Bu çalışmanın amacı, sıçanlarda pentilentetrazol (PTZ) ile oluşturulan nöbetlerde diazepamın antikonvulzif etkinliğinde nitrik oksit sentaz (NOS) ve beyin kaynaklı nörotrofik faktör (BDNF) üzerine etkisini araştırmaktır. Çalışmada 24 adet erkek Wistar Albino sıçan kullanılmıştır. Sıçanlar kontrol grubu, salin (1 mL kg-1) + PTZ, diazepam (0,5 mg PTZ (2 kg-1)+PTZ grubu olarak 4 gruba ayrılmıştır ...

Diazepam is a benzodiazepine derivative with anxyolitic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, antitremor, and amnestic activity. It is metabolized in the liver by the cytochrome P (CYP) 450 enzyme system. Diazepam is N-demethylated by CYP3A4 and CYP2C19 to the active metabolite N-desmethyldiazepam, and is hydroxylated by CYP3A4 to the active metabolite temazepam. N-desm...

The currently recommended treatment for metronidazole toxicosis is drug discontinuation and supportive therapy. Reported recovery times are 1-2 weeks. The records of 21 dogs with metronidazole toxicosis were retrospectively analyzed to determine whether diazepam improved recovery. The dosage and duration of metronidazole therapy and the response and recovery times of 13 dogs treated with diazep...

1. After intravenous administration to 19 subjects, aged 18-95 years, plasma diazepam concentrations were measured over 160 h. Plasma protein binding of diazepam was also measured in each subject. 2. The terminal plasma half-life of diazepam ranged from 15.0 to 125 h and was positively correlated with age (r = 0.797). Total plasma diazepam clearance was not correlated with age (r = -0.017). 3. ...

BACKGROUND/AIM Diazepam is a benzodiazepine anxyolitic. Metabolism of diazepam takes place in liver which generates pharmacologically active metabolites N-desmethyldiazepam, temazepam and oxazepam. The aim of this study was to develop and validate the method of liquid chromatographymass spectrometry (LC-MS) for separation and determination of diazepam and its active metabolites in the serum of ...

Abstract Objective: This study evaluates the role of oral sedation, using 5 mg diazepam, on postoperative sequelae (Pain, trismus and swelling) following impacted mandibular third molar surgery. Materials methods: is a randomised control involving 100 patients whose anxiety levels were assessed with Modified Dental Anxiety Scale (MDAS) just before drug administration thirty minutes after admini...

BACKGROUND Behavioral effects of benzodiazepines following repeated exposure vary according to the intrinsic efficacy of the benzodiazepine studied, treatment schedule and the behavioral parameters evaluated. METHODS We applied the behavioral paradigms of spontaneous locomotor activity, elevated plus maze and grip strength to investigate the sedative, anxiolytic and myorelaxant effect of acut...

Different subtypes of GABAA (gamma-aminobutyric acid A) receptors, through their specific regional and cellular localization, are involved in the manifestation various functions, both at central peripheral levels. We hypothesized that non-neuronal receptors expressed on blood vessels, which positive allosteric modulators exhibit vasodilatory effects. This study two parts: one to determine prese...

Diazepam is metabolized by CYP2C19 and CYP3A4 in the liver. CYP2C19 shows genetic polymorphism associated with the poor metabolizer (PM) and extensive metabolizer (EM) phenotypes. The aim of this study was to assess the effect of diltiazem, a CYP3A4 inhibitor, on pharmacokinetics and dynamics of diazepam in relation to CYP2C19 genotype status. Thirteen healthy volunteers (eight EMs and five PMs...

[3H]Diazepam appears to bind specifically to a single, saturable, binding site located on rat brain membranes, with an affinity constant near 3 nM at pH 7.4. Specific binding constitutes more than 90% of total binding at 0 degrees and less than 10% of total binding at 37 degrees. Arrhenius plots suggest a sharp conformational change in the diazepam receptor near 18 degrees. Mitochondrial fracti...