Opiate-like analgesic activity in general anaesthetics

British Journal of Pharmacology
D Lawrence, A Livingston

Abstract

1 The interaction of naloxone with various anaesthetics was studied both in vivo and in vitro.2 Naloxone (10 mg/kg) did not significantly alter the anaesthetic duration of halothane, diethylether, ketamine, pentobarbitone or Althesin.3 Naloxone (10 mg/kg) reduced the analgesic activity of nitrous oxide, ketamine and morphine in the rat tail-flick test. With the exception of pentobarbitone and Althesin, the other anaesthetic agents also induced analgesia but were not antagonized by naloxone.4 Specific [(3)H]-dihydromorphine binding was displaced by the opiates naloxone (IC(50) = 7.6 nm), methionine-enkephalin (Met-enkephalin, IC(50) = 40 nm) and morphine (IC(50) = 54 nm). Similarly, displacement was observed with xylazine (IC(50) = 9 mum), ketamine (IC(50) = 130 mum) and Althesin (IC(50) = 150 mum); other anaesthetics agents tested were inactive in mm concentrations.5 Ketamine (IC(50) = 200 mum) and xylazine (IC(50) = 9.5 mum) were also capable of displacing specific [(3)H]-D-Ala(2)-enkephalin (D-Leu) binding, as were morphine (IC(50) = 95 nm) and Met-enkephalin (IC(50) = 40 nm).6 On the stimulated guinea-pig ileum, Met-enkephalin and morphine inhibited the contractions, the IC(50) values were 30 nm and 50 nm respectively. The a...Continue Reading

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Citations

Feb 2, 1988·Brain Research·R M Quock, L M Graczak
Jun 1, 1995·Pharmacology, Biochemistry, and Behavior·V PirecJ P Zacny
Nov 1, 1994·Pharmacology, Biochemistry, and Behavior·J P ZacnyP Thapar
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Jul 1, 1995·Intensive Care Medicine·J FassV Schumpelick
Mar 14, 2007·Anesthesia Progress·Dimitris E Emmanouil, Raymond M Quock
May 1, 1990·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·R M QuockD C Chen
Dec 1, 1992·Pain·Douglas S RamsayStephen C Woods
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Aug 17, 2001·International Anesthesiology Clinics·Y NakataS Morita
Jan 1, 1991·Drug Metabolism and Drug Interactions·M R DzoljicS L Cappendijk

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