Non-benzodiazepines

Non-benzodiazepines are distinct from benzodiazepines in their therapeutic uses. They treat anxiety disorders such as generalized anxiety disorder (also called GAD) effectively, without the risk of dependence. This classification of medications does not increase the effects of CNS depressants, such as alcohol, benzodiazepines, etc., and they have no misuse potential.

Prototype and Other Medications

The prototype medication for non-benzodiazepines or miscellaneous anxiolytics is buspirone.

Expected Pharmacologic Action

Buspirone works to reduce anxiety by binding to serotonin and dopamine receptors in the brain, and increases norepinephrine metabolism in the brain. It doesn’t bind at all to receptors for GABA like the benzodiazepines do. It seems buspirone’s anti-anxiety effects are due to its inhibition of serotonin reuptake and its agonistic actions on dopamine receptors. As a result of its distinctive activity, it doesn’t cause sedation, doesn’t interact with other CNS depressants, and doesn’t pose a risk for dependence and misuse.

Adverse Drug Reactions

The non-benzodiazepine buspirone can cause paradoxical effects, such as insomnia, anxiety, and restlessness. It also has the potential to cause gastrointestinal upset, in particular nausea. Headache, dizziness, and lightheadedness are also possible effects, but, in general, clients tolerate this medication well.

Interventions

For clients taking buspirone, monitor for paradoxical effects, such as an increase in anxiety. Also monitor for gastrointestinal effects, such as nausea, and for any dizziness, lightheadedness, or headache. It’s essential to take precautions that help prevent falls and other injuries following administration in case dizziness occurs. This is especially crucial for older clients, who might have other risk factors for falling.

Administration

Give buspirone orally on a regular basis for anxiety, not PRN. Begin medication therapy 2 to 4 weeks before tapering benzodiazepines due to the delayed therapeutic effect of buspirone. It can take a week for the first manifestations of effectiveness to manifest and several more weeks for therapeutic effects to reach a peak level.

Client Instructions

Make sure clients taking buspirone report any occurrences of paradoxical, gastrointestinal, or CNS effects. For nausea, suggest that they take the medications with food. For dizziness or lightheadedness, advise them to rise slowly from a reclining or sitting position and avoid participating in activities that require mental alertness. For headache, suggest that they try an over-the-counter analgesic.

Contraindications and Precautions

The only real contraindication for buspirone use is a previous hypersensitivity reaction to the medication. Use it with caution in clients who have liver or kidney insufficiency. Concurrent use with MAO inhibitors can cause severe hypertension.

Interactions

MAOI antidepressants that clients take within 2 weeks of buspirone may cause severe hypertension. Grapefruit juice, erythromycin (an antibiotic), and ketoconazole (an anti-fungal) can also interact with buspirone.

Safety Alert

Erythromycin, ketoconazole, and grapefruit juice can increase the blood levels of buspirone. Clients may become excessively drowsy or report feeling “spacey” if the serum buspirone level is too high.