Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0184567 (acute pain)
 3,962 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Rofecoxib is a selective cyclooxygenase (COX)-2 inhibitor that is approved for the treatment of acute pain and osteoarthritis in adults. A sensitive and rapid high-performance liquid chromatographic (HPLC) method of determining rofecoxib in human serum is described. Alkalinized plasma samples are extracted into an organic solvent containing an internal standard and evaporated under nitrogen. The dried sample residues are reconstituted with mobile phase and analyzed by HPLC. The method uses 100 microL of the sample and is linear from 20 to 2000 ng/mL of rofecoxib. Precision and accuracy studies are performed. Stability of the drug in serum over four weeks is documented. This new method is simple, sensitive, precise, and accurate. Its use will translate into faster laboratory turnaround time, and the small sample volume required (100 microL) makes this assay suitable for pediatric patients. This assay will expedite pharmacokinetic studies and the therapeutic drug monitoring of rofecoxib and possibly other COX-2 inhibitors.
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PMID:A rapid and sensitive high-performance liquid chromatography assay for rofecoxib in human serum. 1186 83

Opioids represent the frontline treatment for acute pain, despite their side effects, motivating efforts toward developing novel opioid analgesics. To facilitate these efforts, a novel modeling approach, the conformationally sampled pharmacophore (CSP), has been developed that increases the probability of including the receptor bound form in the model. This method, originally used for developing a nonpeptidic delta opioid efficacy pharmacophore, is extended to peptidic ligands using replica exchange molecular dynamics simulation for conformational sampling. The developed 2D CSP indicates that the spatial relationship of the basic nitrogen and the hydrophobic moiety in the delta opioid ligands differentiates activity. In addition, results indicate that both peptidic and nonpeptidic ligands have the same binding mode with the receptor. Thus, the CSP approach distinguishes both peptidic and nonpeptidic delta opioid agonists and antagonists and is anticipated to be of general utility for the development of pharmacophores for species with multiple rotatable bonds.
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PMID:Conformationally sampled pharmacophore for peptidic delta opioid ligands. 1630 16

The clinical severity of sickle-cell disease (SCD) is dependent on genetic and environmental variables. Environmental factors have been poorly studied. We have investigated possible links between air pollution and acute pain in SCD. We retrospectively studied the numbers of daily admissions with acute sickle-cell pain to King's College Hospital, London, in relation to local daily air quality measurements. We analysed 1047 admissions over 1400 d (1st January 1998-31st October 2001). Time series analysis was performed using the cross-correlation function (CCF). CCF showed a significant association between increased numbers of admissions and low levels of nitric oxide (NO), low levels of carbon monoxide (CO) and high levels of ozone (O(3)). There was no association with sulphur dioxide (SO(2)), nitrogen dioxide or PM(10) (dust). The significant results were further examined using quartile analysis. This confirmed that high levels of O(3) and low levels of CO were associated with increased numbers of hospital admissions. Low NO levels were also associated with increased admissions but did not reach statistical significance on quartile analysis. Our study suggests air quality has a significant effect on acute pain in SCD and that patients should be counselled accordingly. The potential beneficial effect of CO and NO is intriguing and requires further investigation.
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PMID:The associations between air quality and the number of hospital admissions for acute pain and sickle-cell disease in an urban environment. 1734 Dec 71

Celecoxib is intended for acute pain, menstrual cramps, pain, and inflammation of osteoarthritis and rheumatoid arthritis. The aim of this study was to evaluate the effects of celecoxib (10 and 50 mg/kg/day) treatment on rats orally for 28 days. We examined effects on some biochemical parameters and kidney and liver tissues of celecoxib-treated Wistar albino male rats. At the end of the study, hepatic and renal function tests were performed and liver and kidney of rats were microscopically examined to detect systemic toxicity of celecoxib. Celecoxib-treated rats had statistically significant decreases of cholesterol, total bilirubin, total protein, urea, globulin, blood urea nitrogen, phosphorus, and calcium. Serum gamma glutamyl transferase levels increased in 10- and 50-mg/kg/day celecoxib-treated rats. Histological examinations showed mononuclear cell infiltration, hyperplasia, and cellular degeneration in liver and tubular damage and mononuclear cell infiltration in kidney. We suggest that high doses of celecoxib may cause changes in liver and kidney histopathology, liver function, and in some biochemical parameters.
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PMID:Pathological and biochemical effects of therapeutic and supratherapeutic doses of celecoxib in Wistar albino male rats. 2012 24

Novel chroman and tetrahydroquinoline ureas were synthesized and evaluated for their activity as TRPV1 antagonists. It was found that aryl substituents on the 7- or 8-position of both bicyclic scaffolds imparted the best in vitro potency at TRPV1. The most potent chroman ureas were assessed in chronic and acute pain models, and compounds with the ability to cross the blood-brain barrier were shown to be highly efficacious. The tetrahydroquinoline ureas were found to be potent CYP3A4 inhibitors, but replacement of bulky substituents at the nitrogen atom of the tetrahydroisoquinoline moiety with small groups such as methyl can minimize the inhibition.
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PMID:Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists. 2131 87

Compartment syndrome is known to develop after a prolonged surgery in the lithotomy position. We experienced acute renal failure following compartment syndrome after the surgery in hemilithotomy position. A 62-year-old man underwent a left hip fixation for femoral neck fracture. The surgical leg was placed into traction in a foot piece and the intact leg was placed in the hemilithotomy position. Because of the difficulty in repositioning and the trouble with fluoroscope, the surgery took over 5 hours. He suffered acute pain, swelling and spasm in his intact leg placed into hemilithotomy after the surgery. Creatine kinase, blood urea nitrogen and creatinine markedly increased and myoglobinuria was recognized. We diagnosed an acute renal failure following compartment syndrome and treated him in the ICU on close monitoring. In spite of the treatment with massive transfusion and diuretics, he needed hemodialysis twice and then his renal function improved. Prevention is most essential for compartment syndrome after a prolonged surgery in the lithotomy position. Risk factors should be recognized before surgery and appropriate action should be taken such as using Allen stirrups and avoiding hypotension, hypovolemia and the prolonged lithotomy position with exaggerated elevation of legs.
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PMID:[A case of acute renal failure following compartment syndrome after the surgery for femoral neck fracture]. 2347 27