苯二氮卓類電子教案

1、苯二氮卓類NNR4123456791/2/3/4/5/6/ABCR1O8R2R3NNClNHCH3O氯氮卓NNClCH3O地西泮NR1NOR3R1=H, R2=H, R3=NO2, 硝西泮R1=H, R2=Cl, R3=NO2,氯硝西泮R1=(CH2)2N(C2H5)2, R2=F, R3=Cl 氟西泮R2NHNOClOHR1R1 = H 奧沙西泮R1 = Cl 勞拉西泮NNSClFCH2CF3夸西泮NNClFNH3C咪達(dá)唑倫NHNOBrOF鹵f唑侖SNNNNCH3 依替唑倫ClCH3NNNClR2NR1R1=H R2=H 艾司唑倫R1=CH3 R2=H 阿普唑倫R1=CH3 R2=Cl 三唑

2、倫NNClCH3O地西泮NNClCH3ONNClCH3OHHHHabNNClCH3ONNClCH3OHCH3CH3HSR穩(wěn)定,活性強(qiáng)NNOClCH3diazepanNHNOClOH4hydroxydesoxydemoxepamNHNOClnordazepamNHNOClOH9-hydroxydesoxydemoxepamNHNOClOHoxazepamNNCH3OCl（CH3)2SO4CH3C6H5Fe , HClC2H5OHClON3-苯-5-氯嗯呢ClON+CH3ClNHCH3OClCH2COClC6H12ClNCOCH2ClOCH3NNCH3OCl(CH2)6N4.HClCH3OHIII

3、NHNOCl2) NaNO2, HCl3)-萘酚ClNONHO1)H+NNCH3OClH+OH-ClNHCH3O+ H2NCH2COOH2-甲氨基-5-氯-二苯甲酮ONCH3OClNH2H+NNHCH3ClCOOHNHNOR2 R2=H, R3=NO2, 硝西泮 R2=Cl, R3=NO2,氯硝西泮R1NNNClR2NR1R1=H R2=H 艾司唑倫R1=CH3 R2=H 阿普唑倫R1=CH3 R2=Cl 三唑倫NNClFNH3C咪達(dá)唑倫NNCH3OClNH2NCH3OClOClNOCH3NHNH2OONH2Ro7355肽酶前藥Ro7355NNNClNHNNNClNHONNClNHH+NH3+

4、NNCH3H3CN(CH3)2ONNNONN CH3NClOCOHNNHOOO124563R1R2HNNHOOONNHOOHONNOHOHONNOHOHHO巴比妥酸單內(nèi)酰亞胺雙內(nèi)酰亞胺三內(nèi)酰亞胺124563HNNHOOO124563R1R2R3NNHOXO124563R1R2名稱名稱pKa分子態(tài)藥物分子態(tài)藥物離子態(tài)藥物離子態(tài)藥物巴比妥酸巴比妥酸4.120.0599.955-苯基巴比妥苯基巴比妥酸酸3.750.0299.98苯巴比妥苯巴比妥7.2943.7056.30海索比妥海索比妥8.4090.919.09HNNHOOO124563R1R2NHNHC6H5C2H5OOONHNHC2H5OOOH

5、ONHNHC2H5OOONHNHC2H5OOOOHNHNHR1R2OOOCHCNHCNH2R1R2OOCR1R2CONH2CONH2NHNHC2H5OSOH3CNHNHC2H5OOOH3CNNHH3COOOCH3NHNHH3COOONHNHR1R2OO(S)OH2CCOOC2H5COOC2H5R1XC2H5ONa CHCOOC2H5COOC2H5R1R2XC2H5ONa CCOOC2H5COOC2H5R1R2NHNHR1R2OO(S)OH2NCNH2C2H5ONaO(S)IIIIIINNHOOONaR1R2CHCONHCONH2R1R2+ NaHCO3CHCOONa + NH3R1R2室溫NH

6、NHC6H5C2H5OOONHNHC6H5C2H5OOOC6H5CH2COOC2H5COOC2H5COOC2H5C2H5ONa CHCOCOOC2H5COOC2H5C6H5CO CHCOOC2H5COOC2H5C6H5C2H5BrC2H5ONa CCOOC2H5COOC2H5C6H5C2H5H2NCONH2C2H5ONaHClNHNHC6H5C2H5OOOIIIIIICHOHOHCl3C 水合氯醛安全的催眠、抗驚厥藥代謝CH2OHCl3CCH2OPO3H2Cl3C三氯乙醇膦酸酯CHNHCOOC2H5Cl3C氨基甲酸乙酯水合氯醛OH三氯乙醇活性前藥CCH2OCONH2CH2OCONH2H3CCH

