1、 r9O i# “5il沙维伟, 刘进文, 周朝昀, 张晓斌(vD D * S, , 225003)K 1: “ 4 F r9O i,) “5ilbZE 56 *s 3a4a5 mg,4 HPLC r9O ib -# 4| V( PANSS) bT Y g 4 #9O iiAsb3a4a5 mgF9O 0 iiAs, 4 9O iAM1b4 9O iPANSS9shs q AM17s Vshs qAM1b 9O i g 4 1, o g 4 #9O i 3, n5 b1oM: ; 9O ;0 i; *s ms |: R 74913 DS M : A cI|: 1672O2353( 2004)
2、06O0036O03PLASMA 9OHYDROXYRISPRRIDONE LEVEL OFRISPERIDONEcS ACTIVE METABOLITE ANDITS CLINICAL SIGNIFICANCESHA WeiOwei, LIU JinOwen, ZHOU ChaoOyun, ZHANG XiaoObin( Department of Psychiatry, Affiliated Yangzhou Wutaishan Hospita of Medical College ofYangzhou University , Yangzhou, Jiangsu 225003)ABSTR
3、ACT: Objective To observe the relationship among oral dose, plasma drug level andthe clinical significance of risperidone. Methods The study w as conducted in 56 patients w ithschizophrenia. They were divided to receive 3 m g, 4 mg or 5 mg risperidone for 4 w eeks. T heplasma drug levels of 9Ohydrox
4、yrisperidone w ere measured by H PLC method at the end of Week 4.The PANSS w ere evaluated at Week 1 and 4. Results T he difference of oral dose of risperidoneand plasma levels of 9Ohydroxyrisperidone were significant between male and female patients. T heplasma levels of 9Ohydroxyrisperidone were s
5、ignificantly different among the 3 mg, 4 mg and 5 mggroup. The oral dose of risperidone w as significant positive correlated w ith the plasma levels of 9Ohydroxyrisperidone. The plasma level of 9Ohydroxyrisperidone w as not correlation w ith the de-creased rate in PANSS total scores but w as signifi
6、cant positive correlation w ith the decreased rate inpositive scores. Conclusions The oral dose of risperidone was correlated w ith the plasma level of 9Ohydroxyrisperidone. T he oral dose of risperidone and the plasma level of 9Ohydroxyrisperidonewere low er in female patients than that in male pat
7、ients so risperidone can improve the patientcspositive sym ptoms firstly.KEY WORDS: risperidone; 9Ohydroxyrisperidone; plasma drug level B5O s8 Ed F *h0,.d F *h0M1, *s |“ rT, OQ bl : 2004- 07- 11 “: 8 g?Z “( “I|: 040350)Te: ( 1963- ) , 3, , V 3, D =bL “5D0# 36 # Journal of Clinical Medicine in Pract
8、ice 2004 M8 6 8 0 s#r 4 s v, Ya 4 9O i# r1“,T r9O i ,C|T /b1 “5 ZE111 一般资料2003 M10 2004 M9 l56 *s , (S *%hs ZS *s , M -( 3416 ? 1217) ,| V( PANSS) s 60sb x8%h#0 N, -T F *h01; h h f 0 s f sY 3 mga4 mg#5 mgFb3 mgF19 , 36, o13 , M -( 3719 ? 1517) ,8( 5817 ?815) kg; 4 mgF23 , 39 , o14 , M-( 3412 ? 1017)
9、 ,8( 6016 ? 1012) kg; 5 mgF14 , 39 , o5 , M -( 3416 ? 1217),8( 5919 ? 1016) kgb3F M -#8M1 (Asb112 方法 S4 ( Y015mg/Q, 2Q/ d, 3d (1 mg/Q, 2Q/ d; 1sY93a4a5 mg/ db W F *h0, 4 a ib 0,8“Q i&Z #l4 M :b4 16 B0 0 | 4 ml , (3 000 r/ min) , |- 25 ebQ ibH PLCE r9O 0 ib Hq: WatersrAM “d,cWaters1525,aWaters7171“ a
