Peptides, as neurotransmitters, neuromodulators, and hormones, influence a multitude of physiological processes by signal transduction mediated through receptors. In addition, during the last 20 years their role in the appearance or maintenance of various diseases could be unequivocally proven. Agents that can imitate or block the biological functions of bioactive peptides (agonists or antagonists, respectively) can be considered as aids for the investigation of peptidergic systems and also as therapeutic agents. The suitability of bioactive peptides as therapeutic agents was examined after preliminary pharmacological experiments. It was thereby shown that based on their pharmacological properties, for example degradation by peptidases or poor bioavailability, they could be employed as drugs in only a few cases. To solve this problem peptidomimetics, compounds that act as substitutes for peptides in their interaction with receptors, have been synthesized. In comparison with native peptides they show higher metabolic stability, better bioavailability, and longer duration of action. Peptidomimetics with antagonistic properties were also developed within the range of these investigations. As a result, new types of treatment and therapy for a series of diseases are possible. Although peptidomimetics have been developed largely by empirical methods (e.g. modification of native peptides, optimization of lead structures), methods for rational design based on investigations into the structure of peptidepeptide receptor complexes and studies of conformation energies, among others, are gradually being established.

Peptidomimetics for Receptor Ligands—Discovery, Development, and Medical Perspectives

Pain can be effectively diminished by various endogenous mechanisms within the central nervous system One region where these mechanisms have been well characterized is the dorsal horn of the spina

The Control of Pain in Peripheral Tissue by Opioids

BACKGROUND:Thoracotomy induces severe postoperative pain and impairment of pulmonary function, and therefore regional analgesia has been intensively studied in this procedure. Thoracic epidural analgesia is commonly considered the “gold standard” in this setting; however, evaluation of the evidence is needed to assess the comparative benefits of alternative techniques, guide clinical practice and identify areas requiring further research. METHODS:In this systematic review of randomized trials we evaluated thoracic epidural, paravertebral, intrathecal, intercostal, and interpleural analgesic techniques, compared to each other and to systemic opioid analgesia, in adult thoracotomy. Postoperative pain, analgesic use, and complications were analyzed. RESULTS:Continuous paravertebral block was as effective as thoracic epidural analgesia with local anesthetic (LA) but was associated with a reduced incidence of hypotension. Paravertebral block reduced the incidence of pulmonary complications compared with systemic analgesia, whereas thoracic epidural analgesia did not. Thoracic epidural analgesia was superior to intrathecal and intercostal techniques, although these were superior to systemic analgesia; interpleural analgesia was inadequate. CONCLUSIONS:Either thoracic epidural analgesia with LA plus opioid or continuous paravertebral block with LA can be recommended. Where these techniques are not possible, or are contraindicated, intrathecal opioid or intercostal nerve block are recommended despite insufficient duration of analgesia, which requires the use of supplementary systemic analgesia. Quantitative meta-analyses were limited by heterogeneity in study design, and subject numbers were small. Further well designed studies are required to investigate the optimum components of the epidural solution and to rigorously evaluate the risks/benefits of continuous infusion paravertebral and intercostal techniques compared with thoracic epidural analgesia. (Anesth Analg 2008;107:1026‐40)

A Systematic Review of Randomized Trials Evaluating Regional Techniques for Postthoracotomy Analgesia

An expanding knowledge of neuropeptides and their function has led to a profound change in our view of how the PAN contributes to pain. In addition to their expected direct action on postsynaptic cells in the dorsal horn, neuropeptides can modify transmitter release from nearby terminals of other PANs and/or diffuse to act on dorsal horn neurons at a considerable distance from their site of release (Fig. 2). Contrary to early expectations and despite the evidence that several neuropeptides excite central nociceptive neurons, there is no clear correspondence between neuropeptide content and physiologically defined classes of small-diameter primary afferents. There is, however, a tendency for populations of afferents innervating different organs to differ consistently in their peptide content. In fact, the peptide content of primary afferents is, in part, determined by specific factors in the tissues that they innervate. Furthermore, peptide content can change dramatically in response to certain prolonged stimuli or nerve damage. The lack of correspondence of peptide content and physiological response pattern, the plasticity of peptide content, its tissue specificity, and the possibility for action at a distance from the site of their release from central PAN terminals strongly suggest that PAN peptides have functions that are fundamentally different from those of the short-range actions of amino acid neurotransmitters that are also found in the PAN. Finally, nowhere is the plasticity of function of the PAN more evident than at its peripheral terminals. Long-term changes are produced in these terminals by a host of peptides that derive from a variety of cell types. The complexity of this transduction process is augmented by the activity- induced release of peripherally active neuropeptides from the PAN itself. In addition to the variety of fundamental neurobiological issues that recent studies of PANs have raised, they have also generated a great deal of clinical interest, in view of the role of the PAN in inflammation and its accessibility for study and for therapeutic intervention.

