

  14. Thiopental inhibits global protein synthesis by repression of eukaryotic elongation factor 2 and protects from hypoxic neuronal cell death.

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    Christian I Schwer

    Full Text Available Ischemic and traumatic brain injury is associated with increased risk for death and disability. The inhibition of penumbral tissue damage has been recognized as a target for therapeutic intervention, because cellular injury evolves progressively upon ATP-depletion and loss of ion homeostasis. In patients, thiopental is used to treat refractory intracranial hypertension by reducing intracranial pressure and cerebral metabolic demands; however, therapeutic benefits of thiopental-treatment are controversially discussed. In the present study we identified fundamental neuroprotective molecular mechanisms mediated by thiopental. Here we show that thiopental inhibits global protein synthesis, which preserves the intracellular energy metabolite content in oxygen-deprived human neuronal SK-N-SH cells or primary mouse cortical neurons and thus ameliorates hypoxic cell damage. Sensitivity to hypoxic damage was restored by pharmacologic repression of eukaryotic elongation factor 2 kinase. Translational inhibition was mediated by calcium influx, activation of the AMP-activated protein kinase, and inhibitory phosphorylation of eukaryotic elongation factor 2. Our results explain the reduction of cerebral metabolic demands during thiopental treatment. Cycloheximide also protected neurons from hypoxic cell death, indicating that translational inhibitors may generally reduce secondary brain injury. In conclusion our study demonstrates that therapeutic inhibition of global protein synthesis protects neurons from hypoxic damage by preserving energy balance in oxygen-deprived cells. Molecular evidence for thiopental-mediated neuroprotection favours a positive clinical evaluation of barbiturate treatment. The chemical structure of thiopental could represent a pharmacologically relevant scaffold for the development of new organ-protective compounds to ameliorate tissue damage when oxygen availability is limited.

  15. Anti-NMDA-R encephalitis: Should we consider extreme delta brush as electrical status epilepticus?

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    Chanson, Eve; Bicilli, Élodie; Lauxerois, Michel; Kauffmann, Sophie; Chabanne, Russell; Ducray, François; Honnorat, Jérome; Clavelou, Pierre; Rosenberg, Sarah

    2016-02-01

    Seizures are common clinical manifestations in anti-N-methyl-d-aspartate receptor (anti-NMDA-R) encephalitis, among other neurological and psychiatric symptoms. During the course of the disease, some specific EEG patterns have been described: generalized rhythmic delta activity (GRDA) and extreme delta brush (EDB). In comatose patients, the association of these EEG abnormalities with subtle motor manifestations can suggest ongoing non-convulsive status epilepticus (NCSE). We report the case of a 28-year-old woman admitted for a clinical presentation typical of anti-NMDA-R encephalitis, which was confirmed by CSF analysis. She was rapidly intubated because of severe dysautonomia and disturbed consciousness. Clinical examination revealed subtle paroxysmal and intermittent myoclonic and tonic movements, correlated on video-EEG with GRDA and/or EDB. NCSE was then suspected, but electroclinical manifestations persisted despite many anti-epileptic drugs combinations, or reappeared when barbiturate anesthesia was decreased. In order to confirm or dismiss the diagnosis, intracranial pressure (ICP) and surface video-EEG monitoring were performed simultaneously and revealed no ICP increase, thus being strongly against a diagnosis of seizures. Sedation was progressively weaned, and clinical condition as well as EEG appearance progressively improved. Literature review revealed 11 similar cases, including 2 with focal NCSE. Of the nine other cases, NCSE diagnosis was finally excluded in 5 cases. NCSE diagnosis in association with anti-NMDA-R encephalitis is sometimes very difficult and its occurrence might be overestimated. Video-EEG is highly recommended and more invasive techniques may sometimes be necessary.

  16. Serotonin reuptake inhibitor discontinuation syndrome: a hypothetical definition. Discontinuation Consensus panel.

    Science.gov (United States)

    Schatzberg, A F; Haddad, P; Kaplan, E M; Lejoyeux, M; Rosenbaum, J F; Young, A H; Zajecka, J

    1997-01-01

    Adverse events following discontinuation from serotonin reuptake inhibitors (SRIs) are being reported in the literature with increasing frequency; the frequency and severity of these symptoms appear to vary according to the half-life of the SRI, e.g., the incidence appears higher with the shorter half-life agents than with fluoxetine, which has an extended half-life. Yet, there have been no systematic studies of the phenomenon to date. Therefore, a group of experts convened in Phoenix, Arizona, to develop a clear description or definition of the phenomenon based on these reports. The SRI discontinuation syndrome, referred to as "withdrawal symptoms" in many anecdotal case reports, is distinctly different from the classic withdrawal syndrome associated with alcohol and barbiturates. Anti-depressants are not associated with dependence or drug-seeking behavior. SRI discontinuation symptoms tend to be short-lived and self-limiting, but can be troublesome. They may emerge when an SRI is abruptly discontinued, when doses are missed, and less frequently, during dosage reduction. In addition, the symptoms are not attributable to any other cause and can be reversed when the original agent is reinstituted, or one that is pharmacologically similar is substituted. SRI discontinuation symptoms, in most cases, may be minimized by slowly tapering antidepressant therapy, but there have been several case reports where symptoms occurred consistently even through repeated attempts to taper therapy. Physical symptoms include problems with balance, gastrointestinal and flu-like symptoms, and sensory and sleep disturbances. Psychological symptoms include anxiety and/or agitation, crying spells, and irritability. Further analyses of data bases and clinical studies are needed to define this proposed syndrome more clearly.

  17. 金属离子Zn2+对精氨酸酶抑制作用的研究%Investigation on the inhibition against arginase catalyzed reaction by Zn2+

    Institute of Scientific and Technical Information of China (English)

    史竞艳; 王志勇; 刘欲文; 汪存信

    2012-01-01

    The influence of Zn2+ on arginase catalyzed reaction was studied by microcalorimetry at 37°C ,pH = 9. 4,40 mmol · L-1 sodium barbiturate-hydrochloric acid buffer solution. The result indicated that Zn2+ has remarkable inhibition effect on the catalytic activity of arginase and the inhibitory type belongs to the reversible competitive inhibition with the inhibition constants of 6. 85xlCT7 mol · L-1. According to the inhibition type and ion radius,we suggest that the reason for inhibition is the competition of Zn 2+on the active site of arginase and thus inhibits the reaction activity of arginase.%在37℃,pH=9.4,40 mmol·L-1的巴比妥钠-盐酸缓冲体系中,利用微量热法研究了金属离子Zn2+对牛肝精氨酸酶催化L-精氨酸水解反应的影响.实验表明,Zn2+对精氨酸酶催化反应存在着明显抑制作用,其抑制类型为竞争性可逆抑制,并求得抑制常数K1为6.85×10-7 mol·L-1.根据其抑制类型和离子半径,推测Zn2+对精氨酸酶的抑制主要是夺取Mn2+的位置,从而使酶失活.

  18. Drug addiction. Part I. Psychoactive substances in the past and presence.

    Science.gov (United States)

    Vetulani, J

    2001-01-01

    Substances capable of changing the functions of the central nervous system are widely distributed in plant kingdom, and many of them were discovered by ancient food-gatherers at the dawn of humanity. In the Old World only a few substances producing euphoria or altered states of consciousness and having habit-forming properties are still widely used. They are the products of poppy (opium, morphine), hemp (hashish, marijuana), and of fermentation of various organic materials alkohol. This list has recently been joined by the psilocybin-containing mushrooms. The addiction-forming compounds originated in the New World and widely spread are tobacco (nicotine) and cocaine. In the 19th and 20th, century the development of medicinal chemistry resulted in several synthetic compounds, originally proposed as therapeutics, such as barbiturates, benzodiazepines and amphetamines. Due to legal problems, to avoid production of the substances already prohibited, many designer drugs were manufactured. In addition, several compounds were synthesized as recreational drugs. Also some compounds that were not regarded as drugs, such as aromatic hydrocarbons and other cleansing agents, as well as steroids were found to have properties of dangerous, habit-forming agents. The attitude of society and the pattern of use of psychoactive substances have changed with time, particularly in the last decades. The active principles are now more addictive because of concentration, purification, chemical modifications and the way of ingestion, which now favors most rapid transport to the central nervous system. The substance abuse approaches the level of global epidemics, and the recent usage of drugs of addition is also reviewed.

  19. Pharmacist Theodor Salzer (1833-1900) and the discovery of bisphosphonates.

    Science.gov (United States)

    Petroianu, G A

    2011-10-01

    Herbert Fleisch, the father of the therapeutic use of bisphosphonates in modern medicine, repeatedly stated in his numerous reviews that bisphosphonates were first synthesized 1865 in Germany by the Russian chemist Menschutkin. He was wrong on two counts. Had Menschutkin synthesized bisphosphonates, as he was a student of Wurtz at the time of the "synthesis", the birthplace of the substances would have been France and not Germany; but he did not. By reacting phosphorous acid with acetyl-chloride he obtained derivatives of pyro-phosphorous and pyro-phosphoric acids (P-O-P backbone) and not bisphosphonates (P-C-P backbone). The discovery of the first bisphosphonate occurred indeed in Germany but some thirty years later and not without some drama. First 1894 the pharmacist Theodor Salzer (1833-1900) described an impurity contained in commercially available phosphoric acid but failed to identify it as acetodiphosphoric acid, a bisphosphonate. 1896, an undergraduate student, Hans von Baeyer working in Munich at the Royal Academy of Sciences in the chemical laboratory of his father Adolf (the 1905 Nobel Prize laureate and discoverer of the barbiturates) synthesized an unknown substance which his famous father summarily rejected as some "Dreck" or impurity. Only due to the tenacity of young Hans work on the matter was continued and the paper describing the synthesis published a year later. The correctness of the chemical structure of the compound as assumed by von Baeyer (and his Ph.D. supervisor Hofmann) was confirmed 1901 by Heidepriem, a Ph.D. student of Hofmann. This short report attempts to shed some light on the life of the lesser known pharmacists and chemists involved in the synthesis of the first bisphosphonate, focusing on Salzer, Heidepriem and von Baeyer.

  20. Comparison of Alcohol Withdrawal Outcomes in Patients Treated with Benzodiazepines Alone versus Adjunctive Phenobarbital: a Retrospective Cohort Study

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    Lauren Z. Gashlin

    2015-03-01

    Full Text Available Background: For treatment of severe alcohol withdrawal syndrome, high dose benzodiazepines (BZDs may cause delirium and over-sedation. Phenobarbital (PBT is a long-acting barbiturate effective for the treatment of alcohol withdrawal. Given the potential benefits of PBT, we sought to investigate the effectiveness of PBT as adjunctive treatment for alcohol withdrawal. Methods: This was a retrospective cohort study on patients with a diagnosis of alcohol withdrawal who had a CIWA-Ar score > 10 treated with either BZDs alone (BZD alone group or BZDs with adjunctive PBT (PBT-adjunct group. The patients received at least one dose of PBT in addition to BZDs (variable doses in the PBT-adjunct group, and three doses of 20 mg diazepam equivalents within 6 hours in the BZD alone group. The primary endpoint was the proportion of patients with a CIWA-Ar score < 10 at 24 hours after initial treatment. Duration of withdrawal and cumulative dose of BZDs were also assessed. Results: Seven subjects in the adjunctive phenobarbital and 21 in the benzodiazepine group were included in the final analysis. Two patients (28.6% in the PBT-adjunct group and 5 patients (23.8% in the BZD only group achieved the primary endpoint, though the difference between the two groups was not statistically significant (P = 0.588. The median (IQR duration of withdrawal symptoms was 44 (12-62 hours in the PBT-adjunct group compared to 53 (37-87 hours in the BZD only group, with no significant difference between the groups (P = 0.249. The median (IQR cumulative BZD dose requirement (diazepam equivalent in the PBT-adjunct group was significantly lower than BZD alone group (25 (20-226 vs. 326 (160-550 mg, P = 0.02. Conclusion: PBT appears to be a safe and effective alternative to BZDs for the treatment of alcohol withdrawal in non-critically ill patients and may be BZD sparing.

  1. Steroid modulation of the chloride ionophore in rat brain: structure-activity requirements, regional dependence and mechanism of action

    Energy Technology Data Exchange (ETDEWEB)

    Gee, K.W.; Bolger, M.B.; Brinton, R.E.; Coirini, H.; McEwen, B.S.

    1988-08-01

    Further in vitro studies of steroids active at the gamma-aminobutyric acidA (GABAA) receptor regulated Cl- channel labeled by (35S)-t-butylbicyclophosphorothionate ((35S)TBPS) reveal additional structural requirements necessary for activity. Evaluation of selected steroids for activity against TBPS-induced convulsions show similar requirements for activity. Interestingly, steroids (e.g., 5 alpha-pregnan-3 alpha, 20 alpha-diol) were identified that have high potency but limited efficacy as modulators of (35S)TBPS binding. These characteristics are reminiscent of the clinically useful benzodiazepines (BZs) such as clonazepam. However, interactions between the prototypical anesthetic-barbiturate, sodium pentobarbital, and steroids active at the Cl- channel suggest that they do not share a common site of action as allosteric modulators of (35S)TBPS and BZ receptor binding. The most potent steroid evaluated, 5 alpha-pregnan-3 alpha-ol-20-one, modulates (35S)TBPS binding at low concentrations (IC50 approximately 17 nM) in a regionally dependent manner. All (35S)TBPS binding sites appear to be functionally coupled to a steroid modulatory site. Because several of the active steroids are metabolites of progesterone, their ability to inhibit the binding of (3H)promegestrone to the cytosolic progestin receptor in rat uterus was evaluated. Those steroids showing potent activity at the GABAA receptor-Cl- ionophore were inactive at the intracellular progestin receptor. Such specificity coupled with their high potency provide additional support for the hypothesis that some of these steroids may be involved in the homeostatic regulation of brain excitability via the GABAA-BZ receptor complex.

