PubMed · 1973328
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S Mackay. 1990. Side effects--constipation.. https://pubmed.ncbi.nlm.nih.gov/1973328/
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OBJECTIVE: To analyse the results of the policy of encouraging rational use of analgesics in Spain. DESIGN: Longitudinal retrospective and observational study, on the exhaustive information deriving from the filling out of Analgesic Extra-therapeutic Dose notebooks. SITE. Primary Care treatment of terminal oncological patients carried out basically in the Province of Barcelona. PARTICIPANTS: All treatments carried out under the extra-therapeutic dose notebook during the last quarter of 1988 and the first quarters of 1989, 1990, and 1991. MAIN MEASUREMENTS AND RESULTS: Revision of initial treatment, change of medication and posology and returns on the basis of the extensive documentation generated. Consumption has risen from 157 authorized cases in 1989 to 404 in 1991. CONCLUSIONS: Consumption has increased sharply, although the opinion that such analgesics are under-used still predominates. Along with the quantitative increase there has been a corresponding deterioration in the rationale informing use and control, both medically (patterns of treatment, excesses) and socially (cost effectiveness, fair allocation). The evaluation in force before the advent of new technology and policies should be reinstated if we wish to achieve the desired level of effectiveness, adapting national health care by coordinating social and health care and bringing up to standard the training and supply of information to health workers. It is suggested that a "Consensus" Conference should be organised to bring up to date the basis on which analgesics are used and regulated.
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Receptor binding assays using [3H]DAGO ([D-Ala2,MePhe4-Gly5-ol]enkephalin) (mu), [3H]DPDPE ([D-Pen2,D-Pen5]enkephalin) (delta) and [3H]U-69593 (kappa) were done in guinea pig whole brain membranes. Agonist activity was determined in norbinaltorphimine or beta-funaltrexamine (beta-FNA) treated guinea pig ileum (mu and kappa, respectively) and beta-FNA-treated mouse vas deferens (delta). The compounds with highest affinity were the most potent at the mu-receptor. The selectivity observed in the binding affinities was also found in in vitro activity. No correlation was found between mu-affinity and selectivity; the highest affinity analog, lofentanil, was found to be among the least selective, while another high affinity analog, R30490, was the most mu-selective. The results show that not all fentanyls are highly mu-selective, and could produce actions through delta- and kappa-opiate receptors.