7、3CH2CH2NNCH3OH3CNHNHC6H5C2H5OO撲米酮（撲癇酮） NHNHC6H5C2H5OOO苯巴比妥NHNHC6H5C6H5OO苯妥英ONH3CH3COOCH3 三甲雙酮 毒性大（f唑烷雙酮類） 失神性小發(fā)作NHC2H5H3COO 乙琥胺（丁二酰亞胺類） 癲癇小發(fā)作NHNHC6H5C2H5OO5-乙基-5-苯基-乙內(nèi)酰脲 毒性大生物電子等排v抑制大腦皮層運(yùn)動(dòng)中樞，提高驚厥的閾值。NHNC6H5C6H5OONa135NHNC6H5C6H5OONaNHCONH2COOHC6H5C6H5NH2COOHC6H5C6H5NaOH+ NH3NHNC6H5C6H5OONaNHNHC6H5OO

8、HONHNHC6H5OOGluONHCONH2COOHC6H5C6H5+NH2COOHC6H5C6H5NNClCH3OONCONH2NCONH2NCONH2ONCONH2OHOH環(huán)氧化物酶卡馬西平CYP450CHCORCH3CH2CH2CH3CH2CH2R = HR=ONaR = NH2丙戊酸丙戊酸鈉丙戊酰胺H2NOHOv作用機(jī)理可能是通過抑制腦內(nèi)興奮性介質(zhì)谷氨酸和天門冬氨酸的過量釋放，產(chǎn)生抗癲癇作用。NNNClClNH2紋狀體中NSCH2CH2CH2NRRRNSCH2CHN(CH3)2CH3異丙嗪NSCH2CH2CH2N(CH3)2Cl12345678910氯丙嗪 NSCH2CH2CH2R1

9、R2NNCH2CH2OHNNCH3NNCH2CH2OHClCF3CF3 奮乃靜氟奮乃靜 三氟拉嗪NSCH2CH2CH2CF3NNCH2CH2OCOC6H13氟奮乃靜庚酸酯23周注射一次 R1 R2N(CH3)2 COCH3 乙乙酰酰丙丙嗪嗪N(CH3)2 CF3 三三氟氟丙丙嗪嗪1045013NHRSI2NHSR+NHSR少量NaNH2Cl(CH2)3NR2/NSCH2CH2CH2NR2/ClNSCH2CH2CH2NRRRNSCH2CH2CH2N(CH3)2.HClClNSCH2CH2CH2ClNNCH2CH2OHXRCl -N(CH3)2 氯普噻噸CF3NNCH2CH2OH氟哌噻噸Cl 珠氯

10、噻醇NNCH2CH2OHNSCH2CH2CH2RXSCHCH2CH2RXNCOOC2H5H3C哌替啶FCO(CH3)3NR1R2123456R1 OH OHR2ClCF3氟哌啶醇三氟哌多NNNOFCO(CH2)3氟哌利多廣泛用于治療急、慢性精神分裂癥和躁狂癥RCO(CH2)3NR1R2急、慢性FCO(CH2)3NOHCl234561FCO(CH2)3NOHClFCO(CH2)2CHOFCO(CH2)2COOHFCH(CH2)3NOHClOHFCH(CH2)2CHOOHFCH(CH2)2COOHOHFCO(CH3)3NR1R2123456FCH(CH2)3NR2R1FR1 HNNHOR2匹莫齊特

11、Cl五氟利多OHCF3NHNC6H5O 氟司必林一天一次 兩周一次 一周一次H2NO2SCONHCH2OCH3NC2H5NNHNNCH3Cl二苯并氧氮卓類，和氯丙嗪、氟哌啶醇一樣能阻斷紋狀體多巴胺受體，因而臨床應(yīng)用、療效及不良反應(yīng)相似，也可導(dǎo)致NONNCH3ClNNOONNNNSCH2CH2CH2NRRRN(CH2)3NRRRN(CH2)3NRRR 丙咪嗪類抗抑郁作用增強(qiáng)N(CH2)3NRCH3R CH3 丙咪嗪Cl H 地昔帕明作用快，副作用小NONHNClNSCH2CH2CH2NRRRN(CH2)3NRRR丙咪嗪SCH2CH2CH2RXCH(CH2)2NRCH3R=CH3 阿米替林 R=H 去甲替林拼合原理CH(CH2)2N(CH3)2.HCl1234567891011a