Hypnotic activity of an imidazo‐pyridine (zolpidem).

Abstract

1 Effects of an imidazo-pyridine (zolpidem: 10, 20 and 30 mg) on overnight sleep and on performance the next day were studied in young adults and in middle aged individuals. The young adults were used particularly as an homogenous group to establish any possible adverse effects of the drug on sleep and on performance the next day, and the middle aged subjects with their less restful sleep were used to study efficacy. 2 In the young adults zolpidem led to a marked increase in slow wave sleep with a reduction in stage 2 sleep. There were no significant changes in REM sleep, though there was a tendency for REM sleep to be delayed. 3 In the middle aged there was a reduction in awake activity and drowsy sleep with an increase in stage 2 sleep. The latency to REM sleep was increased but the duration of REM sleep over the whole night was not reduced. 4 Digit symbol substitution and a complex reaction time task were used to study performance, but there were no residual effects with zolpidem (9 h after ingestion). 5 Zolpidem is likely to prove useful in the management of transient and short-term insomnia in healthy middle aged individuals when impaired performance the next day is to be avoided.

Daytime wakefulness following a bedtime oral dose of zolpidem 20 mg, flunitrazepam 2 mg and placebo.

“…Although the 10 mg dose of zolpidem is the commonly marketed dose in France, and clinical data have shown this dose to be the first active one (Monti, 1989;Nicholson & Pascoe, 1986;Oswald & Adam, 1988), the choice of zolpidem dosage in this study was directed by the facts that other data have shown the 20 mg dose to be more effective (Weintraub et al, 1988), and, in general practice, that increasing the dose to 20 mg is recommended in case of inadequate response.…”

“…Zolpidem is a new imidazo(1-2a)pyridine derivative with potent hypnotic activity in animals and humans (Depoortere et al, 1988;Nicholson et al, 1986). Although chemically unrelated to benzodiazepine compounds, zolpidem was shown to bind with affinity to the omega 1 site of the macromolecular complex which includes the chloride channel and the GABA A receptor (subtype 1 benzodiazepine) (Langer et al, 1988).…”

Operator Functional State Assessment (L'evaluation de l'aptitude operationnelle de l'operateur humain)

“…Total sleep time (TST) has been shown to be increased by zolpidem at doses of 5, 10, 15, and 20 mg compared to placebo (Walsh et al, 1988), at doses of 7.5, 10.0 and 20.0 mg , and at a 30 mg dose (Nicholson & Pascoe, 1986, 1988. Zolpidem reduces the number of awakenings during sleep at doses of 20 and 30 mg (Nicholson & Pascoe, 1986, 1988 and at doses as low as 7.5 mg .…”

“…Total sleep time (TST) has been shown to be increased by zolpidem at doses of 5, 10, 15, and 20 mg compared to placebo (Walsh et al, 1988), at doses of 7.5, 10.0 and 20.0 mg , and at a 30 mg dose (Nicholson & Pascoe, 1986, 1988. Zolpidem reduces the number of awakenings during sleep at doses of 20 and 30 mg (Nicholson & Pascoe, 1986, 1988 and at doses as low as 7.5 mg . Sleep efficiency (total sleep time/time in bed) has been found to increase across a range of zolpidem doses (5-20 mg, Koshorek et al, 1988;Vogel, Thurmond, MacIntosh, & Clifton, 1988); 20 and 30 mg, Nicholson & Pascoe, 1986, 1988 Nicholson & Pascoe, 1986, 1988, whereas the REM sleep amount was reduced by zolpidem at doses of 15 mg , 20 mg Merlotti et al, 1988;Nicholson & Pascoe, 1986, 1988, and 30 mg (Nicholson & Pascoe, 1986, 1988.…”

Electrochemical Study of Zolpidem at Glassy Carbon Electrode and Its Determination in a Tablet Dosage Form by Differential Pulse Voltammetry

“…3,4) Many analytical methods have been published for the determination of zolpidem based on high-performance liquid chromatography (HPLC) combined with ultraviolet, 5) fluorescence 6,7) and with photodiode-array detection, 8) gas chromatography-nitrogen phosphorus detection, 9) gas chromatography-mass spectrometry, 10,11) capillary electrophoresis with laser-induced fluorescence detection 12) and radioimmunoassay. 13) However, to our knowledge no information about the electrochemical redox properties of zolpidem and its analytical application has appeared in the literature.…”