Sedative

From Citizendium, the Citizens' Compendium

Contents 1 Classification 1.1 Alcohols 1.1.1 Ethylene glycols 1.2 Anti-adrenergics 1.3 Anti-histamines 1.4 Gamma-aminobutyric acid (GABA) agonists 1.4.1 Barbituates 1.4.2 Benzodiazepines 1.4.2.1 Non-selective agonists 1.4.2.2 BZ1 selective agonists 1.5 Serotonin (5-HT) agonists 2 References

Classification

Below are examples of available sedative drugs.

Alcohols

Ethylene glycols

• Chloral hydrate

Anti-adrenergics

Inhibitors of the adrenergic alpha-2 receptor can cause sedation.

• Dexmedetomidine. In some settings, dexmedetomidine may cause less adverse drug reactions than non-selective benzodiazepams.^[1]

Anti-histamines

• Diphenhydramine

Gamma-aminobutyric acid (GABA) agonists

Gamma-aminobutyric acid (GABA) the major inhibitory neurotransmitter in the central nervous system.^[2] Drugs that increase the effect of GABA are called GABAergic.

Many sedatives work by increasing receptiveness of GABA_A receptors.

Barbituates

Barbituates are GABAergic by increasing receptiveness of the GABA_A receptors. Barbituates do this by increasing the duration of openings of channels in the cell membrane.^[2]

• Phenobarbital

Benzodiazepines

Benzodiazepines are also GABAergic by increasing receptiveness of the GABA_A receptors. However, benzodiazepines do this by increasing the frequency of openings of channels in the cell membrane.^[2]

Benzodiazepine receptors are BZ₁ and BZ₂.

Non-selective agonists

• Diazepam (Valium)

BZ₁ selective agonists

• Zaleplon
• Zolpidem

Serotonin (5-HT) agonists

Agonists of the 5-HT_1A receptor can cause sedation.

• Buspirone

References

1. ↑ Pandharipande PP, Pun BT, Herr DL, et al (2007). "Effect of sedation with dexmedetomidine vs lorazepam on acute brain dysfunction in mechanically ventilated patients: the MENDS randomized controlled trial". JAMA 298 (22): 2644–53. DOI:10.1001/jama.298.22.2644. PMID 18073360.
2. ↑ ^{2.0 2.1 2.2} Katzung, Bertram G. (2006). Basic and clinical pharmacology. New York: McGraw-Hill Medical Publishing Division. ISBN 0-07-145153-6.