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.