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Related Concept Videos

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...
536
Anxiolytic Drugs: Benzodiazepines and Buspirone01:29

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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: Barbiturates and Benzodiazepines01:14

CNS Depressants: Barbiturates and Benzodiazepines

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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...
918
Sedatives and Hypnotics: Overview01:23

Sedatives and Hypnotics: Overview

1.0K
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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Sedatives and Hypnotics Drugs: Barbiturates01:20

Sedatives and Hypnotics Drugs: Barbiturates

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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...
692
Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

337
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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Benzodiazepines: Thinking outside the black box.

Joseph V Pergolizzi1,2, Jo Ann LeQuang2, Robert B Raffa1,3,4

  • 1Neumentum Inc., Summit, NJ, USA.

Journal of Clinical Pharmacy and Therapeutics
|December 21, 2020
PubMed
Summary

The U.S. Food and Drug Administration (FDA) updated benzodiazepine warnings due to risks. New guidance emphasizes patient-specific tapering plans to manage withdrawal and improve safe prescribing of these medications.

Keywords:
FDAbenzodiazepineboxed (black box) warningoverusewithdrawal

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Area of Science:

  • Pharmacology
  • Drug Safety
  • Public Health

Background:

  • Benzodiazepines are widely prescribed, with 92 million prescriptions dispensed in 2019.
  • Current prescribing information inadequately warns about serious risks and harms.
  • Inappropriate prescribing and use of benzodiazepines are significant concerns.

Purpose of the Study:

  • To highlight the FDA's updated Drug Safety Communication regarding benzodiazepines.
  • To emphasize the need for improved warnings and safer prescribing practices.
  • To address the critical aspect of benzodiazepine discontinuation and withdrawal.

Main Methods:

  • Review of the FDA's Drug Safety Communication on benzodiazepines.
  • Analysis of the rationale behind the updated warnings and recommendations.
  • Examination of guidance on patient-specific tapering and withdrawal management.

Main Results:

  • The FDA mandates updated Boxed Warnings and other changes for benzodiazepines.
  • The communication validates patient reports of serious risks and harms.
  • Guidance is provided on managing benzodiazepine discontinuation and protracted withdrawal.

Conclusions:

  • Benzodiazepines remain important for indicated disorders but require reassessment due to widespread use.
  • Healthcare providers must be reminded of serious risks and harms.
  • Patient-specific tapering plans and ongoing support are crucial for safe discontinuation.