TY - JOUR T1 - THE INFLUENCE OF CO<sub>2</sub> AND pH ON LOCAL ANESTHETIC ACTION JF - Journal of Pharmacology and Experimental Therapeutics JO - J Pharmacol Exp Ther SP - 298 LP - 309 VL - 181 IS - 2 AU - RICHARD F. H. CATCHLOVE Y1 - 1972/05/01 UR - http://jpet.aspetjournals.org/content/181/2/298.abstract N2 - Local anesthetic solutions having different combinations of pCO2 and pH were applied to sheathed and desheathed frog nerves while recording the compound action potential. CO2 (1-50%) and local anesthetic (1.0 mM) caused a much greater block when given together than when applied separately. The effect was maximal at a relatively high pH (7.3). The permeability of the nerve sheath to radioactive lidocaine and sucrose was measured while perfusing these substances through a segment of isolated sheath. The apparent permeability to the anesthetic was a linear function of the fraction of nonionized lidocaine and this permeability was not changed by varying pCO2 or pH. It was concluded that CO2 potentiates the action of local anesthetics by 1) a direct depressant effect of CO2 on the axon, 2) concentrating local anesthetic inside the nerve trunk (diffusion trapping) and 3) converting local anesthetic to the active cation through its effect on pH at the site of action inside the nerve. © 1972 by The Williams &amp; Wilkins Co. ER -