10、Waters2487_ ,Breeze“d ) ,|q C 1 8( 2 5 0nm ,416 Lm) , MJ?O ( 65B35) ,FY A5ml, pH715b_o280nm,4 0 e ,K_K015 ngb s ,9O = HW418 min, 9O ( l q( 9718 ? 318) %, 9O v 4b| V( PANSS) *,TESS NQbSPSS 1010 qt_aF_#PartialM1sb2 T211 不同性别的利培酮剂量及9O羟利培酮血浆浓度比较 324 , o32 , g 4: 3( 4115 ? 0188) mg, o( 3166 ?0177) mg, P
11、b HT?C4 3F9O iPANSSVy0shs qM1, 9O 1rs, “5 n5 b g4 9O i1“ sy Y, B4 0i8sv, Norio 6?C% P450 ( CYP) CYP2D6 ylMCYP2D6 Y,Y 9O ibyN “5 7Z9O i_ “5ilb ID 1 M artin D, Almila E, Mohandel M , et al. Effectiveness of an-tipsychotic treatments for schizophrenia: interim 6Omonthanalysis from a prospective observa
12、tion study ( ICOSOHO )comparing olanzapine, quetiapine, risperidone and haloperidolJ . J Clin Psychiatry, 2004, 65( 3) : 312.2 Bork J A, Rogers T , Wedlund P J, et al. A pilot study onrisperidone metabolism: the role of cytochromes P4502D6 and3A J . J Clin Psychiatry. 1999, 60( 7) : 469. 3 Balant G
13、A, Gex F M, Genet C, et al. Therapeutic drugmonitoring of risperidone using a new , rapid HPLC method:reappraisal of interindividual variability factors J . T her DrugM onit, 1999, 21( 1) : 105. 4 Z,Z, I,. 0 i# “5 J .S0, 2001, 10( 6) : 450. 5 Markianos M, Hatzimanolis J, Lykouras L. Gonadal axis hor
14、-mones in male schizophrenic patients during treatment w ithhaloperidol and after sw itch to risperidone J . Psychopharma-cology, 1999, 143( 3) : 270. 6 Norio Y F, Kazuo M , Tsuyoshi K, et al. Effects of CYP2D6genotypes on plasma concentrations of risperidone and enan-tiomers of 9Ohydroxyrisperidone
15、 in Japanese patients w ithschizophrnia J . J Clin Pharmacology, 2003, 43( 1) : 122.(上接第35面)CD44v6Vr q 6bYamam ichi 2TB,4 UCD44v6 VT? 3?ZVB_SbCEA h ?K V L ?S:B 3b 8 ?% Vs CEA,i s % ,yN 8ACEA+sb 4 89!ATCEAmRNA_, 8 !ACEA mRNA_ MrZEbF 8ACEA qr49% ,DMb “ ?Z#M, 8ACEA q A9bT l“ 8ATCEAb_, ,eL, 8 =?M B Sb 8
16、l BnM T,5 7 m H X M“ ?, 8X/0 L =hM, 5 M 40%Z % l 1 5bCD44v6CEA M1, _ VT “5 8/l 10# 1 89 Sb ID 1 Kurozumi K, Nishida T, Nakao K, et al. Expression of CD44variants 6 and lymphatic invasion: im portance to lymph nodemetastasis in gastric cancer J . W orld J Surg, 1998, 22:853.2 Yamamichi K, Uehara Y, K
17、itamura N, et al. Increased ex-pression of CD44v6 mRNA significantly correlates w ith distantmetastasis and poor prognosis in gastric cancer J . Int J Can-cer, 1998, 79: 256.3 Holyoke E D, Che T M , Murphy G P. CEA as a monitor ofgastrointestinal malignancy J . Cancer, 1975, 35: 830.4 , c. 8A%CEA mR-NA_1 il J . S Ll, 2003, 8 ( 1 ) :37.5 l B,?,. bCEAFEOCDVrM1“ J .D Sv, 1998, 19( 4) : 597.#38# L “5D08