  2. Binding interactions of convulsant and anticonvulsant gamma-butyrolactones and gamma-thiobutyrolactones with the picrotoxin receptor

    Energy Technology Data Exchange (ETDEWEB)

    Holland, K.D.; McKeon, A.C.; Covey, D.F.; Ferrendelli, J.A. (Washington Univ. School of Medicine, St. Louis, MO (USA))

    1990-08-01

    Alkyl-substituted gamma-butyrolactones (GBLs) and gamma-thiobutyrolactones (TBLs) are neuroactive chemicals. beta-Substituted compounds are convulsant, whereas alpha-alkyl substituted GBLs and TBLs are anticonvulsant. The structural similarities between beta-alkyl GBLs and the convulsant picrotoxinin suggested that alkyl substituted GBLs and TBLs act at the picrotoxin receptor. To test this hypothesis we examined the interactions of convulsant and anticonvulsant GBLs and TBLs with the picrotoxin, benzodiazepine and gamma-aminobutyric acid (GABA) binding sites of the GABA receptor complex. All of these convulsants and anticonvulsants studied competitively displaced 35S-t-butylbicyclophosphorothionate (35S-TBPS), a ligand that binds to the picrotoxin receptor. This inhibition of 35S-TBPS binding was not blocked by the GABA antagonist bicuculline methobromide. The convulsant GBLs and TBLs also partially inhibited (3H)muscimol binding to the GABA site and (3H)flunitrazepam binding to the benzodiazepine site, but they did so at concentrations substantially greater than those that inhibited 35S-TBPS binding. The anticonvulsant GBLs and TBLs had no effect on either (3H)muscimol or (3H)flunitrazepam binding. In contrast to the GBLs and TBLs, pentobarbital inhibited TBPS binding in a manner that was blocked by bicuculline methobromide, and it enhanced both (3H)flunitrazepam and (3H)muscimol binding. Both ethosuximide and tetramethylsuccinimide, neuroactive compounds structurally similar to GBLs, competitively displaced 35S-TBPS from the picrotoxin receptor and both compounds were weak inhibitors of (3H) muscimol binding. In addition, ethosuximide also partially diminished (3H)flunitrazepam binding. These data demonstrate that the site of action of alkyl-substituted GBLs and TBLs is different from that of GABA, barbiturates and benzodiazepines.

  3. Bizarre behavior during intracarotid sodium amytal testing (Wada test: are they predictable? Reações bizarras durante o teste do amital sódico intracarotídeo (TASI ou Teste de Wada: é possível prevê-las?

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    Luciano de Paola

    2004-06-01

    Full Text Available The intracarotid sodium amytal test (ISAT or Wada Test is a commonly performed procedure in the evaluation of patients with clinically refractory epilepsy candidates to epilepsy surgery. Its goal is to promote selective and temporary interruption of hemispheric functioning, seeking to define language lateralization and risk for memory compromise following surgery. Behavioral modification is expected during the procedure. Even though it may last several minutes, in most cases it is subtle and easily manageable. We report a series of patients in whom those reactions were unusually bizarre, including agitation and aggression. Apart of the obvious technical difficulties (patients required physical restraining those behaviors potentially promote testing delay or abortion and more importantly, inaccurate data. We reviewed those cases, seeking for features that might have predicted their occurrence. Overall, reactions are rare, seen in less than 5% of the ISAT procedures. The barbiturate effect, patients' psychiatric profiles, hemisphere dominance or selectiveness of the injection were not validated as predictors. Thorough explanation, repetition and simulation may be of help in lessening the risk of those reactions.O teste do amital sódico intracarotídeo (TASI ou teste de Wada é procedimento comum na avaliação de pacientes portadores de epilepsia clinicamente refratária candidatos a cirurgia de epilepsia. Tem por objetivo promover interrupção seletiva e temporária da função hemisferial, definindo lateralização de linguagem e risco de comprometimento de memória no pós-operatório. São esperadas mudanças comportamentais durante o teste, as quais podem durar vários minutos, porém, em geral, são sutis e facilmente manejáveis. Relatamos uma série de casos em que ocorreram comportamentos pouco usuais, bizarros, incluindo agitação e agressividade. Estes comportamentos comprometem o teste (paciente deve ser contido, podendo levar a

  4. Tratamento da epilepsia na infância com mogadon Treatment of epilepsy in children with Mogadon

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    Antonio B. Lefèvre

    1969-06-01

    Full Text Available São analisados os resultados obtidos com o emprego do Mogadon em 68 casos de epilepsia em crianças (34 com síndrome de West, 14 com epilepsia tipo P.M. ausência simples e 20 com formas atípicas de P.M., todos rebeldes aos tratamentos convencionais experimentados em várias combinações, e durante tempo variável, porém quase sempre bastante longo. A maioria dos pacientes apresentava intenso retardamento psicomotor, provavelmente decorrente da longa evolução não controlada da epilepsia. Os resultados foram muito bons no que diz respeito ao controle das crises (100% em 28, 75% em 22, 50% em 10, 25% em um e nulo apenas em 7 casos. O resultado sôbre o desenvolvimento psicomotor foi menos brilhante, pois poucos pacientes melhoraram com o controle das crises. Os efeitos colaterais foram pouco importantes, tendo sido nulos em 41; em 23 foi notada sonolëncia (em dois acompanhada de ataxia; em 4 houve queixa de insônia controlável com barbitúricos. O seguimento após o tratamento variou de 6 a 18 meses.Therapeutic results with Mogadon in 68 children with epilepsy (34 cases of West syndrome, 14 with tipical P.M. seizures, 20 with atypical P.M. seizures resistant to conventional therapy employed previously in various combinations for prolonged periods, is reported. The majority of the patients showed intense psychomotor retardation, probably due to the non-controlled evolution of the cases, before the administration of Mogadon. Results were excellent in regard to the control of the crise's frequency (100% in 28, 75% in 22, 50% in 10, 25% in one, and null in 7 cases. Concerning the psychomotor development the results were less evident. Side effects were negligible, being absent in 41 cases; 23 patients showed somnolence, accompanied by ataxia in two cases. Four patients complained of insomnia, promptly controlled with barbiturates. The period of post-treatment follow-up ranged between 6 and 18 months.

  5. Simultaneous analysis method for GHB, ketamine, norketamine, phenobarbital, thiopental, zolpidem, zopiclone and phenytoin in urine, using C18 poroshell column.

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    Anilanmert, Beril; Çavuş, Fatma; Narin, Ibrahim; Cengiz, Salih; Sertler, Şefika; Özdemir, Ali Acar; Açikkol, Münevver

    2016-06-01

    Date-rape drugs have the potential to be used in drug-facilitated sexual assault, organ theft and property theft. Since they are colorless, tasteless and odorless, victims can drink without noticing, when added to the beverages. These drugs must be detected in time, before they are cleared up from the biofluids. A simultaneous extraction and determination method in urine for GHB, ketamine, norketamine, phenobarbital, thiopental, zolpidem, zopiclone and phenytoin (an anticonvulsant and antiepileptic drug) with LC-MS/MS was developed for the first time with analytically acceptable recoveries and validated. A 4 steps liquid-liquid extraction was applied, using only 1.000mL urine. A new age commercial C18 poroshell column with high column efficiency was used for LC-MS/MS analysis with a fast isocratic elution as 5.5min. A new MS transition were introduced for barbital. 222.7>179.8 with the effect of acetonitrile. Recoveries (%) were between 80.98-99.27 for all analytes, except for GHB which was 71.46. LOD and LOQ values were found in the ranges of 0.59-49.50 and 9.20-80.80ngmL(-1) for all the analytes (except for GHB:3.44 and 6.00μgmL(-1)). HorRat values calculated (between 0.25-1.21), revealed that the inter-day and interanalist precisions (RSD%≤14.54%) acceptable. The simultaneous extraction and determination of these 8 analytes in urine is challenging because of the difficulty arising from the different chemical properties of some. Since the procedure can extract drugs from a wide range of polarity and pKa, it increases the window of detection. Group representatives from barbiturates, z-drugs, ketamine, phenytoin and polar acidic drugs (GHB) have been successfully analyzed in this study with low detection limits. The method is important from the point of determining the combined or single use of these drugs in crimes and finding out the reasons of deaths related to these drugs.

  6. Immunological GABAergic interactions and therapeutic applications in autoimmune diseases.

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    Prud'homme, Gérald J; Glinka, Yelena; Wang, Qinghua

    2015-11-01

    medicine, and include benzodiazepines, barbiturates, anticonvulsants, and anesthetic drugs such as propofol. Native GABA can be administered orally to humans as a drug, and has few adverse effects. However, the immune effects of GABAergic drugs in patients are not well documented. GABAergic immunobiology is a recent area of research, which shows potential for the development of new therapies for autoimmune diseases.

  7. Xilazina como pré-medicação para anestesia com tiopental sódico em cães Xylazine as a pre-medicant for thiopental sodium anaesthesia in the dog

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    Orlando Ribeiro Prado Filho

    2000-06-01

    Full Text Available A xilazina produz um bom efeito sedativo-analgésico quando associado à drogas anestésicas. O tiopental sódico é um barbitúrico de curta duração que produz sonolência, sedação e hipnose. O objetivo deste trabalho é verificar a eficiência da associação da xilazina como pré-medicação e do tiopental sódico na manutenção da anestesia, em cães. Foram usados 32 cães sem raça definida, adultos, machos e com peso entre 8 e 10 kg, que foram submetidos à procedimento operatório no esôfago cervical. A dose média de xilazina administrada foi de 3,8 mg/kg e de tiopental sódico foi de 7,7 mg/kg. Não houve necessidade de intubação endotraqueal e não ocorreu óbito relacionado com as medicações anestésicas. Concluindo, o procedimento anestésico descrito é de fácil execução, é seguro e diminui o estresse do animal.The xylazine produce reliable sedative-analgesic effect when coadministered with anesthetics drugs. Thiopental sodium is a shorter duration barbituric, produced somnolence, sedation and hypnosis. The aim of this work is to verify the efficiency in association of xylazine and thiopental sodium to anesthesia in dogs. Thirty-two male mongrel dogs with an average weight between 8 and 10 kg were submitted to surgical procedure with approach of cervical aesophagus. The average dose was 3,8 mg/kg to xilazine and 7,7 mg/kg to thiopental sodium. Was not necessary endotracheal intubation and no deaths due anesthesic procedure were observed. The anesthesic procedure described is easy, safe and decreases the stress of the animal.

  8. Efficacy and the discriminative stimulus effects of negative GABAA modulators, or inverse agonists, in diazepam-treated rhesus monkeys.

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    McMahon, Lance R; Gerak, Lisa R; France, Charles P

    2006-08-01

    In benzodiazepine (BZ)-dependent animals, the effects of negative GABA(A) modulators at BZ sites are not clearly related to differences in negative efficacy (i.e., inverse agonist activity). A flumazenil discriminative stimulus in diazepam (5.6 mg/kg/day)-treated rhesus monkeys was used to test the hypothesis that the effects of negative GABA(A) modulators at BZ sites do not vary as a function of efficacy in BZ-dependent animals. Negative GABA(A) modulators varying in efficacy were studied in combination with positive modulators acting at different modulatory sites (BZ, barbiturate, and neuroactive steroid sites). The negative modulators Ro 15-4513 (ethyl 8-azido-6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-alpha]-[1,4]benzodiazepine-3-carboxylate) and ethyl beta-carboline-3-carboxylate (beta-CCE) substituted for the flumazenil discriminative stimulus. Acute pretreatment with diazepam (3.2 and 10 mg/kg s.c., in addition to 5.6 mg/kg/day p.o.), pentobarbital (3.2 and 10 mg/kg), or pregnanolone (1 and 3.2 mg/kg) attenuated the flumazenil discriminative stimulus and also attenuated the flumazenil-like discriminative stimulus effects of Ro 15-4513 and beta-CCE. Attenuation of the discriminative stimulus effects of flumazenil, Ro 15-4513, and beta-CCE did not systematically vary as a function of negative efficacy. Compared with their discriminative stimulus effects in untreated monkeys discriminating midazolam, both pregnanolone and pentobarbital were relatively more potent than diazepam in attenuating the discriminative stimulus effects of flumazenil, Ro 15-4513, and beta-CCE in diazepam-treated monkeys. These results show that the discriminative stimulus effects of BZ-site neutral and negative modulators are not different in BZ-dependent animals trained to discriminate flumazenil, and extend the results of a previous study showing that positive modulators acting at non-BZ sites are especially potent in attenuating the effects of flumazenil in diazepam-treated monkeys (i

