[Beta activation following the intravenous administration of benzodiazepines and the specific antagonist flumazenil (Ro 15-1788)].
In a prospective randomized study involving 32 male subjects aged 18 to 38, the effects of flunitrazepam (0.25 to 2 mg/70 kg), lormetazepam (0.5 to 4 mg/70 kg), midazolam (1.5 to 12 mg/70 kg) and diazepam (4 to 32 mg/70 kg) on the beta-activity (13 to 20/s) were investigated. Each subject received four benzodiazepine injections of increasing dosage. The doses were selected so that the lowest had only a slight effect on the test person's condition, while the highest resulted in deep sedation. The increase in beta-activity started off with a latency of 30 to 60 s; it was proportional to the dosage and reached its maximum between the 2. and 3. minutes. The subsequent decrease in beta-activity could be represented by an exponential function. The effect could be cancelled temporarily by administering repeated doses of the specific antagonist, flumazenil (0.1, 0.3 and 0.9 mg/70 kg). The method is suited for describing pharmacodynamic processes, determining equipotential doses of benzodiazepines and detecting the interaction between benzodiazepines and specific antagonists.
Suttmann
H
H
Institut für Anaesthesiologie der Ludwig-Maximilians-Universität München.
Rampf
U
U
Juhl
G
G
Greim
M
M
Doenicke
A
A
D000328:Adult; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D001569:Benzodiazepines; D001611:Beta Rhythm / Q000187:drug effects*; D003975:Diazepam / Q000008:administration & dosage / Q000037:antagonists & inhibitors / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004569:Electroencephalography / Q000187:drug effects*; D005442:Flumazenil / Q000494:pharmacology*; D005445:Flunitrazepam / Q000008:administration & dosage / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006801:Humans; D007275:Injections, Intravenous; D008140:Lorazepam / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008297:Male; D008874:Midazolam / Q000008:administration & dosage / Q000037:antagonists & inhibitors / Q000494:pharmacology; D011446:Prospective Studies; D016032:Randomized Controlled Trials as Topic; D013268:Stimulation, Chemical
D014151:Anti-Anxiety Agents; D001569:Benzodiazepines; D005442:Flumazenil; D005445:Flunitrazepam; C023842:lormetazepam; D008140:Lorazepam; D003975:Diazepam; D008874:Midazolam
Beta-Aktivierung nach intravenöser Gabe von Benzodiazepinen und dem spezifischen Antagonisten Flumazenil (Ro 15-1788).