The binding of ketamine to plasma proteins: Emphasis on human plasma

Effects of Alcohols and Anesthetics on Recombinant Voltage-Gated Na+ Channels

“…Another study showed that ketamine inhibited both TTX-sensitive and TTX-resistant Na ϩ channels with IC 50 values of 150 to 850 M in rat DRG neurons (Zhou and Zhao, 2000). We estimated the anesthetic EC 50 of ketamine as 2 M based on the free serum concentration of ketamine measured in blood on awaking (Idvall et al, 1979;Dayton et al, 1983), and we did not observe statistically significant inhibition by ketamine at clinically relevant concentrations. For urethane, we observed significant inhibition by urethane at both 1 and 2 MAC.…”

Effects of Anesthetics on Mutant N-Methyl-d-Aspartate Receptors Expressed in Xenopus Oocytes

“…All compounds were tested at a concentration corresponding to MAC (or the predicted MAC for F6) in the final bath concentration. Calculated 1 MAC for isoflurane, halothane, chloroform, n-hexanol, n-octanol, F3, F6, and ketamine were 0.32 mM, 0.25 mM, 1 mM, 0.57 mM, 57 M, 0.8 mM, 17.8 M, and 2 M, respectively (Saidman et al, 1967;Idvall et al, 1979;Dayton et al, 1983;Mihic et al, 1994;Dildy-Mayfield et al, 1996). The bath concentration of cyclopropane (0.57 atm, 12.2 mM) corresponded to approximately 1 MAC .…”

Effects of Ketamine on Human UDP-Glucuronosyltransferases In Vitro Predict Potential Drug-Drug Interactions Arising from Ketamine Inhibition of Codeine and Morphine Glucuronidation

“…The inhibitor concentration ([I]) in vivo was taken as either the total or unbound concentrations of KTM in plasma after anesthetic and analgesic doses (see Results and Discussion). The mean unbound fraction of KTM in the plasma of healthy subjects has been reported as 0.73 (Dayton et al, 1983).…”