How is benzodiazepines metabolized?
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 consideration when prescribing these agents.
What enzymes metabolize benzodiazepines?
Cytochrome P450(CYP)3A4 is one of the CYP enzymes catalyzing oxidative metabolism, and involved in the metabolism of many drugs. Among benzodiazepines, alprazolam, triazolam, brotizolam and midazolam are mainly metabolished by CYP3A4, and quazepam, diazepam and flunitrazepam are partly metabolised by this enzyme.
How is lorazepam metabolized?
Lorazepam is metabolized by the liver to inactive metabolites and is considered the benzodiazepine best tolerated by patients with advanced liver disease. Liver injury from benzodiazepines is probably due to the toxic effects of a rarely produced intermediate metabolite.
Are Benzos bad for your liver?
As a class, the benzodiazepines do not cause significant serum enzyme elevations and have been linked to only very rare instances of acute, symptomatic liver disease.
Are benzodiazepines hard on the kidneys?
Mixed with prescription muscle relaxers, benzodiazepines can also damage liver and kidney function. Withdrawal from benzodiazepines can result in painful symptoms, such as the return of anxiety, insomnia and sensory hypersensitivity.
Is it OK to not take lorazepam?
Do not stop taking this medication or take fewer doses without talking to your doctor. Stopping lorazepam suddenly can worsen your condition and cause withdrawal symptoms that may last for several weeks to more than 12 months.
How are benzodiazepines metabolized in the liver?
All benzodiazepines are metabolized by the liver. However, some benzodiazepines (i.e. – lorazepam, oxazepam, and tamazepam) do not go through cytochrome P450 metabolism (Phase I metabolism), and are only metabolized via glucuronidation (Phase II metabolism).
What are the pharmacokinetic properties of benzodiazepines?
Benzodiazepine Pharmacokinetics. The pharmacokinetic properties of a drug determine its onset of action and the duration of its effect. Specifically, pharmacokinetics describes the absorption, distribution, metabolism, and excretion of a drug (ie, what the body does to the drug).
Are there any benzodiazepines that are cross tolerant with ethanol?
Benzodiazepines are cross-tolerant with ethanol and are considered first-line therapy for treating AWS. Chlordiazepoxide and diazepam are first metabolized by hepatic oxidation, then glucuronidation. Lorazepam and oxazepam undergo only hepatic glucuronidation. Benzodiazepine oxidation is decreased in persons with liver disease and the elderly.
Which is the most lipophilic benzodiazepine in the body?
Diazepam and midazolam are the most lipophilic, and have the fastest onset of action. All benzodiazepines are metabolized by the liver. However, some benzodiazepines (i.e. – lorazepam, oxazepam, and tamazepam) do not go through cytochrome P450 metabolism (Phase I metabolism), and are only metabolized via glucuronidation (Phase II metabolism).