scholarly journals Administration of a co-crystal of tramadol and celecoxib in a 1:1 molecular ratio produces synergistic antinociceptive effects in a postoperative pain model in rats

2018 ◽  
Vol 833 ◽  
pp. 370-378 ◽  
Author(s):  
Manuel Merlos ◽  
Enrique Portillo-Salido ◽  
Alex Brenchat ◽  
Bertrand Aubel ◽  
Jordi Buxens ◽  
...  
2015 ◽  
Vol 53 (11) ◽  
pp. 1621-1627 ◽  
Author(s):  
Sonja Vuckovic ◽  
Dragana Srebro ◽  
Katarina Savic Vujovic ◽  
Milica Prostran

2013 ◽  
Vol 65 (1) ◽  
pp. 55 ◽  
Author(s):  
In Ji Kim ◽  
Cheon Hee Park ◽  
Seong Heon Lee ◽  
Myung Ha Yoon

2020 ◽  
Vol 11 ◽  
Author(s):  
Chizuko Watanabe ◽  
Asami Komiyama ◽  
Masaru Yoshizumi ◽  
Shinobu Sakurada ◽  
Hirokazu Mizoguchi

The antinociceptive effect of methadone in the morphine-resistant inflammatory pain state was described in the paw-withdrawal test using the complete Freund’s adjuvant (CFA)-induced mouse inflammatory pain model. After intraplantar (i.pl.) injection of CFA, thermal hyperalgesia was observed in the ipsilateral paw. The antinociceptive effects of subcutaneous (s.c.) injection of morphine, fentanyl, and oxycodone against thermal hyperalgesia in the inflammatory pain state were reduced in the ipsilateral paw 7 days after CFA pretreatment. On the contrary, the antinociceptive effect of s.c. injection of methadone was maintained in the ipsilateral paw 7 days after CFA pretreatment. The suppressed morphine antinociception in the CFA model mice was bilaterally restored following s.c. treatment with methadone 20 min prior to or 3 days after CFA pretreatment. The suppressed morphine antinociception was also bilaterally restored by intraperitoneal treatment with MK-801 30 min prior to CFA pretreatment; however, the s.c. injection of morphine 30 min prior to CFA pretreatment failed to restore the suppressed morphine antinociception in the CFA model mice. The expression level of mRNA for µ-opioid receptors 7 days after i.pl. pretreatment was not significantly changed by i.pl. pretreatment with CFA or s.c. pretreatment with methadone. In conclusion, methadone is extremely effective against thermal hyperalgesia in the morphine-resistant inflammatory pain state, and restores suppressed morphine antinociception in the inflammatory pain state without altering the expression level of mRNA for µ-opioid receptors.


2012 ◽  
Vol 2012 ◽  
pp. 1-5 ◽  
Author(s):  
Claudio Laurido ◽  
Alejandro Hernández ◽  
Teresa Pelissier ◽  
Luis Constandil

N-methyl-D-aspartic acid receptor (NMDAr) activation requires the presence of D-serine, synthesized from L-serine by a pyridoxal 5′-phosphate-dependent serine racemase (SR). D-serine levels can be lowered by inhibiting the racemization of L-serine. L-serine-O-sulfate (LSOS) and L-erythro-3-hydroxyaspartate (LEHA), among others, have proven to be effective in reducing the D-serine levels in culture cells. It is tempting then to try these compounds in their effectiveness to decrease nociceptive levels in rat arthritic pain. We measured the C-reflex paradigm and wind-up potentiation in the presence of intrathecally injected LSOS (100 μg/10 μL) and LEHA (100 μg/10 μL) in normal and monoarthritic rats. Both compounds decreased the wind-up activity in normal and monoarthritic rats. Accordingly, all the antinociceptive effects were abolished when 300 μg/10 μL of D-serine were injected intrathecally. Since noin vivoresults have been presented so far, this constitutes the first evidence that SR inhibitions lower the D-serine levels, thus decreasing the NMDAr activity and the consequent development and maintenance of chronic pain.


1999 ◽  
Vol 55 (6) ◽  
pp. 425-429 ◽  
Author(s):  
G. B. Curtis ◽  
G. H. Johnson ◽  
P. Clark ◽  
R. Taylor ◽  
J. Brown ◽  
...  

2022 ◽  
Vol 14 (1) ◽  
Author(s):  
Walid Y. Kamel ◽  
Aktham Adel Shoukry

Abstract Background Magnesium (Mg) is a non-competitive N-methyl d-aspartate receptor antagonist with antinociceptive effects. Multimodal therapy is the optimal strategy for perioperative pain control to minimize the need for opioids. Inflammation caused by tissue trauma or direct nerve injury is responsible for the perioperative pain. The concept of “pre-emptive” analgesia, analgesic strategies administered prior to the stimulus, can modify the peripheral and central nervous system processing of noxious stimuli, thereby reducing central sensitization, hyperalgesia, and allodynia remains controversial. A more encompassing approach to the reduction of postoperative pain is the concept of “preventive” analgesia. The purpose of the study is to detect the proper use of MgSO4 as an analgesic being a non-competitive N-methyl d-aspartate (NMDA). Results There is no statistically significant difference in the haemodynamic parameters, intraoperative (33% vs 20%) and postoperative requirement for analgesics 6.6% vs 10% among groups I and II, respectively. There is no significant difference in the numerical analogue scale, where 16 vs 17 patients with no pain, 12 vs 10 with mild pain, and 2 vs 3 with moderate pain in groups I and II, respectively. Conclusion The use of MgSO4 in a bolus with or without infusion is comparable in the control of intraoperative and postoperative pain.


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