Articles: opioid-analgesics.
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J. Pharmacol. Exp. Ther. · Oct 1989
Kappa-opioid receptor-mediated antinociception in the rat. II. Supraspinal in addition to spinal sites of action.
This study examines whether there is a supraspinal, in addition to spinal, component to the antinociceptive actions against heat and pressure stimuli of kappa-opioid receptor agonists (U-69,593, U50,488H, bremazocine and tifluadom) as compared to mu-opioid receptor agonists (Tyr-D-Ala-Gly-NMe-Gly-ol, fentanyl and morphine) in the rat. The antinociception induced by kappa- and mu-opioids (applied s.c.) was unaffected by systemic quaternary naltrexone (50 mg/kg) revealing that it is mediated in the central nervous system. All kappa- and mu-opioids produced dose-dependent antinociception upon intrathecal application, in each case reversible by naloxone (5 mg/kg s.c.). ⋯ Naltrexone was 10-fold more potent in blocking morphine as compared to U50,488H whereas nor-binaltorphimine, a preferential kappa-antagonist, was 6-fold more potent against U50,488H than morphine. Indeed, whereas a dose of 0.2 mg/kg of naltrexone reversed mu-agonist actions, this dose was inactive against all kappa-agonists: the actions of these could be antagonized only by 2.0 mg/kg. These data indicate that in addition to kappa-receptors in the spinal cord, kappa-receptors in the brain can mediate antinociception against noxious heat and pressure.
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Six groups of ten women each in active labor at term had epidural catheters placed in the usual manner and received a 3 mL test dose of 2% lidocaine with epinephrine. Groups 1-6 received, respectively, 5, 10, 20, 30, 40 and 50 micrograms of sufentanil diluted to 10 mL with normal saline. Significantly effective analgesia was provided at all sufentanil doses studied, with pain scores decreasing from 8.1 +/- 0.2 at baseline to 2.9 +/- 0.3 at 10 minutes and 1.1 +/- 0.2 at 30 minutes (mean +/- SEM, average for all groups). ⋯ There were no serious maternal side effects, although ten patients developed pruritus, four became dizzy, two experienced mild sedation, and one had transient hypotension. No neonatal side effects occurred. Maternal serum sufentanil levels remained below the sensitivity of the assay, or 0.1 ng/ml.
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Randomized Controlled Trial Comparative Study Clinical Trial
A comparison of the incidence of pruritus following epidural opioid administration in the parturient.
Epidural morphine is associated with a high incidence of pruritus when used for pain control in the post-Caesarean section population. The purpose of this study was to compare the incidence of pruritus associated with epidural morphine, fentanyl, buprenorphine and butorphanol. ⋯ This study demonstrated that the incidence of pruritus was significantly higher following the use of epidural morphine and fentanyl. Even though epidural butorphanol and buprenorphine exhibited a low incidence of pruritus, their duration of analgesia was not long enough to make either attractive for single-dose administration.
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Klinische Pädiatrie · Jul 1989
[Use of strong opioids in the treatment of cancer pain in adults and children].
A high percentage of adults and children with advanced cancer suffer from pain. Strong opioids for pain control, e.g. morphine, slow-released morphine or buprenorphine, should be administered early according to the intensity of pain. The analgesics should be given orally whenever possible. ⋯ Correctly used strong opioids produce only a few side-effects, especially constipation and vomiting. Many studies in adult cancer patients all over the world demonstrate the effectiveness of strong opioids for pain control. Children should be treated in the same way and comparable data in children with cancer pain must be collected.
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Patients receiving intraspinal opiates should be monitored in the intensive care unit for at least 24 hours to prevent potentially lethal outcomes. These include respiratory depression caused by sequestration of the morphine in the cerebrospinal fluid and migration of epidural catheters in the subarachnoid or intravascular space. At this time, most hospitals are not equipped or staffed adequately to guarantee the safety of these patients outside the intensive care unit.