Increased brain uptake of lidocaine during bicuculline-induced status epilepticus in rats.
Following rapid IV injection (0.1 mg per kilogram) lidocaine HCl concentrations were measured in the blood and brain of paralyzed, ventilated rats during bicuculline-induced status epilepticus and in identically prepared controls. The concentration of lidocaine in blood and brain was consistently higher in convulsing than in nonconvulsing rats. At 1 minute, increased brain lidocaine reflected elevated blood concentrations; increased brain and blood partitioning after 1 minute is responsible for subsequent increases in brain lidocaine uptake. The therapeutic index of lidocaine is low; the concentration of lidocaine is increased in the convulsing brain. Our data suggest that conventional lidocaine doses may perpetuate rather than control refractory convulsions.
D000818:Animals; D001640:Bicuculline / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D001812:Blood-Brain Barrier / Q000187:drug effects*; D001921:Brain / Q000378:metabolism; D004569:Electroencephalography / Q000379:methods; D005071:Evoked Potentials / Q000187:drug effects; D008012:Lidocaine / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013226:Status Epilepticus / Q000139:chemically induced* / Q000378:metabolism
D008012:Lidocaine; D001640:Bicuculline