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The rest of the benzodiazepines are primarily metabolized via hepatic CYP-mediated oxidation. These may have prolonged duration of effect in patients with marked liver impairment, particularly the drugs with active metabolites such as diazepam, clonazepam, and midazolam.
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. The benzodiazepines are a large class of medications that have multiple clinical uses including therapy of anxiety, insomnia, muscle spasm, alcohol withdrawal and seizures.
Benzodiazepines with fast onset and short half-life (alprazolam, triazolam) cause a “rush” due to rapid increase in plasma concentration and increased craving due to short duration of effect, thereby increasing abuse potential. Benzodiazepines with high lipophilicity (eg: diazepam) can
Benzodiazepines: ones not metabolized by the liver (safe to use in liver failure) LOT: Lorazepam Oxazepam Temazepam. Thanks to MedExcel. Remember to check the animation on the mechanism of action of benzodiazepines.
Of the featured benzodiazepines and Z-drugs generally used long-term in palliative care, all are significantly hepatically metabolized and contra-indicated in severe hepatic impairment. For those drugs metabolized by CYP450 enzymes, e.g. diazepam, zopiclone, the risk of toxicity is greater from a pharmacokinetic drug–drug interaction ...
This activity provides an overview of the indications, mechanism of action, safe administration, adverse effects, contraindications, toxicology, and monitoring associated with the diverse physiological possibilities when using benzodiazepines in the clinical setting.
Rectal, buccal, and intranasal formulations of benzodiazepines are frequently used in outpatient setting for abortive therapy. The RAMPART study ( Silbergleit 2011 ) demonstrated IM midazolam was non-inferior to IV lorazepam (2-4 mg) in the pre-hospital setting.
dexmedetomidine is two hours. It is cleared by hepatic metabolism via enzyme systems that are unlikely to suffer interactions with other medications. Conclusion A wide range of therapeutically useful compounds are active against the systems described above. Research in recent years hints at the futuretherapeutic potential of these systems for
Benzodiazepines and related sedatives are frequently prescribed and misused medications with potentially serious risks including overdose, respiratory depression, over-sedation, memory disturbances, and falls/injury, particularly when combined with opioids, alcohol, and other non-related sedatives. •.
Benzodiazepines are widely used as hypnotics and sedatives for anxiety, but some of them induce liver injury in humans. To clarify whether benzodiazepines are metabolically activated, 14 benzodiazepines were investigated for their cytotoxic effects on HepG2 cells treated with recombinant CYP3A4.