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Abstract  

In order to study “in vivo” the brain specific receptor sites of benzodiazepines, a method for carbon-11 labelling of diazepam and flunitrazepam without irradiation risk to personnel is described. 70 mCi (max. 140 mCi) of injectable labelled product, chemically and radiochemically pure, are obtained in 45 minutes with a specific activity of 810 Ci/m mole.

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Abstract  

In the present study, we report on the thermal properties of a series of benzodiazepines. The heat of fusion varied between approximately 25 and 40 kJ mol–1, except for oxazepam and lorazepam where dimerization in the solid state increased the heat of fusion to 78.54(±0.37) and 77.03 (±0.84)kJ mol–1, respectively. Heating alprazolam at a low rate (0.5 K min–1) showed that polymorphs I and II are an enantiotropic pair with a solid-solid transition at 481.4 K It was shown that all benzodiazepines could be transformed to the glassy state by cooling fused samples, irrespective of the cooling rate. The size of the relaxation endotherm accompanying the glass transition increased by heating the glassy drugs at a higher rate through T g or by cooling the fused samples at a slower rate. The time dependence of the glass to liquid transition can be described to a good approximation as a first order transformation. The Gordon-Taylor equation was used to predict T g of a binary mixture of temazepam, diazepam or prazepam with polyHEMA. It was shown that the predictability was acceptable as long as the drug concentration was below 10%w/w; at higher concentration, specific drug-polymer interactions causing changes in free volume of the system could not be ignored.

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Anew sensitive chromogenic TLC spray reagent is described for the detection of the benzodiazepine drug diazepam in biological tissues, blood, urine, vomit, and tablets. Diazepam standard and extracts of these samples in alkaline chloroform-isopropyl alcohol 9:1 were applied to TLC plates coated with 0.25 mm layers of silica gel G. Plates were developed with chloroform-methanol 9:1 as mobile phase, dried, and then sprayed with 5% sodium hydroxide solution followed by 1% m -dinitrobenzene in dimethyl sulfoxide (DMSO). Violet bands were obtained for diazepam but other benzodiazepines, for example oxazepam, nitrazepan, lorazepam, chlordiazepoxide, and flurazepam, did not react. The sensitivity of this reagent for diazepam is approximately 5 μg.

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Orvosi Hetilap
Authors: József Janszky, Beáta Bóné, Réka Horváth, Zsófia Sütő, László Szapáry, Vera Juhos, Sámuel Komoly, and Norbert Kovács

Absztrakt:

A status epilepticus a második leggyakoribb, sürgősségi kezelést igénylő neurológiai állapot. Halálozása 15–25%. A „time is brain” elve a status epilepticus kezelésére is igaz: minél korábban kezdjük a megfelelő kezelést, annál nagyobb valószínűséggel tudjuk megállítani a progressziót. Magas szintű evidenciákon alapuló kezelési protokollal a status epilepticus progressziója az esetek 75–90%-ában megelőzhető, az indukált kóma és a halálos kimenetel elkerülhető. A status epilepticus kezelése akkor a legsikeresebb, ha már a korai szakban megkezdjük a parenteralis benzodiazepinterápiát: im. midazolám (0,2 mg/tskg, max. 10 mg). Szabad véna esetén lehet vénásan is adni a benzodiazepint (10 mg diazepám iv). Ha az első benzodiazepinbolusra nem reagál a status epilepticus, állandósult (benzodiazepinrefrakter) status epilepticusról beszélünk. Ilyenkor a benzodiazepin ismétlésével párhuzamosan nem benzodiazepin típusú, gyorsan ható vénás antiepileptikumot is adni kell: iv. valproát (40 mg/kg, max. 3000 mg, 10 perc alatt) vagy levetiracetám (60 mg/kg, max. 4500 mg, 10 perc alatt) javasolt. Az 1 órán túl is tartó, sem benzodiazepinre, sem antiepileptikumra nem reagáló, refrakter status epilepticust neurointenzív osztályon, teljes narcosissal (indukált kómával) kell kezelni. Az indukált kómát gyors hatású anesztetikummal lehet elérni, elsősorban propofol–midazolám kombinációval. Orv Hetil. 2020; 161(42): 1779–1786.

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2005 Benzodiazepine use, cognitive impairment, and cognitive-behavioral therapy for anxiety disorders: Issues in the treatment of a patient in need Journal of Clinical Psychiatry 66

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347 353 Berridge KC, Pecina S: Benzodiazepines, appetite, and taste palatability. Neurosci. Biobehav. Rev. 19, 121–131 (1995) Pecina S

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F Cornet AF Cohen JMA van Gerven 2003 Biomarkers for the effects of benzodiazepines in healthy

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://drogfokuszpont.hu/eves-jelentesek [accessed: September 22, 2018]. [Hungarian] 6 Ashton H. Benzodiazepine withdrawal: outcome in 50 patients. Br J Addict. 1987; 82: 665–671. 7 Paksi

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. 1997 10 1 8 Begg, D. P., Hallam, K. T., Norman, T. R. (2005) Attenuation of benzodiazepine withdrawal anxiety in the rat

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