Chemical formula: C₁₅H₁₁N₃O₃ Molecular mass: 281.266 g/mol PubChem compound: 4506
Nitrazepam is a benzodiazepine compound with sedative properties. It acts in 30 to 60 minutes to produce sleep lasting 6 to 8 hours.
The drug is well absorbed form the GI tract with peak blood levels being achieved within 2 hours of administration. Two hours after administration, the concentration of nitrazepam in the cerebrospinal fluid is about 8% and after 36 hours approximately 16% of the concentration in the plasma. The cerebrospinal fluid concentration thus corresponds to the non-protein-bound fraction of active ingredient in the plasma. Steady-state levels are achieved within 5 days.
In younger persons the volume of distribution is 2L/kg, in elderly patients the volume of distribution is greater and the mean elimination half-life rises to 40 hours.
Nitrazepam undergoes biotransformation to a number of metabolites, none of which possess significant clinical activity.
About 5% of the metabolites are excreted unchanged in the urine together with less than 10% each of the 7-amino- and 7-acetylamino- metabolites in the first 48 hours. In younger persons the volume of distribution is 2L/kg, in elderly patients the volume of distribution is greater and the mean elimination half-life rises to 40 hours.
The half-life is on average 24 hours.
No clear correlation has been demonstrated between the blood levels of nitrazepam and its clinical effects.
None stated.
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