Mechanism of action of naloxone and clinical application of.doc

 PAGE \* MERGEFORMAT 13 Mechanism of action of naloxone and clinical application of Keywords:: Naloxone Naloxone (naloxone) in 1960, Synthesis, 1963, for clinical use. In recent years, with in-depth, endogenous opioid peptides is mainly β-endorphin (β-EP) in a variety of diseases, to further clarify the pathophysiological process. The specificity of naloxone as an opioid receptor antagonist, can block and reverse the endogenous opioid peptide toxicity has been widely in clinical various academic subjects. Clinical application of the current situation in the nearest years are summarized below. A pharmacological effect of naloxone 1.1 Pharmacokinetics of naloxone also known as propylene ketone of morphine, in order to hydroxyl derivatives of dihydro-ketone of morphine and its hydrochloride salt, melting point of 200 ℃ ~ 205 ℃, soluble in water and ethanol, insoluble in ether. Intravenous and intratracheal administration of 1 ~ 2min into force; intramuscular and subcutaneous injection of 5 ~ 10min bear fruit; oral poor results, only the role of parenteral administration of 1 / 50. Plasma half-life of 90min, repeat the medication in order to maintain an effective blood concentration, the role of the duration of 45 ~ 90min. Naloxone can free passage of blood-brain barrier, and its adoption to 12 times faster than morphine, administered 5min brain concentrations 4.6 times higher than in plasma, systemic plasma concentrations decline in parallel. The main way of naloxone in the liver metabolism of biological transformation and glucuronic acid binding, 72h in 70% of naloxone in the liver metabolism, the urine discharge [1]. 1.2 The role of the principle of naloxone Naloxone is a competitive antagonist μ.κ.δ receptor activity without excited, and opioid receptor affinity than morphine and enkephalin, can competitively block the opioid-like substance and endogenous opioid peptides mediate a variety of effects [2]. Endogenous opioid pept