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. 2007 Mar 12;151(1):24–34. doi: 10.1038/sj.bjp.0707192

Table 1.

Pharmacokinetic parameters of DA-8159 and DA-8164 after single i.v. administration of DA-8159 at a dose of 30 mg kg−1 without and with simultaneous single i.v. administration of terazosin at a dose of 5 mg kg−1, and of terazosin after single i.v. administration of terazosin at a dose of 5 mg kg−1 without and with simultaneous single i.v. administration of DA-8159 at a dose of 30 mg kg−1 to rats

Parameter DA-8159
 Parameter Terazosin
  Without terazosin With terazosin   Without DA-8159 With DA-8159
DA-8159     Terazosin    
 AUC (μg min ml−1) 514±56.0 553±77.3  AUC (μg min ml−1) 202±27.4 318±70.3a
 Terminal t1/2 (min) 192±70.4 212±69.2  Terminal t1/2 (min) 141±28.2 143±73.0
 MRT (min) 85.3±22.5 101±32.0  MRT (min) 84.3±11.2 157±39.3a
 Vss (ml kg−1) 4630±1520 5160±1430  Vss (ml kg−1) 2020±488 2420±404
 CL (ml min−1 kg−1) 58.4±6.26 54.3±8.61  CL (ml min−1 kg−1) 24.7±3.41 15.5±3.87a
 CLR (ml min−1 kg−1) 3.21±1.27 0.844±1.11b  CLR (ml min−1 kg−1) 6.69±1.65 2.62±2.40c
 CLNR (ml min−1 kg−1) 54.7±4.86 53.0±8.23  CLNR (ml min−1 kg−1) 17.9±2.26 12.1±2.99a
 Ae0–24 h (% of DA-8159 dose) 6.29±1.68 2.37±1.75b  Ae0–24 h (% of terazosin dose) 28.6±2.73 22.7±11.5
 GI24 h (% of DA-8159 dose) 1.46±0.693 0.650±0.418d  GI24 h (% of terazosin dose) 0.245±0.238 0.308±0.242
           
DA-8164
 AUC (μg min ml−1) 113±32.5 115±40.0      
 Terminal t1/2 (min) 134±75.4 124±68.0      
 CLR (ml min−1 kg−1) 0.386±0.0741 0.134±0.117b      
 Cmax (μg ml−1) 0.411±0.294 0.382±0.260      
 Tmax (min) 30 (15–30) 45 (15–120)      
 Ae0–24 h (% of DA-8159 dose) 0.150±0.0534 0.0778±0.0317d      
 GI24 h (% of DA-8159 dose) 0.325±0.255 0.314±0.260      

Abbreviations: Ae0–24 h, percentage of dose excreted in 24 h urine; AUC, total area under the plasma concentration–time curve from time zero to time infinity; CL, time-averaged total body clearance; CLR, time-averaged renal clearance; CLNR, time-averaged nonrenal clearance; Cmax, peak plasma concentration; GI24 h, percentage of dose recovered from the entire gastrointestinal tract (including its contents and feces) at 24 h; i.v., intravenous; MRT, mean residence time; Tmax, time to reach a Cmax; t1/2, half-life; Vss, apparent volume of distribution at steady state.

Data are expressed as mean±s.d. (without terazosin, n=8; with terazosin, n=10 for DA-8159, without DA-8159, n=8; with DA-8159, n =10 for terazosin). Significant difference from without DA-8159

a

P<0.001

c

P<0.01.

Significantly different from without terazosin,

b

P<0.001 and

d

P<0.01.