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Related Concept Videos

Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

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: Overview

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: Benzodiazepines

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...
Management of Insomnia01:19

Management of Insomnia

The sleep cycle, an integral part of human health, consists of several stages with distinct characteristics and functions. It begins with a transition from wakefulness to sleep, known as the light sleep phase, followed by the restorative deep sleep phase, essential for physical recovery and growth. The cycle concludes with the Rapid Eye Movement (REM) phase, characterized by high brain activity and vivid dreaming. Insomnia, a prevalent sleep disorder, involves difficulty falling asleep, staying...
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The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
Drugs in...
Sedatives and Hypnotics Drugs: Barbiturates01:20

Sedatives and Hypnotics Drugs: Barbiturates

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 key...

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Drug-Induced Sleep Endoscopy (DISE) with Target Controlled Infusion (TCI) and Bispectral Analysis in Obstructive Sleep Apnea
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Sublingual zolpidem (Edluar™; Sublinox™).

Lily P H Yang1, Emma D Deeks

  • 1Adis, Private Bag, Mairangi Bay, North Shore, Auckland, New Zealand. CNS@adis.com

CNS Drugs
|October 5, 2012
PubMed
Summary

Sublingual zolpidem offers a faster onset of action for insomnia treatment compared to oral formulations. This new formulation demonstrated improved sleep latency while maintaining similar tolerability and sleep duration.

Area of Science:

  • Pharmacology
  • Sleep Medicine
  • Drug Delivery Systems

Background:

  • Zolpidem is a widely prescribed non-benzodiazepine hypnotic for short-term insomnia treatment.
  • Traditional oral formulations have limitations in onset of action.
  • Development of novel drug delivery systems aims to improve therapeutic efficacy.

Purpose of the Study:

  • To evaluate the efficacy and safety of a sublingual orally disintegrating tablet formulation of zolpidem.
  • To compare the pharmacokinetic profile and sleep-onset characteristics of sublingual zolpidem against immediate-release oral zolpidem.
  • To assess the impact of sublingual zolpidem on sleep architecture and patient-reported outcomes.

Main Methods:

  • A randomized, double-blind, double-dummy, crossover, multi-center study.

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  • Inclusion of adult patients (n=70) diagnosed with primary insomnia.
  • Administration of a single 10-mg dose of sublingual zolpidem versus oral immediate-release zolpidem.

    • Main Results:

    • Sublingual zolpidem significantly reduced latency to persistent sleep compared to oral zolpidem.
    • Sleep-onset latency and latency to stage 1 sleep were significantly shorter with the sublingual formulation.
    • Total sleep time and wake after sleep onset showed non-inferiority and no significant difference, respectively, for sublingual zolpidem.

    Conclusions:

    • Sublingual zolpidem provides a faster onset of action for treating insomnia.
    • The sublingual formulation is bioequivalent and demonstrates comparable tolerability to oral zolpidem.
    • Sublingual zolpidem represents a viable alternative for patients requiring rapid sleep onset.