当前位置： SCI文献检索 > EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS期刊下所有文献 > Pharmacokinetics of nefazodone in the dog following single oral administration.

Pharmacokinetics of nefazodone in the dog following single oral administration.

Abstract：

:The pharmacokinetics of nefazodone (NEF) and two of its pharmacologically active metabolites viz hydroxynefazodone (HO-NEF) and m-chlorophenylpiperazine (mCPP) were determined following single oral administration of 100, 200 and 400 mg NEF to 6 beagle dogs in a three-way crossover study. Blood samples were collected for 48 h and plasma was analyzed for NEF, HO-NEF and mCPP by a validated HPLC assay. NEF was rapidly absorbed after oral administration. Cmax values for all three compounds and AUCinf values for HO-NEF and mCPP were dose-proportional; AUCinf values for NEF were dose-linear but not dose-proportional. The T1/2 values for NEF and HO-NEF following the 400 mg dose were significantly greater than those for the 100 mg dose. No differences in mCPP T1/2 were observed among the doses. The Cmax and AUCinf ratios for metabolite:NEF were about 2-fold lower for the 200 and 400 mg doses than those observed for the 100 mg dose. However, due to extensive variability, the ratios for three doses were not significantly different based on statistical analysis. Overall, these data suggest the pharmacokinetics of NEF are dose-dependent in the beagle dog. Statistical significance for dose-dependency for many of the pharmacokinetic parameters could not be demonstrated due to high variability associated with the plasma concentration vs time profiles.

journal_name

Eur J Drug Metab Pharmacokinet

journal_title

European journal of drug metabolism and pharmacokinetics

authors

Shukla UA,Marathe PH,Labudde JA,Pittman KA,Barbhaiya RH

doi

10.1007/BF03190163

keywords:

subject

Has Abstract

pub_date

1992-10-01 00:00:00

pages

301-8

issue

4

eissn

0378-7966

issn

2107-0180

journal_volume

17

pub_type

杂志文章

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