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7-amino-clonazepam

7-amino-clonazepam as use of the parent drug

The metabolic transformation of Clonazepam is produced by oxidative hydroxylation and reduction of the 7-nito group, with the formation of 7-amino or 7-acetylamino compounds, which can be conjugated to form new metabolites. The major metabolite is 7-amino-clonazepam, with little anticonvulsant activity. In addition, four other metabolites have been identified, but to a lesser extent.

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Clonazepam is mainly metabolized by reduction to 7-amino-clonazepam and by N-acetylation to 7-acetamido-clonazepam. Hydroxylation of C-3 also occurs. The metabolites present in urine are found both as free and conjugated compounds (Glucuronide and Sulfate). Clonazepam is a benzodiazepine that acts at the level of limbic, pituitary and hypothalamic regions of the CNS inducing sedation, hypnosis, anticonvulsant activity, skeletal muscle relaxation and coma. Its action is mediated through the inhibitory system GABA (Gamma-aminobutyric acid).

Central benzodiazepine receptors interact with GABA enhancing their inhibitory effects and increasing inhibition of the ascending reticular system. Clonazepam suppresses tip-and-wave discharge in absence seizures and decreases the frequency, amplitude, duration, and dissemination of discharge in mild motor seizures.

Clonazepam is well absorbed from the oral route, reaching peak plasma concentrations in one to two hours. Clonazepam is extensively metabolized in the liver, its main metabolite being 7-amino clonazepam, with little antiepileptic activity; Minor metabolites are 7-acetamido and 3-hydroxy derivatives. It is almost completely excreted in urine under the form of its metabolites in a free or conjugated way.

Less than 0.5% of the dose is excreted unchanged in the urine. Fecal excretion is 9 to 27%. The half-life of the parent compound ranges from 18 to 50 hours. The binding to proteins is 85%. Its action begins at 20-60 minutes of the oral dose and persists for 12 hours in adults. The therapeutic range of plasma concentrations has not been established.

Its oral bioavailability is 82-98%. The time for the action to appear after administration orally is 20-60 minutes and the duration of the action is 6-8 hours in children and up to 12 hours in adults. The plasma half-life varies considerably, between 18 and 50 hours. The mean distribution volume of clonazepam is likely to be about 3 L / kg. Its degree of protein binding is 85%. It is estimated that it crosses the placental obstacle, and its presence and it has been discovered in breast milk.

The metabolic transformation of clonazepam occurs in the liver, with the formation of new metabolites and compounds that can be conjugated to be excreted by the renal route. The major metabolite is 7-amino-clonazepam, with little anticonvulsant activity. Four other metabolites have been identified, to a lesser extent.

Like other benzodiazepines, the drug apparently crosses the blood-brain barrier and placenta. The average lifespan is 18.7 – 39 hours. Clonazepam is metabolized in the liver and includes several metabolites such as 7-amino clonazepam, 7-acetaminoclonazepam, and 3-hydroxy derivatives of these metabolites. The metabolites of clonazepam are excreted in the urine, mainly conjugated as glucuronic and/or sulfate. Only a small amount of drug is excreted unchanged.