  9. Management of cancer pain: 1. Wider implications of orthodox analgesics

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    Lee SK

    2014-01-01

    Full Text Available Susannah K Lee,1 Jill Dawson,2 Jack A Lee,3 Gizem Osman,4 Maria O Levitin,5 Refika Mine Guzel,5 Mustafa BA Djamgoz5,61Pomona College, Claremont, CA, USA; 2Healthcare Communications Consultancy, Danville, CA, USA; 3College of Arts and Sciences, Vanderbilt University, Nashville, TN, USA; 4Department of Chemical Engineering, Loughborough University, Loughborough, UK; 5Division of Cell and Molecular Biology, Neuroscience Solutions to Cancer Research Group, South Kensington Campus, Imperial College London, London, UK; 6Cyprus International University, Biotechnology Research Centre, Haspolat, North Cyprus, Mersin, TurkeyAbstract: In this review, the first of two parts, we first provide an overview of the orthodox analgesics used commonly against cancer pain. Then, we examine in more detail the emerging evidence for the potential impact of analgesic use on cancer risk and disease progression. Increasing findings suggest that long-term use of nonsteroidal anti-inflammatory drugs, particularly aspirin, may reduce cancer occurrence. However, acetaminophen may raise the risk of some hematological malignancies. Drugs acting upon receptors of gamma-aminobutyric acid (GABA and GABA “mimetics” (eg, gabapentin appear generally safe for cancer patients, but there is some evidence of potential carcinogenicity. Some barbiturates appear to slightly raise cancer risks and can affect cancer cell behavior in vitro. For cannabis, studies suggest an increased risk of squamous cell carcinoma of the tongue, larynx, and possibly lung. Morphine may stimulate human microvascular endothelial cell proliferation and angiogenesis; it is not clear whether this might cause harm or produce benefit. The opioid, fentanyl, may promote growth in some tumor cell lines. Opium itself is an emerging risk factor for gastric adenocarcinoma and possibly cancers of the esophagus, bladder, larynx, and lung. It is concluded that analgesics currently prescribed for cancer pain can

  10. La anestesiología, profesión signada por la drogadicción Anesthesiology and drug addiction

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    Tiberio Alvarez Echeverri

    1994-03-01

    Full Text Available

    Se informa sobre la prevalencia de drogadicción y alcoholismo entre los anestesiólogos, cuyas cifras alcanzan el 2% del total. Las drogas más utilizadas son: fentanil y otros opioides, diazepam, alcohol, anestésicos inhalados, ketamina, barbitúricos, sulfentanil, cocaína, morfina y heroína. Entre los factores de riesgo figuran algunos comunes a la población adicta en general (predisposición genética, exposición ambiental, falta de educación, de programas preventivos y de estrategias de control, estrés y otros peculiares a estos profesionales: disponibilidad de las drogas, autoprescripción, actitud permisiva de los colegas. El tratamiento tiene como objetivos desintoxicar a la persona y lograr que viva sin usar fármacos, que recupere sus aspectos social y ocupacional, que mantenga el tratamiento interdisciplinario, se vincule a grupos de soporte y psicoterapia y se reintegre plenamente a las actividades de la vida diaria una vez haya signos de franca recuperación. Incluye, además, identificar los problemas psiquiátricos de fondo, establecer metas de recuperación a largo plazo y utilizar, si es necesario, drogas antagonistas.

    Prevalence of drug addiction and alcoholism among anesthesiologists has been reported to be around 2%. Most frequently utilized drugs are phentanyl and other opioids, diazepam, alcohol, inhaled anesthetics, ketamine, barbiturates, sulphentanyl, cocaine, morphine and heroine. Besides risk factors that are common to the whole population (genetic predisposition, environmental exposure, stress and lack of education, preventive programs and control strategies, there are others peculiar to anes. thesiologists: availability of drugs, self. prescription and permissivenes of colleagues. Objectives of treatment are: to achieve detoxification and a drug-free life, to recuperate the social and occupational aspects of life, to adhere to

  11. Papain: a novel urine adulterant.

    Science.gov (United States)

    Burrows, David L; Nicolaides, Andrea; Rice, Peter J; Dufforc, Michelle; Johnson, David A; Ferslew, Kenneth E

    2005-01-01

    The estimated number of employees in the United Stated screened annually for illicit drugs is approximately 20 million, with marijuana being the most frequently abused drug. Urine adulterants provide an opportunity for illicit drug users to obtain a false-negative result on commonly used primary drug screening methods such as the enzyme multiplied immunoassay technique and the fluorescence polarized immunoassay technique (FPIA). Typical chemical adulterants such as nitrites are easily detected or render the urine specimen invalid as defined in the proposed SAMHSA guidelines for specimen validity testing based on creatinine, specific gravity, and pH. Papain is a cysteine protease with intrinsic ester hydrolysis capability. The primary metabolite of the psychoactive chemical in marijuana, 11-norcarboxy-Delta9-tetrahydrocannibinol (THC-COOH), was assayed by FPIA in concentrations ranging from 25 to 500 ng/mL, at pH values ranging from 4.5 to 8, over the course of 3 days with papain concentrations ranging from 0 to 10 mg/mL. FPIA analysis of other frequently abused drugs: amphetamines, barbiturates, benzodiazepines, cocaine, opiates, and phencyclidine, along with gas chromatography-mass spectrometry (GC-MS) of THC-COOH and high-pressure liquid chromatography-ultraviolet detection (HPLC-UV) of nordiazepam was performed in order to determine if the mechanism of urine adulteration by papain was analyte specific. Control and adulterated urine specimens (n = 30) were assayed for creatinine, specific gravity, and pH to determine if papain rendered the specimens invalid based on the proposed SAMHSA guidelines. There was a direct pH, temperature, and time-dependent correlate between the increase in papain concentration and the decrease in THC-COOH concentration from the untreated control groups (p < 0.01). The average 72-h THC-COOH concentration decrease at pH 6.2 with a papain concentration of 10 mg/mL was 50%. Papain did not significantly decrease the concentration of the

  12. Uso abusivo de benzidamina no Brasil: uma abordagem em farmacovigilância Use abusive of benzydamine in Brazil: an overview in pharmacovigilance

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    Daniel Marques Mota

    2010-05-01

    Full Text Available O uso abusivo de medicamentos tem sido objeto de crescente interesse em saúde pública e geralmente veiculado na imprensa brasileira. Dentre os medicamentos, objeto de abuso e que causam dependência física e/ou psíquica, incluemse os barbitúricos, benzodiazepínicos, analgésicos opióides e anfetaminas. Os analgésicos, antitérmicos e antiinflamatórios não esteroidais, apesar de não fazerem parte dessa relação de fármacos, estão, geralmente, associados ao uso recreativo ou fins não terapêuticos. O objetivo deste ensaio é apresentar informações sobre o uso abusivo de benzidamina no Brasil. Trata-se de um estudo descritivo do tipo exploratório, em que foram utilizadas diferentes estratégias metodológicas adotadas na prática de regulação em farmacovigilância. O uso abusivo desse fármaco foi constatado na literatura científica, imprensa e internet. Em função da facilidade na compra de medicamentos sujeitos à prescrição médica, entre outros fatores, devem-se exigir meios e formas para monitorar a comercialização e utilização de medicamentos, assegurando seu uso seguro e racional, incluindo o fortalecimento da farmacovigilância no Brasil.The abusive drug use has been object of increasing concern in public health and is commonly issued in the Brazilian press. Amongst medicines, those that are abuse substances and cause physical and/or psychic dependence, barbiturates, benzodiazepines, opioid analgesics and amphetamines are included. Analgesics, antipyretics and non-steroidal anti-inflammatory drugs, even not making part of this list, are generally associated with recreational use or non therapeutical purpose. The objective of this essay is to present information on the abusive use of benzydamine in Brazil. The present study is an exploratory essay in which different methodological strategies adopted in the regulatory practice of pharmacovigilance have been used. The abusive use of this drug was evidenced in

  13. Refractory generalised convulsive status epilepticus : a guide to treatment.

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    Kälviäinen, Reetta; Eriksson, Kai; Parviainen, Ilkka

    2005-01-01

    The patient with status epilepticus has continuous or rapidly repeating seizures. Generalised convulsive status epilepticus (GCSE) is the most common form of the disorder and is a life-threatening condition that requires prompt medical management. Status epilepticus that does not respond to first-line benzodiazepines (lorazepam or diazepam) or to second-line antiepileptic drugs (phenytoin/fosphenytoin, phenobarbital or valproate) is usually considered refractory and requires more aggressive treatment. The optimal treatment of refractory GCSE has not been defined, but patients should be treated in an intensive care unit, as artificial ventilation and haemodynamic support are required. Invasive haemodynamic monitoring is often necessary and EEG monitoring is essential. The drug treatment of refractory GCSE involves general anaesthesia with continuous intravenous anaesthetics given in doses that abolish all clinical and electrographic epileptic activity, often requiring sedation to the point of burst suppression on the EEG. Barbiturate anaesthetics, pentobarbital in the US and thiopental sodium in Europe and Australia, are the most frequently used agents and are highly effective for refractory GCSE both in children and adults. Indeed, they remain the only way to stop seizure activity with certainty in severely refractory cases. Other options are midazolam for adults and children and propofol for adults only.Regardless of the drug selected, intravenous fluids and vasopressors are usually required to treat hypotension. Once seizures have been controlled for 12-24 hours, continuous intravenous therapy should be gradually tapered off if the drug being administered is midazolam or propofol. Gradual tapering is probably not necessary with pentobarbital or thiopental sodium. Continuous EEG monitoring is required during high-dose treatment and while therapy is gradually withdrawn. During withdrawal of anaesthetic therapy, intravenous phenytoin/fosphenytoin or valproate should

  14. Anesthesia and critical-care delivery in weightlessness: A challenge for research in parabolic flight analogue space surgery studies

    Science.gov (United States)

    Ball, Chad G.; Keaney, Marilyn A.; Chun, Rosaleen; Groleau, Michelle; Tyssen, Michelle; Keyte, Jennifer; Broderick, Timothy J.; Kirkpatrick, Andrew W.

    2010-03-01

    BackgroundMultiple nations are actively pursuing manned exploration of space beyond low-earth orbit. The responsibility to improve surgical care for spaceflight is substantial. Although the use of parabolic flight as a terrestrial analogue to study surgery in weightlessness (0 g) is well described, minimal data is available to guide the appropriate delivery of anesthesia. After studying anesthetized pigs in a 0 g parabolic flight environment, our group developed a comprehensive protocol describing prolonged anesthesia in a parabolic flight analogue space surgery study (PFASSS). Novel challenges included a physically remote vivarium, prolonged (>10 h) anesthetic requirements, and the provision of veterinary operating room/intensive care unit (ICU) equivalency on-board an aircraft with physical dimensions of ethical approval, multiple ground laboratory sessions were conducted with combinations of anesthetic, pre-medication, and induction protocols on Yorkshire-cross specific pathogen-free (SPF) pigs. Several constant rate infusion (CRI) intravenous anesthetic combinations were tested. In each regimen, opioids were administered to ensure analgesia. Ventilation was supported mechanically with blended gradients of oxygen. The best performing terrestrial 1 g regime was flight tested in parabolic flight for its effectiveness in sustaining optimal and prolonged anesthesia, analgesia, and maintaining hemodynamic stability. Each flight day, a fully anesthetized, ventilated, and surgically instrumented pig was transported to the Flight Research Laboratory (FRL) in a temperature-controlled animal ambulance. A modular on-board surgical/ICU suite with appropriate anesthesia/ICU and surgical support capabilities was employed. ResultsThe mean duration of anesthesia (per flight day) was 10.28 h over four consecutive days. A barbiturate and ketamine-based CRI anesthetic regimen supplemented with narcotic analgesia by bolus administration offered the greatest prolonged hemodynamic

  15. Nonconsensual withdrawal of nutrition and hydration in prolonged disorders of consciousness: authoritarianism and trustworthiness in medicine.

    Science.gov (United States)

    Rady, Mohamed Y; Verheijde, Joseph L

    2014-11-07

    The Royal College of Physicians of London published the 2013 national clinical guidelines on prolonged disorders of consciousness (PDOC) in vegetative and minimally conscious states. The guidelines acknowledge the rapidly advancing neuroscientific research and evolving therapeutic modalities in PDOC. However, the guidelines state that end-of-life decisions should be made for patients who do not improve with neurorehabilitation within a finite period, and they recommend withdrawal of clinically assisted nutrition and hydration (CANH). This withdrawal is deemed necessary because patients in PDOC can survive for years with continuation of CANH, even when a ceiling on medical care has been imposed, i.e., withholding new treatment such as cardiopulmonary resuscitation for acute life-threatening illness. The end-of-life care pathway is centered on a staged escalation of medications, including sedatives, opioids, barbiturates, and general anesthesia, concurrent with withdrawal of CANH. Agitation and distress may last from several days to weeks because of the slow dying process from starvation and dehydration. The potential problems of this end-of-life care pathway are similar to those of the Liverpool Care Pathway. After an independent review in 2013, the Department of Health discontinued the Liverpool Care pathway in England. The guidelines assert that clinicians, supported by court decisions, have become the final authority in nonconsensual withdrawal of CANH on the basis of "best interests" rationale. We posit that these guidelines lack high-quality evidence supporting: 1) treatment futility of CANH, 2) reliability of distress assessment from starvation and dehydration, 3) efficacy of pharmacologic control of this distress, and 4) proximate causation of death. Finally, we express concerns about the utilitarian-based assessment of what constitutes a person's best interests. We are disturbed by the level and the role of medical authoritarianism institutionalized by these

  16. Review of idiopathic eosinophilic meningitis in dogs and cats, with a detailed description of two recent cases in dogs : review and clinical communication

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    J.H. Williams

    2008-05-01

    Caesarian section after developing a non-responsive inertia 8 days prior to presentation. This animal's clinical signs included status epilepticus seizures unrelated to hypocalcaemia and warranted induction of a barbiturate coma. She died 4 hours later. Post mortem and histopathological findings in the brain were almost identical to those of the Boerboel and she also showed histological evidence of recent active intravascular haemolysis with microcyte formation. Rabies, distemper and Neospora caninum immunohistochemical stains were negative in the brains of both dogs. Immunohistochemical staining of the cerebral and meningeal exudates of the Beagle for T- and B-lymphocyte (CD3 and CD79a markers showed a predominance of T-lymphocytes with fewer scattered B lymphocytes. A possible allergic response to amoxicillin / clavulanate is considered, as this appeared to be the only feature common to the recent history of both animals. An overview of EME in humans, dogs and cats is given and the previously published cases of idiopathic EME in dogs and the single published cat case are briefly reviewed.

