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Chapter 184: Nonbenzodiazepine Sedatives

Frank LoVecchio

INTRODUCTION

The term sedative-hypnotic refers to any drug designed to produce sedation and sleepiness. These drugs can be divided into the benzodiazepines (see Chapter 183, “Benzodiazepines”) and nonbenzodiazepines (Table 184-1).

TABLE 184-1Nonbenzodiazepine Sedative-Hypnotics
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TABLE 184-1 Nonbenzodiazepine Sedative-Hypnotics
Name Recommended Initial Adult Dose (oral; milligrams) Recommended Maximum Adult Daily Dose (milligrams) Time to Peak Plasma Levels Elimination Half-Life
Buspirone 5 three times a day 60 40–90 min 2–3 h
Carisoprodol 250–350 four times a day 1400 1.5 h 2 h
Chloral hydrate 500–1000 Typically single dose 30 minutes before procedure 30 min 4 min for chloral hydrate and 6–10 h for trichloroethanol
γ-Hydroxybutyrate See text See text 30–60 min 0.3–1 h
Melatonin 0.2–5 qhs 5–10 30–60 min 40–50 min
Meprobamate 400 TID or QID 2400 3.6 h 10 h
Ramelteon 8 qhs 8 45 min 1–2.6 h
Tasimelteon 20 qhs 20 0.5–3 h 1.3 h
Zaleplon 5 qhs 20 0.7–1.4 h 0.9–1.2 h
Zolpidem 5 qhs 10 1–2 h 1.4–4.5 h
Zopiclone* 7.5 qhs 7.5 1.5–2 h 5–6 h
Eszopiclone 1 qhs 3 1–1.5 h 6–7 h

Abbreviations: qhs = at bedtime; QID = four times per day; TID = three times per day.

*Not available in the United States.

One is most likely to encounter toxicity from these sedative drugs as part of accidental or nonaccidental overdose, as well as after an assault or trauma. Many nonbenzodiazepines were developed and are marketed for the treatment of insomnia, anxiety, and sedation.1 Other agents with sedative effects, including antihistamines (e.g., diphenhydramine, doxylamine), antidepressants (e.g., amitriptyline, trazodone, mirtazapine), and antipsychotics (e.g., quetiapine), are also used to promote sleep.

Three sedative agents used in the past have been removed from the legal U.S. and Canadian markets: ethchlorvynol, glutethimide, and methaqualone. However, via Internet sites, these drugs are available to North American customers from locations in Eastern Europe, Africa, Asia, and South America.2

BUSPIRONE

Buspirone is approved by the U.S. Food and Drug Administration for treatment of anxiety disorders.3 Off-label uses include treatment of depression and nicotine dependence. Buspirone is a partial agonist at the serotonin-1A receptor and an antagonist of the dopamine-2 receptor. The resultant effect on serotonin and dopamine neurotransmitter levels is complex, depending on the concentration of the drug and specific brain location, but overall effects are primarily suppression of CNS serotonergic activity and enhancement of dopaminergic and, possibly, noradrenergic activity.

Following ingestion, absorption is rapid and nearly complete, with significant first-pass metabolism in the liver (primarily via oxidation) resulting in a low bioavailability. Metabolism of buspirone (by cytochrome P3A4) produces several metabolites, including one active metabolite. Primary elimination is renal, with additional substantial fecal elimination.

Common adverse effects seen with buspirone include sedation, GI discomfort, vomiting, and dizziness. In therapeutic dosing, buspirone does not ...

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