ABSTRACT
The possibility of formation of some liposomal neurotropic drugs was studied by 1H-NMR method. Experiments in animals on catalepsy and epidural anaesthesia confirmed this hypothesis.
Subject(s)
Anesthetics/administration & dosage , Nervous System/drug effects , Anesthesia, Epidural , Anesthetics/pharmacokinetics , Anesthetics/pharmacology , Animals , Catalepsy/chemically induced , Delayed-Action Preparations , Drug Carriers , Liposomes/metabolism , Magnetic Resonance Spectroscopy , Mice , Pain Measurement , Rabbits , Time FactorsABSTRACT
It was found that chlorpromazine and pipolfene potentiating general anaesthesia increase viscosity of phospholipid membrane in the region of polar headgroups and in the hydrophobic area near glycerol sceleton. These results (independently of potentiating mechanism) confuse a mechanism of anaesthetics action as increased fluidity of membrane phospholipids.
Subject(s)
Anesthesia, General , Anesthetics/pharmacology , Lipid Bilayers , Membrane Fluidity/drug effects , Membrane Lipids , Phospholipids , Chlorpromazine/pharmacology , Electron Spin Resonance Spectroscopy , Promethazine/pharmacologyABSTRACT
It is found that neurotropic drugs, whose molecules have positively-charged amino groups and a considerable hydrophobic region (in size), can be incorporated into the phospholipid bilayers. This results in a decrease of the lifetime of Pr3+ cations in the membrane-associated state. No correlation was found to exist between local anaesthesia activity of the study drugs and its capability of displacement polyvalent cations from the membrane surface.