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Flumazenil's short half-life requires multiple doses. Because of the potential risks of withdrawal symptoms and the drug's short half-life, patients must be carefully monitored to prevent recurrence of overdose symptoms or adverse side effects. Flumazenil is also sometimes used after surgery to reverse the sedative effects of benzodiazepines.
IC 50 / pIC 50 values represent binding affinity only and do not reflect efficacy or pharmacokinetics, and some compounds listed are GABA A antagonists rather than agonists (e.g. flumazenil). Low IC 50 or high pIC 50 values indicate tighter binding (pIC 50 of 8.0 = IC 50 of 10nM, pIC 50 of 9.0 = IC 50 of 1nM, etc.)
A benzodiazepine can be placed into one of three groups by its elimination half-life, or time it takes for the body to eliminate half of the dose. [196] Some benzodiazepines have long-acting active metabolites, such as diazepam and chlordiazepoxide, which are metabolised into desmethyldiazepam. Desmethyldiazepam has a half-life of 36–200 ...
Due to its short half life, the duration of action of flumazenil is usually less than 1 hour, and multiple doses may be needed. [48] When flumazenil is indicated the risks can be reduced or avoided by slow dose titration of flumazenil. [47]
Flumazenil was found to be more effective than placebo in reducing feelings of hostility and aggression in patients who had been free of benzodiazepines for 4–266 weeks. [92] This may suggest a role for flumazenil in treating protracted benzodiazepine withdrawal symptoms.
Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine [1] anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different.
Flumazenil is a benzodiazepine antagonist and blocks the binding of benzodiazepines to gamma-aminobutyric acid receptors. Similarly to naloxone, flumazenil has a short half-life, and this needs to be taken into account because the patient may exhibit central nervous depression after the antidote has been cleared.
Etizolam, a thienodiazepine derivative, is absorbed fairly rapidly, with peak plasma levels achieved between 30 minutes and 2 hours. It has a mean elimination half life of about 3.4 hours. [4] [2] [3] Etizolam possesses potent hypnotic properties, [23] and is comparable with other short-acting benzodiazepines. [4]