![]() Numerous studies in healthy subjects have demonstrated that flumazenil 100 to 200mg orally or 2.5 to 20mg intravenously antagonised the pharmacological effects (such as sedation, impaired cognitive and motor function, and anaesthesia) of diazepam, methylclonazepam, flunitrazepam, lorazepam, midazolam and zolpidem when the benzodiazepine agonist and flumazenil were administered concomitantly or separately at various intervals. In vitro binding studies of these receptors using positron emission tomography, support the suggestion that in man, as in animals, flumazenil antagonises the central pharmacological effects of the benzodiazepines by interacting with these drugs at the central benzodiazepine receptor binding sites. The inhibitory effect of flumazenil is specific for central benzodiazepine receptors. diazepam, triazolam, midazolam) and inverse agonists. ![]() 10 mg/kg intraperitoneally, a total dose of 30 to 100mg orally and of 2.5µg by the intracerebroventricular route, has been shown to antagonise the central effects of benzodiazepine agonists (e.g. In various tests in mice, rats and cats, flumazenil 0.3 to 30 mg/kg intravenously, 0.5 to. Pharmacodynamic Propertiesįlumazenil is a benzodiazepine antagonist which inhibits the central effects of benzodiazepine agonists by competing with these drugs for the benzodiazepine receptor. Flumazenil is clearly very useful in treating drug poisoning when benzodiazepines are a major component.īy virtue of its specific benzodiazepine antagonist effects, flumazenil provides an innovative and well tolerated approach in clinical situations requiring rapid reversal of benzodiazepine-induced central nervous system depressant effects. In such patients, flumazenil also facilitates differential diagnosis and reduces the necessity for interventions.įlumazenil thus enhances recovery and allows more rapid discharge of patients sedated with benzodiazepines for diagnostic procedures and facilitates management of patients during the initial recovery period following general anaesthesia supplemented with benzodiazepines, but does not preclude normal monitoring during the recovery period. ![]() After poisoning with high dosages of benzodiazepines alone or combined with other drugs, the initial single dose of flumazenil will require supplementing with repeated low intravenous doses or an infusion to maintain wakefulness. The duration of action is short at generally 30 to 60 minutes and supplemental doses of flumazenil may be needed to maintain the desired level of consciousness in some patients. Following intravenous administration of up to 1mg, flumazenil effectively reverses sedation and improves psychomotor performance following administration of short and longer acting benzodiazepines used for sedation, or general anaesthesia supplemented with benzodiazepines. Flumazenil is a specific benzodiazepine antagonist which is indicated when the central effects of a benzodiazepine need to be attenuated or terminated.
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