Zaleplon indications

Distribution - Zaleplon is a lipophilic compound with a volume of distribution of approximately 1.4 L/kg following IV administration, indicating substantial... 

Duration of therapy Because sleep disturbances may be the presenting manifestation of a physical or psychiatric disorder, initiate symptomatic treatment of insomnia only after careful evaluation of the patient. The failure of insomnia to remit after 7 to 10 days of treatment may indicate the need for evaluation of a primary psychiatric or medical illness. Do not prescribe zaleplon in quantities exceeding a 1-month supply. 

The data on zaleplon to date indicate that it has some advantages over other hypnotics, including a favorable safety profile, as indicated by the absence of rebound insomnia and withdrawal symptoms when zaleplon is discontinued (162). In addition, when taken by a nursing mother, zaleplon is transferred through breast milk to her infant in such very small quantities that this is unlikely to be important ( 163). 

The volume of distribution of zaleplon has been determined to be 1.27 1/kg, or 90 1 for a 70-kg person. This large volume of distribution indicates extensive distribution to extravascular tissue, which is not uncommon for lipophilic compounds such as zaleplon. 

The pharmacokinetics of zaleplon in elderly subjects is not significantly different from that in young healthy subjects [38]. Nevertheless, Drover [39] contends that this conclusion may indicate a lack of adequate studies in this area. As described earlier, zaleplon is metabolized primarily by the liver and undergoes significant presystemic metabolism. Consequently, the oral clearance of zaleplon is reduced, and the drug effect is prolonged in patients with hepatic impairment [40]. The clearance of zaleplon is not altered in patients with mild to moderate renal insufficiency [40] (Tab. 3). 

Although many health care providers have been misled by drug company promotional efforts, the great majority of sleep aids share the same risks as the BZs (see the appendix for a list). Almost all are placed in Schedule IV by the DEA to indicate a risk of abuse and dependence. According the DEA (2006), Ambien and Sonata (zaleplon) are benzodiazepine-like CNS depressants. ... 

Diazepam is better indicated if insomnia is associated with daytime anxiety. Other benzodiazepines prescribed for insomnia include nitrazepam, flur-azepam, loprazolam, lormetazepam and temazepam. The non-benzodiazepine hypnotics zaleplon, zolpidem and zopiclone are not licensed for long-term use. The sedative antipsychotic promethazine hydrochloride is sometimes used to facilitate sleep, with a 25-50 mg recommended dose. Melatonin has proved effective for some clients, mostly in regulating the sleep/waking cycle. Although evidence of efficacy is limited, some clients use herbs such as valerian and chamomile. If Mr AB will finally be diagnosed with depression, a trial with an antidepressant will be indicated. 

Three doses of zaleplon have been compared with placebo in outpatients with insomnia in a 4-week study (11). During week 1, sleep latency was significantly shorter with zaleplon 5, 10, and 20 mg than with placebo. The significant reduction in sleep latency persisted to week 3 with zaleplon 10 mg and to week 4 with zaleplon 20 mg. Compared with placebo, zaleplon 10 mg and 20 mg also had significant positive effects on sleep duration, number of awakenings, and sleep quality. Pharmacological tolerance did not develop with zaleplon and there were no indications of rebound insomnia or withdrawal symptoms after discontinuation. There was no significant difference in the frequency of adverse events with zaleplon compared with placebo. The authors concluded that zaleplon provides effective treatment of insomnia with a favorable safety profile. 

Zaleplon is a sedative and hypnotic that interacts with the gamma-aminobutyric acid-receptor complex. It is indicated in the short-term treatment of insomnia. 

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