7-Amino-clonazepam

Amino clonazepam, (4i) 7-Acetamido clonazepam, (4j) (inactive) (inactive)... 

Clonazepam (8) is almost completely absorbed after oral dosing (96) with an average max of 2-4 h. As with other 7-nitro benzodiazepines, the major metabolic pathway for clonazepam is reduction of the nitro group, acetylation of the resulting amine, and elimination of the acetamide. Hydroxylation of clonazepam or of 7-amino clonazepam to give the 3-hydroxy derivatives represents minor metabolic pathways. The elimination half-life of clonazepam is 20-30 h (97), and no active metabolites are produced. 

Direct Determination of Clonazepam (Rivotril) and 7-Amino-clonazepam in Plasma by Gas Chromatography Toxicol. Eur. Res. 2(l) 25-33 (1979) ... 

Clonazepam 1.5-20 1-2 18-50 Inactive 7-amino or 7-acetyl-amino derivatives-... 

Gas Chromatography. System GA—clonazepam RI 2885, 7-acetamidoclonazepam RI 3263, 7-aminoclonazepam RI 2900, 7-amino-3-hydroxyclonazepam RI 2890 system GG—RI 3600. 

Various aromatic nitro drugs undergo enzymatic reduction to the corresponding aromatic amines. For example, the 7-nitro benzodiazepine derivatives clonazepam and nitrazepam are metabolized extensively to their respective 7-amino meubolitcs in humans. Thc skeletal muscle relaxant dantrolene (Dantrium) also reportedly undergoes reduction to aminodantrolene in humans. ... 

Nitrazepam. As indicated previously, nitrazepam (4e), is similar in structure to clonazepam. Absorption after oral administration occurred within 1 h however, in some cases relatively slow absorption (up to 4 h) has been reported (43-48). Rectal administration provided more rapid absorption (median peak time 18 min versus 38 min orally) (48). Although a good correlation was apparent between the volume of distribution and elimination half-life, when comparing the young, elderly, female, and male subjects, the differences observed in volume of distribution related to sex, age, and body weight seem to depend on the relative proportion of body adipose tissue (49). The metabolic pattern of nitrazepam is similar to that of clonazepam, with the principal formation of the inactive 7-amino (41) and 7-acetamido (4m) compounds. 

Clonazepam (Klonopin) Seizure disorders 20-60 7-amino-3-hydroxy... 

Sjb 0, Hvidberg EF, Naestoft J, Lund M. Pharmacokinetics and side-effects of clonazepam and its 7-amino metabolite in man. EurJ Clin Pharmacol (1975) 8, 249-54. 

Determination of Clonazepam and Its Amino and Acetamido Metabolites in Human Plasma by Combined Gas Chrom-... 

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