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[The inhibition of lidocaine metabolism by various barbiturates in rat hepatic microsome].

Authors
  • Kakinohana, M
  • Taira, Y
  • Kakinohana, O
  • Okuda, Y
Type
Published Article
Journal
Masui. The Japanese journal of anesthesiology
Publication Date
Nov 01, 1998
Volume
47
Issue
11
Pages
1302–1310
Identifiers
PMID: 9852692
Source
Medline
License
Unknown

Abstract

To evaluate the effects of various barbiturates on lidocaine metabolism by cytochrome P-450 (P-450), enzyme kinetics were analyzed in an in vitro study using rat hepatic microsomes. Phenobarbital, amobarbital, hexobarbital, pentobarbital, and thiamylal showed the mixed type inhibition of lidocaine metabolism with inhibition constants being 4.89, 1.08, 2.76, 0.77 and 0.65 mM, respectively. Same as lidocaine, all barbiturates used in the present study, corresponding to binding with P-450, induced the I type of spectral change of P-450. Since these did not affect cytochrome C reductase activity, it was suggested that this inhibition of lidocaine metabolism in hepatic microsomes may have been caused by the reduction of activity on P-450 by the barbiturates.

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