IA Anxiolytics, Hypnotics and Barbiturates

Benzodiazepines vs Non-Benzodiazepines for Anxiety and Insomnia

• Alprazolam is a benzodiazepine commonly used for acute management of panic attacks due to its rapid onset of action and anxiolytic effects.

• Triazolam is a benzodiazepine used for short-term treatment of insomnia. It is not typically used for panic attacks.

• Zolpidem is a non-benzodiazepine used primarily for insomnia treatment. It is not indicated for panic attacks.

• Buspirone is a second-line treatment option for panic disorder.

  • It is considered first-line in patients with comorbid depression or substance abuse, or those at risk for benzodiazepine dependence.

  • Does not interact with fluoxetine and can be safely used in patients receiving SSRI treatment.

  • Onset of action is prolonged so it is not indicated for acute attacks.

• Secobarbital is a barbiturate medication with sedative effects. While it may induce relaxation and sleep, it is not commonly used for panic attacks due to the risk of dependence and overdose.

Mechanisms of Action

• Alprazolam binds in the chloride ion channel between α1 and γ subunits, increasing the affinity of GABA and increasing the frequency with which the channel opens.

• Orexin antagonists block the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R, which is thought to suppress wake drive.

• Zolpidem enhances the activity of γ-GABA via selective agonism at the BZ1 receptor.

• Buspirone is a partial agonist at brain 5-HT1A and 5-HT2 receptors. It also has moderate affinity for brain dopamine D2 receptors.

• Secobarbital binds to specific GABAA receptor subunits at CNS neuronal synapses, facilitating GABA-mediated chloride ion channel opening duration.

Contraindications

• Alprazolam is contraindicated in patients with myasthenia gravis, as benzodiazepines can exacerbate muscle weakness, potentially leading to respiratory depression.

Common Adverse Reactions

• Drowsiness is a common adverse reaction to benzodiazepines like alprazolam, especially shortly after administration.

• Pain at the injection site is not typically associated with alprazolam, as it is usually administered orally.

• Behavioral problems are not commonly reported adverse reactions to alprazolam, but are more associated with clonazepam administration.

• Arrhythmia is not a common adverse reaction associated with alprazolam.

• Diarrhea is not a common adverse reaction to alprazolam.

Antidotes

• Flumazenil is a benzodiazepine receptor antagonist used as an antidote for benzodiazepine overdose.

• Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) antidepressant and is not used as an antidote for benzodiazepine overdose.

• Oxazepam is a benzodiazepine medication used to treat anxiety and alcohol withdrawal symptoms. It is not used as an antidote for benzodiazepine overdose.

• N-acetylcysteine is used as an antidote for acetaminophen overdose and is not effective for benzodiazepine intoxication.

• Naloxone is an opioid receptor antagonist used to reverse opioid overdose and is not effective for benzodiazepine intoxication.

Insomnia Treatment Options

• Flumazenil is not used to promote sleep and may not be suitable for patients with a history of benzodiazepine dependence.

• Tasimelteon is a melatonin receptor agonist used to regulate the sleep-wake cycle in individuals with non-24-hour sleep-wake disorder. It is not typically used for primary insomnia or as a sleep aid in general.

• Amobarbital is a barbiturate medication with sedative effects and not commonly used for insomnia due to its high potential for tolerance, dependence, and overdose.

• Naloxone is an opioid receptor antagonist used to reverse opioid overdose and not used to promote sleep.

• Zolpidem is a non-benzodiazepine sedative-hypnotic medication used to treat insomnia by promoting sleep onset. It is often preferred in cases where benzodiazepines are not desired due to its shorter half-life and lower risk of dependence.

Drug Interactions

• Concomitant use of MAOIs (monoamine oxidase inhibitors) with buspirone can lead to serotonin syndrome, a potentially life-threatening condition. Therefore, combining buspirone with MAOIs is contraindicated.

• There are no specific contraindications for the concurrent use of benzodiazepines with buspirone.

• There are no known contraindications for the concurrent use of buspirone with:

  • vitamin C
  • acetaminophen
  • enalapril

Test your knowledge on the different medication classes used for anxiety and insomnia. This quiz covers benzodiazepines like Alprazolam and Triazolam, as well as non-benzodiazepine options like Zolpidem and Buspirone. Understand their uses, indications, and interactions to enhance your awareness of anxiety treatment options.