This can be a potential problem when attempting to revert the effects of a benzodiazepine overdose. However, flumazenil has a shorter duration of action than most benzodiazepines, with its elimination half-life being 0.7 to 1.3 hours.
Effective benzodiazepine antagonism begins approximately one to two minutes after intravenous injection and reaches peak concentrations in six to 10 minutes, lasting up to one hour. Flumazenil Pharmacokineticsįlumazenil’s effects are fast-acting, a major reason it is clinically effective at reducing the effects of benzodiazepine overdose, such as respiratory depression. This is useful for treating overdoses or waking patients who have been sedated by other benzodiazepines. Flumazenil competes for the binding sites with other benzodiazepines, blocking their effects. This blocking action makes flumazenil helpful in reversing the effects of benzodiazepines. Flumazenil can induce anxiety, insomnia, and muscle tension - rather than alleviate it. Logically, this action delivers the opposite effects to most other benzodiazepine drugs. Still, instead of increasing the chloride flow, flumazenil blocks this compound’s intake, thus increasing the action potential of the cell. This action slows brain activity and is what gives benzodiazepines their sedating qualities.įlumazenil binds to the same benzodiazepine receptors as other members of this class. GABA increases the flow of chloride ions into the neurons, which reduces its ability to fire electrical signals. Traditional benzodiazepine medications increase the activity of the target receptors (GABA-A). Benzodiazepine Dosage Equivalency Calculator Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. The initial distribution half-life of flumazenil is 4 to 11 minutes, and the terminal half-life is 40 to 80 minutes. Very little flumazenil (<1%) is found in the urine.ĭuration of Effects: Short-Acting.
Metabolism: Flumazenil’s metabolism is 99% hepatic. Other Names: Anexate, Lanexat, Mazicon, & Romazicon IUPAC Name: Ethyl 8-fluoro-5-methyl-6-oxo-4H-imidazobenzodiazepine-3-carboxylate Unlike flumazenil, bretazenil maintains the classic benzodiazepine effects.Īpproved by the FDA in 1991, flumazenil is only commercially available as an injectable drug. Structurally, flumazenil is classified as a 1,4-imidazobenzodiazepine closely related to another benzodiazepine derivative called bretazenil. For example, rather than reducing anxiety-like other benzodiazepines, flumazenil induces it.
Flumazenil - commercially available as Anexate, Lanexat, Mazicon, and Romazicon - is a benzodiazepine receptor antidote used for treating overdoses on other members of the benzodiazepine family.įlumazenil has the opposite effects to most benzos.
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