PubMed · 13008030
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E H SEWARD. 1953. Insect nerve blocks?. https://doi.org/10.1111/j.1365-2044.1953.tb12289.x
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Intramuscular injections are still part of routine care in the treatment of children. Vaccines, premedications and analgesics are administered by this route. The pain associated with an intramuscular injection is severe, the risk of complications is increased, and pharmacodynamics and pharmacokinetics are unpredictable. In many cases, equivalent alternatives of rectal, oral or intranasal routes of administering pharmacologic agents exist. Intramuscular injection of analgesics and premedications to children are-except in case of emergencies-obsolete. This demand corresponds to the guidelines of the World Health Organization (WHO) and the International Association for the Study of Pain (IASP).
We are reporting on the case of an 11-year old girl with a malignant tumour. The extreme pain throughout the body could not be treated by conventional methods. By intravenous application of a morphine and s-ketamine mixture we were able to achieve a very effective analgesic result. Apart from the opiate effect of the morphine the decisive factor was the NMDA-antagonism of the s-ketamine. The latter suppresses central sensitisation and chronic pain and reduces or even prevents the development of opioid tolerance. It was possible to use smaller opiate doses more effectively, thus reducing the side effects of the pain therapy. Under associated whole-body thermochemotherapy the girl experienced general pain relief and we were able to return to conventional therapy with a fentanyl plaster.
The development of buprenorphine as a treatment for opiate abuse and dependence has drawn attention to opioid ligands that have agonist actions followed by long-lasting antagonist actions. In a search for alternatives to buprenorphine, we discovered a bridged pyrrolidinomorphinan (BU72). In vitro, BU72 displayed high affinity and efficacy for mu-opioid receptors, but was also a partial delta-opioid receptor agonist and a full kappa-opioid receptor agonist. BU72 was a highly potent and long-lasting antinociceptive agent against both thermal and chemical nociception in the mouse and against thermal nociception in the monkey. These effects were prevented by mu-, but not kappa- or delta-, opioid receptor antagonists. Once the agonist effects of BU72 had subsided, the compound acted to attenuate the antinociceptive action of morphine. BU72 is too efficacious for human use but manipulation to reduce efficacy could provide a lead to the development of a treatment for opioid dependence.