Topic
Fosazepam
About: Fosazepam is a research topic. Over the lifetime, 8 publications have been published within this topic receiving 142 citations.
Papers
Journal Article•
TL;DR: A review is given of the pharmacokinetics of the major benzodiazepines presently available and suggests that compounds with long elimination half-lives of parent drug or active metabolites are of advantage in anticonvulsant and anti-anxiety treatment.
Abstract: Among the various benzodiazepines large differences exist with regard to their pharmacokinetic properties and metabolism in man. Some are eliminated from the body at a relatively slow rate (e. g. diazepam), others are metabolized rather rapidly (e. g. oxazepam, temazepam, triazolam). Several benzodiazepines have the long-acting metabolite N-desmethyldiazepam in common (diazepam, fosazepam, prazepam, clorazepate). Such differences may be very important clinically because pharmacokinetic factors will determine the duration of drug effect and pharmacokinetic parameters constitute the basis for a rational dosage regimen. For the various clinical indications of benzodiazepines the required duration of drug action differs quite fundamentally. In anticonvulsant and anti-anxiety treatment continuous treatment is pursued, so that compounds with long elimination half-lives of parent drug or active metabolites are of advantage. If on the other hand a benzodiazepine is taken as a hypnotic, the duration of action should be restricted to the night, hence a compound with a short elimination half-life is to be preferred. A review is given of the pharmacokinetics of the major benzodiazepines presently available.
55 citations
TL;DR: Fosazepam administration improved subjective sleep quality, sleep was less broken, slow wave sleep stages 3 and 4 diminished in duration and so did REM sleep, suggesting action of a long half-life metabolite.
Abstract: 1 Six volunteers of mean age 59 years received placebo for week, then fosazepam (60 mg) nightly for 3 weeks, then placebo for 3 weeks. Subjective ratings and all-night electrophysiological recordings were made. 2 Fosazepam administration improved subjective sleep quality nut impaired feelings of morning vitality. Its withdrawal was associated with anxiety, impaired concentration and continuing impairment of morning vitality. Measured sleep duration increased on fosazepam, sleep was less broken, slow wave sleep stages 3 and 4 diminished in duration and so did REM sleep. 3 Despite the short-life of fosazepam some drug effects persisted for several days after withdrawal, suggesting action of a long half-life metabolite.
39 citations
TL;DR: Subjects reported an improved sense of well-being during the day after ingestion of diazepam and fosazepam, and with foszepam they reported improved sleep.
Abstract: 1 The effect of diazepam (5 mg and 10 mg), and fosazepam (60 mg and 80 mg), a soluble derivative of diazepam, on sleep was studied in six healthy adult males using electroencephalography for sleep measures, and analogue scales for subjective assessments of well-being and sleep quality. The effect of diazepam was limited to the night of ingestion, but the effect of fosazepam was carried over to the next night and so modified sleep for about 30 h after ingestion.
2 Effects on total sleep time were limited to the night of ingestion. There were increases with diazepam (10 mg) (P = 0.05), and with fosazepam (60 mg and 80 mg) (P = 0.001). For the night of ingestion sleep onset latencies were shortened, and awakenings were reduced by both drugs. The latency to stage 3 was shortened by fosazepam (60 mg and 80 mg) (P = 0.05).
3 The low and high dose of each drug reduced the duration (min) of stage 0 sleep (P = 0.01), but fosazepam also reduced the duration (min) of stage 1 sleep (P = 0.001), and there was an increase in stage 2 sleep (P = 0.01). With fosazepam there were carry over effects to the next night with reduction of stage 1 sleep (P = 0.05). There were no effects on the duration of stage 3, but there was evidence that stage 4 activity was reduced during the recovery night after ingestion of fosazepam (80 mg). No effects were observed on REM sleep.
4 Subjects reported an improved sense of well-being during the day after ingestion of diazepam and fosazepam, and with fosazepam they reported improved sleep. Correlations were calculated for sleep measures and subjective assessments.
37 citations
TL;DR: The drugs were equipotent in maintaining sleep but nitrazepam had more side effects than the other hypnotics, and it induced a rebound insomnia after withdrawal.
Abstract: Efficacy and side effects of flurazepam 15 mg, fosazepam 60 mg, and nitrazepam 5 mg were studied in 17 psychogeriatric patients. The drugs were equipotent in maintaining sleep but nitrazepam had more side effects than the other hypnotics, and it induced a rebound insomnia after withdrawal. All hypnotics lost some of their efficacy towards the end of 7 days' administration. Patients with evident cerebrovascular disease were vulnerable to the side effects of the benzodiazepine hypnotics. The side effects did not correlate with the age of a patient. In addition, no correlations were found between the serum levels of fosazepam or its main metabolite and the side effects.
14 citations
9 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 1980 | 1 |
| 1979 | 1 |
| 1978 | 1 |
| 1977 | 3 |
| 1976 | 2 |