Sedatives and Hypnotics

Definition of Sedatives and Hypnotics

  • Sedatives and hypnotics are central nervous system (CNS) depressants that reduce anxiety (anxiolytic effect), induce sedation (calming effect), or promote sleep (hypnotic effect).
  • The same compound may act as a sedative or hypnotic depending on the dose and pharmacokinetics.

Sedatives and Hypnotics

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Classification

Classification of Sedatives and Hypnotics

1. Benzodiazepines

  • Mechanism (brief)
    • Enhance the effect of GABA (gamma-aminobutyric acid) at the GABA-A receptor, increasing the frequency of chloride channel opening, leading to CNS depression.
  • Examples of Benzodiazepines:
    • Chlordiazepoxide
    • Diazepam
    • Oxazepam
    • Chlorazepate
    • Lorazepam
    • Alprazolam
    • Zolpidem (Note: Chemically distinct but acts at benzodiazepine binding site – often grouped with BZDs for pharmacology)
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2. Barbiturates

  • Mechanism (brief)
    • Act on GABA-A receptors to prolong the duration of chloride channel opening.
    • At higher doses, they can mimic GABA, leading to more profound CNS depression.
  • Examples of Barbiturates:
    • Barbital
    • Phenobarbital
    • Mephobarbital
    • Amobarbital
    • Butabarbital
    • Pentobarbital
    • Secobarbital

3. Miscellaneous Sedatives and Hypnotics

  1. Amides & Imides
    • Structural similarity to barbiturates.
    • Act as CNS depressants.
    • Example:
      • Glutethimide
  2. Alcohols & Carbamate Derivatives
    • Possess sedative-hypnotic
    • Carbamate derivatives act as CNS depressants similar to older sedatives.
    • Examples:
      • Meprobamate
      • Ethchlorvynol
  3. Aldehydes & Their Derivatives
    • Used for short-term sedation.
    • Work by depressing CNS activity, though mechanisms can vary.
    • Examples:
      • Triclofos sodium
      • Paraldehyde
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Classification of Sedatives and Hypnotics

Class Mechanism of Action Examples Key Notes / Uses
Benzodiazepines Enhance GABA-A receptor activity → increase frequency of Cl⁻ channel opening → CNS depression Chlordiazepoxide, Diazepam, Oxazepam, Chlorazepate, Lorazepam, Alprazolam, Zolpidem* Anxiolytics, hypnotics, anticonvulsants, muscle relaxants. Zolpidem is non-BZD but binds same site.
Barbiturates Enhance GABA-A activity → prolong Cl⁻ channel opening; at high doses, mimic GABA → profound CNS depression Barbital, Phenobarbital, Mephobarbital, Amobarbital, Butabarbital, Pentobarbital, Secobarbital Less safe than BZDs; used in epilepsy and anesthesia. Risk of dependence, overdose.
Amides & Imides Structurally similar to barbiturates; act as CNS depressants Glutethimide Formerly used as sedative; replaced due to abuse potential and safer alternatives.
Alcohols & Carbamate Derivatives Depress CNS via uncertain mechanisms; carbamates similar to older sedatives Meprobamate, Ethchlorvynol Meprobamate has anxiolytic properties; now rarely used due to safety concerns.
Aldehydes & Derivatives Depress CNS activity; exact mechanism varies Triclofos sodium, Paraldehyde Used for short-term sedation; paraldehyde historically used in seizures and delirium.

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