title: The penetration of local anesthetics into phosphatidylcholine monolayers.
abstract: The penetration of tetracaine into monolayers of phosphatidylcholine and trioctanoin at different surface pressures, and the penetration of dibucaine, tetracaine, butacaine, lidocaine, and procaine into monolayers of didecanoylphosphatidylcholine at II = 10 mN/m was determined by the use of a modified Gibbs adsorption equation. These data were shown to fit a geometric model and compared favorably with data determined by a method based on the geometric model. The penetration of tetracaine into phosphatidylcholine monolayers was pressure dependent. At II = 10 mN/m, the local anesthetics penetrate into a phosphatidycholine monolayer in the order: dibucaine greater than tetracaine greater than butacaine greater than lidocaine greater than procaine. This correlates with their potencies in blocking nerve conduction and inhibiting phospholipase A2.
mesh_terms: D010129:4-Aminobenzoic Acid; D000779:Anesthetics, Local; D001692:Biological Transport; D003992:Dibucaine; D007700:Kinetics; D008012:Lidocaine; D008567:Membranes, Artificial; D008954:Models, Biological; D010539:Permeability; D010713:Phosphatidylcholines; D011343:Procaine; D013329:Structure-Activity Relationship; D013748:Tetracaine; D014280:Triglycerides
chemical_list: D000779:Anesthetics, Local; D008567:Membranes, Artificial; D010713:Phosphatidylcholines; D014280:Triglycerides; D013748:Tetracaine; D011343:Procaine; D008012:Lidocaine; D003992:Dibucaine; D010129:4-Aminobenzoic Acid