  17. PAD patterns of physiologically identified afferent fibres from the medial gastrocnemius muscle.

    Science.gov (United States)

    Jiménez, I; Rudomin, P; Solodkin, M

    1988-01-01

    Intracellular recordings were made in the barbiturate-anesthetized cat from single afferent fibres left in continuity with the medial gastrocnemius muscle to document the transmembrane potential changes produced in functionally identified fibres by stimulation of sensory nerves and of the contralateral red nucleus (RN). Fifty five fibres from muscle spindles had conduction velocities above 70 m/s and were considered as from group Ia. Stimulation of group I afferent fibres of the posterior biceps and semitendinosus nerve (PBSt) produced primary afferent depolarization (PAD) in 30 (54%) Ia fibres. Stimulation of the sural (SU) nerve produced no transmembrane potential changes in 39 (71%) group Ia fibres and dorsal root reflex-like activity (DRRs) in 16 (29%) fibres. In 17 out of 28 group Ia fibres (60.7%) SU conditioning inhibited the PAD generated by stimulation of the PBSt nerve. Facilitation of the PBSt-induced PAD by SU conditioning was not seen. Repetitive stimulation of the RN had mixed effects: it produced PAD in 1 out of 8 fibres and inhibited the PAD induced by PBSt stimulation in 2 other fibres. Nine fibres connected to muscle spindles had conduction velocities below 70 m/s and were considered to be group II afferents. No PAD was produced in these fibres by SU stimulation but DRRs were generated in 5 of them. In 23 out of 31 fibres identified as from tendon organs group I PBSt volleys produced PAD. However, stimulation of the SU nerve produced PAD only in 3 out of 34 fibres, no transmembrane potential changes in 30 fibres and DRRs in 1 fibre. The effects of SU conditioning on the PAD produced by PBSt stimulation were tested in 19 Ib fibres and were inhibitory in 12 of them. In 9 of these fibres SU alone produced no transmembrane potential changes. Repetitive stimulation of the RN produced PAD in 3 out of 9 Ib fibres. SU conditioning inhibited the RN-induced PAD. The present findings support the existence of an alternative inhibitory pathway from cutaneous

  18. Inputs from regularly and irregularly discharging vestibular nerve afferents to secondary neurons in squirrel monkey vestibular nuclei. III. Correlation with vestibulospinal and vestibuloocular output pathways

    Science.gov (United States)

    Boyle, R.; Goldberg, J. M.; Highstein, S. M.

    1992-01-01

    1. A previous study measured the relative contributions made by regularly and irregularly discharging afferents to the monosynaptic vestibular nerve (Vi) input of individual secondary neurons located in and around the superior vestibular nucleus of barbiturate-anesthetized squirrel monkeys. Here, the analysis is extended to more caudal regions of the vestibular nuclei, which are a major source of both vestibuloocular and vestibulospinal pathways. As in the previous study, antidromic stimulation techniques are used to classify secondary neurons as oculomotor or spinal projecting. In addition, spinal-projecting neurons are distinguished by their descending pathways, their termination levels in the spinal cord, and their collateral projections to the IIIrd nucleus. 2. Monosynaptic excitatory postsynaptic potentials (EPSPs) were recorded intracellularly from secondary neurons as shocks of increasing strength were applied to Vi. Shocks were normalized in terms of the threshold (T) required to evoke field potentials in the vestibular nuclei. As shown previously, the relative contribution of irregular afferents to the total monosynaptic Vi input of each secondary neuron can be expressed as a %I index, the ratio (x100) of the relative sizes of the EPSPs evoked by shocks of 4 x T and 16 x T. 3. Antidromic stimulation was used to type secondary neurons as 1) medial vestibulospinal tract (MVST) cells projecting to spinal segments C1 or C6; 2) lateral vestibulospinal tract (LVST) cells projecting to C1, C6; or L1; 3) vestibulooculo-collic (VOC) cells projecting both to the IIIrd nucleus and by way of the MVST to C1 or C6; and 4) vestibuloocular (VOR) neurons projecting to the IIIrd nucleus but not to the spinal cord. Most of the neurons were located in the lateral vestibular nucleus (LV), including its dorsal (dLV) and ventral (vLV) divisions, and adjacent parts of the medial (MV) and descending nuclei (DV). Cells receiving quite different proportions of their direct inputs

  19. [Hierarchical strategy for treating elevated intracranial pressure in severe traumatic brain injury].

    Science.gov (United States)

    Orban, J-C; Ichai, C

    2007-05-01

    persists, evacuation of CBF or osmotherapy may be advocated. In case of refractory intracranial hypertension, it may be useful to deepen neurosedation. Controlled hypocapnia and barbiturates remain a third line therapy providing to monitor and maintain an appropriate CBF and cerebral oxygenation. Controlled hypothermia and decompressive craniectomy must be individually discussed.

  20. Hair analysis to monitor abuse of analgesic combinations containing butalbital and propyphenazone.

    Science.gov (United States)

    Ferrari, Anna; Tiraferri, Ilaria; Palazzoli, Federica; Verri, Patrizia; Vandelli, Daniele; Marchesi, Filippo; Ciccarese, Michela; Licata, Manuela

    2015-11-10

    Butalbital, a barbiturate, is present in analgesic combinations used by headache sufferers. Overuse/abuse of these combinations may cause dependence, chronic migraine, and medication-overuse headache (MOH). MOH is difficult to manage: it improves interrupting analgesic overuse, but requires monitoring, because relapses are frequent. A gas chromatography-mass spectrometry (GC-MS) method for hair analysis has been developed and validated to document abuse of an analgesic combination containing butalbital and propyphenazone by a patient with MOH. For over ten years the patient managed her headache using eight suppositories/day of an analgesic combination containing butalbital 150mg, caffeine 75mg, and propyphenazone 375mg per suppository. An outpatient detoxification treatment was carried out. After three weeks, the patient reduced the consumption to one suppository/day. At the first control visit, after three months from the beginning of detoxification, the patient increased the use of the combination to four suppositories/day and at the second control visit, after seven months from the beginning of detoxification, she was back to eight suppositories/day. At the two control visits, a hair sample was taken for determination of butalbital and propyphenazone. Moreover blood and urine samples for determination of butalbital were drawn at the beginning of detoxification treatment and at the two control visits. With the segmental analysis of two hair samples the medication history of ten months could be estimated. In the first hair sample, collected at the first control visit, in the distal segment, butalbital and propyphenazone concentrations were, respectively, 17.5ng/mg and 56.0ng/mg, confirming the prolonged abuse; in the proximal segment, concurrently with the detoxification treatment, butalbital and propyphenazone concentrations had reduced respectively to 5.45ng/mg and 11.1ng/mg. The second hair sample, collected at the second control visit, proved the fair course

  1. Antioxidant and antimicrobial effects of condiments paste used as nitrite replacer in chicken mince

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    Meena Goswami

    2014-06-01

    Full Text Available Aim: The present study was conducted to evaluate the antioxidant and antimicrobial effects of 4% Ginger + 4% Garlic + Turmeric 1000ppm (GGT, nitrite 200ppm (N and the control (C on minced chicken stored at 4±10C. Materials and Methods: Physico-chemical properties (pH, Thio Barbituric acid value (TBA, Peroxide value (PV and Free Fatty acid (FFA were evaluated on 0, 3, 6 and 9th day of the storage. The antimicrobial studies viz. Total viable count (TVC, Escherichia coli count, Clostridium sporogenes count and Clostridium perfringens count were carried out on 1, 4, 7 and 10th day of storage. Results: Highly significant difference (P<0.01 was noticed between the treatments and between the storage periods in pH (5.951±0.02-GGT as compared to C-5.898±0.05and N-5.899±0.02, TBA(0.566±0.09-GGT as compared to C-1.569±0.04m and N-0.614±0.11, PV(1.679±0.18-GGT as compared to C-2.595±0.41and N-2.03±0.21, FFA(1.199±0.21-GGT as compared to C-2.284±0.40 and N-1.446±0.24 and N-7.194±0.68, TVC (log CFU/g (7.528±0.70-GGT as compared to C-8.583±0.49 and N-6.446±0.53, Escherichia coli (log CFU/g (6.476±0.54-GGT as compared to C-7.658±0.71 and N-6.609±0.61, Clostridium sporogenes count (log CFU/g (7.746±0.69-GGT as compared to C-8.681±0.74 and N- and Clostridium perfringens count (log CFU/g (6.864±0.76-GGT as compared to C-8.790±0.53 and N-6.864±0.58. Conclusion: The Ginger garlic turmeric paste has an excellent potential to replace the nitrite as a natural antioxidant with other advantages. It is highly effective against Escherichia coli. It is also significantly effective against Clostridium perfringens, Clostridium sporogenes and TVC as compared to C but lesser than N. We recommend further research by replacing the nitrite with various combinations of the spices and the condiments.

  2. 我院2009~2011年二类精神药品的应用情况分析%Application Analysis on the Second Class Psychotropic Drugs in Our Hospital from 2009 to 2011

    Institute of Scientific and Technical Information of China (English)

    王玉娉

    2012-01-01

    Objective To evaluate the application situation and development tendency of the second class psychotropic drugs in our hospital and provide references for the drug management and rational drug use. Methods Using the daily dose limit recommended by the World Health Organization(WHO) as the indicator, to retrospectively analyze the application of the second class psychotropic drugs. Results The annual sales and drug use frequency of benzodiazepine and barbiturate psychotropic drugs are rising year by year, with higher use frequency of Clonazepam, Alprazolam and Estazolam. As a representative of the new generation non-benzodiazepine drugs, Zaleplon has been used in a decreased tendency. Conclusion The application structure of the second class psychotropic drugs is stable, and the clinical use of them is basically reasonable. Benzodiazepine drugs have the dominant position in the clinical use.%目的 评价我院二类精神药品的应用情况与发展趋势,为药品管理及合理用药提供参考.方法 采用世界卫生组织推荐的限定日剂量为指标的分析方法,对我院2009~ 2011年二类精神药品的应用进行回顾性分析.结果 我院苯二氮革类及巴比妥类二类精神药品的年销售金额和用药频度逐年上升,氯硝西泮、阿普唑仑和艾司唑仑的用药频度较高,以扎来普隆为代表的新一代非苯二氮革类药物用量有下降趋势.结论 二类精神药品应用结构稳定,临床用药基本合理.苯二氮革类药物占临床用药的主导地位.

  3. Relating the shape of protein binding sites to binding affinity profiles: is there an association?

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    Bitter István

    2010-10-01

    , except for few specific cases, the shapes of the binding pockets have relatively low weights in the determination of the affinity profiles of proteins. Since the MAF profile is closely related to the target specificity of ligand binding sites we can conclude that the shape of the binding site is not a pivotal factor in selecting drug targets. Nonetheless, based on strong specific associations between certain MAF profiles and specific geometric descriptors we identified, the shapes of the binding sites do have a crucial role in virtual drug design for certain drug categories, including morphine derivatives, benzodiazepines, barbiturates and antihistamines.

  4. Electrical stimulation therapies for CNS disorders and pain are mediated by competition between different neuronal networks in the brain.

    Science.gov (United States)

    Faingold, Carl L

    2008-11-01

    treatment of unanesthetized animals with antagonists (bicuculline or strychnine) of inhibitory neurotransmitter (GABA or glycine) receptors can cause CMR neurons to become consistently responsive to external inputs (e.g., peripheral nerve, sensory, or electrical stimuli in the brain) to which these neurons did not previously respond. Conversely, agents that enhance GABA-mediated inhibition (e.g., barbiturates and benzodiazepines) or antagonize glutamate-mediated excitation (e.g., ketamine) can cause CMR neurons to become unresponsive to inputs to which they responded previously. The responses of CMR neurons exhibit extensive short-term and long-term plasticity, which permits them to participate to a variable degree in many networks. Short-term plasticity subserves termination of disease symptoms, while long-term plasticity in CMR regions subserves symptom prevention. This network interaction hypothesis has value for future research in CNS disease mechanisms and also for identifying therapeutic targets in specific brain networks for more selective stimulation and pharmacological therapies.

  5. Talidomida: indicações em Dermatologia Thalidomide: indications in Dermatology

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    Rubem David Azulay

    2004-10-01

    mucous, pruritus, cutaneous eruption, weight gain, hypothyroidism, neutropenia, bradycardia or tachycardia, and hypotension. It interacts with other medicine: barbiturates, chlorpromazine, reserpine, alcohol, acetaminophen, histamine, serotonin and prostaglandin.

