Pharmacokinetics and pharmacodynamics of a new local anesthetic agent.
We compared the effects of local anesthetics procaine, amethocaine (dicaine), bupivacaine, and a new agent RU-1148 on hydrolytic activity of human plasma butyrylcholinesterase. The butyrylcholinesterase-blocking activity of the test substances decreased in the following order: bupivacaine>amethocaine>procaine>RU-1148. The study of the capacity of these agents to form complexes with human plasma proteins and serum albumin showed that RU-1148 in therapeutic concentrations was transported by human serum albumin,beta-globulin, and acid glycoproteins. Study of the mechanisms of pharmacodynamic interactions between clonidine and RU-1148 demonstrated good prospects of their combined use.
Galenko-Yaroshevskii
A P
AP
Krasnodar Research Center, Russian Academy of Medical Sciences and Administration of the Krasnodar Territory, Moscow.
Derlugov
L P
LP
Ponomarev
V V
VV
Dukhanin
A S
AS
D000779:Anesthetics, Local / Q000493:pharmacokinetics*; D001562:Benzimidazoles / Q000493:pharmacokinetics*; D001798:Blood Proteins / Q000378:metabolism; D002091:Butyrylcholinesterase / Q000097:blood*; D002800:Cholinesterase Inhibitors / Q000493:pharmacokinetics*; D005456:Fluorescent Dyes / Q000378:metabolism; D006801:Humans; D010974:Platelet Aggregation; D012709:Serum Albumin / Q000378:metabolism
D000779:Anesthetics, Local; D001562:Benzimidazoles; D001798:Blood Proteins; D002800:Cholinesterase Inhibitors; D005456:Fluorescent Dyes; D012709:Serum Albumin; C492520:imidaso(1,2-a)benzimidazole; D002091:Butyrylcholinesterase