Diazepam - StatPearls - NCBI Bookshelf
2023年8月28日 · Metabolism: Diazepam is mostly broken down by the microsomal enzymes CYP2C19 and CYP3A4 enzymes to several active metabolites, mainly desmethyldiazepam. Other minor active metabolites include oxazepam and temazepam.
Diazepam - Wikipedia
The main active metabolite of diazepam is desmethyldiazepam (also known as nordazepam or nordiazepam). Its other active metabolites include the minor active metabolites temazepam and oxazepam . These metabolites are conjugated with glucuronide , and …
Benzodiazepine Pharmacology and Central Nervous …
Most BZDs are oxidatively metabolized by the cytochrome P450 enzymes (phase I), conjugated with glucuronide (phase II), and excreted almost entirely in the urine. Some BZDs exert additional action via production of active metabolites, an important …
Classics in Chemical Neuroscience: Diazepam (Valium) - PMC
Diazepam is well metabolized by liver CYP450 enzymes and glucuronidated for elimination according to Scheme 2. Typically, diazepam is demethylated (by CYP 2C9, 2C19, 2B6, 3A4, and 3A5), yielding 10 (desmethyldiazepam, equipotent to diazepam 64 ), and then is 3′ hydroxylated (CYP 3A4, 3A5, and 2C19), giving 12 , although 11 (CYP 3A4 3A5) is ...
A Physiologically Based Pharmacokinetic Model for Predicting Diazepam …
Diazepam is uniquely metabolized in the liver into a pharmacologically active metabolite, N-desmethyldiazepam, by demethylation and hydroxylation [2,5,6]. Diazepam shows wide interindividual variability in its metabolism, which results …
Benzodiazepines with high lipophilicity (eg: diazepam) can penetrate CNS tend to have high abuse potential as well. 2,3,6 Benzodiazepines bind to the to γ-aminobutyric acid type A receptor (GABA-A) at the alpha-subunit and potentiate GABA activity,
Benzodiazepines - StatPearls - NCBI Bookshelf
2024年1月30日 · Diazepam produces the active metabolites oxazepam, temazepam, and desmethyldiazepam, which further increase the drug action duration. The elimination half-life of benzodiazepines is increased in older patients and patients with renal dysfunction.
Diazepam: Uses, Interactions, Mechanism of Action - DrugBank …
Metabolism. Diazepam is N-demethylated by CYP3A4 and 2C19 to the active metabolite N-desmethyldiazepam, and is hydroxylated by CYP3A4 to the active metabolite temazepam 15,16. N-desmethyldiazepam and temazepam are both further metabolized to oxazepam 15,16.
Diazepam Therapy and CYP2C19 Genotype - Medical Genetics …
2018年12月10日 · Diazepam is primarily metabolized via CYP2C19 and CYP3A4 to the major active metabolite (desmethyldiazepam), which is found in the plasma at concentrations equivalent to diazepam. Two minor active metabolites include temazepam and oxazaepam, which are usually not detectable.
Benzodiazepine metabolism: an analytical perspective - PubMed
Benzodiazepines are currently among the most frequently prescribed drugs all over the world. They act as anxiolytics, sedatives, hypnotics, amnesics, antiepileptics and muscle relaxants. Despite their common chemical scaffold, these drugs differ in their pharmacokinetic and metabolic properties. In ….