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Pharmacokinetic-Pharmacodynamic Modeling in Drug Development: Comments and Applications
Published in Hartmut Derendorf, Günther Hochhaus, Handbook of Pharmacokinetic/Pharmacodynamic Correlation, 2019
Joseph C. Fleishaker, James J. Ferry
This series of studies showed that both adinazolam and NDMAD are the right drugs to be monitoring in pharmacokinetic studies. NDMAD is the right drug to measure because it is primarily responsible for the sedative and psychomotor effects after adinazolam. The studies could not separate the contribution of adinazolam and NDMAD to the therapeutic effects of adinazolam administration in the treatment of depression,18,19 panic disorder,29 and anxiety,20 but, based on the pharmacology of these two compounds, it is likely that both compounds contribute to the apparent efficacy of the parent compound. Therefore, both should be measured.
Pharmacotherapy of Mixed Anxiety/Depression Disorders
Published in Siegfried Kasper, Johan A. den Boer, J. M. Ad Sitsen, Handbook of Depression and Anxiety, 2003
A. Carlo Altamura, Roberta Bassetti, Sara Fumagalli, Donato Madaro, Daniele Salvadori, Emanuela Mundo
The so-called high-potency benzodiazepines (i.e., alprazolam and adinazolam) appear to be quite promising in the treament of comorbid anxiety-depression conditions, since they have been shown to have both an anxiolytic and an antidepressant activity. The mechanisms underlying this complex clinical profile are not completely known. Alprazolam has been reported to have an effect on corticotropin-releasing hormone (CRH) [148] as well as noradrenergic properties [149], and both these parmacodynamic properties may well account for its antidepressant activity.
Designer benzodiazepines: an update
Published in Expert Review of Clinical Pharmacology, 2023
Xiao Yu, H Karl Greenblatt, David J Greenblatt
Benzodiazepines first became available for clinical use in the United States in 1960 [13]. They rapidly replaced the more hazardous barbiturates, and other therapeutic options, for the treatment of anxiety and sleep disorders [13–16]. In current clinical practice, benzodiazepines are widely used and essential medications prescribed for anxiety and panic disorders, insomnia, and in anesthesia practice [13–20]. Designer benzodiazepines (DBs), as a subclass of NPS, have increased in usage prevalence owing to online internet availability, low cost, and lack of regulatory control. DBs are not approved for medical use in the United States, but some of the benzodiazepine derivatives are licensed in other countries. These include phenazepam (Russia), etizolam (India, Italy, and Japan), fultazolam (Japan), and adinazolam (Italy) [6–9].
Designer benzodiazepines: a report of exposures recorded in the National Poison Data System, 2014–2017
Published in Clinical Toxicology, 2019
Joseph E. Carpenter, Brian Patrick Murray, Camille Dunkley, Ziad N. Kazzi, Melissa H. Gittinger
We retrieved coded, de-identified data for all intentional single-agent exposures to the following compounds: adinazolam, clonazolam, cloniprazepam, diclazepam, etizolam, flubromazepam, flubromazolam, meclonazepam, nifoxipam, norflurazepam, and pyrazolam. Corresponding Poisindex codes are available in the supplementary material. Etizolam exposures have been tracked since 2007, however specific exposure codes for all other agents were not added until 2016. Though there are additional compounds within the designer benzodiazepine class, at the time of this study these agents did not have a specific coded designation within NPDS, and therefore could not be retrieved. All exposure routes were included. Accidental ingestions and any subjects with exposure to more than one substance were excluded.
Occurrence and time course of NPS benzodiazepines in Sweden – results from intoxication cases in the STRIDA project
Published in Clinical Toxicology, 2019
Matilda Bäckberg, Madeleine Pettersson Bergstrand, Olof Beck, Anders Helander
The NPS BZD covered in this study (Figure 2) were adinazolam, bentazepam, clonazolam, cloniprazepam, diclazepam, deschloroetizolam, flubromazolam, flunitrazolam, 3-hydroxyflubromazepam, ketazolam, meclonazepam, metizolam, nifoxipam, nitrazolam, pivoxazepam, and pyrazolam (1 mg/mL solutions from Chiron, Trondheim, Norway), bromazepam, clobazam, etizolam, estazolam, flurazepam, 3-hydroxyphenazepam, N-desmethylflunitrazepam, nimetazepam, phenazepam, and prazepam (1 mg/mL solutions from Cerilliant, Round Rock, TX), flubromazepam (1 mg/mL solution from LGC, Teddington, UK), and tetrazepam (0.1 mg/mL solution from LGC). All solutes were obtained in acetonitrile or methanol.