Influence of food and body weight on the pharmacokinetics of penticainide.
The pharmacokinetics of penticainide, a class Ic antiarrhythmic drug, was studied in 16 healthy adults (eight males and eight females) after a single 300-mg oral dose in fasting conditions and with a standard meal. Penticainide concentrations in plasma and urine were measured by hplc. The pharmacokinetic parameters of penticainide including Cmax, tmax, AUC and t1/2 were not significantly altered in the presence of food. AUC values (mean +/- sd) were 50.68 +/- 10.8 mg.h.l-1 and 49.52 +/- 9.87 mg.h.l-1 in the absence and presence of food, respectively. However, a significant difference was observed between males and females in both fasting and fed conditions with a higher value of the apparent oral clearance in the second group. The values of apparent oral clearance, expressed in weight-normalized units were 1.33 +/- 0.35 ml.mn-1.kg-1 (male) and 1.93 +/- 0.34 ml.mn-1.kg-1 (female) in fast conditions (P < 0.01) and 1.38 +/- 0.28 ml.mn-1.kg-1 (male) and 1.93 +/- 0.49 ml.mn-1.kg-1 (female) in fed conditions (P < 0.02), respectively. The pharmacokinetics of penticainide is not modified by the presence of food, but an influence of body weight may be considered.
Berdaï
D
D
Service de Pharmacologie Clinique, EA DRED 525, CHU Pellegrin & Université de Bordeaux 2, France.
Demotes-Mainard
F
F
Philip
F
F
Vinçon
G
G
Montels
R
R
Necciari
J
J
Bannwarth
B
B
D000328:Adult; D000704:Analysis of Variance; D000889:Anti-Arrhythmia Agents / Q000493:pharmacokinetics*; D001835:Body Weight / Q000502:physiology*; D005215:Fasting / Q000378:metabolism; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D011437:Propylamines / Q000493:pharmacokinetics*; D011725:Pyridines / Q000493:pharmacokinetics*; D012737:Sex Factors
D000889:Anti-Arrhythmia Agents; D011437:Propylamines; D011725:Pyridines; C045930:propisomide