Kinetic analysis of propranolol‐induced impairment of its own metabolism in rats

NORIKO KAGIMOTO, YASUHIRO MASUBUCHI, SHOICHI FUJITA, SHIZUO NARIMATSU, TOKUJI SUZUKI

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Abstract

Abstract— The effect of repetitive oral administration of propranolol (100 mg kg−1 day−1, 5 days) on the kinetics of liver microsomal propranolol metabolism was investigated in the rat. Vmax values of the high‐affinity phase for biphasic kinetics of propranolol 4‐ and 5‐ hydroxylase activities were decreased by propranolol pretreatment, while those of the low‐affinity phase were unchanged. The Vmax value of monophasic 7‐hydroxylase activity was also decreased. On the other hand, the Vmax value of N‐desisopropylase activity in the propranolol‐treated rats was increased more than 2‐fold compared with non‐treated (control) rats, resulting in a change from monophasic in control rats to biphasic kinetics in propranolol‐treated rats. These findings indicate that repetitive administration of propranolol selectively impairs a CYP2D isozyme that is involved in the high‐affinity phases for propranolol ring‐hydroxylations. 1994 Royal Pharmaceutical Society of Great Britain

Original languageEnglish
Pages (from-to)528-530
Number of pages3
JournalJournal of Pharmacy and Pharmacology
Volume46
Issue number6
DOIs
Publication statusPublished - Jun 1994

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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    KAGIMOTO, NORIKO., MASUBUCHI, YASUHIRO., FUJITA, SHOICHI., NARIMATSU, SHIZUO., & SUZUKI, TOKUJI. (1994). Kinetic analysis of propranolol‐induced impairment of its own metabolism in rats. Journal of Pharmacy and Pharmacology, 46(6), 528-530. https://doi.org/10.1111/j.2042-7158.1994.tb03846.x