Chlorazepate

Benzodiazepines, ie, the hiU BZR agonists, are prescribed for anxiety, insomnia, sedation, myorelaxation, and as anticonvulsants (97). Those benzodiazepines most commonly prescribed for the treatment of anxiety disorders are lorazepam (19), alprazolam (20), diazepam (21), bromazepam (22), chlorazepate (23), and oxazepam (24). These dmgs together represent about 70% of total... 

Azanin - Azathioprine Azapen Methicillin sodium Azapress - Azathioprine Azene Chlorazepate dipotassium Azepamid -Medazepam Azide Chlorothiazide Aziin - Aziocillin... 

Chorazepate Chorazepate, 7-chloro-2,3-dihydro-2,2-dihydroxy-5-phenyl-1H-1,4-benzo-diazepin-3-carboxylic acid (5.1.34), which is used in the form of a dipotassium salt, is synthesized by yet another interesting synthetic scheme. 2-Amino-5-chlorobenzonitrile is used as the initial compound, which upon reaction with phenyhnagnesiumbromide is transformed into 2-amino-5-chlorbenzophenone imine (5.1.32). Reacting this with amino-malonic ester gives a heterocyclization product, 7-chloro-l,3-dihydro-3-carbethoxy-5-phenyl-2H-benzodiazepin-2-one (5.1.33), which upon hydrolysis using an alcoholic solution of potassium hydroxide forms a dipotassium salt (5.1.34), chlorazepate [30-32]. 

Chlorazepate is among the long-acting tranquilizers used upon the same indications as other tranquilizers, and also as an adjuvant drug for epileptic attacks. The most common synonyms are tranxene, noctran, and others. 

Sleep onset latency generally is improved (i.e., shortened) with all BZD hypnotics, although this may vary considerably with individual patients. Those with relatively rapid onset of hypnotic activity include flurazepam, diazepam, and chlorazepate. Somewhat slower onset occurs with triazolam, estazolam, quazepam. 

OFFICIAL NAMES Alprazolam (Xanax), chlorazepate (Tranxene) chlordiazepoxide (Librium, Novopoxide), clonazepam (Klonopin), clorazepate (Tranxene), diazepam (Valium, Vivol), estazolam (ProSom), flurazepam (Dalmane, Novoflupam, Somnol), flunitrazepam (Rohypnol), halazepam (Paxipam), lorazepam (Ativan), nitrazepam (Mogadon), oxazepam (Serax), prazepam (Centrax), quazepam (Doral), temazepam (Restoril), triazolam (Halcion)... 

Sachs B, Erdmann S, Al-Masaoudi T, Merk HF. In vitro drug allergy detection system incorporating human liver microsomes in chlorazepate-induced skin rash drug-specific proliferation associated with interleukin-5 secretion. Br J Dermatol 2001 144(2) 316-20. 

Kiejna A, Kantorska-Janiec M, Malyszczak K. [The use of chlorazepate dipotassium (Tranxene) in the states of restlessness and agitation], Psychiatr Pol f 997 3f 753-60. 

Chlorazepate. See the detailed discussion of chloraze-pate (Tranxene) in the sedative-hypnotic-anxiolytic section. Its principal anticonvulsant use is adjunctively in complex partial seizures. 

The discovery of the benzodiazepines (BZDs) at Hoffmann-La Roche in the late 1950s provided a more formidable arsenal for the treatment of anxiety [5]. Following the introduction of chlordiazepoxide (1, Librium ) in 1960, a large number of analogues were synthesized and developed, including diazepam (2, Valium ), lorazepam (3, Ativan ), prazepam (4, Cen-trax ), oxazepam (5, Serax ), chlorazepate (5a,Tranxene ), and alprazolam (6, Xanax ). Although other structural classes of compounds for treatment of anxiety have been discovered such as hydroxyzine (7, Atarax ), buspirone (8, Buspar ), and chlormezanone (9, Trancopal ), the prescriptions written for (l)-(7) over the years since their introduction equal or exceed that for any disorder [4, 6], presumably because of their effectiveness and rapid onset of action [7],... 

Chlorazepate Tranxene 15-60 1 -hyroxy ediylflurazepam, desall lflurazepam Desmethyldiazepam >100... 

Chlorazepate, which enhances GABAergic transmission (see Figure 50), is indicated in acute alcohol withdrawal, in anxiety disorders, and as an adjunct in seizure management. Chlorazepate is hydrolyzed in the stomach to des-methyldiazepam, which is then absorbed completely and bound to plasma proteins to the extent of 80 to 95%. Des-methyldiazepam is then metabolized to oxazepam, whose inactive metabolite conjugated to glucuronic acid is excreted in the urine. 

Chlorazepate potentiates the CNS-depressant effects of phenothiazines, narcotics, barbiturates, alcohol, antihistamines, monoamine oxidase inhibitors, general anesthetics, and antidepressants. Concomitant use with cimetidine and possibly disulfiram causes diminished hepatic metabolism of chlorazepate, which increases its plasma concentration. 

Clinical manifestations of overdose with chlorazepate include somnolence, confusion, coma, hypoactive reflexes, dyspnea, labored breathing, hypotension, bradycardia, slurred speech, and unsteady gait or impaired coordination. 

Simultaneous mephobarbital, paramethadione, phenobarbital, primidone Noninterfering chlorazepate, clonazepam, diazepam, thioridazine, valproic acid Interfering phenytoin... 

Simultaneous bromazepam, chlorazepate, chlordiazepoxide, clobazam, flunitrazepam, lor-azepam, nitrazepam, oxazepam, tobsopam... 

Chlorazepate is a pharmacologically inactive pro-drug. It is metabolically converted to desmethyldiazepam, which is pharmacologically active. Desmethyldiazepam is in turn metabolized to oxazepam, which is also pharmacologically active. 

Chlorazepate (Tranxene) PRODRUG is hydrolyzed in stomach to active agent. ... 

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