Evidence for analgesia mediated by peripheral opioid receptors in inflamed synovial tissue

Autor: Andrew J Lawrence, A. Michalkiewiczi, W. P. Blunnie, Girish P Joshi, D. C. Moriarty
Rok vydání: 1992
Předmět:
Zdroj: European Journal of Clinical Pharmacology. 43:351-355
ISSN: 1432-1041
0031-6970
DOI: 10.1007/bf02220608
Popis: Intra-articular morphine (5 mg in 25 ml) was administered to patients for post-operative analgesia following arthroscopic knee surgery. At various time intervals, 30 min to 4 h post morphine, venous blood samples were taken in order to determine plasma levels of morphine and its primary metabolites, morphine-3-glucuronide and morphine-6-glucuronide. Measurable amounts of morphine and morphine-3-glucuronide were found in the plasma of 7/10 patients whereas morphine-6-glucuronide was detected in only 2/10 patients. The plasma levels of morphine were lower than that regarded sufficient for post-operative analgesia in all but two patients, indicating a possibility of peripheral analgesia. [p]In addition, synovial biopsy samples were assayed for the presence of opioid binding sites. Tissue samples from 11 different patients were analysed and 6/11 exhibited specific binding of [3H]naloxone, indicating the presence of opioid binding sites/receptors. The receptor type (i. e. μ, δ- or k-) is at present unknown. [p]Taken together, these data provide evidence that locally administered opiates can act on specific opioid receptors in the synovium to mediate analgesia.
Databáze: OpenAIRE