AIM: To study the simultaneous modeling of pharmacokinetics and pharmacodynamics (PK-PD) of @entity2779 (Pro) in healthy subjects. METHODS: Ten healthy Chinese volunteers, 5 extensive metabolizers (EM) and 5 intermediate metabolizers (IM) of @entity5320 , received a single dose (400 mg) of Pro @entity5209 . The blood samples and electrocardiogram (ECG) measurements were taken after administration over 15 h period. The concentrations of Pro in plasma were measured by a reverse-phase HPLC. PR interval was used as an average value of 10 PR interval measurements. RESULTS: There was a delay between Pro level and percentage of PR interval prolongation. After PK-PD simulating, the relationship between effect concentration (Ce) and the effect met the sigmoid E(max) model. @entity5320 (EM _ IM) played an important role in both pharmacokinetics and pharmacodynamics which produced by Pro. The AUC (microg . h . L-1) of IM group was significantly higher than that of EM group (5126 +/- 1030 vs 2948 +/- 1230, P < 0.05). Whereas Ce50 (microg/L) was also greater in IM group than in EM group (747 +/- 281 vs 359 +/- 123, P < 0.05). On the other hand, gamma of EM group was about one fold larger than that of IM group (P < 0.05). CONCLUSION: @entity5320 phenotype of @entity1 may influence not only pharmacokinetic of Pro but also its pharmacological effects.

Simultaneous modeling of pharmacokinetics and pharmacodynamics of XXXX in healthy subjects.

@entity1 :: ('9606', 'Species') :: ['human'] @entity5209 :: ('CHEBI:36807', 'Chemical') :: ['hydrochloride'] @entity2779 :: ('MESH:D011405', 'Chemical') :: ['propafenone'] @entity5320 :: ('1565', 'Gene') :: ['CYP2D6']
@entity2779 :: (MESH:D011405,Chemical) :: ['propafenone']
