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Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

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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

Sedatives and Hypnotics: Overview

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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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Parenteral Anesthetics: Overview01:24

Parenteral Anesthetics: Overview

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Intravenous anesthetics are drugs administered parenterally to induce anesthesia or sedation. Propofol is a widely used agent formulated as a 1% emulsion in soybean oil, glycerol, and egg phosphatide. It induces rapid anesthesia primarily due to its rapid distribution from the bloodstream to target tissues and is metabolized in the liver. However, it can cause significant pain on injection and hypertriglyceridemia. Fospropofol, a water-based prodrug of propofol, lacks these adverse effects.
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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).
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Neurochemical Transmission: Sites of Drug Action01:26

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Neurochemical transmission, the conduction of electrical impulses between neurons mediated by neurotransmitters, plays a vital role in various physiological processes. Autonomic drugs exert their effects by modulating neurotransmission within the autonomic nervous system. For instance, drugs such as hemicholinium block the precursor uptake necessary for synthesizing acetylcholine, an essential autonomic neurotransmitter. Following synthesis, neurotransmitters are stored in vesicles. Metyrosine...
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Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics01:11

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

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All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...
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Classics in Chemical Neuroscience: Medetomidine.

Pedro de Andrade Horn1, Tomayo I Berida1, Lauren C Parr1

  • 1Warren Center for Neuroscience Drug Discovery and Department of Pharmacology, Vanderbilt University, Nashville, Tennessee 37232, United States.

ACS Chemical Neuroscience
|October 15, 2024
PubMed
Summary

Medetomidine, an α2-adrenoreceptor agonist, is increasingly found as an adulterant in illicit drugs, causing sedation not reversed by naloxone. Its misuse is a growing concern amid the opioid crisis.

Keywords:
DexmedetomidineFentanylMedetomidineOpioidVeterinary Medicineα2-Adrenoreceptors

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Area of Science:

  • Pharmacology
  • Toxicology
  • Drug Chemistry

Background:

  • Medetomidine is an FDA-approved α2-adrenoreceptor agonist used in veterinary medicine.
  • Dexmedetomidine, its active enantiomer, is used for human sedation and analgesia.
  • Medetomidine is increasingly detected in illicit drug supplies.

Purpose of the Study:

  • To review the history, chemistry, pharmacology, and DMPK of medetomidine.
  • To discuss the emergence of medetomidine as an adulterant in the context of the opioid crisis.
  • To highlight the challenges in reversing medetomidine's sedative effects.

Main Methods:

  • Literature review of medetomidine's properties and illicit use.
  • Analysis of its presence in seized drug samples and overdose cases.
  • Examination of structure-activity relationships and pharmacokinetics.

Main Results:

  • Medetomidine is present in illicit drug mixtures with fentanyl, xylazine, and others.
  • It produces significant sedative effects that are not reversed by naloxone.
  • Its low cost and lack of regulation contribute to its misuse.

Conclusions:

  • Medetomidine's emergence as an adulterant poses a significant public health risk.
  • Understanding its pharmacology is crucial for addressing the opioid crisis.
  • Further research into detection and reversal strategies is needed.