Flumazenil

2022-03-09: Drugs reference:

Flumazenil #

GABA-A antagonist. May treat narcolepsy and improves vigilance in hypersomnias.

• Perinatal upregulation of benzodiazepine receptor ontogenesis: “fearless” and more efficient goal-directed behavior of adult rat progenies
  • the rats consumed 2.9 mg/kg/day of Ro 15-1788 (flumazenil) or 5.3 mg/kg/day of diazepam over the time period of 3 weeks, from gestation day 14 through postpartum day 14
  • Flumazenil group had 66% increase in the density of benzodiazepine receptors in the hippocampal formation… they rapidly habituated to the novel environment, their exploratory activity was uninhibited by distracting visual and auditory stimuli, they made fewer “working memory” errors in collecting baits, had a much better control over their emotional responses and the autonomic nervous system, as shown by very low defecation/urination scores
• Dose-dependent effects of flumazenil on cognition, mood, and cardio-respiratory physiology in healthy volunteers
  • The majority of cognitive tasks showed dose-dependent declines in performance.

Dosing #

Used intravenously, with ahalf life of 20-30 mins in the brain and 10 mens to peak. Therefore it’s something like 200 μg every 1-2 mins and up to 3 mg/hr.