Elimination of brotizolam in elderly patients after multiple doses

Abstract

Plasma brotizolam levels were measured in 5 elderly patients given 0.25 mg daily. The half-life of brotizolam elimination was 6.0 h after a single dose and 6.9 h after continuous administration for 3 weeks. The brotizolam concentration in plasma 2 h after the dose was 3.5 and 3.4 ng/ml, respectively, on the first and last days of the study. Brotizolam levels measured several times during the study 10 h after dosing were between 1.2 and 1.8 ng/ml. Thus, administration of brotizolam 0.25 mg/d to elderly patients for 3 weeks led neither to its accumulation nor to faster elimination. The half-life of brotizolam elimination in elderly patients was in the upper range of that found in young volunteers.

Variables influencing patient satisfaction for hypnotics: difference between zolpidem and brotizolam

“…Our further interests were focused on the difference between satisfied and dissatisfied patients taking the same categorized agents as the short‐acting hypnotics, zolpidem and brotizolam, the most common hypnotics used for patients with insomnia in Japan. As it is known that the pharmacokinetics of zolpidem and brotizolam is affected by gender and age, that is, increased clearance in males taking zolpidem and younger subjects taking brotizolam, these factors may affect amount of sleep and patient satisfaction.…”

Changes in activity patterns after the oral administration of brotizolam in institutionalized elderly patients with dementia

“…Brotizolam is a triazolo‐thieno‐diazepine, a rapidly eliminated benzodiazepine hypnotic with minimal residual daytime effects 5 . Prior studies suggest that the mean half‐life of brotizolam in the elderly is 6.0–9.3 h, generally, and 4.0–19.5 h in those aged 71–93 years 6,7 . Although 0.125‐ to 0.25‐mg brotizolam has been recommended to treat insomnia in the elderly, efficacy and tolerance data show an association between slower elimination, greater drug sensitivity and altered responses 6–8 .…”

“…Prior studies suggest that the mean half‐life of brotizolam in the elderly is 6.0–9.3 h, generally, and 4.0–19.5 h in those aged 71–93 years 6,7 . Although 0.125‐ to 0.25‐mg brotizolam has been recommended to treat insomnia in the elderly, efficacy and tolerance data show an association between slower elimination, greater drug sensitivity and altered responses 6–8 . Moreover, elderly with dementia may have altered drug sensitivity and responses to the drug, and little is known about the effect of brotizolam on elderly with dementia.…”