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Sedatives and Hypnotics Drugs: Benzodiazepines01:19

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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).
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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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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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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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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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Anxiolytic Drugs: Overview01:26

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Anxiolytic drugs are vital in managing anxiety disorders by effectively alleviating symptoms such as excessive fear, tachycardia, and tremors. There are several classes of anxiolytic medications, each with unique mechanisms of action and potential side effects.
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Designer benzodiazepines: an update.

Xiao Yu1, H Karl Greenblatt1, David J Greenblatt1

  • 1Program in Pharmacology and Drug Development, Tufts University School of Medicine and Graduate School of Biomedical Sciences, Boston, MA, USA.

Expert Review of Clinical Pharmacology
|January 17, 2023
PubMed
Summary
This summary is machine-generated.

Designer benzodiazepines (DBs), a type of novel psychoactive substance (NPS), mimic approved benzodiazepines. While their use is rising, concurrent drug use poses the main public health risk, not the DBs themselves.

Keywords:
Designer benzodiazepine (DBs)gamma-aminobutyric acid type A-benzodiazepine (GABAA-BZ) agonisthealth risksnovel psychoactive substances (NPS)

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Area of Science:

  • Pharmacology
  • Toxicology
  • Medicinal Chemistry

Background:

  • Designer benzodiazepines (DBs) are novel psychoactive substances (NPS) designed to replicate the effects of traditional benzodiazepines.
  • DBs function as full-agonist ligands at the gamma-aminobutyric acid type A-benzodiazepine (GABAA-BZ) receptor system.

Purpose of the Study:

  • To systematically review the classification, structure-activity relationships, pharmacologic properties, and adverse effects of designer benzodiazepines.
  • To assess the public health risks associated with designer benzodiazepine use.

Main Methods:

  • Systematic literature search on designer benzodiazepines.
  • Analysis of structure-activity relationships and pharmacologic profiles.
  • Review of reported adverse effects and concurrent drug use patterns.

Main Results:

  • Designer benzodiazepines exhibit pharmacologic profiles and risks similar to clinically approved benzodiazepines.
  • Concurrent use of DBs with other substances like alcohol and opioids is the primary public health concern.
  • Despite increasing illicit availability, DBs are not considered high-risk designer psychotropic agents.

Conclusions:

  • Designer benzodiazepines share pharmacological similarities and risks with traditional benzodiazepines.
  • The major public health risk stems from polydrug use involving DBs.
  • Regulatory attention is needed due to increasing illicit availability, but DBs pose a relatively lower health risk compared to other designer drugs.