xanthine oxidase inhibitors
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2021 ◽  
Vol 11 (1) ◽  
pp. 166
Author(s):  
Jennifer S. Weaver ◽  
Ernest R. Vina ◽  
Peter L. Munk ◽  
Andrea S. Klauser ◽  
Jamie M. Elifritz ◽  
...  

Gout, a crystalline arthropathy caused by the deposition of monosodium urate crystals in the articular and periarticular soft tissues, is a frequent cause of painful arthropathy. Imaging has an important role in the initial evaluation as well as the treatment and follow up of gouty arthropathy. The imaging findings of gouty arthropathy on radiography, ultrasonography, computed tomography, dual energy computed tomography, and magnetic resonance imaging are described to include findings of the early, acute and chronic phases of gout. These findings include early monosodium urate deposits, osseous erosions, and tophi, which may involve periarticular tissues, tendons, and bursae. Treatment of gout includes non-steroidal anti-inflammatories, colchicine, glucocorticoids, interleukin-1 inhibitors, xanthine oxidase inhibitors, uricosuric drugs, and recombinant uricase. Imaging is critical in monitoring response to therapy; clinical management can be modulated based on imaging findings. This review article describes the current standard of care in imaging and treatment of gouty arthropathy.


2021 ◽  
Vol 59 (6) ◽  
pp. 727-737
Author(s):  
T. S. Panevin ◽  
M. S. Eliseev ◽  
E. L. Nasonov

The main direction of drug therapy for gout and other diseases associated with hyperuricemia is the long-term use of drugs aimed at correcting the level of uric acid. However, in addition to the urate-lowering effect, these drugs may have other beneficial pleiotropic effects. The article will discuss the additional effects of xanthine oxidase inhibitors, as well as drugs used to treat gout-related diseases that have urate-lowering effects.


2021 ◽  
pp. 2100245
Author(s):  
Kentaro Kawai ◽  
Yoshitaka Asanuma ◽  
Toshiki Kato ◽  
Yukiko Karuo ◽  
Atsushi Tarui ◽  
...  

Biomedicines ◽  
2021 ◽  
Vol 9 (10) ◽  
pp. 1443
Author(s):  
João L. Serrano ◽  
Diana Lopes ◽  
Melani J. A. Reis ◽  
Renato E. F. Boto ◽  
Samuel Silvestre ◽  
...  

Xanthine oxidase (XO) is the enzyme responsible for the conversion of endogenous purines into uric acid. Therefore, this enzyme has been associated with pathological conditions caused by hyperuricemia, such as the disease commonly known as gout. Barbiturates and their congeners thiobarbiturates represent a class of heterocyclic drugs capable of influencing neurotransmission. However, in recent years a very large group of potential pharmaceutical and medicinal applications have been related to their structure. This great diversity of biological activities is directly linked to the enormous opportunities found for chemical change off the back of these findings. With this in mind, sixteen bis-thiobarbiturates were synthesized in moderate to excellent reactional yields, and their antioxidant, anti-proliferative, and XO inhibitory activity were evaluated. In general, all bis-thiobarbiturates present a good antioxidant performance and an excellent ability to inhibit XO at a concentration of 30 µM, eight of them are superior to those observed with the reference drug allopurinol (Allo), nevertheless they were not as effective as febuxostat. The most powerful bis-thiobarbiturate within this set showed in vitro IC50 of 1.79 μM, which was about ten-fold better than Allo inhibition, together with suitable low cytotoxicity. In silico molecular properties such as drug-likeness, pharmacokinetics, and toxicity of this promising barbiturate were also analyzed and herein discussed.


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