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Sedatives and Hypnotics Drugs: Benzodiazepines01:19

Sedatives and Hypnotics Drugs: Benzodiazepines

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Benzodiazepines have both sedative and hypnotic properties. They include compounds such as diazepam (Valium) and alprazolam (Xanax). Structurally, their cores are similar, consisting of the fusion of a benzene ring and a diazepine ring, but they share a common mechanism of action in the central nervous system (CNS).
Benzodiazepines work by enhancing the effects of the inhibitory neurotransmitter GABA. They bind to the GABAA receptor, increasing its affinity for GABA, which opens chloride...
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Sedatives and Hypnotics: Overview01:23

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Sedatives are drugs that alleviate anxiety, while hypnotics induce sleep. Both classes of medication suppress neuronal activity, leading to a calming effect for sedatives and facilitating sleep for hypnotics.
Sedative-hypnotics are categorized into barbiturates, benzodiazepines (BZDs), and non-benzodiazepines or Z-drugs. These drugs work by suppressing central nervous system activity, and this suppression is dose-dependent. Older sedative medications, like barbiturates, follow a linear curve in...
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CNS depressants include drugs from the category of barbiturates and benzodiazepines. They are valuable medications for managing anxiety disorders and insomnia. Barbiturates, once used to induce and maintain sleep, have been replaced mainly by benzodiazepines due to barbiturate's toxicity, tolerance, and overdose risks. They interact with GABAA receptors, leading to sedation at low doses and potentially coma and death at higher doses. Phenobarbital, a long-acting barbiturate, possesses...
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Benzodiazepines are a class of anxiolytic drugs known for their rapid efficacy and high therapeutic-to-lethal dose ratio, but with a potential risk of drug dependence. These drugs are lipophilic, allowing for rapid absorption after oral administration, eventually reaching the central nervous system (CNS). Once in the CNS, benzodiazepines bind to the allosteric site of the GABAA receptor. This binding enhances the inhibitory effects of the neurotransmitter GABA. By doing so, they prevent...
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Sedatives and hypnotics encompass a drug class that acts on the central nervous system (CNS) to alleviate anxiety, promote relaxation and induce sleep.These drugs function by amplifying the actions of the neurotransmitter γ-aminobutyric acid (GABA), resulting in reduced neuronal activity. Barbiturates, a subset of sedatives and hypnotics first synthesized in the late 1800s, are categorized into ultra-short, short, intermediate, and long-acting groups based on their duration of effect. A...
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Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

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Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
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High-Throughput Method for Measuring Alcohol Sedation Time of Individual Drosophila melanogaster
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New benzodiazepines for sedation.

Elyse M Cornett1, Matthew B Novitch2, Andrew J Brunk3

  • 1Department of Anesthesiology, LSU Health Shreveport, 1501 Kings Highway, Shreveport, LA, 71103, USA.

Best Practice & Research. Clinical Anaesthesiology
|October 17, 2018
PubMed
Summary
This summary is machine-generated.

Novel benzodiazepine drugs are being developed for enhanced sedation and anesthetic adjuvants. This review covers new agents like remimazolam, detailing their pharmacology, efficacy, and clinical trials for future development.

Keywords:
benzodiazepinesderivativesnon-benzodiazepinenovel benzodiazepinessedation

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Area of Science:

  • Pharmacology
  • Neuroscience

Background:

  • Benzodiazepines are established for sedation and as anesthetic adjuvants.
  • Their mechanism involves GABAergic pathways and affects the amygdala and reticular activating system.

Purpose of the Study:

  • To review novel benzodiazepine agents with potential clinical applications.
  • To examine the pharmacologic profiles, side effects, efficacy, and clinical trials of new benzodiazepines.

Main Methods:

  • Literature review of new benzodiazepine drugs.
  • Analysis of pharmacologic properties, clinical trial data, and future development trends.

Main Results:

  • New benzodiazepines exhibit varying protein binding and lipid solubility.
  • Active metabolites and specific neurological targets are key characteristics.
  • Efficacy and side effect profiles are under investigation for novel agents.

Conclusions:

  • Emerging benzodiazepines show promise as improved sedation and anesthetic adjuncts.
  • Further research is needed to fully understand their therapeutic potential and safety.