AMX - database.japic.or.jp

1 580662-15. 580661-15. 580673-15. 580663-15. 2018 4 ( 12 ) . 2015 4 . 871179.. 2mg 22000 AMX00011 2008 4 2008 4 . ) 4mg 22000 AMX00012 2008 4 2008 4 . 2008 1 . 8mg 22100 AMX02285 2010 4 2010 4 . 2 22000 AMX00013 2008 4 2008 4 . ) . ( ).. (1) . (2) .. (3) ( 1 4mg 1 2 . ) 1 8.. (4) ( ) ( 16mg 2 . 1 24mg . ) HIV ( .. ) (1) .. (5) .. 2mg 4mg . 1 2mg 1 4mg (2) .. 1. ( ). (1) .. DS DS (2) . 032 2 033.. (3) . (mm) (mm) (mg) (mm) (mm) (mg) . 60 120 (4) . DS032 DS033 . (5) . 8mg 2 (6) . 1 8mg 1g 20mg .. (7) .. (8) .. (9) . (10).

2 (Syndrome malin) . 2.. (1) .. (mm) (mm) (mg) . 240 (2) . DS035 .. (3) . 1 . C Y P3A4 ( . HIV ) CYP3A4 . ( ) .. ( ) ( ( CYP3A4 . ) C Y P3A4 ) . ( . ) . (4) ( . ) . ( ( . ) ) . ( AUC.. ) 17 Cmax .. ( 1 3 . ( ) ) . (5) (4) HIV .. ( ) . ( . ). ( ) . ( ). (6) ( . ).. ( .. ). ( . 3. ). CYP3A4 ( . ). (1) ( ) . ( ).. ( . ). ( ( . - ). ) . ( ) - (2) ( ).. - .. CYP3A4 .. AUC . Cmax .. 2 .. 7) ( ). CYP3A4 .. AUC 8) ( ). Cmax AST(GOT) ALT(GPT) -GTP ALP .. CYP3A4 (2) ( ). CYP3A4 .. CYP3A4 . CYP3A4 .. (3) .. 5 . 4. 5 . ( .. ). 891 673 ( ).

3 ( 1). ( ) . ( ) ( ) ( ) . ( ) ( ) ( ) . (1) (QT T .. 1) (Syndrome malin)(5 ) ) . ( 2).. ( . CK(CPK) ( .. ). ) . 2) (5 ) ( 3) ( ) . ( .. ). AST(GOT) ALT(GPT) . 3) ( ) -GTP LDH ALP . ( .. ) .. ( ) .. 4) (SIADH)( ).. (SIADH) .. 5) ( ).. CK(CPK) .. 6) ( ).. 3 . 5 . 5 (3) ( ) . ( .. ).. (4) ( ) 104 .. (1mg/kg/ ) .. (1mg/kg/ ) .. 1.. (1) ( ). ( 8 1 ).. Tmax Cmax t1/2 AUClast (mg) (h)a) (ng/mL)b) (h)b) (ng h/mL)b).. 4 (1 3) . 8 ( 2) .. 12 (1 3) a) ( - ) b) . CK(CPK) (ng/mL). 1. 4mg 8mg 12mg .. BUN . BUN .. 0 10 20 30 40 50.

4 1 . (h).. 2 (2) ( ). 3 Cmax AUC0-12 . Tmax 5. (MRT) . (kel) . ( 12 2mg 1 ). Tmax Cmax AUC0-12 MRT kel . 6. (h) (ng/mL) (ng h/mL) (h) (1/h). (1) .. (ng/mL).. (2) . ( ) .. 7.. 8.. PTP PTP .. PTP .. 9. 0 2 4 6 8 10 12. (1) (h). (2) ( . ) 17 .. 4 . (3) ( ) . 10 1 2mg 1 2 ( )10 .. Tmax Cmax t1/2 AUC0-12 (8 24mg) ( 2 6mg . (h)a) (ng/mL)b) (h)b) (ng h/mL)b) 4 12mg) 1 2 . 2 (2 2) (Positive and Negative Syndrome Scale;. PANSS) 1 . a) ( - ) b) . PANSS . ( ) 1 4mg 1 8 ( 7) ( =10 ) . 16mg 24mg . 2. ( ). 3) 4). 84 ( ). 3.. (in vitro 10ng/mL 2 g/mL ) PANSS a).

5 4. ( ) (156) (144) (114) (111). N- (in vivo 1 95 1/25).. 7,8 . ( / ) (79/155) (81/143) (74/121) (60/117). ( ). 95 N- . ( ) 1 N- a) . N- . 3 .. 5. (1) (2)5) (3)6). 0 a)(2/51) a)(15/61) a)(79/321). ( )6 14C- 4mg 2 28 (22/29) (36/48) (137/264). ( . 59 30 / ) 52 56 (12/17) (33/38) (86/155). (29/48) (41/60) (153/318). ( a) . 5 ) . 6.. P-450 CYP3A4( N- 1.. ) . 7.. ED ED50(mg/kg). 1) . ( 12 2mg ) ( ) . Tmax Cmax t1/2 AUClast . ED50 ED50 (h)a) (ng/mL)b) (h)b) (ng h/mL)b) ( )7) .. ( )7). 2(1 3) . c) 3(2 3) ( ED 3 ED 1 3 . a) ( - ) b) )8).

6 C) 7 1,200mg/ ( 4) . 300mg . ED 1 . 2) ( )8) . ( 12 2mg ).. Tmax Cmax t1/2 AUClast ED50 ED50 ( ) . (h)a) (ng/mL)b) (h)b) (ng h/mL)b).. 2(1 3) ED 1 . ( )7) . c) (1 6) .. a) ( - ) b) ( ED 3 ED 1 3.. c) 60 200mL )7). ( . ED50 ED50 ( ) )7) . SKF38393 10mg/kg/day . ( )12 ED 3. ( )7) . Tmax Cmax t1/2 AUClast ED ED50 50 . (h)a) (ng/mL)b) (h)b) (ng h/mL)b) 2.. 3(1 5) In vitro D2 . c) (2 5) (D2 D3) 5-HT2A . N- D2 . a) ( - ) b) (D2 D3) 5-HT2A . c) 7 400mg/ . D2 .. 1/10 N- 5-HT2C . ( ) 1 4mg 1 8 5-HT6 . 16mg 24mg N- 1 . H1 M1 7).

7 5 .. Blonanserin 2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophe nyl)-5,6,7,8,9,10- hexahydrocycloocta[b]pyridine . CH2CH3. N. N N. F. C23H30FN3. (100) . ( ) . 123 126 .. 2mg PTP 100 (10 10). 4mg PTP 100 (10 10) 1,000 (10 100). 1,000 . 8mg PTP 100 (10 10) 1,000 (10 100). 1,000 . 2 100g . 1) , 11 891, 2008. 2) , 11 901, 2008. 3) , 11 297, 2008. 4) , 10 2059, 2007. 5) , 10 2241, 2007. 6) , 11 135, 2008. 7) , 10 1263, 2007. 8)Noda, Y. et al. : J. Pharmacol. Exp. Ther., 265 745, 1993.. 541-0045 2-6-8.. r . 6.