Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. All treatments were well tolerated during this study, with no serious adverse effects. These results suggest that fimasartan and rosuvastatin have no relevant pharmacokinetic drug-drug interactions. The GMR and 90% CI for the Cmax,ss and AUCτ,ss of rosuvastatin (with/without fimasartan) were 1.090 (0.979 - 1.213) and 0.870 (0.804 - 0.940), respectively. The geometric mean ratio (GMR) and 90% confidence intervals (CI) for the Cmax,ss and AUCτ,ss of fimasartan (with/without rosuvastatin) were 1.109 (0.813 - 1.511) and 1.159 (1.061 - 1.265), respectively. The mean Cmax,ss and AUCτ,ss values of rosuvastatin were 9.94 ± 4.48 ng/mL and 85.29 ± 36.25 ng×h/mL for rosuvastatin alone and 11.94 ± 8.47 ng/mL and 77.33 ± 38.71 ng×h/mL for fimasartan and rosuvastatin coadministration, respectively (p-values for Cmax,ss and AUCτ,ss, 0.066 and 0.009, respectively). The mean Cmax,ss and AUCτ,ss values of fimasartan were 258.03 ± 176.75 ng/mL and 746.52 ± 273.49 ng×h/mL for fimasartan alone, and 289.40 ± 231.44 ng/mL and 848.43 ± 267.45 ng×h/mL for fimasartan and rosuvastatin coadministration, respectively (p-values for Cmax,ss and AUCτ,ss, 0.
1BLOCKER X IPA SERIAL
Serial blood samples were collected for up to 48 hours for fimasartan and for up to 72 hours for rosuvastatin after the last dose of each period to determine the steady-state pharmacokinetics of both drugs. There was a 7-day washout between periods I and II.
In Part B, subjects received rosuvastatin alone, followed by concomitant administration of fimasartan, with the same doses used as in Part A. In part A, subjects received 120 mg of fimasartan alone for 7 days during period I, and 120 mg fimasartan with 20 mg rosuvastatin for 7 days during period II. In this open-label, multiple-dose, two-period, single-sequence study, the enrolled subjects were randomized into two separate parts (A and B). This study evaluated the possible pharmacokinetic interactions between rosuvastatin and fimasartan, an angiotensin II type 1 (AT1) receptor blocker (ARB), approved in Korea for the treatment of mild to moderate hypertension. Multiple doses of fimasartan did not seem to alter the pharmacodynamics or pharmacokinetics of warfarin in this small, select population of healthy male volunteers. The INR values reached 1.93 (0.31) and 1.96 (0.37) at 36 hours and decreased to 4 or reported any symptoms related to hypotension, including fainting or dizziness. Tolerability was assessed via vital sign measurements, physical examinations, ECGs, clinical laboratory tests, and adverse events.Ī total of 15 healthy Korean men aged 20 to 39 years (mean, 26.7 years) and weighing 60.2 to 85.7 kg (mean, 71.4 kg) participated in the study 12 completed the study.
The maximal international normalized ratio (INR) and the AUC-INR curve were evaluated to assess warfarin pharmacodynamics. The plasma concentrations of R- and S-warfarin were analyzed by using HPLC-MS/MS, and the pharmacokinetic parameters were estimated by using noncompartmental analysis. Serial blood samples were collected for 144 hours after each warfarin dose. On day 11, warfarin 25 mg was administered concomitantly with fimasartan. After a 7-day washout period, once-daily fimasartan 240 mg was administered every morning from day 8 to day 16. The subjects were administered a single-dose of warfarin 25 mg on day 1. The aim of this study was to evaluate the effects of fimasartan on the pharmacodynamics and pharmacokinetics of warfarin in healthy volunteers to meet regulatory requirements for drug marketing and labeling in Korea.Īn open-label, 1-sequence, 2-treatment, 2-period crossover study was conducted in healthy male volunteers. Fimasartan is an angiotensin II receptor antagonist used to treat hypertension.
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