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Sedatives and Hypnotics

  • Sedatives, also known as tranquilizers, are substances that reduce excitement or irritability, leading to a state of calmness.

  • They help to reduce anxiety, fear, and tension by slowing down brain activity.

Sedatives can be categorized into two main groups: minor tranquilizers (anxiolytics) and major tranquilizers (antipsychotics).

Hypnotics:

  • Hypnotics, on the other hand, are substances that induce sleep.

  • They are often used to treat conditions like insomnia. While some sedatives can act as hypnotics at higher doses, hypnotics generally have a more pronounced effect on sleep.

Common Sedatives and Hypnotics:

  • Some common sedatives include benzodiazepines (like diazepam and alprazolam), barbiturates, and certain antidepressants.

  • Hypnotics include drugs like zolpidem, eszopiclone, and zaleplon.

Mechanism of Action:

  • Most sedatives and hypnotics work by enhancing the action of a neurotransmitter known as gamma-aminobutyric acid (GABA) in the brain.

  • GABA is an inhibitory neurotransmitter, meaning it reduces the activity of neurons in the brain.

  • By enhancing GABA's action, these drugs effectively slow down brain activity, leading to a state of relaxation or sleep.

Side Effects and Risks:

  • While sedatives and hypnotics can be highly effective, they also carry risks.

  • Side effects can include drowsiness, dizziness, confusion, memory issues, and physical dependence or addiction with long-term use.

  • There is also a risk of overdose, which can lead to severe respiratory depression and even death.

  • Therefore, these medications should always be used under the supervision of a healthcare professional.

Classification of Sedatives and Hypnotics:

·        Sedatives and hypnotics can be classified based on their chemical structure and their mechanism of action.

Here are some of the most common classes:

1.Benzodiazepines:

Mechanism:
  • Act on the GABA-A receptor complex, enhancing the effect of the neurotransmitter GABA.

Use:
  • Anxiety relief, sedation, muscle relaxation, anticonvulsant, and amnesic effects.

Examples:
  • Chlordiazepoxide

  • Diazepam

  • Oxazepam

  • Chlorazepate

  • Lorazepam

  • Alprazolam

  • Zolpidem (Although not a benzodiazepine structurally, it acts on a similar site on the GABA-A receptor complex)

2. Barbiturates:

Mechanism:
  • Act on the GABA-A receptor complex, but in a different manner than benzodiazepines. They prolong the opening of the chloride ion channel.

Use:
  • Sedation, induction of sleep, pre-anesthetic, and treatment of seizures.

Examples:
  • Barbital

  • Phenobarbital

  • Mephobarbital

  • Amobarbital

  • Butabarbital

  • Pentobarbital

  • Secobarbital

3. Miscellaneous:

Amides & Imides:
  • Glutethimide: An older sedative-hypnotic that has largely been replaced by safer medications.

Alcohol & Their Carbamate Derivatives:
  • Meprobamate: An early anxiolytic with muscle relaxant properties.

  • Ethchlorvynol: A sedative and hypnotic medication.

Aldehyde & Their Derivatives:
  • Triclofos Sodium: A prodrug of trichloroethanol used as a sedative and hypnotic.

  • Paraldehyde: An older sedative and hypnotic, not commonly used today.

Sedative -Hypnotics
Sedative -Hypnotics

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