https://www.jneurosci.org/content/jneuro/13/6/2273.full.pdf

Peptides and the primary afferent nociceptor

Summary As more extensive and painful surgical procedures(e.g., laparoscopic cholecystectomy, adrenalectomy,and nephrectomy, as well as prostatectomy, laminec-tomy, shoulder and knee reconstructions, and hyster-ectomy) are performed on an outpatient or short-staybasis, the use of multimodal perioperative analgesicregimens containing non-opioid analgesic therapieswill probably assume an increasingly important rolein facilitating the recovery process and improving pa-tient satisfaction (3). Optimizing pain management isnecessary to maximize the benefits of ambulatory sur-gery for both patients and health care providers. Ad-ditional outcome studies are needed to validate thebeneficial effects of these newer therapeutic ap-proaches with respect to important recovery variables(e.g., resumption of normal activities and return towork). Although many factors other than pain per se must be controlled to minimize postoperative morbid-ity and facilitate the recovery process after ambulatorysurgery, pain remains a major concern of all patientsundergoing surgical procedures (102).It is clear that the anesthetic technique can influencethe analgesic requirement in the early postoperative

/pdf/the-role-of-non-opioid-analgesic-techniques-in-the-pijk9d0epa.pdf

The role of non-opioid analgesic techniques in the management of pain after ambulatory surgery.

Background. Opioids can produce potent antinociceptive effects by interacting with local opioid receptors in inflamed peripheral tissue. In this study we examined the analgesic effects of the intraarticular, as compared with intravenous, administration of morphine after arthroscopic knee surgery. Methods. In a double-blind, randomized trial, we studied 52 patients who had received one of four injections at the end of surgery. The patients in group 1 (n = 18) received 1 mg of morphine intraarticularly and saline intravenously; those in group 2 (n = 15), saline intraarticularly and 1 mg of morphine intravenously; those in group 3 (n = 10), 0.5 mg of morphine intraarticularly and saline intravenously; and those in group 4 (n = 9), 1 mg of morphine and 0.1 mg of naloxone intraarticularly and saline intravenously. The volume of the intraarticular injections was 40 ml, and that of the intravenous injections was 1 ml. After 1, 2, 3, 4, 6, and 24 hours, postoperative pain was assessed with a visual-analo...

https://www.nejm.org/doi/pdf/10.1056/NEJM199110173251602

Analgesic effect of intraarticular morphine after arthroscopic knee surgery.

We have investigated the effect of interpleural morphine on postoperative pain and pulmonary function after thoracotomy. At the end of surgery, an interpleural catheter was inserted in 17 patients and, in a double-blind and randomized manner, either a bolus of morphine 2.5 mg interpleurally (i.p.) and normal saline i.v. (group I) or, as a control for systemic absorption, morphine 2.5mg i.v. and i.p. saline (group II) was injected. After the initial bolus, a continuous infusion of morphine 0.5 mg h−1 i.p. and saline i.v. (group I) or morphine 0.5 mg i.v. and saline i.p. (group II) was maintained for 24 h. Postoperative pain was assessed by a visual analogue scale, a numerical rating scale and the McGill Pain Questionnaire. Pulmonary function was assessed by spirometry. Supplementary analgesics, side effects, degree of sedation, vital signs and chest tube drainage were recorded. All variables were assessed on the day before surgery and 1, 2, 3, 4, 5, 6 and 24 h and 7 days after surgery. Supplementary morphine was given upon request. There was no significant difference in any pain measure or postoperative pulmonary function variable between the groups. We conclude that, after thoracotomy. interpleural morphine does not provide superior analgesia or improve pulmonary function compared with systemic morphine.

Effect of interpleural morphine on postoperative pain and pulmonary function after thoracotomy

Analgesic Effect of Intraarticular Morphine After Arthroscopic Knee Surgery

Analgesic effect of intraarticular morphine after arthroscopic knee surgery

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Analgesic effect of intraarticular morphine after arthroscopic knee surgery.

Effect of interpleural morphine on postoperative pain and pulmonary function after thoracotomy

Analgesic Effect of Intraarticular Morphine After Arthroscopic Knee Surgery

Analgesic effect of intraarticular morphine after arthroscopic knee surgery