Sedative-hypnotics, Antiepileptics and Psychotherapeutic Drugs
Sedative-hypnotics Antiepileptics Psychotherapeutic Drugs
Sedative-hypnotics Benzodiazepines Barbiturates
1. Benzodiazepines
1). 1960
1). ChlordiazepoxideLibrium60
1). DiazepamValium
R1R2R3R4XNamesCH3HHClOHHHNO2OHHClNO2O(CH2)2N(C2H5)2HFClOCH3HFClO CH2 HFClOHOHHClOCH3OHHClOHOHClClOCH2CF3HFClS
1). 1, 2
R1R2NamesHHEstazolamCH3HAlprazolamCH3ClTriazolam
1). 1, 2Midazolam Loprazolam
1). 4, 5
R1R2R3R4NamesCH3HClHOxazolamHFBrHHaloxazolamHClClHCloxazolamCH3ClClHMexazolamHFClCH2CH2OHFlutazolam
1).
RNamesC2H5EtizolamBrBrotizolam
2). A7NO2CF3BrCl689
2). B1 1N 2
2). B2 3 4, 5 5 1, 24, 5
2). C 2 ClFBrNO2CF3H 2 34
2). 3B
3). GABAGABACl-Cl- Cl-GABAGABACl-
Flumazenil
4).
5).
6).
Diazepam
45
13
Chemical name of Diazepam 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one 3H- or 1H-1,4-Benzodiazepine1,2-Dihydro-3H-2,3-Dihydro-1H- 1,4-benzodiazepine1,3-Dihydro-2H-
6).
Diazepam
BZR1 Zolpidem
Sedative-hypnotics Benzodiazepines Barbiturates
2. Barbiturates
1). Barbituric acid Barbiturates
2). 1
R1 R2 R3 X Barbital C2H5 C2H5 H O 4-12h Phenobarbital C2H5 C6H5 H O 4-12h
2). 2
R1 R2 R3 X Amobarbital C2H5 CH2CH2CH(CH3)2 H O 2-8h Cyclobarbital C2H5 H O 2-8h
2). 3
R1 R2 R3 X Secobarbital CH2CH=CH2 H O 1-4h Pentobarbital C2H5 H O 2-4h
2). 4
R1 R2 R3 X Hexobarbital CH3 CH3 O 1h Thiopental sodium C2H5 H -S-Na 0.75h
3).
Lactam LactimBarbituric acid Monolactim Dilactim Trilactim
1-5-1,3-1,5-5,5-
pHpH+ CO2
4).
1lgP2.054 ~ 107 ~ 8OHNH2RNHCOCOOHSO3H
2NN2CNS2,4-2,4,6-
5). 151
4). 252
4). 353
4). 4
4). 5
4). 6N
Sedative-hypnotics Benzodiazepines Barbiturates
3. 1
3. 2 Delta sleep inducing peptide, DSIP Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu Melatonin
Sedative-hypnotics Antiepileptics Psychotherapeutic Drugs
Antiepileptics
11 Phenobarbital 1912 Mephobarbital 1935 Metharbital 1952
12 Phenobarbital Primidone 1954
21 Hydantoins Phenytoin (sodium) 1938
Mephenytoin Ethotoin 1947 1957
22 Oxazolidinediones
Trimethadione Paramethadione 1946 1949
23 Succinimides
Phensuximide Methsuximide 1953 1957 Ethosuximide 1960
24
Phenacemide 1951
X BarituratesPhenobarbitalHydantoins Phenytoin sodium OxazolidinedionesTrimethadione SuccinimidesEthosuximidePhenacemide
3 Diazepam Clobazam Nitrozepam Clonazepam Lorazepam Midazolam
4 Carbamazepine Oxcarbazepine1974
5 Sodium valproate Valpromide1978GABA
61GABA
62GABA Halogabide Gabapentin
Halogabide
63GABA Vigabatrin
71GABA
72
Sedative-hypnotics Antiepileptics Psychotherapeutic Drugs
2019381928ACh19481970FDA19521950
19581968Carlson5-2000Nobel1987941954FDA195419601963
Psychotherapeutic Drugs Antipsychotic drugs Antischizophrenic drugs Antianxiety drugs Antidepressant drugs Antimanic drugs
Antipsychotic drugs-1 Antischizophrenic drugs Phenothiazines Thioxanthenes Butyrophenones Diphenylbutylpiperidines
Antipsychotic drugs-2 Antischizophrenic drugs Benzamides Dibenzodiazepines and Dibenzoxazepines Hydroindolones
1 Phenothiazines 1)2)3)4)5)
1) Promethazine
R1R2 ChlorpromazineN(CH3)2Cl1 AcetylpromazineN(CH3)2COCH3
R1R2 TrifluoperazineCF313 Thiethylperazine SC2H5 ThioridazineSCH3-1 PipotiazineSO2N(CH3)2 MesoridazineSOCH3
2)1 21, 3, 42 CF3 > Cl > COCH3 > H > OH2
2)2 3,
2)3 -O-, -CH2-, -CH=CH-, -CH2CH2--C=
ABC B > C > A BR,>
CN-S22 A
3)
5)
2 Thioxanthenes1
RX ChlorprothixeneN(CH3)2Cl ThiothixeneSO2N(CH3)2 FlupenthixolCF3 ZuclopenthixolCl
2 Thioxanthenes22Zcis-isomerEtrans-isomer cis > trans
3 Butyrophenones 1
R1R2 HaloperidolOH BromoperidolOH TrifluperidolOH
3 Butyrophenones 2
R1R2 BenperidolH TimiperoneH PipamperoneCONH2
3 Butyrophenones 3
3 Butyrophenones 4
4 Diphenylbutylpiperidines1
4 Diphenylbutylpiperidines2
5 Benzamides 1D2
5 Benzamides 2D2
6 Dibenzodiazepines and Dibenzoxazepines
XR1R2R3 ClozapineNHHClCH3 ClothiapineSClHCH3 LoxapineOClHCH3 AmoxapineOClHH
7 Hydroindolones
81
82
Psychotherapeutic Drugs Antipsychotic drugs Antischizophrenic drugs Antianxiety drugs Antidepressant drugs Antimanic drugs
Antidepressant drugs Norepinephrine-reuptake inhibitors5 Serotonin-reuptake inhibitors Monoamine oxidase inhibitors Atypical antidepressants
11
R1R2 ImipramineH(CH2)3N(CH3)2 DesipramineH(CH2)3NHCH3 ClomipramineCl(CH2)3N(CH3)2 TrimipramineHCH2CH(CH3)CH2N(CH3)2
12
13
25Serotonin-reuptake inhibitors1
25Serotonin-reuptake inhibitors2
3 Monoamine oxidase inhibitors1
3 Monoamine oxidase inhibitors2MAOA
4Atypical antidepressants1
4Atypical antidepressants2
1
2
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