Section 7
Chapter 6,094

Pharmaco kinetics and pharmacodynamics of flurazepam in man 1. pharmaco kinetics of dealkyl flurazepam and intra venous injection in comparison with orally administered flurazepam

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

Drugs under Experimental and Clinical Research 9(1): 77-84


ISSN/ISBN: 0378-6501
Accession: 006093519

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The pharmacokinetics of desalkylflurazepam and hydroxyethylflurazepam were studied in 10 healthy volunteers following an i.v. injection of 12 and 20 mg, respectively. For the comparison with flurazepam [a benzodiazepine hypnotic] the subjects received 60 mg flurazepam orally. Blood samples were taken over the first 192-h period after medication. The volume of distribution of desalkylfurazepam ranged from 0.38 and 0.45 l/kg BW [body weight] (median: 0.41 l/kg BW). The half-life (t1/2) of elimination was 40-103 h (median: 72 h) and the plasma clearance was 5.84-9.57 ml/min (median: 7.76 ml/min). The t1/2 of elimination of hydroxyethylflurazepam was short, from 0.88 to 1.1 h (median: 1.0 h). The plasma clearance was 798 and 1791 ml/min (median: 1106 ml/min) and the volume of distribution ranged from 1.2 to 2.3 l/kg BW (median: 1.4 l/kg BW). The systemic availability of desalkylflurazepam and hydroxyethylflurazepam after oral intake of 60 mg flurazepam was 4.0-6.9 and 5.5%, respectively.

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