Articles: opioid-analgesics.
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The ability of morphine, fentanyl, butorphanol, nalbuphine, and dezocine to compete with radiolabeled ligands for binding at the mu1, mu2, kappa1, and delta opioid receptors and the sigma receptor was characterized. In the absence of sodium, the potency of opioid receptor competition at each receptor site was found to be: mu1-fentanyl > butorphanol > morphine > or = dezocine = nalbuphine; mu2-butorphanol > fentanyl > nalbuphine > morphine = dezocine; kappa1-butorphanol > nalbuphine > morphine > or = dezocine > fentanyl; and delta-butorphanol > nalbuphine > or = dezocine > morphine > fentanyl. For all five compounds, competition at the sigma receptor was weak, with nalbuphine and dezocine having Kis of approximately 0.5 microM and the other opioids having Kis of greater than 1 microM. Since the presence of 100 mM NaCl during the competitive binding decreased the K(i), to varying degrees, of all five opioids at the mu1 and delta receptors and of some of the opioids at the mu2 and kappa1 receptors, the five compounds studied appear to differ in efficacy at the five receptor sites.
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The purpose of this review is to emphasise the ineffectiveness of traditional analgesic therapy in paediatric patients after surgery, to examine the sensation of pain in infants and children, and to describe the use of intravenous opioids for postoperative analgesia. The management of acute postoperative pain in the paediatric surgical population has been poor. This is despite the knowledge that infants and children have sufficient neurological development at birth to sense pain, and that the same hormonal and metabolic responses to nociceptive stimuli that occur in adult also occur in the neonate. ⋯ Two of these, continuous intravenous opioid infusion and patient-controlled analgesia, have proved to be very successful. Children older than six months can receive either modality safely with regular monitoring by qualified nursing staff. Infants younger than six months receiving continuous opioid infusions should be monitored in high-dependency units.
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It is commonly recognized than opioids analgesics have an major place in the treatment of pain. In spite of guidelines, opioids drugs remain underutilized in chronic cancer pain and acute severe pain. Among the possible factors, involved in the insufficient use of opioids drugs, is the fear (opiophoby) of physicians, nurses, patients and family to induce or to maintain an addiction. ⋯ We will examined the place of morphine-like drugs in the treatment of severe acute pain and chronic cancer pain, the definition of dependency in pain patients, the assessment of the dependency potential in patients treated for pain. Available studies indicate that iatrogenic addiction is quite scarce and that the risk for a major tolerance is very small. Further studies will be necessary, since opioids analgesics may also be useful in some non-cancer chronic pain.