What is the metabolite of diazepam?
Diazepam is metabolized to either nordiazepam by CYP 2C19 or temazepam by CYP3A4. Nordiazepam and temazepam are hydroxylated and demethylated to oxazepam. Oxazepam is then glucuronidated and excreted in the urine.
Do benzodiazepines have active metabolites?
Benzodiazepines and the Liver The ‘LOT’ drugs are those metabolized mostly by conjugation. These do not have active metabolites, and the half-life remains relatively the same even in the setting of liver disease. The rest of the benzodiazepines are primarily metabolized via hepatic CYP-mediated oxidation.
Where is diazepam metabolised?
Diazepam is metabolized in the liver. The common intermediate metabolite of diazepam and clorazepate, N-desmethyldiazepam (nordiazepam), is in turn biotransformed to the active compound, oxazepam.
Which benzodiazepine has active metabolite?
Oxazepam is a short-acting benzodiazepine and one of the most frequently prescribed anxiolytic drugs. It is also the active metabolite of a wide range of other benzodiazepines, such as diazepam, ketazolam, temazepam, chlordiazepoxide, demoxazepam, halazepam, medazepam, prazepam, pinazepam, and chlorazepate.
How is diazepam excreted?
Diazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates. The clearance of diazepam is 20 to 30 mL/min in young adults. Diazepam accumulates upon multiple dosing and there is some evidence that the terminal elimination half-life is slightly prolonged.
Is diazepam metabolized by the liver?
Diazepam is metabolized in the liver to its active metabolite which is excreted in the urine.
Which benzodiazepines do not have active metabolites?
Midazolam, one of the short-acting BZDs, produces no active metabolites.
What is the structure of diazepam?
C16H13ClN2O
Diazepam/Formula
Is Temazepam a metabolite of diazepam?
Temazepam is a benzodiazepine drug which is a minor metabolite of diazepam.
Is diazepam an enzyme inhibitor?
Diazepam is a benzodiazepine that exerts anxiolytic, sedative, muscle- relaxant, anticonvulsant and amnestic effects. Most of these effects are thought to result from a facilitation of the action of gamma aminobutyric acid (GABA), an inhibitory neurotransmitter in the central nervous system.
Does diazepam raise liver enzymes?
Diazepam, as with other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from diazepam is extremely rare. In particular, parenterally administered diazepam has not been reported to cause serum enzyme elevations, even with prolonged use as with therapy of tetanus.
What kind of metabolite is diazepam temazepam?
Temazepam, another active metabolite of diazepam, also undergoes further metabolic transformation into oxazepam. Figure 1 details the metabolic pathways of diazepam into nordiazepam, temazepam, and oxazepam.
What are the metabolites of benzodiazepines in urine?
Metabolites Benzodiazepines are extensively metabolized, and the parent compounds are not detected in urine. Diazepam is metabolized to nordiazepam, oxazepam, and temazepam; all may be detected after diazepam use. Diazepam → Nordiazepam, Oxazepam, and Temazepam
How does mephenytoin affect the metabolism of diazepam?
Diazepam N-demethylation was apparently promoted by the inclusion of temazepam in the incubation medium, while C3-hydroxylation of diazepam was enhanced in the presence of N-desmethyldiazepam. Mephenytoin in the incubation mixture had no effect on diazepam metabolism by either pathway.
How is diazepam classified as a benzodiazepine?
Diazepam. Diazepam is a Benzodiazepine. The chemical classification of diazepam is Benzodiazepines. Diazepam is a benzodiazepine derivative with anti-anxiety, sedative, hypnotic and anticonvulsant properties. Diazepam potentiates the inhibitory activities of gamma-aminobutyric acid ( GABA) by binding to the GABA receptor,…