The aim of this study was to assess the efficacy of Ro15-1788 and a placebo in reversing diazepam-induced effects after surgery under epidural block, and to evaluate the local tolerance and general safety of Ro15-1788. Fifty-seven patients were sedated with diazepam for surgery under epidural anaesthesia. Antagonism of diazepam-induced effects by Ro15-1788 was investigated postoperatively in a double-blind placebo-controlled trial. The patient's subjective assessment of mood rating, an objective test of performance, a test for amnesia, and vital signs were recorded for up to 300 min after administration of the trial drug. No significant differences between the two groups were observed for mood rating, amnesia, or vital signs. The Ro15-1788 group showed a significant improvement in the performance test up to 120 min after administration of the drug. There was no evidence of reaction at the injection site.
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http://dx.doi.org/10.1111/j.1399-6576.1987.tb02634.x | DOI Listing |
Int J Mol Sci
December 2021
State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Key Laboratory of Neuropsychopharmacology, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
Benzodiazepines (BZDs) produce versatile pharmacological actions through positive modulation of GABA receptors (GABARs). A previous study has demonstrated that high concentrations of diazepam potentiate GABA currents on the αβγ and αβ GABARs in a flumazenil-insensitive manner. In this study, the high-concentration effects of BZDs and their sensitivity to flumazenil were determined on synaptic (αβγ, αβγ, αβγ) and extra-synaptic (αβδ) GABARs using the voltage-clamp electrophysiology technique.
View Article and Find Full Text PDFIBRO Neurosci Rep
June 2022
Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, Federal Ministry of Health, P.M.B 21, Garki, Abuja, Nigeria.
Nevirapine (NVP) is non-nucleoside reverse transcriptase inhibitor and an anti-retroviral drug (ARV) with the highest BBB penetrating ability. Its specific pharmacologic effects on central nervous system (CNS) are not well known. The objective of the study was to investigate some CNS effects of Nevirapine.
View Article and Find Full Text PDFBiomed Pharmacother
October 2021
Department of Psychology, University of Yaoundé I, P.O. Box 755, Yaoundé, Cameroon.
About 30% of epileptic patients continue to have seizures. The present study investigates the anticonvulsant and sedative effects of an aqueous extract of C. schweinfurthii in mice.
View Article and Find Full Text PDFLife Sci
December 2019
State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Key Laboratory of Neuropsychopharmacology, Beijing Institute of Pharmacology and Toxicology, Beijing, China. Electronic address:
Aims: Benzodiazepines (BZDs) produce various pharmacological actions by binding to and allosterically regulating GABA receptors. Several in vitro studies have demonstrated diazepam, the prototypic BZD, produces a high-dose action that cannot be countered with the classical BZD-binding site antagonist flumazenil. Here, we investigate the existence and behavioral relevance of non-classical BZD binding sites in zebrafish larvae.
View Article and Find Full Text PDFMol Pharm
September 2017
School of Pharmacy, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong.
Scutellariae Radix (SR) and its bioactive flavones elicit a variety of effects in the brain. However, the brain uptake of individual SR flavones and its relationship to the elicited effects after SR administration remain unknown. Moreover, previous studies seldom measured pharmacokinetic and pharmacodynamic outcomes simultaneously.
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