Multiple-dose pharmacokinetics of the new H1-receptor antagonist tazifylline in healthy volunteers.
The multiple-dose pharmacokinetics of the new H1-receptor antagonist, tazifylline, were investigated in healthy volunteers. From single-dose data, tazifylline appeared to be rapidly absorbed (median tmax of 0.6 h) and eliminated (t1/2 = 1.0 +/- 0.2 h). However, plasma levels measured on days 3 and 8 of the multiple-dose regimen (10 mg b.i.d. for 8 days) indicated moderate accumulation. A two-compartment model best described multiple-dose data with a terminal half-life of 15.6 +/- 7.6 h consistent with twice-daily dosing of tazifylline.
Bruno
R
R
Recherche Syntex France, Montlhery.
Jullien
I
I
Auger
J
J
Iliadis
A
A
Dow
R
R
McEwen
J
J
Cano
J P
JP
Pinhas
H
H
D000328:Adult; D002851:Chromatography, High Pressure Liquid; D006634:Histamine H1 Antagonists / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D013806:Theophylline / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics
D006634:Histamine H1 Antagonists; D013806:Theophylline; C048398:tazifylline