Benzodiazepine receptor antagonists flumazenil

Hollister LE, HK, G. The benzodiazepine receptor antagonist flumazenil does not block clinical effects of delta-9-tetrahydrocannabinol. Life Sci 1990 47 1655-1650. 

It is uncertain which of these three possibilities apply to patients with anxiety disorders. There is evidence that the binding of the benzodiazepine receptor antagonist, flumazenil, is lower than normal in patients with panic disorder and that it increases the panic attack frequency in these patients but not in normal subjects. This has been interpreted as a slight shift in the benzodiazepine receptor towards the inverse agonist state. 

Probably the most intriguing and controversial CNS-active azide derivative to be investigated is another Hoffman-La Roche compound Ro 15-4513 (233), an analogue of the benzodiazepine receptor antagonist flumazenil (Ro 15-1788) (232). Not surprisingly, this compound was initially... 

As carisoprodol and its metabolite meprobamate are GABA receptor agonists, the use of the benzodiazepine receptor antagonist flumazenil might be considered in some cases of carisoprodol toxicity (5). 

The specific benzodiazepine receptor antagonist flumazenil has been found useful in the treatment of overdose and in reversing the effects of long-acting benzodiazepines used in anesthesia see Chapter 16). 

A number of controlled cUnical trials have been performed to evaluate the efficacy of the benzodiazepine receptor antagonist flumazenil in HE patients. In a subset of these patients, improvements following flumazenil have been spectacular. However, enthusiasm for this approach has been tempered by the possible confounding effects of prior exposure of patients to pharmaceutical benzodiazepines (used as sedatives or as part of an endoscopic work-up in cirrhotic patients) and by the poor correlation between the clinical response and blood levels of benzodiazepines in these patients. Adding to these difficulties is the short half-life and lack of an oral formulation for flumazenil. 

Buldakova S, Weiss M Electrophysiological evidence for agonist properties of flumazenil, a benzodiazepine receptor antagonist, in rat hippocampus slices. J Neurol Sci 149 121-126, 1997... 

The answer is e. (Ka.tzu.ng, pp 373-3743 Flumazenil is a competitive benzodiazepine receptor antagonist. The drug reverses the CNS sedative effects of benzodiazepines and is indicated where general anesthesia has... 

Flumazenil (Mazicon), a benzodiazepine receptor antagonist, is indicated for complete or partial reversal of the sedative effects of benzodiazepines... 

FIGURE 8-27. The benzodiazepine (BZ) receptor antagonist flumazenil is also able to reverse inverse agonist benzodiazepines acting at the benzodiazepine receptors of the GABA A receptor complex. 

IV benzodiazepine used for preoperative sedation and commonly in anesthesia protocols (e.gt, conscious sedation) affording anterograde amnesia. Depresses respiratory function but reversed by the BZ receptor antagonist flumazenil. 

Barbiturates phenobarbital, secobarbital Benzodiazepines alprazolam, diazepam, lorazepam, triazolam Others buspirone, zolpidem BZ receptor antagonist flumazenil Carbamazepine, ethosuximide, valproic acid, phenytoin, clonazepam, diazepam, lorazepam, gabapentin... 

Flumazenil, a specific benzodiazepine-receptor antagonist will antidote and reverse the deleterious effects of triazolam (see Figure 50). 

Flumazenil is a benzodiazepine receptor antagonist (see Chapter 22). It accelerates recovery from postoperative depression of the CNS caused by midazolam and other benzodiazepines used in anesthesia. The short duration of action of flumazenil may necessitate multiple doses. The sedative actions of benzodiazepines are more reliably reversed by flumazenil than is respiratory depression. Use of flumazenil does not obviate the need for adequate monitoring of respiration and provision of ventilatory support when needed. The answer is (D). 

Flumazenil Benzodiazepine receptor antagonist used to reverse CNS depressant effects... 

B. Specific drugs and antidotes. Flumazenil (see p 446) is a specific benzodiazepine receptor antagonist that can rapidly reverse coma. However, because benzodiazepine overdose by itself is rarely fatal, the role of flumazenil in routine management has yet to be established. It Is administered intravenously with a starting dose of 0.1-0.2 mg, repeated as needed up to a maximum of 3 mg. It has some important potential drawbacks ... 

Figure 11.6 Schematic representation of the GABAa receptor complex. Examples of the many structurally diverse compounds that act at different sites on the receptor (see text for details). Picrotoxinin, the active component of picrotoxin, and TBPS act as non-competitive antagonists. The barbiturates, steroids and anaesthetics are positive allosteric modulators, as are the benzodiazepine site ligands shown, with the exception of DMCM (negative allosteric modulator) and flumazenil (benzodiazepine site antagonist)...

Benzodiazepine antagonists, such as flumazenil, possess affinity for benzodiazepine receptors, but they lack intrinsic activity. Flumazenil is an effective antidote in the treatment of benzodiazepine overdosage or can be used postoperatively to arouse patients sedated with a benzodiazepine. 

Flumazenil Romazicon) is a benzodiazepine antagonist that specifically reverses the respiratory depression and hypnosis produced by the benzodiazepine receptor agonists. Its block of the amnesic effect of the agonists is less reliable. Flumazenil is particularly useful when an overdose of benzodiazepines has occurred. It is also employed when a benzodiazepine has been used to produce conscious sedation and rapid recovery of psychomotor competency is desirable. To avoid resedation, flumazenil may require administration by intravenous infusion. 

Flumazenll [floo MAZ eh nill] is a GABA receptor antagonist that can rapidly reverse the effects of benzodiazepines. The drug is available by IV administration only. Onset is rapid but duration is short, with a half-life of about one hour. Frequent administration may be necessary to maintain reversal of a long-acting benzodiazepine. Administration of flumazenil may precipitate withdrawal in dependent patients or may cause seizures if a benzodiazepine is used to control seizure activity. Dizziness, nausea, vomiting, and agitation are the most common side effects. 

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