Pharmacology 2: Block 1 Sedative-Hypnotic and Anxiolytic Drugs

Alprazolam (Xanax)

MOA: Benzodiazepine; facilitates activity of GABA (works only in presence of GABA, exhibits ceiling effect),

Use: Acute anxiety

SE: Can lead to dependence; caution in elderly; can lead to CNS depression; avoid with alcohol and other CNS depressants

Chlordiazepoxide (Librium)

MOA: Benzodiazepine; facilitates activity of GABA,

Use: Alcohol detoxification given longer duration of action,

SE: Can lead to dependence; caution in elderly; can lead to CNS depression; avoid with alcohol and other CNS depressants

Phenobarbital

MOA: Barbiturate; facilitates activity of GABA (works independent of GABA, no ceiling effect),

Use: Seizure disorders,

SE: Respiratory depression; induces Cytochrome P450 enzymes

Diphenhydramine (Benadryl)

MOA: Histamine antagonist,

Use: Mild insomnia and anxiety disorders,

SE: Anticholinergic side effects

Hydroxyzine

MOA: Histamine antagonist,

Use: Mild insomnia and anxiety disorders,

SE: Anticholinergic side effects; less sedating than Benadryl

Zolpidem (Ambien)

MOA: Selectivity at targeting only GABA(A) receptors,

Use: Insomnia,

SE: Shorter duration of action; fewer side effects and less dependence than Benzodiazepines

Buspirone

MOA: Partial agonist at presynaptic 5-HT1 auto-receptor; antagonistic properties at dopamine D2 receptors,

Use: Anxiety,

SE: Used as a non-sedating anxiolytic drug