Pharmacol Rep
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Combinations of non-steroidal anti-inflammatory drugs with opioids are frequently used to reduce opioid doses required in the clinical management of acute pain. The present study was designed to evaluate the possible antinociceptive interaction between morphine and diclofenac at peripheral level in male rats. ⋯ Data suggest that the combination of morphine with diclofenac at the site of injury is synergistic and could be useful in the treatment of wounds, bruises, rheumatisms and other painful peripheral conditions associated with an inflammatory process.
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Recently, we presented a novel compound (PK20, Dmt-D-Lys-Phe-Phe-Lys-Lys-Pro-Phe-Tle-Leu-OH) that targets single entity opioid and neurotensin pharmacophores. This endomorphin-2-like opioid peptide was introduced as a highly active analgesic because it elicited a strong dose- and time-dependent antinociceptive response when administered centrally and peripherally. Its pain-relieving activity was observed as rapidly as 5 min after drug injection. Such promising results led us to perform further studies, such as determining the resistance to enzymatic degradation, which resulted in obtaining a very stable opioid pharmacore PK20 metabolite. ⋯ The novel MOP receptor selective metabolite has been shown to possess opioid subtype receptor selectivity, high potency, and effective analgesic activities as measured in various bioassays.
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Clinical Trial
Effects of pantoprazole on dual antiplatelet therapy in stable angina pectoris patients after percutaneous coronary intervention.
Our aim was to prospectively assess the potential influence of pantoprazole therapy on the antiplatelet effects of acetylsalicylic acid (ASA) and clopidogrel (CLO) in stable angina pectoris (SAP) patients after percutaneous coronary intervention (PCI). ⋯ Pantoprazole treatment does not impair the efficacy of dual antiplatelet therapy in patients with SAP after PCI.
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Comparative Study
Pregabalin antinociception and its interaction with tramadol in acute model of pain.
The aim of present study was to investigate the antinociceptive effect of pregabalin and tramadol either alone and or in combination on acute model of pain. ⋯ Pregabalin revealed a comparative antinociceptive effect as similar to tramadol in acute model of pain, but interaction between these two drugs depends highly on their proportion in the combination. The analgesia may increase but adverse effects such as seizurogenic effect of tramadol can be reduced in clinical setting if right proportion is used. More studies are required to understand the mechanisms and clinical implication of such combinations.
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Interleukin-1β (IL-1β), the major cytokine involved in activation of hypothalamic-pituitary-adrenal (HPA) axis modulates both central and peripheral components regulating HPA activity. The role of nitric oxide (NO) generated by neuronal nitric oxide synthase (nNOS) and inducible nitric oxide synthase (iNOS) in brain structures involved in HPA axis regulation has not been elucidated. The aim of the study was to assess the receptor selectivity of IL-1β stimulatory action on HPA axis and to determine the involvement of nNOS and iNOS in this stimulation. ⋯ The present study suggests that the IL-1β-induced transient stimulation of HPA axis activity is parallel in time and magnitude to the respective changes of nNOS in hypothalamus and prefrontal cortex, the brain structures involved in regulation of HPA axis activity.