2 12

200g

2017 3 8 2017 3 8 2014 3 2014 3

3 3

11

4. 14. 1

224.14.1

200200gg

1212LL

200200gg

18mg18mg

pHpH 4.57.04.57.0

11

66gg //kkgg//1010

0.20.70.20.7gg//kgkg//

6 6gg//kgkg//11000.20.20.0.77gg//kgkg//

11

22

33 0.4g/kg/ 0.4g/kg/0.0.77gg//kgkg//0.0.77gg//kgkg//

44

552mL48mL2mL48mL50mL4g/mL9. 50mL4g/mL9.

12120055

1 1

2 2

12

871129871129

21600AMY0001021600AMY00010

2004 42004 4

2004 52004 5 1999 121999 12

2014 32014 3

2013 62013 6

1

3 3

4 4

5 5

6 6 5.5.

77

8811

2 2 22

3 3

4 4 22

5 5

4. 14. 16 6

77

88

11

2 2

11

22

3344

55

11

224486318631

36.0%36.0%910.5%1112.8%44.7%910.5%1112.8%44.7%102246445.4%102246445.4%21020.5%949.2%21020.5%949.2%616.0%605.9%333.2%616.0%605.9%333.2%242422887755330040.040.0%%121216.016.0%%151520.0%20.0%33

4.04.0%%24241619161923923914.814.873734.5%4.5%60603.7%AST3.7%ASTGOTGOT31311.9%1.9%24241.5%ALT1.5%ALTGPTGPT17171.1%1.1%

20 206616166680.680.6%%885541.341.3%%8844

40.840.8%%660029.129.1%%224411.711.7%%21211010..22%%

11

115%5%

225%5%

335% 5%

440.11%0.11%

550.11%0.11%

6615%15%0.11%0.11%55%%0.10.111%%

22

1%1% 0.11%0.11% 0.1%0.1% 11

AVAV

1%1% 0.11%0.11% 0.1%0.1% 11

AGAGASTAST

GOTGOTALTALT

GPTGPT

-GTP-GTP

NPNNPN

2 2

11

22

11

22

1818

1313AVAV2020AVAV

3

Child-Pugh 6 Grade ABC 0.6g/kg 10CLf 59%51%32%

%

Cmaxng/mL

Cmax, fng/mL

AUC0-nghr/mL

t1/2hr

CLL/hr

CLfL/hr

VssL

Vss, fL

g 39.96.7

89.71.6

0.9010.487

0.1030.016

1.020.28

2.450.47

41.912.7

417.7160.5

119.641.1

1238.7488.6

36.99.0 38.811.7 45.25.1

82.13.8

0.7600.244

0.1360.027

2.030.26

7.451.44

22.42.4

132.934.6

209.240.0

1166.9217.1741.0338.3776.0172.1

102.017.5

247.985.5

31.011.4

3.871.70

1.300.42

0.1200.025

0.9300.319

87.90.9

103.435.3

211.7140.6

27.012.8

5.392.19

1.740.59

0.1230.090

0.8770.498

86.52.0

N=18 N=6 N=7 N=6

S.D.

N=12365

CrCL

J-DEX-99-001

0mg

>0mg50mg

>50mg

0mg

>0mg50mg

>50mg

N=56

N=55

4785.5%

35.5%

59.1%

4887.3%

712.7%

12260.1%

4321.2%

3818.7%

9345.8%

11054.2%

2137.5%

47.1%

3155.4%

4275.0%

1425.0%

PhaseW97-246

N=198

N=203

4723.7%

3015.2%

12161.1%

15075.8%

4824.2%

6

1Fragen R.J. et al. : J.Clin.Anesth. 11: 466-470, 19992Trissel L.A. et al. : Int.J.Pharm. Comp. 6 : 230-233, 20023 : Dexmedetomidine Dose-Ranging

Study to Evaluate the Effects of Dexmedetomidine on Sedation (Caucasian) , 1997

4 : Dexmedetomidine Dose-Ranging Study to Evaluate the Effects of Dexmedetomidine on Sedation in Japanese Subjects, 1999

5 : A Phase I , Single-Center, Open-Label Study Evaluating the Metabolism and Excretion of 3H-Dexmedetomidine in Healthy, Adult Volunteers, 1997

6Pugh R.N. et al. : Br. J. Surg. 60 : 646-649, 19737 : A Phase III, Multi-center,

Randomized, Placebo-Controlled, Double-Blind Study Evaluating the Safety and Efficacy of Dexmedetomidine When Compared to Placebo, With Propofol, For ICU Sedation in Post-Operative Patients, 1998

8DA-9501 2001

9DA-95012009

10DA-95012012

11DA-9501 2012

12 : Gillon J. -Y. et al . : RECEPTOGRAM of Six Compounds, 1992

13Macdonald E. et al. : J.Pharmacol. Exp. Ther. 259 : 848-854, 199114Sabbe M.B. et al. : Anesthesiology 80 : 1057-1072, 199415Cornelis J. J. G. Bol et al. : J. Pharmacol . Exp.Ther. 283 : 1051-

1058, 199716 : ROUX S. et al.: CNS General

Pharmacology Profile in the Mouse and the Rat, 199617Takano Y. et al. : J. Pharmacol. Exp. Ther. 258 : 438-446, 1991

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