Pharmazie
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In order to assess the significance of drug levels measured in clinical and forensic toxicology as well as for Therapeutic Drug Monitoring (TDM) it is essential that good collections of data are readily available. For more than 800 substances, therapeutic ('normal') and, if data was available, toxic, and fatal plasma concentrations as well as elimination half-lives were compiled in a table. The compilation includes data for hypnotics, benzodiazepines, neuroleptics, antidepressants, sedatives, analgesics, anti-inflammatory agents (e.g., NSAIDs), antihistamines, antiepileptics, betaadrenergic antagonists, antibiotics (penicillins, cephalosporins, aminoglycosides, gyrase inhibitors), diuretics, calcium-channel blockers, cardiac glycosides, antiarrhythmics, antiasthmatics, ACE-inhibitors, opiate agonists, and local anesthetics, among others. ⋯ Wherever possible, ranges for therapeutic plasma concentrations are expressed as trough concentration at steady state. The half-life values given for each drug are chosen to represent the terminal log-linear phase at most. It is the purpose to rapidly assess the significance of drug levels for the therapeutic monitoring of patients, and to facilitate the diagnostic and clinical assessment in case of intoxications.
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Comparative Study Clinical Trial
Intranasal administration of midazolam in a cyclodextrin based formulation: bioavailability and clinical evaluation in humans.
Intranasal administration of midazolam has been of particular interest because of the rapid and reliable onset of action, predictable effects, and avoidance of injections. The available intravenous formulation (Dormicum i.v. solution from Hoffmann-La Roche) is however less than optimal for intranasal administration due to low midazolam concentration and acidity of the formulation (pH 3.0-3.3). In this study midazolam was formulated in aqueous sulfobutylether-beta-cyclodextrin buffer solution. ⋯ Mild to moderate, transient irritation of nasal and pharyngeal mucosa was reported. The nasal formulation approaches the intravenous form in speed of absorption, serum concentration and clinical sedation effect. No serious side effects were observed.
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Research activities of the Hungarian Institute of Drug Research in the field of cardiovascular agents are reviewed. Many promising drug candidates were found including a compound already marketed. Novel concepts for drug research were developed as well.
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This study examines the physico-chemical stability of infusion solutions for epidural administration containing bupivacaine hydrochloride 0.06% or 0.125% or lidocaine hydrochloride 0.25% in 0.9% sodium chloride, each with fentanyl 0.0002%. The solutions were prepared in polyvinyl chloride (PVC) infusion bags and stored without overwrap at room temperature (25-30 degrees C) or refrigerated (4-8 degrees C). Over a period of 32 days stability was determined by visual inspection, pH measurement, and HPLC assay of drug concentrations. ⋯ A solution of fentanyl and lidocaine with an initial pH of 6.7 exhibited a rapid decrease of drug concentrations. Supposing fentanyl loss was due to sorption, buffered single drug fentanyl solutions of pH 5.5, 5.8, 6.3, and 6.7 were prepared in glass and PVC containers and stored under the same conditions. All solutions in PVC bags showed relevant fentanyl loss which was more evident at higher pH, whereas fentanyl concentration remained unchanged in glass containers at any of the tested pH values.