Zolpidem modified-release in insomnia

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Zolpidem modified-release in insomnia

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Author(s): Cynthia Kirkwood ¹ , Jason Neill ² , Ericka Breden ³

Publication date (Print): October 2007

Journal: Neuropsychiatric Disease and Treatment

Publisher: Dove Medical Press

Keywords: zolpidem modified-release, hypnotics, insomnia

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Abstract

Zolpidem modified-release (MR) is the first hypnotic agent to be marketed in an extended-release formulation. Zolpidem MR is a two-layered, biphasic release tablet indicated for the management of induction of sleep and sleep maintenance. The pharmacokinetics of the drug are similar to those of immediate-release zolpidem. Two double-blind, placebo-controlled, parallel-group trials demonstrated efficacy in adults and elderly patients treated with zolpidem MR for 3 weeks without significant impairment in next-day psychomotor functioning. The most common adverse effects with zolpidem MR were dizziness, somnolence, and headache. A starting dose of zolpidem MR 12.5 mg is recommended for adults and 6.25 mg for elderly patients.

Most cited references 28

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Medical and socio-professional impact of insomnia.

Emile Levy, Damien Leger, M Paillard … (2002)

Insomnia, a highly prevalent disorder with direct and indirect economic and professional consequences, affects daytime functioning, behavior, and quality of life. Several studies have shown that insomnia affects the workforce and is associated with an increased risk of accidents. Insomnia may also play a role in other disorders. Our study attempted to evaluate the socio-professional correlates of insomnia by comparing a group of insomniacs to a group of good sleepers. With a questionnaire focused on the socio-professional and medical consequences of insomnia, we surveyed a group of severe insomniacs and a group of good sleepers. Persons with psychiatric disorders according to the DSM-IV minimum criteria for anxiety and depression were eliminated from each group. After screening, 240 insomniacs and 391 good sleepers remained and were then compared. Compared to good sleepers, severe insomniacs reported more medical problems, had more physician-office visits, were hospitalized twice as often, and used more medication. Severe insomniacs had a higher rate of absenteeism, missing work twice as often as did good sleepers. They also had more problems at work (including decreased concentration, difficulty performing duties, and more work-related accidents). Our study showed that insomnia has socio-professional consequences and is correlated with lower medical status.

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Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications.

J. Barreiro Guimarães da Costa, P Salvà (1995)

Zolpidem is an imidazopyridine which differs in structure from the benzodiazepines and zopiclone. It is a strong sedative with only minor anxiolytic, myorelaxant and anticonvulsant properties, and has been shown to be effective in inducing and maintaining sleep in adults. The available evidence suggests that zolpidem produces no rebound or withdrawal effects, and patients have experienced good daytime alertness. Zolpidem 10mg in non-elderly and a reduced dose of 5mg in elderly individuals are clinically effective. In humans, the major metabolic routes include oxidation and hydroxylation; none of the metabolites appears to be pharmacologically active. The pharmacological activity of zolpidem results from selective binding to the central benzodiazepine receptors of the omega 1 subtype. Zolpidem is approximately 92% bound to plasma proteins; absolute bio-availability of zolpidem is about 70%. After single 20mg oral doses, typical values of pharmacokinetic variables for zolpidem in humans are: a peak plasma concentration of 192 to 324 micrograms/L occurring 0.75 to 2.6 hours postdose; a terminal elimination half-line of 1.5 to 3.2 hours; and total clearance of 0.24 to 0.27 ml/min/kg. Zolpidem pharmacokinetics are unchanged during multiple-dose treatment. Zolpidem pharmacokinetics are not significantly influenced by gender. Clearance of zolpidem in children is 3 times higher than in young adults, and is lower in very elderly people. There are no significant differences in the pharmacokinetic parameters between various racial groups. Dosage reduction appears to be prudent in patients with renal disease, and caution should be exercised when prescribing zolpidem to elderly patients with hepatic impairment. Coadministration of haloperidol, cimetidine, ranitidine, chlorpromazine, warfarin, digoxin or flumazenil do not alter the pharmacokinetics of zolpidem; flumazenil predictably antagonises the hypnotic effects of zolpidem. Alertness tends to be reduced when cimetidine is combined with zolpidem. Volunteers treated with imipramine plus zolpidem developed anterograde amnesia.

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Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives: zaleplon, zolpidem and zopiclone.

David Drover (2003)

Benzodiazepines have historically been the mainstay of treatment for sleeping disorders, yet they have many shortcomings. A new group of sedative hypnotic agents has been developed for this purpose. Similar to the benzodiazepines, zaleplon, zolpidem and zopiclone have activity at the GABA receptor complex, yet they appear to have more selectivity for certain subunits of the GABA receptor. This produces a clinical profile that is more efficacious with fewer side effects. Zaleplon, zolpidem and zopiclone are structurally distinct. Due to variation in binding to the GABA receptor subunits, these three compounds show subtle differences in their effect on sleep stages, and as antiepileptics, anxiolytics and amnestics. The duration of action of zaleplon, zolpidem and zopiclone can be related to their individual pharmacokinetic profile, which subsequently determines the time course of drug effect. Each of these compounds has a unique pharmacokinetic profile with different bioavailability, volume of distribution and elimination half-lives. Zaleplon has a rapid elimination so there are fewer residual side effects after taking a single dose at bedtime. By comparison, zolpidem and zopiclone have a more delayed elimination so there may be a prolonged drug effect. This can result in residual sedation and side effects but may be useful for sustained treatment of insomnia with less waking during the night. There are also differences in potency based on plasma concentrations suggesting that there are differences in binding to the GABA receptor complex. Although zaleplon has a much lower bioavailability (30%), the treatment dose is similar to zolpidem and zopiclone (bioavilaibility of 70%) because of the increased potency of zaleplon. The pharmacokinetics and pharmacodynamics of zaleplon, zolpidem and zopiclone are significantly different from benzodiazepines. The new drugs are sufficiently unique from each other to allow customisation of treatment for various types of insomnia. While zaleplon may be best indicated for the delayed onset of sleep, zolpidem and zopiclone may be better indicated for maintaining a complete night's sleep. Only the patient's symptoms and response to treatment will dictate the best course of treatment.

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Author and article information

Journal

Journal ID (nlm-ta): Neuropsychiatr Dis Treat

Journal ID (publisher-id): Neuropsychiatric Disease and Treatment

Title: Neuropsychiatric Disease and Treatment

Publisher: Dove Medical Press

ISSN (Print): 1176-6328

ISSN (Electronic): 1178-2021

Publication date (Print): October 2007

Volume: 3

Issue: 5

Pages: 521-526

Affiliations

[1 ] Department of Pharmacy

[2 ] School of Pharmacy, Virginia Commonwealth University

[3 ] Virginia Commonwealth University Medical Center, Richmond, VA, USA

Author notes

Correspondence: Cynthia Kirkwood, Department of Pharmacy, School of Pharmacy, Virginia Commonwealth University, Box 980533, 410 North 12th Street, Smith Room 454, Richmond, VA, 23298-0533, USA, Tel +1 804 828 8318, Fax +1 804 828 8359, Email ckkirkwo@ 123456vcu.edu

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Publisher ID: ndt-3-521

PMC ID: 2656288

PubMed ID: 19300582

SO-VID: eacd1659-097c-4134-9304-ac9cfcbc6c36

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Zolpidem modified-release in insomnia

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Abstract

Most cited references 28

Medical and socio-professional impact of insomnia.

Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications.

Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives: zaleplon, zolpidem and zopiclone.

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