Oxycodone reduced postoperative catheter-related bladder discomfort undergoing transurethral resection prostate. A prospective, double -blind randomized study

Background: Catheter-related bladder discomfort (CRBD) is a common and distressing complication that often occurs caused by urinary bladder catheterization and urethral mucosa injury postoperatively. Oxycodone is a semi-synthetic opioids prepared from opium alkaloid the baine plant derivative. Its μ and κ dual-receptor agonism has a unique effect in the treatment of visceral pain. The aim of this study to observe the efficacy of oxycodone for the treatment of CRBD undergo trans-urethral resection prostate (TURP). Methods: Patients with ASA I-III received trans-urethral resection prostate under general anesthesia were enrolled. Patients who complained CRBD were randomized allocated to the control group (n=42) received placebo and the observed group (n=41) received 0.03mg/kg of oxycodone. The severity of CRBD assessed by NRS were assessed at 0, 5min, 1/2h, and 2h after administration of the study agents. VAS scores were used to assess pain intensity during the same period. Postoperative PCA analgesic sufentanil dose during of PACU times and the incidences of agitation, nausea, vomiting, dizziness, over sedation were recorded in these patients. Results: Compared with the control group, the incidence of CRBD was significantly lower in the oxycodone group at 5min and 1/2h. Compared with the controlled group, VAS scores and incidences of agitation were lower in oxycodone group and significantly decreased sufentanil dosage within 6h (P<0.01). There were no significant differences in the incidence of postoperative adverse effects and during of PACU between two groups(P＜0.05). Conclusion: Oxycodone 0.03mg/kg effectively reduced patients with CRBD after TURP without incurring serious adverse effects.Trial registration: Chinese Clinical Trial Registry, ChiCTR-IPR-16008814.

Biological Evaluation of Noscapine analogues as Potent and Microtubule-Targeted Anticancer Agents

In present investigation, an attempt was undertaken to modify the C-9 position of noscapine (Nos), an opium alkaloid to yield 9 -hydroxy methyl and 9 -carbaldehyde oxime analogues for augmenting anticancer potential. The synthesis of 9-hydroxy methyl analogue of Nos was carried out by Blanc reaction and 9-carbaldehyde oxime was engineered by oxime formation method and characterized using FT-IR, 1H NMR, 13C NMR, mass spectroscopy, and so on techniques. In silico docking techniques informed that 9-hydroxy methyl and 9-carbaldehyde oxime analogues of Nos had higher binding energy score as compared to Nos. The IC50 of Nos was estimated to be 46.8 µM signficantly (P < 0.05) higher than 8.2 µM of 9-carbaldehyde oxime and 4.6 µM of 9-hydroxy methyl analogue of Nos in U87, human glioblastoma cells. Moreover, there was significant (P < 0.05) difference between the IC50 of 9-carbaldehyde oxime and 9-hydroxy methyl analogue of Nos. Consistent to in vitro cytotoxicity data, 9-hydroxy methyl analogue of Nos induced significantly (P < 0.05) higher degree of apoptosis of 84.6% in U87 cells as compared to 78.5% and 64.3% demonstrated by 9-carbaldehyde oxime and Nos, respectively. Thus the higher therapeutic efficacy of 9-hydroxy methyl analogue of Nos may be credited to higher solubility and inhibitory constant (K).