Benzodiazepine-receptor antagonist

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... 

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

Which of the following is described as a competitive benzodiazepine receptor antagonist ... 

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... 

Zolpidem (1) is an effective hypnotic agent indicated for the short-term treatment of insomnia. Zolpidem interacts with the GABAa receptor, and its pharmacological effect is blocked by the benzodiazepine-receptor antagonist fiumazenil (Sanger and Depoortere, 1998). Zolpidem displaces benzodiazepines more selectively from the cerebellum than the hippocampus or spinal cord, consistent with preferential interaction with the ajGABAA receptor subtype (sometimes referred to as the benzodiazepine coi receptor). Studies... 

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

Reverse sedative effects of benzodiazepines general anesthesia Action Benzodiazepine receptor antagonist Dose Adults. 0.2 mg IV over 30 s repeat PRN, to... 

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. 

Therapeutic Function Benzodiazepine receptor antagonist. Anticonvulsant... 

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... 

Bansky, G., Meier, P.J., Riederer, E., Walser, H., Ziegler, W.H., Schmid, M. Effects of the benzodiazepine receptor antagonist flumaz-enil in hepatic encephalopathy in humans. Gastroenterology 1989 97 744-750... 

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). 

Als-Nielsen B, Kjaergard LL, Gluud C. Benzodiazepine receptor antagonists for acute and chronic hepatic encephalopathy. Cochrane Database Syst Rev 2001 4 CD002798. 

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

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). 

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 ... 

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. 

Bosman DK, van den Buijs CA, de Haan JG, Maas MA, Chamuleau RA The effects of benzodiazepine-receptor antagonists and partial inverse agonists on acute hepatic encephalopathy in the rat. Gastroenterology, 101, 772-781, 1991... 

Benzodiazepine receptors, both central and peripheral have been investigated using the benzodiazepine receptor antagonists [ CJflumazenil (Samson et al. 1985) and (+)PK11195 (Shah et al. 1994), respectively (O Fig. 41.42). 

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