title: Ketamine effects on bupivacaine local anaesthetic activity and pharmacokinetics of bupivacaine in mice.
abstract: This study was designed to document possible changes in bupivacaine (B) local anaesthetic activity and pharmacokinetics in mice after a ketamine (K) injection. In the experiments, bupivacaine (8.25 mg.kg(-1)), was injected into the popliteal space of the right posterior limb: the local anaesthetic activity was assessed according to a sciatic nerve blockade method with three different doses (2, 10 and 40 mg/kg) of ketamine and the kinetics were studied after a 10 mg/kg dose. When ketamine was associated, the local anesthetic activity of bupivacaine was significantly enhanced as well as its elimination half-life. Significantly lower levels of the main metabolite, PPX, were observed, when ketamine was associated, suggesting a metabolic inhibition phenomenon. The ketamine-induced increase in the total anaesthetic effect of bupivacaine may thus be explained by kinetic modifications i.e. a possible inhibiting effect of ketamine on the metabolism of bupivacaine.
authors.affiliation: Laboratoire de Pharmacologie Médicale, Faculté de Médecine de Marseille, France.
authors.forename: M
authors.initials: M
authors.lastname: Gantenbein
authors.forename: C
authors.initials: C
authors.lastname: Abat
authors.forename: L
authors.initials: L
authors.lastname: Attolini
authors.forename: P
authors.initials: P
authors.lastname: Pisano
authors.forename: N
authors.initials: N
authors.lastname: Emperaire
authors.forename: B
authors.initials: B
authors.lastname: Bruguerolle
mesh_terms: D000772:Anesthesia, Local; D000778:Anesthetics, Dissociative / Q000494:pharmacology*; D000779:Anesthetics, Local / Q000493:pharmacokinetics*; D000818:Animals; D002045:Bupivacaine / Q000493:pharmacokinetics*; D004347:Drug Interactions; D006207:Half-Life; D007649:Ketamine / Q000008:administration & dosage / Q000494:pharmacology*; D008297:Male; D051379:Mice
chemical_list: D000778:Anesthetics, Dissociative; D000779:Anesthetics, Local; D007649:Ketamine; D002045:Bupivacaine