5.17 Increasing GABA Activity

Sedatives: Overview

  • Sedatives are often referred to as "downers."

  • Function: Depress or slow down the central nervous system.

  • Effects: Induce feelings of drowsiness, relaxation, and in some cases, sleep.

Common Sedatives and Their Mechanisms

  • Examples of commonly prescribed and abused sedatives:

    • Xanax

    • Valium

  • Mechanism of Action:

    • Increase activity of GABA (gamma-aminobutyric acid), the primary inhibitory neurotransmitter in the brain.

    • This increase inhibits action potentials, resulting in calmness and relaxation.

Cultural Reference

  • Example from Ace Ventura:

    • In a scene from the film, the character Ace Ventura gets hit with a dart that likely contains a sedative.

    • Illustration of how sedatives can cause drowsiness and unconsciousness.

Risks and Dangers of Sedative Use

  • Tolerance Development:

    • Tolerance to sedatives develops quickly, leading to increased dosage requirements.

  • Dependence:

    • High risk of dependence, making these drugs dangerous for recreational use.

Barbiturates: An Older Class of Sedatives

  • Description:

    • Older class of sedatives that operate by acting on GABA.

  • Risks Associated:

    • Potential to inhibit parts of the midbrain (e.g., the medulla).

    • Excessive inhibition can lead to fatal consequences, such as stopping the heart or lungs.

  • Current Status:

    • Largely replaced in medical settings by benzodiazepines due to safety concerns.

Benzodiazepines: A Newer Class of Sedatives

  • Description:

    • Newer class of sedatives that also increase GABA activity.

  • Comparison with Barbiturates:

    • Although they work similarly, benzodiazepines do not inhibit the midbrain to the same fatal extent as barbiturates.

Abuse of Sedatives

  • Abuse Patterns:

    • Barbiturates continue to be abused recreationally; often used to fall asleep due to anxiety or stress.

  • Sleep Quality Issues:

    • While barbiturates may induce sleep, they disrupt REM sleep cycles that are crucial for restorative sleep.

  • Important Point:

    • Use of sedatives as sleep aids is counterproductive due to negative effects on sleep quality.