Clinical therapeutic recommendation on ziprasidone in treatment of schizophrenia

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1 (Chin J New Drugs Clin Rem) [ ] (2011) ( ; ; ; ; ; ) [ ] ; ; ; [ ] [ ] R749 [ ] A Clinical therapeutic recommendation on ziprasidone in treatment of schizophrenia patients HUANG Ji-zhong 1 JIANG Kai-da 1 SI Tian-mei 2 JIA Fu-jun 3 MEI Qi-yi 4 HAO Wei 5 LI Ling-jiang 5 ZHAO Jing-ping 5 WANG Gang 6 ( 1. Shanghai Mental Health Center Shanghai Jiaotong University School of Medicine SHANGHAI China; 2. Institute of Mental Health Peking University BEIJING ; 3. Guangdong General Hospital Guangdong Provincial Institute of Mental Health Guangzhou GUANGDONG China; 4. Suzhou Guangji Hospital Suzhou JIANGSU China; 5. Institute of Mental Health the Second Xiangya Hospital of Centre South University Changsha HU-NAN China; 6. Beijing An Ding Hospital BEIJING China) [KEY WORDS] ziprasidone; schizophrenia; drug therapy; therapeutics [ ABSTRACT] Schizophrenia is a group of disabling brain diseases with complex clinical manifestation devasted personal and social functioning and chronic course. The patients with schizophrenia are usually required long-term antipsychotics treatment. Up to date the second generation antipsychotics ( SGAs) become the first line chioce of the treatment of schizophrenia duo to their broad spectrum treatment targets benign adverse [ ] [ ] [ ] (1961 ) Phn: junghjz@yahoo.com.cn

2 642 (Chin J New Drugs Clin Rem) reactions and social function improvement. Ziprasidone an novel SGAs medication has utilized in clinical practice for 5 years in China and remarkably improved positive symptoms negative symptoms cognitive impairment and affective symptoms in the treatment of the schizophrenia. Compared with the other SGAs the application of ziprasidone require the clinicians to prehension more systematic knowledge of psychopharmacology and therapeutics. 10 1% - 2 : (1) 5-HT 2A / D 2 (2) 5-HT 2C / D 2 ; 5-HT 2C (DA) (NE) DA NE (3) 5-HT 1A / D 2 [1-5] 1 (4) 5-HT 1D 6 ~ 8 h 1 ~ 3 d (5) 99% 1.5 L kg -1 NE 5-20 mg 60% HT (6) 2 (t 1 /2 ) α 1 H 1 7 h 7.5 ml min -1 kg-1 (< 1%) (< 4%) 3 4 : (BITP) BITP- S- - M 1 20% 66% 44% H 1 P450 (CYP450) CYP3A4 CYP1A2 1 / 3 CYP450 M 1 ; α 1 H FDA

3 (Chin J New Drugs Clin Rem) [1 6 7] ( 2.3 ) ( ) ( ) [6 7] 1 2 : 2.4 [ ] [1 6] 2.1 / / 1 [ ] d ( mg d -1 ) : 120 mg d -1 (BPRS) 30% 48.8% 40 mg d -1 (37.2%) [2 6 8] 2.2 (25.5%); (CGI-S) 1 2 : (1) 33.3% 20.9% 12.8% 294 ; (2) ; (3) 1 ( 6% 35%)

4 644 (Chin J New Drugs Clin Rem) ) ( ) 10 ( ) [10-12] ~ 80 mg d -1 1 wk 120 ~ 160 mg d -1 1 ~ 2 wk [ ] mg d ~ 160 mg d -1 1 wk 120 mg d ~ 200 mg d -1 2 ; 120 ~ 160 mg d mg d mg 80 mg; 5-HT 2C (2 ~ 6 mg d -1 ) (4 ~ 12 mg d -1 ) / [ ] 1.3 ( ) 40 ~ 80 mg d -1 1 wk ( ) 160 ~ 200 mg d -1 2 ; 60 ~ 80 mg 80 ~ 120 mg; ; β- ; (2 ~ 6 mg d -1 ) 3 ~ 4 wk 120 ~ 200 mg d -1 β- (20 ~ 60 mg d -1 ) (

5 (Chin J New Drugs Clin Rem) % 11% / 40 ~ 80 mg d -1 4 ~ 7 d 120 ~ 200 mg d -1 (2 ~ 6 mg d -1 ) (4 ~ 12 mg d -1 ) ( ) β- (20 ~ 60 mg d -1 ) β- β- 10 ~ 40 mg d : 1 ~ 2 wk ( ) 3 wk ( ) : [2 7 11] 2.2 ( ) 24.8% 2 [9 12] ~ 2 wk

6 646 (Chin J New Drugs Clin Rem) (120 ~ 200 mg d -1 ); 1 ~ 2 wk ; 1 ~ 2 wk ; 2 ; ; β- ; ; 1 ~ 2 wk 2 5-HT 2A 5- HT 2C ( D 2 ) 2 ; ROSSI 10 ( ) β- - 1 wk (3 ~ 7 d) 60 ~ 80 mg bid d mg bid; d ~ 80 mg bid; d 7 2 ~ 4 wk β- : (1) ; (2) ; (3) ( / ( ) ); (4) ( CYP450 ( ) ); (5) - ( ) /

7 (Chin J New Drugs Clin Rem) [13-17] 2.4 ) (100 mg d -1 ( ) DA 5-HT NE [ ] 5-3 HT DA DA 5-HT / DA (FDA) ; 10 ~ 17 / ( ) (Cochrane )

8 648 (Chin J New Drugs Clin Rem) α- ) QTc QT ( QT QT ) QT ( ) a (levacetylmethadol) QTc 500 ms QTc 3 : ( ) ( ) [ ] ( ) 1 ( ) β- ; (BMI < 23) ( 2 QTc QT QRS T 4 QT QT QT QT QTc QTc QTc

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