  6. Atividade elétrica cerebral do rato com lesões da formação reticular mesencefálica Electrocorticographic study of the rats's bram after lesioning of the midbrain reticular formation

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    Walter C. Pereira

    1970-09-01

    , denotando fases de maior ou menor sincronização do traçado; c ondas teta nas áreas límbicas (talvez evidenciando alerta registradas simultâneamente com fusos em áreas neocorticais.Seventy three rats were prepared for acute and chronic experiments. The midbrain reticular formation was electrolitically destroyed (3,5 — 4,0 mA and 5 — 10 sec by means of an active electrode estereotactically guided according with the atlas of König an Klippel. The procedure was destined to provoke parcial, total, unilateral and bilateral lesions in different preparations. The ECoG was recorded with a 4-channel Beckman polygraph. Short bipolar leads were used in all experiments. 1. Spindling wich occurred after the operation was similar to spindling found in phisiological sleep and in barbiturate narcosis as well. Similarity was striking as to the electrophysiological properties and cortical projections. However, the duration of the individual potentials dispersed much more than in the above mentioned conditions (20 — 80 msec, wich may be related to the higlher complexity exhibited by the spindles which appear on the ECoG after destruction of the reticular formation of the midbrain, possibly due to lack of reticular timing of the thalamic synchronizing system activity, since spindling was more regular when circumscribed lesions of the midbrain were made. 2. The mechanisms involved in production of spindles during spontaneous and barbiturate sleep and after lesioning of the midbrain reticular formation are at least partially dependent upon reticular blocking. 3. The midbrain reticular formation activates mainly the ipsilateral hemisphere. The crossed component of the activating system is, probably, brought in action only when arousing stimuli are very strong. 4. Besides midbrain reticular formation other cortical activating mechanisms certainly play a role in arousing, since, in acute preparations, simultaneously with neocortical spindling, we frequently recorded: a short

  7. Experimental pleural empyema model in rabbits: Why, how and what are the next steps

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    Cvijanović Vlado

    2014-01-01

    Full Text Available Bacgraund/Aim. The use of new therapeutic methods to prevent development of fibrothorax as the final complication of the human pleural infections requires research with experimental animals. The aim of this study was to standardize the procedures for the establishment of our own experimental model of empyema in rabbits, since it should be able to offer similar conditions found in human pleural infections. Methods. This experiment included 15 chinchilla rabbits, weighing from 2.3 to 2.8 kg. There were 12 rabbits in the experimental group, while 3 rabbits formed the control group. On the first day, we administered 0.4-0.5 mL of turpentine in the right pleural space of the rabbits from the experimental group in order to provoke sterile exudative pleurisy. After 24 h we injected 1 mL of Staphylococcus aureus and 1 mL of Escherichia coli bacteria in the same concentration of 4.5 x 108 bacteria/mL. Thoracocentesis for the pleural fluid analysis was performed 24, 48, 72, and 96 h after bacteria instillation. In these pleural samples we estimated the number of leucocytes and the values of lactate dehydrogenase (LDH, glucose and pH in pleural fluid, as well as the presence of bacteria. We did not protect the animals with antibiotics, and on the day 7 of the experiment they were sacrificed with the lethal dose of barbiturate (iv. The lung from the empyemic side of all experimental animals and the lung of one control animal were histopathologically examined. Results. A total of 4 animals had a small amount of clear pleural fluids or there was no fluid obtained with thoracocentesis 24 and 48 h after the bacteria instillation. after the bacteria instillation. In the remaining 8 rabbits 24 h after bacteria administration the mean values (± SD of the parameters monitored were as follows: Le 34.75 ± 6.13 x 109/L, LDH 17,000 ± 4,69 U/L, glucose 1.23 ± 0.45 mmol/L, and pH 6.975 ± 0.15. The obtained values met the criteria for the evaluation of effusion as

  8. Anestesia por infusão contínua de propofol em cães pré-medicados com acepromazina e fentanil Anesthesia by continuous infusion of propofol in dogs premedicated with acepromazine and fentanyl

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    Jefferson da Silva Pires

    2000-10-01

    Full Text Available O propofol (2,6 diisopropilfenol é um agente hipnótico de ultra curta duração que produz sedação e hipnose similar aos barbitúricos, sendo desprovido de ação analgésica. Quimicamente, é o único agente anestésico venoso que pode ser usado tanto na indução como na manutenção anestésica. O presente trabalho objetivou avaliar freqüência cardíaca, respiratória, oximetria, pressão arterial média, volume minuto e volume corrente em cães pré-medicados com acepromazina e fentanil e anestesiados por infusão contínua de propofol. Dez cães foram submetidos à medicação pré-anestésica com acepromazina (0,1mg.kg-1 e fentanil (0,01mg.kg-1, indução (3,16mg.kg-1 e manutenção anestésica com propofol em infusão contínua por noventa minutos, na velocidade de 0,4mg.kg-1.min-1. Os parâmetros foram mensurados imediatamente após a indução, 10, 20, 30, 60 e 90 minutos após; final da infusão e 30 minutos após o seu término. Os parâmetros foram analisados por análise de variância para valores repetidos e as médias foram analisadas pelo teste de Tuckey em nível de 5%. O protocolo utilizado não produziu variações estatisticamente significativas em nenhum dos parâmetros analisados. Um animal apresentou apnéia durante a indução. Embasado nesses resultados, verifica-se que o presente protocolo é seguro e eficaz para a realização de anestesia venosa em caninos.Propofol (2,6 diisopropylphenol is an ultra short duration hypnotic agent that produces sedation and hypnosis similar to barbituric agent, but lacks analgesic action. This is a chemically unique anesthetic agent that can be used for induction and anesthetic maintenance. The objective of this research was to evaluate the cardiac and respiratory rate, oximetry, mean arterial blood pressure and tidal volume and minute volume in dogs premedicated with acepromazine and fentanyl and anesthetized by continuous infusion by propofol. Ten dogs were submitted to

  9. Effect of arsenic on antioxidative ability of human keratinocytes%砷对人皮肤角质形成细胞抗氧化能力影响

    Institute of Scientific and Technical Information of China (English)

    孙鲜策; 王少鹏; 高娜; 刘爽; 杨光; 朴丰源

    2009-01-01

    目的 研究亚砷酸钠(NaAsO2)对人皮肤角质形成细胞(HaCaT)抗氧化能力的影响.方法 用流式细胞仪检测细胞内二氯荧光素(DCF)的荧光强度;用改良硫代巴比妥酸荧光法制定细胞内丙二醛(MDA)含量;用Ni-trite-kit法检测超氧化物歧化酶(SOD)活性;用紫外速率直接法测定过氧化氢酶(CAT)的活性.结果 各实验组(2.5,5,10和20 μmol/L NaAsO2)的DCF荧光强度均显著增高(P<0.05),分别是对照组的1.3,1.6,1.7和1.8倍;各实验组MDA含量显著增高(P<0.05),分别是对照组的1.1,1.4,1.5和2.2倍;10和20 μmol/L NaAsO2组SOD活性显著下降,分别为对照组的78%和61%;10和20μmol/L NaAsO2组SIOD和CAT活性显著下降,分别为对照组的50%和34%.结论 砷可以引起人皮肤细胞的氧化损伤,降低抗氧化能力.%Objective To explore the effect of sodium arsenite( NaAsO2) on antioxidative ability in human keratino-cytes (HaCaT). Methods The fluorescence intensity of dichlorofluorescein(DCF) was detected by flow cytometry. The malondialdehyde(MDA) content was detected by improved thio-barbituric acid fluorometric method. Superoxide dismutase (SOD) activity was determined by Nitrite-kit. The catalase(CAT) activity was determined by ultraviolet velocity direct method. Results The fluorescence intensity of DCF increased to 1.3,1.6,1.7, and 1. 8 times of the control' s in 2. 5,10, and 20 μmol/L NaAsO2 treated groups,respectively (P < 0. 05). The MDA content increased to 1.1,1.4,1.5, and 2.2 time of the control's in 2. 5,10, and 20 μmol/L NaAsO2 treated groups,respectively (P < 0. 05). While the activity of SOD de-creased to 78% and 61% of the control's in 10μmol/L and 20 μmol/L NaAsO2 groups. And CAT activity decreased to 50% and 34% of the control's in 10 μmol/L and 20 μmol/L NaAsO2 groups. Conclusion Arsenic can cause oxidative damage and decrease antioxidative ability in human keratinocytes.

  10. Consumo de drogas y violencia laboral en mujeres trabajadoras de Monterrey, N. L., México Consumo de drogas e violência ocupacional em mulheres trabalhadoras de Monterrey, N. L. México Drug consumption and occupational violence in working women of Monterrey, N. L., Mexico

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    Maria Magdalena Alonso Castillo

    2005-12-01

    qualitative approach. Results indicated that 37.1% of women consumed alcohol, 29.1% tobacco, 0.4% marihuana, 0.1% inhalants, and, among medical drugs, 5% consumed tranquilizers, and 1% other substances (barbiturates, antidepressive agents, Tylenol/codeine. The c² test found no significant difference between sociodemographic and occupational factors and drug consumption (p<.05, except for the work form (c²=18.08, gl=4, p=.001. However, violence rate showed a positive association with drug consumption (p<.05. This study found 126 cases of violence, 34 of which narrated their experience. Drug consumption and violence perception was identified in 2 categories: Conceptualization of Occupational Violence and Relationship between Violence and Drug Consumption.

  11. General unknown screening in hair by liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry (LC-QTOF-MS).

    Science.gov (United States)

    Broecker, Sebastian; Herre, Sieglinde; Pragst, Fritz

    2012-05-10

    data known from case histories and from the analysis of blood, urine and gastric content showed only a low agreement, with many unexpected drugs detected and many reported drugs not detected in hair. Basic drugs and metabolites such as opioides, cocaine, amphetamines, several groups of antidepressants, neuroleptics, beta-blockers or the metamizole metabolite noramidopyrine were found with high frequency whereas acidic and several neutral drugs such as cannabinoids, salicylic acid, furosemide, barbiturates, phenprocoumone or cardiac glycosides could not be detected with sufficient sensitivity, mainly because of the low ion yield of positive ESI for these compounds. The advantage of a comprehensive acquisition of all substances is paid by a lower sensitivity in comparison to targeted screening LC-MS/MS procedures. In conclusion, the procedure of sample preparation and LC-QTOF-MS analysis proved to be a robust and sensitive routine method in which the qualitative screening for a wide variety of toxic substances in hair is combined with the quantitative determination of selected illegal drugs.

  12. Comparative study of drug use among undergraduate students at the University of São Paulo: São Paulo campus in 1996 and 2001 Estudo comparativo entre 1996 e 2001 do uso de drogas por alunos da graduação da Universidade de São Paulo: Campus São Paulo

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    Vladimir de Andrade Stempliuk

    2005-09-01

    Full Text Available OBJECTIVE: To compare the rate of drug use prevalence and to investigate opinions regarding such use among undergraduate students at the University of São Paulo - São Paulo campus in 1996 and again in 2001. METHODS: Both studies followed the same procedures of sampling and data collection. A random sample of undergraduate students, divided into the areas Humanities, Exact Sciences and Biologic Sciences, responded to an anonymous and self-report survey regarding the use of licit and illicit drugs within the last 30 days, within the last 12 months and over the lifetime of the subject. The two surveys were compared through the construction of (95% confidence intervals for the prevalence differences for each substance by area and by total number of students. The Wald test for homogeneity was applied in order to compare the prevalences. RESULTS: High approval of regularly trying and using cocaine, crack, amphetamines and inhalants was observed. The drugs that showed statistic significant increasing were:lifetime use: alcohol, tobacco, marijuana, inhalants, hallucinogens, amphetamines, anticholines, barbiturics and any illicit drug;last-12-month use: marijuana, inhalants, amphetamines, hallucinogens and any illicit drug;last-30-day use: marijuana, inhalants, amphetamines and any illicit drug. DISCUSSON: The observed difference in the use of some drugs between the two surveys appears to be a consequence of the higher rates of favorable opinions regarding trying and regularly using some psychoactive substances, a finding that mirrors global trends in drug use.OBJETIVO: Esta pesquisa teve como objetivo comparar as prevalências de uso de diversas drogas e as opiniões sobre esses usos entre estudantes de graduação da Universidade de São Paulo (USP nos anos de 1996 e 2001. MÉTODOS: Os dois estudos seguiram as mesmas metodologias de amostragem e coleta de dados. Os alunos foram randomicamente selecionados de acordo com suas áreas de estudo (Biol

  13. The alga Bryothamnion seaforthii contains carbohydrates with antinociceptive activity

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    L.A.P. Vieira

    2004-07-01

    opioid receptor antagonist naloxone (2 mg/kg, sc. Moreover, both fractions retained antinociceptive activity in the acetic acid-induced writhing test following heating, a procedure which abolished the hemagglutinating activity of the fraction, presumably due to lectins also present. Finally, both fractions also prolonged the barbiturate-induced sleeping time. These results indicate that carbohydrate molecules present in the PII (26.8% carbohydrate and CF (21% of the alga dried weight obtained from B. seaforthii display pronounced antinociceptive activity which is resistant to heat denaturation and is mediated by an opioid mechanism, as indicated by naloxone inhibition.

