A review, with 9 references, describing the pharmacokinetics and pharmacodynamics of the propafenone analog diprafenone, a sodium channel antagonist with β-blocking properties.It is local anesthetic and combined class Ic and class II antiarrhythmic activities.

1997-02-01·Die Pharmazie

Enantioselective determination of diprafenone in human plasma.

Article

作者: Zhong, D ; Fieger-Büschges, H ; Chen, R ; Blume, H

A sensitive (10.0 ng/ml) and stereoselective HPLC method for analysis of S(-)- and R(+)-diprafenone in human plasma has been developed. The assay is based on derivatization with homochiral R(-)-1-(1-naphthyl)ethyl isocyanate to give the diastereomeric derivates and their separation and quantitation using HPLC with UV-detection (220 nm). Details of this stereoselective assay procedure which has already been applied to the multisample analyses from a human pharmacokinetic study are described. The data obtained indicated that the stereoselective disposition of diprafenone enantiomers is quite different from their structural and pharmacological analog propafenone.

1996-06-03·European Journal of Clinical Pharmacology3区 · 医学

Influence of food on the bioavailability and some pharmacokinetic parameters of diprafenone - a novel antiarrhythmic agent

3区 · 医学

Article

作者: R.-G. Alken ; R. Koytchev ; I. Smith ; M. Greenwood ; O. Mayer

OBJECTIVEThe present study was done to investigate the effect of food on the bioavailability of diprafenone.METHODSThe most important pharmacokinetic parameters (Cmax, t1/2, AUC) and the relative oral availability of a solid oral preparation of racemic diprafenone were investigated when administered to fasting subjects and 10 min after a standard meal, in an open, randomised, crossover trial. Single oral doses of 100 mg were given on two different occasions, at least 1 week apart. The serum concentrations of diprafenone and its hydroxy-metabolite were determined up to 24 hours after administration by a sensitive, specific HPLC method. Fifteen healthy, male volunteers were enrolled in the trial. Their mean height, weight and age were 183 cm, 80 kg and 22 years, respectively. Fourteen volunteers were found to be rapid hydroxylators and one was a slow hydroxylator of debrisoquine. Only data from the rapid hydroxylators were used in the statistical analysis.RESULTSFood increased the oral bioavailability of diprafenone by approximately 50%. This effect was similar in rapid and in slow hydroxylators. The only slow hydroxylator in this trial had an AUCzero-last ratio (with food/fasting) of 1.54. These findings suggest that diprafenone should be administered in a constant temporal relationship to food.

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适应症	最高研发状态	国家/地区	公司	日期
室性心律失常	临床3期	-	Bayer AG	-
室性心律失常	临床3期	-	Astellas Pharma, Inc.	-
室性心律失常	临床3期	-	Helopharm W. Petrik GmbH & Co. KG	-
室性心律失常	临床3期	-	C.H. Boehringer Sohn AG & Co. KG	-