Metabolism of Flurazepam, a Benzodiazepine, in Man and Dog

Schwartz, Morton A.; Postma, Edward

doi:10.1002/jps.2600591220

Cited by 61 publications

(19 citation statements)

References 4 publications

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“…Impaired performance after nitrazepam persisted throughout the next day, but with flurazepam hydrochloride a rapid recovery of performance was observed after 16 hours. Unlike nitrazepam, enhanced performance on the third day was not observed after flurazepam hydrochloride and, as with heptabarbitone, it is suggested that this was related to the more rapid metabolism of the drug (Schwartz & Postma, 1970).…”

Section: Discussionmentioning

confidence: 93%

Comparison of the residual effects of two benzodiazepines (nitrazepam and flurazepam hydrochloride) and pentobarbitone sodium on human performance.

Borland¹,

Nicholson²

1975

Brit J Clinical Pharma

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1 The residual effects of two benzodiazepines, nitrazepam (10 mg) and flurazepam hydrochloride (30 mg), and pentobarbitone sodium (200 mg) were studied by adaptive tracking and by reaction time. Performance was measured at 10 h, 13 h, 16 h, 19 h and 34 h after ingestion of each drug. Impaired performance on adaptive tracking was observed at 10 h, 13 h, 16 h and 19 h after nitrazepam and pentobarbitone sodium and at 10 h, 13 h and 16 h after flurazepam hydrochloride. Enhanced performance was observed at 34 h after nitrazepam and pentobarbitone sodium. 2 Increased reaction time persisted to 16 h after nitrazepam, flurazepam hydrochloride and pentobarbitone sodium and reaction time was also increased at 34 h after nitrazepam and pentobarbitone sodium. 3 During the morning immediately after ingestion, the subjects as a group were able to differentiate correctly between placebo and drugs, but they were not able to assess accurately the persistence of the residual effects of nitrazepam and pentobarbitone sodium. 4 Flurazepam hydrochloride would appear to be a more promising benzodiazepine than nitrazepam for use as a hypnotic by persons involved in skilled activity. There was a rapid recovery of performance during the afternoon and, unlike pentobarbitone sodium and nitrazepam, subjects retained the ability to recognize impaired skill.

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Section: Discussionmentioning

confidence: 93%

Comparison of the residual effects of two benzodiazepines (nitrazepam and flurazepam hydrochloride) and pentobarbitone sodium on human performance.

Borland¹,

Nicholson²

1975

Brit J Clinical Pharma

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“…Radioimmunoassay Specificity-The specificity of the antiserum initially was evaluated by cross-reactivity studies involving all of the flurazepam metabolites known to be present in plasma (3). The monoand didesethyl metabolites exhibited a cross-reactivity of 17 and 3.7%, respectively, while the other possible competitors cross-reacted less than 1% (Table I).…”

Section: Resultsmentioning

confidence: 99%

Radioimmunoassay of flurazepam in human plasma

Glover

Barley

Delaney

et al. 1980

Journal of Pharmaceutical Sciences

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“…Clazepam's major plasma metabolite (II) carries, like flurazepam's (Schwartz & Postma, 1970), a primary alcohol group which makes it considerably more hydrophilic than clazepam itself and accounts for rapid urinary excretion. Indeed, its half-life during the plasma distribution phase is 90 min and over twothirds of total 24-h excretion of (II) takes place within the first 4 h. In contrast, (III) is a highly lipophilic molecule which accounts for its prolonged stable concentration in the plasma.…”

Section: Discussionmentioning

confidence: 99%

Clazepam: pharmacokinetics and effects on performance.

Jf¹,

Berdeaux²,

Idrissi³

et al. 1978

Brit J Clinical Pharma

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I The effects of clazepam, a new benzodiazepine (30 mg orally) on performance tests and the cardiovascular system have been compared to those of chlordiazepoxide (30 mg orally) and a placebo in a double-blind trial involving six healthy volunteers. Simultaneously, the pharmacokinetics of clazepam were investigated. 2 While clazepam itself could be detected neither in plasma nor in urine, it gave rise to two plasma metabolites, the former, an alcoholic derivative with a short half-life, and the second, desmethyldiazepam, with a long half-life. These two metabolites and oxazepam were excreted in urine and, within the 24 h period following drug intake, accounted for 73% of the ingested dose. 3 Seven hours after its administration, clazepam slightly improved performance and reduced anxiety. The kinetics of these effects and the metabolic data suggest that clazepam acts mainly through the formation of desmethyldiazepam. However, owing to the low blood levels of this metabolite, the activity of clazepam was very moderate.

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Metabolism of Flurazepam, a Benzodiazepine, in Man and Dog

Cited by 61 publications

References 4 publications

Comparison of the residual effects of two benzodiazepines (nitrazepam and flurazepam hydrochloride) and pentobarbitone sodium on human performance.

Comparison of the residual effects of two benzodiazepines (nitrazepam and flurazepam hydrochloride) and pentobarbitone sodium on human performance.

Radioimmunoassay of flurazepam in human plasma

Clazepam: pharmacokinetics and effects on performance.

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