  14. Health promotion: Alcohol and drug misuse prevention.

    Science.gov (United States)

    1983-01-01

    Currently, average apparent consumption of alcohol for all persons older than 14 is 10 percent higher than 10 years ago, and is equivalent to about 2.75 gallons of ethanol per person per year. Approximately 10 million adult Americans (i.e., 7 percent of those 18 or older) can be considered problem drinkers. Youthful problem drinkers, aged 14 to 17, are estimated to number more than 3 million and comprise 19 percent of this age group. In addition to the social costs, the economic costs to society as a result of alcohol misuse are substantial--an estimated +49.4 billion in 1977. Ten percent of all deaths in the United States are alcohol-related. Cirrhosis, which is largely attributable to alcohol consumption, ranks among the 10 leading causes of death. Alcohol use also is associated with cancer of the liver, pancreas, esophagus, and mouth. Alcohol consumption during pregnancy is associated with a wide range of possible harmful effects to the fetus--among them decreased birth weight, spontaneous abortion, and physical and mental birth defects. Drug misuse is also an expanding problem. There are some 16 million current marijuana users. The popularity of cocaine continues to increase--over 10 million Americans have tried cocaine at least once and there are an estimated 1 to 2 million current users. Misuse of barbiturates remains a significant problem with at least 1 million persons believed to misuse these drugs and the 30,000 estimated to be addicted to them. In addition, heroin addiction is still considered by many to be the most serious drug problem in the United States. Drug misuse leads to a number of social and health problems. Excessive doses of depressants can result in both physical and psychological dependence. The toll from heroin includes premature death and severe disability, family disruption, and crime committed to maintain the habit. Misuse of hallucinogens often results in emergency room visits. A special problem is the relationship of marijuana to

  15. La estimulación eléctrica de la corteza motora para el tratamiento del dolor central y dolor periférico por desaferentización Electrical stimulation of the motor cortex for the management of central pain and peripheral pain caused by desafferentiation

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    J. V. Pesudo

    2004-09-01

    published on the matter. Currently, its major indications are central pain, mainly thalamic, and trigeminal pain caused by desafferentation. The response to barbiturates without response to opiates, the relative preservation of motor and sensitive pathways and the response to transcranial magnetic stimulation predict a good result. Several methods are used to determine the area that has to be stimulated: SSEP, intraoperatory stimulation, neuronavegation, functional MRI. The stimulation parameters recommended vary according to the author. Its mechanism of action is still not well understood, but the most accepted theories are the activation of areas that modulate pain and the inhibition of the transmission of nociceptive stimuli at the medullar level.

  16. A radioterapia profunda em doses elevadas na epilepsia focal: contrôle clínico e eletrencefalográfico

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    Paulo Pinto Pupo

    1954-06-01

    Full Text Available Radiotherapy in high doses has been used in cases of symptomatic epilepsy with the purpose of to act against the focal epileptic activity, as coadjuvancy to the common medical treatment. Patients with clinical manifestations of epilepsy in whom convulsive foci were demonstrated in the EEG, have been selected; these foci have been recognized as well localized and well circunscribed, and in all them the etiology has been the same (atrophic lesions, according to the clinical and radiological (craniogram, pneumoencephalogram and arteriogram examinations. The purpose of a so homogenous group was to study the results to be obtained in similar conditions. Twenty patients have been selected from a group of forty-eight, because it was possible to obtain a good follow-up for at least three months in each case. In all cases, a medical treatment (barbiturate plus hidantoi-nate has been used in uniform manner, with the purpose of avoiding influence on the judgement of the value of radiotherapy, for it was impossible to interrupt the drug therapy. Radiotherapy has been used in high doses over the epileptic lesion, which had been localized by the EEG. Two different techniques were used; in both 200 kv, 0.5 mm. filter of Cu were employed. Fourteen patients were irradiated in four different areas, of 4 cm. in diameter each one; they received 150 r daily, 2 areas by day, performing an average total of 3,000 r. In the other 6 cases the technique of kinetic convergent radiotherapy was employed, using the Siemens apparatus; each patient received, through a cutaneous area, an average doses of 3,000 r into the focus and 2,000 r in the skin; they received from 100 r to 150 r in the focus daily. Studying the twenty cases individually, there was marked EEG improvement in 4, relative improvement in 8 and no change in 8; there was marked decrease in the number of seizures in 8, relative decrease in 10 and no change in 2; the mental status was markedly improved in 7

  17. Uso de substâncias psicoativas entre universitários de medicina da Universidade Federal do Espírito Santo Psychoactive substance use among Medicine students from Espirito Santo Federal University

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    Denis Soprani Pereira

    2008-01-01

    prevalence of alcohol was founded (86.9%, followed by tobacco (22.0%, solvents (15.5%, amphetamines (10.1%, cannabis (9.5%, hallucinogens (1.8% and barbiturates (0.6%. CONCLUSION: It is necessary to prevent the psychoative substance abuse among college students, introducing curricular disciplines on the theme or specific programs to attend these students.

  18. PECULIARITIES OF TREATMENT OF EPILEPSY AT GIRLS AND WOMEN

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    O. A. Pylaeva

    2015-01-01

    epilepsy and on the kind of seizures, but also provided its influence on the neuroen docrinal status of a woman, as well as on its influence on the reproductive system. With that it should be kept in mind that the reproductive function is very important not only from the point of view of woman’s health, but also from the point of view of her family and social status. If possible, women and men of reproductive age (including adolescents should avoid AED with strong induction of the fermentative system of the liver (all barbiturates, hydantoins, carbamazepine, women should also avoid AED, containing valproic acid. In such cases the priority can be given to new AED, not affecting neuroendocrinal functions and the reproductive system.

  19. In normal rat, intraventricularly administered insulin-like growth factor-1 is rapidly cleared from CSF with limited distribution into brain

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    Gorevic Peter D

    2005-07-01

    Full Text Available Abstract Background Putatively active drugs are often intraventricularly administered to gain direct access to brain and circumvent the blood-brain barrier. A few studies on the normal central nervous system (CNS have shown, however, that the distribution of materials after intraventricular injections is much more limited than presumed and their exit from cerebrospinal fluid (CSF is more rapid than generally believed. In this study, we report the intracranial distribution and the clearance from CSF and adjacent CNS tissue of radiolabeled insulin-like growth factor-1 after injection into one lateral ventricle of the normal rat brain. Methods Under barbiturate anesthesia, 125I-labeled insulin-like growth factor-1 (IGF-1 was injected into one lateral ventricle of normal Sprague-Dawley rats. The subsequent distribution of IGF-1 through the cerebrospinal fluid (CSF system and into brain, cerebral blood vessels, and systemic blood was measured over time by gamma counting and quantitative autoradiography (QAR. Results Within 5 min of infusion, IGF-1 had spread from the infused lateral ventricle into and through the third and fourth ventricles. At this time, 25% of the infused IGF-1 had disappeared from the CSF-brain-meningeal system; the half time of this loss was 12 min. The plasma concentration of cleared IGF-1 was, however, very low from 2 to 9 min and only began to rise markedly after 20 min. This delay between loss and gain plus the lack of radiotracer in the cortical subarachnoid space suggested that much of the IGF-1 was cleared into blood via the cranial and/or spinal nerve roots and their associated lymphatic systems rather than periventricular tissue and arachnoid villi. Less than 10% of the injected radioactivity remained in the CSF-brain system after 180 min. The CSF and arteries and arterioles within the subarachnoid cisterns were labeled with IGF-1 within 10 min. Between 60 and 180 min, most of the radioactivity within the cranium was

  20. Effects of the Epichloёgansuensis endophyte on the disease resistance of drunken horse grass to powdery mildew%内生真菌对醉马草白粉病抗性的影响

    Institute of Scientific and Technical Information of China (English)

    柳莉; 郭长辉; 吕卉; 古丽君; 李春杰

    2015-01-01

    Previous studies have shown that endophytes can increase the resistance of drunken horse grass (Ach-natherum inebrians )to many stresses,such as insects,diseases,waterlogging,drought,salt,and heavy met-als.The aim of this study was to compare the resistance of endophyte-infected (E+ )and endophyte-free (E- ) drunken horse grass to powdery mildew (Blumeria graminis ).Forty pots of drunken horse grass (20 E+plants and 20 E- plants)were grown in a greenhouse.After 2 months,the natural infection rates,the percent-age of diseased leaves,and the disease indexes of powdery mildew in both E+ and E- plants were estimated and recorded.At the same time,the E+ and E- drunken horse grass plants were scored as healthy,slightly dis-eased,or severely diseased based on a disease index.Then,four replicates of E+ and E- plants were randomly selected to measure several physiological indexes;chlorophyll content,activities of superoxide dismutase (SOD)and peroxidase (POD),and the contents of malondialdehyde (MDA)and proline (Pro).Chlorophyll content was measured by acetone extraction,SOD and POD activities were evaluated using nitroblue tetrazoli-um and guaiacol assays,respectively,and MDA and Pro contents were determined using the sulfosalicylic acid and glucosinolate barbituric acid methods,respectively.The disease infection rate,the percentage of diseased leaves,and disease indexes of E- plants were 97%,86%,and 82.49,respectively,significantly higher (P <0.05)than their respective values in E+ plants (48%,60%,and 50.76).The chlorophyll and proline contents and SOD and POD activities were higher in E+ plants than in E- plants,regardless of whether the plants were slightly or severely infected.The MDA content was significantly (P <0.05 )lower in E+ plants than in E-plants.These results provide evidence that endophyte infection can increase the resistance of drunken horse grass to powdery mildew disease.%为研究内生真菌对醉马草白粉病抗性的影响,在温室条件下,

  1. Study of the Therapeutic Effect on Rats Chronic Pelvic Inflammatory Dis-ease of Bullbrier Polysaccharide%金刚藤口服液基于免疫调节对大鼠慢性盆腔炎的治疗作用研究

    Institute of Scientific and Technical Information of China (English)

    邢人鑫

    2014-01-01

    目的:从免疫调节角度研究金刚藤口服液对大鼠慢性盆腔炎的治疗作用。方法:选择未交配的 SPF 级雌性 SD 大鼠60只,随机分为空白组、模型组、阳性(金刚藤胶囊)组、金刚藤口服液低、中、高剂量组。实验第1天,除空白组外,其余各组大鼠用戊巴比妥麻醉,采用双侧输卵管注入30%苯酚胶浆生理盐水溶液,制作大鼠盆腔炎模型。造模后正常组和模型组 ig 给予纯净水,其余各组 ig 给予药物,其中阳性组日给药量为540 mg·kg-1,金刚藤口服液低、中、高剂量组日给药量分别为:15 mg·kg-1、30 mg·kg-1、60 mg·kg-1,每天1次,共 ig 治疗20天。第21天断颈处死动物,ELISA 法测定各实验组大鼠血浆 IgA、IgM 和 IgG 含量;剖取子宫,称重后做病理形态分析。结果:与正常组比较,模型组大鼠子宫重量系数[(11.7±1.92) mg·g-1]极显著增大(P<0.01),血浆IgA[(27.99±5.49)μg·mL-1]、IgM[(21.94±1.98)μg·mL-1]和 IgG[(4.85±1.97)μg·mL-1]含量均有极显著减少(P<0.01);子宫炎症性病变显著加重;与模型组比较,金刚藤口服液组可显著减小大鼠子宫重量系数(P<0.05),增加血浆 IgA、IgM 和 IgG 含量(P<0.05),且能减轻子宫炎症性病变。结论:金刚藤口服液可通过调节大鼠血浆免疫球蛋白浓度而对慢性盆腔炎产生治疗作用。%Objective: To study the therapeutic effect on rat chronic pelvic inflammatory disease of bullbrier polysaccharide. Methods: unmated SPF 60 female SD rats were randomly divided into control group, model group, positive group (Bullbrier capsules) group, bullbrier polysaccharide low, medium and high dose groups. On the 1d of experiment, except the blank group, the rest of the rats were anesthetized with amyl barbiturate, phenol 30% slurry injection of saline solution was injected from bilateral tubal to make rats pelvic inflammatory disease

  2. Changes of dynamical balance of free radicals induced by levodopa in rat glia-containing mesencephalic culture fluid

    Institute of Scientific and Technical Information of China (English)

    Wenxia Li; Shenggang Sun; Jingru Wang; Baoliang Sun; Yanbo Zhang

    2006-01-01

    content with thiol-barbituric acid method.MAIN OUTCOME MEASURES: GSH and MDA contents, GSH-Px and SOD activities in the glia-containing mesencephalic culture fluid at 4, 24, 48 and 72 hours after L-DOPA of different concentrations were added. RESULTS: In the glia-containing mesencephalic culture fluid after 100 μmol/L L-DOPA was added for 24, 48 and 72 hours, the GSH contents were lower than those in the blank control group [(174.14±39.28), (161.55± 40.79), (144.97±57.59) mg/L; (220.66±32.61), (221.10±32.98), (220.43±31.98) mg/L, P < 0.05]; The GSH-Px activities were lower than those in the blank control group [(4.03±1.05), (3.99±1.12), (3.47±1.00) μmol/L; (5.45±1.14), (5.69±1.21), (5.49±1.28) μmol/L, P < 0.05]; The SOD activities were also lower than those in the blank control group [(42.02±5.08), (39.38±5.34), (38.87±5.75) kNU/L; (51.35±8.87), (51.78±8.96), (50.99± 9.09) kNU/L, P < 0.05]; Whereas the MDA contents were higher than those in the blank control group [(3.51 ± 1.05), (3.99±1.03), (4.45±1.58) μmol/L; (2.09±1.13), (2.18±1.29), (2.01±1.05) μ mol/L, P< 0.05]. In the glia-containing mesencephalic culture fluid after 100 μmol/L L-DOPA was added for 4, 24, 48 and 72 hours, the GSH contents were (172.27±26.07), 140.15±61.44), (137.30±50.87), (121.09±66.07) mg/L, the GSH-Px activities were (3.89±1.20), (3.56±1.23), (3.38±1.18), (3.01±1.09) μmol/L, the SOD activities were (38.18±6.75),(35.23±7.85), (4.59±1.24), (31.42±7.01) kNU/L, which were all lower than those in the blank control group (P < 0.05-0.01); The MDA contents were (3.65±0.86), (3.87±1.14), (4.59±1.24), (4.79±1.32) μmol/L, which were higher than those in the blank control group (P < 0.05-0.01). In the glia-containing mesencephalic culture fluid added by 50 μmol/L L-DOPA, the GSH and MDA contents, GSH-Px and SOD activities at each time point were all close to those in the blank control group (P> 0.05).CONCLUSTON: L-DOPA of certain concentration

  3. Anestesia venosa total em regime de infusão alvo-controlada: uma análise evolutiva Anestesia venosa total en régimen de infusión objeto controlada: un análisis evolutivo Total intravenous anesthesia as a target-controlled infusion: an evolutive analysis

