Identification of Urinary Metabolites of Befunolol in Dog and Man principally by Mass Spectrometry

Tohno, Masao; Kimura, Kazuhiko; Nagahara, Michiko; Sakai, Yasuo; Ofuji, Tatsuya; Nadai, Tanekazu

doi:10.1248/yakushi1947.99.9_944

Cited by 6 publications

(1 citation statement)

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“…Some examples are loxoprofen (Tanaka et al, 1983;Noguchi et al, 2005), befunolol (Tohno et al, 1979), and acetohexamide ( Fig. 12A) (McMahon et al, 1965).…”

Section: Carbonyl Reductases/aldo-keto Reductasesmentioning

confidence: 99%

Cytochrome P450 and Non-Cytochrome P450 Oxidative Metabolism: Contributions to the Pharmacokinetics, Safety, and Efficacy of Xenobiotics

Foti

Dalvie

2016

Drug Metabolism and Disposition

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The drug-metabolizing enzymes that contribute to the metabolism or bioactivation of a drug play a crucial role in defining the absorption, distribution, metabolism, and excretion properties of that drug. Although the overall effect of the cytochrome P450 (P450) family of drug-metabolizing enzymes in this capacity cannot be understated, advancements in the field of non-P450-mediated metabolism have garnered increasing attention in recent years. This is perhaps a direct result of our ability to systematically avoid P450 liabilities by introducing chemical moieties that are not susceptible to P450 metabolism but, as a result, may introduce key pharmacophores for other drug-metabolizing enzymes. Furthermore, the effects of both P450 and non-P450 metabolism at a drug's site of therapeutic action have also been subject to increased scrutiny. To this end, this Special Section on Emerging Novel Enzyme Pathways in Drug Metabolism will highlight a number of advancements that have recently been reported. The included articles support the important role of non-P450 enzymes in the clearance pathways of U.S. Food and Drug Administration-approved drugs over the past 10 years. Specific examples will detail recent reports of aldehyde oxidase, flavin-containing monooxygenase, and other non-P450 pathways that contribute to the metabolic, pharmacokinetic, or pharmacodynamic properties of xenobiotic compounds. Collectively, this series of articles provides additional support for the role of non-P450-mediated metabolic pathways that contribute to the absorption, distribution, metabolism, and excretion properties of current xenobiotics.

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“…Some examples are loxoprofen (Tanaka et al, 1983;Noguchi et al, 2005), befunolol (Tohno et al, 1979), and acetohexamide ( Fig. 12A) (McMahon et al, 1965).…”

Section: Carbonyl Reductases/aldo-keto Reductasesmentioning

confidence: 99%

Cytochrome P450 and Non-Cytochrome P450 Oxidative Metabolism: Contributions to the Pharmacokinetics, Safety, and Efficacy of Xenobiotics

Foti

Dalvie

2016

Drug Metabolism and Disposition

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Clinical pharmacology of a new ?-adrenoceptor blocking drug, befunolol

Ebihara

Tawara

et al. 1982

Eur J Clin Pharmacol

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Repeated doses of a new beta-adrenoceptor blocking agent, befunolol, were administered orally to adult male volunteers for a cross-over comparison with propranolol. The beta-adrenoceptor blocking activity of befunolol was greater than that of propranolol when assessed by the percentage reduction in exercise-induced tachycardia. The elimination half-life of drug was significantly prolonged on repeated administration of propranolol, but not of befunolol. The percentage reduction in exercise-induced tachycardia was highly correlated with the log plasma level of each drug. Both drugs produced a significant reduction in pre-exercise systolic and diastolic blood pressure, and significant attenuation of exercise-induced rise in systolic blood pressure.

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Reduction of drug ketones by dihydrodiol dehydrogenases, carbonyl reductase and aldehyde reductase of human liver

Ohara

Miyabe

Deyashiki

et al. 1995

Biochemical Pharmacology

152

114

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Identification of Urinary Metabolites of Befunolol in Dog and Man principally by Mass Spectrometry

Cited by 6 publications

References 0 publications

Cytochrome P450 and Non-Cytochrome P450 Oxidative Metabolism: Contributions to the Pharmacokinetics, Safety, and Efficacy of Xenobiotics

Cytochrome P450 and Non-Cytochrome P450 Oxidative Metabolism: Contributions to the Pharmacokinetics, Safety, and Efficacy of Xenobiotics

Clinical pharmacology of a new ?-adrenoceptor blocking drug, befunolol

Reduction of drug ketones by dihydrodiol dehydrogenases, carbonyl reductase and aldehyde reductase of human liver

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