Recent Developments in the Pharmacology of the Benzodiazepines

Schallek, William; Schlosser, Walter; Randall, Lowell O.

doi:10.1016/s1054-3589(08)60523-2

Cited by 62 publications

(19 citation statements)

References 80 publications

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“…The first two mechanisms are unlikely to apply to benzoctamine and chlordiazepoxide since neither drug inhibits monoamine oxidase nor stimulates 5-HT receptors directly (Bein, 1970;Maitre et al, 1970;Randall, Heise, Schallek, Bagdon, Banziger, Boris, Moe & Abrams, 1961;Schallek, Schlosser & Randall, 1972). To determine whether these drugs affect the 5-HT neuronal membrane uptake mechanism, the method of Carlsson et al (1969) was used.…”

Section: Methodsmentioning

confidence: 99%

Effects of Benzoctamine and Chlordiazepoxide on Turnover and Uptake of 5‐hydroxytryptamine in the Brain

Lippmann¹,

Pugsley²

1974

British J Pharmacology

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Benzoctamine, a new psychoactive drug, known to exert in man an anti‐anxiety effect resembling that of chlordiazepoxide, decreased the disappearance of intraventricularly‐injected [14C]‐5‐hydroxytryptamine (5‐HT) from rat brain, as did chlordiazepoxide. Both drugs partially inhibited the α‐ethyl‐3‐hydroxy‐4‐methylphenylethylamine‐induced depletion of rat brain 5‐HT. It is concluded that benzoctamine, like chlordiazepoxide, decreases 5‐HT turnover in the brain and that this action may play a role in the anti‐anxiety effect of these drugs observed in man.

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Section: Methodsmentioning

confidence: 99%

Effects of Benzoctamine and Chlordiazepoxide on Turnover and Uptake of 5‐hydroxytryptamine in the Brain

Lippmann¹,

Pugsley²

1974

British J Pharmacology

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“…Thus, conditioned suppression of feeding used as an index of fear was increased rather than decreased by the administration of these compounds (Stein and Berger, 1969). Similarly, a number of previously sup pressed responses in behavioral tests in animals can be released by benzo diazepines (Schallek et al, 1972;Wise et al, 1972). Particularly, punished re sponses are increased.…”

Section: Discussionmentioning

confidence: 98%

“…However, the turnover of DA in limbic structures, and particularly in the septum, was not examined in these experiments. It is known from electrophysiological studies that limbic structures are one of the main targets of benzodiazepines in the central nervous system (Schallek et al, 1972).…”

Section: Discussionmentioning

confidence: 99%

Benzodiazepine-Induced Modifications of Dream Content: The Effect of Flunitrazepam

Gaillard¹,

Phelippeau²

1976

Neuropsychobiology

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The purpose of this study was to investigate the effect of flunitrazepam, a benzodiazepine with strong hypnotic properties, on dream content. Eight normal subjects were studied in laboratory by the awakening technique, and the dream contents were rated by two judges according to nine scaled dimensions: unreality, participation of the dreamer, pleasantness, unpleasantness, verbal aggressivity, physical aggressivity, sexuality, sensoriality and time of reference in the dreamer’s life. By comparison with placebo condition, flunitrazepam induced more unpleasantness, more verbal aggressivity, more physical aggressivity, and more sexuality in dreams. This increase of emotionally loaded contents can be related to a disinhibitory effect of this drug, and the possible involvement of dopaminergic or serotoninergic systems is discussed.

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“…acid (GABA) intensifying effects of the benzodiazepines, 25 , 26 and to the reports by Andersen and his colleagues 2 7-29 and Rhodes 30 that spindle waves originate from an increase of inhibitory post-synaptic potentials (IPSPs) in thalamic neurons. With these two considerations, GABA potentiation by benzodiazepines and sleep spindles as an IPSP of thalamic neurons, in mind, Azumi and Shirakawa assumed that the originating mechanism of spontaneous spindles is facilitated due to the intensifying inhibitory action of a GABA-like substance, or some other inhibitory neurotransmitter by benzodiazepines.…”

mentioning

confidence: 94%

Effects of a Short-Acting Benzodiazepine on Brain Electrical Activity During Sleep

Johnson¹,

Spinweber²

PsycEXTRA Dataset

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1, SUMMARYThe changes seen in EEG activity with administration of long-acting benzodiazepines are a significant decrease In delta, 0.5-3 Hz, and a significant increase in sleep spindles, bursts of 11-15 Hz activity. These changes often persist for several days after the medication is discontinued.The introduction of a new benzodiazepine hypnotic, triazolam, in which the half-life of both the parent compound and its metabolite is less than 10 hours, raises questions as to whether its use will produce similar EEG changes during sleep and whether there will be a build-up effect over nights. Of particular interest is whether electrophysiological and performance changes will persist at the same level during a 7.5-hour sleep period and whether there will be a quick return to baseline EEG activity during withdrawal. As part of a larger study on the effects of benzodiazepines on EEG, sleep, arousal levels, and performance, delta and spindle activity were measured during baseline, treatment, and withdrawal. The auditory cortical evoked potential was also obtained during the last baseline and during the fifth drug night.Twenty male chronic poor sleepers, mean age 21.02 ± 2.37 years, with EEG measured sleep latencies of greater than 30 minutes, participated in the double-blind study. All received a placebo for 3 nights, 10 continued to receive the placebo and 10 were given 0.5 mg triazolam for 6 nights, and all received placebo on 2 withdrawal nights. Subjects received click stimulation on the last night of the baseline and the fifth night of hypnotic administration (study nights 4 and 9).Subjects receiving triazolam showed a significant increase in sleep spindles and a significant decrease in delta count during drug administration. Both values returned to baseline on the first withdrawal night. The auditory evoked potential (AEP) peak-to-trough amplitude was also significantly reduced during sleep by triazolam, but, as the time since drug ingestion increased, the amplitude of the AEP also increased. There was no difference in AEP amplitude between the two groups 5 hours post-drug ingestion.In morning performance batteries, there were no cognitive or visual motor performance decrements. While the long-acting metabolites of some benzodiazepines, further influenced by dose levels, may be the neuropharmacological basis for daytime performance decrements, these data indicate that the EEG changes occur in the absence of long-acting metabolites. As with flurazepam, there was no relationship between the EEG changes, sleep efficiency, and morning performance.2

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Recent Developments in the Pharmacology of the Benzodiazepines

Cited by 62 publications

References 80 publications

Effects of Benzoctamine and Chlordiazepoxide on Turnover and Uptake of 5‐hydroxytryptamine in the Brain

Effects of Benzoctamine and Chlordiazepoxide on Turnover and Uptake of 5‐hydroxytryptamine in the Brain

Benzodiazepine-Induced Modifications of Dream Content: The Effect of Flunitrazepam

Effects of a Short-Acting Benzodiazepine on Brain Electrical Activity During Sleep

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