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Behavioural pharmacology
Published in Adam Doble, Ian L Martin, David Nutt, Calming the Brain: Benzodiazepines and related drugs from laboratory to clinic, 2020
Adam Doble, Ian L Martin, David Nutt
The most parsimonious conclusions that can be drawn from the studies performed with the receptor-specific benzodiazepine receptor ligands, concerning the respective behavioural functions mediated by the BZ1 and the BZ2 receptor subtype are relatively limited. The data suggest that all BZ1-preferring drugs produce less myorelaxation and ataxia than non-selective drugs, and have strong sedative/ hypnotic activity. Data are inconsistent concerning the receptor responsible for anxiolytic effects, and anticonvul-sant effects have not been systematically evaluated. There is also only limited information on the behavioural pharmacology of BZ2-specific agents. However, important progress has been made recently following the development of transgenic mice in which specific GABA receptor subunits have been deleted or modified.
Techniques for Isolation and Evaluation
Published in Shojiro Inoué, Biology of Sleep Substances, 2020
The production of sleep substances may increase in accordance with an elevation of sleep pressure. Sleep deprivation is apparently one of the best ways to artificially elevate the demand for sleep. Indeed, the earliest pioneer works by Ishimori1 and Legendre and Piéron2 demonstrated the presence of a hypnogenic factor in the brain tissue of long-term sleep-deprived dogs. A majority of candidate substances pursued in later studies were also extracted directly from the cerebral tissue, either from the whole brain or from the brainstem, of different animals (Factor S3 in cattle, goats, rabbits, and sheep, interleukin-1 [IL1]4 in mice, rapid-eye-movement [REM] sleep proteins5 in cats, sleep-promoting substance [SPS]6 in rats, etc.). Many sleep-related substances are known to be present in the brain, i.e., cholecystokinin (CCK),7 corticotropin-releasing factor (CRF),8 delta-sleep-inducing peptide (DSIP),9 growth hormone-releasing factor (GRF),8 insulin,10 prostaglandin D2 (PGD2),n piperidine,12 somatostatin (SRIF),8 vasoactive intestinal polypeptide (VIP),13 etc. Benzodiazepine receptor agonists are present in both peripheral organs and the central nervous system.14
Treatment of Psychological Disorders
Published in Mohamed Ahmed Abd El-Hay, Understanding Psychology for Medicine and Nursing, 2019
Benzodiazepines derive their name from their molecular structure. They share a common effect on benzodiazepine receptors, which in turn modulate gammaaminobutyric acid (GABA) activity. Because benzodiazepines have a rapid anxiolytic sedative effect, they are most commonly used for immediate treatment of insomnia, acute anxiety, and agitation or anxiety associated with any psychiatric disorder. In addition, the benzodiazepines are used as anesthetics, anticonvulsants, and muscle relaxants. Because of the risk of dependence, benzodiazepines are not recommended for long-term use. Flumazenil, a benzodiazepine receptor antagonist, is used to reverse benzodiazepine-induced sedation and in emergency care of benzodiazepine overdosage.
Impact of timing of midazolam administration on incidence of postoperative nausea and vomiting in patients undergoing laparoscopic gynecological surgery: A randomized, double-blinded, controlled study
Published in Egyptian Journal of Anaesthesia, 2022
Samar Rafik Amin, Taghreed Elshahat Sakr, Shaimaa Ezzat Amin
Midazolam is a short-acting sedative which attaches to benzodiazepine receptors placed on gamma-aminobutyric acid (GABA) type-A receptors within the central nervous system. Releasing GABA neurotransmitters restrains the central dopaminergic pathway, leading to sedation and anxiolysis. However, it is not entirely clear how midazolam acts as an antiemetic. Some hypothesized mechanisms involve reduced dopaminergic stimulation in the chemoreceptor trigger zone, along with reduced 5-hydroxytryptamine outflux by attaching to GABA-benzodiazepine complex [6]. Also, it is unclear whether midazolam antiemetic properties are correlated with its anxiolytic action. Previous research has revealed that preoperative anxiety increases stomach acidity and decreases gastric motility, which could raise the risk of PONV [7].
Neuroimaging in primary lateral sclerosis
Published in Amyotrophic Lateral Sclerosis and Frontotemporal Degeneration, 2020
Erik P. Pioro, Martin R. Turner, Peter Bede
[11C]-flumazenil binds to the benzodiazepine receptor subunit of the GABAA receptor (R) localized to brain neurons. A study of 9 PLS patients included [11C]-flumazenil PET at a single time-point in 5 patients alongside longitudinal clinical and electrophysiologic evaluations (98). PET measurement of regional cerebral blood flow (rCBF), an index of synaptic brain function, was reduced in the precentral gyrus (fronto-opercular region), ventrolateral prefrontal region, and anterior cingulate cortex. GABAA-R density, a potential surrogate for neuronal cell body and proximal dendrite integrity, was not as diffusely decreased but localized within the foci of rCBF reduction. Whether reduced [11C]-flumazenil binding represents neuronal loss, changes in GABAA-R functional properties, or both, is uncertain. However, this study confirmed the motor system dysfunction in PLS is similar to that in ALS, at least for rCBF.
Management of insomnia in alcohol use disorder
Published in Expert Opinion on Pharmacotherapy, 2020
Pierre A. Geoffroy, Michel Lejoyeux, Benjamin Rolland
Given these numerous aftermaths related to insomnia disorder in AUD (Figure 1), an increasing interest has emerged regarding the therapeutic strategies on insomnia symptoms. This interest is also justified by the fact that treating insomnia might be challenging for physicians, who are used to prescribe hypnotics, especially short- to intermediate-acting benzodiazepine receptor agonists (e.g. zolpidem or zopiclone), but not in the context of AUD. Indeed, in patients with AUD, benzodiazepine receptor agonists are generally not recommended to avoid the risk of abuse and overdose when used combined with alcohol [16]. In this context, and compared to other populations, patients with AUD are mostly under-treated for their insomnia symptoms [17], as emphasized by a survey addressed to addiction medicine physicians [18].