Structure-activity relationships (SAR) are studied in the series of 4,4-disubstituted piperidine morphinomimetics (42 compounds) by means of the Electronic-Topological Method (ETM). In the frameworks of this approach, its input data were taken as the results of conformational and quantum-mechanical calculations. These calculations had been carried out for all compounds from the series under study, taking into account their neutral and protonated by the nitrogen of piperidine cycle forms. The ETM application resulted in a set of pharmacophores and anti-pharmacophores, which formed a basis of a system used to predict analgesic activity. First of all, the system was tested on known analgesics. Testing has shown a good agreement with the experimental data. Then, the system was applied to a few compounds with similar structures but unknown activity. The results of the study could be used for computer screening and design of novel compounds with analgesics properties as new potential drugs.

Delirium is a common complication in hospitalized patients and is often associated with significant morbidity. It is important to recognize this syndrome early so that potential causes can be identified and properly managed. Although the etiology of delirium in critically or terminally ill patients is often multifactorial, opioid analgesics are often implicated as a potential underlying cause. Certain opioids, such as meperidine, have been identified as having a greater potential for causing delirium than others. There have been no published reports of anileridine-induced delirium and an illustrative case is presented.

This article describes our experience in the clinical use of nebulized opioids for the management of dyspnoea in patients with terminal cancer by reviewing three specific patient case studies in which this treatment was found to be both safe and effective in controlling breathlessness. The patients were treated with morphine, hydromorphone or anileridine in various doses according to their prior use of opioids. Additional formal studies are being initiated at this Centre.

The method for the analysis of anileridine, levorphanol, nalbuphine and ethamivan in urine by means of GC/NPD and GC/MSD is described. TFAA and MSTFA-MBTFA have been used in this procedure for TFA and TMS derivatization. The parent forms and the metabolites of the four drugs can be found by GC/NPD screening and GC/MSD confirmation. The method is reliable, fast and sensitive.

The analgesic effects of meperidine, anileridine, codeine and codeine + acetominophen on surgical and non-surgical pain in 101 patients were assessed using the McGill Pain Questionnaire. The quality of analgesia was determined by analyzing the changes in the pain descriptors chosen 1 hour after medication. Meperidine and anileridine differentially reduced pain qualities rated as "bright-phasic" by a student sample. Codeine and codeine + acetominophen produced similar patterns of analgesia that were homogeneous across "bright-phasic" and "dull-tonic" types of pain. The data suggest the possibility that opioids may differ in the quality of analgesia produced either as dose increases or different opioid receptor types are recruited.

Haemodynamic effects of equianalgesic doses of pethidine (1 mk kg -1) and anileridine (0.25 mg kg -1) were compared in patients with coronary artery disease, after induction of anaesthesia with flunitrazepam - N2O - pancuronium. Contrary to previous findings made in conscious patients, these analgesics produced a moderate circulatory depression. Heart rate, cardiac index and rate-pressure product were decreased by both drugs, and anileridine alone decreased mean arterial pressure. The only statistically significant differences in the haemodynamic changes between the two groups were those in pulmonary capillary wedge pressure and rate pressure product, which were slightly lower after anileridine than after pethidine.

Pigeons responded under a multiple fixed-ratio 30-response, fixed-interval 5-min schedule of food presentation. Daily administration of clorgyline (10 mg/kg, IM) tended to decrease rates of responding in both schedule components. Before daily clorgyline, tetrabenazine had no effect or decreased responding in the FI component at doses that markedly increased responding during chronic clorgyline. The clorgyline treatment resulted in a slight increase in sensitivity to the rate-decreasing effects of morphine, but no increased sensitivity to the rate-decreasing effects of meperidine, anileridine, alphaprodine, or fentanyl.

The haemodynamic effects of large bolus doses of metocurine 0.45 mg kg-1 and pancuronium 0.1 mg kg-1 were compared in patients with coronary artery disease anaesthetized with diazepam, anileridine and nitrous oxide. Hypotension occurred more frequently after metocurine and was a result of a decrease in systemic vascular resistance. After pancuronium there was no increase in arterial pressure or heart rate, but a small increase in cardiac index. The decrease in heart rate after metocurine was the principal cause of the statistically significant difference in cardiac index between the two groups. Contrary to previous findings, metocurine did not attenuate circulatory responses to tracheal intubation. During surgical stimulation, two of the 10 patients of the pancuronium group developed significant ST segment depression and three patients had a rate-pressure product greater than 12 000 mm Hg beat min-1. However, the difference in rate-pressure product between the groups was not statistically significant.