Benzodiazepines
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Benzodiazepines are used for the brief treatment of sleep disturbances which are caused by fear, excitation or internal unrest, but are also abused. While suicides with benzodiazepines do not occur, the danger exists by strengthening effect with simultaneous consumption with other CNS effective substances as alcohol, barbiturates, opioids etc., which often leads to deaths. Some preparations were used also as K.O.-drugs or Date-Rape-Drugs.

Physiological Effect

All benzodiazepines are docking in special connection places of the nerve cells in the central nervous system (GABAA-receptors) and strengthen the effect of the body-own messenger γ-aminobutyric acid (GABA). GABA restrains the activity of nerve cells and works thereby against sleep-knocking, eases muscles and solves cramps.

Psychological Effect

Benzodiazepines are reducing the conscious perception and the intensity of feelings, in addition reducing the internal tension and absorbing aggressions.

Adverse Effects

Benzodiazepines are making tired and are reducing the attention and concentration. Thus it can come to impairments when leading motor vehicles or serving machines. Likewise, at the beginning of the income or for dose increases, restrictions of the mental and intellectual efficiency are particularly indicated. Benzodiazepine should not be given during the pregnancy, since it crosses into the mother's milk. Already after an uptake of a period of 4 weeks, a psychological dependence can develop. No tendency exists for dose increase. Frequently formation of konjugates occures (Glucuronidates) preceding the elimination over urine and bile. The metabolism is particularly various: N-desalkylation, hydroxylilation, desamination, reduction, acetylation, N-oxidation and hydrolysis lead to numerous metabolits.

 

Alprazolam

Alprazolam

8-Chloro-1-methyl-6-phenyl-4H[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
C17H13ClN4, M 308,8 g/mol
T1/2 12 to 15 h
Trade Marks: Xanax, Cassadan, Esparon, Tafil

Bromazepam

Bromazepam

7-Bromo-2,3-dihydro-5-(2-pyridyl)-1H-1,4-benzodiazepine-2-one
C15H10BrN3O, M 316,2 g/mol
T1/2 15 to 28 h
Trade Marks: Bromazanil, Durazanil, Gityl, Lexotan, Lexotanil, Lexostad, Normoc more info

Chlordiazepoxide

Chlordiazepoxide

7-Chloro-2-methylamino-5-phenyl-3H-1,4-benzodiazepine-4-oxide
C16H14ClN3O, M 299,75 g/mol
T1/2 10 to 15 h, metabolites 50 to 90 h
Trade Marks: Librium, Multum, Radepur more info

Clobazam

Clobazam

7-Chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4(3H,5H)-dione
C16H13ClN2O2, M 300,74 g/mol
T1/2 18 h, metabolites 36 to 120 h
Trade Mark: Frisium

Clonazepam

Clonazepam

5-(2-Chlorophenyl)-7-nitro-1,3-dihydrobenzo[e][1,4]diazepine-2-one
C15H10ClN3O3, M 315,71 g/mol
T1/2 18 to 50 h
Trade Marks: Rivotril more info

Clorazepate

Clorazepate

[(3-Carboxy-7-chlor-2-hydroxy-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine-2yl)oxy]-dipotassium
C16H11ClK2N2O4, M 408,92 g/mol
T1/2 metabolites 25 to 82 h
Trade Marks: Tranxilium, Tranxene
discontinued in the UK since 02/2006

Diazepam

Diazepam

7-Chloro-2,3-dihydro-1-methyl-5-phenyl-1H-1,4-benzodiazepine-2-one
C16H13ClN2O, M 284,76 g/mol
T1/2 24 to 48 h, metabolites 50 to 80 h
Trade Marks: Valium, Faustan, Lamra, Stesolid, Tranquase, Valiquid more info

Flunitrazepam

Flunitrazepam

5-(2-Fluorophenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one
C16H12FN3O3, M 313,3 g/mol
T1/2 18 h
abused as Date-Rape-Drug
Trade Marks: Rohypnol, Flunimerck, Fluninoc

