Single dose pharmacokinetics and pharmacodynamics of oral loprazolam in the elderly.

Swift, CG; Swift, M.R.; Ankier, S. I.; Pidgen, A W; Robinson, Joseph D.

doi:10.1111/j.1365-2125.1985.tb05041.x

Cited by 45 publications

(12 citation statements)

References 31 publications

(22 reference statements)

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“…1977b, Triggs et af. 1975: Moreover, this result is in accordance with the results of Swift et al (1985), in both young and elderly healthy volunteers, following administration in the morning after an overnight fast. There was considerable inter-subject variability between the times to peak concentration, which is not uncommon with benzodiazepines.…”

Section: Discussionsupporting

confidence: 86%

Pharmacokinetics of loprazolam and its principal metabolite in young subjects and elderly hospital patients

Ford

Ankier²,

Corless

et al. 1987

Xenobiotica

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1. The pharmacokinetics of loprazolam and its principal pharmacologically active metabolite, the piperazine N-oxide, were compared in young subjects (aged 21-25 years) and elderly patients (aged 63-86 years) following single oral evening doses (0.5 mg and 1 mg). 2. Plasma loprazolam was assayed by a specific h.p.l.c./g.c. method. The N-oxide metabolite was assayed by gas chromography. 3. Mean times to peak plasma concentration of loprazolam did not differ significantly between young and elderly subjects and ranged from 1.6-2.7 h. There was, however, a longer mean time to peak concentration of the N-oxide metabolite in the elderly but this was only statistically different after the 0.5 mg dose (4.5 mg young, 6.4 h elderly). 4. Mean peak plasma concentrations of loprazolam did not differ significantly between young and elderly nor did plasma concentrations of the N-oxide metabolite. 5. Although the mean elimination half-life of loprazolam was not statistically significantly different between young and elderly subjects (range 10.9-16.0 h) there was a trend towards somewhat longer half-lives in the elderly. Furthermore, there was a small but significant increase in the half-life of the N-oxide metabolite in the elderly after the 1 mg dose from 11.7 h to 16.7 h. 6. The areas under the plasma concentration time curves for both loprazolam and its N-oxide were greater in the elderly being some 50-68% (mean 132.0 and 111.5 ng/ml h) above those found in young subjects (mean 89.8 and 66.0 ng/ml h).(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Discussionsupporting

confidence: 86%

Pharmacokinetics of loprazolam and its principal metabolite in young subjects and elderly hospital patients

Ford

Ankier²,

Corless

et al. 1987

Xenobiotica

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“…In a series of experimental trials, Swift et al have found that benzodiazepines impair reaction time and postural sway in elderly people [10,11]. In a previous case-control study of factors associated with injurious falls we also found associations between psychoactive medication use and quadriceps strength, postural sway and two clinical balance measures: static and dynamic balance [12].…”

Section: Introductionmentioning

confidence: 59%

Psychoactive medication use, sensori‐motor function and falls in older women.

Lord

Anstey

Williams

et al. 1995

Brit J Clinical Pharma

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and number of medical conditions. Use of any two psychoactive medications was also significantly associated with falling frequency (Chi-square = 13.91, df = 1, P < 0.01). 4 Path analysis revealed a significant direct association (P < 0.001) between psychoactive medication use and falls, and a significant indirect association mediated via reduced physiological functioning (P < 0.001). Postural hypotension was not significantly associated with falls (RR = 1.37, 95% CI = 0.84-2.22). 5 The findings suggest that psychoactive medication use may predispose older people to falling by impairing important sensori-motor systems that contribute to postural stability.

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“…Following a single dose administration of loprazolam (0.5 mg and 1.0 mg) elderly and young adults did not differ significantly on Tmax nor on peak plasma concentrations of the drug, whereas T and area under the curve were significantly greater among the elderly, possibly reflecting slowing in drug metabolism and reduced hepatic clearance, or other age-related effects [60]. Residual effects (11 h after bedtime administration) for loprazolam 1.0 mg were significant on a standing steadiness test, but not on tests of critical flicker fusion nor on choice reaction time.…”

Section: Loprazolammentioning

confidence: 82%

Effects of Sleep Medications on Cognition, Psychomotor Skills, Memory and Driving Performance in the Elderly

Verster¹,

Volkerts²,

Spence

et al. 2007

CPSR

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Sleep disturbances occur more often in the elderly than in patients in any other age category. Traditional treatment regimens for insomnia in older patients have emphasized benzodiazepines. The useful anxiolytic and hypnotic properties of these agents have made them the most widely prescribed class of drugs in the world. Concern has been expressed however about the significant side effect profile associated with these agents. There is now considerable evidence that all benzodiazepines show significant dose-dependent impaired daytime performance on a variety of memory, cognitive and psychomotor tests. In addition, the risk of falls, hip fractures, and traffic accidents is significantly increased in patients who are treated with benzodiazepines. There is little evidence that benzodiazepine hypnotics are still effective after chronic use. On the other hand, several impairments persist when using these hypnotics over long time. Recently, the nonbenzodiazepine drugs zolpidem and zaleplon have been introduced and are claimed to be relatively safe (i.e. less daytime sedation) when compared to benzodiazepines. Zopiclone, a non-benzodiazepine hypnotic, shows no advantages over benzodiazepines with respect to daytime performance.Several factors may interact with the effects of hypnotics on daytime functioning, including normal cognitive decline during aging, the effects of insomnia itself on daytime functioning, the presence or absence of co-morbid disorders, and pharmacokinetic changes accompanying aging. The impact of hypnotics on daytime performance further depends on various drug-related factors including the administered dose, half-life, time between intake and performance, duration of treatment, gender, and individual differences.In contrast, zolpidem and zaleplon do not significantly impair daytime performance when administered at bedtime at the recommended dose. Although further studies of drug effects in elderly insomniacs are necessary, the available evidence suggests that these short acting and relatively safer non-benzodiazepine hypnotics are a preferred alternative therapy for treating insomnia in the elderly.

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Single dose pharmacokinetics and pharmacodynamics of oral loprazolam in the elderly.

Cited by 45 publications

References 31 publications

Pharmacokinetics of loprazolam and its principal metabolite in young subjects and elderly hospital patients

Pharmacokinetics of loprazolam and its principal metabolite in young subjects and elderly hospital patients

Psychoactive medication use, sensori‐motor function and falls in older women.

Effects of Sleep Medications on Cognition, Psychomotor Skills, Memory and Driving Performance in the Elderly

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