Prolonged sensory-selective nerve blockade.
Sensory-selective local anesthesia has long been a key goal in local anesthetic development. For example, it allows women to be pain-free during labor without compromising their ability to push. Here we show that prolonged sensory-selective nerve block can be produced by specific concentrations of surfactants-such as are used to enhance drug flux across skin-in combination with QX-314, a lidocaine derivative that has relative difficulty penetrating nerves. For example, injection of 25 mM QX-314 in 30 mM octyltrimethylammonium bromide (OTAB) lasted up to 7 h. Sensory selectivity was imparted to varying degrees by cationic, neutral, and anionic surfactants, and also was achieved with another lidocaine derivative, QX-222. Simultaneous injection of OTAB at a s.c. injection site remote from the sciatic nerve did not result in prolonged sensory-specific nerve blockade from QX-314, suggesting that the observed effect is due to a local interaction between the surfactant and the lidocaine derivative, not a systemic effect.
Department of Anesthesiology, Children's Hospital, Harvard Medical School, Boston, MA 02115, USA.
Itay
I
Sagie
Daniel S
DS
Kohane
D000779:Anesthetics, Local / Q000008:administration & dosage*; D000818:Animals; D004347:Drug Interactions; D007279:Injections, Subcutaneous; D008012:Lidocaine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D008297:Male; D009407:Nerve Block / Q000379:methods*; D000644:Quaternary Ammonium Compounds / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012584:Sciatic Nerve / Q000187:drug effects; D011984:Sensory Receptor Cells / Q000187:drug effects*; D013501:Surface-Active Agents / Q000008:administration & dosage*
D000779:Anesthetics, Local; D000644:Quaternary Ammonium Compounds; D013501:Surface-Active Agents; C042006:octyltrimethylammonium; C006072:QX-222; C012647:QX-314; D008012:Lidocaine