Flurazepam

Flurazepam

7-Chloro-1-(diethylaminoethyl)-5-(2-fluorphenyl)-1,3-dihydro-2H-1,4-benzodiazepine-2-one
C21H23ClFN3O, M 387,89 g/mol
T1/2 1.5 h, metabolites up to 100 h
Trade Marks: Dalmadorm, Dalmane, Staurodorm

Lorazepam

Lorazepam

7-Chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepine-2-one
C15H10Cl2N2O2, M 321,2 g/mol
T1/2 13 to 14 h
Trade Marks: Ativan, Tavor, Tolid, Somagerol, Laubeel

Lormetazepam

Lormetazepam

(RS)-7-Chloro-5-(2chlorphenyl)-2,3-dihydro-3-hydroxy-1-methyl-1H-1,4-benzodiazepine-2-one
C16H12Cl2N2O2, M 335,19 g/mol
T1/2 10 to 14 h
Trade Marks: Ergocalm, Loramet, Loretam, Noctamid

Medazepam

Medazepam

7-Chloro-2,3,-dihydro-1-methyl-5-phenyl-1H-1,4-benzodiazepine
C16H15ClN2, M 270,76 g/mol
T1/2 2 to 5 h, metabolites 50 to 80 h
Trade Mark: Rudotel

Midazolam

Midazolam

8-Chloro-6-(2-fluorphenyl)-1-methyl-4H-imidazol[1,5-a][1,4]benzodiazepine
C18H13ClFN3, M 325,77 g/mol
T1/2 1.5 to 2.5 h
Trade Mark: Dormicum

Nitrazepam

Nitrazepam

2,3,-Dihydro-7-nitro-5-phenyl-1H-1,4-benzodiazepine-2-one
C15H11N3O3, M 281,26 g/mol
T1/2 18 to 30 h
Trade Marks: Mogadan, Radedorm, DORMO-PUREN, Eatan N, imeson, Novanox

Nordazepam

Nordazepam

7-Chloro-2,3,-dihydr-5-phenyl-1H-1,4-bezodiazepine-2-one
C15H11ClN2O, M 270,72 g/mol
T1/2 50 to 90 h
Trade Mark: Tranxilium N

Oxazepam

Oxazepam

(RS)-7-Chloro-1,3-dihydro-3-hydroxy-5-phenyl-1H-1,4-benzodiazepine-2-one
C15H11ClN2O2, M 286,7 g/mol
T1/2 5 to 15 h
Trade Marks: Adumbran, Azotranquil, durazepam, Mirfudorm, Noctazepam, PRAXITEN Sigacalm, Uskan, Serax

Prazepam

Prazepam

7-Chloro-1-(cyclopropylmethyl)-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-one
C19H17ClN2O, M 324,83 g/mol
T1/2 metabolites 50 to 90 h
Trade Mark: Centrax, Demetrin

Temazepam

Temazepam

(R,S)-7-Chloro-3-hydroxy-1-methyl-5-phenyl-1H-1,4-benzodiazepine-2(3H)-one
C16H13ClN2O2, M 300,74 g/mol
T1/2 5 to 13 h
Trade Marks: Euhypnos, Levanxol, Maeva, Normison, Restoril

Tetrazepam

Tetrazepam

7-Chloro-5-(cyclohex-1-enyl)-1-methyl-1H-1,4-benzodiazepine-2(3H)-one
C16H17ClN2O, M 288,77 g/mol
muscle relaxant for treatment of muscle spasm with little sedative effect
Trade Marks: Mobiforton, Musaril, Rilex

Triazolam

Triazolam

8-Chlor-6-(2-chlorphenyl)-1-methyl-4H-1,2,4-triazolo[4,3-a][1,4]benzodiazepine
C17H12Cl2N4, M 343,22 g/mol
T1/2 1.4 bis 4.6 h
Trade Mark: Halcion

 

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Last modification (M-D-Y): 08/09/2010 - IMPRINT - FAQ