Section 7
Chapter 6,094

Pharmaco kinetics and pharmacodynamics of flurazepam in man 2. investigation of the relative efficacy of flurazepam dealkyl flurazepam and placebo under steady state conditions

Amrein, R.; Bovey, F.; Cano, J.P.; Eckert, M.; Ziegler, W.H.; Coassolo, P.; Schalch, E.; Burckhardt, J.

Drugs under Experimental and Clinical Research 9(1): 85-99


ISSN/ISBN: 0378-6501
Accession: 006093520

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In a 4-day double-blind, placebo-controlled, cross-over study, 8 healthy volunteers received an initial loading dose of 6.6 mg desalkylflurazepam i.v., followed by either 30 mg flurazepam p.o. [orally] or 1.8 mg desalkylflurazepam [benzodiazepine hypnotics] i.v. on subsequent 3 days. On the average, only 5% of orally administered flurazepam is metabolized to desalkylflurazepam. The effect of flurazepam can be described as the sum of the pharmacological effects of flurazepam, hydroxyethylflurazepam and desalkylflurazepam. Under steady-state conditions, the elimination half-life of the desalkyl metabolite is only one of many factors influencing efficiency and performance during the day. There was no indication that, after chronic administration of 30 mg flurazepam, performance and vigilance were influenced during the day. Under steady-state conditions, the clinical state and the results of the psychometric test scores returned to the baseline level within 6-8 h after each medication.

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