[Pharmacokinetics and efficacy of phenazepam after transdermal and enteral administration in rats].
The concentration of fenazepam in the blood plasma of rats upon application of the transdermal therapeutic system (TTS) fenapercuten was very low, incomparable to the drug concentration (recalculated to equal input doses) upon intravenous or enteral administration. Nevertheless, the TTS exhibited a pronounced anxiolytic and weak sedative action in the absence of any side myorelaxant effect. The agent responsible for adverse side effects (3-hydroxyfenazepam) was not determined in the blood plasma upon the TTS application. A steady-state concentration of fenazepam in the blood plasma of rats was observed between 2nd and 8th hours upon fenapercuten application, which agrees with the duration of anxiolytic action of the parent drug.
Zherdev
V P
VP
Laboratory of Pharmacokinetics and Laboratory of Clinical Psychopharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya Str., 8, Moscow, 125315 Russia.
Voronina
T A
TA
Garibova
T L
TL
Kolyvanov
G B
GB
Litvin
A A
AA
Sariev
A K
AK
Tokhmakhchi
V N
VN
Vasil'ev
A E
AE
D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001569:Benzodiazepines; D007275:Injections, Intravenous; D008297:Male; D051381:Rats
D014151:Anti-Anxiety Agents; D001569:Benzodiazepines; C017928:phenazepam