    Directory of Open Access Journals (Sweden)

    Fernando Squeff Nora

    2008-04-01

    ón objeto controlada (IOC. El primer modelo farmacocinético descrito para uso en IOC, fue descrito por Schwilden en 1981. Quedó demostrado a partir de entonces, que era posible mantener la concentración plasmática deseada de un fármaco utilizando bomba de infusión por computador. CONTENIDO: Este artigo quiso dejar sentadas las bases teóricas de la IOC, presentar una propuesta de desarrollo de un vocabulario común en IOC todavía no publicado en Brasil y hacer un análisis crítico de los aspectos actuales de la IOC en el mundo y en Brasil. CONCLUSIONES: La llegada de nuevas bombas de infusión dotadas de los modelos farmacocinéticos del remifentanil, sufentanil y propofol inaugura otro capítulo de la AVT y coloca a Brasil a tono con la tendencia mundial en IOC. Esos sistemas facilitarán la IOC de hipnóticos y opioides concomitantemente. La conclusión más importante, sin embargo, se refiere a la economía en la medida en que los fármacos utilizados en esas bombas no quedarán restrictos a solamente una empresa farmacéutica, como por ejemplo lo que ocurrió con el propofol. Hoy ya disponemos de equipos para la utilización de propofol y opioides en IOC, que aceptan cualquier presentación farmacéutica con la ventaja de poder alterar la concentración del fármaco en la jeringuilla de acuerdo con la dilución que se desee.BACKGROUND AND DOBJECTIVES: Total intravenous anesthesia (TIVA has seen several developments since it was first used. Since the synthesis of the first intravenous anesthetics, with the introduction of barbiturates (1921 and thiopental (1934, TIVA has evolved until the development of TIVA with target-controlled infusion pumps (TCI. The first pharmacokinetic model for the use of TCI was described by Schwilden in 1981. From that moment on, it was demonstrated that it is possible to maintain the desired plasma concentration of a drug using an infusion pump managed by a computer. CONTENTS: The objective of this report was to describe the

  4. γ-氨基丁酸A受体功能性结构与抑郁、焦虑及癫痫相关的研究%Functional structure of γ-aminobutyric acid A receptor and depression, anxiety and epilepsy-related study

    Institute of Scientific and Technical Information of China (English)

    张瑞华; 李丽琴; 王惠芳; 李艳军

    2005-01-01

    OBJECTIVE: Because A type γ-aminobutyric acid (GABAA) receptor is widely used in clinical medicine, the receptor related drugs and relationship between structures and functions of GABAA receptor have been discussed according to the study at home and abroad.DATA SOURCES: Literatures related to GABAA receptor were searched from Medline and Elesiver science database by a computer, key word is "GABAA or GABAA benzodiazepine", and the language was restricted in English. And simultaneously, they were searched from CNKI database with the word-GABAAin Chinese. Time of search is January 1994 to August 2004.STUDY SELECTION: First trial for data, literatures related to GABAA receptor structures and pharmacological functions was selected, and then looking for full text. Functions or activities dissertated in literatures without relation to central nervous system and clinical therapy were excluded.DATA EXTRACTION: Thirty-six pieces of literatures that are related to GABAA receptor structures and functions were found, among which 24 pieces were excluded, 16 pieces were repeated and 8 pieces were Meta analysis study.DATA SYNTHESIS:There are 12 pieces of literatures measuring up in which receptor structures, functions and pharmacological functions were studied. Four kinds of drugs including sedative-diazepam, inhibitor-barbiturate, spasmogen-picxition and neuroactivesteoid act on this receptor.CONCLUSION: To study thoroughly the function of GABAA receptor subunits could provide techniques and approaches for screening the receptor subunit related anti-epilepsy drugs%目的:鉴于γ-氨基丁酸A受体在临床医学上的广泛应用,从国内外对其受体研究的现状出发,分析其受体的结构与功能的关系以及与其相互作用的有关药物进行讨论.资料来源:应用计算机分别在Medline和Elesiver science数据库检索与γ-氨基丁酸A受体相关的文献,检索词"GABAA0r GABAA benzadizene",并限定文献语种为英文.同时在CNKI数据库中

  5. Sedação e analgesia em neonatologia Sedación y analgesia en neonatología Sedation and analgesia in neonatology

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    Yerkes Pereira e Silva

    2007-10-01

    dolor en Unidades de Terapia Intensiva Neonatal y también para hacer el ambiente más humanizado y menos estresante para los pacientes y sus familiares. El tratamiento del dolor en el recién nacido consiste en medidas no farmacológicas (succión no nutritiva, glicosis y farmacológicas (analgésicos no-opioides, opioides y anestésicos locales. La sedación en recién nacidos es producida por fármacos que actúan disminuyendo la actividad, la ansiedad y la agitación del paciente, pudiendo conllevar a la amnesia de eventos dolorosos o no dolorosos. La sedación puede ser hecha a través del uso de hidrato de cloral, barbitúricos, propofol y benzodiazepínicos. CONCLUSIONES: La prevención del dolor y la indicación de analgesia deben ser individualizadas y siempre consideradas en todos los recién nacidos portadores de enfermedades potencialmente dolorosas y/o sometidos a procedimientos invasivos, quirúrgicos o no.BACKGROUND AND OBJECTIVES: The study of pain in neonatology is important because pain and stress mean suffering and discomfort for newborns and, despite it, very little has been done to minimize them. In this revision we discuss: prevention of pain, non-pharmacological and pharmacological treatment, and sedation in newborns. CONTENTS: Several non-pharmacological measures can be taken to prevent pain in Neonatal Intensive Care Units, and to humanize and reduce the stress on the environment for patients and their families. Pain treatment in the newborn consists of non-pharmacological (non-nutritive suckling, glucose and pharmacological (non-opioid analgesics, opioids, and local anesthetics measures. Sedation in the newborn is achieved with drugs that decrease activity, anxiety, and agitation of the patient, and that could lead to amnesia of painful and non-painful events. Sedation can be accomplished with chloral hydrate, barbiturates, propofol, and benzodiazepines. CONCLUSIONS: Prevention of pain and the indication of analgesia should be individualized

  6. Recorrência da Crise Convulsiva após Terapia Anticonvulsivante com Sulfato de Magnésio em Pacientes com Eclâmpsia Recurrence of Seizures after Anticonvulsant Therapy with Magnesium Sulfate in Patients with Eclampsia

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    Melania Maria Ramos de Amorim

    2000-04-01

    . Patients and Methods: a prospective cohort study was conducted, enrolling all cases of eclampsia managed at IMIP between January/1995 and June/1998. Magnesium sulfate and oxygen therapy were administered routinely and interruption of pregnancy was performed after maternal stabilization. The frequency of recurrence of seizures and its association with maternal complications were determined. chi² test for association was used at a 5% level of significance. Results: twelve cases presented recurrence of convulsions after magnesium sulfate (10% and all received a repeated dose. In four of them convulsions persisted and they received intravenous diazepam. After diazepam, one patient still had seizures, with unsuccessful administration of phenytoin and therefore barbituric coma was induced (thionembutal. This patient had a CT-scan with evidence of intracerebral hemorrhage. Maternal complications were significantly more frequent in the group with recurrence: coma (16.7% versus 0.95, acidosis (50% versus 2.9%, pulmonary edema (16.7% versus 2.9%, cerebral hemorrhage (16.7% versus 0% and acute renal failure (16.7% versus 1.9%. Three cases of maternal death occurred in patients with recurrence (25% versus 2 cases in patients without recurrence (1.9%. Conclusions: rate of recurrence after anticonvulsant therapy with magnesium sulfate is low (10% but it is associated with increased maternal morbidity and mortality. These cases must be managed in an intensive care unit and submitted to routine CT-scan because cerebral hemorrhage can be the cause of recurrence.

  7. Vladimir Prelog i Zavod za organsku kemiju

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    Jakopčić, K.

    2007-03-01

    -operation from the small but prosperous pharmaceutical company "Kaštel" in Zagreb. On behalf of the agreement, Prelog and his department obtained funds to fit up the laboratory and to start very prosperous research in the synthesis and studies of pharmaceutically interesting compounds. With his assistants, students and other collaborators, Prelog started research of cinchona bark alkaloids, preferentially oriented to the synthesis of quinine. For example, Prelog's method of double intramolecular alkylation to synthetize the quinuclidine moiety of quinine was patented by "Kaštel". With R. Seiwerth he developed the first useful synthesis of adamantane. Prelog's group started research in the field of sulphonamides and commercial success of "Streptazole" stimulated the development of the research laboratories within "Kaštel". The collaboration in the research continued in fields of other chemotherapeutics, analeptics, spasmolitics, barbiturates etc. Within the period 1935-1941, Prelog published 48 scientific papers and 8 patents. In less than seven years, his results enormously influenced the entire organic chemistry in Zagreb till nowadays. Under the confused and uncertain circumstances caused by the beginning of World War II, Prelog left Zagreb in 1941 and continued his extraordinary scientific career at the ETH in Zürich.During the war (1942-1945 the tuition and the Department were run by Dr. Rativoj Seiwerth, former collaborator and first assistant to V. Prelog. In almost unbelievable conditions, the young assistant, then assistant professor (since January 1943, R. Seiwerth fully succeeded in continuing most activities founded by Professor Prelog. After the war (1945, R. Seiwerth was forced to resign. Nevertheless, soon after R. Seiwerth continued his research work, firstly in the Institute for Industrial Research in Zagreb (1946-1952, and later in the Research Institute of "Pliva" in Zagreb. He retired in 1980.In post-war conditions (1945/46, the activity of the Technical

  8. Use of psychoactive drugs and related falls among older people living in a community in Brazil Uso de medicamentos psicoativos e seu relacionamento com quedas entre idosos

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    Flávio Chaimowicz

    2000-12-01

    Full Text Available INTRODUCTION: Population aging in Brazil has increased the prevalence of neurodegenerative diseases (Parkinson's and Alzheimer's disease and affective disorders (anxiety, depression, all common in old age. A retrospective study was carried out with the purpose of ascertaining if there is an association between falls and psychoactive medication use among older residents of a community in Brazil. METHODS: All residents aged 65+ (n=161 of one neighborhood of Campo Belo, Brazil (population of 48,000 were evaluated regarding the use of psychoactive drugs and the occurrence of falls in the 12 months preceding the study. Vision and hearing screenings were also performed. RESULTS: From the study population, 9.3% were taking prolonged half-life benzodiazepines, 4.4% anticonvulsants (mostly barbiturates, 2.5% antidepressants (all cyclics and 8.1% alpha-methyldopa. No subject reported use of hypnotics, neuroleptics or drugs to treat Alzheimer's or Parkinson's diseases (except biperiden. As a whole, drugs that increase the risk of falls were used by 1/5 of this population. In the 12-month period preceding the study, 27 residents (16.8% experienced falls and, of those, 4 (14.8% had fracture(s. There was an independent association between psychoactive drug use and falls when variables such as age, gender, vision and hearing were controlled (p=0.02. CONCLUSIONS: Although the population of this neighborhood must be considered young (only 4% are 65 years old or more, there are already problems related to the use of psychoactive drugs among people. Prescribed anxiolytics, anticonvulsants, antidepressants and antihypertensives are not appropriate for this age group and their use is associated with falls.INTRODUÇÃO: O envelhecimento populacional no Brasil tem aumentado a prevalência de doenças neurodegenerativas (Parkinson, Alzheimer e psiquiátricas (depressão, ansiedade, comuns em idosos. Realizou-se estudo retrospectivo com o objetivo de determinar se h

  9. [Early achievements of the Danish pharmaceutical industry-7].

    Science.gov (United States)

    Grevsen, Jørgen V; Kirkegaard, Hanne; Kruse, Edith; Kruse, Poul R

    2014-01-01

    of Health was, however, at that time of the opinion that there were no serious problems with organotherapeutics from those companies marketing such products. It requires studies in the unprinted journals of the Ministry of Health and the National Board of Health to find the background for and the causes of the request from the Ministry at this point concerning the control of the organotherapeutic products of the pharmaceutical industry. Neither were GEA's barbiturates innovative products. The "Gad Andresen Case" is interesting for two reasons. Firstly, it illustrates that the development of generics at this stage could not always take place exclusively in a pharmaceutical-chemical laboratory, but also required a certain minimum of clinical trials including human beings. Secondly, it shows that the industrial products had now slowly, but surely gained market shares and displaced the pharmacy-produced medicinal products to such an extent that it did not only worry the pharmacy owners and their trade orga- nization. Now this concern had also resulted in a counteract so that the pharmacies in the manufacture of their products had to copy the industrial products, however, in certain cases with a dubious result. Gealgica tablets and especially their content of fenacetine is not only a model example of how the opinion of the positive and negative properties of a medicinal product changes over time. It also shows how long time could pass before the health authorities took measures against a substance with problematic side effects in spite of the fact that less damaging substances had been available for a long time, in this case paracetamol. Medicinal products containing fenacetine were on the market for almost 100 years. On the contrary meprobamat is a model example of a drug substance where the opinion of its positive and negative properties changed essentially over a relatively short period. In spite of this it remained on the market for a little less than 40 years

  10. Consumo de substâncias psicoativas por adolescentes escolares de Ribeirão Preto, SP (Brasil. I - Prevalência do consumo por sexo, idade e tipo de substância The consumption of psychoactive substances by adolescents in schools in an urban area of Southeastern region of Brazil. I - Prevalence by sex, age and kind of substance

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    Gilson M. Muza

    1997-02-01

    pelos meninos como pelas meninas, muitas vezes em idades bem precoces.INTRODUCTION: Concern over the consumption of psychoactive substances by teenagers has given rise to a great wordwide effort to produce information about this phenomenon. This study set out to investigate the prevalence of consumption of legal and illegal psychoactive substances, its distribution by age, sex and age at first experience of them, among teenage pupils in county, Ribeirão Preto, SP, Southeastern Brazil. MATERIAL AND METHOD: A self-applicable questionnaire duly adapted and submitted to a reliability test was applied to a proportional sample of 1,025 teenagers enrolled in 8th, 9th, 10th and 11th grads at public and private city schools. The questionnaire contained questions about the use of ten classes of psychoactive substances, demographic questions and validation information, as well as questions about the perception and intrinsic behavior related to drug consumption. RESULTS: The sample of 88.9% had consumed alcoholic beverages sometime in their lives, 37.7% had used tobacco, 31.1% solvents, 10.5% medicines, 6.8% marihuana, 2.7% cocaine, 1.6% hallucinogens, and 0.3% of the sample had consumed some opiate substance. The rates of consumption increased with age for all substances; however, the use of tobacco and of illegal substances was less intense during the later years of adolescence. As to sex distribution, boys consumed more than girls, except for medicines, with girls consuming barbiturates, amphetamines and tranquilizers in proportions similar to or higher than those observed among boys. Age at first experience showed that access to psychoactive substances occurred at very early ages. CONCLUSIONS: Experimenting with psychoactive substances, whether legal or illegal, is a frequent phenomenon during adolescence, both among boys and girls, often at very early ages.

