Clorazepate potassium

Levels After Oral Administration of Clorazepate Potassium Salts J. Pharm. Sci. 64(10) 1668-1671 (1975) CA 84 61e... 

The antianxiety effects of chlordiazepoxide (165) were described in 1960 and this compound was followed by diazepam (135). These two drugs have captured 75% of the market for sedatives in the USA. Other benzodiazepines used as antianxiety agents include oxazepam (166 R = H), a metabolite of diazepam that is better tolerated, lorazepam (166 R = Cl) and potassium clorazepate (167). Prazepam is the iV-cyclopropylmethyl analogue of diazepam. The benzodiazepines have other therapeutic applications, many being used for inducing sleep, diazepam and nitrazepam are anticonvulsants and flurazepam (168) is both an antianxiety agent and a potent hypnotic. Thieno- and pyrazolo-1,4-diazepinones isosteric with diazepam have similar pharmacological properties (B-81 Ml 10604). 

Potassium Clorazepate Tranxene Sanofi/Abbott Benzodiazepine carboxylate 1967 5-20 p.o. 

Figure 5.4. Biotransformation pathways of potassium clorazepate, diazepam, nordazepam, oxazepam, and temazepam.

The effects of nordazepam and a precursor, potassium clorazepate, on sleep were evaluated in humans (92). A dose of 5 or 10 mg nordazepam or 15 mg of potassium cloraz-... 

Potassium clorazepate is decarboxylated rapidly at the pH of the stomach to form nordazepam (desmethyldiazepam), which is quickly absorbed. The peak plasma nordazepam concentration is obtained 45 min after clorazepate administration of 15 mg (93). 

Dipotassium clorazepate is available as Tranxene containing 50 mg and the additives mannitol and potassium carbonate. According to the product information, the powder should be dissolved in a phosphate buffer until a concentration of 20 mg/mL at a pH of 6.7-7.2 is reached. How long can the reconstituted solution be kept before administration as injection solution How long can a diluted solution as infusion be kept before administration ... 

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