title: Pharmacokinetic nature of tachyphylaxis to lidocaine: peripheral nerve blocks and infiltration anesthesia in rats.
abstract: Tachyphylaxis to peripheral neural blockade was determined with repeated injections of a constant dose of lidocaine in three experimental models: sciatic nerve block, produced by intraneural or extraneural injections, and infiltration anesthesia. A decrease in the duration of the subsequent blocks was used as the index of tachyphylaxis development. The anesthetic content in the nerve or skin was determined using radiolabeled lidocaine. Repeated injections of a constant dose of lidocaine resulted in a marked decrease in the duration of the blocks. Accelerated decline in lidocaine content of nerve or skin was observed with repeated blocks. Our data show that tachyphylaxis rapidly develops with both sciatic nerve blocks and infiltration anesthesia. The data also suggest that the mechanism is largely pharmacokinetic in nature.
authors.affiliation: Department of Anesthesia, Harvard Medical School, Brigham and Women's Hospital, Boston, Massachusetts 02115, USA. choi@zeus.bwh.harvard.edu
authors.forename: R H
authors.initials: RH
authors.lastname: Choi
authors.forename: J K
authors.initials: JK
authors.lastname: Birknes
authors.forename: F A
authors.initials: FA
authors.lastname: Popitz-Bergez
authors.forename: I
authors.initials: I
authors.lastname: Kissin
authors.forename: G R
authors.initials: GR
authors.lastname: Strichartz
mesh_terms: D000772:Anesthesia, Local; D000818:Animals; D008012:Lidocaine / Q000494:pharmacology*; D008297:Male; D009407:Nerve Block; D051381:Rats; D017207:Rats, Sprague-Dawley; D012584:Sciatic Nerve / Q000187:drug effects / Q000502:physiology; D012867:Skin / Q000187:drug effects / Q000294:innervation; D012879:Skin Physiological Phenomena; D013618:Tachyphylaxis
chemical_list: D008012:Lidocaine