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Abstract

The effect of the cytochrome P-450 suicide inactivator, 1-aminobenzotriazole, on the in vivo metabolism and pharmacologic activity of flurazepam.

S Capello, L Henderson, F DeGrazia, D Liberato, W Garland and C Town
Drug Metabolism and Disposition March 1990, 18 (2) 190-196;
S Capello
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L Henderson
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F DeGrazia
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D Liberato
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W Garland
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C Town
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Abstract

Flurazepam (F) is an extensively prescribed hypnotic (Dalmane) whose in vivo activity has been suggested to be due to its primary metabolites, hydroxyethyl flurazepam (HEF) and N-desalkylflurazepam (DAF). In order to determine the intrinsic pharmacologic activity of F, mice were administered various doses of the cytochrome P-450 suicide inactivator, 1-aminobenzotriazole (ABT), 1 hr before the ip administration of 1 mg/kg 14C-F. One hr after 14C-F, 70 mg/kg pentylenetetrazole was administered iv and the mice were observed for convulsions. F alone offered no protection from convulsion (mean brain concentrations were 3.9, 32, and 11 ng/g for F, DAF, and HEF, respectively). F with 25 mg/kg ABT also offered no protection despite a 6-fold increase in brain concentrations of F. F with 100 mg/kg ABT offered a 57% protection from convulsions (mean brain concentrations were 99, 62, and 41 ng/g for F, DAF, and HEF, respectively). One mg/kg F with 400 mg/kg ABT offered 100% protection from convulsions (brain concentrations were 190, 47, and 18 ng/g for F, DAF, and HEF, respectively). These data indicate that F has intrinsic pharmacologic activity which must be considered when evaluating the pharmacodynamics of F.

 

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Drug Metabolism and Disposition
Vol. 18, Issue 2
1 Mar 1990
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Abstract

The effect of the cytochrome P-450 suicide inactivator, 1-aminobenzotriazole, on the in vivo metabolism and pharmacologic activity of flurazepam.

S Capello, L Henderson, F DeGrazia, D Liberato, W Garland and C Town
Drug Metabolism and Disposition March 1, 1990, 18 (2) 190-196;

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Abstract

The effect of the cytochrome P-450 suicide inactivator, 1-aminobenzotriazole, on the in vivo metabolism and pharmacologic activity of flurazepam.

S Capello, L Henderson, F DeGrazia, D Liberato, W Garland and C Town
Drug Metabolism and Disposition March 1, 1990, 18 (2) 190-196;
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