  11. Prevalência do consumo de drogas na FEBEM, Porto Alegre Drug use prevalence at FEBEM, Porto Alegre

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    Maristela Ferigolo

    2004-03-01

    já terem utilizado drogas ilícitas.OBJECTIVE: This study aimed to determine the prevalence of drug use among institutionalized children and adolescents; to assess the degree of associated use of illicit drugs with alcohol and tobacco; and to determine which is the gateway drug to illicit drug use. METHODS: A cross-sectional study was carried out in the Fundação Estadual do Bem-Estar do Menor, in Porto Alegre (FEBEM Southern Brazil. A questionnaire developed by the World Health Organization to determine prevalence off drug use was answered anonymously by a population of literate minors who were in FEBEM because of delinquency or due to social risk. The analysis aimed to describe the frequency of use of each drug and relate it to gender, age of beginning, and reason of institutionalization. RESULTS: A total of 382 participants answered the questionnaire. The substances most frequently used on an experimental basis were: alcohol (81,3%, tobacco (76,8%, marijuana (69,2%, cocaine (54,6%, inhalants (49,2%, anxiolytic drugs (13,4%, hallucinogens (8,4%, amphetamines (6,5% and barbiturates (2,4%. Overall, around 80% of the respondents reported having used some illicit drug at least once in the past. Licit drugs, like alcohol and tobacco, were used mainly by males, while medicines were used mostly by females. Adolescents with delinquency records showed a significantly higher frequency of alcohol, marijuana, cocaine, and solvent use. The mean age of beginning was under 12 years for alcohol and tobacco use, under 13 years for marijuana and inhalants, and under 14 years for cocaine. Concomitant use of illicit and licit drugs was found to be high in this population. CONCLUSIONS: A high prevalence of precocious drug use was found among institutionalized children and adolescent, with alcohol and tobacco being used earlier than illicit drugs. Delinquent males were more likely to have used illicit drugs.

  12. Erythrogram, oxidative stress and mineral interaction in naturally infected lambs supplemented with different forms of oral ironEritrograma, estresse oxidativo e interação mineral em cordeiros naturalmente infectados por parasitas gastrintestinais suplementados com diferentes formas de ferro oral

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    Marta Lizandra Rêgo Leal

    2012-05-01

    Full Text Available The present study aimed to assess the oxidative profile, erythrogram and mineral interaction in lambs with anemia due to worm infection supplemented with different forms of oral iron. It was used 27 lambs, 6 to 8 month old, naturally infected by Haemonchus contortus, which showed packed cell volume between 16 and 18%. The animals were divided in three groups: Control Group (GC n=9, Ferrous Sulphate Group (G2 n=9 and Ferric Sulphate Group (G3 n=9. The animals of G2 received 1 g of ferrous sulphate (Fe+2 orally daily, equivalent to 200 milligram of iron, the animals of G3 received 1 g of ferric sulphate (Fe+3 orally daily, or equivalent to 200 milligram of iron, whereas the GC received no treatment. The samples were taked on day 0, 7, 14, 21 and 28 of the experiment, and during four days two animals of each group were kept in metabolic cages to measure the faecal minerals excretion. There was no difference among the groups about serum iron values and parameters of red blood cells. The serum copper and zinc values were lower in the G2 and G3 on days 21 and 28 of the experiment, whereas the faecal copper, iron and zinc excretion was higher in the same groups. The superoxide dismutase (SOD levels were lower in the G2 and G3 on day 28 whereas the levels of non-protein thiol groups (NPTH showed a decrease on days 21 and 28. In relation to reactive species thio-barbituric acid (TBARS, there was an increase on day 28 in the G2 and G3. Based on these results, it was concluded that the oral supplementation with 200 mg of iron, irrespective of its form, ferrous or ferric, does not increase the erythrocyte response in lambs. As well as, it has antagonist action on copper and zinc, reducing its serum concentrations and increasing the faecal excretion of these minerals. Moreover, the decrease of the serum copper and zinc concentrations causes a decrease in activity of superoxide dismutase, causing an oxidative stress situation.O presente estudo teve por

  13. Antidepressant effect of lentinan in chronically stressed mice and its possible mechanism%香菇多糖对慢性应激抑郁模型小鼠的抗抑郁作用及可能机制研究

    Institute of Scientific and Technical Information of China (English)

    马倩; 蒲燕; 袁文清; 吕路线; 杜志敏; 李万里

    2015-01-01

    model of chronic stress behavior,serum TNF-αand IL-6 content.To investigate the mechanism of antidepressant LNT.Methods:Healthy adult mice were 50,male,body weight (20 ±2) g,SPF grade,based on 1% sucrose water partial addicted degrees and were randomly divided into four groups,namely,normal control group (Normal controls,NG),model in the control group ( Model control,MG) ,LNT dose group ( L-LNT,2.5 mg/kg;H-LNT,5.0 mg/kg).Before the experiment began modeling 1 h daily oral administration,continuous administration 28 d, each experimental group administered according 1.0 ml/100 g weight.Application chronic unpredictable mild stress model of depression produced,and make improvements.Normal control group,not to stimulate,food and water properly.Model group and the experimental intervention group with the lone support,fasting,water deprivation (24 h),and accept the unpredictable stressors,the 28 d of the experiment,the animals were randomized to receive daily each only one stimulus, within five days after making the choreography the stimulus program was not repeated and unpredictable.Animals were observed daily behavior change,with a strange environment to start feeding feeding experimentally observed incubation period,forced swim stress test record swim immobility time,enzyme-linked immunosorbent assay of serum TNF-α,IL-6 content ,NBT assay of total SOD activity,thio-barbituric acid (thiobarbituric acid,TBA) MDA content assay,immune proteins mark (Western blot) to detect 5-HT1A receptor expression levels.Results:MG mice in an unfamiliar environment, feeding latency was significantly prolonged after giving LNT intervention can shorten lead to chronic stress in mice feeding latency in an unfamiliar environment,prolonged chronic stress leads to significantly reduce the stress in mice swimming in water immobility time extension,and 5-HT1A receptor expression enhancing,LNT intervention group increased SOD,MDA content decreased serum TNF-αand IL-6 was significantly reduced

  14. A serendipidade na medicina e na anestesiologia A serendipidade en la medicina y en la anestesiologia Serendipity in medicine and anesthesiology

    Directory of Open Access Journals (Sweden)

    Nilton Bezerra do Vale

    2005-04-01

    biología, anatomía, física, química, fisiología, farmacología, astronomía, arqueología y... mucha suerte. CONCLUSIONES: Aunque accidentes en la pesquisa y en la sala de operación sean lamentables, hay aquéllos que acontecen y, a veces, pueden llevar a avances espectaculares, como tratamientos heroicos y hasta Premios Nobel. Mantener la mente abierta es un trazo común a aquellos que desean contar con la gran suerte, como afirmaba el físico americano Henry (1842: "Las semillas del hallazgo flotan constantemente alrededor nuestro, pero apenas lanzan raíces en las mentes bien preparadas para recibirlas".BACKGROUND AND OBJECTIVES: This study has evaluated more than a hundred of the most fortunate couplings of a brilliant mind with fortunate luck (serendipity, through the re-reading of most relevant histories on science-related (n = 46 and anesthesiology-related (n = 16 inventions and discoveries. CONTENTS: This educational article encourages anesthesiologists to appreciate events related to scientific inventions and discoveries, showing that serendipity is possible, provided it is expected. Each discovery or invention includes history, references and scientific or anecdotal explanation. In addition to traditional discoveries, such as wine, gravity, photograph, Velcro, airbag, etc., there are other Medicine-related (microscope, X-rays, vaccine, penicillin, insulin, laser, Paps smear, etc. and Anesthesiology-related (isometry, gloves, N2O, ether, barbiturates, benzodiazepines, blood patch, etc. discoveries. Creativity and serendipity may act as cornerstones for clinical and basic research of pioneer inventions for medical and anesthesiologic advances. In fact, topics related to biology, anatomy, physics, chemistry, physiology, pharmacology, astronomy and archeology should be master and … lots of luck. CONCLUSIONS: Although research and operating room accidents are regrettable, some of them happen and may sometimes lead to spectacular advances, such as heroic

  15. 中等强度运动对大鼠DDT累积代谢、肝脏应激及结构影响%The Changes of DDT Accumulation Metabolism, Liver Oxidative Stress and Structure Intervened by Moderate Intensity Exercise

    Institute of Scientific and Technical Information of China (English)

    李可峰; 胡一平; 董贵俊; 朱晓华; 李丽; 周兴忠; 王玉站; 郑淑倩; 葛新发; 韩勇

    2015-01-01

    Objective :To reveal the influence of aerobic exercise on DDT accumulation metabolic rules ,changes of oxidative stress and structure in liver induced by DDT under the background of national fitness .Methods :90 male Wistar rats were randomly assigned into control group (CON ) ,placebo group (PG ) ,aerobic exercise group (AG ) ,CON with DDT group (CDG ) and aerobic exercise with DDT group (ADG) .CDG and ADG were fed with DDT solution ac‐cording to 40 mg/kg body weight for 2 weeks ;ADG and AG were exercised with 18 m/min speed movement for 30 min every day .During 15d ,30d and 45d after exercise ,DDT concen‐tration was investigated by gas chromatography after grinding and freeze‐drying and the distri‐bution of DDT in different organizations were studied ;the activities of SOD ,GSH‐Px and CAT were evaluated by xanthine oxidase method ,enzyme kinetic method and visible light method re‐spectively ,the MDA content was determined with glucosinolates barbituric acid colorimetric method .The live samples were stained with HE for liver biopsy ,and uranium acetate ,citrate for liver ultrastructure ,then observed and took photos with DP70 digital microscope imaging system and Tecnai Spirit transmission electron microscope and imaging system (120 kv ) .Re‐sults :DDT concentrations decreased gradually in CDG liver ,whereas it rose first and then fell in ADG liver .DDT concentrations in ADG liver were significantly higher than that in CDG from 15d to 30d (P< 0 .01) ,and lower than the CDG at 45d (P< 0 .05) .Compared with the CDG ,DDT concentrations in ADG heart showed a significant rise at 15d and 45d ,and a significant decline at 30d .DDT concentrations in CDG skeletal muscle decreased gradually but rose in ADG .From 15d to 30d ,DDT concentrations in ADG blood was significantly lower than that in CDG ( P< 0 .01 ) .DDT concentrations in CDG feces declined gradually but were relatively stable in ADG feces .Aerobic exercise can promote SOD activity in ADG from 15d

  16. Prevention of suicide and attempted suicide in Denmark. Epidemiological studies of suicide and intervention studies in selected risk groups.

    Science.gov (United States)

    Nordentoft, Merete

    2007-11-01

    The suicide rates in Denmark have been declining during the last two decades. The decline was relatively larger among women than among men. All age groups experienced a decline except the very young with stable rates and the very old with increasing rates. The Universal, Selective, Indicated (USI) model recommended by Institute of Medicine was used as a framework for the thesis. Universal preventive interventions are directed toward the entire population; selective interventions are directed toward individuals who are at greater risk for suicidal behaviour; and indicated preventions are targeted at individuals who have already begun self-destructive behaviour. At the universal level, a review was carried out to highlight the association between availability of methods for suicide and suicide rate. There were mostly studies of firearms, and the conclusion of the review was that there was clear indication of restricted access to lethal means was associated with decline in suicide with that specific method, and in many cases also with overall suicide mortality. Restricting access is especially important for methods with high case fatality rate. Our own study indicated a beneficial effect on suicide rates of restrictions in access to barbiturates, dextropropoxyphen, domestic gas and car exhaust with high content of carbon monoxide. Although a range of other factors in the society might also be of importance, it was concluded that restrictions in access to dangerous means for suicide were likely to play an important role in reducing suicide rates in Denmark, especially for women. At the selective level, there are several important risk groups such as psychiatric patients, persons with alcohol and drug abuse, persons with newly diagnosed severe physical illness, all who previously attempted suicide, and groups of homeless, institutionalized, prisoners and other socially excluded persons. The thesis focused on homeless persons and psychiatric patients, especially patients